Synthesis and Evaluation of Antipsychotic Compounds from Lupeol

A. Wal, R. Srivastava, A. Rai, P. Wal, R. Tiwari
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引用次数: 3

Abstract

Aim: The current study was designed to evaluate the antipsychotic potential of lupeol and their semisynthetic derivatives to get a new and potent antipsychotic agent. Methodology: Lupeol was isolated from bark of Crateava nurvala. the current study was designed to evaluate the antipsychotic potential of lupeol and its semisynthetic derivatives. C. Nurvala stem bark was extracted by cold maceration with 95% ethanol and concentrated through rotary vacuum evaporator under reduced pressure. The concentrated ethanolic extract was defatted with petroleum ether and fractionated with chloroform successively. Lupeol derivatives were prepared through a three step reaction with different amines, aliphatic and aromatic moieties. A series of derivatives of lupeol were assayed for antipshychotic activity in actophotometer and compulsive behaviour (Stereotypy) in Plus Maze Model in rats. Few derivatives of lupeol showed more potent activity as compared to the basic molecule, lupeol. Results: The results of the present study clearly indicated that the derivatives and lupeol isolated from C. Nurvala and synthetic lupeol analogs possess significant antipsychotic activity. Conclusion: Lupeol skeleton deserves further investigation for the development of more potent and non-toxic new antipshychotic agents for therapeutic applications.
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芦皮醇类抗精神病化合物的合成与评价
目的:评价芦荚醇及其半合成衍生物的抗精神病潜能,以期获得一种新的有效的抗精神病药物。方法:从山楂树皮中分离得到鹿皮醇。本研究旨在评价芦皮醇及其半合成衍生物的抗精神病潜能。C.采用95%乙醇冷浸法提取木耳茎皮,减压旋转真空蒸发器浓缩。将浓缩乙醇提取物用石油醚脱脂,再用氯仿分馏。以不同的胺类、脂肪类和芳香族为原料,通过三步反应制备了槲皮醇衍生物。采用光敏计和Plus迷宫模型大鼠的强迫行为(刻板印象)测定了一系列芦皮酮衍生物的抗精神病活性。很少有lupeol衍生物显示出比基本分子lupeol更强的活性。结果:本研究结果清楚地表明,从金缕莲中分离得到的衍生物和芦皮醇以及合成的芦皮醇类似物具有显著的抗精神病活性。结论:芦皮酮骨架值得进一步研究,以开发更有效、无毒的新型抗精神病药物。
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