Planta Med 2020; 86(16): 1204-1215
DOI: 10.1055/a-1209-1254
Biological and Pharmacological Activity
Original Papers

Involvement of the Benzodiazepine Site in the Anticonvulsant Activity of Tapinanthus globiferus against Pentylenetetrazole-induced Seizures in Mice

Christianah A. Elusiyan
1  Drug Research and Production Unit, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Osun State, Nigeria
,
Ana Luiza Gonçalves Faria
2  University center, UniEVANGÉLICA, Cidade Universitária, Anápolis, GO, Brazil
,
Ane Emanuelle Queiroga Mendes
2  University center, UniEVANGÉLICA, Cidade Universitária, Anápolis, GO, Brazil
,
Iransé Oliveira Silva
2  University center, UniEVANGÉLICA, Cidade Universitária, Anápolis, GO, Brazil
,
José Luis Rodrigues Martins
2  University center, UniEVANGÉLICA, Cidade Universitária, Anápolis, GO, Brazil
,
Daniel Alves Rosa
3  Department of Physiological Sciences, Institute of Biological Sciences, Federal University of Goiás, Goiânia, GO, Brazil
,
Gustavo Rodrigues Pedrino
3  Department of Physiological Sciences, Institute of Biological Sciences, Federal University of Goiás, Goiânia, GO, Brazil
,
Elson Alves Costa
4  Department of Pharmacology Sciences, Institute of Biological Sciences, Federal University of Goiás, Goiânia, GO, Brazil
,
Mohamed Ali Ibrahim
5  National Center for Natural Products Research, University of Mississippi, University, Mississippi, United States
,
Jordan K. Zjawiony
5  National Center for Natural Products Research, University of Mississippi, University, Mississippi, United States
6  Department of Biomolecular Sciences, School of Pharmacy, University of Mississippi, University, Mississippi, United States
,
4  Department of Pharmacology Sciences, Institute of Biological Sciences, Federal University of Goiás, Goiânia, GO, Brazil
› Author Affiliations

Abstract

Tapinanthus globiferus is often referred to as an all-purpose herb for the treatment of stroke and epilepsy. The present study investigates the anticonvulsant effect of methanolic leaf extract, active fractions, and lupeol (isolate) of Tapinanthus globiferus in mice as well as the underlying mechanisms. Following phytochemical studies of T. globiferus, preliminary assays were performed to evaluate MLE-induced toxic effect and behavioral changes. The pentylenetetrazol (70 mg/kg, i. p.)-induced seizure was evaluated in mice that were pretreated orally with vehicle 10 mL/kg, MLE (4, 20, or 100 mg/kg), fractions (F1 to F6), lupeol 10 mg/kg or diazepam (3 mg/kg). Methanolic leaf extract preserved neuron viability as well as the relative organ weight, and hematological and biochemical parameters. The behavioral endpoints, neuromuscular coordination, and sensory response parameters revealed a dose-dependent effect of methanolic leaf extract. This extract, active fractions, lupeol, and diazepam potentiated the hypno-sedative effect of the barbiturate and attenuated PTZ-induced acute seizure. This antiseizure effect was completely reversed by flumazenil 2 mg/kg (benzodiazepine site antagonist). Altogether, the benzodiazepine site-mediated anticonvulsant effects of methanolic leaf extract, active fractions, and lupeol corroborate traditional application of T. globiferus against epilepsy.

Supporting Information



Publication History

Received: 07 March 2020

Accepted after revision: 29 June 2020

Publication Date:
15 July 2020 (online)

© 2020. Thieme. All rights reserved.

Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany