著者

三浦 孝次 池田 政男 大橋 冨次 岡田 いく子 五十嵐 良子

出版者

公益社団法人 日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.84, no.4, pp.341-345, 1964

被引用文献数

5

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Antitumor activity of a large number of nitrofuran derivatives of quinoline was tested with mice bearing Ehrlich ascites tumor EY-33. Pure strain healthy <i>ddN</i> mice, weighing 18-22g., were intraperitoneally inoculated with this Ehrlich ascites tumor. After 24 hours, 0.2ml. of 5% glucose solution of the test compound was injected intraperitoneally, once a day for 7 days, to test antitumor activity. Normal mice inoculated with this ascites tumor generally died from accumulation of the ascites after about 10-19 days. Compounds were considered effective when the mice survived 50 days after the inoculation of the ascites. The compounds found to be effective by this test were sodium 2-[2-(5-nitro-2-furyl)vinyl]-4-quinolinecarboxylate (I), 2-[2-(5-nitro-2-furyl)-vinyl]-4-aminoquinoline lactate (II), and 4-[2-(5-nitro-2-furyl)vinyl]-2-aminoquinoline lactate (III). For the sake of comparison, panfuran hydrochloride and mitomycin-C were tested at the same time.<br>The data obtained with these compounds were as follows (given in the order of the name of compound, LD₅₀ in mg./kg., ED₆₀ in mg.&times;kg., and C. I.): I, 240, 20, 12; II, 23.8, 1, 23.8; III, 26.3, 5, 5.2; panfuran hydrochloride, 72.5, 0, 0; mitomycin-C, 5.2, 0.5, 12.4.<br>In order to clarify the action mechanism of these compounds, their action in suppressing the dehydronase of Ehrlich ascites tumor, and syntheses of nucleic acid and protein by <i>coli bacilli</i> was examined. It was presumed from its results that the antitumor action of I was due mainly to the suppression of dehydrogenase action, and that of II and III to the suppression of dehydrogenase action and DNA synthesis.