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三欣卡辛是一种来源于链霉菌的具有良好抗肿瘤活性的芳香聚酮类天然产物.我们通过对三欣卡辛的发酵和分离条件进行优化,显著地提高了其产量.通过对基因簇中一个酰基转移酶(Trx49)编码基因的敲除,改动了三欣卡辛的生物合成途径,获得了C-4位糖基上O-乙酰基缺失的三欣卡辛类似物1.体外细胞毒性测试考察糖基上的O-乙酰基修饰缺失对三欣卡辛的影响,发现化合物1的生物活性比三欣卡辛A有所降低,但仍具有IC50为4.86 nmol?L-1的优异抗肿瘤细胞活性.
Three Xin Cassassin is a kind of aromatic polyketone natural product with good antitumor activity derived from Streptomyces.We optimized the fermentation and separation conditions of the three Xin Cassassin significantly increased its yield.By gene Knockout of an acyltransferase (Trx49) -coding gene in the cluster altered the biosynthetic pathway of the threexinxin to obtain an oxyacetylcarnate analogue of C-4 at the C-4 position.1 In vitro Cytotoxicity test The influence of O-acetyl modification on glycosyl group on the activity of cinchocardix was investigated. The biological activity of compound 1 was found to be lower than that of cinchucaine A. However, IC50 was 4.86 nmol? L-1 Excellent anti-tumor cell activity.