2. Academic Validation
  3. Synthesis and biological evaluation of chrysin derivatives containing α-lipoic acid for the treatment of inflammatory bowel disease

Synthesis and biological evaluation of chrysin derivatives containing α-lipoic acid for the treatment of inflammatory bowel disease

  • Front Chem. 2024 May 27:12:1406051. doi: 10.3389/fchem.2024.1406051.
Pengyu Zhao 1,  Yusen Hou 2 3,  Tingting Yan 4,  Jie Kang 5,  Ye Tian 6,  Jiaxin Li 7,  Chenjuan Zeng 6,  Funeng Geng 2 4,  Qi Liao 4
Affiliations

Affiliations

  • 1 School of Clinical Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • 2 School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • 3 State Key Laboratory of Southwestern Chinese Medicine Resources, College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • 4 Sichuan Key Laboratory of Medical American Cockroach, Chengdu, China.
  • 5 Yunnan Shengke Pharmaceutical Co., Ltd., Kunming, China.
  • 6 Guizhou Yunfeng Pharmaceutical Co., Ltd., Xingyi, China.
  • 7 Sichuan Engineering Research Center for Medicinal Animals, Chengdu, China.
PMID: 38860236 DOI: 10.3389/fchem.2024.1406051
Abstract

This study introduces newly discovered chrysin derivatives that show potential as candidate molecules for treating inflammatory bowel disease (IBD). Compound 4b, among the synthesized compounds, displayed significant inhibitory effects on monocyte adhesion to colon epithelium induced by TNF-α, with an IC50 value of 4.71 μM. Further mechanistic studies demonstrated that 4b inhibits the production of Reactive Oxygen Species (ROS) and downregulates the expression of ICAM-1 and MCP-1, key molecules involved in monocyte-epithelial adhesion, as well as the transcriptional activity of NF-κB. In vivo experiments have shown that compound 4b exhibits a dose-dependent inhibition of 2, 4, 6-trinitrobenzenesulfonic acid (TNBS)-induced colitis in rats, thereby validating its effectiveness as a colitis inhibitor in animal models. These results indicate that 4b shows considerable promise as a therapeutic agent for managing IBD.

Keywords

TNF-α; anti-inflammatory activity; chrysin derivatives; inflammatory bowel disease; small molecules.

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