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

• Published in: Andrologia Vol. 46; no. 6; pp. 592 - 601
• Main Authors: Nahata, A., Dixit, V. K.
• Format: Journal Article
• Language: English
• Published: Germany Blackwell Publishing Ltd 01.08.2014
• Subjects: 3-Oxo-5-alpha-Steroid 4-Dehydrogenase - metabolism; 5-alpha Reductase Inhibitors - pharmacology; 5α-reductase; Androgen Antagonists - pharmacology; antiandrogens; antioxidant activity; Asteraceae; Cucurbitaceae; Drug Evaluation, Preclinical; Humans; in vitro; In Vitro Techniques; Male; NADP - metabolism; NADPH; Plant Extracts - pharmacology; Plants, Medicinal; Prostate - drug effects; Prostate - enzymology; Reishi; Urtica dioica; NADPH; 5α-reductase; antiandrogens; antioxidant activity; in vitro
• ISSN: 0303-4569; 1439-0272
• DOI: 10.1111/and.12115

Summary 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.