Biotransformation of rosamicin antibiotic into 10,11-dihydrorosamicin with enhanced in vitro antibacterial activity against MRSA.
A biotransformation approach using microbes as biocatalysts can be an efficient tool for the targeted modification of existing antibiotic chemical scaffolds to create previously uncharacterized therapeutic agents. By employing a recombinant Streptomyces venezuelae strain as a microbial catalyst, a reduced macrolide, 10,11-dihydrorosamicin, was created from rosamicin macrolide. Its chemical structure was spectroscopically elucidated, and the new rosamicin analog showed 2-4-fold higher antibacterial activity against two strains of methicillin-resistant Staphylococcus aureus compared with its parent rosamicin. This kind of biocatalytic approach is able to expand existing antibiotic entities and can also provide more diverse therapeutic resources.
Department of Pharmaceutical Engineering, SunMoon University, Asan 336-708, Republic of Korea.
Nguyen Lan
NL
Huong
Nguyen Huu
NH
Hoang
Anil
A
Shrestha
Jae Kyung
JK
Sohng
Yeo Joon
YJ
Yoon
Je Won
JW
Park
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D001711:Biotransformation; D007933:Leucomycins / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D018942:Macrolides / Q000378:metabolism / Q000494:pharmacology; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D013057:Spectrum Analysis; D013302:Streptomyces / Q000378:metabolism*
D000900:Anti-Bacterial Agents; D007933:Leucomycins; D018942:Macrolides; C060286:rosaramicin