Biologically active drug - oil moronica

 

(57) Abstract:

Biologically active product contains the extract of roots and rhizomes of plants of the genus Hellebore (Helleborus), represents at least the amount of lipids from these parts of the plant and at least contains, wt%: free fatty acid 50-70, diol lipids to 2.5, esters Starinov to 1.2, esters of fatty acids up to 3, triacylglyceride to 7, a hydrocarbon of up to 10. The invention allows to obtain a tool with including antitumor effect. 12 C.p. f-crystals.

The invention relates to the field of pharmacology, and relates to biologically active compounds from plant material, which, on the one hand, can be used as biologically active food supplements as a nonspecific measure to increase the body's resistance to adverse influences, prevention of morbidity and normalize the functioning of the body, and on the other hand, can be used as the basis for medicines, in particular for the treatment of cancer.

Know the use of powder from a plant of the genus hellebore slimming (newspaper "Arguments and facts", 2001, 27, p. 16).

However, cardiac glycosides of moronica tend to accumulate in the body and cause toxic effects (newspaper "Arguments and facts", 2001 , 27, p. 16).

On the other hand, it was found that in the rhizomes and roots of moronica contains up to 15% of lipids.

The proposed biologically active drug - oil moronica is new and has no analogues.

The proposed product contains the extract (the extract from the roots and rhizomes of plants of the genus Hellebore (Helleborus), representing at least the amount of lipids contained in these parts of the plant.

While specified extract at least contains, wt%: free fatty acid - 50-70, diol lipids to 2.5, esters of sterols to 1.2, esters of fatty acids of up to 3, triacylglyceride to 7, a hydrocarbon of up to 10.

As fatty acids specified the extract contains at least linoleic, oleic, palmitic and stearic, and esters of fatty acids - alevai acid 30-55, oleic acid - 3-6, palmitic acid - 3-7, stearic acid - 0,35-1,1, methylvalerate - 0,002-0,006, aterballetto - 0,006-0,012, merlinoite - 0,5-0,93, ethyllinoleate - 1,2-2,1.

The biologically active agent may optionally contain vegetable oil, and it contains the following ratio of components, wt.%: the specified extract - 0,05-30, oil - rest.

For the implementation of political action on the plasma membrane of tumor cells it contains preferably the following ratio of components, wt.%: of the extract is 0.05 to 10.0, vegetable oil - the rest.

For external use biologically active agent preferably contains the following ratio of components, wt.%: the specified extract - 3-10, vegetable oil - the rest.

Biologically active drug as a food Supplement preferably contains the following ratio of components, wt.%: of the extract is 0.3 to 1.5, vegetable oil - the rest.

The proposed biologically active product is a viscous liquid yellowish-brown color, having a density of 0.9-0,965, a refractive index of 1.45 to 1.48 and sour is cennych roots and rhizomes organic solvent, able to extract the fats, with constant stirring, followed by infusion of a mixture of the above ground roots and rhizomes with an organic solvent, separating and discarding the precipitate and the final product after the distillation of the organic solvent from the supernatant.

As the organic solvent take petroleum ether.

In the case of use as a solvent petroleum ether, the roots and rhizomes and petroleum ether charge / mass ratio of 1: 1-4, the processing of petroleum ether are within 1-3 hours, and the insistence within 2-4 hours.

For the qualitative chemical composition analysis of the obtained extract was used thin-layer chromatography (TLC), preparative thin-film chromatography, with subsequent analysis by gas chromatographs.

Was installed the following chemical composition of the oil of moronica.

The total composition, wt.%:

Free fatty acid - 50-70

Diol lipids - 0,7-1,8

Esters of sterols - 0,5-1,0

Esters of fatty acids - 2-3

Triacylglyceride - 5-7

The composition of the fraction of free fatty acids, wt.%:

Linoleic - 65-75

ABOUT THE R>
Methylpyrimidin - 1-2

Etisalat - 3-4

Meilleret - 25-31

The ethyllinoleate - 60-70

It was also established that the proposed product contains 1,2-(2,3-)-diacylglyceride, derivatives of ethylene glycol, butanediol-2,3, butanediol-1,2, propane diol-1,3.

Glycosides were not detected.

The invention is illustrated by the following example.

Took air dried, ground roots and rhizomes of moronica Caucasian (Helleborus caucasicus), put them in the extractor and filled with petroleum ether in a weight ratio of vegetable raw material:ether 1:2. Carried out the extraction of the final product when mixing the crushed material with petroleum ether for 2 hours. Then the mixture was pressed within 3 hours, after which the supernatant was filtered and collected. The precipitate was discarded. Then petroleum ether drove from the supernatant completely. The distillation was produced using a rotary evaporator, which is a flask fitted with a refrigerator and furnished with the heater. After distillation, petroleum ether the extract obtained was passed the night without stirring. The whole process of oil extraction was conducted at room temperature.

Received extreme of 1.46 and an acid number of 160.

For the qualitative chemical composition analysis of the obtained extract was used thin-layer chromatography (TLC), preparative thin-film chromatography, with subsequent analysis by gas chromatographs.

Was installed the following chemical composition of the oil of moronica.

The total composition, wt.%:

Free fatty acids - 65

Diol lipids - 1,6

Esters of sterols - 1,0

Esters of fatty acids - 3

Triacylglyceride - 6

Unidentified balance - Rest

The composition of the fraction of free fatty acids, wt.%:

Linoleic - 72

Oleic - 8

Palmitic - 9

Stearic - 1,0

Unidentified free fatty acids - Rest

The composition of the fractions of fatty acid esters, wt.%:

Methylpyrimidin - 1,8

Etisalat - 3,2

Meilleret - 27

The ethyllinoleate - 68

Researched lytic effect on the plasma membrane of tumor cells offer a product containing 20 wt.% of the extract and 80 wt.% vegetable (olive) oil. Took antiseptic cells following strains: tumors of the ovary of the rat (HHS), of Ehrlich ascites carcinoma (era) and sarcoma - 37" mice, to which was added the MCA is ivali after 5-minute incubation of tumor cells with 20% oil moronica. These phenomena represented the formation of micro bubbles and blisters on the periphery of the cells, swelling and rarefaction of the cytoplasm, increase the motility of cytoplasmic inclusions. In further observed generalized edema tumor cells and the appearance of bare nuclei, indicating lysis of the plasma membrane.

Adding to tumor cells of the indicated strains of the drug containing 0.05% oil moronica and 99.95% of olive oil, substantially violated the transport function of the plasma membrane, as evidenced by the fact that after removing the effect of 0.05% drug intracellular ion content K+recovered within 60 minutes only to 1/2 of the original level after exposure to 0.1% drug intracellular ion content K+recovered within 60 minutes only to 1/4 of the original level, and after exposure to 0.2% drug intracellular ion content TO+were not recovered. It was found that the normal (non-tumor and healthy cells remain intact. Thus, the proposed drug acts selectively.

Investigated the influence of the oil moronica on the sensitivity of the oil moronica a concentration of 0.5% and irradiated their x-rays at a dose of 3000 RUB. Served as control cells not treated with oil moronica and irradiated by x-rays in the same dose. Then the test and control cells was administered to experimental animals (laboratory mice, rats) and counted the number of grafted tumors in the experiment and the control.

In that case, when cultivated in tumor cells treated with oil moronica and x-ray radiation, tumors developed only 20% of animals, while in the control tumors developed in 80% of vaccinated animals.

In a similar experiment with cells of Ehrlich ascites carcinoma and in control, and in the experience of the tumor developed in the same number of animals. However, the observation of subsequent development (increase of liquid volume and mass ascitic cells) tumors derived from cells treated with oil moronica and x-ray irradiation (experience), and tumors derived from cells treated only by x-ray irradiation (control) showed that the development of experimental tumors was significantly delayed compared with the control tumors. Thus, the oil moronica significantly increases the sensitivity of tumor cells to x-irradiation.

Was studied distiibution laboratory mice and rats), then on humans of different age groups. It was found that for overall health, the best option is 1% concentration in a dose of at least 1 g per day.

After taking the oil of moronica within 1 month quality improvement of health said 70% treated his patients. It was noted overall improvement in body tone, reduction of excess weight, normalization of the functions of the gastrointestinal tract, in blood pressure. There was also a slowdown in the development of some inflammatory processes.

The proposed product containing 0.3 to 1.5% of the extract, the rest to 100 vegetable oil, such as olive or sunflower oil can be used as an additive to food intended for the prevention of diseases associated with metabolic disorders, and in the complex therapy of neoplastic diseases.

5% oil solution of oil of moronica can be used for outdoor applications, including in the treatment of cancer.

Negative consequences associated with the accumulation in the body, cardiac glycosides, is not mentioned in connection with the complete absence of the latter in the proposed biologically and stenia kind of Hellebore (Helleborus), characterized in that the extract of at least contains, wt%: free fatty acid - 50-70, diol lipids to 2.5, esters of sterols to 1.2, esters of fatty acids of up to 3, triacylglyceride to 7, a hydrocarbon of up to 10.

2. Biologically active drug under item 1, characterized in that the extract contains as fatty acids at least linoleic, oleic, palmitic and stearic, and esters of fatty acids is at least metallurgical, Etisalat, meilleret and ethyllinoleate.

3. Biologically active drug under item 2, characterized in that the extract contains, wt %: linoleic acid 30-55, oleic acid 3-6, palmitic acid 3-7, stearic acid 0.35-1,1, methylvalerate 0,002-0,006, aterballetto 0,006-0,012, merlinoite 0,5-0,93, ethyllinoleate 1,2-2,1.

4. Biologically active drug under item 1, characterized in that it further comprises a vegetable oil.

5. Biologically active drug under item 4, characterized in that it contains the following ratio of components, wt.%: of the extract of 0.3-30, oil - rest.

6. Biologically active drug under item 5, characterized in that for assests is it the ratio of the components, wt.%: the specified extract 15-30, vegetable oil - the rest.

7. Biologically active drug under item 5, characterized in that for external application, it preferably contains the following ratio of components, wt.%: the specified extract 3-10, vegetable oil - the rest.

8. Biologically active drug under item 5, characterized in that for food additives it contains preferably the following ratio of components, wt.%: the specified extract 0.3 to 1.5, vegetable oil - the rest.

9. Biologically active drug under item 1, characterized in that it is a viscous liquid yellowish-brown color, having a density of 0.9-0,965, a refractive index of 1.45 to 1.48 and an acid number of from 120 to 180.

10. Biologically active drug under item 1, characterized in that it is obtained from Moronica Caucasian (Helleborus caucasicus).

11. Biologically active drug under item 1, characterized in that it is obtained by processing these roots and rhizomes, taken in powdered form, an organic solvent with constant stirring, followed by infusion, by separating and discarding the precipitate and distillation of the organic solvent.

12. The biological is roform, or petroleum ether or carbon tetrachloride.

13. Biologically active drug on p. 11, characterized in that the roots and rhizomes and petroleum ether charge / mass ratio of 1 : 1 to 4, the processing of petroleum ether are within 1-3 h, and the insistence within 2-4 hours

 

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