This invention discloses the application of the
small molecule compound Z2114502286 in the preparation of drugs for the prevention and treatment of liver-related diseases. This invention reveals for the first time that Z2114502286 is a THBS2-specific
small molecule inhibitor and verifies its feasibility in preventing and treating
liver fibrosis by targeting and inhibiting the THBS2
protein. Through
virtual screening and molecular docking, this compound can directly bind to the THBS2
protein.
In vitro and
in vivo studies show that this compound inhibits THBS2-mediated HSC activation in a concentration- and time-
dependent manner, inhibits ECM deposition in a mouse model of
liver fibrosis, downregulates the expression of
fibrosis-related genes, and alleviates liver
inflammation and
macrophage infiltration. Simultaneously, the targeted
efficacy was verified in a transgenic mouse model specifically expressing human THBS2, demonstrating significant clinical translational value. Furthermore, it exhibits
bioavailability and safety at effective dosages, showing broad clinical application prospects.