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来自……的新型抗增殖吉马烷型倍半萜内酯

New antiproliferative germacranolides from .

作者信息

Zhang Tao, Zhang Qiu-Bo, Fu Lu, Li Ling-Yu, Ma Li-Yan, Si Jin-Guang, Zhang Hong-Wu, Wei Jian-He, Yu Shi-Shan, Zou Zhong-Mei

机构信息

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Peking Union Medical College Beijing 100193 P. R. China

School of Pharmacy, Henan University of Traditional Chinese Medicine Zhengzhou 450008 P. R. China.

出版信息

RSC Adv. 2019 Apr 11;9(20):11493-11502. doi: 10.1039/c9ra00478e. eCollection 2019 Apr 9.

DOI:10.1039/c9ra00478e
PMID:35520265
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9063262/
Abstract

Six new highly oxygenated (2-7) and one known (1) germacranolides were isolated from the whole plant of . The planar structures and relative configurations of the new compounds were determined by detailed spectroscopic analysis. The absolute configurations of 1 and 3 were established by circular dichroism (CD) and X-ray crystallographic analyses, and the stereochemistry of the new compounds 2 and 4-6 were determined by similar CD data to 1 and 3, respectively. All isolates were evaluated for their antiproliferative activities against three human tumor cell lines, and compounds 3 and 6 show antiproliferative activities against HeLa and Hep G2 cells with IC values of 4.13-8.37 μM. Intensive mechanism study showed that 3 caused cell-cycle arrest at the S/G2 phase and induced apoptosis in Hep G2 cells through a mitochondria-related pathway.

摘要

从[植物名称]全株中分离出6个新的高度氧化的吉马烷型倍半萜内酯（2 - 7）和1个已知的（1）。通过详细的光谱分析确定了新化合物的平面结构和相对构型。通过圆二色光谱（CD）和X射线晶体学分析确定了1和3的绝对构型，新化合物2和4 - 6的立体化学分别通过与1和3相似的CD数据确定。评估了所有分离物对三种人类肿瘤细胞系的抗增殖活性，化合物3和6对HeLa和Hep G2细胞显示出抗增殖活性，IC值为4.13 - 8.37μM。深入的机制研究表明，3导致细胞周期停滞在S/G2期，并通过线粒体相关途径诱导Hep G2细胞凋亡。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/707cef3aad7c/c9ra00478e-f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/7de355ff3d12/c9ra00478e-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/80c93ef8c27f/c9ra00478e-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/51d124107031/c9ra00478e-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/c03f9a4596ed/c9ra00478e-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/b4c4906e75c9/c9ra00478e-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/dd57800ac6c4/c9ra00478e-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/c809015b2c05/c9ra00478e-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/5eb35575537e/c9ra00478e-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/707cef3aad7c/c9ra00478e-f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/7de355ff3d12/c9ra00478e-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/80c93ef8c27f/c9ra00478e-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/51d124107031/c9ra00478e-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/c03f9a4596ed/c9ra00478e-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/b4c4906e75c9/c9ra00478e-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/dd57800ac6c4/c9ra00478e-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/c809015b2c05/c9ra00478e-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/5eb35575537e/c9ra00478e-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fb/9063262/707cef3aad7c/c9ra00478e-f9.jpg

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