Effects of XW630 on cell proliferation, iNOS activity, and cGMP content in human osteoblast-like cell line TE85

Acta Pharmacol Sin. 2000 Mar;21(3):261-4.

Abstract

Aim: 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.

Conclusion: XW630 stimulated cell proliferation, enhanced iNOS activity and cGMP content in human osteoblast-like cell line TE85.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bone Neoplasms / pathology
  • Cell Division / drug effects
  • Cyclic GMP / metabolism*
  • Estrogens, Conjugated (USP) / pharmacology
  • Estrone / pharmacology
  • Humans
  • Nitric Oxide Synthase / metabolism*
  • Nitric Oxide Synthase Type II
  • Osteoblasts / cytology*
  • Osteosarcoma / pathology
  • Piperazines / pharmacology*
  • Tetracycline / pharmacology*
  • Tetracyclines
  • Tumor Cells, Cultured

Substances

  • 2-(3-estrone-N-ethyl-piperazine-methyl)tetracycline
  • Estrogens, Conjugated (USP)
  • Piperazines
  • Tetracyclines
  • Estrone
  • NOS2 protein, human
  • Nitric Oxide Synthase
  • Nitric Oxide Synthase Type II
  • Tetracycline
  • Cyclic GMP