Balaei-Kahnamoei Majid, Saeedi Mina, Rastegari Arezoo, Shams Ardekani Mohammad Reza, Akbarzadeh Tahmineh, Khanavi Mahnaz
Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Evid Based Complement Alternat Med. 2021 Jul 19;2021:5965061. doi: 10.1155/2021/5965061. eCollection 2021.
Using L. (henna) seeds has been frequently recommended for the improvement of memory in Iranian Traditional Medicine (ITM). In this respect, different fractions of the plant were prepared and evaluated for their biological assays related to Alzheimer's disease (AD), including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity as well as metal chelating ability and DPPH antioxidant activity. The dichloromethane and ethyl acetate fractions were able to inhibit the BChE selectively with IC values of 113.47 and 124.90 g/mL, respectively, compared with donepezil as the reference drug (IC = 1.52 g/mL). However, all fractions were inactive toward AChE. Phytochemical analysis of the dichloromethane fraction indicated the presence of -sitosterol (), 3-acetyloleanolic acid (), 3--()-coumaroyl oleanolic acid (), betulinic acid (), and oleanolic acid (). The inhibitory activity of isolated compounds was also evaluated toward AChE and BChE. Among them, compounds and showed potent inhibitory activity toward BChE with IC values of 77.13 and 72.20 M, respectively. However, all compounds were inactive toward AChE. Moreover, molecular docking study confirmed desired interactions between those compounds and the BChE active site. The ability of fractions and compounds to chelate biometals (Cu, Fe, and Zn) was also investigated. Finally, DPPH antioxidant assay revealed that the ethyl acetate (IC = 3.08 g/mL) and methanol (IC = 3.64 g/mL) fractions possessed excellent antioxidant activity in comparison to BHA as the positive control (IC = 3.79 g/mL).
在伊朗传统医学（ITM）中，经常推荐使用指甲花种子来改善记忆力。在这方面，制备了该植物的不同馏分，并对其与阿尔茨海默病（AD）相关的生物学测定进行了评估，包括乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）抑制活性以及金属螯合能力和DPPH抗氧化活性。二氯甲烷和乙酸乙酯馏分能够选择性地抑制BChE，IC值分别为113.47和124.90μg/mL，而多奈哌齐作为参考药物（IC = 1.52μg/mL）。然而，所有馏分对AChE均无活性。二氯甲烷馏分的植物化学分析表明存在β-谷甾醇、3-乙酰齐墩果酸、3-β-（E）-香豆酰齐墩果酸、桦木酸和齐墩果酸。还评估了分离化合物对AChE和BChE的抑制活性。其中，化合物和对BChE表现出较强的抑制活性，IC值分别为77.13和72.20μM。然而，所有化合物对AChE均无活性。此外，分子对接研究证实了这些化合物与BChE活性位点之间的理想相互作用。还研究了馏分和化合物螯合生物金属（铜、铁和锌）的能力。最后，DPPH抗氧化试验表明，与作为阳性对照的丁基羟基茴香醚（IC = 3.79μg/mL）相比，乙酸乙酯（IC = 3.08μg/mL）和甲醇（IC = 3.64μg/mL）馏分具有优异的抗氧化活性。
