Somani Gauresh, Kulkarni Chinmay, Shinde Prashant, Shelke Rupesh, Laddha Kirti, Sathaye Sadhana
Department of Pharmaceutical Sciences and Technology, Pharmacology Research Lab II, Mumbai, Maharashtra, India.
Department of Pharmaceutical Sciences and Technology, Medicinal Natural Products Research Laboratory, Mumbai, Maharashtra, India.
J Pharm Bioallied Sci. 2015 Jan-Mar;7(1):32-6. doi: 10.4103/0975-7406.148775.
Alzheimer's disease (AD) has increased at an alarming rate and is now a worldwide health problem. Inhibitors of acetylcholinesterase (AChE) leading to inhibition of acetylcholine breakdown constitute the main therapeutic strategy for AD. Psoralen was investigated as inhibitor of AChE enzyme in an attempt to explore its potential for the management of AD.
Psoralen was isolated from powdered Psoralea corylifolia fruits. AChE enzyme inhibitory activity of different concentrations of psoralen was investigated by use of in vitro enzymatic and molecular docking studies. Further, the enzyme kinetics were studied using Lineweaver-Burk plot.
Psoralen was found to inhibit AChE enzyme activity in a concentration-dependent manner. Kinetic studies showed psoralen inhibits AChE in a competitive manner. Molecular docking study revealed that psoralen binds well within the binding site of the enzyme showing interactions such as π-π stacking and hydrogen bonding with residues present therein.
The result of AChE enzyme inhibitory activity of the psoralen in this study is promising. It could be further explored as a potential candidate for further development of new drugs against AD.
阿尔茨海默病（AD）的发病率以惊人的速度上升，现已成为一个全球性的健康问题。抑制乙酰胆碱分解的乙酰胆碱酯酶（AChE）抑制剂构成了AD的主要治疗策略。对补骨脂素作为AChE酶抑制剂进行了研究，以探索其在AD治疗中的潜力。
从补骨脂果实粉末中分离出补骨脂素。通过体外酶学和分子对接研究，考察了不同浓度补骨脂素对AChE酶的抑制活性。此外，使用Lineweaver-Burk图研究了酶动力学。
发现补骨脂素以浓度依赖的方式抑制AChE酶活性。动力学研究表明补骨脂素以竞争性方式抑制AChE。分子对接研究表明，补骨脂素与酶的结合位点结合良好，与其中的残基表现出π-π堆积和氢键等相互作用。
本研究中补骨脂素对AChE酶的抑制活性结果很有前景。它可作为一种潜在的候选药物进一步开发用于治疗AD的新药。
