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来自Ganoderma lucidumGanoderma lucidumGanoderma lucidumGanoderma lucidumGanoderma lucidumGanoderma lucidumGanoderma

Yu Liu^1,2, Hong-Kai Wen^1,2, Rui-Xuan Xu^1,2

¹College of Life Science, Hebei University, Baoding, China. duqiangluo@hbu.edu.cn.

Organic & biomolecular chemistry

|June 4, 2024

概括

光的三基 (GTs) 显示出抗瘤的潜力. 合成的GTEndertiin B通过PI3K-AKT通路诱导细胞亡和细胞循环停止,有效地抑制了乳腺癌细胞的增殖.

科学领域:

自然产品化学化学
药理学药理学是指药理学的学科.
在瘤学瘤学.

背景情况:

瑞 (Ganoderma lucidum) 是一种中国传统医学的生物活性化合物的来源.
甘三 (GTs) 具有药用特性,但在大规模隔离中面临挑战.
高效的GT合成对于其作为候选药物的发展至关重要.

研究的目的:

为了从兰醇中合成甘菌三基 (GTs).
评估合成GTs,特别是Endertiin B.的体内抗瘤活性.
阐明Endertiin B抗癌作用背后的分子机制.

主要方法:

来自兰醇的四个GT的化学合成.
在体内对抗乳腺癌细胞的抗瘤活性进行评估.
对细胞循环调节剂 (p21,p27,cyclinD1),细胞亡标记物 (BCL-2,BAX,BAK) 和PI3K-AKT通路的分析.

主要成果:

恩德丁B对乳腺癌细胞表现出强大的抑制作用 (IC50值为9.85±0.91μM和12.12±0.95μM).
恩德丁B诱导G0/G1细胞循环停止通过上调p21和p27和下调环林D1.1.
恩德丁B通过调节BCL-2,BAX和BAK的表达和抑制PI3K-AKT通路来触发亡.

结论:

恩德丁B是一种合成的Ganoderma三基,具有显著的抗瘤活性.
恩德丁B通过细胞循环停止和亡诱导有效地抑制癌细胞的增殖.
PI3K-AKT信号通路是Endertiin B抗癌作用的关键目标.

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