Microbial transformation of glycyrrhetinic acid and potent neural anti-inflammatory activity of the metabolites |
| |
| Authors: | Yuan Ma Ji-Mei Liu Ri-Dao Chen Xi-Qiang An Jun-Gui Dai |
| |
| Institution: | a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China;
b Xinjiang Institute of Materia Medica, Urumqi 830004, China;
c Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China |
| |
| Abstract: | 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 6 showed significant neural anti-inflammatory activity by inhibiting lipopolysaccharide-induced NO production in mouse microglia BV2 cells with IC50 values of 0.76, 0.94, and 0.16 μmol/L, respectively. |
| |
| Keywords: | Glycyrrhetinic acid Microbial transformation Anti-inflammatory activity Cunninghamella blakesleana Triterpenoid |
| 本文献已被 CNKI 等数据库收录！ |
| 点击此处可从《中国化学快报》浏览原始摘要信息 |
| 点击此处可从《中国化学快报》下载免费的PDF全文 |
|
