Hepatoprotective agent

FIELD: medicine, pharmaceutical industry.

SUBSTANCE: invention relates to agents used for treatment of chronic hepatitis. The hepatoprotective agent representing extract prepared from biomass of Maackia amurensis Rupr. et Maxim and obtained by the callus culture method comprises polyphenolic complex consisting of daidzein, retusin, genistein, formononetin, maackianin and medicarpin. The hepatoprotective agent promotes to effective treatment of chronic hepatitis.

EFFECT: valuable medicinal properties of agent.

2 tbl

 

The invention relates to medicine and pharmacology, and relates to assets that can be used for the treatment of chronic hepatitis.

Known hepatic vegetable origin, such as LIV-52, Kateryn, Zelibor. Currently, the most widely used drug Carsil (synonyms: Legalon, Silymarin, Silibinin), obtained from the seeds of the Thistle, which is similar to the national drug Celebra [1].

However, treatment with these drugs in some cases there is a low therapeutic efficacy, and the presence of these drugs have various side effects [2, 3].

Closest to the proposed hepatoprotective tool is hepatoprotector Maxar representing a dry extract from the trunk wood of maackii Amur. It has a higher efficacy in the treatment of chronic hepatitis compared with drug Carsil and no side effects [4].

However, Maxar obtained from wood of the plant make Amur (Maackia amurensis Rupr. et Maxim)related to rare species. Recursivedescribe studies show that intensive harvesting of wild medicinal plants lead to widespread depletion of their reserves, the extinction of populations and some species of plants, so the search for alternative the positive raw sources is an important issue. Currently, the development of biotechnology (cell cultivation with the aim of obtaining biologically active substances) allows to solve the problem.

The objective of the invention - expanding Arsenal of hepatoprotective funds.

The problem is solved by creating a new hepatoprotective based tools extract Maackia amurensis and represents an extract of biomass Maackia amurensis Rupr. et Maxim, obtained by the method of culture of calli, and contains polyphenolic complex, consisting of daidzein, retsina, genistein, formononetin, maceina, medicarpin.

Culture calli plants Maackia amurensis Rupr. et Maxim was obtained as follows: explants of different parts of the plant Maackia amurensis Rupr. et Maxim placed in an Erlenmeyer flask with a volume of 230 ml containing 50 ml of nutrient agar medium of the following composition, mg/l water:

NH4NO3350-450

KNO31500-2300

To2NRA4150-190

CaCl2×6H2O 600-730

MgSO4× 7H2O 350-390

H3IN4of 4.2 to 8.0

MnSO4× 4H2O the 15.6-26,7

CuSO4× 5H2About 0,02-0,03

CoCl2× 2H2O 0,02-0,03

ZnSO4× 7H2O to 6.0 and 10.3

Na2MoO4× 2H2O 0,2-0,3

KI 0,52-0,90

FeSO4× 7H2O 25,0-30,6

Na2EDTA× 2H2O 33,6-41,0

Metainit 80-120

Thiamine hydrochloride 0,15-0,25

Nicotine KIS the PTA 0,4-0,6

Pyridoxine hydrochloride 0,4-0,6

6-Benzylaminopurine 0,45-0,55

α -Naphthyloxy acid 1,5-2,5

Casein hydrolysate 40-60

Sucrose 24000-26000

Agar 5800-6200

Water to 1 liter

pH of 5.6 to 5.8 before autoclaving

The explants incubated for 30 days in the dark at 25° C. Formed on the explants, the calli are separated and cultured in the medium of the same composition within ten passages at monthly intervals to stabilize the biosynthetic activity of the calli. Then calli removed from the culture vessel and dried in a current of hot air at 50-55° C.

Dried calli treated with 95%ethanol at 50-55° ratio of raw material:extractant is 1:5 in the battery percolation followed by evaporation and drying alcohol extracts under vacuum. The resulting powder dark brown color is a preparation containing a complex of polyphenols, which are analyzed by high performance liquid chromatography.

Chemical and pharmacological studies of the drug from calli of maackii Amur conducted in comparison with a drug Maxar of wood maackii Amur (PKM-CORES).

Chemical study of polyphenolic complex contained in the calli of maackii Amur (PKM-CL), showed that the composition was significantly different from ifeeling complex, contained in the extract from the trunk wood of maackii Amur. It is established that culture calli of maackii Amur does not contain unlike wood plants stilbene, namely piceatannol and resveratrol. In addition, unlike native plant derived callus culture is not producing the stilbene and dimeric stilbene, while the polar fractions of extracts of wood maackii Amur contain up to 30% oligomeric stilbene (Scirpus And, Scirpus, meakin, makin A) [5-7], as well as stilbenoids macolin [7] and isoflavonones maciain [8]. However, the calli synthesize more than in the plant, the amount of isoflavones (retsina, genistein and formononetin) and, especially, pterocarpus (maceina and medicarpin) (table 1).

Table 1

The composition of polyphenols wood and calli of maackii Amur (mg/g dry weight)
ComponentsPiceatannolResveratrolDaidzeinRetuinGenisteinFormononetinMaciainMedicarpin
Wood6.32±

0.52
6.10±

0.18
traces1.15±

0.06
1.92±

0.23
1.15±

0.19
0.35±
/br> 0.06
0.28±

0.05
The calli--0.52±

0.18
0.91±

0.34
2.53±

0.42
4.23±

1.01
5.78±

1.94
2.68±

0.45

Total polyphenol content in wood and calli was 17.3±0,18 and 16.7±0.27 mg/g dry weight, respectively. Thus, the calli of maackii accumulate comparable with wood maackii Amur amount of polyphenols. But there are significant differences both in structure and in the ratio of polyphenols, synthesized by calli of maackii Amur and wood of this plant. So it was impossible to clearly suggest that polyphenolic complex calli Maackia amurensis Rupr. et Maxim will possess hepatoprotective activity, like polyphenolic complex wood Maackia amurensis Rupr. et Maxim.

Study the hepatoprotective activity of the drug calli of maackii conducted on a group of laboratory mice, which were called artificial hepatitis action of carbon tetrachloride (CCl4) (table 2).

Table 2

Hepatoprotective activity of polyphenolic complex maackii derived from callus culture, compared to the complex, isolated from the trunk wood, when the CL 4-hepatitis in mice
The experimental group

Indicators
Intact animalsCCl4-hepatitisCCl4-hepatitis + (PKM-CORES)CCl4-hepatitis + (PKM-CL)
Mortality, %03312,50
Change of body weight, g+0,95±0,24-1,63±0,97a-1,15±0,75aof 1.13±0,64and
Unit weight of liver mg60,6±3,378,3±3,9and66,0±5,770,6±2,6and
Duration geksenalovy sleep, min18,5±0,970,2±2,2and40,5±2,4a,b45,3±3,0a,b
Fatty liver, points0±03,0±0a2,1±0,33a,b1,9±0,22a,b
Note: (M± m, average of 6-8 observations), p<0.05 with respect to:and- to intact animals;b- CCL4-hepatitis

As a result of these studies found that on the seventh day of the experiment the animals had developed a pronounced CCL4-hepatitis, which was characterized by a fourfold increase in the length geksenalovy with whom and, testifying about the inhibition of the activity of liver microsomal enzymes. Against lowering the body weight by the end of the experiment at 30% increased specific gravity of the liver. The degree of fatty infiltration of hepatocytes meet on a scale of 3 points. Death in the group of mice with induced hepatitis was 33%. Mortality in the group of mice treated with the drug from the trunk wood, was 12.5%. In the group of animals treated with the drug from the culture of calli, mortality was not observed. Both drugs significantly (more than 50%) reduced the duration geksenalovy sleep and the degree of fatty hepatocytes (up to 1.9-2.1 points), marked by a more moderate value of the specific mass of the liver. Thus, the results obtained indicate the presence of pronounced hepatoprotective properties of polyphenolic complex isolated from cell culture of maackii Amur. This polyphenol complex from the culture of calli of maackii Amur has a more pronounced pharmacological activity.

Simultaneously pharmacological studies carried out on rats with induced CCL4-hepatitis. The results revealed that the drug of sound wood in a dose of 150 mg/kg (previously established optimal effective dose) prevents hyperlipidemia and hyperbilirubinemia, reduces the activity of alanine and participantcentered, and alkaline phosphatase. The preparation of callus culture has equal effect with the drug of sound wood in its application in a smaller dose, 100 mg/kg of the drug from callus culture is logged tendency to a more pronounced normalizing influence on higher toxicant concentration of lipids in blood serum. Therefore, the effective dose from callus culture in 1.5 times lower than the effective dose of sound wood that is obviously due to the higher content of biologically active substances in the product obtained from callus culture.

Thus, pharmacological studies of the drug callus culture Maackia amurensis has shown that he has a significant hepatoprotective effect.

LITERATURE

1. Yakovenko AP etc. the Effectiveness of therapy in patients with chronic hepatitis with hepatic // materials of the final scientific and practical conference “problems of clinical medicine, Ministry of health of the RSFSR, M., 1989, s-231.

2. Grigoriev PA and other “Diagnosis and treatment of chronic hepatitis and cirrhosis of the liver” // Soviet medicine, 1985, No. 12, pp.61-67.

3. Blinkov I. and other clinical Experience hepatoprotective tools legalon // Symposium : Clinical significance of drug legalon”, M, 1981, p.113-123.

4. RF patent №2175237 AND K 35/78, A 61 P 1/16, 2001.

5. Chem. nature. Conn., 1988, No. 6, s-804.

6. Chem. nature. Conn., 1992, No. 5, s-476.

7. Phytochemistry, 1995, vol.40, No. 3, p.1001-1003.

8. Chem. nature. Conn., 1986, No.1, p.39-42.

Hepatoprotective agent based on the extract of Maackia amurensis, characterized in that it is an extract of biomass Maackia amurensis Rupr. et Maxim, obtained by the method of culture of calli, and contains polyphenolic complex, consisting of daidzein, retsina, genistein, formononetin, maceina, medicarpin.



 

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