论文部分内容阅读
本文报道了对喜树碱前体(A-CPT)及喜树碱前体多相脂质体(A-CPT-pl)的药理学研究结果。结果表明,A-CPT腹腔注射给药(ip)及经口腔给药(PO),寇氏法求得小鼠的LD50分别为159.3mg/kg及33.7mg/kg,较喜树碱钠盐(CTP-Na)的毒性降低,按最大允许给药容量(0.5ml/10g)ip或PO A-CPT-pl 50mg/kg,在观察期间未见死亡。抑瘤试验结果表明,A-CPT-pl对S180及HepS的抑制率可达74%及82%,可使荷EAC小鼠的生命延长126%;A-CPT对S180及HepS的抑制率可达52%及53%,可使荷EAc小鼠的生命延长54%。肿瘤相伴免疫试验结果表明,每日ip,A-CPT-pl 0.5mg/kg,连续9天,对小鼠肿瘤相伴免疫没有明显影响。
This article reports the results of pharmacological studies on camptothecin precursor (A-CPT) and camptothecin precursor multiphase liposomes (A-CPT-pl). The results showed that A-CPT was administered via intraperitoneal injection (ip) and oral administration (PO). The LD50 of the mice was determined to be 159.3 mg/kg and 33.7 mg/kg, respectively, which is comparable to the camptothecin sodium salt ( The toxicity of CTP-Na was reduced by ip or PO A-CPT-pl 50 mg/kg according to the maximum allowable dosing volume (0.5 ml/10 g), and no death was observed during the observation period. The results of tumor inhibition test showed that the inhibition rate of A-CPT-pl on S180 and HepS was up to 74% and 82%, and the lifespan of EAC mice was prolonged by 126%. The inhibitory rate of A-CPT on S180 and HepS was up to 52% and 53% can extend the life span of EAc mice by 54%. The results of tumor-associated immunoassay showed that daily ip, A-CPT-pl 0.5 mg/kg, for 9 consecutive days, had no significant effect on mouse tumor concomitant immunity.