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Semisynthesis and antitumor activity of endertiin B and related triterpenoids from Ganoderma lucidum

文献类型： 外文期刊

作者： Liu, Yu 1 ; Wen, Hong-Kai 1 ; Xu, Rui-Xuan 1 ; Liu, Chang 1 ; Li, Xiao-Han 1 ; Qin, Xiang-Dong 4 ; Zhao, You-Xing 5 ; Jia, Yan-Xing 2 ; Luo, Dou-Qiang 1 ;

作者机构： 1.Hebei Univ, Coll Life Sci, Baoding, Peoples R China

2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing, Angola

3.Peking Univ, Chem Biol Ctr, Beijing, Peoples R China

4.Hebei Univ, Hebei Innovat Ctr Bioengn & Biotechnol, Baoding, Peoples R China

5.Chinese Acad Trop Agr Sci, Hainan Inst Trop Agr Resources, Inst Trop Biosci & Biotechnol, Haikou, Peoples R China

期刊名称：ORGANIC & BIOMOLECULAR CHEMISTRY （ 影响因子：3.2； 五年影响因子：3.0 ）

ISSN： 1477-0520

年卷期： 2024 年

页码：

收录情况： SCI

摘要： Ganoderma lucidum, a fungus used in traditional Chinese medicine, is known for its medicinal value attributed to its active components called Ganoderma triterpenoids (GTs). However, the limited isolation rate of these GTs has hindered their potential as promising drug candidates. Therefore, it is imperative to achieve large-scale preparation of GTs. In this study, four GTs were effectively synthesised from lanosterol. The antitumor activity of these GTs was evaluated in vivo. Endertiin B exhibited potent inhibitory activity against breast cancer cells (9.85 +/- 0.91 mu M and 12.12 +/- 0.95 mu M). Further investigations demonstrated that endertiin B significantly upregulated p21 and p27 and downregulated cyclinD1 expression, arresting the cell cycle at the G0/G1 phase and inducing apoptosis by decreasing BCL-2 and increasing BAX and BAK levels. Additionally, endertiin B was found to reduce the expression of proteins associated with the PI3K-AKT signaling pathway. To summarize, endertiin B effectively inhibited cell proliferation by blocking the cell cycle and inducing apoptosis through the PI3K-AKT pathway.

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