期刊
PHYTOCHEMISTRY
卷 183, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2020.112593
关键词
Euphorbia fischeriana; Euphorbiaceae; Abietane; Mycobacterium tuberculosis; Human carboxylesterase 2
资金
- National Natural Science Foundation of China [81872970, 81930112]
- Liaoning Provincial Key RD Program [2019JH2/10300022]
- Liaoning Revitalization Talents Program [XLYC1907017]
- Program for High-level Talents of Dalian City [2017RQ119]
- Distinguished professor of Liaoning Province
- Support Program for Innovative Talents in the Universities of Liaoning Province
The roots of Euphorbia fischeriana contain 15 diterpenoids that show moderate inhibitory effects on the proliferation of Mycobacterium tuberculosis, with eupholides F-H being the most effective. Additionally, some of these compounds significantly inhibit the lyase activity of human carboxylesterase 2.
The roots of Euphorbia fischeriana known as Langdu in traditional Chinese medicine have been used for the treatment of tuberculosis in China. Through a bioactive phytochemical investigation of the roots of E. fischeriana, 15 diterpenoids were obtained by various chromatographic techniques. On the basis of wide spectroscopic data, including NMR, UV, IR, HR-ESI-MS, ECD and X-ray crystallography, all of the isolated compounds were elucidated to be ent-abietane diterpenoid analogs, including undescribed eupholides A-H and seven known diterpenoids. In the bioassay for anti-tuberculosis, eupholides F-H moderately inhibited the proliferation of Mycobacterium tuberculosis H37Ra, with the MIC determined to be 50 mu M. Furthermore, eupholides G, ent-11 alpha-hydroxyabieta-8(14), 13(15)-dien-16,12 alpha-olide, and jolkinolide F significantly inhibited the lyase activity of human carboxylesterase 2 (HCE 2), with IC50 values of 7.3, 150, and 34.5 nM, respectively.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据