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从. 中分离得到具有抗非酒精性脂肪性肝炎活性的多种多环多聚异戊烯基酰基间苯三酚同系物。

Diverse Polycyclic Polyprenylated Acylphloroglucinol Congeners with Anti-Nonalcoholic Steatohepatitis Activity from .

机构信息

Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.

出版信息

J Nat Prod. 2021 Apr 23;84(4):1135-1148. doi: 10.1021/acs.jnatprod.0c01202. Epub 2021 Mar 31.

Abstract

The new polycyclic polyprenylated acylphloroglucinols, hyperforcinols A-J (-), were isolated from the fruits of , together with 30 biogenetic congeners of known structures. The structures of hyperforcinols A-J were determined by HRESIMS and 1D/2D NMR spectroscopic analysis, and their absolute configurations were determined by a combination of the electronic circular dichroism (ECD) exciton chirality method, ECD calculations, and X-ray diffraction analysis. A selection of 25 isolates, possessing seven types of carbon skeletons, were assessed for their in vitro effects against nonalcoholic steatohepatitis (NASH) using a free fatty acid-induced L02 cell model. Compounds and significantly decreased intracellular lipid accumulation. QRT-PCR analyses revealed that compounds and regulate the expression of lipid metabolism-related genes, including , , , and .

摘要

新型多环多聚异戊烯基酰基间苯三酚类化合物,hyperforcinols A-J(-),从 的果实中分离得到,同时还分离得到了 30 种已知结构的生物合成同系物。通过高分辨质谱(HRESIMS)和 1D/2D NMR 波谱分析确定了 hyperforcinols A-J 的结构,通过电子圆二色性(ECD)外消旋手性法、ECD 计算和 X 射线衍射分析相结合的方法确定了它们的绝对构型。对具有七种碳骨架的 25 种分离物进行了体外非酒精性脂肪性肝炎(NASH)的评估,采用游离脂肪酸诱导的 L02 细胞模型进行评估。化合物 和 显著降低了细胞内脂质积累。QRT-PCR 分析表明,化合物 和 调节脂质代谢相关基因的表达,包括 、 、 、和 。

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