This invention relates to methods of reversing and inhibiting liver fibrosis and hepatitis using a small indolinone molecule Hesperadin and related compounds. Methods of identifying such agents and using them to inhibit the expression of collagens and ECM proteins including MMPs and TIMPs in purified hepatic stellate cells are provided. In vivo data of Hesperadin in inhibiting induced collagen production are presented. This method of specifically targeting drugs to hepatic stellate cells in vivo, provides a novel therapy for liver diseases.
本发明涉及使用小
吲哚啉酮分子 Hesperadin 和相关化合物逆转和抑制肝纤维化和肝炎的方法。本发明提供了鉴定此类制剂并使用它们抑制胶原和
ECM 蛋白(包括纯化肝星状细胞中的
MMPs 和 TIMPs)表达的方法。介绍了 Hesperadin 抑制诱导
胶原蛋白生成的体内数据。这种在体内将药物特异性靶向肝星状细胞的方法为治疗肝病提供了一种新的疗法。