The antitumor activity of STAT3 target inhibitor Bt354 andmolecular mechanism of anti-prostate cancer
10.16438/j.0513-4870.2019-0668
- VernacularTitle:STAT3靶点抑制剂Bt354抗前列腺癌作用及其分子机制研究
- Author:
Yu-chen WANG
1
;
Yue CHEN
1
;
Ming JI
1
;
Ni-na XUE
1
;
Xiao-guang CHEN
1
Author Information
1. State Key Laboratory of Bioactive Substances and Functions of Natural Medicines/Beijing Key Laboratory of Non-clinical Drug Metabolism and PK/PD Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:Research Article
- Keywords:
Bt354;
prostate cancer;
signal transducer and activator of transcription 3;
apoptosis;
inhibitor
- From:
Acta Pharmaceutica Sinica
2019;54(10):1851-1857
- CountryChina
- Language:Chinese
-
Abstract:
Signal transducer and activator of transcription 3 (STAT3) was found in an abnormal constitutively active status in certain cancer tissues, and under these circumstances the interruption of STAT3 signaling pathway was proposed with the potential anti-cancer efficacy. In this study, our previous reported STAT3 inhibitor Bt354 can inhibit tumor growth in DU145 xenograft mice without affecting body weight. In groups treated with Bt354, the inhibition rate of tumor weight was 58.8%, 62.7% and 73.5% in 10, 20, 40 mg·kg-1 group, respectively. Particularly, the number of Ki 67 positive cells in the tumor sections was significantly decreased in Bt354 groups. Furthermore, Bt354 inhibited the nuclear translocation of STAT3 and consequently induced cell growth inhibition, apoptosis in DU145 cells. These findings suggest that Bt354 may be a potent anticancer agent for STAT3 activated prostate cancer cells. Procedures for animal study were performed with approval of the Animal Care and Use Committee of the Chinese Academy of Medical Sciences and Peking Union Medical College.
