Tsukamoto Sachiko, Yoshida Takushi, Hosono Hidetaka, Ohta Tomihisa, Yokosawa Hideyoshi
Graduate School of Natural Science and Technology, Kanazawa University, Kanazawa 920-1192, Japan.
Bioorg Med Chem Lett. 2006 Jan 1;16(1):69-71. doi: 10.1016/j.bmcl.2005.09.052. Epub 2005 Oct 21.
A new inhibitor of p53-HDM2 interaction was isolated from a culture of marine-derived fungus, Arthrinium sp. The structure was identified to be (-)-hexylitaconic acid (1) by spectroscopic analysis. The inhibition of p53-HDM2 binding was tested by the ELISA method, and 1 inhibited the binding with an IC(50) value of 50 microg/mL. Although a number of synthetic inhibitors of p53-HDM2 interaction have been reported so far, 1 is the second inhibitor isolated from natural resources.
从海洋来源的真菌节菱孢属（Arthrinium sp.）培养物中分离出一种新型的p53-HDM2相互作用抑制剂。通过光谱分析确定其结构为（-）-己基衣康酸（1）。采用酶联免疫吸附测定（ELISA）法检测了其对p53-HDM2结合的抑制作用，化合物1对该结合具有抑制作用，半数抑制浓度（IC50）值为50μg/mL。尽管迄今为止已报道了许多p53-HDM2相互作用的合成抑制剂，但化合物1是从自然资源中分离得到的第二种抑制剂。
