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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，用改良逆相蒸发法制备脂质体包裹ＲＴ修饰物，实验观察脂质体包裹前后ＲＴ修饰物急性毒性及体内外抗肿瘤活性。结果：脂质体包裹ＲＴ修饰物小鼠腹腔ＬＤ５０比原毒素大３．２３倍，体外对胃癌细胞（ＳＧＣ－７９０１）有较强的杀伤性，体内对Ｓ１８０实体癌的抑癌率５４．５％（Ｐ＜０．０１），能显著延长荷癌小鼠的存活期，（Ｐ＜０．０１）。结论：脂质体包裹ＲＴ修饰物的毒性较原毒素低，有较强的抗肿瘤活性，有进一步研究价值。
Objective: To reduce the toxicity of ricin (RT) and retain its anti-tumor activity. METHODS: RT was modified with 3-(2-pyridyldithio)-N-hydroxypropionic acid succinimidyl ester (SPDP), liposome-encapsulated RT modification was prepared by modified reverse phase evaporation method, and liposomal packaging was observed experimentally. Before and after RT modification acute toxicity and anti-tumor activity in vitro and in vivo. RESULTS: The liposome-encapsulated RT modified mice had a 3.23-fold greater LD50 in the peritoneal cavity than the original toxin, and had a strong killing effect on gastric cancer cells (SGC-7901) in vitro. The tumor suppression rate in vivo was 54.5 for S180 solid cancers. % (P<0.01) could significantly prolong the survival of mice bearing cancer (P<0.01). Conclusion: The liposome-encapsulated RT modification has lower toxicity than the original toxin and has strong anti-tumor activity. It has further research value.