43-O-(β-D-glucoside)-rapamycin, a microbial conversion product by Bacillus subtilis CGMCC7764

Abstract

Rapamycin is a macrolide antibiotic with antifungal, immunosuppressive, antitumor, and lifespan-extension activities etc. In order to increase its structural diversity, microbial transformation of rapamycin was conducted. More than 3 converted compounds were shown in the microbial conversion culture of rapamycin by Bacillus subtilis CGMCC7764. By extensive NMR and MS spectroscopic analyses, the major compound was identified as 43-O-(β-D-glucoside)-rapamycin. This compound has an inhibitory effect on tumour growth, and its activity is similar to rapamycin.

keywords:

• Rapamycin
• microbial transformation
• Bacillus subtilis CGMCC7764
• glycosylation

Acknowledgments

Financial support from Major National Science and Technology Projects [2020L3016] are gratefully acknowledged.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This work was supported by the Special Foundation for State major Basic Research Program of China (2020L3016).