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白术中的多样多炔类化合物及其抗破骨细胞生成活性。

Diverse polyacetylenes from Atractylodes chinensis and their anti-osteoclastogenesis activity.

机构信息

Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.

Research Center for Drug Discovery, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People's Republic of China.

出版信息

Fitoterapia. 2022 Sep;161:105233. doi: 10.1016/j.fitote.2022.105233. Epub 2022 Jun 8.

Abstract

The phytochemical investigation on Atractylodes chinensis afforded 15 polyacetylenes 1-15 and one meroterpenoid 16. Of the 16 isolates, compounds 4 and 9 are new ones, and compounds 8 and 16 are first reported from nature. In addition, the relative configuration of 1 and the available NMR data of compounds 1, 8, and 16 were first provided. Their structures were elucidated by extensive analysis of MS, UV, IR, and NMR spectroscopic data. Besides, all isolated compounds were evaluated for their effects on RANKL-induced osteoclastogenesis in BMMs. Among them, polyacetylenes 12-14 showed potent inhibitory activity with IC values of 0.67 ± 0.05 μM, 0.72 ± 0.31 μM, and 2.40 ± 0.41 μM, respectively. The current work demonstrates the polyacetylenes are the main active constituents of A. chinensis against osteoclastogenesis.

摘要

白术的植物化学研究得到了 15 个聚乙炔 1-15 和一个倍半萜 16。在 16 个分离物中,化合物 4 和 9 是新化合物,化合物 8 和 16 是首次从自然界中报道的。此外,首次提供了化合物 1 的相对构型和化合物 1、8 和 16 的可用 NMR 数据。它们的结构通过对 MS、UV、IR 和 NMR 光谱数据的广泛分析来阐明。此外,所有分离得到的化合物都评估了它们对 BMMs 中 RANKL 诱导的破骨细胞分化的影响。其中,聚乙炔 12-14 表现出很强的抑制活性,IC 值分别为 0.67±0.05 μM、0.72±0.31 μM 和 2.40±0.41 μM。本研究表明,聚乙炔是白术抑制破骨细胞分化的主要活性成分。

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