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Home Semiconductor manufacture Homocysteine-thiolactone-perchlorate-as-a-tumor-promotor

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 Homocysteine thiolactone perchlorate as a tumor promotor

Details
Inventors: McCully, Kilmer S.;
Assignee: The United States of America as represented by the Department of Health, (Washington, DC)
Primary Examiner: Siegel; Alan
Assistant Examiner:
Attorney, Agent or Firm: Roberts, Jr.; John S.

Homocysteine thiolactone perchlorate is prepared from the corresponding homocysteine thiolactone hydrochloride and optimally about two equivalents of perchloric acid as reactants. A preferred solvent utilized is chloroform-methanol (4:1) solution and a preferred temperature range is 0.degree.-85.degree. C. with the lower limit dependent upon the particular solvent and the upper limit of about 186.degree. C. dependent upon the melting point of the product crystals. The preferred perchloric acid reactant may be replaced with perchlorate salts such as AgClO.sub.4 or KClO.sub.4. The product perchlorate salt is soluble in organic solvents, whereas other known salts such as the hydrochloride are only water soluble. This property is thought to influence the growth effect of the perchlorate salt in animals, such as rabbits, and to influence the unique effect of the perchlorate salt on the growth of malignant tumors in animals, such as mice.

DETAILED DESCRIPTION I claim: 1.
A method of promoting the growth of malignant tumors in laboratory animals such as mice and rabbits which comprises utilizing intraperitoneally an effective amount of homocysteine thiolactone perchlorate in said laboratory animals.




Description:
The present invention relates to a specific compound homocysteine thiolactone perchlorate and a method of making same.
Homocysteine is HSCH.
sub.
2 CH.
sub.
2 CH(NH.
sub.
2)COOH and the thiolactone is shown below.
Of the known salts of homocysteine thiolactone, the present perchlorate is deemed unique in that it is soluble in organic solvents, whereas other salts such as the hydrochloride are only water soluble.
This is of peculiar interest in the unique biologic effect of the perchlorate which is described below.
The reactant homocysteine thiolactone hydrochloride is taught in DP No.
1,081,466 (1958) and this hydrochloride is also the starting material for the present process.
Additionally, British Pat.
No.
903,322 and Canadian Pat No.
611,437 relate to the homocysteine thiolactone hydrohalide.
British Pat No.
903,322 notes the compound at column 2, first page, and Canadian Pat.
No.
611,437 describes the chlorohydride at column 2, line 62.
Neither of these patent references describes a process or product for the present perchlorate salt.
The literature prior art is listed below: Kilmer S.
McCully, "Homocysteine Metabolism in Scurvy, Growth and Arteriosclerosis," Nature, 231:391-392, June 11, 1971.
Kilmer S.
McCully, "Homocysteinemia and Arteriosclerosis," American Heart Journal, 83:571-573, April 1972.
Eliot Spindel and Kilmer S.
McCully, "Conversion of Methionine to Homocysteine Thiolactone in Liver," Biochimica et Biophysica Acta, 343:687-691, 1974.
Kilmer S.
McCully and Robert B.
Wilson, "Homocysteine Theory of Arteriosclerosis," Atherosclerosis, 22:215-227 (1975).
Kilmer S.
McCully and Peter Clopath, "Homocysteine Compounds Which Influence the Growth of a Malignant Neoplasm," In Press, Chemotherapy, 1976



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