Effects of XW630 on cell proliferation, iNOS activity, and cGMP content in human osteoblast-like cell line TE85.
OBJECTIVE
To study the effects of 2-[3-estrone-N-ethyl-piperazine-methyl] tetracycline (XW630) in human osteoblast-like cell line TE85.


METHODS
[3H]Thymidine incorporation and cell count for cell proliferation, radioimmunoassay for cyclic GMP (cGMP) content, and monitoring the conversion of [3H]arginine for inducible nitric-oxide synthase (iNOS) activity assay.


RESULTS
After treatment with XW630 for 48 h, [3H]thymidine incorporation and cell numbers increased by 62.7% and 96.9%, respectively. NG-monomethyl-L-arginine (L-NMMA, an NOS inhibitor) induced a concentration-dependent inhibitory effect on the proliferation after treatment for 48 h. The inhibitory effect was prevented partially by XW630 (1.0 nmol.L-1). After treatment with XW630 for 12-48 h, iNOS activity and cGMP concentration increased in time-dependent manners.


CONCLUSIONS
XW630 stimulated cell proliferation, enhanced iNOS activity and cGMP content in human osteoblast-like cell line TE85.
Sun
L
L
Department of Pharmacology, Institute of Basic Medical Sciences, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100005, China.
Weng
L L
LL
Zheng
H
H
Liu
J S
JS
D001859:Bone Neoplasms / Q000473:pathology; D002455:Cell Division / Q000187:drug effects; D006152:Cyclic GMP / Q000378:metabolism*; D004966:Estrogens, Conjugated (USP) / Q000494:pharmacology; D004970:Estrone / Q000494:pharmacology; D006801:Humans; D019001:Nitric Oxide Synthase / Q000378:metabolism*; D052247:Nitric Oxide Synthase Type II; D010006:Osteoblasts / Q000166:cytology*; D012516:Osteosarcoma / Q000473:pathology; D010879:Piperazines / Q000494:pharmacology*; D013752:Tetracycline / Q000494:pharmacology*; D013754:Tetracyclines; D014407:Tumor Cells, Cultured
C428143:2-(3-estrone-N-ethyl-piperazine-methyl)tetracycline; D004966:Estrogens, Conjugated (USP); D010879:Piperazines; D013754:Tetracyclines; D004970:Estrone; C496319:NOS2 protein, human; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; D013752:Tetracycline; D006152:Cyclic GMP