02 February 2011

A new drug for parkinsonism?

Russian scientists have tested a new remedy for Parkinson's diseaseNatalia Reznik, STRF.ru
About 3.7 million people (7 percent of people over 60)
 
they suffer from Parkinson's disease. Patients are traditionally treated with drugs containing levodopa (L-DOPA, L-dioxyphenylalanine), but they have many side effects, and they cannot be used for a long time. In this regard, the search for new drugs is very relevant. Specialists of the Novosibirsk Institute of Organic Chemistry named after N. N. Vorozhtsov SB RAS synthesized a substance they named I, which has antiparkinsonian activity. The tests conducted on mice are encouraging.

In Parkinson's disease, a part of the brain called the black substance is affected, in which dopamine is produced. One of the functions of this neurotransmitter is to ensure normal mobility. Due to the disease, dopamine becomes less, and the patient suffers from slow and constrained movements, trembling of the limbs at rest, it is difficult for him to maintain balance and speak articulately. Due to damage to the neurons of the substantia nigra, depression develops. The main drug for Parkinson's disease is L–DOPA, a precursor to dopamine. With prolonged use, this drug causes impaired coordination of movements and heart rhythm, as well as impairs memory.

A potential replacement for levodopa, substance I, or 4S, 5R, 6R-para-menta-1,8-diene-5,6-diol, was tested on mice. To make them sick, scientists used the neurotoxin MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine), which selectively damages the neurons of the substantia nigra synthesizing dopamine. MPTP was injected into mice intraperitoneally once or for three days, and 15 minutes after the last injection into the stomach was injected I. After an hour and a half, the researchers evaluated the effect of the drug and made sure that in all cases it effectively neutralizes the effect of the toxin and eliminates the symptoms of Parkinsonism. In mice, motor activity, movement speed, and research activity – an indicator of emotional status - improved and almost approached the control indicators.

Parkinson's disease can be fatal. To test how the new drug affects survival, mice were injected with the toxin for 10 days, and drug I was also injected daily, four hours after the injection of MFTP. In the group of animals receiving only neurotoxin, six out of ten mice died by the end of the experiment. In the group that also received substance I, one mouse died. At the same time, I was not inferior in effectiveness to the "gold standard" treatment of Parkinson's disease – levodopa, when using which two mice died.

In conclusion, scientists note that I has a high antiparkinsonian activity, and with prolonged use of neurotoxin significantly reduces mortality.

Source of information:
T. G. Tolstikova et al., "A highly effective antiparkinsonian agent of a new structural type".
Reports of the Academy of Sciences, 2010, volume 435, No. 5.

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02.02.2011

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