Anticholinesterase Activity of Methanolic Extract of Amorpha fruticosa Flowers and Isolation of Rotenoids and Putrescine and Spermidine Derivatives

Plants Pub Date : 2024-04-24 DOI:10.3390/plants13091181
D. Jankovská, Nikol Jurčová, Renata Kubínová, Jiří Václavík, Emil Švajdlenka, A. Mascellani, Petr Maršík, Kateřina Bouzková, Milan Malaník
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Abstract

Five putrescine and spermidine derivatives (1–5) together with five rotenoids (6–10) were isolated from a methanolic extract of the flowers of A. fruticosa that displayed promising inhibition of 76.0 ± 1.9% for AChE and 90.0 ± 4.0% for BuChE at a concentration of 1 mg/mL. Although the anticholinesterase activities of the isolated compounds did not reach that of galantamine, molecular docking revealed that all-trans-tri-p-coumaroylspermidine and trans-trans-cis-tri-p-coumaroylspermidine showed binding poses mimicking the known inhibitor galantamine and thus could serve as model molecules in future searches for new AChE and BuChE inhibitors.
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Amorpha fruticosa 花甲醇提取物的抗胆碱酯酶活性以及轮烯类化合物和 Putrescine 与 Spermidine 衍生物的分离
从A. fruticosa花的甲醇提取物中分离出了五种腐胺和亚精胺衍生物(1-5)以及五种鱼藤酮类化合物(6-10),在浓度为1毫克/毫升时,它们对AChE的抑制率为76.0 ± 1.9%,对BuChE的抑制率为90.0 ± 4.0%。虽然分离出的化合物的抗胆碱酯酶活性没有达到加兰他敏的水平,但分子对接显示,全反式-三对香豆酰过氧吡啶和反式-反式-顺式-三对香豆酰过氧吡啶显示出与已知抑制剂加兰他敏相似的结合位置,因此可以作为未来寻找新的 AChE 和 BuChE 抑制剂的模型分子。
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