Microbial transformation of three bufadienolides by Nocardia sp. and some insight for the cytotoxic structure-activity relationship (SAR).

@article{Zhang2007MicrobialTO,
  title={Microbial transformation of three bufadienolides by Nocardia sp. and some insight for the cytotoxic structure-activity relationship (SAR).},
  author={Jian Feng Zhang and Yang Sun and Ji-Hua Liu and Boyang Yu and Qiang Xu},
  journal={Bioorganic & medicinal chemistry letters},
  year={2007},
  volume={17 22},
  pages={6062-5}
}
Resibufogenin, cinobufagin, and bufalin are cytotoxic steroids isolated from the Chinese drug Chan'su. Biotransformation of these three bufadienolides by Nocardia sp. NRRL 5646 was investigated. Notably, resibufogenin was converted to 3-acetyl 15beta-hydroxyl bufotalin, via an unprecedented 14beta,15beta-epoxy ring cleavage and a regio-selective acetoxylation. This product showed significantly increased cytotoxic activity. The regio-selective acetylation of the 3-OH was also involved in the… CONTINUE READING