不飽和七員環化合物の實驗的及び臨床的研究 : 第20報 Tropolone 及びその誘導体の數種Leptospiraに對する殺滅及び發育阻止作用
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For the measurement of sensitivity of Leptospirae (L) for drugs, the medium-sized test-tube method is usually applied, according to which 5 to 10 cc. of medium containing test drugs are necessary. The author applied, however, the small-sized test-tube method in order to spare the amount of materials, and by this method examined leptospirocidal (L-cidal) and leptospirostatic (L-static) action (put together called antileptospiral activity) of seven-membered ring compounds. To 2 cc. of Korthofs medium were added derivatives of hinokitiol (Hi) and tropolone (Trp) in various concentrations and L were cultured in these media, whereby their growth was observed from time to time in the dark-field. The concentration of the compounds in the media in which the number of L remained in less than 80% of the control was regarded as L-static, while the concentration at which L lost their motion or they were dissolved was regarded as L-cidal. Now, Hi-Na had L-cidal action on L. icterohaemorrhagiae at 0.5 γ/cc. and L-static action at 0.062 γ/cc. These compounds, unlike anti-biotics, showed no marked difference in the strength of the antileptospiral action at different stages of the growth of L. As to the various kinds of L., Hi-Na showed L-cidal action on L. autumnalis at 1.0 γ/cc. and on other kinds of L at 2 γ/cc. while L-static action on L. autumnalis and L. australis was seen at 0.062 γ/cc., on L. pyrogenes at 0.5 γ/cc., and on L. canicola at 0.125 γ/cc. Finally, antileptospiral activity of 14 kinds of Trp-derivatives on L. icterohaemorrhagiae was measured, Tween 80 being used as a solvent. Trp and Hi had the L-cidal action at 0.5 γ/cc., Hi-Na at 1.0 γ/cc., mercapto-Tpn at 2.0 γ/cc., and 7-monobromo-Hi, 3-7-dichloro-Hi, 3-monobromo-Trp, 3-7-dibromo-Hi and 3-5-dibromo-Trp at 4.0 γ/cc. On the other hand, Trp and Hi showed L-static action at 0.062 γ/cc., Hi-Na at 0.125 γ/cc., mercapto-tropone at 0.5 γ/cc., 7-monobromo-Hi, 3-7-dichloro Hi, 3-monobromo-Trp and 3-7-dibromo-Hi at 1.0 γ/cc., 3-5-dibromo-Trp at 2.0 γ/cc., and the other derivatives at higher concentrations. From these results we noticed that, among the examined compounds Hi and Trp had the most powerful anti-leptospiral activity and that the activity showed nearly the same strength at any stage of the growth of L.
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