2. Academic Validation
  3. New derivatives of ursolic acid through the biotransformation by Bacillus megaterium CGMCC 1.1741 as inhibitors on nitric oxide production

New derivatives of ursolic acid through the biotransformation by Bacillus megaterium CGMCC 1.1741 as inhibitors on nitric oxide production

  • Bioorg Med Chem Lett. 2017 Jun 1;27(11):2575-2578. doi: 10.1016/j.bmcl.2017.03.076.
Chao Zhang 1,  Shao-Hua Xu 1,  Bai-Ling Ma 2,  Wei-Wei Wang 2,  Bo-Yang Yu 2,  Jian Zhang 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
  • 2 Jiangsu Key Laboratory of TCM Evaluation and Translational Research, China Pharmaceutical University, Nanjing, Jiangsu 211198, China.
  • 3 State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China. Electronic address: 1020071849@cpu.edu.cn.
PMID: 28427811 DOI: 10.1016/j.bmcl.2017.03.076
Abstract

Microbial transformation of ursolic acid (1) by Bacillus megaterium CGMCC 1.1741 was investigated and yielded five metabolites identified as 3-oxo-urs-12-en-28-oic acid (2); 1β,11α-dihydroxy-3-oxo-urs-12-en-28-oic acid (3); 1β-hydroxy-3-oxo-urs-12-en-28, 13-lactoe (4); 1β,3β, 11α-trihydroxyurs-12-en-28-oic acid (5) and 1β,11α-dihydroxy-3-oxo-urs-12-en-28-O-β-d-glucopyranoside (6). Metabolites 3, 4, 5 and 6 were new Natural Products. Their nitric oxide (NO) production inhibitory activity was assessed in lipopolysaccharide (LPS) - stimulated RAW 264.7 cells. Compounds 3 and 4 exhibited significant activities with the IC50 values of 1.243 and 1.711μM, respectively. A primary structure-activity relationship was also discussed.

Keywords

Bacillus megaterium CGMCC 1.1741; Microbial transformation; Nitric oxide production; Ursolic acid.

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