Discovery of tanshinone derivatives with anti-MRSA activity via targeted bio-transformation  

作　　者：Wenni He Miaomiao Liu Pei Huang Wael M.Abdel-Mageed Jianying Han Jeramie D.Watrous Don D.Nguyen Wenzhao Wang Fuhang Song Huanqin Dai Jingyu Zhang Ronald J.Quinn Tanja Grkovi Houwei Luo Lixin Zhang Xueting Liu 

机构地区：[1]Key Laboratory of Pathogenic Microbiology and Immunology,Institute of Microbiology,Chinese Academy of Sciences,Beijing 100101,China [2]Department of Chemistry&Biochemistry,University of California San Diego,La Jolla,CA 92093,United States [3]Department of Pharmacognosy,College of Pharmacy,King Saud University,Riyadh 11451,Saudi Arabia [4]Department of Pharmacognosy,Faculty of Pharmacy,Assiut University,Assiut 71526,Egypt [5]Department of Natural Products,China Pharmaceutical University,Nanjing 210009,China [6]Graduate University of Chinese Academy of Sciences,Beijing 100049,China [7]State Key Laboratory of Mycology,Institute of Microbiology,Chinese Academy of Sciences,Beijing,China [8]Eskitis Institute,Griffith University,Brisbane,QLD 4111,Australia

出　　处：《Synthetic and Systems Biotechnology》2016年第3期187-194,共8页合成和系统生物技术（英文）

基　　金：the National Program on Key Basic Research Project(973 program,2013CB734000);by grants from the China Ocean Mineral Resources R&D Association(DY125-15-T-07);the National Natural Science Foundation of China(81573341,81102369,81302678,31430002,31400090,31320103911,31125002);the Ministry of Science and Technology of China(2013ZX10005004-005 and 2011ZX09102-011-11);the European Union's Seventh Framework Programme(FP7/2007e2013)under grant agreement no.312184.

摘　　要：Two potent anti-MRSA tanshinone glycosides(1 and 2)were discovered by targeted microbial biotransformation,along with rapid identification via MS/MS networking.Serial reactions including dehydrogenation,demethylations,reduction,glycosylation and methylation have been observed after incubation of tanshinone IIA and fungus Mucor rouxianus AS 3.3447.In addition,tanshinosides B(2)showed potent activities against serial clinical isolates of oxacillin-resistant Staphylococcus aureus with MIC values of 0.78 mg/mL.This is the first study that shows a significant increase in the level and activities of tanshinone glycosides relative to the substrate tanshinone IIA.

关 键 词：BIOTRANSFORMATION GLYCOSYLATION Tanshinone IIA Mucor rouxianus 

分 类 号：O62[理学—有机化学]