• Journal of Microbiology and Biotechnology
• /
• v.12 no.6
• /
• pp.1006-1009
• /
• 2002

The biological activities of farnesoic acid derivatives against pathogenic fungi and bacteria were investigated. Farnesoic acid and its derivatives showed growth inhibitory activities against various bacteria. Among the compounds tested, geranylgeranoic acid (3) had potent antibacterial activity against Salmonella typhimurium, Proteus vulgaris, and Bacillus subtilis with minimum inhibitory concentration (MIC) in the range of $6.25-12.5{\mu}g/ml$. On the other hand, amide derivatives of farnesoic acid showed some antifungal activities. In particular, 3,7,11-trimethyl-dodeca-2,6,10-trienoic acid amide (5a) had a potent antifungal activity against Aspergillus niger, Candida albicans, and Trichophyton sp. with MIC in the range of $6.25-12.5{\mu}g/ml$.

• Archives of Pharmacal Research
• /
• v.27 no.3
• /
• pp.295-299
• /
• 2004

The antifungal activities of the essential oil from Agastache rugosa and its main component, estragole, combined with ketoconazole, one of the azole antibiotics commonly used to treat infections caused by Trichophyton species, were evaluated in this study. The combined effects were measured by the checkerboard microtiter and the disk diffusion tests, against T. erinacei, T. mentagrophytes, T. rubrum, T. schoenleinii and T. soudanense. Susceptibility of the five Trichophyton species to the oil alone, or ketoconazole alone, differed distinctly. The fractional inhibitory concentration indices (FICI) of ketoconazole combined with estragole or A. rugosa essential oil, against the tested Trichophyton species, were between 0.05 and 0.27, indicating synergistic effects. These drug combinations exhibited the most significant synergism against T. mentagrophytes, with FICIs of 0.05 and 0.09 for estragole and the essential oil fraction from A. rugosa, respectively. Isobolograms based on the data from checkerboard titer tests also indicated significant synergism between ketoconazole and the Agastache oil fraction or estragole, against the Trichophyton species evaluated. Trichophyton susceptibility to ketoconazole was significantly improved by combination with the Agastache rugosa oil fraction or its main component, estragole.

• YAKHAK HOEJI
• /
• v.43 no.4
• /
• pp.509-515
• /
• 1999

To search for new chitin biosynthesis inhibitors from natural sources, several higher plants were examined the inhibitory activity against chitin synthase IIby enzymatic assay. Among them, the extract of Schizandra chinensis strongly showed the inhibitory activity against chitin synthase II. Gomisin N and wuweizisu C were isolated from Schizandra chinensis and showed $IC_50$ value of $62.4{\;}\mu\textrm{g}/ml$ and $19.2{\;}\mu\textrm{g}/ml$, respectively. Activities of these compounds were more stronger than that of polyxin D. However, gomisin N and wuweizisu C showed weakly antifungal activities against various human pathogens.

• YAKHAK HOEJI
• /
• v.58 no.1
• /
• pp.58-61
• /
• 2014

The essential oil was extracted from the roots of Angelica dahurica Bentham et Hooker f. by steam distillation and its composition was analyzed by GC-MS. The antifungal activities were evaluated by micro-dilution method against five Aspergillus and three Trichophyton species. The most abundant component was ${\alpha}$-pinene (17.21%) among 40 compounds identified in this oil. The essential oil fraction of A. dahurica and ${\alpha}$-pinene exhibited marked inhibiting activities against the tested Aspergillus and Trichophyton species with MICs (minimum inhibitory concentrations) between 0.12 mg/ml and 8 mg/ml.

• Journal of Pharmacopuncture
• /
• v.27 no.2
• /
• pp.91-100
• /
• 2024

Objectives: Candida albicans is an opportunistic pathogen that occurs as harmless commensals in the intestine, urogenital tract, and skin. It has been influenced by a variety of host conditions and has now evolved as a resistant strain. The aim of this study was thus detect the fluconazole resistant C. albicans from the root caries specimens and to computationally evaluate the interactions of an opaque-phase ABC transporter protein with the Psidium guajava bio-active compounds. Methods: 20 carious scrapings were collected from patients with root caries and processed for the isolation of C. albicans and was screened for fluconazole resistance. Genomic DNA was extracted and molecular characterization of Cdrp1 and Cdrp2 was done by PCR amplification. P. guajava methanolic extract was checked for the antifungal efficacy against the resistant strain of C. albicans. Further in-silico docking involves retrieval of ABC transporter protein and ligand optimization, molinspiration assessment on drug likeness, docking simulations and visualizations. Results: 65% of the samples showed the presence of C.albicans and 2 strains were fluconazole resistant. Crude methanolic extract of P. guajava was found to be promising against the fluconazole resistant strains of C. albicans. In-silico docking analysis showed that Myricetin was a promising candidate with a high docking score and other drug ligand interaction scores. Conclusion: The current study emphasizes that bioactive compounds from Psidium guajava to be a promising candidate for treating candidiasis in fluconazole resistant strains of C. albicans However, further in-vivo studies have to be implemented for the experimental validation of the same in improving the oral health and hygiene.

• Journal of the Korean Wood Science and Technology
• /
• v.40 no.4
• /
• pp.276-286
• /
• 2012

In this study, the antifungal activity of Cryptomeria japonica essential oil against superficial and allergic fungi, Trichophyton schoenleinii, Trichophyton tonsurans, Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum, and Aspergillus fumigatus, was evaluated for determining the potential compound as dermatitis treatment. Minimum Inhibitory Concentration (MIC) measurement, TLC bioassay and agar dilution methods were used for determining the antifungal activity of crude essential oil and its fractions from C. japonica. Also, their major constituents were analyzed by GC/MS. The MICs were below 500 ppm at all superficial fungi, and spot 1 of C. japonica essential oil showed highly effective antifungal activity by TLC bioassay. In antifungal activity by agar dilution methods, crude oil showed high antifungal effect at more than 500 ppm and fraction D was significantly effective at even 100 ppm except for A. fumigatus. The major compounds of spot 1 and fraction D of C. japonica oil determined by GC/MS were elemol, ${\gamma}$-eudesmol, and ${\beta}$-eudesmol, which could be used as atopic dermatitis treatment material.

• Mycobiology
• /
• v.45 no.1
• /
• pp.25-30
• /
• 2017

Metal-based drugs, such as 1,10-phenanthroline, have demonstrated anticancer, antifungal and antiplasmodium activities. One of the 1,10-phenanthroline derivatives compounds (1)-N-2-methoxybenzyl-1,10-phenanthrolinium bromide (FEN), which has been demonstrated an inhibitory effect on the growth of Candida spp. This study aimed to explore the in vitro antifungal activity of FEN and its effect on the membrane integrity of Candida albicans. The minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) of FEN against planktonic C. albicans cells were determined using the broth microdilution method according to the Clinical and Laboratory Standards Institute guidelines. Cell membrane integrity was determined with the propidium iodide assay using a flow cytometer and were visualized using scanning electron microscopy (SEM). Planktonic cells growth of C. albicans were inhibited by FEN, with an MIC of $0.39-1.56{\mu}g/mL$ and a MFC that ranged from 3.125 to $100{\mu}g/mL$. When C. albicans was exposed to FEN, the uptake of propidium iodide was increased, which indicated that membrane disruption is the probable mode of action of this compound. There was cells surface changes of C. albicans when observed under SEM.

• The Korean Journal of Pesticide Science
• /
• v.2 no.1
• /
• pp.40-45
• /
• 1998

An antagonistic fungus inhibiting growth of various phytopathogenic fungi was isolated from greenhouse soils and identified. Mophological features of fruiting structures on potato dextrose agar and colorless globose to ovate heavy walled hyaline cells from the vegetative mycelium grown on MY20 agar indicate that this antagonist is Aspergillus terreus. The antagonistic activity is due to the production of antifungal compounds. An antifungal compound was purified from its culture filtrate using chloroform extraction, column chromatography, and thin layer chromatography. The purified antibiotic was effective to various phytopathogenic fungi and identified as butyrolactone I. $ED_{50}$ values measured by petri-plate assay through effective dosage(ED)-probit analysis were 9.7, 13.7, 23.3, 42.6 and 102.7 ppm on Botrytis cinerea, Rhizoctonia solani, Pythium ultimum, Phytophthora capsici, and Fusarium oxysporum, respectively.

• Journal of Microbiology and Biotechnology
• /
• v.15 no.3
• /
• pp.652-655
• /
• 2005

This paper describes the development of an enzymatic assay system for the identification of inhibitors of isocitrate lyase (ICL), one of the key enzymes of the glyoxylate cycle that is considered as a new target for antifungal drugs. A 1.6 kb DNA fragment encoding the isocitrate lyase from Candida albicans ATCC10231 was amplified by PCR, cloned into a vector providing His-Patch-thioredoxin-tag at the N-terminus, expressed in Escherichia coli, and purified by metal chelate affinity chromatography. The molecular mass of the purified ICL was approximately 62 kDa, as determined by SDS-PAGE, and the enzyme activity was directly proportional to incubation time and enzyme concentration. The effects of itaconate-related compounds on ICL activity were also investigated. Among them, itaconic acid, 3-nitropropionate, and oxalate had strong inhibitory activities with $IC_{50}$ values of 5.8, 5.4 and $8.6\;{mu}g/ml$, respectively. These inhibitors also exhibited antifungal activity on YPD agar media containing acetate as a sole carbon source, albeit at high concentration. The results indicate that the C. albicans ICL may be a regulatory enzyme playing a crucial role in fungal growth and is a prime target for antifungal agents.

• The Korean Journal of Pesticide Science
• /
• v.8 no.3
• /
• pp.168-174
• /
• 2004

In a course of the process for a lead optimization of 2-imino-l,3-thiazolines 1 which show a selective in vivo antifungal activity against rice blast, new compounds 2 in which C-5 was substituted by methyl group of the lead compound were synthesized and tested for the biological activity. Bromination of $\beta$-keto ester 7 followed by the reaction with thiourea and hydrolysis gave 2-imino-5-methyl-l,3-thiazoline carboxylic acid 3. Coupling reactions of 3 with aniline derivatives afforded 17 kinds of the corresponding 2-imino-5-methyl-l,3-thiazoline carboxanilides 2. Their in vivo antifungal activity against rice blast was weaker than that of 1, indicating that the in vivo antifungal activity of 2-imino-l,3-thiazolines was affected by the substituent at C-5. These results would be an important data for the molecular design in the lead optimization process of this series.