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卡氏乳香树胶中的抗炎和保肝的角鲨烯醇类化合物。

Anti-inflammatory and hepatoprotective cembranoid alcohols 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), China.

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

出版信息

Fitoterapia. 2021 Nov;155:105064. doi: 10.1016/j.fitote.2021.105064. Epub 2021 Oct 14.

Abstract

Five undescribed cembranoid alcohols, boscartinols A-E (1-5) were discovered from the gum resin of Boswellia carterii. Their structures were elucidated by analyzing the spectroscopic data. Notably, all these five compounds preserved an isopropyl type cembranoid skeleton, featured the same groups of one epoxy ring at C-C and one hydroxy group at C-11, as well as two double bonds migrating from C to C and one hydroxy group from C to C within the cembranoid structure. These cembranoids were evaluated for the hepatoprotective and anti-inflammatory activities using two cell models of APAP-induced HepG2 and LPS-induced RAW 264.7. For hepatoprotective activity, compounds 1 and 5 showed remarkable hepatoprotective activity (inhibition rate of 51.6% and 39.8%, respectively) at 10 μM, with the other three compounds of 2-4 showing less potently hepatoprotective. For anti-inflammatory activity, compounds 2-4 showed significant inhibitory effects on NO produced by LPS-induced RAW 264.7 cell (IC values of 13.40 μM, 7.08 μM and 14.26 μM), with the other two compounds of 1 and 5 showing less potently anti-inflammatory activities.

摘要

从乳香树的胶树脂中发现了五种未描述的海松烷醇,即博斯卡丁醇 A-E(1-5)。通过分析光谱数据阐明了它们的结构。值得注意的是,所有这五个化合物都保留了异丙基型海松烷骨架,具有相同的环氧环和 C-11 上的一个羟基基团,以及 C-C 上的两个双键和 C-C 上的一个羟基基团从 C 迁移到 C 。在这五个海松烷中,评估了它们对 APAP 诱导的 HepG2 和 LPS 诱导的 RAW 264.7 两种细胞模型的保肝和抗炎活性。对于保肝活性,化合物 1 和 5 在 10 μM 时表现出显著的保肝活性(抑制率分别为 51.6%和 39.8%),而另外三个化合物 2-4 的保肝活性较弱。对于抗炎活性,化合物 2-4 对 LPS 诱导的 RAW 264.7 细胞产生的 NO 表现出显著的抑制作用(IC 值分别为 13.40 μM、7.08 μM 和 14.26 μM),而另外两个化合物 1 和 5 的抗炎活性较弱。

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