Aversa Antonio, Fittipaldi Simona, Francomano Davide, Bimonte Viviana M, Greco Emanuela A, Crescioli Clara, Di Luigi Luigi, Lenzi Andrea, Migliaccio Silvia
Department of Experimental and Clinical Medicine, Magna Græcia University, Catanzaro, Italy.
IRCCS SDN, Napoli, Italy.
Endocrine. 2017 Jun;56(3):639-648. doi: 10.1007/s12020-016-1208-y. Epub 2017 Jan 30.
Phosphodiesterase type-5 inhibitor administration in diabetic men with erectile dysfunction (ED) is associated with reduced waist circumference. We evaluated potential effects of daily tadalafil administration on body composition and investigated its possible mechanism(s) of action in CC skeletal muscle cells in vitro.
Forty-three men on stable caloric intake (mean age 48.5 ± 7; BMI 25.5 ± 0.9 kg/m) complaining mild ED and/or low urinary tract symptoms (LUTS) were randomly assigned to receive tadalafil (TAD) 5 mg/daily (once-a-day=OAD-TAD; n = 23) or 20 mg on-demand (on-demand=OD-TAD; n = 20) for 2 months. Primary outcomes were variations of body composition measured by Dual-energy X-ray absorptiometry; secondary outcomes were ED/LUTS questionnaire scores along with hormone (testosterone, estradiol, insulin) and endothelial function (Endopat2000) variations.
OAD-TAD increased abdominal lean mass (p < 0.01) that returned to baseline after 2 months withdrawal. LUTS scores improved (p<0.01) in OD-TAD while ED scores improved (p < 0.01) in both groups. We found significant improvements in endothelial function (p < 0.05) that directly correlated with serum insulin (p < 0.01; r = 0.3641) and inversely correlated with estradiol levels (p < 0.01; r = 0.3655) even when corrected for potential confounders. Exposure of CC cells upon increasing tadalafil concentrations (10 to 10 M) increased total androgen receptor mRNA and protein expression as well as myogenin protein expression after 24 and 72 h (2.8 ± 0.4-fold and 1.4 ± 0.02-fold vs. control, respectively, p < 0.05).
Daily tadalafil improved lean mass content in non-obese men probably via enhanced insulin secretion, estradiol reduction, and improvement of endothelial function in vivo. The in vitro increased myogenin and androgen receptor protein expression in skeletal muscle cells suggests a translational action of phosphodiesterase type-5 on this receptor.
在患有勃起功能障碍(ED)的糖尿病男性中给予5型磷酸二酯酶抑制剂与腰围减小有关。我们评估了每日服用他达拉非对身体成分的潜在影响,并在体外研究了其在CC骨骼肌细胞中的可能作用机制。
43名热量摄入稳定(平均年龄48.5±7岁;体重指数25.5±0.9kg/m²)、主诉轻度ED和/或下尿路症状(LUTS)的男性被随机分配接受他达拉非(TAD)5mg/每日(每日一次=OAD-TAD;n=23)或按需服用20mg(按需服用=OD-TAD;n=20),持续2个月。主要结局是通过双能X线吸收法测量的身体成分变化;次要结局是ED/LUTS问卷评分以及激素(睾酮、雌二醇、胰岛素)和内皮功能(Endopat2000)的变化。
OAD-TAD增加了腹部瘦体重(p<0.01),在停药2个月后恢复到基线水平。OD-TAD组的LUTS评分改善(p<0.01),而两组的ED评分均改善(p<0.01)。我们发现内皮功能有显著改善(p<0.05),即使校正潜在混杂因素后,其与血清胰岛素直接相关(p<0.01;r=0.3641),与雌二醇水平呈负相关(p<0.01;r=0.3655)。在增加他达拉非浓度(10至10⁻⁶M)后,CC细胞暴露24小时和72小时后,总雄激素受体mRNA和蛋白表达以及生肌调节因子蛋白表达增加(分别为对照组的2.8±0.4倍和1.4±0.02倍,p<0.05)。
每日服用他达拉非可能通过增强胰岛素分泌、降低雌二醇和改善体内内皮功能,改善非肥胖男性的瘦体重含量。体外骨骼肌细胞中生肌调节因子和雄激素受体蛋白表达增加表明5型磷酸二酯酶对该受体具有转化作用。