Fang J, Shi Y, Zhang L
Beijing Institute for Cancer Research.
Zhonghua Zhong Liu Za Zhi. 1995 Jan;17(1):5-8.
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.
8-氯腺苷对小鼠实体瘤肝癌22(H22)和腹水白血病L-1210显示出显著活性。在100mg·kg⁻¹·d×7的剂量下,H22的抑制率腹腔注射和静脉注射分别为71.7±13.3%(P<0.01)和66.1±4.46%(P<0.01);在相同剂量下,荷L-1210小鼠的生命延长率腹腔注射和静脉注射分别为124.0±22.1%(P<0.01)和104.2±20.1%(P<0.01)。8-氯腺苷在体外对3种人类癌细胞系也显示出活性。IC50值通过台盼蓝染料排斥法测量细胞生长来确定。结果显示,HL-60和K562以及人胃癌细胞系MGc80-3的IC50值分别为1.8μmol/L、4.2μmol/L和1.56μmol/L。8-氯腺苷的毒性较低,单次腹腔注射对小鼠的LD50为1025.0±52.4mg/kg,对大鼠为793.4±70.1mg/kg。