Antifungal effects

Hammer KA, Carson CF, Riley TV. (2004) Antifungal effects of Melaleuca alternifolia (tea tree) oil and its components on Candida albicans, Candida glabrata and Saccharomyces cerevisiae. J Antimicrob Chemother 53 1081-1085. 

A related sequence was used by Kozikowski and Park (74) to prepare the ring skeleton of streptazolin (200), a compound that exhibits antibacterial and antifungal effects. In this approach, the tricyclic isoxazoline intermediate 198 was formed in the key cycloaddition step (Scheme 6.86). Thus, the reaction of oxime 197 (obtained from 4-piperidone) with sodium hypochlorite-triethylamine afforded tricyclic isoxazoline 198 in very good yield. This cycloadduct was converted to p-hydroxyketone 199 by reduction/hydrolysis using Raney Ni in the presence of acetic acid. Racemic streptazolin (200) was obtained from 199 in several additional steps (74). 

It is a synthetic allylamine derivative, which exerts its antifungal effect by inhibiting squalene epoxidase leading to deficiency of ergosterol and corresponding accumulation of squalene which causes fungal cell death. 

Antibacterial and antifungal effects of nanosilver-based water paint are summarized in Table 18.2... 

Silver nanoparticles synthesized by a cost-effective three-stage electrochemical technique have demonstrated great promise as antimicrobial agents. Nanosilver was less effective against E. coli, S. aureus, B. subtilis and P. phoeniceum compared to silver ions. However silver nanoparticles have prolonged bactericidal effect as a result of continuous release of Ag ions in sufficient concentration and thus nanoparticles can be more suitable in some bactericidal applications. The synthesized silver nanoparticles added to water paints or cotton fabrics have demonstrated a pronounced antibacterial/antifungal effect, despite the fact that they tend to agglomerate into clusters up to 200 nm. 

Okamoto, M., Matsumoto, K., Wada, Y. and Kuwahara, Y. (1981). Studies on antifungal effect of mite alarm pheromone citral. 2. Antifungal effect of the hexane extracts of the grain mites and some analogues of citral. Japanese Journal of Sanitary Zoology 32 265-270. (In Japanese with English summary.)... 

Nowicki and Bara ska-Rybak (2007) studied the protective effect of shark liver oil. They observed a significant protection against bacterial and fungal infections by shark liver oil treatment which contains mostly squalene and alkylglycerol. Further, this treatment showed improved effects on xerosis and skin lesion-induced atopic dermatitis. This antibacterial and antifungal effect could be accounted for the high-squalene-including composition of the shark liver oil however, detailed studies are needed to be carried out for reputed activity of squalene as an anti-infectant. 

Amphotericin B imposes its antifungal effects by binding to the sterol moiety of the membrane and damaging its structural and functional integrity (Figure 45.1). 

Wahlroos, O. and Virtanen, A. I. 1958. On the antifungal effect of benzoxazolinone and 6-methoxy-benzoxazolinone, respectively, on Fusarium nivale. Acta Chem. Scand. 12, 124-128... 

Secondary drug ANTIFUNGALS Effect Mechanism Precautions... 

The co-administration of 5-flucytosine with AmB, which is commonly used dinically to obtain a synergistic antifungal effect, protects against acute and chronic nephrotoxicity [107]. The mechanisms by which flucytosine influences the renal response to AmB are not clear but may relate to (i) its administration in 0.9% NaCl, which itself is protective, (ii) a renal vasodilator effect of flucytosine that antagonizes AmB-induced vasoconstriction, and (iii) reduction in renal uptake of AmB [107]. 

To evaluate whether incorporation of AmB into lipid formulations reduces nephrotoxicity, any comparison of conventional AmB with a new formulation of the drug should address the following questions 1) do the different formulations have the same or different actions 2) if they have the same action, what is the dose ratio between antifungal and toxic effects, especially nephrotoxicity and 3) is there a selective advantage in the dose ratios indicating a wider therapeutic margin, i.e., is the dose ratio of lipid formulation of AmB/ AmB lower for the antifungal effect compared to the nephrotoxic effect ... 

Barrett JP, Vardulaki KA, Conlon C, et al. A systematic review of the antifungal effectiveness and tolerability of amphotericin B formulations. Clin Ther 2003 25 1295-320. 

Lisa M, Leifertova I, Baloun J. A contribution to the antifungal effect of propolis [in German]. Folia Pharm 1989 13(1) 29-44. 

Adults have an acidic, fatty substance in and on the skin called sebum. Sebum functions as a natural antifungal agent, put of the innate immune system. Fatty acids have been iitetl for years with the idea that if a substance similar to sebum could be applied to the infected area, the effect of the sebum would be augmented and fungi could be eradi-caicd. The application of fatty acids or their salts does in fxi have an antifungal effect, albeit a feeble one. 

Benzoic Acid. Bcn/oic acid possesses appreciable antifungal effects, but it cannot penetrate the outer layer of the skin in infected areas. Therefore, benzoic acid when u.sed as an antifungal agent must be admixed with a kcratolytic agent. Suitable mixtures arc benzoic acid and. salicylic acid and benzoic acid and resorcinol. An old preparation that is. still in u.se is Whitfield s Ointment. USP. litis ointment contains benzoic acid. 6%, and. salicylic acid, 6%, in a petrolatum base. The cure rates from preparations like thc.se are low. 

Karamenderes et al. [67] reported the composition and antimicrobial activity of the essential oils obtained from Achillea millefolium L. subsp. pannonica (Scheele) Hayek, Achillea millefolium subsp. millefolium, Achillea arithmifolia Waldst Kitt and Achillea kotschyi Boiss. subsp. kotschyi, four Achillea species from Turkey. 1,8-cineole, Fig. (2), artemisia alcohol and ascaridole were identified as major components. The essential oils showed antibacterial and antifungal effects even with low concentrations. The essential oil of the flowering tops of another Achillea species, Achillea fragantissimum (Forsk.) Sch. Bip growing in Sinai, was analyzed [68]. Santolina alcohol, a- and P-thujone, Fig. (5) and artemisia ketone account for approximately 80% of the oil. The oil showed marked antimicrobial activities against Escherichia coli. Bacillus subtilis and Staphylococcus aureus. 

Diterpenoids are the most important compounds responsible of the biological activities found in numerous Salvia species. Antituberculous effects have been established for S. blepharochlyna [5], S. multicaulis also reported for it s antifungic effect [6] and S. prionitis which possess antiphlogistic and antibacterial properties [7,8] beside its antituberculous activity. 

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