Contragestazol (DL111-IT) inhibits proliferation of human androgen-independent prostate cancer cell line PC3 in vitro and in vivo / 亚洲男科学杂志(英文版)
Asian Journal of Andrology
;
(6): 389-393, 2005.
Article
in English
| WPRIM
| ID: wpr-270837
ABSTRACT
<p><b>AIM</b>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.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>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.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Pharmacology
/
Prostatic Neoplasms
/
Transplantation, Heterologous
/
Triazoles
/
In Vitro Techniques
/
Cell Division
/
Resting Phase, Cell Cycle
/
G1 Phase
/
Retinoblastoma Protein
Limits:
Animals
/
Female
/
Humans
/
Male
Language:
English
Journal:
Asian Journal of Andrology
Year:
2005
Type:
Article
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