RU2489162C1 - Cardioprotective drug with manifested antioxidant activity - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a cardioprotective and antioxidant drug. The cardioprotective and antioxidant drug prepared by the three-staged extraction of ground tick trefoil (Hedysarum alpinum) herb in aqueous-alcoholic solutions to be randomly agitated at room temperature in a blacked-out place under certain circumstances; then the fractions are poured out and dried in a thermostat.

EFFECT: drug prepared by the above method possesses no side action and shows manifested cardioprotective and antioxidant action.

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Description

The invention relates to medicine and specifically to preventive pharmacology and relates to agents that improve the cardiovascular activity of both healthy and sick people. The proposed tool is a phytopreparation from the grass of Alpine penny (Hedysarum alpinum). The tool does not have a side effect and exhibits a pronounced cardioprotective and antioxidant effect.

Recent studies have shown that excessive activation of free radical oxidation reactions is a typical pathological process that occurs in a variety of diseases (atherosclerosis; cerebral, coronary and peripheral circulation disorders; diabetes mellitus; rheumatoid, inflammatory and degenerative diseases of the musculoskeletal system; pulmonary diseases, etc. .). Also, reactions involving free radical oxygen derivatives play an important role in the development of cardiovascular diseases.

In the human body there is a system of protection against the damaging effects of oxygen radicals. The enzymatic components of this system are superoxide dismutases, catalases and peroxidases. Non-enzymatic substances are mainly low-molecular substances: β-carotene, vitamins A, C and E. The antioxidant system of the body in a number of pathological disorders is not able to withstand the massive release of oxygen radicals. Therefore, in order to influence free radical oxidation, antioxidants have recently been used in the treatment of various cardiovascular diseases.

Such substances with antioxidant activity as α-tocopherol, dibutinol, hydroxypyridines have found widespread use. However, many well-known antioxidants have serious drawbacks: they act only at the final stage of free radical oxidation, and upon decomposition of free radicals of polyunsaturated fatty acids form toxic products. In connection with the foregoing, the search for more effective antioxidants is an urgent problem.

Today, a group of flavonoid compounds with antioxidant properties is known. It was found that flavonoids (quercetin, rutin) contained in the P-vitamin preparation terminate the chains of radicals involved in lipid peroxidation, thereby freeing from active oxygen and protect capillaries from fragility. High anti-radical activity was also noted in the group of hydroxycinnamic acids, xanthones, and triterpenes.

Currently, a fairly large number of herbal medicines are used that can act as antioxidants (p.2169481, p.93014335, p.2057799, p.2180584, p.2130314), the lack of drugs is not sufficient suppression of lipid peroxidation (about 50 %) and the absence of a cardioprotective effect.

It is known that biochemical parameters of blood plasma can diagnose various cardiovascular diseases in the early stages. When muscle damage occurs, the enzyme leaves the cells - an increase in the activity of creatine kinase in the blood. Therefore, the determination of creatine phosphokinase and creatine kinase MB in the blood is widely used in the early diagnosis of myocardial infarction. Also, aspartate aminotransferase and alanine aminotransferase enzymes are biochemical markers of myocardial damage in the blood of the coronary sinus. A decrease in these indicators indicates a positive effect on energy metabolism and stabilization of cell membranes, including cardiomyocytes.

The authors did not find in the literature a combination of cardioprotective and antioxidant effects.

An object of the present invention is to provide a herbal medicine with cardioprotective and antioxidant activity. The novelty of this invention is the development of a phytopreparation having both cardioprotective and antioxidant activity, as well as the identification of new pharmacological effects of Alpine penny.

The problem is solved as follows. A phytopreparation from Alpine penny grass (Hedysarum alpinum) is proposed, which is obtained by a method previously developed by us (Patent RU 2402344 C1, publ. 10.27.2010):

From the crushed plant material of Alpine penny grass (Hedysarum alpinum) by phased extraction with a water-alcohol solution with various concentrations of ethyl alcohol, maceration and percolation methods:

The first fraction was obtained after processing the starting material with an aqueous-alcoholic solution in a ratio of 2: 1 for 8 days, a total volume of 300 ml. The 2nd fraction was obtained by treating the remainder of the penny grass with an Alpine water-alcohol solution in the ratio 1: 1 for 6 days, the total volume of 300 ml. The 3rd fraction was obtained by treating the remainder of the plant material with an aqueous-alcoholic solution in a ratio of 1: 2 for 5 days, a total volume of 300 ml. The obtained fractions were poured and dried in a thermostat at a temperature of 37 ° C.

Phytopreparation from Alpine penny grass is a dark brown crystalline powder.

Cardioprotective effect was determined by a known method (R.U. Khabriev 2005). The study was carried out on outbred white rats; an alpine penny herbal medicine was administered once a day intragastrically at a dose of 200 mg / kg of the animal’s body weight, having previously dissolved in a sufficient amount of purified water. The control group received an equivalent amount of purified water. The results of the study are shown in table 1.

Table 1 The effect of phytopreparation Alpine penny on biochemical blood parameters Indicator Units rev. The control H.alpinum Alanine aminotransferase U / L 121.56 93.11 * Aspartate aminotransferase U / L 318.37 190.67 * Creatine Phosphokinase U / L 2243,329 1289.4 * Creatine Phosphokinase MB U / L 87.13 43.77 * * - significant differences in data relative to control Pt <0.5
A decrease in these biochemical parameters proves the presence of a cardioprotective effect in the phytopreparation of Alpine penny.

The antioxidant properties of Alpine penny grass are associated with the presence of a group of flavonoids (rutin, quercetin, hyperoside), xanthones, and chlorogenic acid.

Antioxidant activity was evaluated by the degree of inhibition of malondialdehyde formation (Yu.A. Vladimirov et al. 1972). The calculation of the concentration of malondialdehyde in the homogenate was carried out according to the formula:

$$\underset{\_}{\begin{array}{l}\mathrm{FROM}=\frac{(D_{\mathrm{one}}-D_2)*U_2*U_3}{\Sigma *\mathrm{one}*P*U_{\mathrm{one}}*10}\\ mm\mathrm{about}lb/g\end{array}}$$

where D ₁ is the optical density of the sample with a homogenate; D ₂ - optical density control; U ₁ - the volume of homogenate taken for determination, ml; U ₂ - the final volume of the mixture, ml; U ₃ - total homogenate volume, ml; P - tissue sample, g; l is the length of the cell, cm; Extinction coefficient of Σ 156 mM ^-1 cm ^-1; 10 - conversion factor in ml.

As reference drugs, widely known drugs with antioxidant effects were used: Red Root Drops (Russia, Biysk), 1% Emoxipin (eye drops). Alpine penny has the highest antioxidant activity - 83%. The results are presented in table 2.

table 2 Comparative characteristics of antioxidant activity of drugs A drug D λ = 532 nm With _MDA , mol / g MDA inhibition% Alpine penny 0.1 * 0,0004 83 Drops "Red root" (Russia, Biysk) 0.22 * 0.00115 51 Emoxipin 1% (eye drops) 0.24 * 0.0013 45.7 Control 1 0.43 0,00235 - Control 2 0,03 - - control 1 - with tissue homogenate; control 2 - without tissue homogenate; * - the difference is significant compared with the control P <0,01.

The proposed phytopreparation from Alpine penny grass, which has a cardioprotective effect, as well as high antioxidant activity, is promising for the prevention and treatment of cardiovascular diseases.

Since the claimed invention provides a technical result, expressed in the creation of a new phytopreparation having cardioprotective and antioxidant effects, and can be used for serial production of a medicinal product from plant materials of Alpine penny grass (Hedysarum alpinum), meets the criterion of "industrial applicability".

Analogs

Item 2180584, Item 2130314, Item 2402344, Item 2002101609 Item 22238747

p.2169481, p 93014335, p.2057799

Bibliography

1. Vladimirov, Yu.A. Lipid peroxidation in biological membranes / Yu.A. Vladimirov, A.I. Archakov. - M .: Nauka, 1972.- 252 p.

2. Guidance on the experimental (preclinical) study of new pharmacological substances / under total. ed. prof. RU. Khabrieva. - M.: Publishing House Medicine, 2005. - 832 p.

Claims (1)

A cardioprotective and antioxidant agent, characterized in that it is obtained by extracting the ground grass of Alpine cepa (Hedysarum alpinum) in three stages with water-alcohol solutions with periodic shaking at room temperature in a dark place, and the first fraction is obtained after processing the starting material with an aqueous-alcohol solution in a ratio of 2: 1 for 8 days, the second is obtained by treating the rest of the grass with an aqueous-alcoholic solution in a ratio of 1: 1 for 6 days, the third fraction is obtained with a sample Botko vegetable raw residue hydroalcoholic solution in a ratio of 1: 2 for 5 days, then the fractions were pooled and dried in a thermostat at 37 ° C.