Chen Ming-hua, Wu Ye-xiang, Xu Yan-ni, Yu Li-yan, Hong Bin, Jiang Wei, Si Shu-yi
Zhongguo Zhong Yao Za Zhi. 2015 May;40(9):1751-4.
By using a cell-based high throughput screening model for the CLA-1 up-regulator, Streptomyces 203909 was found to produce up-regulator of CLA-1. A novel trichostatin analogue was isolated from the rice fermentation of Streptomyces sp. CPCC 203909by a combination of various chromatographic techniques including column chromatography (CC) over silica gel, flash C18 CC, and reversed-phase HPLC. Its structure was identified as (-)-(R,2E,4Z)-7-[(4'-dimethylamino) phenyl]-4,6-dimethyl-7-oxohepta-2,4-dienoyl-L-glutamine (1) by the spectroscopic and chemical methods, and combination with the CD spectroscopy and Marfey's method. In the prelimi- nary assays, Compound 1 showed cytotoxicity against human embryonic kidney 293 cell line with IC50 value 35.3 [µmol · L(-1).
通过使用基于细胞的CLA-1上调调节剂高通量筛选模型，发现链霉菌203909可产生CLA-1上调调节剂。通过多种色谱技术相结合，包括硅胶柱色谱（CC）、快速C18 CC和反相HPLC，从链霉菌属CPCC 203909的大米发酵物中分离出一种新型曲古抑菌素类似物。通过光谱和化学方法，并结合圆二色光谱和马尔费伊法，确定其结构为(-)-(R,2E,4Z)-7-[(4'-二甲氨基)苯基]-4,6-二甲基-7-氧代庚-2,4-二烯酰-L-谷氨酰胺(1)。在初步试验中，化合物1对人胚肾293细胞系显示出细胞毒性，IC50值为35.3[µmol·L(-1)]。
