AUTHOR=Li Canjie , Sun Xin , Yin Wenjing , Zhan Zhaochun , Tang Qing , Wang Wenzhi , Zhuo Xuefang , Wu Zhongnan , Zhang Haipeng , Li Yaolan , Zhang Yubo , Wang Guocai 

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

JOURNAL=Frontiers in Chemistry

VOLUME=9

YEAR=2021

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2021.733350

DOI=10.3389/fchem.2021.733350

ISSN=2296-2646

ABSTRACT=<p>Seven new clerodane diterpenoids, crassifolins Q−W (<bold>1</bold>–<bold>7</bold>), along with five known analogues (<bold>8</bold>–<bold>12</bold>), were isolated from the roots of <italic>Croton crassifolius</italic>. 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 <bold>1</bold>–<bold>5</bold> against inflammatory cytokines IL-6 and TNF-<italic>α</italic> levels on LPS-induced RAW 264.7 macrophages were assessed, and compound <bold>5</bold> showed the most significant activity with the secretion levels of IL-6 and TNF-<italic>α</italic> at 32.78 and 12.53%, respectively. Moreover, compounds <bold>1</bold>–<bold>5</bold> were screened for their anti-angiogenesis using a human umbilical vein endothelial cells <italic>in vitro</italic> mode; the results showed all of them exhibited obvious anti-angiogenesis activities, in particular, compound <bold>5</bold> showed the strongest anti-angiogenesis effect in the range of 6.25–50 μM.</p>