2. Academic Validation
  3. Biotransformation of Betulonic Acid by the Fungus Rhizopus arrhizus CGMCC 3.868 and Antineuroinflammatory Activity of the Biotransformation Products

Biotransformation of Betulonic Acid by the Fungus Rhizopus arrhizus CGMCC 3.868 and Antineuroinflammatory Activity of the Biotransformation Products

  • J Nat Prod. 2021 Oct 22;84(10):2664-2674. doi: 10.1021/acs.jnatprod.1c00480.
Kai-Nan Song 1,  You-Jia Lu 1,  Cheng-Jiao Chu 1,  Yan-Ni Wu 1,  Hui-Lian Huang 2,  Bo-Yi Fan 1,  Guang-Tong Chen 1
Affiliations

Affiliations

  • 1 School of Pharmacy, Nantong University, 19 Qixiu Road, Nantong, Jiangsu 226001, People's Republic of China.
  • 2 Key Laboratory of Modern Preparation of TCM, Jiangxi University of Traditional Chinese Medicine, 818 Xingwan Road, Nanchang, Jiangxi 330004, People's Republic of China.
PMID: 34546050 DOI: 10.1021/acs.jnatprod.1c00480
Abstract

Biotransformation of betulonic acid (1) by Rhizopus arrhizus CGMCC 3.868 resulted in the production of 16 new (3, 5, 6, and 9-21) and five known compounds. Structures of the new compounds were established by analysis of spectroscopic data. Hydroxylation, acetylation, oxygenation, glycosylation, and addition reactions involved the C-20-C-29 double bond. Antineuroinflammatory activities of the obtained compounds in NO production were tested in lipopolysaccharides-induced BV-2 cells. Compared with the substrate betulonic acid, biotransformation products 3, 8, 9, 14, and 21 exhibited an improved inhibitory effect, with IC50 values of 10.26, 11.09, 5.38, 1.55, and 4.69 μM, lower than that of the positive control, NG-monomethyl-l-arginine.

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