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Abstract

Volume 7, Issue 4 (July 2005) 7, 389–393; 10.1111/j.1745-7262.2005.00072.x

Contragestazol (DL111-IT) inhibits proliferation of human an-drogen-independent prostate cancer cell line PC3 in vitro and in vivo

Qiao-Jun He, Bo Yang, Yi-Jia Lou and Rui-Ying Fang

Department of Pharmacology, College of Pharmaceutical Science, Zhejiang University, Hangzhou 310031, China

Correspondence: Prof. Yi-Jia Lou, Department of Pharmacology, College of Pharmaceutical Science, Zhejiang University, 353 YanAn Road, Hangzhou 310031, China. Tel/Fax: +86-571-8721-7206 E-mail: Yijialou@zju.edu.cn

Received: 2005-01-17 Accepted: 2005-03-18

Abstract

Aim: To evaluate the antiproliferative activity of contragestazol (DL111-IT) on the human prostate cancer cell line PC3 in vitro and in vivo and to elucidate its potential molecular mechanisms.

Methods: The cell killing ability of DL111-IT was measured by the 3-(4,5-dimethylthia-zol,2-yl)-2,5-diphenyltetrazolium bromide (MTT) reagent assay method and the tumor xenograft model. The cell cycle was analyzed by flow cytometry and protein expression, including retinoblastoma (pRb), cyclin-dependent kinase 4 (CDK4) and cyclin D1, was detected by Western blotting.

Results: DL111-IT exhibited high efficiency on cell growth inhibition of the human androgen-independent prostate cancer cell line PC3. The drug concentration that yielded 50 % cell inhibition (IC50 value) was 9.9 mg/mL. In the PC3 tumor xenograft study, DL111-IT (1.25 mg/kg-20.0 mg/kg) given once a day for 10 days significantly inhibited tumor growth, with the inhibition rate ranging from 21 % to 50 %. Flow cytometric analysis indicated that DL111-IT could cause G1 arrest in the PC3 cell line, but not apoptosis. DL111-IT enhanced pRb expression and down-regulated CDK4 and cyclin D1 expression, suggesting that cell cycle regulation might contribute to the anticancer property of DL111-IT.

Conclusion: DL111-IT inhibits the proliferation of human androgen-independent prostate cancer cell line PC3 in vitro and in vivo by a cell cycle regulation pathway.

Keywords: DL111-IT, prostate cancer, pRb, cyclin-dependent kinase 4, cyclin D1, PC3, cell line

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Asian Journal of Andrology CN 31-1795/R ISSN 1008-682X  Copyright © 2023  Shanghai Materia Medica, Chinese Academy of Sciences.  All rights reserved.