Bioactivity Study of Tricyclic and Tetracyclic Genipin Derivatives as Anti-inflammatory Agents

Li, Sin-Min; Chiang, Chia-Yin; Zeng, Wei-Zheng; Chung, Cheng-Yen; Tseng, Ching‐Chun; Hu, Yu-Pei; Lin, Yu-Ching; Huang, Guan‐Jhong; Arai, Ichiro; Lee, Der-Yen; Tsai, Shu-Yao; Wong, Fung Fuh

doi:10.1016/j.bioorg.2022.105881

Cited by 5 publications

(1 citation statement)

References 30 publications

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“…Studies have shown that Genipin has antiinflammatory Li et al (2022), antiangiogenic ?, antioxidant Koriyama et al (2010), and antiinsulin resistance Guan et al (2013) effects and is used to treat a variety of inflammatory diseases, including cancer Yang et al (2013). It has been reported that the antitumor effects of Genipin may be mediated by various mechanisms, including apoptosis Xia et al (2021), stopping of cell cycle Bai et al (2022), inhibiting invasion and metastasis Lee et al (2018).…”

Section: Discussionmentioning

confidence: 99%

Genipin as the Active Compound of Gardenia fruits Inhibit Proliferation, Migration and Autophagy of Prostate Cancer through PI3K/AKT Signaling Pathway

Dai,

Chen,

Wei

et al. 2024

Preprint

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Purpose:Prostate cancer is the second most diagnosed cancer type and the most common cause of cancer-related deaths in men. Genipin is a protein cross-linking agent extracted from Gardenia (Gardenia jasminoides Ellis) fruits, which has been reported to exhibit antitumor activity against several types of cancer. The aim of the present study was to investigate the antitumor effect of Genipin on prostate cancer and the underlying molecular mechanisms.Methods:CCK-8 assays were performed to determine the cell viability of genipin prostate cancer cells lines (DU145, PC-3, RM-1) and normal prostate cell lines (WPMY1). Colony formation assays, and wound-healing assays used to detect the effect of genipin on DU145, PC-3 and RM-1 cell lines. Immunofluorescence and western blotting were carried out to investigate its mechanism.Results:Genipin inhibited the survival of DU-145, PC-3 and RM-1 cells in a time-dependent and dose-dependent manner. And Genipin induced apoptosis of prostate carcinoma cells, including DU-145, PC-3 and RM-1 cells. Moreover, the expression of p62 in DU-145 and PC-3 cells was down-regulated, whereas Beclin1 and LC3II/ I were up-regulated. In addition, genipin also decreased p-PI3K, p-AKT, p-NF-\(\kappa\)B and p-mTOR.Conclusion:Genipin is the active compound to inhibit proliferation and migration of prostate cancer through PI3K/AKT/NF-\(\kappa\)B signaling pathway and promoted prostate cancer cells autophagy through PI3K/AKT/mTOR signaling pathway, indicating that Genipin may serve as a potential lead drug for prostate cancer treatment. Therefore, Genipin may be used as a novel therapeutic agent in the treatment of prostate cancer.

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Section: Discussionmentioning

confidence: 99%

Genipin as the Active Compound of Gardenia fruits Inhibit Proliferation, Migration and Autophagy of Prostate Cancer through PI3K/AKT Signaling Pathway

Dai,

Chen,

Wei

et al. 2024

Preprint

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Small Molecules as Anti‐inflammatory Agents: Molecular Mechanisms and Heterocycles as Inhibitors of Signaling Pathways

Basha¹

2023

ChemistrySelect

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Cancer and inflammation interlink with many pathways. Millions of people died because of these two disorders. Major pathways that cause both inflammation and cancer are STAT3, NF‐κB, COX, and histone acetylation. However, these are the target for medicinally potent heterocycles such as pyrimidines, indole, and pyrazole. Many NSAIDs reported in the literature belong to both natural and synthetic molecules. This review encompasses molecular mechanisms for inflammation, NSAIDs derived from natural sources and synthetic methods, and recent reports on heterocycles as potent anti‐inflammatory agents and their significance in cancer treatment. Literature for the study, accomplished from 2019 to 2022.

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Genipin’s potential as an anti-cancer agent: from phytochemical origins to clinical prospects

Natallia,

Dama,

Gorica

et al. 2024

Med Oncol

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Bioactivity Study of Tricyclic and Tetracyclic Genipin Derivatives as Anti-inflammatory Agents

Cited by 5 publications

References 30 publications

Genipin as the Active Compound of Gardenia fruits Inhibit Proliferation, Migration and Autophagy of Prostate Cancer through PI3K/AKT Signaling Pathway

Genipin as the Active Compound of Gardenia fruits Inhibit Proliferation, Migration and Autophagy of Prostate Cancer through PI3K/AKT Signaling Pathway

Small Molecules as Anti‐inflammatory Agents: Molecular Mechanisms and Heterocycles as Inhibitors of Signaling Pathways

Genipin’s potential as an anti-cancer agent: from phytochemical origins to clinical prospects

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