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Journal articles on the topic 'CURCUMIN DERIVATIVES'

Author: Grafiati

Published: 4 June 2021

Last updated: 12 June 2025

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Taguchi, Hiroyasu, Daijiro Yanagisawa, Shigehiro Morikawa, Koichi Hirao, Nobuaki Shirai, and Ikuo Tooyama. "Synthesis and Tautomerism of Curcumin Derivatives and Related Compounds." Australian Journal of Chemistry 68, no. 2 (2015): 224. http://dx.doi.org/10.1071/ch14464.

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1,7-Bis(4′-hydroxy-3′-trifluoromethoxyphenyl)-1,6-heptadiene-3,5-dione (2a), related to curcumin, and thirteen 4-substituted derivatives were prepared and their keto/enol ratio in DMSO[D6] was determined by 19F NMR because the enolic form of these related curcumins had been shown to bind to amyloid plaques in the Alzheimer brain. The parent compound and the 4-ethoxycarbonyl derivative were almost 100 % in the enolic form that contains a conjugated hepta-1,4,6-trien-3-on-5-ol backbone. Enolisation decreased to varying amounts in the derivatives that had 4-substituted alkyl groups. Attempts to prepare the 4-hydroxypropyl derivative by hydrolysis of O-methoxymethyl 2m or O-tetrahydropyranyloxy 2n protected derivatives led to cyclised products. A related pyrimidine compound 6b that mimicked a fixed enol form was also prepared.

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Akishina, E. A., E. A. Dikusar, S. K. Petkevich, and V. I. Potkin. "Synthesis of isoxazole and isothiazole derivatives of curcumin." Proceedings of the National Academy of Sciences of Belarus, Chemical Series 56, no. 2 (2020): 187–91. http://dx.doi.org/10.29235/1561-8331-2020-56-2-187-191.

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Curcumin is a chemical compound with antioxidant properties as well as strong anti-inflammatory, antiviral, analgesic, antimicrobial and antitumor effect, contained in the tuberous rhizomes of the turmeric plant (Curcuma longa). Curcumin derivatives are being intensively studied as potential drugs – antitumor drugs for the treatment of certain forms of cancer. The presence of reactive functional groups makes curcumin a convenient starting compound for the further chemical modification. The esters of curcumin and 5-phenylisoxazole-3-carboxylic acid, 5-(p-tolyl)isoxazole-3-carboxylic acid, 4,5- dichloroisothiazole-3-carboxylic acid and adduct of 5-(p-tolyl)isoxazol-3-carbaldehyde with curcumin were synthesized. Esters were obtained by acylation of curcumin with heterocycle-containing carboxylic acid chloride in diethyl ether in the presence of triethylamine. The IR and NMR spectra of the obtained compounds are described.

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Malik, Neelam, Priyanka Dhiman, and Anurag Khatkar. "In SilicoDesign and Synthesis of Targeted Curcumin Derivatives as Xanthine Oxidase Inhibitors." Current Drug Targets 20, no. 5 (2019): 593–603. http://dx.doi.org/10.2174/1389450120666181122100511.

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Background: Curcumin is a well-known pharmacophore and some of its derivatives are shown to target xanthine oxidase (XO) to alleviate disorders caused by the excess production of uric acid. Objective: Curcumin based derivatives were designed, synthesized and evaluated for their antioxidant and xanthine oxidase inhibitory potential. Method: In this report, we designed and synthesized two series of curcumin derivatives modified by inserting pyrazole and pyrimidine ring to central keto group. The synthesized compounds were evaluated for their antioxidant and xanthine oxidase inhibitory potential. Results: Results showed that pyrazole analogues of curcumin produced excellent XO inhibitory potency with the IC50 values varying from 06.255 &#181;M to 10.503 &#181;M. Among pyrimidine derivatives compound CU3a1 having ortho nitro substitution exhibited more potent xanthine oxidase inhibitory activity than any other curcumin derivative of this series. Conclusion: Curcumin derivatives CU5b1, CU5b2, CU5b3, and CU3a1 showed a potent inhibitory activity against xanthine oxidase along with good antioxidant potential.

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Mbese, Zintle, Vuyolwethu Khwaza, and Blessing Atim Aderibigbe. "Curcumin and Its Derivatives as Potential Therapeutic Agents in Prostate, Colon and Breast Cancers." Molecules 24, no. 23 (2019): 4386. http://dx.doi.org/10.3390/molecules24234386.

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Cancer is a life-threatening disease and is the second leading cause of death around the world. The increasing threats of drug-resistant cancers indicate that there is an urgent need for the improvement or development of more effective anticancer agents. Curcumin, a phenolic compound originally derived from turmeric plant (Curcuma longa L. (Zingiberaceae family)) widely known as a spice and a coloring agent for food have been reported to possess notable anticancer activity by inhibiting the proliferation and metastasis, and enhancing cell cycle arrest or apoptosis in various cancer cells. In spite of all these benefits, the therapeutic application of curcumin in clinical medicine and its bioavailability are still limited due to its poor absorption and rapid metabolism. Structural modification of curcumin through the synthesis of curcumin-based derivatives is a potential approach to overcome the above limitations. Curcumin derivatives can overcome the disadvantages of curcumin while enhancing the overall efficacy and hindering drug resistance. This article reports a review of published curcumin derivatives and their enhanced anticancer activities.

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Barua, Nilakshi, and Alak Kumar Buragohain. "Therapeutic Potential of Curcumin as an Antimycobacterial Agent." Biomolecules 11, no. 9 (2021): 1278. http://dx.doi.org/10.3390/biom11091278.

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Curcumin is the principal curcuminoid obtained from the plant Curcuma longa and has been extensively studied for its biological and chemical properties. Curcumin displays a vast range of pharmacological properties, including antimicrobial, anti-inflammatory, antioxidant, and antitumor activity. Specifically, curcumin has been linked to the improvement of the outcome of tuberculosis. There are many reviews on the pharmacological effects of curcumin; however, reviews of the antitubercular activity are comparatively scarcer. In this review, we attempt to discuss the different aspects of the research on the antitubercular activity of curcumin. These include antimycobacterial activity, modulation of the host immune response, and enhancement of BCG vaccine efficacy. Recent advances in the antimycobacterial activity of curcumin synthetic derivatives, the role of computer aided drug design in identifying curcumin targets, the hepatoprotective role of curcumin, and the dosage and toxicology of curcumin will be discussed. While growing evidence supports the use of curcumin and its derivatives for tuberculosis therapy, further preclinical and clinical investigations are of pivotal importance before recommending the use of curcumin formulations in public health.

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Cheng, Yatian, Jian Zhang, Yan Shao, et al. "Enzyme-Catalyzed Glycosylation of Curcumin and Its Analogues by Glycosyltransferases from Bacillus subtilis ATCC 6633." Catalysts 9, no. 9 (2019): 734. http://dx.doi.org/10.3390/catal9090734.

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Curcumin is a naturally occurring polyphenolic compound that is commonly used in both medicine and food additives, but its low aqueous solubility and poor bioavailability hinder further clinical applications. For assessing the effect of the glycosylation of curcumin on its aqueous solubility, two glycosyltransferase genes (BsGT1 and BsGT2) were cloned from the genome of the strain Bacillus subtilis ATCC 6633 and over-expressed in Escherichia coli. Then, the two glycosyltransferases were purified, and their glycosylation capacity toward curcumin and its two analogues was verified. The results showed that both BsGT1 and BsGT2 could convert curcumin and its two analogues into their glucosidic derivatives. Then, the structures of the derivatives were characterized as curcumin 4′-O-β-D-glucoside and two new curcumin analogue monoglucosides namely, curcumoid-O-α-D-glucoside (2a) and 3-pentadienone-O-α-D-glucoside (3a) by nuclear magnetic resonance (NMR) spectroscopy. Subsequently, the dissolvability of curcumin 4′-O-β-D-glucoside was measured to be 18.78 mg/L, while its aglycone could not be determined. Furthermore, the optimal catalyzing conditions and kinetic parameters of BsGT1 and BsGT2 toward curcumin were determined, which showed that the Kcat value of BsGT1 was about 2.6-fold higher than that of BsGT2, indicating that curcumin is more favored for BsGT2. Our findings effectively apply the enzymatic approach to obtain glucoside derivatives with enhanced solubility.

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Effendi, Nurmaya. "Radiolabeled curcumin as β amyloid imaging and tumor targeting imaging agents". Jurnal Fitofarmaka Indonesia 8, № 3 (2021): 5–11. http://dx.doi.org/10.33096/jffi.v8i3.708.

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Curcumin, a polyphenolic compound, derived from the rhizomes of Curcuma longa L. Curcumin shows potential pharmacological action against numerous disorders, including cancer, neurodegenerative, and infection diseases. Curcumin-based molecular imaging agents could be useful for early detection of Alzheimer Disease and tumor and monitor the progress of therapy. Radiolabeled curcumin and its derivatives become promising compounds as imaging agents. In this review, radiolabeled curcumin bearing radionuclides including fluorine-18, Technetium-99m, Iodine-125, and Gallium-68 are reviewed as an effort to develop curcumin-based probes not only for β amyloid imaging but also for tumor imaging.

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Mague, Joel T., William L. Alworth, and Florastina L. Payton. "Curcumin and derivatives." Acta Crystallographica Section C Crystal Structure Communications 60, no. 8 (2004): o608—o610. http://dx.doi.org/10.1107/s0108270104015434.

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Obregón-Mendoza, Marco A., Imilla I. Arias-Olguín, M. Mirian Estévez-Carmona, et al. "Non-Cytotoxic Dibenzyl and Difluoroborate Curcuminoid Fluorophores Allow Visualization of Nucleus or Cytoplasm in Bioimaging." Molecules 25, no. 14 (2020): 3205. http://dx.doi.org/10.3390/molecules25143205.

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Curcumin, the most important secondary metabolite isolated from Curcuma longa, is known for its numerous purported therapeutic properties and as a natural dye. Herein, based on curcumin’s intrinsic fluorescence, a search for improved curcumin-based fluorophores was conducted. Within the set of semi-synthetic curcumin derivatives i.e. mono (1), di (2), tri (3), tetra (4) benzylated and dibenzyl-fluoroborate (5), the fluorescence properties of 2 and 5 in solution outstood with a two-fold quantum yield compared to curcumin. Furthermore, all benzylated derivatives showed a favorable minimal cytotoxic activity upon screening at 25 μM against human cancer and non-tumoral COS-7 cell lines, with a reduction of its cytotoxic effect related to the degree of substitution. Fluorophores 2 and 5 are versatile bioimaging tools, as revealed by Confocal Fluorescence Microscopy (CFM), and showed permeation of living cell membranes of astrocytes and astrocytomas. When 2 is excited with a 405- (blue) or 543-nm (green) laser, it is possible to exclusively and intensively visualize the nucleus. However, the fluorescence emission fades as the laser wavelength moves towards the red region. In comparison, 5 allows selective visualization of cytoplasm when a 560-nm laser is used, showing emission in the NIR region, while it is possible to exclusively observe the nucleus at the blue region with a 405-nm laser.

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Jacob, James N., Dinesh K. Badyal, Suman Bala, and Masoud Toloue. "Evaluation of the in vivo Anti-inflammatory and Analgesic and in vitro Anti-cancer Activities of Curcumin and its Derivatives." Natural Product Communications 8, no. 3 (2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800321.

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Curcumin, obtained from turmeric, has several biological properties to make it a desirable template for drug development. A lipophilic derivative of curcumin, diacetyl curcumin (DAC) and a hydrophilic derivative, diglutaryl curcumin (DGC) were synthesized and their in vivo analgesic and anti-inflammatory activities were compared with those of curcumin and aspirin. The in vitro anti-cancer activities of curcumin and the two derivatives against three cell cancer lines were compared with those against a non-cancerous cell line. The inhibitory effects were comparable to each other and nearing that of curcumin while they showed low inhibitory effect towards the non-cancerous cell line. The mouse tail flick assay showed that curcumin, DAC and DGC increased latency time. DGC was most effective as an analgesic, even more so than aspirin. The maximum percentage effect (MPE) was highest with DGC at 3 hours. The carrageenan induced paw edema model indicated anti-inflammatory activity of all three curcumin formulations. The percentage inhibition of paw edema was maximum for DAC, followed by aspirin and curcumin.

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Chainoglou, Eirini, and Dimitra Hadjipavlou-Litina. "Curcumin in Health and Diseases: Alzheimer’s Disease and Curcumin Analogues, Derivatives, and Hybrids." International Journal of Molecular Sciences 21, no. 6 (2020): 1975. http://dx.doi.org/10.3390/ijms21061975.

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Worldwide, Alzheimer’s disease (AD) is the most common neurodegenerative multifactorial disease influencing the elderly population. Nowadays, several medications, among them curcumin, are used in the treatment of AD. Curcumin, which is the principal component of Curcuma longa, has shown favorable effects forsignificantly preventing or treating AD. During the last decade, the scientific community has focused their research on the optimization of therapeutic properties and on the improvement of pharmacokinetic properties of curcumin. This review summarizes bibliographical data from 2009 to 2019 on curcumin analogues, derivatives, and hybrids, as well as their therapeutic, preventic, and diagnostic applications in AD. Recent advances in the field have revealed that the phenolic hydroxyl group could contribute to the anti-amyloidogenic activity. Phenyl methoxy groups seem to contribute to the suppression of amyloid-β peptide (Aβ42) and to the suppression of amyloid precursor protein (APP) andhydrophobic interactions have also revealed a growing role. Furthermore, flexible moieties, at the linker, are crucial for the inhibition of Aβ aggregation. The inhibitory activity of derivatives is increased with the expansion of the aromatic rings. The promising role of curcumin-based compounds in diagnostic imaging is highlighted. The keto-enol tautomerism seems to be a novel modification for the design of amyloid-binding agents. Molecular docking results, (Q)SAR, as well as in vitro and in vivo tests highlight the structures and chemical moieties that are correlated with specific activity. As a result, the knowledge gained from the existing research should lead to the design and synthesis ofinnovative and multitargetedcurcumin analogues, derivatives, or curcumin hybrids, which would be very useful drug and tools in medicine for both diagnosis and treatment of AD.

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Tomeh, Mhd, Roja Hadianamrei, and Xiubo Zhao. "A Review of Curcumin and Its Derivatives as Anticancer Agents." International Journal of Molecular Sciences 20, no. 5 (2019): 1033. http://dx.doi.org/10.3390/ijms20051033.

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Cancer is the second leading cause of death in the world and one of the major public health problems. Despite the great advances in cancer therapy, the incidence and mortality rates of cancer remain high. Therefore, the quest for more efficient and less toxic cancer treatment strategies is still at the forefront of current research. Curcumin, the active ingredient of the Curcuma longa plant, has received great attention over the past two decades as an antioxidant, anti-inflammatory, and anticancer agent. In this review, a summary of the medicinal chemistry and pharmacology of curcumin and its derivatives in regard to anticancer activity, their main mechanisms of action, and cellular targets has been provided based on the literature data from the experimental and clinical evaluation of curcumin in cancer cell lines, animal models, and human subjects. In addition, the recent advances in the drug delivery systems for curcumin delivery to cancer cells have been highlighted.

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Zorofchian Moghadamtousi, Soheil, Habsah Abdul Kadir, Pouya Hassandarvish, Hassan Tajik, Sazaly Abubakar, and Keivan Zandi. "A Review on Antibacterial, Antiviral, and Antifungal Activity of Curcumin." BioMed Research International 2014 (2014): 1–12. http://dx.doi.org/10.1155/2014/186864.

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Curcuma longaL. (Zingiberaceae family) and its polyphenolic compound curcumin have been subjected to a variety of antimicrobial investigations due to extensive traditional uses and low side effects. Antimicrobial activities for curcumin and rhizome extract ofC. longaagainst different bacteria, viruses, fungi, and parasites have been reported. The promising results for antimicrobial activity of curcumin made it a good candidate to enhance the inhibitory effect of existing antimicrobial agents through synergism. Indeed, different investigations have been done to increase the antimicrobial activity of curcumin, including synthesis of different chemical derivatives to increase its water solubility as well ass cell up take of curcumin. This review aims to summarize previous antimicrobial studies of curcumin towards its application in the future studies as a natural antimicrobial agent.

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Sanghvi, Heli, and Satyendra Mishra. "Structure-Activity Relationship and Antimicrobial Evaluation of N-Phenylpyrazole Curcumin Derivatives." Current Bioactive Compounds 16, no. 4 (2020): 481–88. http://dx.doi.org/10.2174/1573407215666190124115010.

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Background: Curcumin, one of the most important pharmacologically significant natural products, has gained significant consideration among scientists for decades since its multipharmacological activities. 1, 3-Dicarbonyl moiety of curcumin was found to be accountable for the rapid degradation of curcumin molecule. The aim of present work is to replace 1, 3-dicarbonyl moiety of curcumin by pyrazole and phenylpyrazole derivatives with a view to improving its stability and to investigate the role of substitution in N-phenylpyrazole curcumin on its antibacterial activity against both Gram-positive as well as Gram-negative bacteria. Methods: Pyrazole derivatives of curcumin were prepared by heating curcumin with phenyhydrazine/ substituted phenyhydrazine derivatives in AcOH. The residue was purified by silica gel column chromatography. Structures of purified compounds were confirmed by 1H NMR and Mass spectroscopy. The synthesized compounds were evaluated for their antibacterial activity by the microdilution broth susceptibility test method against gram positive (S. aureus) and gram negative (E. coli). Results: Effects of substitution in N-phenylpyrazole curcumin derivatives against S. aureus and E. coli were studied. The most active N-(3-Nitrophenylpyrazole) curcumin (12) exhibits twenty-fold more potency against S. aureus (MIC: 10μg/mL)) and N-(2-Fluoroophenylpyrazole) curcumin (5) fivefold more potency against E. coli (MIC; 50 μg/mL) than N-phenylpyrazole curcumin (4). Whereas, a remarkable decline in anti-bacterial activity against S. aureus and E. coli was observed when electron donating groups were incorporated in N-phenylpyrazole curcumin (4). Comparative studies of synthesized compounds suggest the effects of electron withdrawing and electron donating groups on unsubstituted phenylpyrazole curcumin (4). Conclusion: The structure-activity relationship (SAR) results indicated that the electron withdrawing and electron donating at N-phenylpyrazole curcumin played key roles for their bacterial inhibitory effects. The results of the antibacterial evaluation showed that the synthesized pyrazole derivatives of curcumin displayed moderate to very high activity in S. aureus. In conclusion, the series of novel curcumin derivatives were designed, synthesized and tested for their antibacterial activities against S. aureus and E. coli. Among them, N-(3-Nitrophenylpyrazole curcumin; 12) was most active against S. aureus (Gram-positive) and N-(2-Fluoroophenylpyrazole) curcumin (5) against E. coli (Gram-negative) bacteria.

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Zam, Wissam. "Gut Microbiota as a Prospective Therapeutic Target for Curcumin: A Review of Mutual Influence." Journal of Nutrition and Metabolism 2018 (December 16, 2018): 1–11. http://dx.doi.org/10.1155/2018/1367984.

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Background. Turmeric is a spice that has recently received much interest and has been widely used in Ayurvedic medicine. Turmeric products are diarylheptanoids and have been characterized as safe. They are termed as curcuminoids that consists essentially of three major compounds: curcumin, demethoxycurcumin, and bisdemethoxycurcumin. Curcumin is a lipophilic polyphenol that has poor systemic bioavailability and suffers from biotransformation by human intestinal microflora to yield different metabolites that are easily conjugated to glucuronides and sulfate O-conjugated derivatives. Recently, an increasing number of studies have indicated that dysbiosis is linked with many metabolic diseases, though gut microbiota could be a novel potential therapeutic target. Scope and Approach. Thus, it is suspected that curcumin and its derivatives exert direct regulative effects on the gut microbiota which could explain the paradox between curcumin’s poor systemic bioavailability and its widely reported pharmacological activities. Key Findings and Conclusions. This article summarizes a range of studies that highlight the interaction between curcumin and gut microbiota and considers opportunities for microbiome-targeting therapies using turmeric extract.

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Roman, Barbara, Monika Retajczyk, Łukasz Sałaciński, and Robert Pełech. "Curcumin - Properties, Applications and Modification of Structure." Mini-Reviews in Organic Chemistry 17, no. 5 (2020): 486–95. http://dx.doi.org/10.2174/1570193x16666190621110247.

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In recent years, the interest in biologically active compounds of natural origin has increased significantly. Researchers' research focuses on increasing the activity of curcumin by forming complexes with metals such as vanadium, iron, copper or gallium. Introduction of metal compounds to curcumin increases the scope of application in pharmacology. The main direction of research development is the treatment of tumors, among others stomach cancer or leukemia. Curcuminoids are the main components of turmeric (Curcuma longa L.), a plant from India and South-East Asia. Due to its intense yellow-orange color and pleasant aroma, the powdered rootstalk is widely used in the food industry, as natural dye and spice. The chemical compound responsible for the characteristic color of rhizomes of curcuma is 1,6-heptadien-3,5-dione-1,7-bis(4-hydroxy-3-methoxyphenyl) - (1E, 6E) called curcumin. This work aims to characterize curcumin in terms of its structure, therapeutic properties and also as a substrate for the synthesis of valuable derivatives like tetrahydrocurcumin. Knowledge about this relationship based on literature analysis will enable a better understanding of the factors responsible for its biological activity.

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Zandi, Keivan, Elissa Ramedani, Khosro Mohammadi, et al. "Evaluation of Antiviral Activities of Curcumin Derivatives against HSV-1 in Vero Cell Line." Natural Product Communications 5, no. 12 (2010): 1934578X1000501. http://dx.doi.org/10.1177/1934578x1000501220.

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Antiviral drug resistance is one of the most common problems in medicine, and, therefore, finding new antiviral agents, especially from natural resources, seems to be necessary. This study was designed to assay the antiviral activity of curcumin and its new derivatives like gallium-curcumin and Cu-curcumin on replication of HSV-1 in cell culture. The research was performed as an in vitro study in which the antiviral activity of different concentrations of three substances including curcumin, Gallium-curcumin and Cu-curcumin were tested on HSV-1. The cytotoxicity of the tested compounds was also evaluated on the Vero cell line. The CC50 values for curcumin, gallium-curcumin and Cu-curcumin were 484.2 μg/mL, 255.8 μg/mL and 326.6 μg/mL, respectively, and the respective IC50 values 33.0 μg/mL, 13.9 μg/mL and 23.1 μg/mL. The calculated SI values were 14.6, 18.4 and 14.1, respectively. The results showed that curcumin and its new derivatives have remarkable antiviral effects on HSV-1 in cell culture.

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Kostrzewa, Tomasz, Karol Wołosewicz, Marek Jamrozik, et al. "Curcumin and Its New Derivatives: Correlation between Cytotoxicity against Breast Cancer Cell Lines, Degradation of PTP1B Phosphatase and ROS Generation." International Journal of Molecular Sciences 22, no. 19 (2021): 10368. http://dx.doi.org/10.3390/ijms221910368.

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Breast cancer is the most common cancer of women—it affects more than 2 million women worldwide. PTP1B phosphatase can be one of the possible targets for new drugs in breast cancer therapy. In this paper, we present new curcumin derivatives featuring a 4-piperidone ring as PTP1B inhibitors and ROS inducers. We performed cytotoxicity analysis for twelve curcumin derivatives against breast cancer MCF-7 and MDA-MB-231 cell lines and the human keratinocyte HaCaT cell line. Furthermore, because curcumin is a known antioxidant, we assessed antioxidant effects in its derivatives. For the most potent cytotoxic compounds, we determined intracellular ROS and PTP1B phosphatase levels. Moreover, for curcumin and its derivatives, we performed real-time microscopy to observe the photosensitizing effect. Finally, computational analysis was performed for the curcumin derivatives with an inhibitory effect against PTP1B phosphatase to assess the potential binding mode of new inhibitors within the allosteric site of the enzyme. We observed that two tested compounds are better anticancer agents than curcumin. Moreover, we suggest that blocking the -OH group in phenolic compounds causes an increase in the cytotoxicity effect, even at a low concentration. Furthermore, due to this modification, a higher level of ROS is induced, which correlates with a lower level of PTP1B.

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Nakamae, Ikuko, Tsumoru Morimoto, Hiroki Shima, et al. "Curcumin Derivatives Verify the Essentiality of ROS Upregulation in Tumor Suppression." Molecules 24, no. 22 (2019): 4067. http://dx.doi.org/10.3390/molecules24224067.

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Background: Curcumin has been shown to exert pleiotropic biological effects, including anti-tumorigenic activity. We previously showed that curcumin controls reactive oxygen species (ROS) levels through the ROS metabolic enzymes, to prevent tumor cell growth. In this study, we synthesized 39 novel curcumin derivatives and examined their anti-proliferative and anti-tumorigenic properties. Methods and Results: Thirty-nine derivatives exhibited anti-proliferative activity toward human cancer cell lines, including CML-derived K562 leukemic cells, in a manner sensitive to an antioxidant, N-acetyl-cysteine (NAC). Some compounds exhibited lower GI50 values than curcumin, some efficiently induced cell senescence, and others markedly increased ROS levels, efficiently induced cell death and suppressed tumor formation in a xenograft mouse model, without any detectable side effects. A clustering analysis of the selected compounds and their measurement variables revealed that anti-tumorigenic activity was most well-correlated with an increase in ROS levels. Pulldown assays and a molecular docking analysis showed that curcumin derivatives competed with co-enzymes to bind to the respective ROS metabolic enzymes and inhibited their enzymatic activities. Conclusions: The analysis of novel curcumin derivatives established the importance of ROS upregulation in suppression of tumorigenesis, and these compounds are potentially useful for the development of an anti-cancer drug with few side effects.

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Bonaccorsi, Paola Maria, Manuela Labbozzetta, Anna Barattucci, Tania Maria Grazia Salerno, Paola Poma, and Monica Notarbartolo. "Synthesis of Curcumin Derivatives and Analysis of Their Antitumor Effects in Triple Negative Breast Cancer (TNBC) Cell Lines." Pharmaceuticals 12, no. 4 (2019): 161. http://dx.doi.org/10.3390/ph12040161.

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We analyzed antitumor effects of a series of curcumin analogues. Some of them were obtained by reaction of substitution involving the two phenolic OH groups of curcumin while the analogues with a substituent at C-4 was prepared following an original procedure that regards the condensation of benzenesulfenic acid onto the nucleophilic central carbon of the curcumin skeleton. We analyzed cytotoxic effects of such derivatives on two TNBC (triple negative breast cancer) cell lines, SUM 149 and MDA-MB-231, but only three of them showed an IC50 in a lower micromolar range with respect to curcumin. We also focused on these three derivatives that in both cell lines exhibited a higher or at least equivalent pro-apoptotic effect than curcumin. The analysis of molecular mechanisms of action of the curcumin derivatives under study has highlighted that they decreased NF-κB transcriptional factor activity, and consequently the expression of some NF-κB targets. Our data confirmed once again that curcumin may represent a very good lead compound to design analogues with higher antitumor capacities and able to overcome drug resistance with respect to conventional ones, even in tumors difficult to treat as TNBC.

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Matiadis, Dimitris, Panagiota G. V. Liggri, Eftichia Kritsi, et al. "Curcumin Derivatives as Potential Mosquito Larvicidal Agents against Two Mosquito Vectors, Culex pipiens and Aedes albopictus." International Journal of Molecular Sciences 22, no. 16 (2021): 8915. http://dx.doi.org/10.3390/ijms22168915.

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Vector-borne diseases have appeared or re-emerged in many Southern Europe countries making the transmission of infectious diseases by mosquitoes (vectors) one of the greatest worldwide health threats. Larvicides have been used extensively for the control of Aedes (Stegomyia) albopictus (Skuse, 1895) (Diptera: Culicidae) and Culex pipiens Linnaeus, 1758 (Diptera: Culicidae) mosquitoes in urban and semi-urban environments, causing the increasing resistance of mosquitoes to commercial insecticides. In this study, 27 curcuminoids and monocarbonyl curcumin derivatives were synthesised and evaluated as potential larvicidal agents against Cx. pipiens and Ae. albopictus. Most of the compounds were more effective against larvae of both mosquito species. Four of the tested compounds, curcumin, demethoxycurcumin, curcumin-BF2 complex and a monocarbonyl tetramethoxy curcumin derivative exhibited high activity against both species. In Cx. pipiens the recorded LC50 values were 6.0, 9.4, 5.0 and 32.5 ppm, respectively, whereas in Ae. albopictus they exhibited LC50 values of 9.2, 36.0, 5.5 and 23.6 ppm, respectively. No conclusive structure activity relationship was evident from the results and the variety of descriptors values generated in silico provided some insight to this end.

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Urano, Yasuomi, Mina Takahachi, Ryo Higashiura, et al. "Curcumin Derivative GT863 Inhibits Amyloid-Beta Production via Inhibition of Protein N-Glycosylation." Cells 9, no. 2 (2020): 349. http://dx.doi.org/10.3390/cells9020349.

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Amyloid-β (Aβ) peptides play a crucial role in the pathogenesis of Alzheimer’s disease (AD). Aβ production, aggregation, and clearance are thought to be important therapeutic targets for AD. Curcumin has been known to have an anti-amyloidogenic effect on AD. In the present study, we performed screening analysis using a curcumin derivative library with the aim of finding derivatives effective in suppressing Aβ production with improved bioavailability of curcumin using CHO cells that stably express human amyloid-β precursor protein and using human neuroblastoma SH-SY5Y cells. We found that the curcumin derivative GT863/PE859, which has been shown to have an inhibitory effect on Aβ and tau aggregation in vivo, was more effective than curcumin itself in reducing Aβ secretion. We further found that GT863 inhibited neither β- nor γ-secretase activity, but did suppress γ-secretase-mediated cleavage in a substrate-dependent manner. We further found that GT863 suppressed N-linked glycosylation, including that of the γ-secretase subunit nicastrin. We also found that mannosidase inhibitors that block the mannose trimming step of N-glycosylation suppressed Aβ production in a similar fashion, as was observed as a result of treatment with GT863. Collectively, these results suggest that GT863 downregulates N-glycosylation, resulting in suppression of Aβ production without affecting secretase activity.

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Dutta, Sabari, Anupa Murugkar, Nitasha Gandhe, and Subhash Padhye. "Enhanced Antioxidant Activities of Metal Conjugates of Curcumin Derivatives." Metal-Based Drugs 8, no. 4 (2001): 183–88. http://dx.doi.org/10.1155/mbd.2001.183.

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Antioxidant properties of three Curcumin derivatives in which the 1,3-diketone system is appended with nitrogen and sulfur donors and their copper conjugates are examined for the first time. Metal conjugation seems to offer distinct advantages in radical scavenging activities of curcumin compounds.

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Wu, Zheng, Xiao-bu Lan, and Wei-zhe Jiang. "3D-QSAR research of curcumin derivatives." Medicinal Chemistry Research 24, no. 9 (2015): 3460–66. http://dx.doi.org/10.1007/s00044-015-1406-9.

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Ligeret, Heidi, Sophie Barthelemy, Roland Zini, Jean-Paul Tillement, Serge Labidalle, and Didier Morin. "Effects of curcumin and curcumin derivatives on mitochondrial permeability transition pore." Free Radical Biology and Medicine 36, no. 7 (2004): 919–29. http://dx.doi.org/10.1016/j.freeradbiomed.2003.12.018.

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Song, Hwan-Jun, Jeong-Hwa Lee, and Moo-Ryong Huh. "Isolation and Structural Identification of Curcumin Derivatives form of Curcuma longa." Journal of Agriculture & Life Science 49, no. 5 (2015): 79–88. http://dx.doi.org/10.14397/jals.2015.49.5.79.

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Slika, Layal, and Digambara Patra. "Traditional Uses, Therapeutic Effects and Recent Advances of Curcumin: A Mini-Review." Mini-Reviews in Medicinal Chemistry 20, no. 12 (2020): 1072–82. http://dx.doi.org/10.2174/1389557520666200414161316.

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Studies regarding the uses and biological benefits curcumin have long been paid worldwide attention. Curcumin is a polyphenol found in the turmeric spice, which is derived from the rhizomes of Curcuma longa. Curcumin is a major constituent of the traditional Indian holistic system, Ayurveda, and it is well-known in treating diverse ailments. The aim of this study is to conduct an overview that introduces the traditional uses and therapeutic effects of this valuable phytochemical with more focus on the antitumor results. This review was conducted based on published articles on PubMed, Medline, and Web of Science databases. In this study, the search strategy identified 103 references. Curcumin is found to possess many functions in recent years. It is commonly used for its antioxidant, antimicrobial, anti-inflammatory, antitumor, anti-diabetic, hypolipidemic, hepatoprotective, and neuroprotective effects. Curcumin has been greatly reported to prevent many diseases through modulating several signaling pathways, and the molecular bases of its anti-tumor bioactivities are imputed to the antiproliferative, anti-inflammatory, pro-apoptotic, anti-angiogenesis and anti-metastasis effects. The antitoxic potential of curcumin against various toxin like Aflatoxin B1 is reported. Although curcumin is a safe and promising phytochemical, it suffers from bioavailability problems that limit its therapeutic efficacy. Thus, various promising strategies allowed for the achievement of multiple and effective varieties of curcumin formulations, such as adjuvants, nanoparticles, liposome, micelle and phospholipid complexes, metal complexes, derivatives, and analogues. In conclusion, curcumin is widely used for myriad therapeutic purposes that trigger its significant value. This short review aims to highlight the known biological activities of curcumin and provide evidence for its antitumor effects.

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Shabbir, Umair, Momna Rubab, Akanksha Tyagi, and Deog-Hwan Oh. "Curcumin and Its Derivatives as Theranostic Agents in Alzheimer’s Disease: The Implication of Nanotechnology." International Journal of Molecular Sciences 22, no. 1 (2020): 196. http://dx.doi.org/10.3390/ijms22010196.

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Curcumin is a polyphenolic natural compound with diverse and attractive biological properties, which may prevent or ameliorate pathological processes underlying age-related cognitive decline, Alzheimer’s disease (AD), dementia, or mode disorders. AD is a chronic neurodegenerative disorder that is known as one of the rapidly growing diseases, especially in the elderly population. Moreover, being the eminent cause of dementia, posing problems for families, societies as well a severe burden on the economy. There are no effective drugs to cure AD. Although curcumin and its derivatives have shown properties that can be considered useful in inhibiting the hallmarks of AD, however, they have low bioavailability. Furthermore, to combat diagnostic and therapeutic limitations, various nanoformulations have also been recognized as theranostic agents that can also enhance the pharmacokinetic properties of curcumin and other bioactive compounds. Nanocarriers have shown beneficial properties to deliver curcumin and other nutritional compounds against the blood-brain barrier to efficiently distribute them in the brain. This review spotlights the role and effectiveness of curcumin and its derivatives in AD. Besides, the gut metabolism of curcumin and the effects of nanoparticles and their possible activity as diagnostic and therapeutic agents in AD also discussed.

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Mari, Matteo, Debora Carrozza, Erika Ferrari, and Mattia Asti. "Applications of Radiolabelled Curcumin and Its Derivatives in Medicinal Chemistry." International Journal of Molecular Sciences 22, no. 14 (2021): 7410. http://dx.doi.org/10.3390/ijms22147410.

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Curcumin is a natural occurring molecule that has aroused much interest among researchers over the years due to its pleiotropic set of biological properties. In the nuclear medicine field, radiolabelled curcumin and curcumin derivatives have been studied as potential radiotracers for the early diagnosis of Alzheimer’s disease and cancer. In the present review, the synthetic pathways, labelling methods and the preclinical investigations involving these radioactive compounds are treated. The studies entailed chemical modifications for enhancing curcumin stability, as well as its functionalisation for the labelling with several radiohalogens or metal radionuclides (fluorine-18, technetium-99m, gallium-68, etc.). Although some drawbacks have yet to be addressed, and none of the radiolabelled curcuminoids have so far achieved clinical application, the studies performed hitherto provide useful insights and lay the foundation for further developments.

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Jennings, Morgan R., and Robin J. Parks. "Curcumin as an Antiviral Agent." Viruses 12, no. 11 (2020): 1242. http://dx.doi.org/10.3390/v12111242.

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Curcumin, the primary curcuminoid compound found in turmeric spice, has shown broad activity as an antimicrobial agent, limiting the replication of many different fungi, bacteria and viruses. In this review, we summarize recent studies supporting the development of curcumin and its derivatives as broad-spectrum antiviral agents.

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Antonelli, Anthony C., Yu Zhang, Lorne M. Golub, Francis Johnson, and Sanford R. Simon. "Inhibition of anthrax lethal factor by curcumin and chemically modified curcumin derivatives." Journal of Enzyme Inhibition and Medicinal Chemistry 29, no. 5 (2013): 663–69. http://dx.doi.org/10.3109/14756366.2013.837901.

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Odes-Barth, Shlomit, Marina Khanin, Karin Linnewiel-Hermoni та ін. "Inhibition of Osteoclast Differentiation by Carotenoid Derivatives through Inhibition of the NF-κB Pathway". Antioxidants 9, № 11 (2020): 1167. http://dx.doi.org/10.3390/antiox9111167.

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The bone protective effects of carotenoids have been demonstrated in several studies, and the inhibition of RANKL-induced osteoclast differentiation by lycopene has also been demonstrated. We previously reported that carotenoid oxidation products are the active mediators in the activation of the transcription factor Nrf2 and the inhibition of the NF-κB transcription system by carotenoids. Here, we demonstrate that lycopene oxidation products are more potent than intact lycopene in inhibiting osteoclast differentiation. We analyzed the structure–activity relationship of a series of dialdehyde carotenoid derivatives (diapocarotene-dials) in inhibiting osteoclastogenesis. We found that the degree of inhibition depends on the electron density of the carbon atom that determines the reactivity of the conjugated double bond in reactions such as Michael addition to thiol groups in proteins. Moreover, the carotenoid derivatives attenuated the NF-κB signal through inhibition of IκB phosphorylation and NF-κB translocation to the nucleus. In addition, we show a synergistic inhibition of osteoclast differentiation by combinations of an active carotenoid derivative with the polyphenols curcumin and carnosic acid with combination index (CI) values < 1. Our findings suggest that carotenoid derivatives inhibit osteoclast differentiation, partially by inhibiting the NF-κB pathway. In addition, carotenoid derivatives can synergistically inhibit osteoclast differentiation with curcumin and carnosic acid.

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Istyastono, Enade Perdana, Rr Sri Untari Siwi S.M.P, Andreas Asdi Utama, and Supardjan A.M. "SYNTHESIS NEW POTENTIAL ANTI-INFLAMMATORY AGENT SODIUM SALT OF PENTAGAMAVUNON-0." Indonesian Journal of Chemistry 4, no. 3 (2010): 180–85. http://dx.doi.org/10.22146/ijc.21850.

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Inflammation is the response of living tissues to injury. The process affects physiological changes such as erythema, edema, asthma and fever. Non-steroid Anti-inflammatory Drugs (NSAIDs) have been developed since they could inhibit inflammation process because of its ability to inhibit biosynthesis of prostaglandin, one of inflammation mediators, through inhibition of cyclooxigenase (COX) enzymes. Molecules, which have been reported having anti-inflammatory activity, for example, are curcumin, some curcumin derivatives and curcumin analogues. One of curcumin analogues that has been developed is pentagamavunon-0 (PGV-0) whose IUPAC name is 2,5-bis(4'-hidroxy-3'-methoxy-benzylidene)cyclo-pentanone. But PGV-0, which is like curcumin, practically insoluble in water, so it causes problems in the development. The aim of this research is to synthesize a derivative of PGV-0, a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0), which is hoped to have a better anti-inflammatory activity and solubility in water than PGV-0. PGV-0 was synthesized by reacting vanillin and cyclopentanone catalized by acid. Na-pentagamavunonate-0 was synthesized with PGV-0 as a starting material using an appropriate method. This research was able to synthesize new compound that was estimated as a natrium salt of PGV-0 (natrium pentagamavunonate-0/Na-pentagamavunonate-0). Keywords: Curcumin, PGV-0, Na-pentagamavunonate-0, anti-inflammation

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Stoica, Laura, Elena Carmen Cotrutz, Cristian Onisor, et al. "Cyclodextrins Increase the Cytotoxicity of Curcumin Derivatives in Osteosarcoma Cell Culture." Revista de Chimie 71, no. 5 (2020): 150–56. http://dx.doi.org/10.37358/rc.20.5.8123.

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Cyclodextrins (CDs), a group of oligosaccharides formed by glucose units bound togetherin a ring, showed a promising ability to form supramolecular complexes with drug molecules and improved theirphysicochemical properties without any molecular modifications. On the other hand, a large number of synthetic curcumin derivatives showed promising anticancer results on malignant cell cultures in recent years. This study presents the advantages and limitations of CDs (potential enhancers of solubility and stability) when are used together with a series of curcumin complexes. All the CD-curcumin complex mixtures were tested as potential anticancer agents on a human osteosarcoma cell culture. A variant of beta-cyclodextrin (monochlorotriazinyl-β-cyclodextrin sodium salt) was found to exhibit the best results in terms of solubility and cytotoxicity enhancements. The results(expressed as inhibitory concentrations for 50 % cell viability - IC50) showed significant improvements for manganese and cooper curcumin complexes and had no effects for boron and thorium complexes.

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Munia, Ingrid, Laurent Gafray, Marie-Agnès Bringer, et al. "Cytoprotective Effects of Natural Highly Bio-Available Vegetable Derivatives on Human-Derived Retinal Cells." Nutrients 12, no. 3 (2020): 879. http://dx.doi.org/10.3390/nu12030879.

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Retinal pigment epithelial cells are crucial for retina maintenance, making their cytoprotection an excellent way to prevent or slow down retinal degeneration. In addition, oxidative stress, inflammation, apoptosis, neovascularization, and/or autophagy are key pathways involved in degenerative mechanisms. Therefore, here we studied the effects of curcumin, lutein, and/or resveratrol on human retinal pigment epithelial cells (ARPE-19). Cells were incubated with individual or combined agent(s) before induction of (a) H2O2-induced oxidative stress, (b) staurosporin-induced apoptosis, (c) CoCl2-induced hypoxia, or (d) a LED-autophagy perturbator. Metabolic activity, cellular survival, caspase 3/7 activity (casp3/7), cell morphology, VEGF levels, and autophagy process were assessed. H2O2 provoked a reduction in cell survival, whereas curcumin reduced metabolic activity which was not associated with cell death. Cell death induced by H2O2 was significantly reduced after pre-treatment with curcumin and lutein, but not resveratrol. Staurosporin increased caspase-3/7 activity (689%) and decreased cell survival by 32%. Curcumin or lutein protected cells from death induced by staurosporin. Curcumin, lutein, and resveratrol were ineffective on the increase of caspase 3/7 induced by staurosporin. Pre-treatment with curcumin or lutein prevented LED-induced blockage of autophagy flux. Basal-VEGF release was significantly reduced by lutein. Therefore, lutein and curcumin showed beneficial protective effects on human-derived retinal cells against several insults.

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Ligeret, Heidi, Sophie Barthélémy, Géraldine Bouchard Doulakas, et al. "Fluoride curcumin derivatives: new mitochondrial uncoupling agents." FEBS Letters 569, no. 1-3 (2004): 37–42. http://dx.doi.org/10.1016/j.febslet.2004.05.032.

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Shi, Wei, Sukanta Dolai, Samar Rizk, et al. "Synthesis of Monofunctional Curcumin Derivatives, Clicked Curcumin Dimer, and a PAMAM Dendrimer Curcumin Conjugate for Therapeutic Applications." Organic Letters 9, no. 26 (2007): 5461–64. http://dx.doi.org/10.1021/ol702370m.

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Kazantzis, K. T., K. Koutsonikoli, B. Mavroidi, et al. "Curcumin derivatives as photosensitizers in photodynamic therapy: photophysical properties and in vitro studies with prostate cancer cells." Photochemical & Photobiological Sciences 19, no. 2 (2020): 193–206. http://dx.doi.org/10.1039/c9pp00375d.

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Increased absorption maximum for the dimethylaminocurcumin with strong PD effect on prostate cancer cells; Intense PD effect of curcumin III on prostate cancer cells; Exciting biphasic PD response by curcumin I and cinnamaldehyde-derived curcumin.

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Pröhl, Michael, Ulrich S. Schubert, Wolfgang Weigand, and Michael Gottschaldt. "Metal complexes of curcumin and curcumin derivatives for molecular imaging and anticancer therapy." Coordination Chemistry Reviews 307 (January 2016): 32–41. http://dx.doi.org/10.1016/j.ccr.2015.09.001.

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Omidi, Sakineh, and Ali Kakanejadifard. "A review on biological activities of Schiff base, hydrazone, and oxime derivatives of curcumin." RSC Advances 10, no. 50 (2020): 30186–202. http://dx.doi.org/10.1039/d0ra05720g.

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Belluti, Silvia, Giulia Orteca, Valentina Semeghini, et al. "Potent Anti-Cancer Properties of Phthalimide-Based Curcumin Derivatives on Prostate Tumor Cells." International Journal of Molecular Sciences 20, no. 1 (2018): 28. http://dx.doi.org/10.3390/ijms20010028.

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Metastatic castration-resistant prostate cancer is commonly treated with chemotherapy, whose effect is less than satisfactory. This raised the need for novel agents for the treatment of prostate cancer. In the present study, five phthalimide-based curcumin derivatives were synthesized and completely characterized to assess improved stability, pharmacodynamics, and radical scavenging ability. To investigate the potential application in anti-cancer therapy, the anti-proliferative activity of the synthesized molecules was determined on aggressive prostate tumor cells. We demonstrated that the K3F21 derivative has increased potency compared to curcumin, in terms of GI50, anti-proliferative and anti-migrating activities. K3F21 inhibits anchorage-dependent and -independent growth of prostate cancer cells by altering the expression of key genes controlling cell proliferation, such as Cylins D1, B1 and B2, and apoptosis, among which Puma, Noxa, and Bcl-2 family members. Finally, the anti-cancer activity of K3F21 was demonstrated by the analysis of cancer-associated PI3K/AKT, ERK, and p38 signaling pathways.

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Kumar, Anil, and Utpal Bora. "In Silico Inhibition Studies of Jun-Fos-DNA Complex Formation by Curcumin Derivatives." International Journal of Medicinal Chemistry 2012 (December 6, 2012): 1–8. http://dx.doi.org/10.1155/2012/316972.

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Activator protein-1 (AP1) is a transcription factor that consists of the Jun and Fos family proteins. It regulates gene expression in response to a variety of stimuli and controls cellular processes including proliferation, transformation, inflammation, and innate immune responses. AP1 binds specifically to 12-O-tetradecanoylphorbol-13-acetate (TPA) responsive element 5′-TGAG/CTCA-3′ (AP1 site). It has been found constitutively active in breast, ovarian, cervical, and lung cancers. Numerous studies have shown that inhibition of AP1 could be a promising strategy for cancer therapeutic applications. The present in silico study provides insights into the inhibition of Jun-Fos-DNA complex formation by curcumin derivatives. These derivatives interact with the amino acid residues like Arg155 and Arg158 which play a key role in binding of Jun-Fos complex to DNA (AP1 site). Ala151, Ala275, Leu283, and Ile286 were the residues present at binding site which could contribute to hydrophobic contacts with inhibitor molecules. Curcumin sulphate was predicted to be the most potent inhibitor amongst all the natural curcumin derivatives docked.

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Martono, Sudibyo. "BENZYLIDENE CYCLOPENTANONE DERIVATIVES AS INHIBITORS OF RAT LIVER GLUTATHIONE S-TRANSFERASE ACTIVITIES." Indonesian Journal of Chemistry 5, no. 1 (2010): 71–75. http://dx.doi.org/10.22146/ijc.21842.

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The effect of the curcumin analogues, 2,6-bis-(4-hydroxy-3-methoxy benzylidene) cyclopentanone (B1) and two of its derivatives on m class glutathione S-transferases (GSTs) from phenobarbital-induced and uninduced rat liver cytosol has been studied to elucidate their anti-inflammatory activity. GST activity was monitored spectrophotometrically using 1,2-dichloro-4-nitrobenzene. B1 was the most potent inhibitor of GSTs, both in uninduced and in phenobarbital-induced rat liver cytosol. These inhibitory properties might be explained as part of the anti-inflammatory activity of benzylidene cyclopentanone derivatives (B1 and B12). Keywords: curcumin; benzylidene cyclopentanone; inhibitory potency; glutathione S-transferases mesoporous

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Pawara, J. M., S. S. Patil, D. K. Patil, and V. S. Kamble. "A NEWER METHODDEVELOPED FOR THE SYNTHESIS OF DIFERULOYL METHANE AND ITS DERIVATIVES." International Journal of Advanced Research 9, no. 02 (2021): 332–37. http://dx.doi.org/10.21474/ijar01/12451.

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Here in the current research work we have developed newer method for the synthesis of diferuloyl methane(curcumin)Ca-q. MangnesiumHydroxide were found to be an effective and mild base for synthesis of curcumin and its derivatives obtained by reaction of one equivalent of acetyl acetone with two equivalent of corresponding aromatic aldehyde in microwave(240 W). The existingscheme offers severalaids such as high yield, less time, and environmentally friendly.

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Barazesh, A., M. Fouladvand, F. Farrokhzad, S. Tajbakhsh, B. Naeimi, and K. Mohammadi. "Evaluation of in vitro anti-leishmanial activities of curcumin and its derivatives “gallium curcumin, indium curcumin and diacetylecurcumin”." International Journal of Infectious Diseases 16 (June 2012): e151-e152. http://dx.doi.org/10.1016/j.ijid.2012.05.343.

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Hoan, Duong Quoc. "SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF SOME DERIVATIVES SYNTHESIZED FROM CURCUMIN AND CURCUMIN ANALOG." Hue University Journal of Science: Natural Science 126, no. 1B (2017): 127. http://dx.doi.org/10.26459/hueuni-jns.v126i1b.4139.

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The acetohydrazides A5 containing an isoxazole ring and B5 containing an indazole ring were synthesized from the corresponding acetohydrazide derivatives with acetic anhydride in about 80% high yield. Also, two acetohydrazones B6 and B7 were driven from acetohydrazide B4 by condensation reaction. Bioactivity testes showed that none of them were active against on bacteria except acetohydrazones B7 showing moderate reactivity against KB cancer cell line at IC50 = 57 mg/L.

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Lo Cascio, Filippa, Paola Marzullo, Rakez Kayed, and Antonio Palumbo Piccionello. "Curcumin as Scaffold for Drug Discovery against Neurodegenerative Diseases." Biomedicines 9, no. 2 (2021): 173. http://dx.doi.org/10.3390/biomedicines9020173.

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Neurodegenerative diseases (NDs) are one of major public health problems and their impact is continuously growing. Curcumin has been proposed for the treatment of several of these pathologies, such as Alzheimer’s disease (AD) and Parkinson’s disease (PD) due to the ability of this molecule to reduce inflammation and aggregation of involved proteins. Nevertheless, the poor metabolic stability and bioavailability of curcumin reduce the possibilities of its practical use. For these reasons, many curcumin derivatives were synthetized in order to overcome some limitations. In this review will be highlighted recent results on modification of curcumin scaffold in the search of new effective therapeutic agents against NDs, with particular emphasis on AD.

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Greish, Khaled, Valeria Pittalà, Sebastien Taurin, et al. "Curcumin–Copper Complex Nanoparticles for the Management of Triple-Negative Breast Cancer." Nanomaterials 8, no. 11 (2018): 884. http://dx.doi.org/10.3390/nano8110884.

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Breast cancer is the most common cancer diagnosed among females worldwide. Although breast cancer survival has largely improved in the past 30 years, it remains highly heterogeneous in its response to treatment. Triple-negative breast cancer (TNBC) is a subtype of breast cancer that lacks the expression of the estrogen receptor (ER), progesterone receptor (PR) and epidermal growth factor receptor-2 (Her2). While TNBC may initially be responsive to chemotherapy, recurrence and subsequent high mortality rates are frequently reported. Studies have shown curcumin and its derivatives to be effective against TNBC cell lines in vitro. To improve its anti-cancer effects, we have synthesized Fe3+–curcumin (Fe–Cur3) and Cu2+–curcumin (CD) complexes and investigated them experimentally. Further, CD was encapsulated into a poly(styrene)-co-maleic acid (SMA) micelle to enhance its stability. We assessed the cytotoxicity of these formulations both in vitro and in vivo. SMA–CD demonstrated dose-dependent cytotoxicity and abolished TNBC tumor growth in vivo. The encapsulation of the curcumin–copper complex improved its anti-cancer activity without overt adverse effects in a murine model of TNBC. These results provide evidence and insights into the value of nanoformulations in enhancing drug-delivery and increasing the potential therapeutic efficacy of curcumin derivatives.

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Quezada, Elías, Fernanda Rodríguez-Enríquez, Reyes Laguna, et al. "Curcumin–Coumarin Hybrid Analogues as Multitarget Agents in Neurodegenerative Disorders." Molecules 26, no. 15 (2021): 4550. http://dx.doi.org/10.3390/molecules26154550.

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Neurodegenerative diseases have a complex nature which highlights the need for multitarget ligands to address the complementary pathways involved in these diseases. Over the last decade, many innovative curcumin-based compounds have been designed and synthesized, searching for new derivatives having anti-amyloidogenic, inhibitory of tau formation, as well as anti-neuroinflammation, antioxidative, and AChE inhibitory activities. Regarding our experience studying 3-substituted coumarins with interesting properties for neurodegenerative diseases, our aim was to synthesize a new series of curcumin–coumarin hybrid analogues and evaluate their activity. Most of the 3-(7-phenyl-3,5-dioxohepta-1,6-dien-1-yl)coumarin derivatives 11–18 resulted in moderated inhibitors of hMAO isoforms and AChE and BuChE activity. Some of them are also capable of scavenger the free radical DPPH. Furthermore, compounds 14 and 16 showed neuroprotective activity against H2O2 in SH-SY5Y cell line. Nanoparticles formulation of these derivatives improved this property increasing the neuroprotective activity to the nanomolar range. Results suggest that by modulating the substitution pattern on both coumarin moiety and phenyl ring, ChE and MAO-targeted derivatives or derivatives with activity in cell-based phenotypic assays can be obtained.

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Zhao, Fei, Huai-Huai Dong, Yuan-Hua Wang, et al. "Synthesis and synergistic antifungal effects of monoketone derivatives of curcumin against fluconazole-resistant Candida spp." MedChemComm 8, no. 5 (2017): 1093–102. http://dx.doi.org/10.1039/c6md00649c.

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