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卡氏乳香树胶脂中的生物活性海松二萜。

Bioactive cembrane diterpenoids from the gum resin of Boswellia carterii.

机构信息

School of Pharmaceutical Sciences, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250014, China; Key Laboratory for Applied Techonology of Sophisticated Analytical Instruments of Shandong Province, Shandong Analysis and Test Center, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250014, China.

Reyoung Pharmaceutical Co., Ltd, No. 44 Cultural West Road, Jinan 250012, China.

出版信息

Fitoterapia. 2020 Oct;146:104699. doi: 10.1016/j.fitote.2020.104699. Epub 2020 Aug 4.

DOI:10.1016/j.fitote.2020.104699
PMID:32763364
Abstract

Eight new cembrane-type diterpenoids, boscartins AP-AW (1-8) were obtained from the gum resin of Boswellia carterii. Among which, six ones (2-7) were isomers, with one hydroxy group and two double bonds migrating along the carbocycle. The structures were elucidated by spectroscopic examination. All isolates were evaluated for anti-inflammatory activity and hepatoprotective activity by cell models of LPS-induced RAW 264.7 mouse peritoneal macrophages and APAP-induced HepG2 cells, respectively. As for anti-inflammatory activity assay, compound 1 exhibited potent activity against NO production (IC of 13.1 μM), with the other ones exhibiting weak anti-inflammatory activity (IC > 50 μM). As for hepatoprotective activity assay, compound 1 exhibited more significant activity (inhibition rate of 30.7%) than that of the positive control (bicyclol, inhibition rate of 27.2%), and compounds 4, and 6 showed nearly the same activities as the control (inhibition rates of 26.7% and 25.9%, respectively), with the other ones exhibiting weak hepatoprotective activity.

摘要

从乳香树的胶树脂中分离得到了 8 个新的贝壳杉烷二萜类化合物,boscartins AP-AW(1-8)。其中,6 个化合物(2-7)为异构体,具有一个羟基和两个沿着碳环迁移的双键。通过光谱检查阐明了结构。所有分离物均通过 LPS 诱导的 RAW 264.7 小鼠腹腔巨噬细胞和 APAP 诱导的 HepG2 细胞的细胞模型分别评估了抗炎活性和保肝活性。在抗炎活性测定中,化合物 1 对 NO 产生具有很强的抑制活性(IC50 为 13.1 μM),而其他化合物的抗炎活性较弱(IC > 50 μM)。在保肝活性测定中,化合物 1 比阳性对照(双环醇,抑制率为 27.2%)表现出更显著的活性(抑制率为 30.7%),化合物 4 和 6 表现出与对照几乎相同的活性(抑制率分别为 26.7%和 25.9%),而其他化合物则表现出较弱的保肝活性。

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