喜树碱前体多相脂体的药理学研究

STUDIES ON THE PHARMACOLOGY OF POLY-PHASE LIPOSOME OF PRO-CAMPTOTHECIN

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。

Reported in the present article are the results of our studies on the pharmacology of pro-camptothecin (A-CPT)and its poly-phase liposome (A-CPT-PL). The ip and po LD50 of A-CPT were 159.3rng/kg and 33.7mg/kg in mice, respectively, No death was recorded in the period of observation after the administration of A-CPT-PL 50mg/kg by the same route. The inhibitory rates of A-CPT-PL against S180 and HepS were 74% and 82%, respectively. The life span of mice bearing EAC was prolonged to 126% by ip administration of A-CPT-PL 0.5mg/kg for 6 days. A-CPT- PL had no effect on tumor concomity immunity after ip administration of A-CPT-PL 0.5mg/kg daily for 9 days.