Melis G B, Paoletti A M, Cagnacci A, Bufalino L, Spinetti A, Gambacciani M, Fioretti P
Istituto di Ginecologia Ostetricia e Fisiopatologia della Riproduzione Umana, University of Cagliari, Italy.
J Endocrinol Invest. 1992 Nov;15(10):755-61. doi: 10.1007/BF03347647.
Estrogen replacement therapy (ERT) has been demonstrated to prevent osteoporosis in postmenopausal women (PMW). However, several contraindications exist for ERT and many PMW cannot be treated. It has also been shown that too low doses of ERT are able to exert therapeutical effects on some climacteric symptoms but not on bone and compounds exerting synergic actions with ERT on bone without effects on other organs could be useful. The isoflavone derivative, ipriflavone, seems to have this effect but data are lacking on its endocrine effect in humans; thus, this study was undertaken to clarify in PMW whether ipriflavone exerts estrogenic activity. Evaluation of LH and FSH secretion during a 24-h period was performed in a group of 15 PMW after a single oral dose of 600 or 1,000 mg of ipriflavone or placebo, and after 7, 14 and 21 days of oral treatment with ipriflavone 600 mg and 1,000 mg/daily, administered in three divided doses. LH secretion was also evaluated during naloxone infusion before and after 21 days of ipriflavone, placebo or conjugated estrogen treatment (0.625 mg/day; CE). LH response to NAL treatment was absent during ipriflavone and placebo such as it was observed before treatments. By contrast, a significant increase of LH plasma levels was measured during naloxone infusion in CE-treated women. This result demonstrates that ipriflavone is unable to exert the same effects that estrogens do in PMW. In addition, no changes like in placebo group were seen on vaginal cytology in this group of subjects after 21 days, whereas a significant increase of superficial vaginal cells was observed after 21 days of CE treatment.(ABSTRACT TRUNCATED AT 250 WORDS)
雌激素替代疗法(ERT)已被证明可预防绝经后妇女(PMW)的骨质疏松症。然而,ERT存在一些禁忌症,许多PMW无法接受治疗。也有研究表明,低剂量的ERT能够对某些更年期症状产生治疗作用,但对骨骼无作用,而与ERT在骨骼上具有协同作用且对其他器官无影响的化合物可能会有用。异黄酮衍生物依普黄酮似乎具有这种作用,但缺乏其对人体内分泌作用的数据;因此,本研究旨在阐明依普黄酮在PMW中是否具有雌激素活性。在一组15名PMW中,单次口服600或1000毫克依普黄酮或安慰剂后,以及在每天分三次服用600毫克和1000毫克依普黄酮进行口服治疗7、14和21天后,对24小时内的促黄体生成素(LH)和促卵泡生成素(FSH)分泌进行评估。在依普黄酮、安慰剂或共轭雌激素治疗(0.625毫克/天;CE)21天前后,在输注纳洛酮期间也对LH分泌进行了评估。在依普黄酮和安慰剂治疗期间,对纳洛酮治疗的LH反应与治疗前一样不存在。相比之下,在接受CE治疗的女性中,输注纳洛酮期间测得LH血浆水平显著升高。该结果表明,依普黄酮在PMW中无法发挥与雌激素相同的作用。此外,在这组受试者中,21天后阴道细胞学检查未见如安慰剂组那样的变化,而CE治疗21天后观察到阴道表层细胞显著增加。(摘要截短至250字)