HIGHER ANTI-TUMOR EFFICACY OF DAUNOMYCIN WHEN LINKED TO DEXTRAN - INVIVO AND INVITRO STUDIES

HIGHER ANTI-TUMOR EFFICACY OF DAUNOMYCIN WHEN LINKED TO DEXTRAN - INVIVO AND INVITRO STUDIES
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DOI:
10.1093/jnci/60.2.379
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发表时间:
1978-01-01
影响因子:
10.3
通讯作者:
WILCHEK, M
WILCHEK, M
中科院分区:
医学1区
文献类型:
--
作者:
BERNSTEIN, A;HURWITZ, E;WILCHEK, M

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将道诺霉素偶联到各种分子大小的葡聚糖上。结合葡聚糖载体增强了抗肿瘤剂在小鼠淋巴瘤系(YAC)中的治疗效果。当用药物或其缀合物在不同部位与肿瘤细胞同时给予治疗时,未结合的药物能够在其最佳有效剂量下预防40%的小鼠的肿瘤,而药物-葡聚糖在80%的小鼠中有效。当在肿瘤移植后6天给予治疗时,药物右旋糖酐相对于游离药物的优势也得到了体现。治疗的进一步延迟导致药物-葡聚糖效力的降低。当移植增加的肿瘤负荷(105-108个细胞)和立即给予治疗时,观察到类似的行为。药物-葡聚糖对107个细胞获得最有利的效果,但对108个细胞,游离药物和结合药物均无效。
Daunomycin was coupled to dextrans of various molecular sizes. Binding to dextran carriers augmented the therapeutic efficacy of the antitumor agent in a murine lymphoma line (YAC). When treatment with the drug or its conjugates was given concomitantly with tumor cells at separate sites, the unbound drug was able, at its optimally effective doses, to prevent tumors in 40% of mice, whereas the drug-dextran was efficient in 80% of mice. The advantage of the drug-dextran over the free drug was also manifested when treatment was given 6 days after tumor transplantation. A further delay of treatment resulted in a decrease in potency of the drug-dextran. Similar behavior was observed when increasing tumor loads were transplanted (105-108 cells) and when treatment was administered immediately. The most favorable effect of the drug-dextran was obtained with 107 cells, but against 108 cells neither the free drug nor the bound one was effective.