Effects of 2-[3-estrone-N-ethyl-piperazine-methyl]tetracycline (XW630) on osteoporosis in ovariectomized rats

Acta Pharmacol Sin. 2000 Mar;21(3):200-4.

Abstract

Aim: To study the effects of 2-[3-estrone-N-ethyl-piperazine-methyl]tetracycline (XW630) on experimental osteoporosis in ovariectomized (OVX) rats.

Methods: Serum estradiol (E2) content and bone 1-carboxyglutamic acid-containing protein (BGP) content were measured by radioimmunoassay. With undecalcified bone section and tetracycline intraperitoneal labeling, the bone static and dynamic data were studied in right femur samples.

Results: After treatment with XW630 2.5 mg.kg-1, serum BGP content increased by 75.7% but there was no change in serum E2 content and uterus weight compared with OVX rats. Compared with OVX rats, the static data of trabecular bone volume/total tissue volume, trabecular bone volume/sponge bone volume, and mean trabecular plate density were enhanced after treatment with XW630 for 13 wk. The dynamic data of single-labeled surface, double-labeled surface, trabecular osteoid surface, and bone formation rate in tissue level in XW630 group were increased and osteoid maturation period was shortened.

Conclusion: XW630 enhanced bone activation frequency and increased trabecular connectivity, stability, and strength. XW630 stimulated bone formation and inhibited bone resorption with no effect on reproductive system.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Estradiol / blood
  • Estrogens, Conjugated (USP) / pharmacology*
  • Estrone / pharmacology
  • Female
  • Femur / drug effects*
  • Humans
  • Osteoporosis, Postmenopausal / metabolism*
  • Ovariectomy
  • Piperazines / pharmacology*
  • Rats
  • Rats, Wistar
  • Tetracycline / pharmacology*
  • Tetracyclines
  • Uterus / drug effects

Substances

  • 2-(3-estrone-N-ethyl-piperazine-methyl)tetracycline
  • Estrogens, Conjugated (USP)
  • Piperazines
  • Tetracyclines
  • Estrone
  • Estradiol
  • Tetracycline