[Analgesic, anti-inflammatory and toxic effects of 3-substituted benzo-1,2,4-triazines].
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Biomedical subjects
Publications and source records attributed to M Paintz.
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After a survey of the literature on the antimicrobial activity of the bee product propolis, the authors discuss their own findings as compared to the chemotherapeutical agents streptomycin, oxytetracycline, chloramphenicol, nystatin, griseofulvin and sulphamerazine. According to the results obtained by testing 25 isolated constituents on Bacillus subtilis, Staphylococcus aureus, Candida albicans and Trichophyton mentagrophytes, the antimicrobial properties of this mixture of natural substances are mainly attributable to the flavonoids pinocembrin, galangin, pinobanksin, pinobanksin-3-acetate as well as to the p-coumaric acid benzyl ester and a caffeic acid ester mixture. None of the isolated substances was as potent as the antibiotics tested for the purpose of comparison. The relatively good antimycetic activity of the 5,7-dihydroxyflavanone pinocembrin seems noteworthy. Finally, possible mechanisms of the antimicrobial action of the flavonoids are discussed.
The relative surface tension xi = (Pi/Mv)4 can be used in structure-activity studies as additional parameter. Here, Pi = parachor, Mv = molar volume (Tables 1 and 2) of the substituents. Some examples demonstrate the application.
An ethanolic propolis extract and some constituents isolated from propolis were tested on the cornea of the rabbit and of the mouse for local anaesthetic activity. Total anaesthesia was obtained with the total extract as well as with the compounds 5,7-dihydroxyflavanone (pinocembrin), 5-hydroxy-7-methoxyflavanone (pinostrobin) and with a mixture of caffeic acid esters. Each of these compounds was nearly thrice as potent as the total extract. Propoxypiperocaine which was tested for the purpose of comparison was still efficient in an almost 10-fold lower concentration. When applied subcutaneously, pinocembrin and the mixture of caffeic acid esters produced nearly the same anaesthesia as lidocaine.