Scientists from the Russian city of Novosibirsk currently work on developing new effective and cheap anticonvulsants, which are also less toxic than existing anti-epileptic drugs.

Patients with epilepsy desperately need effective and non-toxic treating agents. Researchers from Novosibirsk Institute of Organic Chemistry (Siberian branch of Russian Academy of Sciences) suggest making anticonvulsants, based on pinene amino acids. Scientists have already performed some pharmacology studies of the new drug on non-pedigree laboratory mice.

Statistics says that about 3 per cent of Earth’s population suffers from epileptic seizures to a greater or lesser degree. In order to prevent convulsions, doctors usually recommend their patients to take pharmaceuticals, containing gamma-aminobutyric acid. However, this kind of therapy is almost useless for about one fourth of epileptics. That is why doctors and scientists continue their search for anticonvulsants, which are more effective than existing ones and have as little side effects as possible.

Basic substances for such therapeutic agents can vary, and amino acid derivatives, for instance, which are produced from alpha-pinenes, fit perfectly, researchers from Novosibirsk think. Alpha-pinenes belong to hydrocarbons of terpene type and are among most common natural terpenes – pine needle oil (turpentine) contains many of these chemical compounds, for example. Amino acids from alpha-pinenes have rigid structure and are more selective during binding with target molecules. During studies scientists also discovered that abovementioned chemical compounds showed higher biological activity than derivatives of gamma-aminobutyric acid.

 

 

Anticonvulsant activity of new possible therapeutic agents was tested on white non-pedigree mice, which received intraperitoneal injections of pentylenetetrazol and nicotine, which are well-known drugs, affecting nervous system and causing convulsions. Amino ester of an amino acid, belonging to alpha-pinenes, showed great anticonvulsant activity in 7-fold dilution compared to Phenobarbital, a common anticonvulsant agent. Moreover, this substance showed only a slight effect on general emotional state and motion behaviour. In addition, said amino ester causes no sleepiness and has moderate toxicity level.

Median lethal dose (LD50) of new possible anticonvulsant is 8.1 times less than that of Phenobarbital and exceeds 1000 mg (1 g) of the drug per one kilogram of body weight, when introduced intragastrically – scientists claim you should eat a lot of this drug before it does you any harm.

All abovementioned properties of the amino ester and simple extraction technique (it contains only two stages) from a common substance – alpha-pinene – allow scientists to suggest this derivative becoming the basic substance for development of new almost non-toxic anticonvulsant agents, thus making life of epilepsy patients easier.

Source: Science & Technology

Kizilova Anna