首页> 外国专利> Pharmaceutical composition for preventing and treating for gallstone or cholecystitis containing with Carfilzomib as active ingredient

Pharmaceutical composition for preventing and treating for gallstone or cholecystitis containing with Carfilzomib as active ingredient

机译:含有卡非佐米作为有效成分的预防和治疗胆结石或胆囊炎的药物组合物

摘要

The present invention relates to a pharmaceutical composition for the prevention or treatment of gallstone disease containing carfilzomib or a pharmaceutically acceptable salt thereof as an active ingredient. In the present invention, carfilzomib inhibits gallstone formation in a high cholesterol diet-induced rats, reduces gene expression of SREBP-2 and HMGCR involved in cholesterol synthesis, and inhibits CYP7A1, CYP7B1 , CYP27A1, and CYP8B1, and cholesterol secretion of cholesterol, as well as ABCG5 and ABCG8 gene expression. Furthermore, it was confirmed that expression of SHP, FXR and PXR was inhibited and protein phosphorylation of JNK and ERK was increased. The above-mentioned calfirazomib inhibits the production of cholesterol and inhibits the secretion of bile into bile, and thus a composition containing calfirazomib as an active ingredient can be usefully used for prevention or treatment of gallstone disease.
机译:本发明涉及用于预防或治疗胆结石疾病的药物组合物,其含有卡非佐米或其药学上可接受的盐作为活性成分。在本发明中,卡非佐米抑制高胆固醇饮食诱导的大鼠的胆结石形成,降低参与胆固醇合成的SREBP-2和HMGCR的基因表达,并抑制CYP7A1,CYP7B1,CYP27A1和CYP8B1以及胆固醇的胆固醇分泌。以及ABCG5和ABCG8基因表达。此外,证实了SHP,FXR和PXR的表达被抑制并且JNK和ERK的蛋白质磷酸化增加。上述卡非拉佐米抑制胆固醇的产生并抑制胆汁向胆汁的分泌,因此含有卡非拉佐姆作为有效成分的组合物可有效地用于预防或治疗胆结石病。

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