Journal articles: 'Antifungal agents industry'

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Álvarez, Micaela, Alicia Rodríguez, Elena Bermúdez, Elia Roncero, and María J. Andrade. "Development of a Methodology for Estimating the Ergosterol in Meat Product-Borne Toxigenic Moulds to Evaluate Antifungal Agents." Foods 10, no. 2 (February 17, 2021): 438. http://dx.doi.org/10.3390/foods10020438.

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Antifungal agents are commonly used in the meat industry to prevent the growth of unwanted moulds, such as toxigenic ones, on dry-cured meat products. For enhancing the application of antifungals, their mode of action must be evaluated. Their effect on the mould ergosterol content is one of the most studied ones, since it is the target site of some commercialised antifungals or of those that are in development. The aim of this study was to develop a methodology for determining how the antifungal agents used in the meat industry work. A method for analysing ergosterol was firstly developed using high-performance liquid chromatography with fluorescence detection coupled to a diode array detector (HPLC-FLD/DAD). The chromatographically optimised conditions (gradient and mobile phases) allowed us to reduce the time per analysis with respect to previously published methods up to 22 min. Withing the six checked extraction methods, method 5, showing the best mean recovery values (99.51%), the shortest retention time (15.8 min), and the lowest standard deviation values (9.92) and working temperature (60 °C), was selected. The limit of detection and limit of quantification were 0.03 and 0.1 µg/mL, respectively. All the validation parameters corroborated the method’s suitability. Finally, its feasibility for evaluating the effect of a commercial antifungal preparation (AP) and different herbs that are frequently added to meat products on the ergosterol content of several toxigenic moulds was studied. Differences at the strain level were obtained in the presence of AP. Moreover, the addition of herbs significantly reduced the ergosterol content in Penicillium nordicum up to 83.91%. The developed methodology is thus suitable for screening the antifungals’ role in altering mould ergosterol biosynthesis before their application in real meat products.

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Torrijos, Raquel, Tiago de Melo Nazareth, Juan Manuel Quiles, Jordi Mañes, and Giuseppe Meca. "Application of White Mustard Bran and Flour on Bread as Natural Preservative Agents." Foods 10, no. 2 (February 16, 2021): 431. http://dx.doi.org/10.3390/foods10020431.

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In this study, the antifungal activity of white mustard bran (MB), a by-product of mustard (Sinapis alba) milling, and white mustard seed flour (MF) was tested against mycotoxigenic fungi in the agar diffusion method. The results obtained were posteriorly confirmed in a quantitative test, determining the minimum concentration of extract that inhibits the fungal growth (MIC) and the minimum concentration with fungicidal activity (MFC). Since MF demonstrated no antifungal activity, the MB was stored under different temperature conditions and storage time to determine its antifungal stability. Finally, an in situ assay was carried out, applying the MB as a natural ingredient into the dough to avoid P. commune CECT 20767 growth and increase the bread shelf life. The results demonstrated that the antifungal activity of MB was dose-dependent. The higher assayed dose of MB (10 g/kg) reduced the fungal population in 4.20 Log CFU/g regarding the control group. Moreover, the shelf life was extended four days compared to the control, equaling its effectiveness with the synthetic preservative sodium propionate (E-281). Therefore, MB could be an alternative to chemical additives in bread formulations since it satisfies consumer requirements. Also, the formulation of bread with MB valorizes this by-product generated during mustard seed milling, thereby helping the industry move forward sustainably by reducing environmental impact.

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Muñoz-Tebar, Nuria, Emilio J. González-Navarro, Teresa María López-Díaz, Jesús A. Santos, Gonzalo Ortiz de Elguea-Culebras, M. Mercedes García-Martínez, Ana Molina, Manuel Carmona, and María Isabel Berruga. "Biological Activity of Extracts from Aromatic Plants as Control Agents against Spoilage Molds Isolated from Sheep Cheese." Foods 10, no. 7 (July 7, 2021): 1576. http://dx.doi.org/10.3390/foods10071576.

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The aim of this work was to assess the antifungal and antioxidant activity of essential oils and ethanolic extracts from distilled solid by-products from aromatic plants (Artemisia dracunculus, Hyssopus officinalis, Lavandula stoechas, Origanum vulgare and Satureja montana) against 14 fungi strains isolated from sheep cheese and identified at species level using DNA barcoding based on β-tubulin sequence analysis. In addition, capacity of fungi to produce ochratoxin A, patulin, cyclopiazonic acid and sterigmatocystin was analyzed. Of the isolates, 85.7% belonged to Penicillium (P. commune/biforme, P. crustosum) and 14.3% to Aspergillus (A. puulaauensis and A. jensenii), the first time that these Aspergillus species have been found in sheep’s cheese. All P. commune isolates were producers of cyclopiazonic acid, and the two Aspergillus strains produced sterigmatocystin, but the others did not produce any tested mycotoxin. Among the essential oils tested, oregano, savory and tarragon had a significant antifungal activity against all the isolated strains, but no ethanolic extract showed antifungal activity. By contrast, ethanolic extracts showed great potential as antioxidants. The identification of new molds in cheese will help the dairy industry to know more about those molds affecting the sector, and the use of aromatic plants in the control of fungal spoilage could be a suitable alternative to chemical preservatives used in the agri-food industry.

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Thambidurai, Punitha, Vinodhini Raja, Saranya Ashokapuram Selvam, Moorthy Kannaiyan, and Gnanendra Shanmugam. "Prioritization of Drugs for Fungal Keratitis Eye Infections: An In-Silico Analysis." Applied Sciences 9, no. 12 (June 18, 2019): 2485. http://dx.doi.org/10.3390/app9122485.

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The fungal keratitis (FK) infections that cause cornea inflammations are more virulent than other bacterial keratitis infections and remain one of the most ethereal and challenging infections for ophthalmologists to diagnose and treat. Thus, the urgency in understanding the current perspectives of antifungal agents and their interactions with novel therapeutic targets and the identification of novel anti-fungal agents are at the frontline of studies in the pharmaceutical industry. In this study, DNA dependent RNA polymerase was modelled and virtually screened against eight antifungal agents, and it was found that Itraconazole (−22.0427 kJ/mol), Ketoconazole (−20.2194 kJ/mol), and Voriconazole (−12.6388 kJ/mol) exhibited better binding interactions. further, the structural and electronic properties of Itraconazole calculated through density functional theory studies revealed the sites of chemical reactivity that are vital in the compounds for possible interactions with RNA polymerase (RNAP). Hence, this study explores the binding efficacies of various anti-fungal agents through docking studies and their chemical entities, which might pave a significant path for the design of novel anti-fungal agents against hyalohyphomycetes causing keratitis.

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M.Sunar, N., M. Subramaniam, N. F. Zulkifly, U. K. Parjo, C. M. Er, A. M. Leman, A. Khalid, et al. "Indoor Fungal Growth on Variable Antifungal at Different Wall Finishing on Plasterboard." International Journal of Engineering & Technology 7, no. 3.23 (August 9, 2018): 53. http://dx.doi.org/10.14419/ijet.v7i3.23.17260.

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Various health complaints often been attributed to pollution and the poor quality of the indoor air. If there is good practice in building design, construction, and maintenance, the structures should remain dry. However, when there is moisture damage, the materials may be in contact with water for prolonged times, which inevitably leads to microbial growth or even total deterioration of the building material. Antimicrobial coating is designed to generate a surface that is easy to clean and can also incorporate active agents, commonly called antifungal, that prevent microbial colonization, the subsequent growth and bio-deterioration of the substrate. This paper presents the sustainable treatment for indoor environment quality in buildings by examining the application of potassium sorbate, zinc salicylate, and calcium benzoate that used as food industry preservatives as indoor antimicrobial agents. Four types of wall finishing used on plasterboard substrate: acrylic paint, glycerol based-paint, thin wallpaper, and thick wallpaper. The result indicated that potassium sorbate is the best bio compound to react as antifungal agent to prohibit the growth of indoor fungi. All the antifungal shows difference level of their effectiveness from each other. Only 40% of fungi were able to grow on thin wallpaper by using potassium sorbate as antifungal agent.

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Palou, Lluís, Silvia Valencia-Chamorro, and María Pérez-Gago. "Antifungal Edible Coatings for Fresh Citrus Fruit: A Review." Coatings 5, no. 4 (December 4, 2015): 962–86. http://dx.doi.org/10.3390/coatings5040962.

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According to their origin, major postharvest losses of citrus fruit are caused by weight loss, fungal diseases, physiological disorders, and quarantine pests. Cold storage and postharvest treatments with conventional chemical fungicides, synthetic waxes, or combinations of them are commonly used to minimize postharvest losses. However, the repeated application of these treatments has led to important problems such as health and environmental issues associated with fungicide residues or waxes containing ammoniacal compounds, or the proliferation of resistant pathogenic fungal strains. There is, therefore, an increasing need to find non-polluting alternatives to be used as part of integrated disease management (IDM) programs for preservation of fresh citrus fruit. Among them, the development of novel natural edible films and coatings with antimicrobial properties is a technological challenge for the industry and a very active research field worldwide. Chitosan and other edible coatings formulated by adding antifungal agents to composite emulsions based on polysaccharides or proteins and lipids are reviewed in this article. The most important antifungal ingredients are selected for their ability to control major citrus postharvest diseases like green and blue molds, caused by Penicillium digitatum and Penicillium italicum, respectively, and include low-toxicity or natural chemicals such as food additives, generally recognized as safe (GRAS) compounds, plant extracts, or essential oils, and biological control agents such as some antagonistic strains of yeasts or bacteria.

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Matei, Gabi Mirela, Sorin Matei, Adrian Matei, and Elena Draghici. "Antifungal activity of a biosurfactant-producing lactic acid bacteria strain." EuroBiotech Journal 1, no. 3 (July 20, 2017): 212–16. http://dx.doi.org/10.24190/issn2564-615x/2017/03.02.

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Abstract Lactic acid bacteria are frequently utilized in food industry and they are also recognized as antimicrobial agents due to their capability to produce metabolites such as: organic acids, biosurfactants, bacteriocins, hydrogen peroxide, cyclic dipeptides, exopolysaccharides. The main goal of this paper was to present the results of the research carried out on the strain LCM2 of lactic acid bacteria isolated from brined cucumbers, for production of biosurfactants and to assess its antifungal properties. The emulsification capacity of biosurfactant was measured using kerosene as the hydrophobic substrate. The value of emulsification index E24 was 89.04% showing a high emulsification activity of the biosurfactant. The structural characterization of biosurfactant by TLC revealed its glycolipidic nature. Assay of the ionic charge established the anionic charge of the biosurfactant revealed by the presence of precipitation lines towards the cationic surfactant dodecyl-dimethyl-ammonium chloride. The biosurfactant presented antibiofilm activity with low adherence capacity, structural damages of the hyphal net, conidiophores and delays or lack of sporulation and decreased biomass accumulation in four mycotoxigenic Penicillium and Aspergillus isolates. Results of in vitro assays recommend the biosurfactant produced by the new lactic acid bacteria strain LCM2 for biotechnological purposes, as alternative antifungal agent in food industry.

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Dopazo, Victor, Carlos Luz, Jordi Mañes, Juan Manuel Quiles, Raquel Carbonell, Jorge Calpe, and Giuseppe Meca. "Bio-Preservative Potential of Microorganisms Isolated from Red Grape against Food Contaminant Fungi." Toxins 13, no. 6 (June 10, 2021): 412. http://dx.doi.org/10.3390/toxins13060412.

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Fungal spoilage is one of the main reasons of economic losses in the food industry, especially in the wine sector. Consequently, the search for safer and new preservation techniques has gained importance in recent years. The objective of this study was to investigate the antifungal and anti-mycotoxigenic activity from 28 microorganisms (MO) isolated from red grape. The antifungal activity of a cell free supernatant of fermented medium by the isolated MO (CFS) was tested with the agar diffusion method and the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) assay. Additionally, different antifungal compounds from the CFS were identified and quantified (organic acids, phenolic compounds, and volatile organic compounds). Finally, the most active CFS were tested as red grape bio-preservative agents. Results evidenced that CFS fermented by the strain UTA 6 had the highest antifungal activity, above all isolates, and produced a wide pool of antifungal compounds. The use of UTA 6 CFS as bio-preservative agent showed a reduction of 0.4 and 0.6 log10 spores per gram of fruit in grapes contaminated by A. flavus and B. cinerea, respectively. Moreover, UTA 6 CFS treatment reduced the occurrence of aflatoxin B1 and fumonisin (B2, B3, and B4) production in grapes contaminated by 28–100%.

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Jadhav, P. M. "A review on biological activities of Schiff base ligand and their metal complexes." International Journal of ChemTech Research 13, no. 1 (2020): 217–21. http://dx.doi.org/10.20902/ijctr.2019.130126.

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Schiff bases and their metal complexes are wide range of biological applications and are synthesized from the condensation reaction of amino compounds with carbonyl compounds. Schiff base and their metal complexes have a wide variety of applications in food and dye industry, agrochemical, polymer, catalysis, analytical chemistry, antifertility, antiinflammatory activity, antiradical activity, and biological system as enzymatic agents. Several have reviewed them of their antimicrobial, antibacterial, antifungal, antitumor, and cytotoxic activities. This review summarized the most promising biological activities of Schiff bases and their metal complexes

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Nayarisseri, Anuraj. "Most Promising Compounds for Treating COVID-19 and Recent Trends in Antimicrobial & Antifungal Agents." Current Topics in Medicinal Chemistry 20, no. 24 (November 2, 2020): 2119–25. http://dx.doi.org/10.2174/156802662023201001094634.

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Multidrug resistance in microbes poses a major health crisis and demands for the discovery of novel antimicrobial agents. The recent pandemic of SARS-CoV-2 has raised a public health emergency in almost all the countries of the world. Unlike viruses, a bacterium plays a significant role in various environmental issues such as bioremediation. Furthermore, biosurfactants produced by various bacterial species have an edge over traditionally produced chemical surfactants for its biodegradability, low toxicity and better interfacial activity with various applications in agriculture and industry. This special issue focuses on the global perspective of drug discovery for various antimicrobial, antiviral, and antifungal agents for infectious diseases. The issue also emphasizes the ongoing developments and the role of microbes in environmental remediation. We wish the articles published in this issue will enhance the current understanding in microbiology among the readers, and serve as the "seed of an idea" for drug development for ongoing COVID-19 pandemic.

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Varijakzhan, Disha, Jiun-Yan Loh, Wai-Sum Yap, Khatijah Yusoff, Rabiha Seboussi, Swee-Hua Erin Lim, Kok-Song Lai, and Chou-Min Chong. "Bioactive Compounds from Marine Sponges: Fundamentals and Applications." Marine Drugs 19, no. 5 (April 27, 2021): 246. http://dx.doi.org/10.3390/md19050246.

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Marine sponges are sessile invertebrates that can be found in temperate, polar and tropical regions. They are known to be major contributors of bioactive compounds, which are discovered in and extracted from the marine environment. The compounds extracted from these sponges are known to exhibit various bioactivities, such as antimicrobial, antitumor and general cytotoxicity. For example, various compounds isolated from Theonella swinhoei have showcased various bioactivities, such as those that are antibacterial, antiviral and antifungal. In this review, we discuss bioactive compounds that have been identified from marine sponges that showcase the ability to act as antibacterial, antiviral, anti-malarial and antifungal agents against human pathogens and fish pathogens in the aquaculture industry. Moreover, the application of such compounds as antimicrobial agents in other veterinary commodities, such as poultry, cattle farming and domesticated cats, is discussed, along with a brief discussion regarding the mode of action of these compounds on the targeted sites in various pathogens. The bioactivity of the compounds discussed in this review is focused mainly on compounds that have been identified between 2000 and 2020 and includes the novel compounds discovered from 2018 to 2021.

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Lapinska, Barbara, Aleksandra Szram, Beata Zarzycka, Janina Grzegorczyk, Louis Hardan, Jerzy Sokolowski, and Monika Lukomska-Szymanska. "An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens." Materials 13, no. 19 (October 1, 2020): 4383. http://dx.doi.org/10.3390/ma13194383.

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Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

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Sader, Helio S., Paul R. Rhomberg, Andrew S. Fuhrmeister, Rodrigo E. Mendes, Robert K. Flamm, and Ronald N. Jones. "Antimicrobial Resistance Surveillance and New Drug Development." Open Forum Infectious Diseases 6, Supplement_1 (March 2019): S5—S13. http://dx.doi.org/10.1093/ofid/ofy345.

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Abstract Surveillance represents an important informational tool for planning actions to monitor emerging antimicrobial resistance. Antimicrobial resistance surveillance (ARS) programs may have many different designs and can be grouped in 2 major categories based on their main objectives: (1) public health ARS programs and (2) industry-sponsored/product-oriented ARS programs. In general, public health ARS programs predominantly focus on health care and infection control, whereas industry ARS programs focus on an investigational or recently approved molecule(s). We reviewed the main characteristics of industry ARS programs and how these programs contribute to new drug development. Industry ARS programs are generally performed to comply with requirements from regulatory agencies responsible for commercial approval of antimicrobial agents, such as the US Food and Drug Administration, European Medicines Agency, and others. In contrast to public health ARS programs, which typically collect health care and diverse clinical data, industry ARS programs frequently collect the pathogens and perform the testing in a central laboratory setting. Global ARS programs with centralized testing play an important role in new antibacterial and antifungal drug development by providing information on the emergence and dissemination of resistant organisms, clones, and resistance determinants. Organisms collected by large ARS programs are extremely valuable to evaluate the potential of new agents and to calibrate susceptibility tests once a drug is approved for clinical use. These programs also can provide early evaluations of spectrum of activity and postmarketing trends required by regulatory agencies, and the programs may help drug companies to select appropriate dosing regimens and the appropriate geographic regions in which to perform clinical trials. Furthermore, these surveillance programs provide useful information on the potency and spectrum of new antimicrobial agents against indications and organisms in which clinicians have little or no experience. In summary, large ARS programs, such as the SENTRY Antimicrobial Surveillance Program, contribute key data for new drug development.

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Buzón-Durán, Laura, Jesús Martín-Gil, Eduardo Pérez-Lebeña, David Ruano-Rosa, José L. Revuelta, José Casanova-Gascón, M. Carmen Ramos-Sánchez, and Pablo Martín-Ramos. "Antifungal Agents Based on Chitosan Oligomers, ε-polylysine and Streptomyces spp. Secondary Metabolites against Three Botryosphaeriaceae Species." Antibiotics 8, no. 3 (July 20, 2019): 99. http://dx.doi.org/10.3390/antibiotics8030099.

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Grapevine trunk diseases (GTDs) are a major threat to the wine and grape industry. The aim of the study was to investigate the antifungal activity against Neofusicoccum parvum, Diplodia seriata, and Botryosphaeria dothidea of ε-polylysine, chitosan oligomers, their conjugates, Streptomyces rochei and S. lavendofoliae culture filtrates, and their binary mixtures with chitosan oligomers. In vitro mycelial growth inhibition tests suggest that the efficacy of these treatments, in particular those based on ε-polylysine and ε-polylysine:chitosan oligomers 1:1 w/w conjugate, against the three Botryosphaeriaceae species would be comparable to or higher than that of conventional synthetic fungicides. In the case of ε-polylysine, EC90 values as low as 227, 26.9, and 22.5 µg·mL−1 were obtained for N. parvum, D. seriata, and B. dothidea, respectively. Although the efficacy of the conjugate was slightly lower, with EC90 values of 507.5, 580.2, and 497.4 µg·mL−1, respectively, it may represent a more cost-effective option to the utilization of pure ε-polylysine. The proposed treatments may offer a viable and sustainable alternative for controlling GTDs.

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Shafiq, Nusrat, Uzma Arshad, Gul Zarren, Shagufta Parveen, Irum Javed, and Aisha Ashraf. "A Comprehensive Review: Bio-Potential of Barbituric Acid and its Analogues." Current Organic Chemistry 24, no. 2 (April 15, 2020): 129–61. http://dx.doi.org/10.2174/1385272824666200110094457.

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In our present work, we emphasized on the potential of barbituric acid (1) derivatives as drugs like anti-bacterial, hypnotic, sedative, anti-microbial and antifungal agents. As naturally occurring, barbituric acid (1) is inactive but in the derivative form, it has a large number of medicinal uses and nowadays, it has a great demand in the pharmaceutical industry. Barbituric acid has a wide range of applications in the synthesis of a diverse class of compounds like heterocyclic, carbocyclic, synthetic alkaloids, and due to its broad-spectrum applications, barbituric acid acquired the position of building blocks in synthetic chemistry. Through the history of humanity, a number of bioactive agents have been applied to cure the disease related to hypnotics and sedatives, while the exact efficacy of these agents was found to be limited. Till now, review articles on barbituric acid only express their specific aspect but in present review article, all aspects are discussed in detail to provide a platform to readers and researchers so that they could obtain all information and background knowledge from a single point.

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Dieng, Sidy Mouhamed, Madieye Séne, Ahmedou Bamba Koueimel Fall, Moussa Diop, Papa Mady Sy, Louis Augustin Diaga Diouf, Alphonse Rodrigue Djiboune, et al. "Formulation of shea butter Nanoparticle containing griseofulvin: a combination of antifungal and anti-inflammatory treatments." Journal of Drug Delivery and Therapeutics 11, no. 2-S (April 15, 2021): 59–65. http://dx.doi.org/10.22270/jddt.v11i2-s.4796.

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Nanomedicine has been a booming industry with the development of nanovectors to encapsulate water-soluble or amphiphilic molecules for drug delivery. As the new therapeutic agents synthesized are increasingly lipophilic, the development of new nanoparticulate vectors allowing their transport and targeting is now a major challenge. These particles are lipid nanoparticles, a few hundred nanometers in diameter, stabilized by a layer of surfactants composed of castor oil and stealth agents. Solid lipid nanoparticles based on shea butter, stabilized by cremophor® ELP, encapsulating griseofulvin, were formulated by the temperature phase inversion method. The shea butter nanoparticles thus obtained were the subject of characterization relating to: determination of the morphology, size, polydispersity index, pH and zeta potential. The results confirm the stability of our preparations. The anti-inflammatory activity of shea butter being known, the tests were carried out on mice. The inflammation was induced by a solution of croton oil acetone. There is a very big improvement in anti-inflammatory activity. This is due to better penetration of the preparation through the different layers of the skin. Griseofulvin release studies have been carried out on our various preparations. Systems designed as reservoirs of active ingredients and intended for a priori controlled release obey kinetics of the order of one-half (½) corresponding to a proportionality between the quantity released and the square root of time. Shea butter in nanoparticulate forms has thus enabled us to considerably prolong the release of griseofulvin. Keywords: Nanoparticles; Shea Butter; Inflammation; Griseofulvin.

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Vella, Filomena Monica, Roberto Calandrelli, Domenico Cautela, Immacolata Fiume, Gabriella Pocsfalvi, and Bruna Laratta. "Chemometric Screening of Fourteen Essential Oils for Their Composition and Biological Properties." Molecules 25, no. 21 (November 4, 2020): 5126. http://dx.doi.org/10.3390/molecules25215126.

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Essential oils (EOs) obtained from aromatic plants are widely used worldwide, especially in cosmetic and food products due to their aroma and biological properties and health benefits. Some EOs have significant antimicrobial and antioxidant activities, and thus could effectively increase the shelf lives of foodstuff and beverages. In this study, fourteen essential oils (clove, eucalyptus, fennel, lavender, oregano, palmarosa, pepper, star anise, tea tree, turmeric, Chinese yin yang, Japanese yin yang, and ylang ylang) from different medicinal plant families were screened by gas-chromatography–mass spectrometry (GC–MS) for their different chemical profiles and bioassays were performed to assess their antifungal and antioxidant activities. The results obtained were assessed by principal component analysis (PCA). PCA distinguished six groups characterized by different terpene chemotypes. Amongst the EOs studied, the clove EO showed the strongest antioxidant activity characterized by an EC50 of 0.36 µL/mL. The oregano EO had the greatest antiyeast activity characterized by a minimal inhibitory concentration of 10 µL/mL. In conclusion, clove and oregano EOs are strong antifungal and antioxidant agents, respectively, with great potential in the food industry to avoid spoilage and to increase shelf life.

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HALAMOVA, KATERINA, LADISLAV KOKOSKA, JAROSLAV FLESAR, OLGA SKLENICKOVA, BLANKA SVOBODOVA, and PETR MARSIK. "In Vitro Antifungal Effect of Black Cumin Seed Quinones against Dairy Spoilage Yeasts at Different Acidity Levels." Journal of Food Protection 73, no. 12 (December 1, 2010): 2291–95. http://dx.doi.org/10.4315/0362-028x-73.12.2291.

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The antiyeast activity of the black cumin seed (Nigella sativa) quinones dithymoquinone, thymohydroquinone (THQ), and thymoquinone (TQ) were evaluated in vitro with a broth microdilution method against six dairy spoilage yeast species. Antifungal effects of the quinones were compared with those of preservatives commonly used in milk products (calcium propionate, natamycin, and potassium sorbate) at two pH levels (4.0 and 5.5). THQ and TQ possessed significant antiyeast activity and affected the growth of all strains tested at both pH levels, with MICs ranging from 8 to 128 μg/ml. With the exception of the antibiotic natamycin, the inhibitory effects of all food preservatives against the yeast strains tested in this study were strongly affected by differences in pH, with MICs of ≥16 and ≥512 μg/ml at pH 4.0 and 5.5, respectively. These findings suggest that HQ and TQ are effective antiyeast agents that could be used in the dairy industry as chemical preservatives of natural origin.

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Tumbarski, Yulian, Anna Lante, and Albert Krastanov. "Immobilization of Bacteriocins from Lactic Acid Bacteria and Possibilities for Application in Food Biopreservation." Open Biotechnology Journal 12, no. 1 (March 21, 2018): 25–32. http://dx.doi.org/10.2174/1874070701812010025.

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Bacteriocins are biologically active compounds produced by a large number of bacteria, including lactic acid bacteria (LAB), which exhibit antimicrobial activity against various saprophytic and pathogenic microorganisms. In recent decades, bacteriocins are increasingly becoming more important in different branches of the industry due to their broad antibacterial and antifungal spectrum - in the food industry for natural food preservation and expiry date extension; in the health sector for preparation of probiotic foods and beverages; in the clinical practice as alternatives of conventional antibiotics; in the agriculture as biocontrol agents of plant pathogens and alternatives of chemical pesticides for plant protection. The broad antimicrobial spectrum of bacteriocins has stimulated the research attention on their application mainly in the food industry as natural preservatives. Most scientific achievements concerning the application food biopreservation are related to bacteriocins produced by LAB. The lactic acid bacteria bacteriocins can be produced in the food substrate during its natural fermentation or can be added in the food products after obtaining byin vitrofermentations under optimal physical and chemical conditions. Moreover, the immobilization of LAB bacteriocins on different matrices of organic and inorganic origin has been proposed as an advanced approach in the natural food preservation for their specific antimicrobial activity, anti-biofilm properties and potential use as tools for pathogen detection.

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Upmanyu, Neeraj, Sanjay Kumar, Kamal Shah, and Pradeep Mishra. "Synthesis and Antimicrobial Studies of Some 4-(Substituted)-Ethanoylamino-3-Mercapto-5- (4-Substituted) Phenyl-1,2,4-Triazoles." Dhaka University Journal of Pharmaceutical Sciences 11, no. 1 (November 4, 2012): 7–18. http://dx.doi.org/10.3329/dujps.v11i1.12481.

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Triazoles and triazoles with different substituent groups are found to possess diverse application in the field of medicine and industry. A series of 4-(substituted) ethanoylamino-3-mercapto-5-(4-substituted) phenyl-1,2,4- triazoles were synthesized as novel antimicrobial agents starting from different 4-substituted benzoic acids. The chemical structures of these newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR, FAB+-mass spectral data and elemental analyses. The antimicrobial activity of title compounds were examined against two gram positive bacteria (Staphylococcus aureus, Bacillus subtilis), two gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and three fungi (Candida albicans, Aspergillus niger and Fusarium oxysporum) using disc diffusion method. Some of the compounds bearing methoxy group exhibited moderate to good antibacterial and antifungal activities. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12481 Dhaka Univ. J. Pharm. Sci. 11(1): 7-18, 2012 (June)

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Berber, Didem. "Antibacterial Activities of Lichen Derived Extracts against Different Bacillus Species from Soak Liquor Samples." Journal of the American Leather Chemists Association 115, no. 03 (March 2, 2020): 96–104. http://dx.doi.org/10.34314/jalca.v115i03.1627.

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In the leather industry, some bacterial strains may become resistant to antibacterial agents utilized in the soaking process due to long-term use and/or not using in sufficient doses. Alternative approaches or novel agents need to be investigated to overcome antibacterial resistance of bacteria present in the soaking process. These alternative approaches may be from natural resources such as lichens which are known to have various biological activities such as antibacterial, antifungal etc. For this purpose, soak liquor samples from different tanneries were collected and eight isolates from these samples were identified by cultural and molecular techniques. Also, the antibacterial effects of acetone extracts of Hypogymnia physodes, Evernia divaricata, Pseudevernia furfuracea and Usnea sp. at different concentrations were tested on these isolates. They were all Gram (+), rod shaped, oxidase (+), catalase (+), protease (+). Six isolates had lipase activities. The isolates were assigned to Bacillus toyonensis, B. mojavensis, B. subtilis, B. amyloliquefaciens, B. velezensis, B. cereus, and B. licheniformis in molecular analyses. The acetone extracts of Evernia divaricata totally killed B. toyonensis, B. mojavensis, B. amyloliquefaciens, and B. subtilis at the concentrations of 240, 120, 60 and 30 µg/ml, respectively. These extracts had also significant antibacterial efficacies on B. cereus, B. velezensis, B. licheniformis at the concentration of 240 µg/ml. The acetone extracts of P. furfuracea had a great inhibitory effect on the growth of most species (80.24-88.65%) only at the concentration of 240 µg/ml. H. physodes acetone extracts totally killed B. amyloliquefaciens and had considerably high suppressive effect on the growth of other tested bacteria at the concentrations of 120 and 240 µg/ml. Usnea sp. acetone extracts had inhibitory effect on Bacillus species (86.6-97.9%) even at the 30 µg/ml concentration. In this respect, lichens may provide an alternative approach for the leather industry to overcome bacterial resistance to the antibacterial agents.

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Ravoitytė, Bazilė, Juliana Lukša, Vyacheslav Yurchenko, Saulius Serva, and Elena Servienė. "Saccharomyces paradoxus Transcriptional Alterations in Cells of Distinct Phenotype and Viral dsRNA Content." Microorganisms 8, no. 12 (November 30, 2020): 1902. http://dx.doi.org/10.3390/microorganisms8121902.

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Killer yeasts are attractive antifungal agents with great potential applications in the food industry. Natural Saccharomyces paradoxus isolates provide new dsRNA-based killer systems available for investigation. The presence of viral dsRNA may alter transcriptional profile of S. paradoxus. To test this possibility, a high-throughput RNA sequencing was employed to compare the transcriptomes of S. paradoxus AML 15-66 K66 killer strains after curing them of either M-66 alone or both M-66 and L-A-66 dsRNA viruses. The S. paradoxus cells cured of viral dsRNA(s) showed respiration deficient or altered sporulation patterns. We have identified numerous changes in the transcription profile of genes including those linked to ribosomes and amino acid biosynthesis, as well as mitochondrial function. Our work advance studies of transcriptional adaptations of Saccharomyces spp. induced by changes in phenotype and set of dsRNA viruses, reported for the first time.

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Mahmad, Noraini, R. M. Taha, Rashidi Othman, Sakinah Abdullah, Nordiyanah Anuar, Hashimah Elias, and Norlina Rawi. "Anthocyanin as potential source for antimicrobial activity inClitoria ternateaL. andDioscorea alataL." Pigment & Resin Technology 47, no. 6 (November 5, 2018): 490–95. http://dx.doi.org/10.1108/prt-11-2016-0109.

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PurposeThe purpose of this paper is to validate the antimicrobial activity (both antibacterial and antifungal) ofin vivoandin vitroethanolic anthocyanin extracts ofClitoria ternateaL. (vivid blue flower butterfly-pea) andDioscorea alataL. (purple yam) against selected bacteria (Bacillus subtilis,Staphylococcus aureusandEscherichia coli) and fungi (Fusarium sp.,Aspergillus nigerandTrichoderma sp.).Design/methodology/approachThe freeze-dried samples (0.2 g) fromin vivovivid blue flowers ofC. ternateaL. were extracted using 10 mL ethanol (produced ethanolic red extraction) and 10 mL distilled water (produced aqueous blue extraction) separately. Two-month-oldin vitrocallus samples (0.2 g) were only extracted using 10 mL ethanol. The anthocyanin extractions were separated with the addition (several times) of ethyl acetate and distilled water (1:2:3) to remove stilbenoids, chlorophyll, less polar flavonoids and other non-polar compounds. Furthermore, the antimicrobial properties were determined using agar diffusion technique. Three bacteria (B. subtilis,S. aureusandE. coli) and fungi (F. sp.,A. nigerandT. sp.) were streaked on bacteria agar and dextrose agar, respectively, using “hockey stick”. Then, the sterile paper discs (6 mm diameter) were pipetted with 20 µL of 1,010 CFU/mL chloramphenicol (as control for antibacterial) and carbendazim (as control for antifungal)in vivoandin vitroextracts. The plates were incubated at room temperature for 48 h, and the inhibition zones were measured.FindingsBased on the results, bothin vivoandin vitroethanolic extracts from vivid blue flowers ofC. ternateaL. showed the best antibacterial activity against the same bacteria (B. subtilis), 11 and 10 mm inhibition zones, respectively. However, different antifungal activity was detected inin vitroethanolic callus extract (12 mm), which was againstT. sp., contrary toin vivoethanolic extract (10 mm), which was againstF. sp.; antibacterial activity ofD. alataL. was seen against the same bacteria (E. coli) with the highest inhibition zone forin vivoextract (8.8 mm), followed byin vitroextract (7.8 mm).Research limitations/implicationsAnthocyanins are responsible for the water soluble and vacuolar, pink, red, purple and blue pigments present in coloured plant pigments. These pigments (pink, red, purple and blue) are of important agronomic value in many crops and ornamental plants. However, anthocyanins are not stable and are easy to degrade and fade whenever exposed to light.Social implicationsPlant extracts containing bioactive agents with antimicrobial properties have been found to be useful in treating bacterial and fungal infections, as well as showed multiple antibiotic resistance.Originality/valueBothin vivoandin vitroextracts from vivid blue flower petals (C. ternateaL.) and purple yam (D. alataL.) have important applications as natural antimicrobial (antibacterial and antifungal) agents in the coating industry, instead of natural pharmaceutical products.

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Astray, Gonzalo, Patricia Gullón, Beatriz Gullón, Paulo E. S. Munekata, and José M. Lorenzo. "Humulus lupulus L. as a Natural Source of Functional Biomolecules." Applied Sciences 10, no. 15 (July 23, 2020): 5074. http://dx.doi.org/10.3390/app10155074.

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Hops (Humulus lupulus L.) are used traditionally in the brewing industry to confer bitterness, aroma, and flavor to beer. However, in recent years, it has been reported that female inflorescences contain a huge variety of bioactive compounds. Due to the growing interest of the consumers by natural ingredients, intense research has been carried out in the last years to find new sources of functional molecules. This review collects the works about the bioactive potential of hops with applications in the food, pharmaceutical, or cosmetic industries. Moreover, an overview of the main extraction technologies to recover biomolecules from hops is shown. Bioactivities of hop extracts such as antibacterial, antifungal, cardioprotective, antioxidant, anti-inflammatory, anticarcinogenic, and antiviral are also summarized. It can be concluded that hops present a high potential of bioactive ingredients with high quality that can be used as preservative agents in fresh foods, extending their shelf life, and they can be incorporated in cosmetic formulation for skincare as well.

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Guo, Zhang, Li, Li, Duan, Zhang, Hu, and Huang. "Label-Free Proteomic Analysis of Molecular Effects of 2-Methoxy-1,4-naphthoquinone on Penicillium italicum." International Journal of Molecular Sciences 20, no. 14 (July 14, 2019): 3459. http://dx.doi.org/10.3390/ijms20143459.

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Penicillium italicum is the principal pathogen causing blue mold of citrus. Searching for novel antifungal agents is an important aspect of the post-harvest citrus industry because of the lack of higher effective and low toxic antifungal agents. Herein, the effects of 2-methoxy-1,4-naphthoquinone (MNQ) on P. italicum and its mechanism were carried out by a series of methods. MNQ had a significant anti-P. italicum effect with an MIC value of 5.0 µg/mL. The label-free protein profiling under different MNQ conditions identified a total of 3037 proteins in the control group and the treatment group. Among them, there were 129 differentially expressed proteins (DEPs，up-regulated > 2.0-fold or down-regulated < 0.5-fold, p < 0.05), 19 up-regulated proteins, 26 down-regulated proteins, and 67 proteins that were specific for the treatment group and another 17 proteins that were specific for the control group. Of these, 83 proteins were sub-categorized into 23 hierarchically-structured GO classifications. Most of the identified DEPs were involved in molecular function (47%), meanwhile 27% DEPs were involved in the cellular component and 26% DEPs were involved in the biological process. Twenty-eight proteins identified for differential metabolic pathways by KEGG were sub-categorized into 60 classifications. Functional characterization by GO and KEGG enrichment results suggests that the DEPs are mainly related to energy generation (mitochondrial carrier protein, glycoside hydrolase, acyl-CoA dehydrogenase, and ribulose-phosphate 3-epimerase), NADPH supply (enolase, pyruvate carboxylase), oxidative stress (catalase, glutathione synthetase), and pentose phosphate pathway (ribulose-phosphate 3-epimerase and xylulose 5-phosphate). Three of the down-regulated proteins selected randomly the nitro-reductase family protein, mono-oxygenase, and cytochrome P450 were verified using parallel reaction monitoring. These findings illustrated that MNQ may inhibit P. italicum by disrupting the metabolic processes, especially in energy metabolism and stimulus response that are both critical for the growth of the fungus. In conclusion, based on the molecular mechanisms, MNQ can be developed as a potential anti-fungi agent against P. italicum.

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Vargas-Hernandez, Marcela, Israel Macias-Bobadilla, Ramon Gerardo Guevara-Gonzalez, Enrique Rico-Garcia, Rosalia Virginia Ocampo-Velazquez, Luciano Avila-Juarez, and Irineo Torres-Pacheco. "Nanoparticles as Potential Antivirals in Agriculture." Agriculture 10, no. 10 (September 30, 2020): 444. http://dx.doi.org/10.3390/agriculture10100444.

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Viruses are estimated to be responsible for approximately 50% of the emerging plant diseases, which are difficult to control, and in some cases, there is no cure. It is essential to develop therapy practices to strengthen the management of these diseases caused by viruses in economically important crops. Metal nanoparticles (MeNPs) possess diverse physicochemical properties that allow for them to have a wide range of applications in industry, including nanomedicine and nano-agriculture. Currently, there are reports of favorable effects of the use of nanoparticles, such as antibacterial, antifungal, and antiviral effects, in animals and plants. The potential antiviral property of MeNPs makes them a powerful option for controlling these histological agents. It is crucial to determine the dosage of NPs, the application intervals, their effect as a biostimulant, and the clarification of the mechanisms of action, which are not fully understood. Therefore, this review focuses on discussing the ability of metal nanoparticles and metal oxides to control viruses that affect agriculture through an exhaustive analysis of the characteristics of the particles and their interaction processes for a possibly beneficial effect on plants.

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Modarresi Chahardehi, Amir, Darah Ibrahim, and Shaida Fariza Sulaiman. "Antioxidant, Antimicrobial Activity and Toxicity Test ofPilea microphylla." International Journal of Microbiology 2010 (2010): 1–6. http://dx.doi.org/10.1155/2010/826830.

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A total of 9 plant extracts were tested, using two different kinds of extracting methods to evaluate the antioxidant and antimicrobial activities fromPilea microphylla(Urticaceae family) and including toxicity test. Antioxidant activity were tested by using DPPH free radical scavenging, also total phenolic contents and total flavonoid contents were determined. Toxicity assay carried out by using brine shrimps. Methanol extract of method I (ME I) showed the highest antioxidant activity at69.51±1.03. Chloroform extract of method I (CE I) showed the highest total phenolic contents at72.10±0.71and chloroform extract of method II (CE II) showed the highest total flavonoid contents at60.14±0.33. The antimicrobial activity ofPilea microphyllaextract was tested in vitro by using disc diffusion method and minimum inhibitory concentration (MIC). ThePilea microphyllaextract showed antibacterial activity against some Gram negative and positive bacteria. The extracts did not exhibit antifungal and antiyeast activity. The hexane extract of method I (HE I) was not toxic against brine shrimp (LC50 value was 3880 μg/ml). Therefore, the extracts could be suitable as antimicrobial and antioxidative agents in food industry.

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May, André, Luciana Fontes Coelho, Evandro Henrique Figueiredo Moura da Silva, Ronaldo da Silva Viana, Nilson Aparecido Vieira Junior, and Williams Pinto Marques Ferreira. "Graphene: A new technology for agriculture." Research, Society and Development 10, no. 2 (February 28, 2021): e56610212827. http://dx.doi.org/10.33448/rsd-v10i2.12827.

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This article presents a review on the use of graphene in various segments, elucidating that this product can be used in various industrial sectors. These include mainly agriculture (as in large crops of high relevance, such as coffee), the food industry and the environment, as a plant growth stimulator and in fertilizers, nanoencapsulation and smart-release systems, antifungal and antibacterial agents, smart packaging, water treatment and ultrafiltration, contaminant removal, pesticide and insecticide quantitation, detection systems and precision agriculture. However, some challenges can be overcome before the graphene-based nanoparticle is used on a large scale. In this way, before using the product in the environment, it is necessary to determine whether the technology is safe for the soil-plant system and consumers. Furthermore, the cost of its use can also be a limiting factor depending on the level applied. Therefore, this review proposes to examine the diverse literature to explain the effects of the use of graphene in agriculture, plants and soil microorganisms. Accordingly, this article discusses and presents the possibilities of application of graphene in agriculture, plants and soil microorganisms.

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Matei, Adrian, Sorin Matei, Gabi-Mirela Matei, Gina Cogălniceanu, and Călina Petruța Cornea. "Biosynthesis of silver nanoparticles mediated by culture filtrate of lactic acid bacteria, characterization and antifungal activity." EuroBiotech Journal 4, no. 2 (April 30, 2020): 97–103. http://dx.doi.org/10.2478/ebtj-2020-0011.

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AbstractSilver nanoparticles (AgNPs) are nanomaterials obtained by nanotechnology and due to their antimicrobial properties have a major importance in the control of various species of bacteria, fungi and viruses, with applications in medicine, cosmetics or food industry. The goal of the paper was to present the results of the research carried out on rapid extracellular biosynthesis of silver nanoparticles mediated by culture filtrate of lactic acid bacteria Lactobacillus sp. strain LCM5 and to assess the antimicrobial activity. Analysis of transmission electron microscopy (TEM) micrographs evidenced that the size of AgNPs synthesized using culture filtrates of lactic acid bacteria strain LCM5 ranged between 3 and 35 nm diameter, with an average particle size of 13.84±4.56 nm. AgNPs presented a good dispersion, approximately spherical shape, with parallel stripes certifying crystal structure. Frequency distribution revealed that preponderant dimensions of biosynthesized AgNPs were below 20 nm (94%). Antimicrobial activity of AgNPs was variable depending on both species and group of test microorganisms (bacteria or fungi) involved. Diameter of growth inhibition zone of Aspergillus flavus and Aspergillus ochraceus caused by silver nanoparticles synthesized by lactic acid bacteria strain LCM5 were similar (12.39 ± 0.61mm and 12.86 ± 0.78 mm) but significant stronger inhibition was registered against Penicillium expansum (15.87 ± 1.01mm). The effectiveness of biosynthesized silver nanoparticles was more pronounced against Gram-negative bacteria Chromobacterium violaceum with larger zone of inhibition (18 ± 0.69 mm diameter) when compared to those from fungi. Results recommend the silver nanoparticles biosynthesized using culture filtrate of the lactic acid bacteria Lactobacillus sp. strain LCM5 for biotechnological purposes, as promising antimicrobial agents.

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Monteiro, Mariana, Andreia F. R. Silva, Daniela Resende, Susana S. Braga, Manuel A. Coimbra, Artur M. S. Silva, and Susana M. Cardoso. "Strategies to Broaden the Applications of Olive Biophenols Oleuropein and Hydroxytyrosol in Food Products." Antioxidants 10, no. 3 (March 13, 2021): 444. http://dx.doi.org/10.3390/antiox10030444.

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Oleuropein (OLE) and hydroxytyrosol (HT) are olive-derived phenols recognised as health-promoting agents with antioxidant, anti-inflammatory, cardioprotective, antifungal, antimicrobial, and antitumor activities, providing a wide range of applications as functional food ingredients. HT is Generally Recognised as Safe (GRAS) by the European Food Safety Authority (EFSA) and the Food and Drug Administration (FDA), whereas OLE is included in EFSA daily consumptions recommendations, albeit there is no official GRAS status for its pure form. Their application in food, however, may be hindered by challenges such as degradation caused by processing conditions and undesired sensorial properties (e.g., the astringency of OLE). Among the strategies to overcome such setbacks, the encapsulation in delivery systems and the covalent and non-covalent complexation are highlighted in this review. Additionally, the synthesis of OLE and HT derivatives are studied to improve their applicability. All in all, more research needs however to be carried out to investigate the impact of these approaches on the sensory properties of the final food product and its percussions at the gastrointestinal level, as well as on bioactivity. At last limitations of these approaches at a scale of the food industry must also be considered.

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Motelica, Ludmila, Denisa Ficai, Anton Ficai, Ovidiu Cristian Oprea, Durmuş Alpaslan Kaya, and Ecaterina Andronescu. "Biodegradable Antimicrobial Food Packaging: Trends and Perspectives." Foods 9, no. 10 (October 11, 2020): 1438. http://dx.doi.org/10.3390/foods9101438.

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This review presents a perspective on the research trends and solutions from recent years in the domain of antimicrobial packaging materials. The antibacterial, antifungal, and antioxidant activities can be induced by the main polymer used for packaging or by addition of various components from natural agents (bacteriocins, essential oils, natural extracts, etc.) to synthetic agents, both organic and inorganic (Ag, ZnO, TiO2 nanoparticles, synthetic antibiotics etc.). The general trend for the packaging evolution is from the inert and polluting plastic waste to the antimicrobial active, biodegradable or edible, biopolymer film packaging. Like in many domains this transition is an evolution rather than a revolution, and changes are coming in small steps. Changing the public perception and industry focus on the antimicrobial packaging solutions will enhance the shelf life and provide healthier food, thus diminishing the waste of agricultural resources, but will also reduce the plastic pollution generated by humankind as most new polymers used for packaging are from renewable sources and are biodegradable. Polysaccharides (like chitosan, cellulose and derivatives, starch etc.), lipids and proteins (from vegetal or animal origin), and some other specific biopolymers (like polylactic acid or polyvinyl alcohol) have been used as single component or in blends to obtain antimicrobial packaging materials. Where the package’s antimicrobial and antioxidant activities need a larger spectrum or a boost, certain active substances are embedded, encapsulated, coated, grafted into or onto the polymeric film. This review tries to cover the latest updates on the antimicrobial packaging, edible or not, using as support traditional and new polymers, with emphasis on natural compounds.

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Guzow, Katarzyna, Ewa Mulkiewicz, Michał Obuchowski, and Wiesław Wiczk. "Biological activity of 3-(2-benzoxazol-5-yl)alanine derivatives." Amino Acids 53, no. 8 (July 8, 2021): 1257–68. http://dx.doi.org/10.1007/s00726-021-03030-7.

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AbstractSearching for new drugs is still a challenge for science, mainly because of civilization development and globalization which promote the rapid spread of diseases, which is particularly dangerous in the case of infectious ones. Moreover, readily available already known antibiotics are often overused or misused, possibly contributing to the increase in the number of multidrug-resistant microorganisms. A consequence of this is the need for new structures of potential drugs. One of them is a benzoxazole moiety, a basic skeleton of a group of fluorescent heterocyclic compounds already widely used in chemistry, industry, and medicine, which is also present in naturally occurring biologically active compounds. Moreover, synthetic benzoxazoles are also biologically active. Considering all of that, a large group of non-proteinogenic amino acids based on 3-(2-benzoxazol-5-yl)alanine skeleton was studied in search for new antimicrobial and anticancer agents. Screening tests revealed that antibacterial potential of 41 compounds studied is not very high; however, they are selective acting only against Gram-positive bacteria (B. subtilis). Moreover, almost half of the studied compounds have antifungal properties, also against pathogens (C. albicans). Most of studied compounds are toxic to both normal and cancer cells. However, in a few cases, toxicity to normal cells is much lower than for cancer cells indicating these compounds as future anticancer agents. The research carried out on such a large group of compounds allowed to establish a structure–activity relationship which enables to select candidates for further modifications, necessary to improve their biological activity and obtain a new lead structure with potential for therapeutic use.

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Jasicka-Misiak, Izabela, Jacek Lipok, Izabela A. Świder, and Paweł Kafarski. "Possible Fungistatic Implications of Betulin Presence in Betulaceae Plants and their Hymenochaetaceae Parasitic Fungi." Zeitschrift für Naturforschung C 65, no. 3-4 (April 1, 2010): 201–6. http://dx.doi.org/10.1515/znc-2010-3-406.

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Betulin and its derivatives (especially betulinic acid) are known to possess very interesting prospects for their application in medicine, cosmetics and as bioactive agents in pharmaceutical industry. Usually betulin is obtained by extraction from the outer layer of a birch bark. In this work we describe a simple method of betulin isolation from bark of various species of Betulaceae trees and parasitic Hymenochaetaceae fungi associated with these trees. The composition of the extracts was studied by GC-MS, whereas the structures of the isolated compounds were confirmed by FTIR and 1H NMR. Additionally, the significant fungistatic activity of betulin towards some fi lamentous fungi was determined. This activity was found to be strongly dependent on the formulation of this triterpene. A betulin-trimyristin emulsion, in which nutmeg fat acts as emulsifier and lipophilic carrier, inhibited the fungal growth even in micromolar concentrations - its EC50 values were established in the range of 15 up to 50 μM depending on the sensitivity of the fungal strain. Considering the lack of fungistatic effect of betulin applied alone, the application of ultrasonic emulsification with the natural plant fat trimyristin appeared to be a new method of antifungal bioassay of water-insoluble substances, such as betulin.

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Mustafayeva, Fatima A., and Najaf T. Kakhramanov. "BROMINATION OF AROMATIC AMINES." IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENII KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA 62, no. 4 (April 6, 2019): 47–59. http://dx.doi.org/10.6060/ivkkt.20196204.5673.

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It is known that the antipyrenes, biological active substances (antitumor, antibacterial, antifungal, antiviral), pharmacological preparations on the basis of bromine-containing aromatic compounds are widely used in the industry. Considering this and increased demand for these substances the purpose of this work was to summarize and systematize the accumulated knowledge in this area. The article presents methods and reagent systems used in the bromination of aromatic amines. There have been described the bromination of aromatic amines with hydrogen bromide, sodium bromide, potassium bromide, ammonium bromide, copper (II) bromide, N-bromosuccinimide, N-bromosaccharin, polymer-supported halogenation agents, and difference of these methods from the point of view of the used oxidizer, the medium and the solvent, the catalyst, the regioselectivity, the quantity of bromine atoms in the obtained product. The influence of solvents, catalysts, the nature (electron-donor or electron-acceptor) and position (ortho-, meta-, para-) of the substituents in the aromatic ring, reaction conditions, molar ratio of the reagents, reaction temperature and carrying out time of bromination reaction of aromatic amines has been shown. The bromination reactions courses of aromatic amines in different solvents, in solvent free conditions, in solid states has been described. The bromination of aromatic amines under thermal, microwave, ultraviolet radiation conditions has been studied. In the paper the regioselective monobromination and also obtaining of di-, tri- bromo derivatives of aromatic amines has been shown. Taking into account today's priority to environmentally safe methods of bromination of aromatic amines they have been also mentioned. Given the above, in our opinion, the information presented in this article will help to optimize the production of bromo derivatives of aromatic amines used in industry, technics and technology.

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Cabarkapa, Ivana, Marija Skrinjar, Nevena Nemet, and Ivan Milovanovic. "Effect of Origanum heracleoticum L. essential oil on food-borne Penicillium aurantiogriseum and Penicilium chrysogenum isolates." Zbornik Matice srpske za prirodne nauke, no. 120 (2011): 83–93. http://dx.doi.org/10.2298/zmspn1120083c.

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Molds are ubiquitously distributed in nature and their spores can be found in the atmosphere even at high altitudes. The difficulty of controlling these undesirable molds, as well as the growing interest of the consumers in natural products, have been forcing the industry to find new alternatives for food preservation. The modern trends in nutrition suggest the limitation of synthetic food additives or substitution with natural ones. Aromatic herbs are probably the most important source of natural antimicrobial agents. Origanum heracleoticum L. essential oil has been known as an interesting source of antimicrobial compounds to be applied in food preservation. In the this work, we have investigated the effect of essential oil obtained from O. heracleoticum on growth of six isolates of Penicillium aurantiogriseum and four isolates of Penicillium chrysogenum isolated from meat plant for traditional Petrovacka sausage (Petrovsk? klob?sa) production. The findings reveal that the essential oil of O. heracleoticum provides inhibition of all of fungal isolates tested. O. heracleoticum L. essential oil exhibited higher antifungal activity against the isolates of P. chrysogenum than the isolates of P. aurantiogriseum. O. heracleoticum essential oil showed a MIC value ranging from 25 to 100 ?L/mL. The fungi cultivated in the medium with higher concentration of essential oil showed certain morphological changes. The alterations included lack of sporulation and loss of pigmentation.

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Alomari, Abdulaziz Ali, Abdalfatah Abdalla Fadlelmula, and Hassen Harzali. "Phytochemical Study and Antimicrobial Activity of Two Medicinal Plants from Al-Baha Region." Oriental Journal of Chemistry 35, no. 6 (December 17, 2019): 1782–88. http://dx.doi.org/10.13005/ojc/350622.

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The plant is a huge therapeutic source with enormous applications in curative industry. For new sources of antimicrobial agents, chloroform, ethyl acetate, and n–butanol extracts of two medicinal plants (Dodonaea viscose and Capparis spinosa) were prepared by liquid – liquid extraction. The plants were collected from Shuda mountain / Al-Baha region/ Saudi Arabia and then evaluated systematically. Phytochemical screening tests detect the existence of flavonoids, alkaloids, tannin, terponoids, saponnins and carbohydrates in most of the performed extracts. Antimicrobial activity was assessed against five bacterial and one fungal race. The extracts of the two plants leaves showed wide vision antibacterial activity and significant antifungal activity. The antibacterial activity (zone of inhibition) of Dodonaea viscose species varied from 30 to 18 mm, whereas of Capparis spinosa the range from 20 to 16 mm for ethyl acetate extracts, for n- butanol extracts the inhibition zone differ from 15 – 10 and 16 - 10 mm respectively. These results indicated that antimicrobial activities of plant species differ to a wide range not only between species themselves but also within the tests for antimicrobial evaluation. The current result supports the medicinal use of the leaves of these studied plants which works as an antimicrobial agent. These results compare to other studies carried out for the same plants in different countries in different environments exhibited diverse outcome in chemical constituents in the plant extracts and in their effects on tested types of micro organismswhich may have been due to a number of factors, including geographical location, season and environmental factors, and the method of extraction. This study for the two plant species was first time performed in this area of Saudi Arabia.

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Gupta, Akshi, Ebenezer Jeyakumar, and Rubina Lawrence. "Journey of Limonene as an Antimicrobial Agent." Journal of Pure and Applied Microbiology 15, no. 3 (June 22, 2021): 1094–110. http://dx.doi.org/10.22207/jpam.15.3.01.

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Injudicious consumption of antibiotics in the past few decades has arisen the problem of resistance in pathogenic organisms against most antibiotics and antimicrobial agents. Scenarios of treatment failure are becoming more common in hospitals. This situation demands the frequent need for new antimicrobial compounds which may have other mechanisms of action from those which are in current use. Limonene can be utilized as one of the solutions to the problem of antimicrobial resistance. Limonene is a naturally occurring monoterpene with a lemon-like odor, which mainly present in the peels of citrus plants like lemon, orange, grapefruit, etc. The study aimed to enlighten the antimicrobial properties of limonene as per previous literature. Advantageous contributions have been made by various research groups in the study of the antimicrobial properties of limonene. Previous studies have shown that limonene not only inhibits disease-causing pathogenic microbes, however, it also protects various food products from potential contaminants. This review article contains information about the effectiveness of limonene as an antimicrobial agent. Apart from antimicrobial property, some other uses of limonene are also discussed such as its role as fragrance and flavor additive, as in the formation of nonalcoholic beverages, as solvent and cleaner in the petroleum industry, and as a pesticide. Antibacterial, antifungal, antiviral, and anti-biofilm properties of limonene may help it to be used in the future as a potential antimicrobial agent with minimal adverse effects. Some of the recent studies also showed the action of limonene against COVID-19 (Coronavirus). However, additional studies are requisite to scrutinize the possible mechanism of antimicrobial action of limonene.

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Vallières, Cindy, Cameron Alexander, and Simon V. Avery. "Potentiated inhibition of Trichoderma virens and other environmental fungi by new biocide combinations." Applied Microbiology and Biotechnology 105, no. 7 (March 18, 2021): 2867–75. http://dx.doi.org/10.1007/s00253-021-11211-3.

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Abstract Fungi cause diverse, serious socio-economic problems, including biodeterioration of valuable products and materials that spawns a biocides industry worth ~$11 billion globally. To help combat environmental fungi that commonly colonise material products, this study tested the hypothesis that combination of an approved fungicide with diverse agents approved by the FDA (Food and Drug Administration) could reveal potent combinatorial activities with promise for fungicidal applications. The strategy to use approved compounds lowers potential development risks for any effective combinations. A high-throughput assay of 1280 FDA-approved compounds was conducted to find those that potentiate the effect of iodopropynyl-butyl-carbamate (IPBC) on the growth of Trichoderma virens; IPBC is one of the two most widely used Biocidal Products Regulations–approved fungicides. From this library, 34 compounds in combination with IPBC strongly inhibited fungal growth. Low-cost compounds that gave the most effective growth inhibition were tested against other environmental fungi that are standard biomarkers for resistance of synthetic materials to fungal colonisation. Trifluoperazine (TFZ) in combination with IPBC enhanced growth inhibition of three of the five test fungi. The antifungal hexetidine (HEX) potentiated IPBC action against two of the test organisms. Testable hypotheses on the mechanisms of these combinatorial actions are discussed. Neither IPBC + TFZ nor IPBC + HEX exhibited a combinatorial effect against mammalian cells. These combinations retained strong fungal growth inhibition properties after incorporation to a polymer matrix (alginate) with potential for fungicide delivery. The study reveals the potential of such approved compounds for novel combinatorial applications in the control of fungal environmental opportunists. Key points • Search with an approved fungicide to find new fungicidal synergies in drug libraries. • New combinations inhibit growth of key environmental fungi on different matrices. • The approach enables a more rapid response to demand for new biocides.

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Mishra, Rahul C., Mayurika Goel, Colin J. Barrow, and Sunil K. Deshmukh. "Endophytic Fungi - An Untapped Source of Potential Antioxidants." Current Bioactive Compounds 16, no. 7 (October 28, 2020): 944–64. http://dx.doi.org/10.2174/1573407215666191007113837.

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Background: Antioxidants are the substances that interact inside and outside of a biological system against the damaging effects of highly reactive free radicals produced during metabolism. Among various natural alternative sources of bioactive metabolites, endophytic fungi have emerged as a significant reservoir of potent antioxidant compounds. These scantly explored micro-organisms are prolific producers of novel compounds and have the capability to produce metabolites that are exclusively isolated from Plantae. A wide array of compounds like nucleobases, polyketides, terpenoids, flavonoids, coumarins, xanthones, semiquinones, peptides, and phenolic acids have been identified as natural antioxidants produced by these micro-organisms. Methods: A detailed review of the literature published recently was undertaken using bibliographic database like Sci-finder and Google scholar. Questions to be reviewed and criteria for selection as a part of the study were fixed. The key features like information on the structure of isolated metabolites and antioxidant activities were summarised after a critical examination. A skeleton was established which gives insight into the type of novel chemical moieties which can be explored as a future antioxidant (s). Results: The review substantially covers the recently discovered compounds, in the period 2013 – 2018, having potent antioxidant activity, isolated from endophytic fungi colonizing diverse plant types such as terrestrial plants, mangrove plants and marine algae. Among the 96 compounds discussed here, thirtynine are from the first report of their occurrence. The present study reports 96 compounds obtained from 34 endophytic fungi out of which 15 fungi belonging to 13 genera of Ascomycetes produced 44 compounds, 14 fungi belonging to 5 genera of hyphomycetes yielded 33 compounds and 6 fungi belonging to 2 genera of Coelomycetes yielded 19 compounds. : The antioxidant potency of these compounds against different free radicals is briefly described and some details such as host organisms, plant sources, place of collection and the antioxidant properties of these compounds are tabulated in this review. Conclusion: Some of these free radical scavengers have shown wide applications in the food and pharmaceutical industry as potential food preservatives, nutraceuticals, antibacterial, anticancer and antifungal agents. This review aims at highlighting some of the novel compounds isolated recently from endophytic fungi, and their applications as potential antioxidant candidates.

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Castanheira, Mariana, Cecilia G. Carvalhaes, Mary Motyl, Seongah Han, and Havilland Campbell. "1148. Activity of Posaconazole and Comparator Antifungal agents Tested Against Filamentous Fungi." Open Forum Infectious Diseases 7, Supplement_1 (October 1, 2020): S601. http://dx.doi.org/10.1093/ofid/ofaa439.1334.

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Abstract Background Posaconazole (POS) is a broad-spectrum triazole antifungal that exhibits potent antifungal activity against a variety of yeasts and molds. We evaluated the in vitro activities of posaconazole and comparator antifungal agents against 2,554 isolates of filamentous fungi including 2,100 Aspergillus species and 454 non-Aspergillus moulds (98 Fusarium, 81 Mucorales and 76 Scedosporium species isolates) collected worldwide in 2010-2018 from clinically significant infections. Methods Isolates were identified using sequencing and/or MALDI-TOF MS methods. Posaconazole, itraconazole, voriconazole, caspofungin, anidulafungin, micafungin, and amphotericin B were tested using the reference broth microdilution method according to CLSI guidelines. Results Posaconazole showed comparable activity to itraconazole and voriconazole against A. fumigatus. Categorical agreement between posaconazole and the other azoles tested against A. fumigatus ranged from 98.2-98.7%. Most of the Aspergillus species isolates tested (>90%) were WT to all azoles and echinocandins. Among the isolates of A. fumigatus, the rate of NWT strains varied across the different geographic regions. The frequency of azole NWT strains of A. fumigatus from Europe increased steadily from 2010 to 2018. There was no consistent trend for an increased frequency of NWT strains from other geographic areas. The azoles and echinocandins showed poor activity against Fusarium and Scedosporium species. Posaconazole (MIC50/90, 1/2 mg/L) and amphotericin B (MIC50/90, 1/2 mg/L) were the most active agents against the Mucorales isolates. Conclusion Posaconazole exhibited excellent activity against most species of Aspergillus and was comparable to itraconazole and voriconazole. Most Aspergillus species remain susceptible to triazoles. Although there was no evidence for an increasing frequency of NWT strains among A. fumigatus isolates from North America, Latin America or the Asia-Pacific region, we confirm an increase in the rate of NWT strains to all three triazoles among isolates from Europe. Disclosures Mariana Castanheira, PhD, 1928 Diagnostics (Research Grant or Support)A. Menarini Industrie Farmaceutiche Riunite S.R.L. (Research Grant or Support)Allergan (Research Grant or Support)Allergan (Research Grant or Support)Amplyx Pharmaceuticals (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Fox Chase Chemical Diversity Center (Research Grant or Support)GlaxoSmithKline (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Merck (Research Grant or Support)Merck (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Paratek Pharma, LLC (Research Grant or Support)Pfizer (Research Grant or Support)Qpex Biopharma (Research Grant or Support) Cecilia G. Carvalhaes, MD, PhD, A. Menarini Industrie Farmaceutiche Riunite S.R.L. (Research Grant or Support)Allergan (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Fox Chase Chemical Diversity Center (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Merck (Research Grant or Support)Merck (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Pfizer (Research Grant or Support) Mary Motyl, PhD, Merck & Co, Inc (Employee, Shareholder) Seongah Han, PhD, Merck & Co, Inc. (Employee) Havilland Campbell, BS, Merck & Co, Inc. (Employee)

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Atillasoy, Cem, and Panagiotis Gourlias. "1235. On the Edge of Tomorrow: Expedited Regulatory Pathways for Anti-Infective Therapies." Open Forum Infectious Diseases 7, Supplement_1 (October 1, 2020): S637. http://dx.doi.org/10.1093/ofid/ofaa439.1420.

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Abstract Background The FDA has developed expedited review programs and pathways to increase drug development for products that have a major clinical benefit. These programs include: Fast Track, Orphan Drug Status, Accelerated Approval, Priority Review, Breakthrough Therapy (BTD) and Qualified Infectious Disease Products (QIPD). Given the heightened awareness of infectious diseases--and emerging global threats, such as resistant bacteria and Ebola—academia and industry have developed and received approval for 88 new infectious disease agents. The objective of this study was to assess the use of expedited review pathways for the 88 anti-infective agents that were approved between 2001-2020. FDA Expedited Drug Development Programs Methods We analyzed the FDA Drug Approval Database entitled, “Compilation of CDER New Molecular Entity (NME) Drug and New Biologic Approvals” for anti-infective therapies that were approved after 2000. Anti-infective therapies were defined as agents that were used to treat or prevent infectious diseases and include antibiotics, antivirals and antifungals. Our analysis focused on a comparison of the percentage of approved anti-infective agents that used each of the aforementioned designations across 2 decades (2001-2010 & 2011-2020). A drug may have one, none, or multiple of these designations. Results There were significant differences in the percentage of anti-infective agents approved with priority review, fast track and accelerated approval in 2001-2010 compared to 2011-2020 (See Results Figure 1) BTD and QIDP did not exist until 2012, thus preventing comparisons between decades. QIDP • Between 2012-2020, 16 anti-infectives have been approved with QIDP. From 2017-2020, 40% (n=10) of approved anti-infectives had QIDP. Orphan Drug Status: • Between 2017-2020, 32% of anti-infectives approved have the orphan drug designation. Comparison of FDA Expedited Drug Development Programs use between 2001-2010 and 2011-2020 Conclusion Our findings indicate Priority Review and Fast Track use has increased since 2010 among anti-infective products. Additionally, our analyses indicate that since 2017 there has been increased use of Orphan Drug Status and QIDP. However, there has been limited use of Breakthrough Therapy and Accelerated Approvals. These two pathways should be increasingly considered by academia, industry and the FDA to further expedite innovative anti-infective development. Disclosures All Authors: No reported disclosures

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Huband, Michael D., Michael A. Pfaller, Robert K. Flamm, Shawn A. Messer, Beth A. Schaefer, Paul Bien, and Mariana Castanheira. "1260. Activity of Manogepix (APX001A) against 2,669 Fungal Isolates from the SENTRY Surveillance Program (2018-2019) Stratified by Infection Type." Open Forum Infectious Diseases 7, Supplement_1 (October 1, 2020): S646—S647. http://dx.doi.org/10.1093/ofid/ofaa439.1444.

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Abstract Background Existing antifungal agents are active against many common fungal pathogens; however, breakthrough fungal infections occur and often involve less frequently encountered yeast and mould isolates. These rarer isolates tend to exhibit diminished susceptibility to current agents. Manogepix (MGX, APX001A) is a novel inhibitor of the fungal Gwt1 enzyme. The prodrug (fosmanogepix), is being evaluated in Phase 2 clinical trials for invasive candidiasis/candidemia, Candida auris infections, and invasive aspergillosis. In this study, we evaluated the in vitro activity of MGX and comparators against 2,669 clinical fungal isolates collected worldwide (2018-2019) and stratified by infection type. Methods Fungal isolates were collected from medical centers located in North America (34 sites; 42.3%), Europe (30 sites; 37.9%), Asia-Pacific (11 sites; 12.3%), and Latin America (7 sites; 7.6%). Isolates were collected from bloodstream infections (BSI; 51.7%), pneumonia in hospitalized patients (PIHP; 21.1%), skin and skin structure infections (SSSI; 5.5%), urinary tract infections (UTI; 2.3%), intraabdominal infections (IAI; 1.9%), and other infection types (17.5%). Results MGX demonstrated potent in vitro activity against 1,887 Candida spp. isolates from BSI, PIHP, SSSI, and all infection types (MIC50/90, 0.008/0.03-0.06 mg/L) outperforming all comparator agents (Table). Similarly, MGX was equally active against 578 Aspergillus spp. isolates (MEC50/90, 0.015/0.03 mg/L), regardless of infection type. MGX was active against Cryptococcus neoformans var. grubii isolates from BSI and ALL infection types with MIC50/90 values of 0.5/2 mg/L. Scedosporium spp. isolates from PIHP and all infection types were inhibited by low concentrations of MGX (MEC50/90, 0.03/0.03 mg/L). Table 1 Conclusion MGX demonstrated potent antifungal activity against Candida spp., Aspergillus spp., C. neoformans var. grubii, and non-Aspergillus moulds, including Scedosporium spp. isolates. Notable activity was seen against C. auris, echinocandin-resistant Candida spp., azole-resistant Aspergillus, and Scedosporium spp. isolates. Further clinical development of fosmanogepix in difficult-to-treat resistant fungal infections is warranted. Disclosures Michael A. Pfaller, MD, Amplyx Pharmaceuticals (Research Grant or Support)Basilea Pharmaceutica International, Ltd (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Department of Health and Human Services (Research Grant or Support)Fox Chase Chemical Diversity Center (Research Grant or Support)Paratek Pharma, LLC (Research Grant or Support) Robert K. Flamm, PhD, A. Menarini Industrie Farmaceutiche Riunite S.R.L. (Research Grant or Support)Amplyx Pharmaceuticals (Research Grant or Support)Basilea Pharmaceutica International, Ltd (Research Grant or Support)Department of Health and Human Services (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support) Shawn A. Messer, PhD, Amplyx Pharmaceuticals (Research Grant or Support)Fox Chase Chemical Diversity Center (Research Grant or Support) Beth A. Schaefer, n/a, Amplyx Pharmaceuticals (Research Grant or Support) Paul Bien, MS, Amplyx Pharmaceuticals (Employee) Mariana Castanheira, PhD, 1928 Diagnostics (Research Grant or Support)A. Menarini Industrie Farmaceutiche Riunite S.R.L. (Research Grant or Support)Allergan (Research Grant or Support)Allergan (Research Grant or Support)Amplyx Pharmaceuticals (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Fox Chase Chemical Diversity Center (Research Grant or Support)GlaxoSmithKline (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Merck (Research Grant or Support)Merck (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Paratek Pharma, LLC (Research Grant or Support)Pfizer (Research Grant or Support)Qpex Biopharma (Research Grant or Support)

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Castanheira, Mariana, Leah Woosley, Mary Motyl, Seongah Han, and Havilland Campbell. "1169. In Vitro Activity of Posaconazole versus Voriconazole for the Treatment of Invasive Aspergillosis in Adults Enrolled in a Clinical Trial." Open Forum Infectious Diseases 7, Supplement_1 (October 1, 2020): S609—S610. http://dx.doi.org/10.1093/ofid/ofaa439.1355.

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Abstract Background Invasive aspergillosis (IA) is a life-threatening disease with limited treatment options and is associated with delays in effective treatment and significant early mortality. Posaconazole (POS) is a broad-spectrum triazole antifungal, that exhibits potent activity against yeasts and molds. We evaluated the antifungal susceptibility profiles of isolates collected during a randomized, prospective, phase 3, double-blind, double-dummy study comparing posaconazole with voriconazole (1:1 randomization) given for ≤12 weeks in the primary treatment of IA (ClinicalTrials.gov, NCT01782131; EudraCT, 2011-003938-14) using CLSI and EUCAST reference testing methodologies. Methods More than 90 study sites located in 23 countries enrolled subjects in the clinical trial. A total of 127 isolates were recovered from documented infections during 2013 through 2019. Fungal isolates were identified using molecular methods and antifungal susceptibility testing was performed by reference broth microdilution methods. The following antifungal agents tested were: posaconazole, itraconazole, voriconazole, caspofungin, and amphotericin B Results Of the 127 samples tested, 119 were identified as Aspergillus species. Aspergillus fumigatus (N=76) was the most prevalent species, followed by A. flavus species complex (N=19), A. section Nigri (N=10), A. section Terrei (N=7). Overall, posaconazole (MIC50/MIC 90, 0.5/1 mg/L) displayed similar activity to voriconazole (MIC50/MIC90, 0.5/1 mg/L) and itraconazole (MIC50/MIC90, 1/2 mg/L) against 119 Aspergillus species Isolates, by both, CLSI and EUCAST method. Posaconazole (MIC50/MIC90, 0.5/0.5 mg/L) and voriconazole (MIC50/MIC90, 0.25/0.5 mg/L) inhibited all 76 A. fumigatus isolates at MIC of 1 mg/L. Among 19 A. flavus species complex isolates recovered from this study, posaconazole (MIC50/MIC90, 0.5/1 mg/L), voriconazole (MIC50/MIC90, 1/1 mg/L) and itraconazole (MIC50/MIC90, 0.5/1 mg/L) displayed equivalent activity. Conclusion Posaconazole displayed good activity against all Aspergillus species isolates included in this study. In addition, posaconazole in vitro activity against Aspergillus species was similar to that observed by voriconazole and itraconazole. Disclosures Mariana Castanheira, PhD, 1928 Diagnostics (Research Grant or Support)A. Menarini Industrie Farmaceutiche Riunite S.R.L. (Research Grant or Support)Allergan (Research Grant or Support)Allergan (Research Grant or Support)Amplyx Pharmaceuticals (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cidara Therapeutics (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Cipla Ltd. (Research Grant or Support)Fox Chase Chemical Diversity Center (Research Grant or Support)GlaxoSmithKline (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Melinta Therapeutics, Inc. (Research Grant or Support)Merck (Research Grant or Support)Merck (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Merck & Co, Inc. (Research Grant or Support)Paratek Pharma, LLC (Research Grant or Support)Pfizer (Research Grant or Support)Qpex Biopharma (Research Grant or Support) Leah Woosley, n/a, Merck & Co, Inc. (Research Grant or Support) Mary Motyl, PhD, Merck & Co, Inc (Employee, Shareholder) Seongah Han, PhD, Merck & Co, Inc. (Employee) Havilland Campbell, BS, Merck & Co, Inc. (Employee)

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Yang, Ruopeng, Xiu Chen, Qiang Huang, Chuying Chen, Kannan R. R. Rengasamy, Jinyin Chen, and Chunpeng (Craig) Wan. "Mining RNA-Seq Data to Depict How Penicillium digitatum Shapes Its Transcriptome in Response to Nanoemulsion." Frontiers in Nutrition 8 (September 14, 2021). http://dx.doi.org/10.3389/fnut.2021.724419.

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Penicillium digitatum is the most severe pathogen that infects citrus fruits during storage. It can cause fruit rot and bring significant economic losses. The continuous use of fungicides has resulted in the emergence of drug-resistant strains. Consequently, there is a need to develop naturally and efficiently antifungal fungicides. Natural antimicrobial agents such as clove oil, cinnamon oil, and thyme oil can be extracted from different plant parts. They exhibited broad-spectrum antimicrobial properties and have great potential in the food industry. Here, we exploit a novel cinnamaldehyde (CA), eugenol (EUG), or carvacrol (CAR) combination antifungal therapy and formulate it into nanoemulsion form to overcome lower solubility and instability of essential oil. In this study, the antifungal activity evaluation and transcriptional profile of Penicillium digitatum exposed to compound nanoemulsion were evaluated. Results showed that compound nanoemulsion had a striking inhibitory effect on P. digitatum in a dose-dependent manner. According to RNA-seq analysis, there were 2,169 differentially expressed genes (DEGs) between control and nanoemulsion-treated samples, including 1,028 downregulated and 1,141 upregulated genes. Gene Ontology (GO) analysis indicated that the DEGs were mainly involved in intracellular organelle parts of cell component: cellular respiration, proton transmembrane transport of biological process, and guanyl nucleotide-binding molecular function. KEGG analysis revealed that metabolic pathway, biosynthesis of secondary metabolites, and glyoxylate and dicarboxylate metabolism were the most highly enriched pathways for these DEGs. Taken together, we can conclude the promising antifungal activity of nanoemulsion with multiple action sites against P. digitatum. These outcomes would deepen our knowledge of the inhibitory mechanism from molecular aspects and exploit naturally, efficiently, and harmlessly antifungal agents in the citrus postharvest industry.

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Panwar, Kirti, Pardeep Kumar, Mangesh Pradeep Kulkarni, Rajesh Kumar, and Gurvinder Singh. "NATURAL PRODUCTS: THE LEADING INDUSTRY AS PHARMACEUTICAL DRUGS." PLANT ARCHIVES 21, supplement 1 (December 31, 2020). http://dx.doi.org/10.51470/plantarchives.2021.v21.s1.385.

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This review is being focused on the importance and emergence of natural products in therapeutic field due to their multiple sources and their multiple biological use. The uses of natural products are as old as 40’s and 50’s century. Many natural products are being discussed in this review that focuses on different targets, like anti-bacterial natural products in which different antibacterial agents from natural sources is being discussed with brief discussion on plant Hyssopus caspidatus. Many more activities is being discussed in this review like antifungal, anti-tumor, anti-diabetic, anti-malarial in which their mechanisms and their suitable example is described in this review

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Alghamdi, Saleh B. "MoO₃ Nano-Bricks as Novel Antimicrobial Agents." European Journal of Biology and Biotechnology 1, no. 6 (December 28, 2020). http://dx.doi.org/10.24018/ejbio.2020.1.6.134.

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Multiple drug resistance in microorganisms has impersonated critical vulnerability to existing antibiotics; hence substitutes/or options to encounter resistant pathogenic microbes are desirable. Our focus in this study was the synthesis and characterization of Molybdenum oxide (MoO3) nano-bricks and to explore them in terms of their antimicrobial potential. MoO3 nano-bricks were successfully synthesized by hydrothermal method using (NH4)6Mo7O24⋅4H2O precursor and calcination at 500 °C for 2 h. The synthesized MoO3 nano-bricks determined antibacterial activity against four bacterial isolates and one fungal isolate. The MoO3 bricks were characterized using standard physicochemical characterization viz. XRD, SEM, FTIR, and EDX. In the present investigation, characteristic antibacterial properties of MoO3 nano-bricks against Gram +ve (S. aureus ATCC 29213 and S. epidermidis ATCC 12228) and Gram -ve (E. coli ATCC 35218 and K. pneumoniae ATCC 700603) bacteria is noted. The antifungal activity was tested using C. albicans ATCC 10231 as model organism. Molybdenum oxides generate acidic medium and demonstrated potent antimicrobial action for various pathogenic bacterial strains causing infections. The MoO3 nano-bricks depicted broad spectrum antimicrobial potential which strongly recommends their use as material of choice as potential antimicrobial material to be used in food industry, water purification, textile industry etc.

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HAGGAG, M. W., S. M. ABOU EL ELLA, and H. F. ABOUZIENA. "Phytochemical Analysis, Antifungal, Antimicrobial Activities and Application of Eichhornia crassipes Against Some Plant Pathogens." Planta Daninha 35 (2017). http://dx.doi.org/10.1590/s0100-83582017350100026.

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ABSTRACT Water hyacinth (Eichhornia crassipes) is an oceanic macrophyte and one of the worst sea-going weeds in the world and Egypt. The grouping of substantial metals in water hyacinth was higher in roots than in shoots. Nutrient content e.g. ammonia, nitrate, nitrite and phosphate was higher in the shoots of water hyacinth. Water hyacinth is a wellspring of phytochemicals which have a medicinal function. In this study, the high degree of peroxidation and nonenzymatic antioxidant systems were detected in leaf extracts. The chemical analysis of the leaf extracts was performed using acetone, ethanol, methanol and n-Butyl alcohol. The fractionated extracts showed the presence of some medicine compounds that include phenols, protein, alkaloids, amino acids, carbohydrate, flavonoids, glycosides, tannins, and terpenoids. The fractionated extracts were screened for antimicrobial and antifungal activities. The leaf extracts of E. crassipes exhibited antimicrobial activities against some bacteria: Escherichia coli, Bacillus subtilis, Bacillus cereus, Lactobacillus casei and Pseudomonas aeruginosa, and antifungal activity against six pathogenic fungi i.e. Aspergillus flavus, A. niger, Alternaria alternata, Colletotrichum gloeosporioides, Candida albicans, and Fusarium solani by using the well diffusion method. Streptomycin and Fluconazole were used as a standard as antimicrobial and antifungal agents, respectively. B. subtilis, F. solani, C. gloeosporioides and A. alternata were the most susceptible to plant extracts. The most effective antifungal and antimicrobial agent against some plant pathogens was the n-Butyl alcohol extract. Also, it reduced the production of mycotoxin e.g. Aflatoxin B1 and Ochratoxin A. The application of the formulation of the plant extract of E. crassipes protected wheat plants against net blotch diseases. The results indicated that the leaf extractsof E. crassipes have potential as biofungicides and can be used in the industry.

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Onuoha, Vivian C., Ifeoma B. Enweani, and Ogbonnia Ekuma Okereke. "Susceptibility Pattern of Different Parts of Moringa oleifera against Some Pathogenic Fungi, Isolated from Sputum Samples of HIV Positive Individuals Co-Infected with Pulmonary Tuberculosis." Journal of Advances in Microbiology, August 10, 2020, 56–82. http://dx.doi.org/10.9734/jamb/2020/v20i730265.

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Background: Opportunistic fungal infection in HIV positive individualshas a high risk of morbidity and mortality as it could be a pointer to systemic infection. Moringa oleifera is one of the 14 species of the family Moringaceae with traditional effectiveness in anti–helminthic, analgesic, anti-ulcerative, anti-microbial, etc. Aim: This study was designed to determine the susceptibility pattern of different parts of Moringa oleifera against some pathogenic fungi using dried Morringa oleifera seed, bark, pod, and leaf extracts/fractions as agents. Materials and Methods: A total of 132 subjects (62 males and 70 females) attending outpatient clinics (OPD) at Nnamdi Azikiwe University Teaching Hospital Nnewi, and Holy Rossary Hospital Emekuku Owerri, Nigeria were recruited for this study. The HIV status of the test subjects was confirmed using immuno-chromatographic technique and their sputum screened for Tuberculosis (TB) using Ziehl Nelsen staining technique. The sputum samples were also cultured on Sabouaurd dextrose agar with and without chloramphenicol incubated at 25oC with examination of growth every 3 days for two weeks. Identification of isolates was done using Gram staining methods, chromogenic media and slide culture.700g, 220g, 500g, and 250g each of the different parts of the pulverized Moringa oleifera (seeds, barks, pods, and leaves) were weighed and exctracted using Soxhlet extractor and methanol as solvent. Results: The prevalence of fungi isolates from test subjects shows that Candida albicans has the highest frequency of 25(26.6%), with the least prevalent being Aspergillus flavus and Phialemonium curvatum at 2(2.1%) respectively. There was also a positive significant correlation between TB and fungi infection in HIV-sero positive subjects (P<0.05).The invitro antifungal activity of these Moringa oleifera extracts/fractions against the test isolates showed no antifungal activity except for ethyl acetate fraction which demonstrated the most prominent activity against A. fumigatus with zones of inhibition of 3-10mm diameter with the least activity against C. krusei with zones of inhibition of 3-6mm diameter. However, the antifungal activities of fluconazole which served as a control in the antifungal susceptibility against the test isolates were more effective than the extract/fractions against the test isolates with a minimum inhibition concentration (MIC) of 50-200mg/ml against 25-100mg/ml for ethylacetate fraction. Conclusion: The comparable antifungi effect of ethylacetate fraction of M. oleifera leaf with that of fluconazole, suggests that ethylacetate fraction of M. oleifera leaf could aid the treatment of pathogenic fungi due to its potential applications in Pharmaceutical industry, thereby ameliorating the morbidity and mortality rate of HIV positive co-infected TB subjects.

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VELUCHAMY, CHANDRA, and RADHA PALANISWAMY. "A REVIEW ON MARINE ALGAE AND ITS APPLICATIONS." Asian Journal of Pharmaceutical and Clinical Research, February 28, 2020, 21–27. http://dx.doi.org/10.22159/ajpcr.2020.v13i3.36130.

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The ocean is the major essential source of structurally unique natural products that are mainly present in living organisms. The essential products extracted from marine microbes and marine algae are highly analyzed areas in instinctive product research. Marine algae are the novel food with potential nutritional values used for multiple purposes in industry and medicine. They show pharmacological activities which are helpful for the invention of bioactive compounds. Furthermore, marine algae have shown to provide an abundant source of natural bioactive compounds with antidiabetic, anti-inflammatory, antiviral, antifungal, hypolipidemic, antioxidant, anti-hypercholesterolemia, antibacterial, and antineoplastic properties. They produce new secondary metabolites that possess biological activities and have the potential to be developed as therapeutic agents. Macroalgal lectins, fucoidans, kainoids, and other substances have been routinely used in the research of biomedical and also have biological activities. The potential pharmaceutical, medicinal, and research applications of these compounds are discussed.

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Outterson, Kevin. "The Vanishing Public Domain: Antibiotic Resistance, Pharmaceutical Innovation and Intellectual Property Law." University of Pittsburgh Law Review 67, no. 1 (April 26, 2005). http://dx.doi.org/10.5195/lawreview.2005.70.

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Penicillin and other antibiotics were the original wonder drugs and laid the foundation of the modern pharmaceutical industry. Human health significantly improved with the introduction of antibiotics. By 1967, the U.S. Surgeon General declared victory over infectious diseases in the United States. But pride goes before a fall. The evolutionary pressure of antibiotic use selects for resistant strains. Effective drugs should be used. But when they are used, no matter how carefully, evolutionary pressure for resistance is created. The problem is not limited to antibiotics. Variants of the human immunodeficiency virus (HIV) develop resistance to anti-retroviral drugs. Antifungal agents face similar challenges. Even cancer cells may develop resistance to pharmaceuticals. Tens of thousands of Americans are dying every year from drug-resistant infections. Some pharmaceutical knowledge is therefore exhaustible, and after patent expiration the public domain may receive a drug which is no longer useful. For these drugs, the public domain vanishes.

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Journal articles on the topic 'Antifungal agents industry'

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