以牛血清白蛋白为中间载体的血卟啉衍生物与抗胃癌单克隆抗体交联物的抗肿瘤作用

THE ANTITUMOR ACTIVITY OF BOVINE SERUM ALBUMIN-MEDIATED CONJUGATE OF HEMATOPORPHYRIN DERIVATIVE WITH ANTIGASTRIC CANCER MONOCLONAL ANTIBODY

以牛血清白蛋白为中间载体,将血卟啉衍生物(HPD)与抗胃癌单克隆抗体3H11交联。交联物3H11-BSA-HPD的克分子比为1:1:200。本文对3H11-BAS-HPD的体内外抗肿瘤作用进行了研究,并与直接交联物3H11-HPD进行比较。3H11-BSA-HPD和3H11-HPD对胃癌靶细胞BGC-823的细胞毒效应相似,并均明显比游离HPD强。在接种靶细胞(2×10~5细胞/只)的裸鼠中,对照组和HPD组均于接种后13天内形成瘤块,而间接和直接交联物处理组在34天实验期内仅有1/6动物形成肿瘤。结果表明3H11-BSA-HPD和3H11-HPD在HPD相等剂量下,具有相似的导向杀伤肿瘤细胞的作用。

Hematoporphyrin derivative (HPD) was conjugated with a murine monoclonal antibody (3H11) against human gastric cancer through bovine serum albumin (BSA) as an intermediate. In this paper, the antitumor activity of indirect conjugate 3H11-BSA-HPD was demonstrated and compared with that of direct conjugate 3H11-HPD in vitro and in, vivo. The molar ratios of the conjugates 3H11-BSA-HPD and 3H11-HPD were 1:200 and 1:37, respectively. The cytotoxicities of 3H11 - BSA - HPD and 3H11 - HPD plus exposure to light were shown to be similar, and much greater than those of free HPD at equivalent HPD concentration in vitro. When tumor-bearing nude mice were treated with the different conjugates or HPD plus exposure to light, all the six mice of the control group formed tumor within 13 days after inoculation of BGC 823 cells (2×10~5 cells /mouse), whereas five of the six mice treated with 3H11-BSA-HPD or 3H11-HPD were tumor, free for the observation period of 34 days.