Will bis-3-cognitin help with Parkinson's disease?
Experimental drug protects parkinsonian neurons
According to scientists, a substance called bis-3-cognitin (bis-3-cognitin) can become a starting point for the search for drugs that slow down the development of Parkinsonism. Bis-3-cognitin protects mitochondria, the "bottleneck" of nerve cells in the brain of people suffering from this neurodegenerative disease.
The experiments of the group led by Zixu Mao were carried out on model mice with symptoms of Parkinsonism, which were induced by special toxins. With simultaneous exposure to toxins and bis-3-cognitin, motor problems characteristic of the disease did not occur in animals.
The results of the study are published in the Journal of Biological Chemistry.
Professor Mao and his colleagues studied myocyte-specific binding (enhancer) factor 2 (Mycyte-specific enhancer factor 2D, MEF2D), which is a protein (encoded by the MEF2D gene). This factor protects neurons from death. In previous studies, scientists have shown that the level of MEF2D in the neurons of patients with parkinsonism is significantly reduced. The protein itself is sensitive to intracellular changes such as oxidative stress, which can lead to damage to neurons in Parkinson's disease.
"For a number of years, we have been talking about looking for drugs that increase the level of MEF2D," says Zixiu Mao. The main problem, he said, was the selection of a screening system. "You can search in the library of small molecules, or in the scientific literature, or make guesses," he explains.
Scientists have guessed about the possible role of bis-3-cognitin, although initially this compound was created for other purposes. Cognitins are a family of compounds derived from tacrine, the first approved drug by the Food and Drug Administration (FDA) to relieve the symptoms of Alzheimer's disease. Takrin was subsequently discontinued due to a number of serious side effects caused by it.
Bis-3-cognitin consists of two tacrine molecules connected by a flexible hydrocarbon bridge with two nitrogen atoms at the ends.
In experiments on cell culture, scientists have demonstrated its ability to protect neurons from the harmful effects of methyl-phenyl-tetrahydropyridine, a neurotoxin that causes symptoms of Parkinson's disease. In the presence of bis-3-cognitin, the level of myocyte-specific enhancer factor 2 in the nucleus and mitochondria increased. Neither tacrine nor bis-7-cognitin produced such an effect.
The authors believe that bis-3-cognitin should not have the side effects that were found in takrin, however, before starting clinical trials of this substance, it is necessary to conduct extensive pharmacological studies.
Portal "Eternal youth" http://vechnayamolodost.ru06.09.2012