Sugiyama M, Kumagai T, Shionoya M, Kimura E, Davies J E
Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Japan.
FEMS Microbiol Lett. 1994 Aug 1;121(1):81-5. doi: 10.1111/j.1574-6968.1994.tb07079.x.
Bleomycin-producing Streptomyces verticillus ATCC15003 possesses a bleomycin acetyltransferase which inactivates the drug in the presence of acetyl coenzyme A. The site of acylation in enzymically prepared acetylbleomycin A2 was determined by nuclear magnetic resonance analysis; the primary amino group of the beta-aminoalanine moiety of bleomycin was acetylated Acetylbleomycin A2 had no detectable antibacterial activity and did not induce in vitro DNA degradation.
产生博来霉素的轮枝链霉菌ATCC15003含有一种博来霉素乙酰转移酶,该酶在乙酰辅酶A存在的情况下会使药物失活。通过核磁共振分析确定了酶促制备的乙酰博来霉素A2中的酰化位点;博来霉素β-氨基丙氨酸部分的伯氨基被乙酰化。乙酰博来霉素A2没有可检测到的抗菌活性,也不会在体外诱导DNA降解。