聚乙二醇修饰对苦瓜籽中RIP抗肿瘤活性及免疫学特性的影响  

Effects of PEGylation on anti-tumor activity and immunological properties of ribosome-inactivating protein from bitter melon seeds

作　　者：白竹梅[1] 沈富兵[2] 吴民泸[2] 邓缅[2] 卞晓晓[2] 陈怡雯[2] 孟延发[1] 

机构地区：[1]四川大学生命科学学院生物资源与生态环境教育部重点实验室,四川成都610064 [2]成都医学院,四川成都610083

出　　处：《华西药学杂志》2009年第6期565-568,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金(批准号:30770232)

摘　　要：目的探讨苦瓜籽核糖体失活蛋白(RIP)经聚乙二醇(PEG)修饰后的体外及动物体内免疫学特性的变化。方法用MTT法测定RIP和RIP-PEG结合物对小鼠黑色素瘤细胞的抑制率;通过间接ELISA法测定RIP和RIP-PEG结合物在小鼠体内的免疫原性;以全身主动过敏实验(ASA)和被动皮肤过敏实验(PCA)来比较二者在豚鼠和大鼠体内的过敏毒性。结果RIP-PEG结合物对小鼠黑色素瘤细胞B16的抑制率约为RIP的70%,产生的特异性IgG与RIP比较显著下降(P<0.01),诱发的过敏反应也显著降低。结论苦瓜籽RIP经PEG修饰后,其抗肿瘤活性、免疫原性和过敏毒性均显著降低。OBJECTIVE To study the alteration of anti - tumor activity and immunological properties of PEGylated ribosome - inactivating protein （RIP） from bitter melon seeds in vivo. METHODS The inhibition percent of RIP and RIP - PEG conjugates to mice melanoma cell - lines B16 were assayed by MTY methods. The immunogenicity of RIP and RIP - PEG conjugate in mice were assayed by indirect ELISA. And the allergic toxicity of them in the guinea pigs and SD rats were compared by active systemic anaphylaxis （ASA） and passive cutaneous anaphylaxis （PCA）. RESULTS Under the same concentration, the inhibition percent of RIP - PEG conjugates to mice melanoma cell - lines B16 was about 70% to RIP, and the level of antigen - specific IgG of mice immunized with RIP - PEG conjugates was significantly lower than that of RIP（ P 〈 0.01 ）, and the allergic responses induced by RIP - PEG conjugates was also reduced markedly. CONCLUSION After PEGylation, the anti - tumor activity, immunogenicity and allergic toxicity of ribosome -inactivating protein （RIP） from bitter melon seeds were decreased significantly.

关 键 词：核糖体失活蛋白 核糖体失活蛋白-聚乙二醇结合物 免疫原性 全身主动过敏试验 被动皮肤过敏试验 

分 类 号：R967[医药卫生—药理学]