Cheng Xiangwei, Zhou Biao, Liu Huazhang, Huo Chao, Ding Wanjing
a College of Chemical Engineering , Zhejiang University of Technology , Hangzhou , China.
b Zhejiang Police College , Hangzhou , China.
Nat Prod Res. 2018 Nov;32(21):2583-2588. doi: 10.1080/14786419.2018.1428595. Epub 2018 Jan 22.
One new indolocarbazole alkaloid, 12-N-methyl-k252c, together with eight known indolocarbazoles were isolated from the rice solid fermentation of the marine-derived Streptomyces sp. A22. Their structures were elucidated on the basis of spectroscopic methods (UV, IR, HRESITOF MS, 1D NMR and 2D NMR). All of these compounds were evaluated for bromodomain-containing protein 4 (BRD4) inhibitory activities and cytotoxic activity assay, respectively. Compounds 4 and 5 showed moderate cytotoxic activity with an IC value of 3.52 and 3.93 μM, respectively. Additionally, compound 1 also was tested for enzyme inhibition activities of protein kinases and showed moderate activity with IC values of 0.91-1.84 μM.
从海洋来源的链霉菌属菌株A22的大米固体发酵物中分离出一种新的吲哚咔唑生物碱12-N-甲基-k252c以及八种已知的吲哚咔唑。基于光谱方法（紫外、红外、高分辨电喷雾电离飞行时间质谱、一维核磁共振和二维核磁共振）阐明了它们的结构。分别对所有这些化合物进行了含溴结构域蛋白4（BRD4）抑制活性和细胞毒性活性测定。化合物4和5表现出中等细胞毒性活性，IC值分别为3.52和3.93 μM。此外，还测试了化合物1对蛋白激酶的酶抑制活性，其表现出中等活性，IC值为0.91 - 1.84 μM。
