卤酶失活突变株来源的具有增强抗菌活性的噻卡霉素同系物。
Tiacumicin Congeners with Improved Antibacterial Activity from a Halogenase-Inactivated Mutant.
机构信息
CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology , Chinese Academy of Sciences , 164 West Xingang Road , Guangzhou 510301 , People's Republic of China.
Institute of Materia Medica , Pharmaceutical College of Henan University , Kaifeng 475004 , People's Republic of China.
出版信息
J Nat Prod. 2018 May 25;81(5):1219-1224. doi: 10.1021/acs.jnatprod.7b00990. Epub 2018 Apr 20.
Tiacumicin B (1, also known as fidaxomicin or difimicin) is a marketed drug for the treatment of Clostridium difficile infections. The biosynthetic pathway of 1 has been studied in Dactylosporangium aurantiacum subsp. hamdenensis NRRL 18085 and has enabled the identification of TiaM as a tailoring dihalogenase. Herein we report the isolation, structure elucidation, and bioactivity evaluation of 14 tiacumicin congeners (including 11 new ones) from the tiaM-inactivated mutant. A new tiacumicin congener, 3, with a propyl group at C-7‴ of the aromatic ring was found to exhibit improved antibacterial activity.
替考拉宁 B（1，也称为非达霉素或地美环素）是一种用于治疗艰难梭菌感染的上市药物。1 的生物合成途径已在 Dactylosporangium aurantiacum subsp. hamdenensis NRRL 18085 中进行了研究，并确定了 TiaM 是一种修饰性二卤化酶。本文报道了来自 tiaM 失活突变体的 14 种替考拉宁类似物（包括 11 种新化合物）的分离、结构阐明和生物活性评价。一种新型替考拉宁类似物 3，其芳香环上的 C-7‴位有一个丙基取代基，表现出改善的抗菌活性。
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