卷柏中的卷柏素衍生物及其抗乳腺癌活性评价。
Selaginellin derivatives from Selaginella tamariscina and evaluation for anti-breast cancer activity.
发表日期：2023 Nov 10
作者：
Jing Wen, Dong-Mei Sha, Xiao-Yong He, Yu-Han Tian, Shuai-Cong Ni, Bin He, Yuan Liu, Xin-Jia Yan
来源：
PHYTOCHEMISTRY
摘要：
对卷柏的植物化学研究分离出 17 种卷柏素衍生物。筛选了它们对乳腺癌细胞的抑制活性，并建立了初步的构效关系。其中，二聚卷柏素17对MDA-MB-231细胞表现出潜在活性，IC50值为3.2±0.1μM，相当于参考化合物5-FU（IC50 14.8±0.2μM）的4倍效力。机制研究表明，17 可以导致 MDA-MB-231 细胞 G2/M 期阻滞，并诱导细胞凋亡，并伴有 ROS 水平增加。版权所有 © 2023。由 Elsevier Ltd 出版。
A phytochemical investigation of Selaginella tamariscina led to the isolation of 17 selaginellin derivatives. Their inhibitory activities against breast cancer cells were screened, and preliminary structure-activity relationships were also established. Among them, dimeric selaginellin 17 showed potential activity against MDA-MB-231 cells with an IC50 value of 3.2 ± 0.1 μM, corresponding to 4-fold higher potency than the reference compound 5-FU (IC50 14.8 ± 0.2 μM). Mechanistic studies indicated that 17 could cause G2/M phase arrest in MDA-MB-231 cells and induce apoptosis accompanied by increased ROS levels.Copyright © 2023. Published by Elsevier Ltd.