济南游动放线菌CPCC 200056产生的3-去甲创新霉素发现与鉴定  

Identification of 3-demethylchuangxinmycin from Actinoplanes tsinanensis CPCC 200056

作　　者：左利杰 赵薇 江志波 江冰娅 李书芬 刘红宇 余利岩 洪斌 胡辛欣 游雪甫 武临专 

机构地区：[1]中国医学科学院、北京协和医学院医药生物技术研究所,卫计委抗生素生物工程重点实验室,北京100050

出　　处：《药学学报》2016年第1期105-109,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81321004);协和青年科研基金资助项目(33320140156);国家微生物资源基础平台资助项目(NIMR-2015-3)

摘　　要：创新霉素是我国科学家于20世纪70年代从游动放线菌中发现的一个具有含氮、含硫杂环新骨架的抗生素,曾作为抗菌药物进行了应用开发等研究。本研究采用ISP2固体培养基对创新霉素产生菌——济南游动放线菌CPCC 200056进行了发酵培养、乙酸乙酯萃取、TLC和LC-MS分析,发现了第一个天然的创新霉素类似物组分。经分离纯化和NMR解析,确定该类似物为3-去甲创新霉素(3-demethylchuangxinmycin),为新天然产物。与创新霉素相比,3-去甲创新霉素的抗菌活性比创新霉素显著降低。3-去甲创新霉素的发现不仅丰富了对创新霉素构效关系的认识,而且为研究创新霉素生物合成机制提供了线索。Chuangxinmycin（CM） from Actinoplanes tsinanensis was an antibiotic discovered by Chinese scientists about 40 years ago. It contains a new heterocyclic system of indole fused with dihydrothiopyran, whose biosynthetic mechanism remains unclear. CM is used as an oral medicine in the treatment of bacterial infections in China. The simple structure makes CM as an attractive candidate of structure modification for improvement of antibacterial activity. Recently, we analyzed the secondary metabolites of Actinoplanes tsinanensis CPCC 200056, a CM producing strain, as a natural CM analogue. We discovered the first natural CM analogue 3-demethylchuangxinmycin（DCM） as a new natural product. Compared to CM, DCM exhibited a much weaker activity in the inhibition of the bacterial strains tested. The finding provides valuable information for the structure-activity relationship in the biosynthesis of CM.

关 键 词：3-去甲创新霉素 创新霉素 济南游动放线菌CPCC 200056 

分 类 号：Q939.9[生物学—微生物学]