Microbial transformation of glycyrrhetinic acid and potent neural anti-inflammatory activity of the metabolites  

作　　者：Yuan Ma Ji-Mei Liu Ri-Dao Chen Xi-Qiang An Jun-Gui Dai 

机构地区：[1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & PekingUnion Medical College, Beijing 100050, China [2]Xinjiang Institute of Materia Medica, Urumqi 830004, China [3]Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences & PekingUnion Medical College, Beijing 100050, China

出　　处：《Chinese Chemical Letters》2017年第6期1200-1204,共5页中国化学快报（英文版）

摘　　要：The microbial transformation of glycyrrhetinic acid（1） by Cunninghamella blakesleana CGMCC 3.970 led to the production of five new metabolites（2-6）.The structures of the metabolites were determined by extensive spectroscopic（HR-ESIMS,1D and 2D NMR） data analyses.The involved reactions exhibited specific hydroxylations at C-24,C-7,and C-15,and oxidation at C-3.Moreover,compounds 2,5,and 6showed significant neural anti-inflammatory activity by inhibiting lipopolysaccharide-induced NO production in mouse microglia BV2 cells with IC（50） values of 0.76,0.94,and 0.16μmol/L,respectively.The microbial transformation of glycyrrhetinic acid（1） by Cunninghamella blakesleana CGMCC 3.970 led to the production of five new metabolites（2-6）.The structures of the metabolites were determined by extensive spectroscopic（HR-ESIMS,1D and 2D NMR） data analyses.The involved reactions exhibited specific hydroxylations at C-24,C-7,and C-15,and oxidation at C-3.Moreover,compounds 2,5,and 6showed significant neural anti-inflammatory activity by inhibiting lipopolysaccharide-induced NO production in mouse microglia BV2 cells with IC（50） values of 0.76,0.94,and 0.16μmol/L,respectively.

关 键 词：Glycyrrhetinic acid Microbial transformation Anti-inflammatory activity Cunninghamella blakesleana Triterpenoid 

分 类 号：TQ460.1[化学工程—制药化工]