Bioactive non-sterol triterpenoid fromStreblus asper: microwave-assisted extraction, HPTLC profiling, computational studies and neuro-pharmacological evaluation in BALB/c mice

Abstract

Context: In folk medicine, the stem bark of Streblus asper Lour. (Moraceae) has been reported to possess anticonvulsant activity. However, no systematic/scientific validation is available. Objective This study explores the constituents in the stem bark, their biosassy-guided isolation and their efficacy in neuro-pharmacological disorders, for validating the traditional claims. Materials and methods: Microwave-assisted extraction (MAE) technique was employed to obtain the crude extract. The n-hexane, dichloromethane and aqueous fractions were prepared and phytoconstituents were ascertained by phytochemical tests. The isolated compound, betulin, was characterized by different physicochemical and spectral methods, including HPTLC. Finally, neuro-pharmacological evaluations were conducted at 100, 200, 400 mg/kg b.w., p.o. (25, 50, 100 mg/kg b.w. for betulin) doses in BALB/c mice. Results: The n-hexane fraction (400 mg/kg), and isolated compound betulin (100 mg/kg), showed maximum anticonvulsant activity in maximal electroshock (87.84% and 85.14% seizure inhibition), and isoniazid induced convulsion models (88.85% and 83.18% seizure inhibition), respectively. A dose-dependent attenuation of epileptic seizures was observed, probably through GABArgic mechanism of anticonvulsant action. Moreover, the antidepressant study was also conducted using behavioural models and the results expound that n-hexane and dichloromethane fractions (400 mg/kg) significantly reduced the duration of immobility, as compared to the control. Discussion and conclusion: This study reports some novel aspects like applying an environmentally benign/green approach of MAE, neuro-pharmacological screening and use of docking studies, for the first time, on the plant S. asper. The findings present a rational explanation for its use in traditional medicine, for the management of neuro-pharmacological disorders.ARTICLE HISTORY

Neuroprotective Effect of Coumarin Nasal Formulation: Kindling Model Assessment of Epilepsy

“…PTZ is reported to interact with the GABA neurotransmission and the GABA receptor complex antagonism by PTZ leads to PTZ-induced seizures ( Bum et al, 2001 ). Since CNF was found to be active against PTZ convulsions, it is probable that it may be interfering with GABA mechanism by enhancing the activation of GABA A receptors owing to the phytoconstituents present in it ( Kundaikar et al, 2015 ). This would facilitate the GABA-mediated opening of chloride channels offering symptomatic relief.…”

Techniques for the analysis of pentacyclic triterpenoids in medicinal plants

“…Apart from chromatographic methods, extraction methods should be performed and optimized along with the corresponding analytical techniques, extraction temperature, time, and cycles, solvents used, solvent‐to‐material ratio, presoaking time of the sources, and properties of the compound itself. Some of the methods that can be used to extract triterpenes, include Soxhlet extraction, heat reflux extraction, maceration extraction, stirring extraction, UAE, MAE, SFE, and pressurized fluid extraction (PFE) . Among these methods, Soxhlet extraction, heat reflux extraction, maceration extraction, and stirring extraction are relatively simple and have a low cost.…”

“…Some of the methods that can be used to extract triterpenes, include Soxhlet extraction, heat reflux extraction, maceration extraction, stirring extraction, UAE, MAE, SFE, and pressurized fluid extraction (PFE) [25, [65][66][67][68][69][70][71][72][73]. Among these methods, Soxhlet extraction, heat reflux extraction, maceration extraction, and stirring extraction are relatively simple and have a low cost.…”

Deep eutectic solvents aqueous two-phase system based ultrasonically assisted extraction of ursolic acid (UA) from Cynomorium songaricum Rupr.

“…Because of the good biological activity, separation of UA from Cynomorium songaricum Rupr.has received more attention. Many methods, such as organic solvent extraction Baranauskaitė et al, 2016), ethanol/non-aqueous solvent by direct-heating extraction (Fan et al, 2016),ultrasound-assisted extraction (UAE) (Chen et al, 2007), microwave-assisted extraction (MAE) (Fernandez-Pastor et al, 2017;Verma et al, 2016;Zhong et al, 2016), enzymatic extraction (EE) (Zhou et al, 2017), and subcritical water extraction (SWE) (Mlyuka et al, 2016)have been used to extract UA from natural products. However,these techniques have disadvantages of large amounts of organic solvents, long extraction times, and high energy consumption.…”