McCullough J L, Weinstein G D
J Invest Dermatol. 1975 Oct;65(4):394-9. doi: 10.1111/1523-1747.ep12607646.
A number of chemotherapeutic drugs have been subjected to intravaginal testing in mice to measure their local inhibitory activity on DNA, RNA, and protein synthesis in vaginal epithelium. The drugs have been tested at various concentrations and in different vehicles and evaluated by autoradiographic techniques. Systemic absorption of the drugs was monitored by simultaneous study of the gastrointestinal mucosa of the rectum. Methotrexate inhibited deoxyuridine incorporation into DNA in both vaginal and rectal epithelium. Several lipid-soluble analogues of methotrexate were found to have no effect on deoxyuridine incorporation. Nitrogen mustard and emetine have been shown to selectively inhibit DNA and protein synthesis, respectively, without systemic effects. This animal assay system may be useful for predicting the effectiveness of potential drugs for the topical treatment of psoriasis.
许多化疗药物已在小鼠体内进行阴道给药测试，以测定它们对阴道上皮细胞中DNA、RNA和蛋白质合成的局部抑制活性。这些药物在不同浓度和不同载体中进行了测试，并通过放射自显影技术进行评估。通过同时研究直肠的胃肠黏膜来监测药物的全身吸收情况。甲氨蝶呤抑制脱氧尿苷掺入阴道和直肠上皮细胞的DNA中。发现甲氨蝶呤的几种脂溶性类似物对脱氧尿苷掺入没有影响。已证明氮芥和吐根碱分别选择性抑制DNA和蛋白质合成，且无全身作用。这种动物检测系统可能有助于预测潜在药物局部治疗银屑病的有效性。
