Natural Products Research Institute, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
Org Lett. 2013 Apr 19;15(8):1834-7. doi: 10.1021/ol4004417. Epub 2013 Apr 3.
Tripartin (1), a new dichlorinated indanone, was isolated from the culture broth of the Streptomyces sp. associated with a larva of the dung beetle Copris tripartitus Waterhouse. The planar structure of tripartin (1) was identified by the spectroscopic analyses of NMR, mass, UV, and IR data. The structure was confirmed, and the absolute configuration of 1 was determined by X-ray crystallography. Tripartin displayed specific activity as an inhibitor of the histone H3 lysine 9 demethylase KDM4 in HeLa cells.
三叶素(1)是从与蜣螂幼虫Copris tripartitus Waterhouse 相关的链霉菌属培养液中分离得到的一种新型二氯茚酮。通过 NMR、质谱、紫外和红外数据分析对三叶素(1)的平面结构进行了鉴定。通过 X 射线晶体学确定了结构,并确定了 1 的绝对构型。三叶素在 HeLa 细胞中作为组蛋白 H3 赖氨酸 9 去甲基化酶 KDM4 的抑制剂具有特异性活性。