Crassifolins Q-W: Clerodane Diterpenoids From Croton crassifolius With Anti-Inflammatory and Anti-Angiogenesis Activities

被引:14
作者
Li, Canjie [1 ]
Sun, Xin [1 ,2 ]
Yin, Wenjing [3 ]
Zhan, Zhaochun [1 ]
Tang, Qing [1 ]
Wang, Wenzhi [1 ]
Zhuo, Xuefang [1 ]
Wu, Zhongnan [2 ]
Zhang, Haipeng [3 ]
Li, Yaolan [1 ]
Zhang, Yubo [1 ,3 ]
Wang, Guocai [1 ]
机构
[1] Jinan Univ, Inst Tradit Chinese Med & Nat Prod, Coll Pharm, Guangdong Prov Key Lab Pharmacodynam Constituents, Guangzhou, Peoples R China
[2] Jinan Univ, Affiliated Hosp 1, Guangzhou, Peoples R China
[3] Jinan Univ, Guangdong Clin Translat Ctr Targeted Drug, Sch Med, Dept Pharmacol, Guangzhou, Peoples R China
来源
FRONTIERS IN CHEMISTRY | 2021年 / 9卷
基金
中国国家自然科学基金;
关键词
Euphorbiaceae; Croton crassifolius; clerodane diterpenoids; anti-inflammatory activity; anti-angiogenic activity; PHORBOL ESTERS; APOPTOSIS; ROOTS;
D O I
10.3389/fchem.2021.733350
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Seven new clerodane diterpenoids, crassifolins Q-W (1-7), along with five known analogues (8-12), were isolated from the roots of Croton crassifolius. Their structures were identified by comprehensive spectroscopic analysis (UV, IR, NMR, and HR-ESI-MS), and their absolute configurations were determined by ECD spectra and X-ray crystallography. The activities of compounds 1-5 against inflammatory cytokines IL-6 and TNF-alpha levels on LPS-induced RAW 264.7 macrophages were assessed, and compound 5 showed the most significant activity with the secretion levels of IL-6 and TNF-alpha at 32.78 and 12.53%, respectively. Moreover, compounds 1-5 were screened for their anti-angiogenesis using a human umbilical vein endothelial cells in vitro mode; the results showed all of them exhibited obvious anti-angiogenesis activities, in particular, compound 5 showed the strongest anti-angiogenesis effect in the range of 6.25-50 mu M.
引用
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页数:12
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