Synthesis and anti-inflammatory activities of oridonin sulfonylurea derivatives
10.12206/j.issn.2097-2024.202401048
- 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
;
Mochenxuan LI
2
;
Zhenyuan MIAO
3
;
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;School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
3. 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.
