Poster presentation
318
SOME DATA ON THE INFLUENCE OF THE BUD AND FLOWER
EXTRACT OF
Capparis spinosa
ON THE DA RECEPTORS
Yu.R. Mirzaev, E.M. Ergashev, R.A. Botirov, G.E. Saidova,
A.Z. Sadikov, Sh.Sh. Sagdullayev
S.Yu. Yunusov Institute of the Chemistry of Plant Substances, Academy of Sciences of
the Republic of Uzbekistan, Tashkent, Uzbekistan
e-mail: botiroovr@mail.ru
Plants of the genus
Capparis spinosa
grows in
arid areas of the Northern
Hemisphere. Several extracts, including those from buds and flowers, consisting of
polyphenols, polysaccharides
and protein compounds, have been isolated from caper
prickly collected in the Tashkent region in the ICPS. These caper extracts have a wide
spectrum of pharmacological activity, including lipid peroxidation of the underlying
neurodegenerative
diseases, which include Parkinson's disease (PD). Our
pharmacological studies of extracts of buds and flowers of caper (PEB) showed that at a
LD
50
of more than 4000 mg/kg, at a dose of 10 mg/kg, it causes an increase in motor
activity (DA) and verticalization behavior in mice, which indicate the activation of DA2
receptors in the CNS. As you know, stimulation of DA2 receptors underlies the
treatment of Parkinson's disease (PD), characterized
by stiffness of movements,
slowness and tremor, to eliminate which DA2 stimulants are used, and primarily the
imported drug Levodopa, long-term use of which, according to E. Nakanishi (2019), is
accompanied by side effects:
1 - confusion;
2 - drowsiness;
3 - excitation,
4 - memory impairment.
This requires the replacement of Levodopa with other DA2 stimulants, the effect of
which is less pronounced.
In view of this, the expansion of the arsenal of
antiparkinsonian drugs with different mechanisms of action is relevant.
When evaluating the possibility of using EBA as such a tool, it was shown that with
a toxicity of less than 4000 mg/kg r.o. EBC at a dose of 10 increases DA and
verticalization from phenamine up to 2 times, and at a dose of 30 mg/kg up to 3 times.
With a daily dose of 30 mg/kg orally for 5 days, there was a decrease in the intensity of
the activating effect on verticalization, i.e. tendency to tachyphylaxis. At a dose of 50
mg/kg, DA is inhibited, and at a dose of 100 mg/kg, DA and verticalization are almost
completely inhibited.
Levodopa at a dose of 3 mg/kg tones D2 receptors to the maximum extent. A dose of
10 starts to inhibit the stimulation of DA
receptors, and at a dose of 30 mg/kg it paralyzes
it.
In EBP, in addition to stimulation of DA2 receptors, one should also expect an
antioxidant effect that prevents the development of PD. In addition, in the experiment,
EBK eliminated the side effects of Levodopa. EBP is of interest as a potential anti-
Parkinson agent in case of loss of the therapeutic effect of Levodopa, as well as a
remedy for its side effects.