含六亚甲基间隔基和氨基甲酰键的5-氟尿嘧啶和壳寡糖缀合物的合成及其抗肿瘤活性。

Drug design and delivery Pub Date : 1990-10-01
T Ouchi, T Banba, T Matsumoto, S Suzuki, M Suzuki
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引用次数: 0

摘要

5-氟尿嘧啶(5-fluorouracil, 5FU)低聚前药具有副作用小、对肿瘤细胞有亲和力、抗肿瘤活性高的特点,5FU通过六亚甲基间隔基团通过氨基甲酰键与3个壳寡糖(COS)共价结合。评估了这些结合物延长淋巴细胞白血病小鼠寿命的能力(在腹腔内给药后)以及它们对甲基a纤维肉瘤或MH-134肝癌小鼠的肿瘤抑制作用(在皮下给药后)。与5FU、COS或5FU和COS的混合物相比,这些结合物显著增加了p-388白血病小鼠的生存时间,对实体瘤的生长抑制作用更高。在最高剂量水平下,缀合物不会引起急性毒性,也不会引起体重迅速下降。
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Synthesis and antitumor activity of conjugates of 5-fluorouracil and chito-oligosaccharides involving a hexamethylene spacer group and carbamoyl bonds.

With the object of providing an oligomeric prodrug of 5-fluorouracil (5FU) with reduced side-effects, affinity for tumor cells and high antitumor activity, 5FU was covalently attached to three chito-oligosaccharides (COS) through hexamethylene spacer groups via carbamoyl bonds. The ability of these conjugates to prolong the life of lymphocytic leukemia mice (following their intraperitoneal administration) and their tumor-inhibitory effects on Meth-A fibrosarcoma or MH-134 hepatoma mice (following their subcutaneous administration) were assessed. The conjugates caused a significant increase in the survival time of the p-388 leukemia mice, and higher growth-inhibitory effects against the solid tumor than either 5FU, COS, or blends of 5FU and COS. At the highest dose levels, the conjugates did not cause acute toxicity, and did not cause rapid decrease in body weight.

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