Ivermectin and application of derivative thereof

Abstract

The invention discloses ivermectin and application of a derivative thereof, and relates to ivermectin. The ivermectin is a derivative of macrolide abamectin generated by streptomyces, and the ivermectin and the derivative thereof are used for preparing medicines for treating metabolism-related diseases such as mammalian hyperglycemia, insulin resistance, hypertriglyceridemia, hypercholesterolemia, diabetes and obesity, and can be applied to medicines for treating diseases such as farnesol receptor-mediated bile obstruction, gallstone, non-alcoholic fatty liver diseases, atherosclerosis, inflammation and cancer.

Description

Technical field

[0001] The present invention relates to a new and effective ligand of ivermectin (ivermectin) and its derivatives for the Farnesoid X receptor (Farnesoid X receptor, FXR), which is different from antiparasitic drugs, and a new use Methods of design, optimization and synthesis of ivermectin derivatives. Background technique

[0002] Nuclear receptor is a transcription factor activated by ligand. FXR is a very important member of the human body's 48 nuclear receptors, and plays an important regulatory role in major diseases such as metabolism, inflammation, tumors, and related physiological functions. The principle of the pharmacological action mediated by the ligand of FXR is that the ligand recruits various co-activators (or co-inhibitors) to regulate downstream target genes by binding to the ligand binding domain (LBD) of FXR. In the body, bile acids are the endogenous ligands of FXR. The activation of FXR can maintain the normal circulation and homeostasis of ...

Images