Planta Med 2001; 67(2): 136-141
DOI: 10.1055/s-2001-11504
Original Paper

© Georg Thieme Verlag Stuttgart · New York

Anticonvulsant Properties and Bio-Guided Isolation of Palmitone from Leaves of Annona diversifolia 1

María Eva González-Trujano2, 3, 4 , Andrés Navarrete2,*, Benito Reyes5 , Ernestina Cedillo-Portugal6 , Enrique Hong4
  • 1 Taken in part from the Ph. D. research work of M.E. González-Trujano
  • 2 Facultad de Química, Departamento de Farmacia. Universidad Nacional Autónoma de México, México D. F., México
  • 3 Instituto Mexicano de Psiquiatría, México, D. F., México
  • 4 Sección de Terapéutica Experimental. Departamento de Farmacología y Toxicología. CINVESTAV IPN, México, D.F., México
  • 5 Laboratorio de Productos Naturales. Area de Química. Universidad Autónoma Chapingo, México
  • 6 Area de Biología. Universidad Autónoma Chapingo, México
Further Information

Publication History

February 11, 2000

July 2, 2000

Publication Date:
31 December 2001 (online)

Abstract

The activity-guided fractionation of the ethanol extract of leaves of Annona diversifolia Saff., led to the isolation of palmitone (16-hentriacontanone) as the only anticonvulsant active compound. This aliphatic ketone was highly effective to diminish pentylenetetrazole (PTZ)-induced clonic-tonic seizures and toxicity. Also, it produced a prolongation of the latency for onset of seizures and a reduction of the death rate produced by 4-aminopyridine (4-AP) and bicuculline (BIC). However, it was inactive to inhibit the kainic acid (KA)- and strychnine (STC)-induced seizures. Palmitone did not produce motor incoordination and loss of righting reflex which are used as signs of neurological impairment. Palmitone (ED50 = 1.85 mg/kg) proved to be a more potent antiepileptic drug against the PTZ-induced seizures than etosuximide (ED50 = 59.6 mg/kg), sodium valproate (ED50 = 63 mg/kg), and carbamazepine (ED50 > 300 mg/kg) and it was only four-fold less potent than diazepam (ED50 = 0.48 mg/kg). The pharmacological profile of palmitone suggests that this compound could be acting on the GABAergic inhibitory system.

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Dr. Andrés Navarrete

Facultad de Química Conjunto E,

Departamento de Farmacia

Universidad Nacional Autónoma de México

Coyoacán 04510

México D.F.

México

Email: anavarrt@servidor.unam.mx.

Fax: (5) 6 22 53 29

Phone: (5) 6 22 52 91