化学生物组学揭示，索法酮通过共价结合 HMGB1 抑制 Caco-2 细胞的炎症反应。

Chemoproteomics reveals Sofalcone inhibits the inflammatory response of Caco-2 cells by covalently targeting HMGB1.

机构信息

Laboratory Medicine, First Affiliated Hospital of Gannan Medical University, Ganzhou, 341000, China.

Artemisinin Research Center, and Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, 100700, China.

出版信息

Chem Commun (Camb). 2023 Jul 18;59(58):8981-8984. doi: 10.1039/d3cc00577a.

DOI:10.1039/d3cc00577a

PMID:37394927

Abstract

Sofalcone (Sof), a synthetic analog of sophoradin, is a type of natural phenol derived from the traditional medicinal herb , with potent anti-inflammatory activity. However, the mechanisms of action of Sof for treating intestinal-associated inflammation are not well known. In this work, we identified high mobility group box 1 (HMGB1) as the key covalent target of Sof for the anti-inflammatory activity in the human colonic epithelial cells through quantitative chemoproteomics profiling.

摘要

苦参素（Sof）是苦参堿的合成类似物，是一种天然酚类化合物，来源于传统中药，具有很强的抗炎活性。然而，Sof 治疗肠道相关炎症的作用机制尚不清楚。在这项工作中，我们通过定量化学蛋白质组学分析，确定高迁移率族蛋白 B1（HMGB1）是 Sof 在人结肠上皮细胞中抗炎活性的关键共价靶标。