Hu Zhijuan, Qin Lele, Wang Qianqian, Ding Wanjing, Chen Zhen, Ma Zhongjun
a Ocean College , Zhejiang University , Hangzhou , P.R. China.
b Zhejiang Key Laboratory of Gastro-Intestinal Pathophysiology , Zhejiang Hospital of Traditional Chinese Medicine , Hangzhou , P.R. China.
Nat Prod Res. 2016 Nov;30(22):2551-2558. doi: 10.1080/14786419.2015.1120730. Epub 2016 Jan 4.
Vineomycin A (1) and B (2) were isolated from the culture broth of marine actinomycete Streptomyces sp. A6H. Five hydrolysis products were obtained by rational hydrolysis and methanolysis of the fermentation extract. Their structures were characterised as aquayamycin (3), vineomycinone B (4), 9-C--olivosyltetrangulol (5), 7-O-methylgaltamycinone (6) and vineomycinone B methyl ester (7). In addition to these compounds, two ester derivatives, vineolactone A (8) and vineomycinone B benzyl ester (9) of compound 4 were generated semisynthetically. Compound 6 is a new analogue of galtamycinone, while compounds 8 and 9 are new members of vineomycins. Cytotoxic activities and antimicrobial activities were determined for all compounds. The results indicate that only compound 1 showed significant activities with IC value of 0.34 μM against H1975 and MIC value of 4 μg/mL against Staphylococcus aureus.
维诺霉素A（1）和B（2）是从海洋放线菌链霉菌属A6H的培养液中分离得到的。通过对发酵提取物进行合理水解和甲醇解得到了5种水解产物。它们的结构被鉴定为水涯霉素（3）、维诺霉素酮B（4）、9-C-α-橄榄糖基四棱菌素（5）、7-O-甲基加耳他霉素酮（6）和维诺霉素酮B甲酯（7）。除了这些化合物外，还通过半合成法制备了化合物4的两种酯衍生物，维诺内酯A（8）和维诺霉素酮B苄酯（9）。化合物6是加耳他霉素酮的新类似物，而化合物8和9是维诺霉素的新成员。测定了所有化合物的细胞毒性活性和抗菌活性。结果表明，只有化合物1表现出显著活性，对H1975的IC值为0.34 μM，对金黄色葡萄球菌的MIC值为4 μg/mL。
