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

Biotransformation of betulonic acid (1) by Rhizopus arrhizusCGMCC 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 21exhibited an improved inhibitory effect, with IC50values of 10.26, 11.09, 5.38, 1.55, and 4.69 μM, lower than that of the positive control, NG-monomethyl-l-arginine.