Re G, Badino P, Odore R, Vigo D, Bonabello A, Rabino S, Capello F, Bruzzese T
Department of Animal Pathology, Division of Pharmacology & Toxicology, University of Torino, via Leonardo da Vinci 44, I-10095 Grugliasco (TO), Italia.
Pharmacol Res. 2001 Aug;44(2):141-7. doi: 10.1006/phrs.2001.0846.
The effects induced by oral administration of 0, 5 and 20 mg of meparticin kg(-1)of body weight for 28 days (group 1, 2 and 3, respectively) upon prostatic estrogen, androgen, alpha(1)- and beta-adrenergic receptor concentrations and on estradiol and testosterone serum levels in adult male rats were studied. The effects produced by mepartricin treatments on the weight and dimension of the gland were investigated. Both mepartricin dosages induced significant decreases (P< 0.05) of the absolute and relative weights and of the dimensions of the prostate. A significant dose-dependent decrease (P< 0.05) in estradiol serum levels was observed in treated rats, whereas no significant modifications were found in testosterone serum levels. As far as prostatic steroid receptor concentrations were concerned, a significant (P< 0.05) decrease in estrogen receptor number was observed in both treated groups, whilst a significant increase (P< 0.05) of androgen receptor concentrations was recorded only in rats treated with 20 mg mepartricin kg(-1). Conversely, a dose-dependent up-regulation of both prostatic alpha(1)- and beta-AR was found. Data obtained suggest that the prostatic alpha(1)-AR expression may be strongly influenced by estrogen deprivation (mepartricin treatment), therefore the combination of estrogen suppression (mepartricin) and adrenergic suppression (alpha(1)-AR blockers) may be suggested as a possible pharmacotherapeutic strategy for the treatment of benign prostatic hyperplasia.
研究了成年雄性大鼠口服0、5和20毫克/千克体重的美帕曲星,持续28天(分别为第1、2和3组)后,对前列腺雌激素、雄激素、α1和β肾上腺素能受体浓度以及雌二醇和睾酮血清水平的影响。研究了美帕曲星处理对前列腺重量和尺寸的影响。两种美帕曲星剂量均导致前列腺绝对重量、相对重量和尺寸显著降低(P<0.05)。在处理的大鼠中观察到雌二醇血清水平显著的剂量依赖性降低(P<0.05),而睾酮血清水平未发现显著变化。就前列腺类固醇受体浓度而言,两个处理组的雌激素受体数量均显著降低(P<0.05),而仅在接受20毫克/千克体重美帕曲星处理的大鼠中记录到雄激素受体浓度显著增加(P<0.05)。相反,发现前列腺α1和β肾上腺素能受体均呈剂量依赖性上调。获得的数据表明,前列腺α1肾上腺素能受体表达可能受雌激素剥夺(美帕曲星处理)的强烈影响,因此,雌激素抑制(美帕曲星)和肾上腺素能抑制(α1肾上腺素能受体阻滞剂)的联合应用可能被建议作为治疗良性前列腺增生的一种可能的药物治疗策略。