甲基莲心碱和异莲心碱对5α-还原酶抑制作用的研究

Inhibitory Effect of Neferine and Isoliensinine on 5α-Reductase

目的:观察甲基莲心碱和异莲心碱对5α-还原酶的抑制作用,为开发5α-还原酶抑制药提供参考依据。方法:设置不同反应管和对照管,将肝脏匀浆液、还原性辅酶Ⅱ(NADPH)、睾酮、待测样品、阳性对照药及缓冲液分别加入到96孔板中,借助酶标仪,测定340 nm处1 h内NADPH的吸光度变化值,空白对照组与实验组比较,计算受试药物对5α-还原酶的抑制率大小。结果:在实验设定的6个浓度梯度(2~40 mg·ml^(-1))中,甲基莲心碱和异莲心碱最佳的抑制作用浓度均为10 mg·ml^(-1),抑制率分别为(25.00±1.030)%和(29.90±2.410)%;与空白组相比,甲基莲心碱和异莲心碱表现出明显的5α-还原酶抑制作用(P<0.05);同浓度(10 mg·ml^(-1))下,甲基莲心碱和异莲心碱对5α-还原酶抑制作用低于阳性对照组(P<0.05);与甲基莲心碱相比,异莲心碱对5α-还原酶抑制作用更显著(P<0.05)。结论:甲基莲心碱和异莲心碱对5α-还原酶有较强抑制作用,在治疗良性前列腺增生疾病方面,有一定的应用前景。

Objective： To compare the inhibitory effect of neferine and isoliensinine on 5α- reductase to provide reference for the development of 5α- reductase inhibitors. Methods： Different reaction tubes and control tubes were prepared,liver was homogenated,and reducing coenzyme Ⅱ（ NADPH）,testosterone,pending test sample,the positive drug and buffer was respectively added into 96-well plates. The change in the absorbance of NADPH at 340 nm in 1h was determined by a microplate reader. Compared the experimental group with the blank control group,the inhibition rate（ I%） of the test drugs against 5α- reductase was calculated. Results： As for the six concentration gradients（2-40 mg·ml（-1）） in the experiments,the best inhibitory concentration of neferine and isoliensinine was10 mg·ml（-1）（I% = 25. 00 ± 1. 030% and 29. 90 ± 2. 410%,respectively）. Compared with the control group,neferine and isoliensinine showed significant inhibition against 5α-reductase（ P 〈0. 05）. Compared with the positive group at the same concentration（10 mg·ml（-1））,the inhibition of neferine and isoliensinine was significantly lower（P 〈0. 05）. The inhibition effect of isoliensinine was relatively better than that of neferine（ P 〈0. 05）. Conclusion： Neferine and isoliensininein have notable inhibitory effect on 5α- reductase,which show certain application prospect in the treatment of prostatic hyperplasia in clinics.