Goswami Sumanta Kumar, Inamdar Mohammed Naseeruddin, Dethe Shekhar M, Gururaj Giligar M, Jamwal Rohitash, Bhaskar Anirban, Mundkinajeddu Deepak, Agarwal Amit
Department of Pharmacology, Al-Ameen College of Pharmacy, Bangalore, 560027, India.
R&D Centre, Natural Remedies Pvt. Ltd., Plot No. 5B, Veerasandra Industrial Area, Bangalore, 560100, India.
Phytother Res. 2016 Jul;30(7):1119-27. doi: 10.1002/ptr.5614. Epub 2016 Mar 28.
Soluble epoxide hydrolase (sEH) inhibitors have been reported to improve penile erection; therefore, sEH could be useful for management of erectile dysfunction. Methanolic and aqueous extracts of 30 Indian medicinal plants were screened for their sEH inhibition potential. Fifteen extracts showed >50% inhibition when screened at 50 µg/mL in sEH inhibition assay. Methanolic extract of Moringa oleifera Lam. (Moringaceae) seeds (MEMO) was most potent with IC50 1.7 ± 0.1 µg/mL and was selected for in vitro studies on isolated rat corpus cavernosum smooth muscle and in vivo sexual behaviour studies on healthy and diabetic rats. Rats were divided into five groups, each containing six animals and treated orally with either water, vehicle (1% Tween-20), MEMO (45 and 90 mg/kg/day for 21 days), and standard drug, sildenafil (5 mg/kg/day for 7 days). An equal number of female rats were used, and the effect of MEMO and sildenafil was compared with that of vehicle. MEMO significantly relaxed isolated rat corpus cavernosum smooth muscle at 0.1-100 µg/mL in vitro and significantly increased (p < 0.05) sexual activity, intracavernous pressure/mean arterial pressure in normal and diabetic rats. The increase in erectile function of rats by MEMO could be because of its sEH inhibitory activity. Copyright © 2016 John Wiley & Sons, Ltd.
据报道,可溶性环氧化物水解酶(sEH)抑制剂可改善阴茎勃起;因此,sEH可能对勃起功能障碍的治疗有用。对30种印度药用植物的甲醇提取物和水提取物进行了sEH抑制潜力筛选。在sEH抑制试验中,当以50μg/mL进行筛选时,15种提取物显示出>50%的抑制率。辣木(辣木科)种子的甲醇提取物(MEMO)最有效,IC50为1.7±0.1μg/mL,并被选用于对离体大鼠海绵体平滑肌的体外研究以及对健康和糖尿病大鼠的体内性行为研究。将大鼠分为五组,每组六只动物,分别口服水、赋形剂(1%吐温-20)、MEMO(45和90mg/kg/天,持续21天)以及标准药物西地那非(5mg/kg/天,持续7天)。使用数量相等的雌性大鼠,并将MEMO和西地那非的效果与赋形剂进行比较。MEMO在体外0.1-100μg/mL时可显著舒张离体大鼠海绵体平滑肌,并显著增加(p<0.05)正常和糖尿病大鼠的性活动、海绵体内压/平均动脉压。MEMO使大鼠勃起功能增强可能是由于其sEH抑制活性。版权所有©2016约翰威立父子有限公司。