[Antitumor activities of 8-chloroadenosine in vivo and in vitro].
8-chloroadenosine showed marked activity against mice solid tumor hepatoma 22 (H22) and ascitic leukemia L-1210. At 100mg. Kg-1. /d x 7, the inhibition rate of H22 was 71.7 +/- 13.3% (P < 0.01) and 66.1 +/- 4.46% (P < 0.01), i.p. and i.v., respectively; at the same dose, the life-prolonging rate of mice bearing L-1210 was 124.0 +/- 22.1% (P < 0.01) and 104.2 +/- 20.1% (P < 0.01), i.p. and i.v., respectively. 8-chloroadenosine also showed activity against 3 human cancer cell lines in vitro. The IC50 values were determined by measuring cell growth using trypan blue dye exclusion. The results showed that HL-60 and K562, and human gastric cancer cell line MGc80-3 and IC50 values of 1. 8 mumol/L, 4.2 mumol/L and 1.56 mumol/L, respectively. The toxicity of 8-chloroadenosine was low, with LD50 of 1025.0 +/- 52.4 mg/kg for mice and 793.4 +/- 70.1 mg/kg for rats by single i.p. injection.
Fang
J
J
Beijing Institute for Cancer Research.
Shi
Y
Y
Zhang
L
L
D015762:2-Chloroadenosine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D005260:Female; D007928:Lethal Dose 50; D007939:Leukemia L1210 / Q000188:drug therapy* / Q000473:pathology; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D009368:Neoplasm Transplantation; D051381:Rats; D017208:Rats, Wistar; D013274:Stomach Neoplasms / Q000473:pathology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D015762:2-Chloroadenosine; C075440:8-chloroadenosine