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目的:为了降低蓖麻毒素(RT)的毒性,保留其抗肿瘤活性.方法:采用3-(2-吡啶二硫基)N-羟基丙酸琥珀酰亚胺酯(SPDP)修饰RT,实验观察修饰前后RT的急性毒性及体外对三株肿瘤细胞杀伤作用的变化.结果:RT-PDP小鼠腹腔LD50为68.2μg/kg,比RT大2.45倍,并且对人子宫颈癌细胞(Helacels),胃癌细胞(SGC-7901)及小鼠乳腺癌细胞(EMT6)均有较强杀伤性.结论:RT-PDP较RT毒性低并有较强的抑制肿瘤细胞生长作用,它可能是一种有研究价值的抗肿瘤药物
Objective: To reduce the toxicity of ricin (RT) and retain its anti-tumor activity. METHODS: RT was modified by 3-(2-pyridyldithio)-N-hydroxypropionic acid succinimidyl ester (SPDP). The acute toxicity of RT before and after modification and the changes of the killing effect on the three tumor cells in vitro were observed. RESULTS: The peritoneal LD50 of RT-PDP mice was 68.2μg/kg, which was 2.45-fold greater than that of RT-PDP mice, and it was positive for human cervical cancer cells (Helacels), gastric cancer cells (SGC-7901) and mouse breast cancer cells (EMT6). ) Have a strong killer. Conclusion:RT-PDP is less toxic than RT and has a stronger effect on inhibiting the growth of tumor cells. It may be a valuable antitumor drug.