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抗肿瘤药物的膜转运及其与肿瘤化疗的相关性(作者译)

[Membrane transport of antineoplastic drugs and its relevance to tumour chemotherapy (author's transl)].

作者信息

Kolassa N

出版信息

Wien Klin Wochenschr. 1980;92(20):707-15.

PMID:7467345
Abstract

The permeation of cell membranes by several antineoplastic drugs (AD) exhibits characteristics of carrier-mediated transport processes (facilitated diffusion or active transport); the main representatives among these AD are mechlorethamine, cyclophosphamide, melphalan, methotrexate, 6-mercaptopurine, 5-fluorouracil, cytarabine, 5-fluorodeoxyuridine, vincristine, vinblastine, adriamycin, daunorubicin and dactinomycin. Inhibition or stimulation of the membrane transport of AD influences absorption, distribution, elimination, therapeutic effectiveness and toxicity. The choice of certain combination therapies may increase the selectivity of AD by influencing membrane transport. A change in the properties of transport systems is one possible reason for the resistance of tumour cells to various AD.

摘要

几种抗肿瘤药物(AD)透过细胞膜呈现出载体介导转运过程(易化扩散或主动转运)的特征;这些抗肿瘤药物中的主要代表有氮芥、环磷酰胺、美法仑、甲氨蝶呤、6-巯基嘌呤、5-氟尿嘧啶、阿糖胞苷、5-氟脱氧尿苷、长春新碱、长春碱、阿霉素、柔红霉素和放线菌素D。抑制或刺激抗肿瘤药物的膜转运影响吸收、分布、消除、治疗效果及毒性。某些联合治疗方案的选择可通过影响膜转运来提高抗肿瘤药物的选择性。转运系统性质的改变是肿瘤细胞对各种抗肿瘤药物产生耐药性的一个可能原因。

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