[Piperazinyl estrone prevents bone loss in ovariectomized rats].
OBJECTIVE
To determine the effect of piperazinyl estrone, a new estrogen derivative, on bone turnover, bone mass and uteri in ovariectomized rats.


METHODS
Female Sprague-Dawley rats were ovariectomized (OVX) or sham operated (sham) at the age of 3 months and treated with estrone (E) at 0.75 mg.kg-1.d-1, or with piperazinyl estrone (P-E) at 1 or 10 mg.kg-1.d-1, orally, for 3 months. At the time of death, the uterine weight was measured. Bone histomorphometric analysis of proximal tibial metaphyses (PTM) was performed in undecalcified sections.


RESULTS
Bone histomorphometric data showed that the percent trabecular area (% Tb.Ar) of OVX rats with bone high turnover was significantly decreased. The uteri were atrophied. The percent trabecular area (% Tb.Ar) of estrone treated group was increased in decreasing bone turnover manner. But the size and weight of uteri in this group were increased vs OVX group. The bone loss induced by OVX was preserved by P-E treatment, but the mechanism of maintaining bone is different from that of E-treated rats. P-E treatment in low dose did not decrease any bone formation indices, such as percent labeling perimeter, bone formation rate per bone volume (BFR/BV), except bone mineral apposition rate (MAR) compared with E-treated group, and maintained them at OVX level. The uteri were found to be in atrophy compared with the match dose (0.75 mg) of E-treated OVX rats. But rats treated with high dose of P-E showed the same change like E-treated group.


CONCLUSIONS
The finding of this study shows that lower dosage of piperazinyl estrone has effect on preventing the bone losses in OVX rats, while the bone formation and the uterus are not affected, thus supporting the hypothesis that piperazinyl estrone has the potential to prevent postmenopausal bone loss in women with less side effects.
Li
Qing-nan
QN
Institute of Biomedical Engineering, West China University of Medical Science, Chengdu 610041, China.
Weng
Ling-ling
LL
Huang
Lian-fang
LF
Hu
Bin
B
Chen
Huai-qing
HQ
Zheng
Hu
H
D000818:Animals; D001284:Atrophy / Q000517:prevention & control; D015519:Bone Density; D045166:Estradiol Congeners / Q000494:pharmacology / Q000627:therapeutic use*; D004970:Estrone / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D009929:Organ Size / Q000187:drug effects; D010012:Osteogenesis / Q000187:drug effects*; D010024:Osteoporosis / Q000517:prevention & control*; D010052:Ovariectomy; D051381:Rats; D017207:Rats, Sprague-Dawley; D014599:Uterus / Q000473:pathology
D045166:Estradiol Congeners; C483802:piperazinyl estrone; D004970:Estrone