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

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机构： [1]Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, China, [2]The First Affiliated Hospital of Jinan University, Guangzhou, China, [3]Department of Pharmacology, School of Medicine, Guangdong Clinical Translational Center for Targeted Drug, Jinan University, Guangzhou, China

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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-α 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-α 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 μM.Copyright © 2021 Li, Sun, Yin, Zhan, Tang, Wang, Zhuo, Wu, Zhang, Li, Zhang and Wang.

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出版当年[2020]版：

大类 | 2 区化学

小类 | 3 区化学综合

最新[2025]版：

大类 | 3 区化学

小类 | 4 区化学：综合

第一作者：

第一作者机构： [1]Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, China,

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通讯机构： [1]Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, China, [3]Department of Pharmacology, School of Medicine, Guangdong Clinical Translational Center for Targeted Drug, Jinan University, Guangzhou, China

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