Anti-Tumor Activity of L-Erythro-α,β-dihydroxybutyraldehyde

Abstract

L-Erythro -α,β-dihydroxybutyraldehyde has been shown to inhibit the incorporation of labelled leucine into protein of normal and neoplastic tissues, at a concentration which did not appreciably affect respiration and glycolysis. The present paper deals with the carcinostatic and carcinolytic activity of this drug against various tumors of mice and rats. The toxicity of L-erythro-α,β-dihydroxybutiraldehyde has been ascertained in mice and rats. Acute DL 50 values of the drug were 2.14 g/kg in mice and 1.62 g/kg in rat. Daily intraperitoneal injections of 500 mg/kg of L-erythro-α,β-dihydroxybutyraldehyde for seven days did not produce loss of weight or morphological lesions in control rats. The intraperitoneal administration of the drug in a dose of 250 mg/kg every 24 hours for seven days in Yoshida ascites hepatoma and in Walker ascites tumor-bearing rats (starting 24 hours after tumor transplantation) produced a complete disappearance of tumors. A daily dose of 500 to 750 mg/kg given intraperitoneally for seven days had a significant inhibitory effect on solid Ehrlich carcinoma and solid sarcoma 180 and increased significantly the average survival time of the animals bearing the same tumors in ascitic form. The drug was not effective on Oberling-Guérin solid or ascites myeloma. The results are briefly discussed.