高三尖杉酯碱的抗癌疗效及药代动力学研究

目的：研究高三尖杉酯碱（HHRT）口服的抗癌疗效及其药代动力学。方法：用肿瘤生长抑制率和荷瘤动物生命延长率来评价HHRT口服的抗癌疗效。用反相高效液相色谱法（HPLC）法检测HHRT口服的药代动力学。结果：口服HHRT在剂量为0．5mg/kg和1．0mg/kg时，对小鼠肉瘤S180及小鼠EC实体癌均有明显疗效，抑制率为38．9％－50．5％；对小鼠腹水型肝癌（HepA)的生命延长率为87．5％；在研究不同给药方案对口服HHRT疗效的影响时发现，间隔给药组疗效与每天连续给药组相近，一次给药组没有明显的疗效；大鼠口服HHRT后，在血液中未检测到原药的存在。结论：口服HHRT具有明显的抗肿瘤作用，发挥此作用的并非原药本身。

STUDY ON ANTITUMOR EFFECT OF ORALADMINISTRATION OF HOMOHARRINGTONINE AND ITS PHARMACOKINETICS

ve To study the antitumor effect of oraladministration of homoharringtonine (HHRT)and itspharmacokinetics.Methods The antitumor effect of oral HHRT wasobserved by the changes of tumor weight and survival time of micebearing solid tumors and ascites tumors respectively.Thepharmacokinetics of oral HHRT was detected by reverse-phaseHPLC method.Results Oral HHRT,at the dosages of 0.5 mg/kgand 1.0 mg/kg.significantly inhibited the growth of mouse sarcoma-180 and EC solid tumor with inhibition rates from 38.9% ~50.0%and prolonged the survival time of mice bearing ascites hepatoma (HepA)by 87.5%.Original compound of HHRT in animal plasmawas not found after it was administered orally.Conclusion HHRTadministered orally could exert obvious antitumor effect and this action was not due to HHRT itself.