グアヤコール・ホルムアルデヒド・レジン(GF レジン)の化学的組成, 消毒作用ならびに毒性に関する研究

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Guaiacol formaldehyde resin (GF-resin) is a polycondensation product of guaiacol and formaldehyde and a solution of 40% GF-resin in organic solvents has been put to use as a medicament for root canal treatment. Its details such as chemical formula and molecular weights, however, are not yet known. High performance liquid chromatography therefore was applied to the estimation of molecular weights of GF-resin and to the quantitative analysis of guaiacol and formaldehyde in GF-resin. Furthermore four biological studies were made to determine the antimicrobial effect and the toxicities of GF-resin and of FR liquid, a solution of 40% GF-resin in organic solvents. Formalin guaiacol (FG), guaiacol, and formalin were included in the test samples to make a comparative study. In the first biological study the antimicrobial effect was tested on five kinds of strains by the paper disc method. Liquefied phenol (liq. phenol) was used as a positive control. In the second study the inflammatory potential was examined by Evan's blue test. A paper disc soaked with 30μl of a sample was stuck on the shaved dorsal skin of rabbits. The minimal inflammatory dose for skin reactions was also obtained. In the third study the cytotoxic effect on L cell tissue culture system was tested, and 50% inhibitory concentration for cell growth was examined. In the fourth study oral acute toxicity in mice was examined. Each LD_<50> with confidence limits was calculated with use of Litchfield-Wilcoxon's method. The results obtained from the above were as follows : 1. Four polycondensation products of guaiacol and formaldehyde were detected in GF-resin, and molecular weight of each was 205, 390, 450 and 720 in terms of the polystyrene. These polycondensation products have a slight antimicrobial effect and cytotoxicity. Inflammatory potential and acute toxicity however were not detected in these tests. Consequently, it is estimated that the polycondensation products have very slight toxicities. 2. The concentration of guaiacol in GF-resin is 27.75% and that of formaldehyde in GF-resin is 0.15%. Guaiacol produces the antimicrobial effect, the inflammatory potential and the cytotoxicity of GF-resin. Formaldehyde content is so small that it makes little contribution to the pharmacological effects of GF-resin. 3. Inhibitory potency ratio on the area of inhibitory zone to liq. phenol is 1.4-10 for formalin, 1.1-10 for FG, 0.6-0.9 for guaiacol, and 0.2-0.6 for GF-resin. GF-resin shows the antimicrobial effect on each strain of microbes tested. 4. The intensity of Evan's blue response of GF-resin corresponds to 1 : 16 dilutions of formalin and to 1 : 4 dilutions of FG and liq. phenol respectively, but it is milder than that of guaiacol. 5. On the basis of 50% L cells inhibitory concentration, the comparative intensity of cytotoxicity is 14 times for formalin, 6 times for FG and 1.3 times for guaiacol, as compared with GF-resin. 6. Mice didn't die from the administration of 10.0g/kg GF-resin which was the maximum that can be administered orally to mice. Oral LD_<50> therefore is over 10.0g/kg for GF-resin. In summary, antimicrobial and cytotoxic effects of GF-resin are brought about not only by guaiacol in it but also by polycondensation products, though inflammatory potential and acute toxicity are brought about by guaiacol alone.
1990-10-25

グアヤコール・ホルムアルデヒド・レジン(GF レジン)の化学的組成, 消毒作用ならびに毒性に関する研究

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