Rodríguez-Guzmán Raquel, Radwan Mohamed M, Burandt Charles L, Williamson John S, Ross Samir A
National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677, USA.
Nat Prod Commun. 2010 Sep;5(9):1463-4.
Phytochemical evaluation of Zanthoxylum monophyllum has led to the isolation of the alkaloid 4-methoxy-N-methyl-2-quinolone (1) with a significant activity against methicillin-resistant Staphylococcus aureus (MRSA), with an IC50 value of 1.5 microg/mL. Xenobiotic biotransformation of 1 has been conducted with the general goal of increasing the bioactivity of the compound and contributing new leads for further pharmacological research. Twenty-nine microorganisms were used for screening and two (Aspergillus flavus and Cunninghamella echinulata var. echinulata) were able to transform compound 1 to 4-methoxy-2-quinolone (2). Structural identification of the compounds was based on NMR, IR, and MS data.
对单叶花椒进行植物化学评估后，分离出了生物碱4-甲氧基-N-甲基-2-喹诺酮（1），其对耐甲氧西林金黄色葡萄球菌（MRSA）具有显著活性，IC50值为1.5微克/毫升。对化合物1进行了异生物质生物转化，总体目标是提高该化合物的生物活性，并为进一步的药理学研究提供新的线索。使用了29种微生物进行筛选，其中两种（黄曲霉和刺孢小克银汉霉刺孢变种）能够将化合物1转化为4-甲氧基-2-喹诺酮（2）。化合物的结构鉴定基于核磁共振（NMR）、红外光谱（IR）和质谱（MS）数据。
