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阿霉素是目前肿瘤化疗上广泛使用的蒽环类细胞毒抗生素。为了改进疗效和减少对人体的毒性,作者认为可将阿霉素(ADR)与天然的或合成的惰性大分子物质结合制备成储存型阿霉素(depot forms)。为此作者设计ADR与牛血清蛋白(BSA)共价结合,借助碳化二亚胺造成酰胺键,制备成阿霉素-牛血清白蛋白(ADR-BSA)复合物(3∶1)。进一步对ADR-BSA测定毒性表明:ADR(32mg/kg)可引起100%的小鼠死亡,ADR-BSA(3∶1)不引起死亡。而高剂量ADR-BSA(3∶1)即相当于ADR48mg/kg时仅导致20%的死亡。说明阿霉素与牛血清白蛋白结合后,毒性降低。ADR-BSA的抗肿瘤活性与ADR相比,无任何增加:其抗肿瘤活性,对小鼠P388的T/C%为19O,对小鼠S180(腹水型)
Adriamycin is currently widely used on cancer chemotherapy anthracycline cytotoxic antibiotics. To improve efficacy and reduce toxicity to humans, the authors believe that adriamycin (ADR) can be combined with natural or synthetic inert macromolecular substances to produce depot forms of storage. For this reason, the authors designed ADR covalently bound to bovine serum albumin (BSA), and formed an ADR-BSA complex (3: 1) by amide bond formation with carbodiimide. Further testing of the toxicity of ADR-BSA showed that ADR (32 mg / kg) caused 100% of the mice to die and ADR-BSA (3: 1) did not cause death. While high dose ADR-BSA (3: 1), which corresponds to only ADR 48 mg / kg, resulted in only 20% of deaths. Description of doxorubicin and bovine serum albumin, the toxicity decreased. The antitumor activity of ADR-BSA was comparable to that of ADR without any increase: its antitumor activity was 19O for mouse P388 and 180 for mouse S180 (ascites)