Phytochemicals in Drug Discovery—A Confluence of Tradition and Innovation

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(16), P. 8792 - 8792

Published: Aug. 13, 2024

Phytochemicals have a long and successful history in drug discovery. With recent advancements analytical techniques methodologies, discovering bioactive leads from natural compounds has become easier. Computational like molecular docking, QSAR modelling machine learning, network pharmacology are among the most promising new tools that allow researchers to make predictions concerning products’ potential targets, thereby guiding experimental validation efforts. Additionally, approaches LC-MS or LC-NMR speed up compound identification by streamlining processes. Integrating structural computational biology aids lead identification, thus providing invaluable information understand how phytochemicals interact with targets body. An emerging approach is learning involving deep neural networks interrelate phytochemical properties diverse physiological activities such as antimicrobial anticancer effects.

Language: Английский

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Sterpiperazines A and B, steroid-indole alkaloids with Tdp1 inhibitory and chemotherapy sensitizing activities from marine fungus Aspergillus sp. EGF 15-0-3

Chinese Chemical Letters, Journal Year: 2025, Volume and Issue: unknown, P. 111048 - 111048

Published: March 1, 2025

Language: Английский

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Advances in triterpene drug discovery

Trends in Pharmacological Sciences, Journal Year: 2024, Volume and Issue: 45(11), P. 964 - 968

Published: Oct. 31, 2024

Triterpenes are structurally complex natural products with promising therapeutic properties. Recalcitrance to chemical synthesis has hindered their use in drug development. Recent advances now make it possible access and harness triterpene structural diversity using engineering biology approaches, enabling the discovery optimisation of a new generation leads.

Language: Английский

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In vivo wound healing activity of electrospun nanofibers embedding natural products

Arabian Journal of Chemistry, Journal Year: 2024, Volume and Issue: 17(12), P. 106019 - 106019

Published: Oct. 15, 2024

Language: Английский

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Uvaol attenuates TGF-β1-induced epithelial-mesenchymal transition in human alveolar epithelial cells by modulating expression and membrane localization of β-catenin

Frontiers in Pharmacology, Journal Year: 2025, Volume and Issue: 15

Published: Jan. 7, 2025

The epithelial-mesenchymal transition (EMT) is a biological process in which epithelial cells change into mesenchymal with fibroblast-like characteristics. EMT plays crucial role the progression of fibrosis. Classical inducers associated maintenance EMT, such as TGF-β1, have become targets several anti-EMT therapeutic strategies. Natural products from pentacyclic triterpene class emerged promising elements inhibiting EMT. Uvaol found olive trees (Olea europaea L.) known for its anti-inflammatory, antioxidant, and antiproliferative properties. Yet, effect on TGF-β1-induced alveolar unknown. present study aimed to investigate impact uvaol upon cultured A549 human cell line, classic vitro model studies Changes shape were measured using phase-contrast confocal microscopy, whereas protein expression levels immunofluorescence, flow cytometry, Western blotting. We also performed wound scratch experiments explore effects migration. had no significant cytotoxic cells. By contrast, changes morphology consistent largely suppressed by treatment uvaol. In addition, increased contents markers, namely, vimentin, N-cadherin, fibronectin cells, downregulated treatment. Furthermore, migration was significantly Mechanistically, prevented nuclear translocation β-catenin reduced ZEB1 These results provide compelling evidence that inhibits regulating proteins related profile likely modulating levels.

Language: Английский

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Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 289, P. 117461 - 117461

Published: Feb. 28, 2025

Language: Английский

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Synthesis, antiproliferative activity, and biological profiling of C-19 trityl and silyl ether andrographolide analogs in colon cancer and breast cancer cells

Bioorganic & Medicinal Chemistry Letters, Journal Year: 2025, Volume and Issue: 121, P. 130163 - 130163

Published: March 3, 2025

Language: Английский

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Identification of SRC, AKT1 and MAPK3 as Therapeutic Targets of Apigenin and Luteolin in Colorectal and Colon Carcinoma through Network Pharmacology

Food Bioscience, Journal Year: 2025, Volume and Issue: unknown, P. 106313 - 106313

Published: March 1, 2025

Language: Английский

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Structurally diverse sesquiterpenes with anti-leukemia activity from the rare medicinal plant Liriodendron chinense

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 158, P. 108341 - 108341

Published: March 8, 2025

Language: Английский

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Privileged natural product compound classes for anti-inflammatory drug development

Natural Product Reports, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 1, 2025

This review highlights six privileged classes of natural products – coumarins, polyphenols, labdane diterpenoids, sesquiterpene lactones, isoquinoline and indole alkaloids—for potential anti-inflammatory drug development.

Language: Английский

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