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

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单位: [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
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关键词: 11 beta-HSD1 inhibitor Citrinal B Natural product Virtual screening

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.

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出版当年[2016]版:
大类 | 3 区 医学
小类 | 3 区 药物化学 3 区 药学
最新[2025]版:
大类 | 3 区 医学
小类 | 3 区 药物化学 3 区 药学
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出版当年[2015]版:
Q2 PHARMACOLOGY & PHARMACY Q3 CHEMISTRY, MEDICINAL
最新[2023]版:
Q3 CHEMISTRY, MEDICINAL Q3 PHARMACOLOGY & PHARMACY

影响因子: 最新[2023版] 最新五年平均 出版当年[2015版] 出版当年五年平均 出版前一年[2014版] 出版后一年[2016版]

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第一作者单位: [1]Huazhong Univ Sci & Technol, Tonsil Med Coll, Union Hosp, Wuhan 430030, Hubei, Peoples R China
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