Medicine of antioxidant action

FIELD: medicine; pharmaceutical industry.

SUBSTANCE: medicine of antioxidant action is powder extract of aerial dropwort (Filipendula vulgaris Moech), made by standard extraction of aerial dropwort under specified conditions. Powder extract contains specified number of flavonoids and coumarins as active agents.

EFFECT: improved antioxidant action.

1 tbl

 

The invention relates to medicine, specifically to clinical pharmacology, and can be used for pharmacological correction of free radical pathology.

Well-known medicinal product with antioxidant action, dihydroquercetin, vitamins (ascorbic acid, tocopherol acetate, retinol acetate) and their analogues, other [1, 2]. Therapeutic efficacy (the ability to inhibit free radical oxidation at different stages of the process) of these antioxidants in the treatment of free radical pathology is not high enough.

Closest to predlagamom is a drug with antioxidant effect, obtained from the aerial parts of meadowsweet, containing flavonoids [3].

A new technical task is the expansion of the means of plant origin with a more pronounced antioxidant effect.

The task to solve a new tool that has an antioxidant effect, representing the dry extract of the aerial parts of Filipendula ordinary (Filipendula vulgaris Moech)obtained in 95% ethanol and containing not less than 2.2% flavonoids and 0.54% of coumarins.

Meadowsweet ordinary (Filipendula vulgaris Moech) is a perennial herbaceous plant that grows in steppe dry meadows, rocky slopes, ratrie the different forests of the South of the European part of Russia, Western and parts of Eastern Siberia, in the Altai [4, 5]. In folk medicine the plant is used as astringent, anti-inflammatory, wound healing and hemostatic agent. Rhizomes and roots meadowsweet common part of the collection of recipes Minstance, which is used as a symptomatic remedy for bladder papillomatosis and antacid gastritis [6, 8]. As a result of studying the chemical composition of the aerial parts of the plant using chemical reactions, chromatography in thin layer and paper, spectral methods, we detected the presence of the following groups of biologically active substances: flavonoids (luteolin, apigenin, quercetin, dihydroquercetin, avikulyarin, isoquercitrin) - 1,72±0,09%, in terms of quercetin; coumarins (coumarin, umbelliferone); phenol carbonic acids (Gallic, gentisic); tannins hydrolyzable groups in the number of 3.23±0,36%; triterpene saponins, polysaccharides composed of D-glucose, D-galactose and D-glucuronic acid - 1,47±0,014%; carotenoids and amino acids.

Antioxidant action of the extracts of the herb are not described in literature. The development of a new tool, has an antioxidant effect, is made possible through the identification of experimentally its new properties and composition, namely the ability to normalize disbale the relationship with systems of free radical oxidation and total antioxidant activity in the body due to the antioxidant action contained complex of biologically active substances, including flavonoids and coumarins.

As shown by experimental studies, our proposed tool - extract of Filipendula vulgaris, obtained in 95% ethanol, has superior antioxidant action infusion of flowers of meadowsweet. In addition, our studies revealed that the extract of Filipendula vulgaris, obtained in 95% ethanol, greater than for the proposed action is similar to the extract of meadowsweet. Thus, the use of the proposed tools will lead to an expanding Arsenal of antioxidant agents of plant origin used in clinical practice.

With this in mind you should consider the claimed solution meets the criterion of "significant differences".

A new kind of activity identified on the basis of the conducted research and experimental research. The study was subjected to aqueous and aqueous-ethanolic extracts(40%, 70%, 95%) aerial parts meadowsweet common. Standardization of the extracts was carried out according to the content of flavonoids [9] and coumarins [10] is the most important group of active complex aerial parts meadowsweet ordinary.

Investigated the antioxidant effects of extracts from the aerial parts (stems, leaves, flowers) Filipendula vulgaris, obtained in the following ways :

Example . The aboveground part (stems, leaves, flowers) meadowsweet common Filipendula vulgaris Moech collected during the flowering and dried air way, pulverized and sieved through a sieve with the hole diameter of 2 mm (moisture content of 7.4%). 50 g of crushed raw material is placed in a glass flask, pour 500 ml of purified water and heated at a temperature of 85°With water bath under reflux for 30 minutes the resulting extract is filtered, raw press. The extract is evaporated under vacuum at a temperature not above 60°With dryness. Output (table 1) dry extract of 7.25 g, which is 14,50% by weight of the feedstock (water extract). The content of flavonoids in dry extract amounted to 0.56%, coumarins - 0,16%.

Example 2. The aboveground part (stems, leaves, flowers) meadowsweet common Filipendula vulgaris Moech collected during the flowering and dried air way, pulverized and sieved through a sieve with the hole diameter of 2 mm (moisture content of 7.4%). 50 g of crushed raw material is placed in a glass flask, pour 500 ml of 40% ethanol and heated at a temperature of 85°With water bath under reflux for 40 minutes, the Obtained extract was filtered, raw press. The extract is evaporated under vacuum at a temperature not above 60°With dryness. The yield of dry extract 8,71 g, which is 17,42% by weight of the feedstock (extract 40% ethanol). Soda is the content of flavonoids in dry extract was 1.65%, coumarins - 0,25%.

Example 3. The aboveground part (stems, leaves, flowers) meadowsweet common Filipendula vulgaris Moech collected during the flowering and dried air way, pulverized and sieved through a sieve with the hole diameter of 2 mm (moisture content of 7.4%). 50 g of crushed raw material is placed in a glass flask, pour 500 ml of 70% ethanol and heated at a temperature of 85°With water bath under reflux for 40 minutes, the Obtained extract was filtered, raw press. The extract is evaporated under vacuum at a temperature not above 60°With dryness. The yield of dry extract 11,35 g, which is 22,70% by weight of the feedstock (extract 70% ethanol). The content of flavonoids in dry extract was 1.72%, coumarins - 0,32%.

Example 4. The aboveground part (stems, leaves, flowers) meadowsweet common Filipendula vulgaris Moech collected during the flowering and dried air way, pulverized and sieved through a sieve with the hole diameter of 2 mm (moisture content of 7.4%). 50 g of crushed raw material is placed in the flask, pour 500 ml of 95% ethanol and heated at a temperature of 80°With water bath under reflux for 40 minutes, the Obtained extract was filtered, raw press. The extract is evaporated under vacuum at a temperature not above 60°With dryness. The yield of dry extract 8,30 g, which is 16,60% by weight of the feedstock (extract 95% of et is zero). The content of flavonoids in dry extract was 2.20%, coumarins - 0,54%.

Antioxidant activity of extracts of Filipendula ordinary was determined by cathodic voltammetry [11, 12]. Antioxidants with restorative nature, react with oxygen and its active radicals, which is reflected in the decrease in cathode current of oxygen reduction at a mercury film electrode in potential from 0 to - 0,6 Century

Experimental studies were performed on serial voltammetric analyzer TA-2 ("Technogenetic" Tomsk). Electrochemical studies were carried out in three-electrode cell with the working of the mercury-film electrode, the reference electrode is silver chloride and auxiliary glassy carbon. As a background electrolyte (chosen experimentally) used phosphate buffer pH 6,86 (10 ml). The volume of the aliquot of the sample (C=0.01 g/ml) was 0.1 ml, respectively, the concentration of the sample in the cell - 1·10-4g/ml electrochemical cell used glass cups with a capacity of 20 cm3. The stirring solution was performed using a magnetic stirrer M-25 for 10 s, followed by soothing for 20 sec. For the variation of oxygen concentration in the solution until its complete removal used the nitrogen supplied in RA is creative under pressure through the gas tube. Shoot voltamperes cathodic oxygen reduction in constant-current mode was carried out under the following conditions: scan rate of the potential of 30 mV/s, the range of working potentials 0 - (minus 0.6)C. the Sensitivity of the device was varied in the range 0.4-4 Áa.

Reportedly built the dependence of the relative change of the limiting current of oxygen reduction from time process in the presence of the sample. On the slope of the tangent to the first plot this curve was calculated kinetic criterion To (Ámol/l·min), which reflects the amount of unreacted sample oxygen forms, resulting in the efficiency of interaction of the extract with oxygen radicals, and is determined by the formula:

where Co2the oxygen concentration in the original solution without the sample, is equal to its solubility in an appropriate solvent under normal conditions, Ámol/l;

Ii- the current value of the limiting current of oxygen reduction, MCA;

Ibeg- the value of the limiting current of oxygen reduction in the absence of a sample in solution, MCA;

T - time of the process, minutes

Periodic monitoring of the oxygen content in the solution (Co2) was carried out with help from slobodnog sensor "MAYOR-LIVRO" (Poland).

As Comparators used standard antioxidants - dihydroquercetin (C=0.01 g/ml) and ascorbic acid (C=0.01 g/ml).

The data obtained in the experiment were processed using the program Statistica 5.0.

It was established that the extracts of aerial parts of Filipendula ordinary exhibited antioxidant activity in relation to the process of electroreduction of oxygen, i.e. all samples interact with active oxygen forms. The use of aqueous-ethanolic extracts helps to increase the studied activity. The results of the experiment showed that the strong antioxidant effect has extract of Filipendula vulgaris, obtained in 95% ethanol. Extraction with 95% ethanol aerial parts of the plant significantly increases the antioxidant effect of the target product at the expense of the most complete extraction of biologically active substances (flavonoids, coumarins, phenol carbonic acids, and others), containing the largest number of free phenolic hydroxyl. The decrease in the concentration of ethanol in the extraction of raw materials meadowsweet from 70% to 0% is associated with changes in a unique ratio of biologically active substances. The results of the studies conducted showed that the antioxidant activity of the extract of the aerial parts (stems, Lis the article, flowers of Filipendula vulgaris, obtained in 95% ethanol (0,928±0,034 Ámol/l·min), exceeds the extract of meadowsweet (0,780±0,050 Ámol/l·min) and significantly superior to infusion of flowers of meadowsweet (0,404±0,023 Ámol/l·min), due to the specific chemical structure of the constituent phenolic compounds (flavonoids, phenol carbonic acids, coumarins and other) and their quantitative content. Last, having a hydroxyl with mobile hydrogen atoms, neutralize the gidroperekisi polyene fatty acids, converting them into non-toxic hydroxy acids. Lipophilic phenolic compounds are embedded in the cell membrane and inhibit the formation of primary and secondary products of lipoperoxidation.

The positive effect achieved through the use of as a source of funds to provide antioxidant protection, dry extract of the aerial parts of Filipendula vulgaris, obtained in 95% ethanol, which expanded the Arsenal of drugs of plant origin with antioxidant effect.

Table 1.
Weight and yield of extracts of aerial parts of Filipendula ordinary
ExtractWeight gOutput %
Aqueous extract7,25±0,1314,50±0,02
Extract 40% ethanol8,71±0,1517,42±0,03
Extract 70% ethanol11,35±0,2522,70±0,05
Extract 95% ethanol8,30±0,1116,60±0,01

Literature

1. Shvets P. Free radicals, the etiopathogenesis of diseases and therapeutic effects // Slovakofarma Revue. 1996. - T. VI, issue 4. - P.75-77.

2. Gerchikov YA, ALFIYA Garifullina, Khairullina V.R. Antioxidant efficiency of quercetin in the reaction of the radical - chain oxidation of ethylbenzene // proc. Dokl. VI international. proc. "Bioantioxidants". - Moscow, 2002, S - 109.

3. Pospelov M., Barnaul OD, Alexandrov L.A. Antioxidant activity (AOA) of planetdata flowers of meadowsweet // the Third international. Congress "Actual problems of creation of new medicinal preparations of natural origin". - Saint-Petersburg-Pushkin, 1999, - P.64-66.

4. Cherepanov, S. Kaliev Vascular plants of Russia and adjacent States (the former USSR). - St. Petersburg: World and family-95. - 1995. S.

5. Encyclopedic dictionary of medicines and foods of animal origin / Ed. by G.P. Yakovlev, CYP Blinova. With the b: Special literature, 1999, - S-171.

6. Plants for us. / Ed. by G.P. Yakovlev, CYP Blinova. - SPb: Academic book, 1996. - 664 S.

7. The GES D.K., humpback whale, NV, Chadaev GN. Medicinal plants and their use. - Minsk: Science and technology, 1976, - 592 S.

8. Plant resources of the USSR: Flowering plants, their chemical composition and use; family Hydrangeaceae - Haloragaceae. - Leningrad: Nauka, 1987, - 328 S.

9. Safonov V.V., Sakanyan H., Lesiovskaja E.E. spectrophotometric method for the determination of the content of the amount of flavonoids in medicinal raw materials Caragana spinosa (L) Vahl ex Normen. // Rast. resources. - 2000. - So 36, issue 2. - S. 129-132.

10. Chemezov I.I., Chubarova S.L., Sakanyan H., Kotovsky B.K., Chizhikov A.I spectrophotometric method for quantitative evaluation of polyphenol content in the dry extract of the aerial parts Melilotus officinalis (L.) Pall. and in its dosage form (tabletas) // Rast. resources. - 2000. - T.36, issue 1 - Pp.86 - 91.

11. Thunder V.F., Shapoval G.S., A. I. Luik pulse voltammetry to study the antioxidant activity of physiologically active substances // Himu farm. gurgy - 1974. - V.28, No. 11. - S. 11 - 14.

12. Korotkov H. Voltammetric method for determining the activity of antioxidants, Zh. structural chemistry. - 2000. - T. 79, No. 9. - S. 1704 - 1706.

Means, having an antioxidant effect, which represents the dry extract of the aerial parts of meadowsweet obyknovenny the CSO (Filipendula vulgaris Moech), obtained by extraction of the aerial parts of Filipendula ordinary 95% ethanol at the ratio of raw material to the extractant 1:10, with a dry extract contains 2.2% flavonoids and 0.54% of coumarins as active substances.



 

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