研究mPEG-ALD修饰CPU-HM的反应条件并对修饰产物的体内药效进行初步筛选。采用正交试验法,利用HPLC的面积归一化法检测各修饰条件下的修饰率,确定不同PEG修饰CPU-HM的反应条件,其中,mPEG-ALD10k修饰CPU-HM的修饰率可达83.1%,mPEG-ALD20k修饰CPU-HM的修饰率可达91.4%。通过B16F10黑色素瘤C57Bl/6黑鼠移植瘤模型检测修饰产物的体内活性,给予不同频率和剂量的mPEG-ALD10k-CPUHM(42 mg/kg)和mPEG-ALD20k-CPU-HM(79.5 mg/kg),其中mPEG-ALD10k-CPU-HM(3 d给药一次)组和mPEGALD20k-CPU-HM(2 d给药一次)组抑瘤效果较好,瘤重抑瘤率与分别达到79.34%和78.76%,与阴性组相比有极显著差异,筛选出了体内活性高,半衰期延长的修饰产物。 The reaction conditions of mPEG-ALD modified CPU-HM were studied and the in vivo efficacy of the modified products was preliminarily screened. The orthogonal test method was used to detect the modification rate of each modified condition using area normalization method of HPLC to determine the reaction conditions of different PEG modified CPU-HM, wherein the modification rate of mPEG-ALD10k modified CPU-HM can reach 83.1% , mPEG-ALD20k modified CPU-HM modification rate of up to 91.4%. The in vivo activity of the modified products was tested by the B16F10 melanoma C57B1 / 6 black mouse xenograft model and mPEG-ALD10k-CPUHM (42 mg / kg) and mPEG-ALD20k-CPU-HM (79.5 mg / kg) were administered at different frequencies and doses , And the inhibitory effect of mPEG-ALD10k-CPU-HM (once for 3 d) and mPEGALD20k-CPU-HM (once for 2 d) were better than those for mPEGALD20k-CPU-HM , Compared with the negative group was significantly different, screened in vivo activity, prolonged half-life modified products.