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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. [ABSTRACT FROM AUTHOR]