N-allyl-d-glucosamin as adaptogene


The invention relates to N-allyl-D-glucosamine formula (1) as adaptogene. The proposed connection improves the General nonspecific resistance of the body during exercise and potentional action of inhalation anaesthesia funds. table 2., 1 Il.

The invention relates to pharmaceutical industry and associated with obtaining biologically active compounds of group of glycosides to increase nonspecific resistance of the organism, and can be used in medicine to improve the vitality weakened patients in the postoperative period, in-patient treatment to increase stamina when dynamic loads of varying intensity and duration, increase physical performance in terms of employment rights, as well as to improve the overall nonspecific resistance when working in emergency situations.

Known liquid extract of Siberian ginseng, raw material which is Eleutherococcus senticosus (Eleuhterococcus senticosus) is a wild shrub from the family Kalievyh (Araliaceae), large quantities of surface (eleutherosides), defining adaptogenic activity of medicinal forms of Siberian ginseng (Brekhman, I. I. materials for the study of ginseng and other medicinal products of the Far East. Far East publishing house, Vladivostok. - Vol.7. - 1966. - 325 S.; Brekhman, I. I. Siberian ginseng. Ed. "Nauka", Leningrad branch, far Eastern branch name C. A. Komarov Institute of biologically active substances. - 1968).

Lack of dosage forms of Siberian ginseng is the instability of the concentration and proportion of eleutherosides in vegetable raw materials, determining the pharmacological action of liquid extract of Siberian ginseng. Quantitative and qualitative value of the eleutherosides in the extract depends on the place of growth of plants, climatic conditions and environmental conditions. Resources known medicinal raw material is limited by the areal growth in some regions of the country.

This disadvantage dosage forms of Siberian ginseng is eliminated by the invention. The invention consists in using for increase nonspecific resistance of the body during physical activity and potentiation of analgesic action of inhalation narkose D-glucose allylamino in ethanol medium at 50-60oWith and subsequent recrystallization from ethanol, with the degree of purity 99.8% and a yield of 90%.

The invention can be used by applying the proposed N-allyl-D-glucosamine to increase endurance under dynamic loads of different length and tension, improving physical performance in terms of employment rights, including when working in extreme situations, and also in medicine for increasing vitality weakened patients during treatment in hospital, including in the postoperative period.

The study of the pharmacological properties of N-allyl-D-glycosylamine.

Example 1.

Synthesis of N-allyl-D-glycosylamine.

10.0 g of dried (100-105oC) D-glucose and 15 ml of allylamine was placed in a reactor equipped with a reflux condenser; the ratio of reactants (mol) is 1:3,6. Spent the mixture heated on a water bath (60o(C) under vigorous stirring until the formation of homogeneous liquid system. The reaction mixture was cooled to room temperature. Within 12 hours there is crystallization of the glycoside. The crystals were separated by filtration, dried in air, and recrystallized from ethyl JV pl. = 125oC, soluble in water and lower alcohols. Output - 10.6 g (87%).

Found, %: N 6.42 Per; 48,92; N 7,89. M 217,3. (C9H17O5N).20d-35,5(C. 2 g in 100 ml water). Calculated, %: N Of 6.31-6,4; 49,29; N. Of 7.75. M 219,1.

The structure of the obtained substance was confirmed by spectral analysis. For the composition of the IR spectrum of N-allyl-D-glycosylamine is characterized by the presence of peaks indicating the presence of unsaturated compounds component: 890 cm-1(out-of-plane deformation vibrations of C=C), 1630 cm-1(stretching vibrations of C= C); a carbohydrate component in the structure of N-allyl-D-glycosylamine characterized by the presence of the peak 1446 cm-1, as well as a series of peaks 1020-1090 cm-1and 1240-1270 cm-1(The IR spectrum of N-allyl-D-glucoseamine - see drawing).

Example 2.

Pharmacological action.

The study of physical performance was conducted experiments on outbred mice weighing 18-25 g using a treadmill at a speed strap two-way conveyor 840 m/h with angle 0o. The conditions the animals were standard. N-allyl-D-glucosamine was administered at a dose of 2.5-5 mg/kg animal body weight by vnutrisubstratny and Eleutherococcus put through three days after the rest of the mice.

The result of this survey, the data obtained are given in table.1.

Analysis of the data given in table.1 shows that intraperitoneal injection of dry residue Eleutherococcus calls after 30 min the increase in physical performance in a dose of 2.5 mg/kg 40.0%, and at a dose of 5 mg/kg by 65.0% and at a dose of 2.5 mg/kg 41.8%, whereas the introduction of N-allyl-D-glucosamine at a dose of 2.5 mg/kg increases the efficiency of 88.3% and a dose of 5 mg/kg - 44.3%.

The data are statistically significant at p<0,05. Thus, N-allyl-D-glucosamin at a dose of 2.5 mg/kg) effect on physical performance is more active than Siberian ginseng.

Example 3.

Pharmacological action.

The experiments were conducted on 15 mice of both sexes, weighing 22-30, sustainability Criteria to the anesthetic agent - diethyl ether - served: the stay of the animal in an upright position (anesthesia) and change the ability of the nervous system to the summation of subthreshold pulses immediately after exiting the lateral position compared to what it was before the introduction of the anaesthetic. To do this, the animal was determined by the magnitude of the voltage (V) at a pulse frequency of 50 Hz, a delay of 20 MS and a duration of 20 MS, the required d is the provisions. Anesthesia was caused by placing animals in a vessel with a capacity of 5 l (one) in the atmosphere of a saturated vapor of diethyl ether to the occurrence of lateral position. Concentration was established by calculation, statistical method, always under the same conditions (time of day, the temperature inside and under the hood).

The data are statistically significant at p<0,05.

The comparison of the obtained data shows that the Amount of force of the electric current (V) required to obtain the response of the animal to the electric irritation under the action of N-allyl-D-glycosylamine immediately after the release of the animal from anesthesia, increases depending on the dose: the dose of 2.5 mg/kg - 94%, at a dose of 5 mg/kg to 47%. In addition, N-allyl-D-glucosamin at a dose of 5 mg/kg causes an increase in pain threshold by 23% after 24 hours after injection compared with initial value.

The duration of stay of animals under anesthesia due to the actions of N-allyl-D-glycosylamine is not changed.

This shows the potentiation of N-allyl-D-glycosylamines analgesic action of vapors of diethyl ether on animals.




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