Format

Send to

Choose Destination
Acta Pharmacol Sin. 2002 Jul;23(7):631-7.

JTE-522, a selective COX-2 inhibitor, inhibits cell proliferation and induces apoptosis in RL95-2 cells.

Author information

1
Department of Pharmacology, Pharmacy College, Ji-nan University, Guangzhou 510632, China.

Abstract

AIM:

To investigate whether JTE-522 [4-(4-cyclohexyl-2-methyloxazol-5-yl)-2-fluorobenzenesulfonamide], a selective COX-2 inhibitor, can induce apoptosis and inhibit cell proliferation in human endometrial cancer cell line RL95-2 cells and to explore the molecular mechanisms.

METHODS:

[3-(4,5)-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT), DNA ladder, enzyme-linked immunosorbent assay (ELISA), flow cytometry, RT-PCR, and Western blot analysis were employed to investigate effect of JTE-522 on human endometrial cancer cell line RL95-2 cells and the related molecular mechanisms.

RESULTS:

JTE-522 inhibited the growth of RL95-2 cells and induced the apoptosis. Furthermore, it arrested G0/G1 phase and inhibited S phase in RL95-2 cells. JTE-522 inhibited the expressions of COX-2 mRNA, phosphorylated Rb, and CDK4 proteins, while increased the levels of p53, p21, cyclin D1 proteins, and the activity of caspase-3 in RL95-2 cells.

CONCLUSION:

JTE-522 inhibits cell proliferation and induces apoptosis in RL95-2 cells, which may be associated with the activation of caspase-3-like proteases, down-regulation of the expression of COX-2 mRNA, phosphorylated Rb, and CDK4 proteins, and up-regulation of the expressions of p53, p21, and cyclin D1 proteins.

PMID:
12100758
[Indexed for MEDLINE]
Free full text

Supplemental Content

Full text links

Icon for Acta Pharmacologica Sinica
Loading ...
Support Center