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采用国内合成的8-氯腺苷经体内、外实验研究,结果表明,用100mg·kg ̄(-1)·d ̄(-1)×7剂量,可使小鼠肝癌实体瘤H_22抑制率达71.7%±13.3%腹腔注射(ip)和66.1%±4.46%静脉注射(iv),使白血病L1210荷瘤小鼠的生命延长率达124.O%±22.1%(ip)和104.2%±20.1%(iv)。体外实验显示,8-氯腺苷对人白血病细胞系HL-60和K_562以及人胃癌细胞系MGC8O-3均有明显抑制生长作用,其IC_50值分别为:1.8μmol/L、4.2μmol/L和1.56μmol/L。该药采用腹腔一次注射测定小鼠的LD_50为:1025.0±52.4mg/kg;大鼠的LD_50为:793.4±70.7mg/kg,表明其急性毒性很低。
The results showed that the inhibitory rate of H_22 in mouse hepatoma solid tumor was up to 100 mg · kg -1 (-1) × 7 with the domestic synthesis of 8-chloro-adenosine in vitro and in vivo. 71.7% ± 13.3% ip and 66.1% ± 4.46% intravenous injection (iv). The leukemia L1210 tumor-bearing mice had a lifesaving rate of 124. O% ± 22.1% (ip) and 104.2% ± 20.1% (iv). In vitro experiments showed that 8-chloro-adenosine inhibited the growth of human leukemia cell lines HL-60 and K_562 and human gastric cancer cell line MGC8O-3 with IC50 values of 1.8μmol / L and 4.2μmol / L and 1.56 μmol / L. The drug LD50 measured by intraperitoneal injection of mice: 1025.0 ± 52.4mg / kg; LD_50 rat: 793.4 ± 70.7mg / kg, indicating that its acute toxicity is very low.