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丁香苷及其天然类似物的全合成及抗炎活性。

Total Syntheses and Anti-inflammatory Activities of Syringin and Its Natural Analogues.

机构信息

Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, School of Pharmacy, Chengdu University, Chengdu 610052, China.

School of Clinical Medical College & Affiliated Hospital, Chengdu University, Chengdu 610052, China.

出版信息

J Nat Prod. 2021 Nov 26;84(11):2866-2874. doi: 10.1021/acs.jnatprod.1c00585. Epub 2021 Oct 18.

DOI:10.1021/acs.jnatprod.1c00585
PMID:34658231
Abstract

Syringin (), a natural bioactive glucoside isolated from the root of (Rupr. Maxim.) Harms, possesses significant anti-inflammatory activity. In this study, we have accomplished the total syntheses of syringin (), along with its natural analogues -, from a common starting material, syringaldehyde (), in 4-8 steps with an overall yields of 11.8-61.3%. The anti-inflammatory activities of these compounds were determined against NO production in the LPS-stimulated RAW264.7 cells. Among them, compounds -, , and exhibited different levels of anti-inflammatory activity.

摘要

丁香苷(),一种从 (Rupr. Maxim.)哈姆斯根中分离得到的天然生物活性葡萄糖苷,具有显著的抗炎活性。在本研究中,我们以丁香醛()为起始原料,通过 4-8 步反应,以 11.8-61.3%的总收率,完成了丁香苷()及其天然类似物 - 的全合成。这些化合物的抗炎活性通过 LPS 刺激的 RAW264.7 细胞中 NO 生成的抑制活性来评价。其中,化合物 - 、- 、- 表现出不同水平的抗炎活性。

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