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[蒽环类药物在敏感和耐药白血病细胞中的转运]

[Anthracycline transport in sensitive and resistant leukemia cells].

作者信息

Erttmann R, Erb N, Forcadell de Dios P, Neurath C, Looft G, Landbeck G

机构信息

Abteilung für Hämatologie und Onkologie, Universitätskinderklinik, Hamburg.

出版信息

Klin Padiatr. 1989 Jan-Feb;201(1):40-5. doi: 10.1055/s-2007-1025273.

Abstract

The in-vitro uptake of four anthracyclines into leukemic cells was investigated. The accumulation was found to be dependent on the extracellular anthracycline concentration in a linear fashion. The steady state intracellular drug level was reached very quickly and was found to be correlated to the extracellular pH-value in the range between 6.4 and 7.4. Intracellular anthracycline accumulation was restricted in a leukemic subline (F 4-6 R), which was found to be 86 times more resistant to doxorubicin compared with its wild tpye (F 4-6). The importance of the initial uptake phase of anthracyclines into leukemic cells raises the question whether long-term "cardioprotective" anthracycline application schedules will retain the same antileukemic effect as conventional bolus injection.

摘要

研究了四种蒽环类药物在白血病细胞中的体外摄取情况。发现积累呈线性依赖于细胞外蒽环类药物浓度。稳态细胞内药物水平很快达到,并且发现在6.4至7.4的范围内与细胞外pH值相关。在一个白血病亚系(F 4-6 R)中,细胞内蒽环类药物的积累受到限制,该亚系对阿霉素的耐药性比其野生型(F 4-6)高86倍。蒽环类药物进入白血病细胞的初始摄取阶段的重要性引发了一个问题,即长期“心脏保护”的蒽环类药物应用方案是否会保持与传统推注注射相同的抗白血病效果。

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