Chemical and Biochemical Studies on Carbohydrate Esters. II. Antitumor Activity of Saturated Fatty Acids and Their Ester Derivatives against Ehrlich Ascites Carcinoma

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Antitumor activity of normal saturated monocarboxylic acids and their ester derivatives was examined with Ehrlich ascites carcinoma in mice. The samples used were a) a series of fatty acids ranging in carbon chain length from C_3 to C_<18>, that is, propionic, butyric, valeric, caproic, caprylic, pelargonic, capric, lauric, myristic, palmitic, and stearic acids, b) their methyl esters, c) 1-O-acyl-β-D-glucopyranose tetraacetates derived from these fatty acids, and d) the so-called "sucrose monoesters" of caprylic, lauric, and myristic acids. Each agent was administered to mice by intraperitoneal injection at the dose of 400 mg/kg/day ×5,and the effect was evaluated with total packed cell volume ratio on the 7th day after the tumor implantation. Among eleven fatty acids tested, lauric and myristic acids were highly effective, while others were either ineffective or toxic. On the other hand, the methyl esters corresponding to the antitumor inactive fatty acids with a carbon chain length of C_6 to C_<10> were found to possess significant effect. The most prominent activity was exhibited with methylcaprylate. All members of the group c proved to show negligible antitumor effect. In contrast, the sucrose monoesters, especially myristate, have been suggested to exert marked activity, although their strong toxicity could not be overlooked.
社団法人日本薬学会の論文
1976-03-25