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Journal articles on the topic 'QUERCETIN ANALOGUES'

Author: Grafiati

Published: 26 October 2023

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1

Otieno, Filex, and Richard Kagia. "Virtual screening for chemical analogues similar to phytochemicals that inhibit aldose reductase in the development of diabetic microvascular complications." F1000Research 12 (March 21, 2023): 314. http://dx.doi.org/10.12688/f1000research.129663.1.

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Background: The polyol pathway contributes to the development of diabetic complications but can be inhibited by plant phytochemicals. This study aimed at assessing analogs of specific flavonoids that delay onset of microvascular complications with better pharmacokinetic and toxicology profiles. Methods: An in silico study design was employed. The phytochemicals luteolin and quercetin were selected. Analogs were obtained from ZINC database and prepared using Avogadro software. Docking analysis was done using AutoDock Vina embedded in Chimera. Ligand enzyme interaction was carried out using Biov

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2

Pardo, Antonelle, Thomas Josse, Laetitia Mespouille, Bertrand Blankert, Philippe Dubois, and Pierre Duez. "Synthesis of Quercetin-imprinted Polymer Spherical Particles with Improved Ability to Capture Quercetin Analogues." Phytochemical Analysis 28, no. 4 (2017): 289–96. http://dx.doi.org/10.1002/pca.2674.

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Biler, Michal, David Biedermann, Kateřina Valentová, Vladimír Křen, and Martin Kubala. "Quercetin and its analogues: optical and acido–basic properties." Phys. Chem. Chem. Phys. 19, no. 39 (2017): 26870–79. http://dx.doi.org/10.1039/c7cp03845c.

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4

Imai, Kohei, Ikuo Nakanishi, Kei Ohkubo, et al. "Synthesis of methylated quercetin analogues for enhancement of radical-scavenging activity." RSC Advances 7, no. 29 (2017): 17968–79. http://dx.doi.org/10.1039/c7ra02329d.

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5

Duan, Yu, Na Sun, Min Xue, Xiaolan Wang, and Hu Yang. "Synthesis of regioselectively acylated quercetin analogues with improved antiplatelet activity." Molecular Medicine Reports 16, no. 6 (2017): 9735–40. http://dx.doi.org/10.3892/mmr.2017.7781.

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Fernández-Aparicio, Mónica, Marco Masi, Alessio Cimmino, Susana Vilariño, and Antonio Evidente. "Allelopathic Effect of Quercetin, a Flavonoid from Fagopyrum esculentum Roots in the Radicle Growth of Phelipanche ramosa: Quercetin Natural and Semisynthetic Analogues Were Used for a Structure-Activity Relationship Investigation." Plants 10, no. 3 (2021): 543. http://dx.doi.org/10.3390/plants10030543.

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Allelopathic potential of buckwheat roots on the radicle growth of the broomrape weed species Orobanche cumana and Phelipanche ramosa was studied. Buckwheat root exudates induced a significant growth inhibition in P. ramosa radicles but radicles of O. cumana were not affected. Among the metabolites present in the root organic extract we identified the flavonol quercetin and the stilbene p-coumaric acid methyl ester with only quercetin showing inhibitory effect on P. ramosa. The activity of quercetin was compared with other two similar flavanoids, the flavone apigenin and the dihydroflavanol 3-

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Litvin, V. A., and R. A. Njoh. "Quercetin as a precursor in the synthesis of analogues of fulvic acids and their antibacterial properties." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 2 (March 2021): 56–64. http://dx.doi.org/10.32434/0321-4095-2021-135-2-56-64.

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A simple, fast and effective method for producing synthetic substances with properties similar to natural humic substances has been proposed. The synthesis method is based on the oxidation of quercetin by molecular oxygen in an alkaline medium, followed by conversion to the acid form by passing through a cation exchange column. Study of elemental and functional compositions, spectral properties (UV/Vis and IR range) and redox characteristics allowed qualifying the resulting product as a synthetic fulvic acid. The enhanced antibacterial properties of the obtained synthetic product were establis

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Atala, Elias, Jocelyn Fuentes, Maria Jose Wehrhahn, and Hernan Speisky. "Oxidation of Quercetin and Its Structural Analogues Differentially Affects Its Antioxidant Properties." Free Radical Biology and Medicine 100 (November 2016): S93. http://dx.doi.org/10.1016/j.freeradbiomed.2016.10.231.

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9

Nayak, Yogendra, Venkatachalam Hillemane, Vijay Kumar Daroji, B. S. Jayashree, and M. K. Unnikrishnan. "Antidiabetic Activity of Benzopyrone Analogues in Nicotinamide-Streptozotocin Induced Type 2 Diabetes in Rats." Scientific World Journal 2014 (2014): 1–12. http://dx.doi.org/10.1155/2014/854267.

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Benzopyrones are proven antidiabetic drug candidate in diabetic drug discovery. In this view novel synthetic benzopyrone analogues were selected for testing in experimental diabetes. Type 2 diabetes (T2D) was induced in Wistar rats by streptozotocin (60 mg/kg, i.p.) followed by nicotinamide (120 mg/kg i.p.). Rats having fasting blood glucose (FBG) >200 mg/dL, 7 days after T2D-induction, are selected for the study. Test compounds and standard treatment were continued for 15 days. FBG, oral glucose tolerance test (OGTT), and insulin tolerance test (ITT) were determined on 21st day after induc

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10

Primikyri, Alexandra, Eleftheria Hatzimichael, Evdoxia Karali, et al. "Decoding The BH3-Mimetic Pro-Apoptotic Activity Of Quercetin In Jurkat Cells." Blood 122, no. 21 (2013): 1672. http://dx.doi.org/10.1182/blood.v122.21.1672.1672.

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Abstract Deregulation of apoptosis contributes largely to the pathogenesis of lymphoid neoplasms allowing the expansion of cell clones that develop resistance to drug-induced cell death. Therefore, subverting inherent resistance to apoptosis is a very challenging therapeutic issue and developing small molecules that can mimic the BH3 domain of the pro-apoptotic Bcl-2 family proteins appears to offer such potentials. Natural products, a rich source of compounds with BH3 mimetic activity, make a sound basis for such an approach. Quercetin, a natural polyphenol, has drawn much attention because i

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Nör, Carolina, Ana Paula Machado Bernardi, Juliana Schulte Haas, Jan Schripsema, Sandra Beatriz Rech, and Gilsane Lino Von Poser. "Phenolic Constituents of Hypericum Flowers." Natural Product Communications 3, no. 2 (2008): 1934578X0800300. http://dx.doi.org/10.1177/1934578x0800300227.

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Species of Hypericum accumulate phenolic compounds with the phloroglucinol substitution pattern, and there are many reports of such substances isolated from the aerial parts of the plants. In this study, flowers of plants grown in south Brazil were analyzed by means of HPLC, verifying the presence of benzopyrans in H. polyanthemum and dimeric phloroglucinol derivatives in H. caprifoliatum, H. connatum, H. myrianthum and H. polyanthemum. All flowers presented flavonoids, mainly quercetin derivatives, whereas hypericin and analogues were not detected.

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12

Coorssen, J. R. "Phospholipase activation and secretion: evidence that PLA2, PLC, and PLD are not essential to exocytosis." American Journal of Physiology-Cell Physiology 270, no. 4 (1996): C1153—C1163. http://dx.doi.org/10.1152/ajpcell.1996.270.4.c1153.

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Numerous studies have identified phospholipase metabolites as membrane fusogens, and phospholipase D (PLD) (J.R. Coorssen and R.J. Haslam. FEBS Lett. 316: 170-174, 1993), C (PLC), and A2 (PLA2) activities correlate with secretion. Do these enzymes have essential or modulatory roles? This study confirms that secretion does not require Ca2+ or PLC (Coorssen et al. Cell Regul. 1: 1027-1041, 1990). Arachidonic acid (AA), phosphatidic acid (PA) and analogues, exogenous metabolites of PLA2 and PLD, were tested in electropermeabilized human platelets. AA potentiated guanosine 5'-O-(3-thiotriphosphate

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Singh, Salam Pradeep, Rocktotpal Konwarh, Bolin Kumar Konwar, and Niranjan Karak. "Molecular docking studies on analogues of quercetin with d-alanine:d-alanine ligase of Helicobacter pylori." Medicinal Chemistry Research 22, no. 5 (2012): 2139–50. http://dx.doi.org/10.1007/s00044-012-0207-7.

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Tasdemir, Deniz, Marcel Kaiser, Reto Brun, et al. "Antitrypanosomal and Antileishmanial Activities of Flavonoids and Their Analogues: In Vitro, In Vivo, Structure-Activity Relationship, and Quantitative Structure-Activity Relationship Studies." Antimicrobial Agents and Chemotherapy 50, no. 4 (2006): 1352–64. http://dx.doi.org/10.1128/aac.50.4.1352-1364.2006.

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ABSTRACT Trypanosomiasis and leishmaniasis are important parasitic diseases affecting millions of people in Africa, Asia, and South America. In a previous study, we identified several flavonoid glycosides as antiprotozoal principles from a Turkish plant. Here we surveyed a large set of flavonoid aglycones and glycosides, as well as a panel of other related compounds of phenolic and phenylpropanoid nature, for their in vitro activities against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania donovani. The cytotoxicities of more than 100 compounds for mammalian L6 cells were als

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Jahangir, Muhammad, Atta-ur-Rehman, Ibrahim Bayoumi Abdel Farid, Robert Verpoorte, Imran Khan, and Jiangnan Peng. "NMR-Based Metabolomics for Geographical Discrimination of Adhatoda vasica Leaves." Plants 12, no. 3 (2023): 453. http://dx.doi.org/10.3390/plants12030453.

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Adhatoda vasica (L.), Nees is a widespread plant in Asia. It is used in Ayurvedic and Unani medications for the management of various infections and health disorders, especially as a decoction to treat cough, chronic bronchitis, and asthma. Although it has a diverse metabolomic profile, this plant is particularly known for its alkaloids. The present study is the first to report a broad range of present compounds, e.g., α-linolenic acid, acetate, alanine, threonine, valine, glutamate, malate, fumaric acid, sucrose, β-glucose, kaempferol analogues, quercetin analogues, luteolin, flavone glucosid

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Biswas, Subhankar, Neetinkumar D. Reddy, B. S. Jayashree, and C. Mallikarjuna Rao. "Evaluation of Novel 3-Hydroxyflavone Analogues as HDAC Inhibitors against Colorectal Cancer." Advances in Pharmacological Sciences 2018 (December 27, 2018): 1–14. http://dx.doi.org/10.1155/2018/4751806.

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Alteration of epigenetic enzymes is associated with the pathophysiology of colon cancer with an overexpression of histone deacetylase 8 (HDAC8) enzyme in this tissue. Numerous reports suggest that targeting HDAC8 is a viable strategy for developing new anticancer drugs. Flavonols provide a rich source of molecules that are effective against cancer; however, their clinical use is limited. The present study investigated the potential of quercetin and synthetic 3-hydroxyflavone analogues to inhibit HDAC8 enzyme and evaluated their anticancer property. Synthesis of the analogues was carried out, a

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Hossion, Abugafar M. L., Yoshito Zamami, Rafiya K. Kandahary, et al. "Quercetin Diacylglycoside Analogues Showing Dual Inhibition of DNA Gyrase and Topoisomerase IV as Novel Antibacterial Agents." Journal of Medicinal Chemistry 54, no. 11 (2011): 3686–703. http://dx.doi.org/10.1021/jm200010x.

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Cai, Weirong, Yong Chen, Liangliang Xie, Hong Zhang, and Chunyuan Hou. "Characterization and density functional theory study of the antioxidant activity of quercetin and its sugar-containing analogues." European Food Research and Technology 238, no. 1 (2013): 121–28. http://dx.doi.org/10.1007/s00217-013-2091-x.

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Darko, Mitrović. "In silico analysis of molecular descriptors for quercetin analogues: a way to improve blood–brain barrier permeation." Intrinsic Activity 11, Suppl.1 (2023): A2.25. http://dx.doi.org/10.25006/ia.11.s1-a2.25.

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Adamus-Grabicka, Angelika A., Magdalena Markowicz-Piasecka, Marcin Cieślak, et al. "Biological Evaluation of 3-Benzylidenechromanones and Their Spiropyrazolines-Based Analogues." Molecules 25, no. 7 (2020): 1613. http://dx.doi.org/10.3390/molecules25071613.

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A series of 3-benzylidenechrmanones 1, 3, 5, 7, 9 and their spiropyrazoline analogues 2, 4, 6, 8, 10 were synthesized. X-ray analysis confirms that compounds 2 and 8 crystallize in a monoclinic system in P21/n space groups with one and three molecules in each asymmetric unit. The crystal lattice of the analyzed compounds is enhanced by hydrogen bonds. The primary aim of the study was to evaluate the anti-proliferative potential of 3-benzylidenechromanones and their spiropyrazoline analogues towards four cancer cell lines. Our results indicate that parent compounds 1 and 9 with a phenyl ring at

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Kondhare, Dasharath, Sushma Deshmukh, and Harshad Lade. "Curcumin Analogues with Aldose Reductase Inhibitory Activity: Synthesis, Biological Evaluation, and Molecular Docking." Processes 7, no. 7 (2019): 417. http://dx.doi.org/10.3390/pr7070417.

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Curcumin, a constituent of Curcuma longa, has shown numerous biological and pharmacological activities, including antidiabetic effects. Here, a novel series of curcumin analogues were synthesized and evaluated for in vitro inhibition of aldose reductase (AR), the first and rate-limiting enzyme of the polyol pathway, which plays a key role in the onset and progression of diabetic complications. Biological activity studies showed that all the curcuminoids exhibited moderate to good AR inhibitory (ARI) activities compared with that of the quercetin standard. Importantly, compounds 8d, 8h, 9c, 9e,

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De Sousa Lages, Adriana, Valentim Lopes, João Horta, João Espregueira-Mendes, Renato Andrade, and Alexandre Rebelo-Marques. "Therapeutics That Can Potentially Replicate or Augment the Anti-Aging Effects of Physical Exercise." International Journal of Molecular Sciences 23, no. 17 (2022): 9957. http://dx.doi.org/10.3390/ijms23179957.

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Globally, better health care access and social conditions ensured a significant increase in the life expectancy of the population. There is, however, a clear increase in the incidence of age-related diseases which, besides affecting the social and economic sustainability of countries and regions around the globe, leads to a decrease in the individual’s quality of life. There is an urgent need for interventions that can reverse, or at least prevent and delay, the age-associated pathological deterioration. Within this line, this narrative review aims to assess updated evidence that explores the

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Ren, Yulin, Tyler Frank, Gunnar Meyer, et al. "Potential Benefits of Black Chokeberry (Aronia melanocarpa) Fruits and Their Constituents in Improving Human Health." Molecules 27, no. 22 (2022): 7823. http://dx.doi.org/10.3390/molecules27227823.

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Aronia berry (black chokeberry) is a shrub native to North America, of which the fresh fruits are used in the food industry to produce different types of dietary products. The fruits of Aronia melanocarpa (Aronia berries) have been found to show multiple bioactivities potentially beneficial to human health, including antidiabetic, anti-infective, antineoplastic, antiobesity, and antioxidant activities, as well as heart-, liver-, and neuroprotective effects. Thus far, phenolic compounds, such as anthocyanins, cyanidins, phenolic acids, proanthocyanidins, triterpenoids, and their analogues have

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Bouktaib, Mohamed, Stéphane Lebrun, Aziz Atmani, and Christian Rolando. "Hemisynthesis of all the O-monomethylated analogues of quercetin including the major metabolites, through selective protection of phenolic functions." Tetrahedron 58, no. 50 (2002): 10001–9. http://dx.doi.org/10.1016/s0040-4020(02)01306-6.

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D.Bharathi, P. Valentina та N. Ramalakshmi. "MOLECULAR DOCKING OF NOVEL BENZOPYRAN ANALOGUES AND INHIBITION PROPERTIES OF ANTIDIABETIC AGENTS AGAINST α-AMYLASE AND αGLUCOSIDASE". RASAYAN Journal of Chemistry 15, № 04 (2022): 2873–78. http://dx.doi.org/10.31788/rjc.2022.1547075.

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Alpha amylase and alpha-glucosidase inhibitors play a key role in treating diabetes mellitus. Based on this idea the present study aimed in designing different benzopyran analogs and investigate the binding interaction with protein PDB: 1HNY and PDB:5NN3 through molecular docking by autodockpyrx. The results evaluated by docking studies found that different substituted derivatives of 4-Hydroxycoumarine, 3-acetyl 4-hydroxy coumarin, 8 hydroxycoumarine, 7-hydroxycoumarine, 4-hydroxy, 5-methoxycoumarine compounds and compared with standard quercetin which is the target protein. The compound showi

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Burchinsky, S. G., and М. A. Kalinichenko. "Neurogeroprotection in neurological practice: new possibilities." Medicine of Ukraine, no. 2-3(258-259) (June 17, 2022): 25–30. http://dx.doi.org/10.37987/1997-9894.2022.2-3(258-259).264051.

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The article is devoted to the issues of effective pharmacotherapy of neurodegenerative and vascular pathology of the CNS, which is possible due to the adequate impact on the fundamental mechanisms of brain aging. Comprehensive, comprehensive consideration of the mentioned mechanisms allows to reasonably approach the problem of optimization of neuroheroprotection and choice of a specific drug. Today, the most promising neuroheroprotectors are quercetin, L-carnitine and L-arginine. A rational combination of all three mentioned components is a domestic drug - L-ACC, which has no analogues in the

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Bonaldo, Federico, Fulvio Mattivi, Daniele Catorci, Panagiotis Arapitsas, and Graziano Guella. "H/D Exchange Processes in Flavonoids: Kinetics and Mechanistic Investigations." Molecules 26, no. 12 (2021): 3544. http://dx.doi.org/10.3390/molecules26123544.

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Several classes of flavonoids, such as anthocyanins, flavonols, flavanols, and flavones, undergo a slow H/D exchange on aromatic ring A, leading to full deuteration at positions C(6) and C(8). Within the flavanol class, H-C(6) and H-C(8) of catechin and epicatechin are slowly exchanged in D2O to the corresponding deuterated analogues. Even quercetin, a relevant flavonol representative, shows the same behaviour in a D2O/DMSOd6 1:1 solution. Detailed kinetic measurements of these H/D exchange processes are here reported by exploiting the time-dependent changes of their peak areas in the 1H-NMR s

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28

Zhang, Jun-Sheng, Han-Zhuang Weng, Jia-Luo Huang, Gui-Hua Tang, and Sheng Yin. "Anti-inflammatory Ingenane Diterpenoids from the Roots of Euphorbia kansui." Planta Medica 84, no. 18 (2018): 1334–39. http://dx.doi.org/10.1055/a-0646-4306.

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AbstractBioassay-guided fractionation of the ethanolic extract of the roots of Euphorbia kansui led to the isolation of two new ingenane diterpenoids, euphorkans A (1) and B (2), together with 16 known analogues (3 – 18). Their structures were determined by combined spectral and chemical methods. All the isolates were evaluated for their inhibitory effects on lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophage cells. Compounds 1 – 6 and 10 – 13 exhibited pronounced inhibitory activity with IC50 values in the range of 2.78 – 10.6 µM, and were more potent than the positive

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Zou, Xiang-Yue, Ying-Jie He, Yi-Hui Yang, Xin-Pei Yan, Zhang-Bao Li, and Hua Yang. "Systematic Identification of Bioactive Compositions in Leaves of Morus Cultivars Using UHPLC-ESI-QTOF-MS/MS and Comprehensive Screening of High-Quality Resources." Separations 9, no. 3 (2022): 76. http://dx.doi.org/10.3390/separations9030076.

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Morus spp. leaves (MSLs) show various beneficial effects in the treatment of metabolic-related diseases, which have created a growing interest in MSL development as dietary supplements and functional foods. The illustration of chemical compositions and screening of high-quality MSL resources are therefore necessary for further application. This study developed a new UHPLC-ESI-QTOF-MS/MS strategy of in-source collision-induced dissociation (IS-CID) and target collision-cell CID (TCC-CID) to quickly capture analogues with consistent skeleton, and combined global natural product social molecular

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Abdizadeh, Tooba. "Efficacy Evaluation of Quercetin and Its Analogues on the Main Protease Enzyme of the COVID-19 Using Molecular Docking Studies." journal of ilam university of medical sciences 30, no. 4 (2022): 66–85. http://dx.doi.org/10.52547/sjimu.30.4.66.

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Chen, Jih-Jung, Tzong-Huei Lee, and Ming-Jen Cheng. "Secondary Metabolites with Anti-Inflammatory Activities from an Actinobacteria Herbidospora daliensis." Molecules 27, no. 6 (2022): 1887. http://dx.doi.org/10.3390/molecules27061887.

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Bioassay-guided fractionation of extracts derived from solid cultures of a Herbidospora daliensis originating from Taiwan led to the isolation of five new compounds, for which we propose the name herbidosporadalins A–E (1–5), one isolated for the first time, herbidosporadalin F (6), together with two known compounds (7 & 8). Their structures were elucidated by spectroscopic analyses, including 1D- and 2D-NMR experiments with those of known analogues, and on the basis of HR-EI-MS mass spectrometry, their anti-inflammatory activities were also evaluated. Of these isolates, herbidosporadalin

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Thangasamy, Thilakavathy, Sivanandane Sittadjody, Kirsten H. Limesand, and Randy Burd. "Tyrosinase Overexpression Promotes ATM-Dependent p53 Phosphorylation by Quercetin and Sensitizes Melanoma Cells to Dacarbazine." Analytical Cellular Pathology 30, no. 5 (2008): 371–87. http://dx.doi.org/10.1155/2008/764086.

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Dacarbazine (DTIC) has been used for the treatment of melanoma for decades. However, monotherapy with this chemotherapeutic agent results only in moderate response rates. To improve tumor response to DTIC current clinical trials in melanoma focus on combining a novel targeted agent with chemotherapy. Here, we demonstrate that tyrosinase which is commonly overexpressed in melanoma activates the bioflavonoid quercetin (Qct) and promotes an ataxia telangiectasia mutated (ATM)-dependent DNA damage response. This response sensitizes melanoma cells that overexpress tyrosinase to DTIC. In DB-1 melano

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Ganesh, Deepa, Hans-Peter Fuehrer, Peter Starzengrüber, et al. "Antiplasmodial activity of flavonol quercetin and its analogues in Plasmodium falciparum: evidence from clinical isolates in Bangladesh and standardized parasite clones." Parasitology Research 110, no. 6 (2012): 2289–95. http://dx.doi.org/10.1007/s00436-011-2763-z.

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Vlasenko, Ludmila, and Kseniya Atlanderova. "Assessment (in vitro) toxicity of small molecules of plant origin." E3S Web of Conferences 390 (2023): 07022. http://dx.doi.org/10.1051/e3sconf/202339007022.

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Small molecules of plant origin can have different effects on bacterial cells. At present, it is of great interest to determine the toxic effects of such compounds in order to assess the potential of their use in veterinary medicine and medicine. The aim of this work was to evaluate the toxicity of various chemically synthesized small molecules of plant origin using a bacterial luminescent biosensor based on Escherichia coli and a cell culture of the freshwater ciliate Stylonychia mytilus. Cinnamic aldehyde had the greatest toxic effect on the E. coli MG1655 pXen7 lux-biosensor, which was expr

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Moalin, Mohamed, Gino P. F. van Strijdonck, Aalt Bast, and Guido R. M. M. Haenen. "Competition between Ascorbate and Glutathione for the Oxidized Form of Methylated Quercetin Metabolites and Analogues: Tamarixetin, 4′O-Methylquercetin, Has the Lowest Thiol Reactivity." Journal of Agricultural and Food Chemistry 60, no. 36 (2012): 9292–97. http://dx.doi.org/10.1021/jf302068v.

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Hladkykh, Feydor V. "Preventive and therapeutic strategies of pharmaco-correction gastropathy induced by nonsteroidal anti-inflammatory drugs." Reviews on Clinical Pharmacology and Drug Therapy 15, no. 4 (2017): 14–23. http://dx.doi.org/10.17816/rcf15414-23.

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Today the problem of prevention and treatment of gastropathy associated with nonsteroidal anti-inflammatory drugs has not lost its relevance. In order to reduce the ulcerogenicity of non-steroidal anti-inflammatory drugs, it is classically accepted to supplement the therapy scheme with preparations of other pharmacological groups - antacids, alginates, M-cholinoblockers, gastrin receptor antagonists, H2-histamine blockers, proton pump inhibitors, synthetic analogues of prostaglandins or stimulators of their synthesis, reparants, gastroprotectors. Nowadays, it was suggested I was suggested the

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Ayoub, Zeenat, Archana Mehta, and Siddhartha Kumar Mishra. "ETHNOPHARMACOLOGICAL REVIEW OF NATURAL PRODUCTS IN CANCER PREVENTION AND THERAPY." Asian Journal of Pharmaceutical and Clinical Research 11, no. 6 (2018): 32. http://dx.doi.org/10.22159/ajpcr.2018.v11i6.24792.

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The World Health Organization reports that approximately 80% population from developing countries are facing complications from synthetic drugs used in maintaining their primary health-care needs. The chemotherapeutic strategies are very striking and have earned serious concern as potential means of controlling the incidence of this dreadful disease. However, the major problem in cancer is the long lasting toxicity of the well reputable chemical drugs. Since ancient times, medicinal plants have attracted enormous attention, to fight against various diseases with their broad-spectrum biological

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Maya-Meraz, Irma Ofelia, José de Jesús Ornelas-Paz, Jaime David Pérez-Martínez, et al. "Foliar Application of CaCO3-Rich Industrial Residues on ‘Shiraz’ Vines Improves the Composition of Phenolic Compounds in Grapes and Aged Wine." Foods 12, no. 8 (2023): 1566. http://dx.doi.org/10.3390/foods12081566.

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The quality of wine grapes and wine depends on their content of phenolic compounds. Under commercial conditions, the phenolic maturity of grapes is mostly achieved by applying abscisic acid analogues. Some Ca forms represent a cost-effective alternative for these compounds. In this study, ‘Shiraz’ vines (veraison of 90%) were sprayed with CaCO3-rich residues from the cement industry (4.26 g of Ca per L). Fruit from treated and untreated vines was harvested 45 days after CaCO3 spraying and evaluated for quality. The fruit was vinified, and the obtained wines were bottled and stored in darkness

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Torres-Piedra, Mariana, Rolffy Ortiz-Andrade, Rafael Villalobos-Molina та ін. "A comparative study of flavonoid analogues on streptozotocin–nicotinamide induced diabetic rats: Quercetin as a potential antidiabetic agent acting via 11β-Hydroxysteroid dehydrogenase type 1 inhibition". European Journal of Medicinal Chemistry 45, № 6 (2010): 2606–12. http://dx.doi.org/10.1016/j.ejmech.2010.02.049.

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Belchor, Mariana Novo, Caroline Ramos da Cruz Costa, Airam Roggero, et al. "In Silico Evaluation of Quercetin Methylated Derivatives on the Interaction with Secretory Phospholipases A2 from Crotalus durissus terrificus and Bothrops jararacussu." Pharmaceuticals 16, no. 4 (2023): 597. http://dx.doi.org/10.3390/ph16040597.

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Quercetin derivatives have already shown their anti-inflammatory potential, inhibiting essential enzymes involved in this process. Among diverse pro-inflammatory toxins from snake venoms, phospholipase A2 is one of the most abundant in some species, such as Crotalus durissus terrificus and Bothrops jararacussu from the Viperidae family. These enzymes can induce the inflammatory process through hydrolysis at the sn-2 position of glycerophospholipids. Hence, elucidating the main residues involved in the biological effects of these macromolecules can help to identify potential compounds with inhi

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Riendeau, D., J. P. Falgueyret, J. Guay, N. Ueda, and S. Yamamoto. "Pseudoperoxidase activity of 5-lipoxygenase stimulated by potent benzofuranol and N-hydroxyurea inhibitors of the lipoxygenase reaction." Biochemical Journal 274, no. 1 (1991): 287–92. http://dx.doi.org/10.1042/bj2740287.

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The purified 5-lipoxygenase from porcine leukocytes was found to catalyse the degradation of lipid hydroperoxides in the presence of potent inhibitors of the lipoxygenase reaction. Derivatives of diphenyl-N-hydroxyureas, 4-hydroxybenzofurans and 5-hydroxydihydrobenzofurans all stimulated the 5-lipoxygenase-mediated destruction of 13-hydroperoxyoctadecadienoic acid (13-HPOD). The reaction was dependent on inhibitor and hydroperoxide concentrations (1-10 microM) and could not be detected using heat-inactivated enzyme, when ATP and Ca2+ were omitted or when the hydroperoxide was replaced by the c

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Szydłowska, Iwona, Jolanta Nawrocka-Rutkowska, Agnieszka Brodowska, Aleksandra Marciniak, Andrzej Starczewski, and Małgorzata Szczuko. "Dietary Natural Compounds and Vitamins as Potential Cofactors in Uterine Fibroids Growth and Development." Nutrients 14, no. 4 (2022): 734. http://dx.doi.org/10.3390/nu14040734.

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An analysis of the literature generated within the past 20 year-span concerning risks of uterine fibroids (UFs) occurrence and dietary factors was carried out. A link between Vitamin D deficiency and UFs formation is strongly indicated, making it a potent compound in leiomyoma therapy. Analogs of the 25-hydroxyvitamin D3, not susceptible to degradation by tissue 24-hydroxylase, appear to be especially promising and tend to show better therapeutic results. Although research on the role of Vitamin A in the formation of fibroids is contradictory, Vitamin A-enriched diet, as well as synthetic reti

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Kwofie, Samuel K., Kweku S. Enninful, Jaleel A. Yussif, et al. "Molecular Informatics Studies of the Iron-Dependent Regulator (ideR) Reveal Potential Novel Anti-Mycobacterium ulcerans Natural Product-Derived Compounds." Molecules 24, no. 12 (2019): 2299. http://dx.doi.org/10.3390/molecules24122299.

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Buruli ulcer is a neglected tropical disease caused by the bacterium Mycobacterium ulcerans. Its virulence is attributed to the dermo-necrotic polyketide toxin mycolactone, whose synthesis is regressed when its iron acquisition system regulated by the iron-dependent regulator (ideR) is deactivated. Interfering with the activation mechanism of ideR to inhibit the toxin’s synthesis could serve as a possible cure for Buruli ulcer. The three-dimensional structure of the ideR for Mycobacterium ulcerans was generated using homology modeling. A library of 832 African natural products (AfroDB), as wel

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Gejalakshmi, S., and N. Harikrishnan. "Molecular Docking Study of Quercetein Analogues for Treating Tumours." International Journal of PharmTech Research 12, no. 4 (2019): 30–34. http://dx.doi.org/10.20902/ijptr.2019.120405.

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Drug discovery leading to robust and viable lead candidate’s remains a challenging scientific task, which is the transition from a screening hit to a drug candidate, requires expertise and experience. Natural products and their derivatives have been recognized for many years as a source of therapeutic agents and of structural diversity. The present research attempts to describe the utilization of compounds derived from natural resources as drug candidates, with a focus on the success of these resources in the process of finding and discovering new and effective drug compounds, an approach comm

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Gao, Buhong, Yu Sun, Yingchun Miao, Li Xu, and Zhongxia Wang. "Fluorometric detection of pH and quercetin based on nitrogen and phosphorus co-doped highly luminescent graphene-analogous flakes." Analyst 145, no. 1 (2020): 115–21. http://dx.doi.org/10.1039/c9an02077b.

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Habtemariam, Solomon. "α-Glucosidase Inhibitory Activity of Kaempferol-3-O-rutinoside". Natural Product Communications 6, № 2 (2011): 1934578X1100600. http://dx.doi.org/10.1177/1934578x1100600211.

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Quercetin, kaempferol and to a lesser extent rutin have been reported to have antidiabetic activities when assessed by various assay models including in vitro α-glucosidase inhibition studies. A related structural analogue, kaempferol-3- O-rutinoside (KR) however has not yet been studied for such biological effects. It was found that KR is a potent inhibitor of α-glucosidase in vitro with over 8-times more activity than the reference antidiabetic drug, acarbose. Furthermore, KR displayed a synergistic effect with a less potent flavonoid aglycones, kaempferol and quercetin. The structure-activi

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Nawwar, Mahmoud, Nahla Ayoub, Mohamed El-Raey, et al. "Acylated flavonol diglucosides from Ammania auriculata." Zeitschrift für Naturforschung C 70, no. 1-2 (2015): 39–43. http://dx.doi.org/10.1515/znc-2014-4165.

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Abstract Chemical investigation of the extract of the whole Ammania auriculata plant resulted in the identification of 13 polyphenols, including the hitherto unknown flavonoids, kaempferol 3-O-β-(6″-galloylglucopyranoside)-7-O-β-glucopyranoside, and its quercetin analogue. The structures of all isolates were elucidated by conventional methods, spectroscopic analysis, including 1D and 2D NMR, and by HRESI-MS as well.

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Kamal, M. Vedant, G. Aadarsh Anand, and Badal Parekh. "Antimicrobial activity of synthetic quercetin analogue on E. coli and S. aureus." Journal of Pharmacognosy and Phytochemistry 10, no. 5 (2021): 205–8. http://dx.doi.org/10.22271/phyto.2021.v10.i5c.14199.

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Speisky, Hernán, María Fernanda Arias-Santé, and Jocelyn Fuentes. "Oxidation of Quercetin and Kaempferol Markedly Amplifies Their Antioxidant, Cytoprotective, and Anti-Inflammatory Properties." Antioxidants 12, no. 1 (2023): 155. http://dx.doi.org/10.3390/antiox12010155.

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The contention that flavonoids’ oxidation would necessarily lead to a loss of their antioxidant properties was recently challenged by the demonstration that quercetin oxidation leads to the formation of 2-(3,4-dihydroxybenzoyl)-2,4,6-trihydroxy-3(2H)-benzofuranone (Que-BZF), a metabolite whose antioxidant potency was notably higher than that of its precursor. Here, we compared and expanded the former observation to that of the quercetin analogue kaempferol. Oxidation of kaempferol led to the formation of a mixture of metabolites that included the 2-(4-hydroxybenzoyl)-2,4,6-trihydroxy-3(2H)-ben

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Braune, Annett, Michael Gütschow, Wolfram Engst, and Michael Blaut. "Degradation of Quercetin and Luteolin byEubacterium ramulus." Applied and Environmental Microbiology 67, no. 12 (2001): 5558–67. http://dx.doi.org/10.1128/aem.67.12.5558-5567.2001.

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ABSTRACT The degradation of the flavonol quercetin and the flavone luteolin by Eubacterium ramulus, a strict anaerobe of the human intestinal tract, was studied. Resting cells converted these flavonoids to 3,4-dihydroxyphenylacetic acid and 3-(3,4-dihydroxyphenyl)propionic acid, respectively. The conversion of quercetin was accompanied by the transient formation of two intermediates, one of which was identified as taxifolin based on its specific retention time and UV and mass spectra. The structure of the second intermediate, alphitonin, was additionally elucidated by1H and 13C nuclear magneti

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