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首页> 外文期刊>British Journal of Cancer >Studies Concerned with Overcoming Resistance to Methotrexate: A Comparison of the Effects of Methotrexate and 2,4-Diamino-5-(3′,4′-Dichlorophenyl)-6-Methylpyrimidine (BW50197) on the Colony Forming Ability of L5178Y Cells
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Studies Concerned with Overcoming Resistance to Methotrexate: A Comparison of the Effects of Methotrexate and 2,4-Diamino-5-(3′,4′-Dichlorophenyl)-6-Methylpyrimidine (BW50197) on the Colony Forming Ability of L5178Y Cells

机译：克服对甲氨蝶呤抗性的研究：甲氨蝶呤和2,4-二氨基-5-（3'，4'-二氯苯基）-6-甲基嘧啶（BW50197）对L5178Y细胞集落形成能力影响的比较

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摘要

The effects of methotrexate (MTX) and 2,4-diamino-5-(3′,4′-dichlorophenyl)-6-methylpyrimidine (BW50197) on the colony forming ability of L5178Y cells were compared. Two sub-lines of cells were used, one sensitive to methotrexate and the other resistant. In addition, the inhibitory effects of BW50197 against dihydrofolate reductase (DHFR) extracted from the MTX resistant cells were compared with those of MTX and pyrimethamine. It was found that although BW50197 was a less effective inhibitor of DHFR than MTX, it was superior to MTX at high concentrations in killing MTX resistant cells, and this superiority increased with the time of exposure to the drugs. These findings suggest that (a) when antifolate compounds are screened for antitumour activity it is insufficient simply to assess them on the basis of their ability to inhibit DHFR and (b) BW50197 should be given clinically so as to achieve the highest possible tissue concentration for the longest possible time consistent with the safety of the patient.
机译：比较了甲氨蝶呤（MTX）和2,4-二氨基-5-（3'，4'-二氯苯基）-6-甲基嘧啶（BW50197）对L5178Y细胞集落形成能力的影响。使用了两个亚细胞系，一个对甲氨蝶呤敏感，另一个对细胞有抵抗力。另外，比较了BW50197对从MTX抗性细胞中提取的二氢叶酸还原酶（DHFR）的抑制作用与MTX和乙胺嘧啶的抑制作用。已经发现，尽管BW50197是DHFR的抑制剂，但它的杀伤力却优于MTX，但在杀死MTX耐药细胞方面，它在高浓度时优于MTX，而且这种优势随着接触药物的时间而增加。这些发现表明（a）当筛选抗叶酸化合物的抗肿瘤活性时，仅根据其抑制DHFR的能力对其进行评估是不够的;（b）临床上应给予BW50197，以达到可能的最高组织浓度与患者安全相符的尽可能长的时间。

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