NEUROPHARMACOLOGICAL EFFECTS OF THE ETHANOLIC EXTRACT OF DERIVATIVES OF LUPEOL IN RATS

Abstract

Objective: The neuropharmacological activities of ethanolic extract derivatives of lupeol are being screened on rats. Prepared derivatives are evaluated for their locomotor, anxiolytic and stereotype activities. The present investigation was designed to evaluate the antipsychotic effect of semisynthetic derivatives of lupeol using rat models of elevated maze model and apomorphine-induced stereotype behavior.

Methods: Lupeol was extracted from Crataeva nurvala bark using ethano. After chemical modification, we made different derivatives using aldol condensation. Different derivatives were obtained from a series of reaction previously published LAH-3, LAP-3, LAPEA-3, LAMP-3, LATS-3, and LAS-3. Neuropharmacological effects, including anxiolytic, central nervous inhibitory, and stereotype antipsychotic effects were evaluated in the different derivatives of lupeol at a dose of 250 mg/kg using standard methods.

Results: The absolute derivatives of LAH3 and LAPEA3 showed a significant reduction in the activity score in actophotometer test. Reduction in the locomotor activity indicates central nervous system (CNS) depressant property of the drug. LAMP3 and LAS3 show a significant anxiolytic effect. From the result of elevated plus maze, it was evident that derivatives of lupeol treated animals exhibit an increased number of entries into open arm when compared to normal control, which shows the anxiolytic activity of the lupeol derivatives. Sniffing, rearing and licking activities for lupeol derivatives LAH3 and LAPEA3 were found to be 35%, 33%, and 40% and 40.33%, 38%, and 33.33% respectively when it compared with standard and control groups. This model is suggestive of the absence of negative symptoms alleviating property of all the treatment groups.

Conclusions: The lupeol and its semisynthetic derivatives possess anxiolytic, CNS inhibitory, and antipsychotic effects to varying degree.