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某些用作抗雄激素的草药的5α-还原酶抑制活性评估。

Evaluation of 5α-reductase inhibitory activity of certain herbs useful as antiandrogens.

作者信息

Nahata A, Dixit V K

机构信息

Department of Pharmaceutical Sciences, Doctor Hari Singh Gour Vishwavidyalaya, Sagar, India.

出版信息

Andrologia. 2014 Aug;46(6):592-601. doi: 10.1111/and.12115. Epub 2013 May 26.

DOI:10.1111/and.12115
PMID:23710567
Abstract

This study demonstrates 5α-reductase inhibitory activity of certain herbs useful in the management of androgenic disorders. Ganoderma lucidum (Curtis) P. Karst (GL), Urtica dioica Linn. (UD), Caesalpinia bonducella Fleming. (CB), Tribulus terrestris Linn. (TT), Pedalium murex Linn. (PM), Sphaeranthus indicus Linn. (SI), Cuscuta reflexa Roxb. (CR), Citrullus colocynthis Schrad. (CC), Benincasa hispida Cogn. (BH), Phyllanthus niruri Linn. (PN) and Echinops echinatus Linn. (EE) were included in the study. Petroleum ether, ethanol and aqueous extracts of these herbs were tested for their 5α-reductase inhibitory activity against the standard 5α-reductase inhibitor, finasteride. A biochemical method to determine the activity of 5α-reductase was used to evaluate the inhibition of different extracts to the enzyme. The optical density (OD) value of each sample was measured continuously with ultraviolet spectrophotometer for the reason that the substrate NADPH has a specific absorbance at 340 nm. As the enzyme 5α-reductase uses NADPH as a substrate, so in the presence of 5α-reductase inhibitor, the NADPH concentration will increase with the function of time. This method thus implicates the activity of 5α-reductase. The method proved to be extremely useful to screen the herbs for their 5α-reductase inhibitory potential. GL, UD, BH, SI and CR came out to be promising candidates for further exploring their antiandrogenic properties.

摘要

本研究证明了某些草药具有5α-还原酶抑制活性,这些草药可用于治疗雄激素紊乱。本研究纳入了灵芝(Curtis)P. Karst(GL)、荨麻(Urtica dioica Linn.,UD)、刺果苏木(Caesalpinia bonducella Fleming.,CB)、刺蒺藜(Tribulus terrestris Linn.,TT)、刺果瓜(Pedalium murex Linn.,PM)、印度香雪球(Sphaeranthus indicus Linn.,SI)、菟丝子(Cuscuta reflexa Roxb.,CR)、药西瓜(Citrullus colocynthis Schrad.,CC)、冬瓜(Benincasa hispida Cogn.,BH)、叶下珠(Phyllanthus niruri Linn.,PN)和蓝刺头(Echinops echinatus Linn.,EE)。对这些草药的石油醚提取物、乙醇提取物和水提取物进行了测试,以检测它们对标准5α-还原酶抑制剂非那雄胺的5α-还原酶抑制活性。采用一种生化方法测定5α-还原酶的活性,以评估不同提取物对该酶的抑制作用。由于底物NADPH在340 nm处有特定吸光度,因此用紫外分光光度计连续测量每个样品的光密度(OD)值。由于5α-还原酶以NADPH为底物,因此在存在5α-还原酶抑制剂的情况下,NADPH浓度会随时间而增加。因此,该方法可反映5α-还原酶的活性。事实证明,该方法对于筛选具有5α-还原酶抑制潜力的草药极为有用。灵芝、荨麻、冬瓜、印度香雪球和菟丝子是进一步探索其抗雄激素特性的有前景的候选草药。

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