Synthesis and anti-inflammatory activities of oridonin sulfonylurea derivatives

VernacularTitle:冬凌草甲素磺酰脲衍生物的设计与抗炎活性研究
Author: Ruonan WU ¹ ; Shuang YE ^{2
,

3} ; Mochenxuan LI ^{2
,

3} ; Zhenyuan MIAO ⁴ ; Chuan LUO ¹
Author Information

1. Anhui Huarun Golden Frog Pharmaceutical Ltd., Huaibei 235000, China.
2. School of Pharmacy, Naval Medical University, Shanghai 200433, China
3. School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
4. School of Pharmacy, Naval Medical University, Shanghai 200433, China.
Publication Type:Originalarticles
Keywords: oridonin; photocatalysis reaction; scaffold hopping; synthesis; anti-inflammatory activity
From: Journal of Pharmaceutical Practice and Service 2025;43(7):335-338
CountryChina
Language:Chinese
Abstract: Objective To study anti-inflammatory activities of oridonin derivatives without Michael fragment. Methods Two oridonin sulfonylureas were designed and synthesized by a photocatalysis reaction and a scaffold hopping strategy. The inhibitory rate of IL-1β was selected for anti-inflammatory activity evaluation. Results Both compound ZM658 and ZM659 revealed potent anti-inflammatory activities with the values of 69.3% and 59.7% in THP-1 cells, respectively. Moreover, two compounds also showed dose-dependent and low cytotoxicity. Conclusion The result indicated that Michael receptor fragment of oridonin could be substituted with sulfonylurea group.