Hexapeptide

Details Hexapeptide Hexapeptide

1986-02-05

1987-10-06

Phillips, Delbert R.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

6 to 7 amino acid residues in defined sequence

C07K 706

Patent

active

046984194

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to the organic chemistry and, more particularly, to a novel hexapeptide.


BACKGROUND OF THE INVENTION

At the present time for the treatment of acute viral hepatitis, aggravation of chronic hepatitis and hepatocirrhosis synthetic glucocorticoidal hormonal preparations such as prednisolone and the like are most widely administered. These preparations are employed, as a rule, over long periods and cause a great number of complications on the part of various organs and systems. Glucocorticoids bring about atrophy of the cortical layer of adrenal glands, increased arterial pressure, development of steroid diabets, obesity, retention of urine, electrolytical disturbances, osteoporosis phenomena, pahological bone fractures. In the gastro-intestinal tract glucocorticoids frequently cause the formation of ulcers complicated with hemorrhages which provides an especially detrimental effect on the progress of chronic liver diseases. An abrupt cancellation of glucocorticoids results in the development of an acute adrenal insufficiency. Remissions in the treatment with preparations of this class are instable and of short duration. (cf. Scott J., Physiological pharmacological and pathological effects of glucocorticoids on the digestive system, Clin. gastroenterol.m 1981, v. 10, p. 627-652).
Known in the art are hexapeptides of a different structure, for example hexapeptide His-D-Trp-Ala-Trp-D-Phe-Lys-NH.sub.2 (Bowers Cy et al., Endocrinology, 1984, v. 114, No. 5, p. 1537-1545) or hexapeptide Tyr-D-Ala-Gly-Phe-Leu-Arg and the like (cf. A. V. Waldman, O. S. Medvedev. Theoretical Prerequisits for Finding New Cardio-Vascular Agents Among Peptides, "Vestnik Akademii Meditsinskikh Nauk SSSR", 1982, No. 5, p. 14-22).
However, the hepatoprotective activity of such compounds is hitherto unknown in the art.


DISCLOSURE OF THE INVENTION

The hexapeptide according to the present invention is novel and hitherto unknown in the literature.
The present invention is directed to the provision of a novel compound-hexapeptide exhibiting a high hepatoprotective activity, causing no side responses and useful in medicine.
This object is accomplished by a novel hexapeptide which, according to the present invention has the following structure: Phe-Ala-Gly-Phe-Gly-Arg
The hexapeptide according to the present invention comprises a white powder well soluble in distilled water, physiological solution, ethanol, insoluble in ether, ethylacetate, benzene. Melting point is 154.degree.-156.degree. C., (.alpha.).sub.D.sup.25 =+8.4 (with 0.5 H.sub.2 O).


BEST MODE FOR CARRYING OUT THE INVENTION

The study of a hepatoprotective effect of the hexapeptide according to the present invention was carried out in comparison with prednisolone on male mice of the line Balb C.
The development of acute hepatitis was induced in mice subjected to a 12-hours' starving by means of D-galactosamine hydrochloride which was administered intraperitoneally diluted in 0.1 ml of a physiological solution in the dose of 700 mg/kg. The control group of animals was administered intraperitoneally with 0.1 ml of a physiological solution. The animals given D-galactosoamine hydrochloride were injected, immediately after its administration, with the hexapeptide according to the present invention (100 .mu.g/kg), prednisolone (5 mg/kg) or a physiological solution (0.1 ml) hypodermally. Repeated injections of the test preparations were made after 6 hours. Each of the groups consisted of 12 animals. The mice were slaughtered by decapitation, blood was collected and in its plasma concentrations of alanine transaminase and glutametedehydrogenase were determined.
The statistical processing of the results obtained was effected using t-criterion. The certain value was regarded as the dirrerence at the level of 95% (at P<0.05).
The results thus obtained are shown in Table 1.


TABLE 1 ______________________________________ Concentration Concentration of alanine of glutamatede- transaminase, hydrogenase, No. Groups of ani

REFERENCES:
patent: 4428941 (1984-01-01), Calibert et al.
patent: 4578217 (1986-03-01), Vnek et al.
Article: Assessment of Antienzymatic Therapy of Destructive Pancreatitis, Yu A. Nesterenko; Yu P. Atanov.

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