Weinstein G D, McCullough J L
Arch Dermatol. 1975 Apr;111(4):471-5.
The effect of several lipid-soluble folic acid antagonists on DNA synthesis in psoriatic and normal skin was studied. The skin samples were incubated in vitro with methotrexate, dichloromethotrexate, and their respective dimethyl esters, followed by exposure to deoxyuridine-3H to assay DNA synthesis radioautographically. Psoriatic epidermal cells were found to be selectively inhibited at lower concentrations (2 times 10-7 M) of these drugs than was normal skin. The ester derivatives were more active than the parent compounds, suggesting that increased lipid solubility of the compounds may potentiate their activity.
研究了几种脂溶性叶酸拮抗剂对银屑病皮肤和正常皮肤中DNA合成的影响。将皮肤样本在体外与甲氨蝶呤、二氯甲氨蝶呤及其各自的二甲酯一起孵育,然后暴露于氚标记的脱氧尿苷以通过放射自显影法测定DNA合成。发现这些药物在较低浓度(2×10-7M)时对银屑病表皮细胞的抑制作用比正常皮肤更强。酯衍生物比母体化合物更具活性,这表明化合物脂溶性的增加可能会增强其活性。