• Journal of the Korean Chemical Society
• /
• v.40 no.12
• /
• pp.711-718
• /
• 1996

The relationship between chemical structure and antifungal activity of benzene ring substituents of 1-phenylpyrrolidine-2,5-diones is studied by testing of model compounds and use of conformational data. The analysis revealed a number of structural features as essential for the antifungal effect: (1) the presence of an intact-NCO group and benzene moiety; (2) the distance between para substituents and the N atom within the 5.318∼5.320 ${\AA}$ range; (3) the distance between substituent X3 and X5 in the interval 5.437∼6.072 ${\AA}$ for the active analogues. And other parameters were discussed.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.12
• /
• pp.3684-3692
• /
• 2010

A series of azole-containing piperazine derivatives have been designed and synthesized. The obtained compounds were investigated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that most compounds exhibited moderate to significant antibacterial and antifungal activities in vitro. 1-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)-2-(1H-imidazol-1-yl)ethanone and 1-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)-2-(2-phenyl-1H-imidazol-1-yl)ethanone gave remarkable and broad-spectrum antimicrobial efficacy against all tested strains with MIC values ranging from 3.1 to $25\;{\mu}g/mL$, and exhibited comparable activities to the standard drugs chloramphenicol and fluconazole in clinic. Moreover, 2-((4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole was found to be the most effective in vitro against the PC-3 cell line, reaching growth inhibition values (36.4, 60.1 and 76.5%) for each tested concentration: $25\;{\mu}g/mL$, $50\;{\mu}g/mL$ and $100\;{\mu}g/mL$ in dose-dependent manner. The results also showed that the azole ring had noticeable effect on their antimicrobial and cytotoxic activities, and imidazole and benzimidazole moiety were much more favourable to biological activity than 1,2,4-triazole.

• Toxicological Research
• /
• v.26 no.2
• /
• pp.117-121
• /
• 2010

The crude ethanol extract of B. repanda showed the cytotoxic activity against Polio virus (25% activity at $150{\mu}g$/disk) and the minor cytotoxic activity against BSC cells (African green monkey kidney). However, the crude ethanol extract of B. repanda was non-toxic to murine leukaemia cells CCL 46 P388D1 ($IC_{50}$, > 62,500 ng/ml). Cytotoxic and antifungal activities were strongly shown by Fr. 64-3 which was eluted with 90% $CH_3CN/H_2O$, 100% $CH_3CN$, and 50% $CH_3CN/H_2O$(SM 2 at $150{\mu}g$/disk). The fraction 64-3 also showed the most cytotoxic activity against murine leukaemia cells (128 mg, $IC_{50}$ 10,051 ng/ml at $75{\mu}g$/disk). These results suggest that this fraction has a potent antifungal activity against the dermatophytic fungus Trichophyton mentagrophytes ATCC 28185.

• Journal of Microbiology and Biotechnology
• /
• v.34 no.4
• /
• pp.783-794
• /
• 2024

The antifungal activity of fisetin against Candida albicans is explored, elucidating a mechanism centered on membrane permeabilization and ensuing disruption of pH homeostasis. The Minimum Inhibitory Concentration (MIC) of fisetin, indicative of its interaction with the fungal membrane, increases in the presence of ergosterol. Hoechst 33342 and propidium-iodide staining reveal substantial propidium-iodide accumulation in fisetin-treated C. albicans cells at their MIC, with crystal violet uptake assays confirming fisetin-induced membrane permeabilization. Leakage analysis demonstrates a significant release of DNA and proteins in fisetin-treated cells compared to controls, underscoring the antifungal effect through membrane disruption. Green fluorescence, evident in both the cytoplasm and vacuoles of fisetin-treated cells under BCECF, AM staining, stands in contrast to controls where only acidic vacuoles exhibit staining. Ratiometric pH measurements using BCECF, AM reveal a noteworthy reduction in intracellular pH in fisetin-treated cells, emphasizing its impact on pH homeostasis. DiBAC4(3) uptake assays demonstrate membrane hyperpolarization in fisetintreated cells, suggesting potential disruptions in ion flux and cellular homeostasis. These results provide comprehensive insights into the antifungal mechanisms of fisetin, positioning it as a promising therapeutic agent against Candida infections.

• Food Science and Biotechnology
• /
• v.14 no.4
• /
• pp.487-492
• /
• 2005

Simple competition plate bioassays of Pichia anomala SKM-T and Galactomyces geotrichum SJM-59 were conducted to evaluate their potential as biological control agents that inhibit growth of Botrytis cinerea during post-harvest storage of strawberries (Fragaria ${\times}$ ananassa Duche, Red-Pearl). Occurrence rates of fungi on the surface of yeast-treated strawberries were evaluated during storage at $4^{\circ}C$. P. anomala SKM-T and G. geotrichum SJM-59 showed antifungal activities on agar plate, and P. anomala SKM-T maintained its desirable antifungal activity on surface of strawberries and its physicochemical properties during storage. Sensory evaluation was based on kinesthetics and consumer acceptability. Due to its potential antifungal activity, P. anomala SKM-T could function as biological control agent against spoilage fungi during post-harvest storage of strawberries.

• Biomolecules & Therapeutics
• /
• v.3 no.3
• /
• pp.182-187
• /
• 1995

The clastogenecity and mutagenicity of antifungal 6-[(N-halophenyl)amino]-7-chloro-5, 8-quinolinedione (RCK 3, 7, 13, 14, and 15) had been evaluated. Salmonella typhimurium reversion assay (Ames test) was used to test the mutagenicity of RCKs. RCK14 was mutagenic in S. typhimurium(TA98 and TA100) with and without rat liver microsomal activation. Whereas RCK3, 7, 13 and 15 were negative in Ames test with Salmonella typhimurium(TA98 and TA100), The clastogenecity was tested on the RCKs with in vivo mouse micronucleus assay. All of RCKs tested did not show any clastogenic effect in mouse peripheral blood. Thus RCKs were not supposed to cause any chromosomal damage termed micronuclei. These results indicate that RCK 3, 7, 13 and 15 have no genotoxic potential under these experimental condition.

• The Korean Journal of Mycology
• /
• v.21 no.2
• /
• pp.140-145
• /
• 1993

Yeast strains were isolated from healthy women(36 isolates), infertile women(15 isolates) and women suffering from local morbidity(82 isolates). On the basis of 37 different physiological and morphological characteristics, the isolated 133 yeast strains were assigned to 10 species belonging to 5 genera. Four pathogenic species were identified. They were Candida albicans, Candida parapsilosis, Candida tropicalis and Trichosporon beigelii. Candida albicans was the dominant species, whereas Saccharomyces cerevisiae prevailed among the saprophytic species. The percentage occurrence as well as the pattern of yeast species differed in the diagnostic groups. It was higher in the women suffering from local morbidity than in the healthy and infertile women. Moreover, a wider spectrum of species was isolated from this group. Women with intrauterine contraceptive devices showed the highest percentage of yeast occurrence which reached 50% of those tested. Five different antifungal agents were tested fro their effects on the growth of the isolated yeast species in vitro. Nystatin was the most effective against the isolated yeast species, followed by pyrithion zink and ciclopiroxolamine, whereas micronazole and clotrimazole, showed a lesser effect.

• Biomolecules & Therapeutics
• /
• v.18 no.4
• /
• pp.420-425
• /
• 2010

The antifungal effects and action mechanisms of styraxjaponoside A and B were investigated. Devoid of hemolytic effect, the compounds had significant effect against several human pathogenic fungal strains, with energy-independent manners. To understand the action mechanisms of the compounds, the flow cytometric analysis plotting the forward scatter and the side scatter, $DiBAC_4$(3) staining and DPH fluorescence analysis were conducted. The results indicated that the actions of the compounds were dependent upon the membrane-active mechanisms. The present study suggests that styraxjaponoside A and B exert their antimicrobial effects via membrane-disruptive mechanisms.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.19 no.3 s.31
• /
• pp.118-133
• /
• 2006

Seborrheic dermatitis is characterized by the appearance of red, flacking, greasy lesions in regions rich in sebaceous glands. There are various opinions about the relation between seborrheic dermatitis and dandruff. Considering all available data, we consider seborrheic dermatitis and dandruff to be differing severity manifestations of similar origin. The known etiologies of seborrheic dermatitis are the abnormality of lipid and hormnes, Malassezia species, immune response. We recently focus on the relation between seborrheic dermatitis and HIV positive and AIDS patients, seborrheic dermatitis and neurological disease. The treatments of seborrheic dermatitis include topical treatments, oral treatments. There are non-specific agents, antifungal medication, corticosteroids in the topical treatments. Narrow band UVB and oral medications are known as the prophylaxis of seborrheic dermatitis but we need further study. In traditional korean medicine, the literature studies and case reports have been published. But we don't know what herbal medicine has antifungal effect against Malassezia species. So we should discriminate herbal medicines which have antifungal effect against Malassezia specieses. Then we could treat seborreic dermatitis by traditional korean medicine effectively.

• Bulletin of the Korean Chemical Society
• /
• v.31 no.12
• /
• pp.3530-3538
• /
• 2010

In this study 1-[4-(2-methoxy benzyl)-6-aryl-pyridazin-3(2H)-ylidene] hydrazines were used for the synthesis of new heterocyclic systems such as thiazolidine, phthalazine, pyrazolo, tetrazolo, hydrazide and new pyridazine derivatives to explore the effect of silver nanoparticles on their biological activity efficiency. Structures of the new heterocycles were characterized by the aid of several analytical techniques including; $^1H$-NMR, FTIR and mass spectra. Silver nanoparticles were synthesized by a simple methodology and the formation of silver nanoparticles was confirmed by transmission electron microscopy (TEM) and UV studies. Most of the new prepared heterocycles were evaluated in vitro as new antimicrobial agents. Combination effects of the silver nanoparticles on the antimicrobial activity of the new heterocycles were investigated using the disk diffusion method. Compound 10a exhibited the strongest enhancing effect of silver nanoparticles solution against Aspergillus flavus and Candida albicans.