SYSTEMIC APPLICATION OF CYSTEINE-2 1-CROTONAL ADDUCT FOR PHARMACOKINETIC STUDIES OF TUMOR-MODELS IN RATS AND MICE/

A selective cytostatic effect is demonstrated for systemic application of the Michael adduct of crotonal (GAS 4170-30-3) with cysteine (GAS 52-90-4). As in earlier studies, our initial model was the Ehrlich asc ites tumor (EAT) in mouse. Tablets containing 150 mg of the substance were implanted subcutaneously. Substance concentrations were found to be higher in the ascites fluid than in the blood. A batter model, the Walker-256 carcinosarcoma (Wa256), was used subsequently. Due to its r apid growth, results are available promptly. The EAT results were conf irmed and it was also found that there are higher substance concentrat ions in the cytoplasma of Wa-256 cells than in cells in neighboring li ver tissue. During the period when substance was being liberated from the tablet, substance concentration in the blood was constant, and con siderably lower than in ascites fluid or cytoplasma. This confirms tha t cysteine-2:1-crotonal adduct can be applied systemically from a subc utaneous depot to a model tumor in a cytostatic concentration.