Prenylflavonoids: a new class of non-steroidal phytoestrogen (Part 2). Estrogenic effects of 8-isopentenylnaringenin on bone metabolism.
In order to examine whether 8-isopentenylnaringenin (1), which has been proven to possess estrogen agonist activity in in vitro tests, also produces in vivo estrogenic properties, the effects of 1 on uterus and on bone metabolism were determined in ovariectomized rats. Rats were ovariectomized and treated with 1 at 30 mg/kg/day subcutaneously for two weeks or 17 beta-estradiol at 0.01 mg/kg/day subcutaneously for two weeks. Ovariectomy resulted in an increase in urinary excretion of bone resorption markers (hydroxyproline, pyridinoline and deoxypyridinoline) and a decrease in bone mineral density of the proximal tibia as well as reduced uterine weight. Treatment with 1 or 17 beta-estradiol completely suppressed these ovariectomy-induced bone and uterine changes in a qualitatively similar manner. These results demonstrate that 1 acts as an estrogen agonist in the uterus as well as in bone in vivo.
Miyamoto
M
M
Pharmacology and Molecular Biology Research Laboratories, Sankyo Co., Tokyo, Japan.
Matsushita
Y
Y
Kiyokawa
A
A
Fukuda
C
C
Iijima
Y
Y
Sugano
M
M
Akiyama
T
T
D000596:Amino Acids / Q000652:urine; D000818:Animals; D015415:Biomarkers / Q000652:urine; D015519:Bone Density / Q000187:drug effects*; D001862:Bone Resorption; D004958:Estradiol / Q000494:pharmacology; D004968:Estrogens, Non-Steroidal / Q000494:pharmacology*; D005260:Female; D006909:Hydroxyproline / Q000652:urine; D007529:Isoflavones / Q000494:pharmacology*; D009929:Organ Size / Q000187:drug effects; D010052:Ovariectomy; D048789:Phytoestrogens; D028321:Plant Preparations; D051381:Rats; D017207:Rats, Sprague-Dawley; D013977:Tibia / Q000187:drug effects* / Q000502:physiology; D014599:Uterus / Q000187:drug effects* / Q000502:physiology
C114744:8-isopentenylnaringenin; D000596:Amino Acids; D015415:Biomarkers; D004968:Estrogens, Non-Steroidal; D007529:Isoflavones; D048789:Phytoestrogens; D028321:Plant Preparations; D004958:Estradiol; C015484:pyridinoline; C036020:deoxypyridinoline; D006909:Hydroxyproline