The method of obtaining geniatulin with holocaustmuseum action

 

(57) Abstract:

The invention relates to the field of medicine. Raw materials - goricanec bearded extracted with ethyl alcohol containing 1-2% HCl at boiling. The extract is evaporated and the amount Kantorovich aglycones extracted with chloroform. Chloroform extract chromatographic on a column of silica gel, and evaporated. Fallen technical gentianales purified by recrystallization from methyl alcohol. The invention improves the product yield. 3 table.

The invention relates to the field of medicine and relates to a method of obtaining biologically active compounds from plant material with holocaustmuseum action.

A method of obtaining Geniatulin 1,7-dihydroxy-3,8 - dimethoxyethane from the aerial parts of Swertia japonica and S. chirata, which has antiviral and anti-TB activities, by extraction of raw materials methyl alcohol, chromatography was carried out amount extraction columns on polyamide and silica gel. The output is 0.1% by weight of the feedstock [Komatsu M. , T. Tomimori , Mikuriga N. japan 7127, 558 ser. 2 Sat. 3288. C1 01 D A 61 K C 07 d; Komatsu M" T. Tomimori 01. 02. 69 7127, 558 C1 01 d A 61 K; Taisho Pharmacephtical Co Ltd] . In addition, there is also known a method of obtaining gentical chromatographic on a column of silica gel. Output Geniatulin is 0.5% by weight of the feedstock [Soloviev, E. C. , Denisova O. A. , Glyzin Century. And. , Paladin A. C. Ksenonovye connection Swertia connata schrenh // Chemistry of natural compounds. - 1980. -N-6, a - C. 840 - 841] . The disadvantages of these methods are low yield of the target product, the duration and the complexity of the technological process (multiple extraction and low yield of the target product).

The closest technological essence and the achieved result is a method of obtaining Geniatulin of S. connata, namely, that the aboveground part is extracted with ethanol, the ethanol extract evaporated and fractionary chloroform, ethyl acetate and butanol. Chloroform extract chromatographic on a column of silica gel and get gentianales. The output is 0.5% by weight of the feedstock [Soloviev, E. C. , Denisova O. A. , Glyzin Century. And. , Paladin A. C. Ksenonovye connection S. connata sclrenh // Chemistry of natural compounds. - 1980. -N-6. - S. 840-841] . The disadvantage of this method is the low yield of the target product.

The objective of the proposed method is to increase the yield of the target product from the aerial parts of Gracanica bearded with holocaustianity activity and Stragiht 95% ethanol, containing from 1 to 2% of hydrochloric acid at boiling, evaporation of the combined extracts and extract Kantorovich aglycones chloroform. The chloroform extract after evaporation and chromatography was carried out on a column of silica gel with elution by chloroform allows you to get the finished product with increased output up to 1.5%. This method leads to increased output of finished product 2 times, having the characteristics presented in table. 1.

The following examples illustrate the inventive method.

Example 1. 100 g chopped vozdushno-dry grass part of Gracanica bearded pour 300 ml of 70% C2H5HE + 25 ml HCl (1%) three times by heating for 2 hours. The combined extract was filtered and evaporated to 400 ml, add 100 ml of water and extracted in a separating funnel with chloroform in a 1 l three times (three times). The combined chloroform extract evaporated to dryness. The output of the sum Kantorovich aglycones - 18,7, Chloroform extract is applied on a column of silica gel L 40/100 and elute with chloroform. In 1300 ml of chloroform is secreted substance gentianales, the end of the elution 1600 ml. Fractions are collected, evaporated to dryness, add 20 ml of 95% alcohol. The precipitate technical Geniatulin filtered and paracrystals the/SUP>C in the refrigerator). The precipitate is filtered off, dried in an oven at 100-105oC for 3 hours. Get 1.50 g Geniatulin that is 1.5% by weight of the feedstock.

The use of the proposed method in comparison with known enhances the yield of the target product from 0.5% to 1.5%.

Example 2 100 grams of powdered air-dried grass Gracanica bearded pour 350 ml of 95% C2H5OH+30 ml HCl (2%) three times by heating for 2 hours. The combined extract was filtered and evaporated to 400 ml, add 100 ml of water and extracted with chloroform 1 l (three times). The combined chloroform extract evaporated to dryness. The output of the sum of aglycones and 17.6 G. of Chloroform extract is applied on a column of silica gel L 40/100 and elute with chloroform. In 1300 ml of chloroform is secreted substance gentianales, the end of the elution 1600 ml. Fractions are collected, evaporated to dryness, add 20 ml of alcohol. The precipitate technical Geniatulin filtered off and recrystallized from ethanol (dissolved in 300 ml evaporated to 100 ml and left for crystallization at 10 hours at a temperature of 2-4oC in the refrigerator). The precipitate is filtered off, dried in an oven at 100-105oC for 3 hours. Obtain 1.20 g vydelennogo GENIATULIN.

Definition choleretic action Geniatulin conducted on 60 white rats of both sexes weighing 180-200 g by the method of N. P. Steed, A. N. Oleinik [Racer N. P. , Olejnik A. N. Comparative effects of atropine and metacin on the exocrine function of the liver //Pharmacology and toxicology. - 1967. - So 30. - N 3. - S. 334 - 337] . The animals were housed for 5 hours under General anesthesia (1% aqueous solution of Barbara in the amount of 1 ml per 100 g of animal) at room temperature. Bile was collected using a special cannula that is inserted in the common bile duct, through every hour. Gentianales studied at doses of 10, 50, 100 mg/kg to Rats of the control group was administered distilled water in equiano number. The degree choleretic action of the investigated tools to be judged by the rate of secretion of bile, the total volume and the number of allocated each time a portion of bile cholesterol [drogbas S. M. Comparative study and action features Zelenih drugs on zheleobrazovatel the function of the liver in norm and pathology. The dissertation of the doctor of medical Sciences. - Kharkov. - 1972. - 34 S. ] , bilirubin [Racer N. P. Neurohumoral mechanism choleretic action of insulin // problems of endocrinology and germinate the Holevo and desoxycholate) bile acids [Karbach Ya I. Quantitative determination of bile acids in bile and blood using chromatographic method // Biochemistry. - 1961. - So 26. - N2. -S. 305-309. ] . The obtained data statistically processed using the t-student criterion [Montevista-öhringen E. C. Simplified mathematical-statistical methods in medical research // Pathological physiology and experimental therapy. - 1964. -N 14. - S. 71-78] . The definition of ED50Geniatulin conducted according to methods described Ivanov, Y. I. , Pogorelec O. N. [Ivanov Y. I. , Pogorelec O. N. Statistical processing of the results of biomedical research in the calculators. - M. : Medicine, 1990. - 224 S. ] .

It is established that the introduction Geniatulin at a dose of 10 mg/kg had no significant effect on the choleretic response in rats (table. 2). Marked only the increased concentration in the bile of animals bilirubin 74% and showed a tendency to increase the excretion of cholesterol and stimulation of the synthesis of bile acids. Against this background, in the spectrum of individual bile acids were increased share conjugated, and unconjugated of Khalatov (PL. 3). Gentianales dose of 50 mg/kg had a mild choleretic effect when the introduction is 15% compared with the control. Then choleretic response in rats tended to increase and only 4 hours after injection Geniatulin increased by 11% compared with the control. This increased the total number of selected bile, and accelerated excretion of bilirubin. Gentianales in the dose stimulated the synthesis and secretion of total bile acids concentrations in bile increased almost 1.5 times compared with the control. When analyzing the spectrum of individual bile acids, gentianales the most significant impact on the synthesis of conjugated bile acids (table. 3). Increasing the dose of the investigated xanthone to 100 mg/kg there were no recorded changes choleretic response in rats. Gentianales contributed to the acceleration of excretion of bilirubin by 40% and excretion of cholesterol (table. 2). At the same time a moderate stimulation of synthesis and secretion of total bile acids due to the increase in the spectrum of individual bile acids only of conjugated Khalatov (PL. 3). Based on these data, gentianales has holocaustmuseum action.

It is established that ED50Geniatulin corresponds to 31.5 5.9 mg/kg of body weight.

The method of obtaining Geniatulin with colatosti ODI chloroform and separation adsorption chromatography, characterized in that the quality of plant raw materials used goricanec bearded, the extraction was carried out with a solution of ethyl alcohol containing 1-2% hydrochloric acid at boiling, and after treatment with chloroform re-evaporation.

 

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FIELD: medicine, cardiology, phytotherapy, pharmacy.

SUBSTANCE: invention relates to the field in development of an agent of vegetable origin used for improvement of the functional state and prophylaxis of organic alterations in cardiovascular system, in particular, atherosclerosis. The biologically active supplement used for prophylaxis of cardiovascular diseases, in particular, atherosclerosis comprises clover dry extract, haw-thorn flowers powder, ascorbic and nicotinic acids, and accessory substances taken in the definite ratio. The biologically active supplement is made in the form of tablet or capsule. No adverse responses observed in intake of the supplement. The blood cholesterol level was reduced to the normal value in 68% of patients and reducing morbidity with acute respiratory-viral infections has been noticed. In patients with ischemic heart disease with cholesterolemia the improvement of the state is noted on the background of conventional therapy: the moderate reducing the arterial pressure value in its elevation, improved in the state of health, enhanced working capacity, reduced retrosternal pains, ear noise, vertigo, headache.

EFFECT: valuable medicinal properties of supplement.

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