Potassium salt of cauloside c, stimulating reparative regeneration of the skin

 

(57) Abstract:

Usage: in medicine, for treatment of burns, wounds. The inventive derived cauloside With formulas

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Reagent 1: cauloside; reagent 2: CON. The reaction of lead in the environment ethyl alcohol. Connection allatoxin, thermostable, highly soluble in water. table 2.

The invention relates to derivatives of cauloside With, in particular the potassium salt of cauloside With formula 1, stimulating reparative regeneration of the skin after burns and linear wounds

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The compound 1, its properties and the method of obtaining not described in literature.

Among the analogs proposed for patenting connection 1 note mentioned in the scientific literature glycosides of oleanolic acid, which significantly enhanced the proliferation of cells in vitro [1] and monosodium salt of 18-glycyrrhizic acid, which has anti-ulcer effect and stimulates reparative regeneration of the skin after burns [2]

The closest in structure and biological activity of 1 compound is a triterpene Pyh glycoside having the structure 3-0 - b-D-glyukopiranozil-(1-2)- a-L-arabinopyranoside of hederagenin (cauloside S) secreted from the roots steam is of 1-100 ng/ml is able to stimulate the proliferation of human embryonic fibroblasts in cell culture in vitro, in higher concentrations (5-10 μg/ml) has a cytotoxic effect. In addition, it was shown that Na-salt of cauloside With concentration of 1 mg/l stimulates the proliferation of plant cells, in particular the growth of calli ginseng [4]

The main disadvantage of cauloside With as a therapeutic agent is its poor solubility in water, which makes its introduction into the body.

Medicine has a wide range of drugs used for treatment of burns, wounds, such as syntomycin emulsion, linecol. However, the search for new drugs that stimulate reparative regeneration of the skin, i.e. having wound healing properties, is still relevant. This is because the skin is rather sensitive part of the body to injury and disease, and often the destruction of even a small area of the skin can lead to very serious complications health.

In addition, the need to expand the Arsenal of drugs, there is because every new tool differs from the known by its mechanism of action and tolerability for patients.

To solve saddow activity.

The proposed connection potassium salt of cauloside From possesses a strong ability to enhance reparative regeneration of the skin. The connection is stable, which is important for sterilization, soluble in water, which allows to use it not only in the form of emulsions and ointments, but in the form of solutions.

Potassium salt of cauloside To get the treatment of hot alcohol solution cauloside With an alcoholic solution of KOH, followed by centrifugation and washing of the precipitate chilled ethyl alcohol. After drying the precipitate receive potassium salt of cauloside S. Exit 17%

Example 1. Obtaining potassium salt of cauloside C.

1.2 g of cauloside C, isolated from the roots of tablelist powerful (Caulophyllum robustum Maxim), dissolved in 200 ml of 96% ethyl alcohol by heating in a boiling water bath. To the solution are added dropwise 1.6 ml of alcohol solution 1NKOH. The precipitation of the potassium salt of cauloside C (0.2 g) was separated by centrifugation, washed with chilled ethyl alcohol (96%) until neutral wash water and dried under vacuum. T square 291-294oC,

[]19578+46,4o(C=0,97 H2O);

gross formula: C41H65KO13, M. C. 804

is the wound healing activity of the potassium salt of cauloside C.

The influence of the potassium salt of cauloside With the linear healing of cutaneous wounds was studied on white Wistar rats weighing 130-150 g At the site pre-obespechennoi the skin and hold a full-layer straight cut length of 5 cm to the fascia. Equidistant impose 3 silk suture, bringing the wound edges. Once daily conduct of the application to the wound of the drug (in the form of an aqueous solution of potassium salt of cauloside C) at various concentrations for 1 min in 10 days after injury carefully inspect and alperujo seams, calculate the percentage of fused fabric with respect to the entire length of the frame. The results are shown in table. 1.

Potassium salt of cauloside To have a stimulating effect on the wound healing skin damage in the local application of the drug in the form of application of an aqueous solution. The effectiveness of the potassium salt of cauloside With depends on the concentration of the compound in solution and is most pronounced for the concentration of 100 µg/L.

Example 3. Study of the effect of the potassium salt of cauloside on reparative regeneration of the skin after a burn.

Burn in rats cause the latch to obezbashennaya in advance to the area of skin a massive metal object (80oC,ha for the formation of an air cushion at the site of contact. Immediately after burn and daily wound is treated with a solution of potassium salt of cauloside With in the form of applications for 1 min. Daily inspection and description of the individual pathological elements, resulting from the evolution of the wound. Static results are analyzed by comparing each experimental group of animals with the control group, according to the formula [5]

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where x2the criterion of conformity (consent);

f1f2frequency of classes of the first and second rows;

n1n2the number of individuals in each of them.

As the reference drug is used linetol, widely used in medicine for treatment of burns.

The results of the experiments are given in table. 2.

Potassium salt of cauloside With the application of an aqueous solution to the skin in concentrations of 0.1 and 100 µg/l has a marked stimulating effect on the regeneration of the skin after a burn. The action of the potassium salt of cauloside With differs from known drug linetolom, the effect which manifests itself during the first three days, while the potassium salt of cauloside With is more distant effect, but greater than that of the linetolom.

Acute toxicity of potassium salt of cauloside To set the RA toxicity with LD50=32 mg/kg, indicating low toxicity of the proposed connection.

Thus, the proposed connection potassium salt of cauloside With is low-toxic compound which has a stimulating reparative regeneration of the skin effect in wound and burn lesions. The advantage of this connection can be attributed to its good solubility, stability, and small effective dose.

Potassium salt of cauloside With formulas

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stimulating reparative regeneration of the skin.

 

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