Citrinal B, natural 11 beta-hydroxysteroid dehydrogennase type 1 inhibitor identified from structure-based virtual screening

被引：4
作者：
Cao, Jie [1 ]
Gao, Limin [1 ]
Chen, Yizhan [2 ]
Sun, Weiguang [3 ]
Wang, Fuqian [4 ]
Li, Hua [3 ]
Zhang, Yonghui [3 ]
机构：
[1] Huazhong Univ Sci & Technol, Tonsil Med Coll, Union Hosp, Wuhan 430030, Hubei, Peoples R China
[2] Huazhong Univ Sci & Technol, Tonsil Med Coll, Tongji Hosp, Wuhan 430030, Hubei, Peoples R China
[3] Huazhong Univ Sci & Technol, Tonsil Med Coll, Hubei Key Lab Nat Med Chem & Resource Evaluat, Wuhan 430030, Hubei, Peoples R China
[4] Wuhan First Hosp, Dept Pharm, Wuhan 430022, Hubei, Peoples R China
来源：
FITOTERAPIA | 2017年 / 123卷
基金：
中国国家自然科学基金;
关键词：
11; beta-HSD1; inhibitor; Citrinal B; Natural product; Virtual screening; ADIPOSE-TISSUE; 11-BETA-HSD1; EXPRESSION; METABOLISM; OBESITY;
D O I：
10.1016/j.fitote.2017.09.018
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Citrinal B, a tricyclic compound from endophytic fungus Colletotrichum capsici in our previous studies, exhibited significant inhibitory activity against 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) in vitro and showed strong binding affinity to 11 beta-HSD1. Moreover, citrinal B treatments decreased the lipid droplet accumulation associate with the inhibition of 11 beta-HSD1 expression in differentiate induced 3T3-L1 preadipocytes. Furthermore, the molecular docking demonstrated that citrinal B coordinated in the active site of 11 beta-HSD1 is essential for the ability of diminishing the enzyme activity.
引用
收藏
页码：29 / 34
页数：6
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