The inhibitory effects of a 4-hydroxy-pentenal: Cysteine adduct against Sarcoma 180 cells in mice☆

摘要: The carcinostatic activity of a 4-hydroxy 2,3-trans-pent-en-1-al(HPE): cysteine adduct was studied against the ascitic form Sarcoma 180 both in vitro and vivo. effect HPE treatment (at concentrations excess 0·16 mM) to depress primarily incorporation 3H-thymidine into DNA; 3H-uridine 3H-leucine incorporations RNA protein respectively were considerably less affected. addition mM before cell suspensions with provided partial protection relation depression incorporation. Tumour preincubated for 30–120 min at 37°C 0.04–1.28 HPE, HPE-cysteine or 3H-thymidine. effectiveness different types preincubation procedure, depressing subsequent tumour cells vitro, compared. results obtained indicate that 4–7 times effective on molar basis than alone. The ld50 mice single i.p. injection 362 mg/kg body weight (expressed as mg HPE); thus is approx. 7 toxic free aldehyde injected Extensions survival time produced by increasing doses vivo, bearing 180. Treated animals received, days 3–7 following transplantation, daily dose equivalent alone 8–256 weight. Significant increases 32 wt./day. Mice treated responded time, compared untreated control animals, 50%, 94% 129% 64, 128 256 wt./day respectively. The are consistent view extended breakdown an cysteine, releasing reactive aldehyde, half-life