Bernstein A, Hurwitz E, Maron R, Arnon R, Sela M, Wilchek M
J Natl Cancer Inst. 1978 Feb;60(2):379-84. doi: 10.1093/jnci/60.2.379.
Daunomycin was coupled to dextrans of various molecular sizes. The binding to the dextran carriers augmented the therapeutic efficacy of the antitumor agent in a murine lymphoma line (YAC). When the treatment with the drug or its conjugates was given concomitantly with the tumor cells at separate sites, the unbound drug was able, at its optimally effective doses, to prevent tumors in 40% of the mice, whereas the drug-dextran was efficient in 80% of the mice. The advantage of the drug-dextran over the free drug was also manifested when the treatment was given 6 days after tumor transplantation. However, a further delay of the treatment resulted in a decrease in the potency of the drug-dextran. Similar behavior was observed when increasing tumor loads were transplanted (10(5)-10(8) cells) and when the treatment was administered immediately. The most favorable effect of the drug-dextran was obtained with 10(7) cells, but against 10(8) cells neither the free drug nor the bound one was effective.
柔红霉素与各种分子大小的葡聚糖偶联。与葡聚糖载体的结合增强了抗肿瘤药物在小鼠淋巴瘤细胞系（YAC）中的治疗效果。当在不同部位将药物或其缀合物与肿瘤细胞同时给药时，未结合的药物在其最佳有效剂量下能够使40%的小鼠预防肿瘤，而药物 - 葡聚糖缀合物在80%的小鼠中有效。当在肿瘤移植6天后给药时，药物 - 葡聚糖相对于游离药物的优势也得以体现。然而，治疗的进一步延迟导致药物 - 葡聚糖的效力降低。当移植增加的肿瘤负荷（10⁵ - 10⁸个细胞）并且立即给药时，观察到类似的情况。药物 - 葡聚糖对10⁷个细胞产生最有利的效果，但对于10⁸个细胞，游离药物和结合药物均无效。
