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


CONCLUSIONS
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.
Sun
L
L
Department of Pharmacology, Institute of Basic Medical Sciences, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100005, China.
Qiu
M C
MC
Weng
L L
LL
Zheng
H
H
Liu
J S
JS
D000818:Animals; D004958:Estradiol / Q000097:blood; D004966:Estrogens, Conjugated (USP) / Q000494:pharmacology*; D004970:Estrone / Q000494:pharmacology; D005260:Female; D005269:Femur / Q000187:drug effects*; D006801:Humans; D015663:Osteoporosis, Postmenopausal / Q000378:metabolism*; D010052:Ovariectomy; D010879:Piperazines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013752:Tetracycline / Q000494:pharmacology*; D013754:Tetracyclines; D014599:Uterus / Q000187:drug effects
C428143:2-(3-estrone-N-ethyl-piperazine-methyl)tetracycline; D004966:Estrogens, Conjugated (USP); D010879:Piperazines; D013754:Tetracyclines; D004970:Estrone; D004958:Estradiol; D013752:Tetracycline