Abstract
Stereoisomers of the monoterpene epoxycarvone (EC), namely (+)-cis-EC, (−)-cis-EC, (+)-trans-EC, and (−)-trans-EC, were comparatively evaluated for anticonvulsant activity in specific methodologies. In the pentylenetetrazole (PTZ)-induced anticonvulsant test, all of the stereoisomers (at 300 mg/kg) increased the latency to seizure onset, and afforded 100% protection against the death of the animals. In the maximal electroshock-induced seizures (MES) test, prevention of tonic seizures was also verified for all of the isomers tested. However, the isomeric forms (+) and (−)-trans-EC showed 25% and 12.5% inhibition of convulsions, respectively. In the pilocarpine-induced seizures test, all stereoisomers demonstrated an anticonvulsant profile, yet the stereoisomers (+) and (−)-trans-EC (at 300 mg/kg) showed a more pronounced effect. A strychnine-induced anticonvulsant test was performed, and none of the stereoisomers significantly increased the latency to onset of convulsions; the stereoisomers probably do not act in this pathway. However, the stereoisomers (+)-cis-EC and (+)-trans-EC greatly increased the latency to death of the animals, thus presenting some protection. The four EC stereoisomers show promise for anticonvulsant activity, an effect emphasized in the isomers (+)-cis-EC, (+)-trans-EC, and (−)-trans-EC for certain parameters of the tested methodologies. These results serve as support for further research and development of antiepileptic drugs from monoterpenes.
Highlights
Epilepsy has been characterized as a brain disease characterized by certain conditions: at least two unprovoked seizures in a range greater than 24 h; an unprovoked seizure and the likelihood of further recurrent crises after two unprovoked seizures, continuation over 10 years; and diagnosis of epileptic syndrome [1]
When considering the development of new antiepileptic drugs from 1981–2002, it is important to emphasize the role of natural products, since most of the synthetic drugs developed have had a natural product as their model
This study aims to comparatively verify the anticonvulsant potential of the four stereoisomers of epoxycarvone in animal models of chemically and electrically induced seizures
Summary
Epilepsy has been characterized as a brain disease characterized by certain conditions: at least two unprovoked seizures in a range greater than 24 h; an unprovoked seizure and the likelihood of further recurrent crises after two unprovoked seizures, continuation over 10 years; and diagnosis of epileptic syndrome [1]. Epileptic patients present recurrent spontaneous seizures [2], and some 30% of them are considered resistant to drug therapy, without adequate response to treatment. It is known that the existing clinical anti-epileptic drugs are not good anti-epileptogenics, since they only increase the onset threshold for seizure [6]. When considering the development of new antiepileptic drugs from 1981–2002, it is important to emphasize the role of natural products, since most of the synthetic drugs developed have had a natural product as their model. This reinforces the role of nature as a source for anticonvulsant agents [8]
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