The invention provides an application of 2-indolecarboxylic acid in preparation of a
tumor targeted therapy
drug. Through computer-aided
drug design and molecular docking optimization, 2-indolecarboxylic acid shows high
binding energy to an HER2
kinase structural domain. In HER2 positive NCI-N87 gastric
cancer cells, the 2-indolecarboxylic acid significantly inhibits
cell proliferation and induces G0 / G1 phase arrest and
apoptosis. The mechanism research shows that the 2-indoleformic acid can play a role by regulating and controlling the HER2 / Akt / beta-
catenin pathway (
Western blot verification). In an NCI-N87
cell tumor-bearing
nude mouse model, 2-indolecarboxylic acid (15 mg / kg) significantly inhibits
tumor growth, and does not cause obvious
weight loss or organ
toxicity. Immunohistochemical analysis shows that the positive rate of a
tumor tissue proliferation marker Ki-67 in a treatment group is remarkably reduced, and
apoptosis detection shows that the proportion of TUNEL positive cells is remarkably increased, which indicates that 2-indolecarboxylic acid inhibits tumor
cell proliferation and promotes
apoptosis at the same time. The invention provides a
lead compound with clinical transformation potential for HER2
targeted therapy.