scholarly journals Antifungal Activities of cis-trans Citral Isomers against Trichophyton rubrum with ERG6 as a Potential Target

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4263
Author(s):  
Yin Zheng ◽  
Yanhong Shang ◽  
Mengyun Li ◽  
Yunzhou Li ◽  
Wuqing Ouyang
Keyword(s):  
Trichophyton Rubrum ◽  
Morphological Changes ◽  
Membrane Damage ◽  
Pathogenic Fungi ◽  
Inhibition Mechanism ◽  
Ergosterol Biosynthesis ◽  
Antifungal Activities ◽  
Pattern Change ◽  
Leakage Measurement ◽  
Inhibition Zones

Trichophyton rubrum causes ringworm worldwide. Citral (CIT), extracted from Pectis plants, is a monoterpene and naturally composed of geometric isomers neral (cis-citral) and geranial (trans-citral). CIT has promising antifungal activities and ergosterol biosynthesis inhibition effects against several pathogenic fungi. However, no study has focused on neral and geranial against T. rubrum, which hinders the clinical application of CIT. This study aimed to compare antifungal activities of neral and geranial and preliminarily elucidate their ergosterol biosynthesis inhibition mechanism against T. rubrum. Herein, the disc diffusion assays, cellular leakage measurement, flow cytometry, SEM/TEM observation, sterol quantification, and sterol pattern change analyses were employed. The results showed geranial exhibited larger inhibition zones (p < 0.01 or 0.05), higher cellular leakage rates (p < 0.01), increased conidia with damaged membranes (p < 0.01) within 24 h, more distinct shriveled mycelium in SEM, prominent cellular material leakage, membrane damage, and morphological changes in TEM. Furthermore, geranial possessed more promising ergosterol biosynthesis inhibition effects than neral, and both induced the synthesis of 7-Dehydrodesmosterol and Cholesta-5,7,22,24-tetraen-3β-ol, which represented marker sterols when ERG6 was affected. These results suggest geranial is more potent than neral against T. rubrum, and both inhibit ergosterol biosynthesis by affecting ERG6.

scholarly journals Production, Characterization, and Antimicrobial Activity of Mycocin Produced byDebaryomyces hanseniiDSMZ70238

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Safaa A. S. Al-Qaysi ◽  
Halah Al-Haideri ◽  
Zaid Akram Thabit ◽  
Wijdan Hameed Abd Al-Razzaq Al-Kubaisy ◽  
Jamal Abd Al-Rahman Ibrahim
Keyword(s):  
Antimicrobial Activity ◽  
Trichophyton Rubrum ◽  
Killer Toxin ◽  
Pathogenic Fungi ◽  
Inhibition Zone ◽  
Toxin Production ◽  
Inhibitory Effect ◽  
Curvularia Lunata ◽  
Nacl Concentration ◽  
Inhibition Zones

The present study was conducted to estimate the antimicrobial activity and the potential biological control of the killer toxin produced byD. hanseniiDSMZ70238 against several pathogenic microorganisms. In this study, the effects of NaCl, pH, and temperature, killer toxin production, and antimicrobial activity were studied. The results showed that the optimum inhibitory effect of killer toxin was at 8% NaCl, and the diameters of clear zones were 20, 22, 22, 21, 14, and 13 mm forStaphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Streptococcus pyogenes, Candida albicans,andCandida neoformans, respectively. The largest inhibition zones were observed at pH 4.5 with inhibition zone of 16, 18, 17, 18, 11, and 12 mm for the same microorganisms. The results also showed that 25°C is the optimal temperature for toxin killing activity against all targeted microorganisms. In addition, the activity of killer toxin significantly inhibited the growth of fungal mycelia for all target pathogenic fungi and the percentages of inhibition were 47.77, 48.88, 52.22, and 61.11% forTrichophyton rubrum, Alternaria alternata, Trichophyton concentricum,andCurvularia lunata, respectively. The results showed the highest growth rate ofD. hanseniiDSMZ70238 under condition of 8% NaCl concentration, pH 4.5, and 25°C for 72 h.

scholarly journals Antifungal activities of the rhizome extract of five member Zingiberaceae against Candida albicans and Trichophyton rubrum

2021 ◽  
Vol 22 (3) ◽  
Author(s):  
Muhammad Evy Prastiyanto ◽  
NI’MATUR ROHMAH ◽  
LESITA EFENDI ◽  
RAHMATIA ARIFIN ◽  
FANDHI ADI WARDOYO ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Fungal Infections ◽  
Curcuma Longa ◽  
Ethanol Extract ◽  
Pathogenic Fungi ◽  
Zingiber Officinale ◽  
Diffusion Method ◽  
Antifungal Activities

Abstract. Prastiyanto ME, Rohmah N, Efendi L, Arifin R, Wardoyo FA, Wilson W, Mukaromah AH, Dewi SS, Darmawati S. 2021. Antifungal activities of the rhizome extract of five member Zingiberaceae against Candida albicans and Trichophyton rubrum. Biodiversitas 22: 1509-1513. Fungal infections have now become serious health issues. One of the strategies to avoid the problems of fungal infections is by using natural product from plants that are effective against many human pathogenic fungi. The study portrayed the use of the extracts of plant rhizomes as the alternatives to fight against number of human pathogenic fungi. This research aimed to investigate the antifungal activities of crude ethanol extract of five member of the family Zingiberaceae (Curcuma longa, Alpinia galanga Zingiber officinale. var. rubrum, Zingiber officinale var. officinarum and Zingiber officinale var. amarum), which are widely used as folk medicines against Candida albicans and Trichophyton rubrum. Crude ethanol extracts of five members of Zingiberaceae were evaluated for their antifungal activities and the results were calculated based on the zones of inhibition using the diffusion method. The extract showed antifungal activity against Candida. albicans in the agar well diffusion assay (10.2-27.1 mm inhibition diameter) and against T. rubrum (27.3-44.3 mm inhibition diameter). The data have revealed that all rhizomes have the potential to be developed as antifungal agents, particularly against C. albicans and T. rubrum. Studies on the antifungal activity against yeast-like (C. albicans) and filamentous (T. rubrum) can provide new information about the benefits of members Zingiberaceae as a source of natural antifungal. Researchers can select the type of rhizome that has more potential for further extraction to obtain pure compounds that can be used as antifungals.

Characterization of squalene epoxidase activity from the dermatophyte Trichophyton rubrum and its inhibition by terbinafine and other antimycotic agents.

1996 ◽  
Vol 40 (2) ◽  
pp. 443-447 ◽  
Author(s):  
B Favre ◽  
N S Ryder
Keyword(s):  
Biochemical Characterization ◽  
Trichophyton Rubrum ◽  
Side Chain ◽  
Ergosterol Biosynthesis ◽  
Squalene Epoxidase ◽  
High Potency ◽  
Whole Cells ◽  
Absolute Requirement ◽  
Tertiary Amino

Squalene epoxidase (SE) is the primary target of the allylamine antimycotic agents terbinafine and naftifine and also of the thiocarbamates. Although all of these drugs are employed primarily in dermatological therapy, SE from dermatophyte fungi has not been previously investigated. We report here the biochemical characterization of SE activity from Trichophyton rubrum and the effects of terbinafine and other inhibitors. Microsomal SE activity from T. rubrum was not dependent on soluble cytoplasmic factors but had an absolute requirement for NADPH or NADH and was stimulated by flavin adenine dinucleotide. Kinetic analyses revealed that under optimal conditions the Km for squalene was 13 microM and its Vmax was 0.71 nmol/h/mg of protein. Terbinafine was the most potent inhibitor tested, with a 50% inhibitory concentration (IC50) of 15.8 nM. This inhibition was noncompetitive with regard to the substrate squalene. A structure-activity relationship study with some analogs of terbinafine indicated that the tertiary amino structure of terbinafine was crucial for its high potency, as well as the tert-alkyl side chain. Naftifine had a lower potency (IC50, 114.6 nM) than terbinafine. Inhibition was also demonstrated by the thiocarbamates tolciclate (IC50, 28.0 nM) and tolnaftate (IC50, 51.5 nM). Interestingly, the morpholine amorolfine also displayed a weak but significant effect (IC50, 30 microM). T. rubrum SE was only slightly more sensitive (approximately twofold) to terbinafine inhibition than was the Candida albicans enzyme. Therefore, this difference cannot fully explain the much higher susceptibility (> or = 100-fold) of dermatophytes than of yeasts to this drug. The sensitivity to terbinafine of ergosterol biosynthesis in whole cells of T. rubrum (IC50, 1.5 nM) is 10-fold higher than that of SE activity, suggesting that the drug accumulates in the fungus.

scholarly journals Antifungal Agents: Design, Synthesis, Antifungal Activity and Molecular Docking of Phloroglucinol Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3116 ◽  
Author(s):  
Xingxing Teng ◽  
Yuanyuan Wang ◽  
Jinhua Gu ◽  
Peiqi Shi ◽  
Zhibin Shen ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antifungal Activity ◽  
Protein Binding ◽  
Binding Site ◽  
Antifungal Agents ◽  
Trichophyton Rubrum ◽  
Trichophyton Mentagrophytes ◽  
Protein Binding Site ◽  
Antifungal Activities ◽  
Phloroglucinol Derivatives

Pseudoaspidinol is a phloroglucinol derivative with Antifungal activity and is a major active component of Dryopteris fragrans. In our previous work, we studied the total synthesis of pseudoaspidinol belonging to a phloroglucinol derivative and investigated its antifungal activity as well as its intermediates. However, the results showed these compounds have low antifungal activity. In this study, in order to increase antifungal activities of phloroglucinol derivatives, we introduced antifungal pharmacophore allylamine into the methylphloroglucinol. Meanwhile, we remained C1–C4 acyl group in C-6 position of methylphloroglucinol using pseudoaspidinol as the lead compound to obtain novel phloroglucinol derivatives, synthesized 17 compounds, and evaluated antifungal activities on Trichophyton rubrum and Trichophyton mentagrophytes in vitro. Molecular docking verified their ability to combine the protein binding site. The results indicated that most of the compounds had strong antifungal activity, in which compound 17 were found to be the most active on Trichophyton rubrum with Minimum Inhibitory Concentration (MIC) of 3.05 μg/mL and of Trichophyton mentagrophytes with MIC of 5.13 μg/mL. Docking results showed that compounds had a nice combination with the protein binding site. These researches could lay the foundation for developing antifungal agents of clinical value.

scholarly journals Potentially pathogenic fungi in the material collected by the Specialist Regional Hospital, Łódź

2013 ◽  
Vol 45 (2) ◽  
pp. 197-205
Author(s):  
Magdalena Rusicka ◽  
Grażyna Lipowczan
Keyword(s):  
Candida Albicans ◽  
Trichophyton Rubrum ◽  
Pathogenic Fungi ◽  
Regional Hospital ◽  
Pathological Changes ◽  
Superficial Mycosis

The mycobiota responsible for the development of pathological changes of the skin and its adnexa in patients presenting at the Specialist Regional Hospital, Łódź, with suspected superficial mycosis between 01 May 2003 and 30 April 2005 is analyzed. In total of 2144 isolations 39.96% were dermatophytes, 39.39% were yeast-like fungi and 20.65% were moulds. <em>Candida albicans</em> was the most frequently diagnosed species in fallowed by <em>Trichophyton rubrum</em>.

scholarly journals Ultra-Morphological Changes of Trichophyton Rubrum Treated with Hydroxychavicol

2020 ◽  
Vol 16 (2) ◽  
Author(s):  
P. M. Ridzuan ◽  
Nasir Mohamad ◽  
Salwani Ismail ◽  
Nor Iza A. Rahman ◽  
Sanusi N.A ◽  
...  
Keyword(s):  
Trichophyton Rubrum ◽  
Morphological Changes ◽  
Treated Group ◽  
Fungal Species ◽  
Skin Infections ◽  
Betel Leaf ◽  
Transmission Electron ◽  
Antifungal Potential ◽  
Resistant Strains ◽  
Preliminary Study

Trichophyton rubrum is a common pathogenic fungal species that is responsible for causing infection on human skin, hair and nail. The antifungal-resistant strains complicate the treatment regime. Hydroxychavicol (HC) is one of the main compounds from Piper betel leaf that have antifungal potential and its mechanism of action has not been studied yet. The objective of this preliminary study to determine the antifungal properties of HC against T. rubrum using transmission electron microscope (TEM) on gross and ultrastructure of T. rubrum hypha. T. rubrum was treated with HC and miconazole (MI) at concentrations of 1.25, 2.5, 5 and 10 mg/mL for 1, 3, 5 and 7 days continuously. Generally, fungi structures became more severely damaged at increasing treatment duration. Microscopically, the fungi’s cell wall treated with HC showed a rough surface, shrinkage and demolition similar to the MI treated group. The fungi organelles were also demolished and disorganized. This study revealed that HC has the ability to inhibit T. rubrum growth and has potential to be an antifungal agent for skin infections.

scholarly journals Bioactive Metabolites Produced by the Endophytic Fungus Phomopsis sp. YM355364

2014 ◽  
Vol 9 (5) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Kai-Xia Ma ◽  
Xin-Tian Shen ◽  
Rong Huang ◽  
Tang Wang ◽  
Xiao-Song Xie ◽  
...  
Keyword(s):  
Spectral Analysis ◽  
Inhibitory Activity ◽  
Endophytic Fungus ◽  
Influenza A ◽  
Pathogenic Fungi ◽  
Bioactive Metabolites ◽  
Antifungal Activities ◽  
Aconitum Carmichaeli

A new compound, 16-acetoxycytosporone B (1), along with four known ones, dankasterone A (2), dankasterone B (3), 3β,5α,9α-trihydroxy-(22E,24R)-ergosta-7,22-dien-6-one (4), and cyclonerodiol oxide (5), were isolated from Phomopsis sp. YM355364, an endophytic fungus of Aconitum carmichaeli. Their structures were characterized by spectral analysis. Compound 2 exhibited significant inhibitory activity against influenza A/Thailand/Kan353/2004(H5N1) pseudovirus with an IC50 value of 3.56 μM. Compounds 1, 2, and 4 showed either moderate or weak antifungal activities against four pathogenic fungi.

Postischemic Morphological Changes of the Dentate Gyrus in the Gerbil During Reperfusion

2001 ◽  
Vol 7 (S2) ◽  
pp. 658-659
Author(s):  
S.M. Yu ◽  
J.C. Wang
Keyword(s):  
Carotid Artery ◽  
Dentate Gyrus ◽  
Common Carotid Artery ◽  
Morphological Changes ◽  
Membrane Damage ◽  
Immunocytochemical Staining ◽  
Silk Suture ◽  
Pathophysiological Mechanism ◽  
Ischemic Lesion ◽  
Ischemic Period

Postischemic lesion following reperfusion have been investigated in the gerbil by temporary occlusion of a common carotid artery. Two phenomena have been reported in injured ischemic cells: the inability to restore mitochondrial function and evidence of plasma membrane damage. For Further understanding the pathophysiological mechanism of ischemic lesion, we have evaluated the various ischemic period and early postischemic reperfusion. in addition to the morphological changes of the dentate gyrus by light microscopy, we employed the immunocytochemical staining for iNOS and eNOS.The mongolian gerbil, Meriones unguiculatus, were anesthetized with α-chloralose (350mg/kg), bilateral common carotid artery occlusion was induced for 90 minutes. The right common carotid artery was ligated with 5-0 silk suture, and the left was clamped by a micro vascular/miniature aneurysmal clip. After an ischemic period of 90 minutes, restoration of the blood flow of the left common carotid artery was accomplished by withdrawing the microvascular clip.

scholarly journals Ellagic Acid Inhibits Trichophyton rubrum Growth via Affecting Ergosterol Biosynthesis and Apoptotic Induction

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Zhi-Jian Li ◽  
Amima Abula ◽  
Abudumijiti Abulizi ◽  
Chun Wang ◽  
Qin Dou ◽  
...  
Keyword(s):  
Cell Membrane ◽  
Ellagic Acid ◽  
Cell Apoptosis ◽  
Trichophyton Rubrum ◽  
Ergosterol Biosynthesis ◽  
Dependent Manner ◽  
Biosynthesis Pathway ◽  
Gene Expressions ◽  
Fungal Cell

Background. Trichophyton rubrum, among other dermatophytes, is a major causative agent for superficial dermatomycoses like onychomycosis and tinea pedis, especially among pediatric and geriatric populations. Ellagic acid (EA) and shikonin (SK) have been reported to have many bioactivities, including antifungal activity. However, the mechanism of EA and SK on Trichophyton rubrum has not yet been reported. Objectives. The purposes of this study were to evaluate the antifungal activities of EA and SK against Trichophyton rubrum and to illuminate the underlying action mechanisms. Methods. The effect of EA (64, 128, and 256 μg/mL) and SK (8, 4, and 2 μg/mL) on Trichophyton rubrum was investigated with different doses via detecting cell viability, ultrastructure with using a scanning electron microscope (SEM), cell apoptosis and necrosis by using the flow cytometry instrument technique (FCIT), and the ergosterol biosynthesis pathway-related fungal cell membrane key gene expressions in vitro. Results. SEM detection revealed that the T. rubrum cell surface was shrivelled, folded, and showed deformation and expansion, visible surface peeling, and broken hyphae, and cell contents overflowed after being treated with EA and SK; the cell apoptosis rate was significantly increased in dose-dependent manner after T. rubrum was treated with EA and SK; the qPCR results showed that mRNA expression of MEP4 and SUB1 was downregulated in EA- and SK-treated groups. Conclusions. Overall, our results revealed the underlying antifungal mechanism of EA and SK, which may be related to the destruction of the fungal cell membrane and inhibition of C14 demethylase and the catalytic rate of squalene cyclooxidase in the ergosterol biosynthesis pathway via downregulation of MEP4 and SUB1, suggesting that EA and SK have the potential to be developed further as a natural antifungal agent for clinical use.

scholarly journals Endosomal trafficking defects can induce calcium dependent azole tolerance inCandida albicans.

2016 ◽  
pp. AAC.01034-16 ◽  
Author(s):  
Arturo Luna-Tapia ◽  
Hélène Tournu ◽  
Tracy L. Peters ◽  
Glen E. Palmer
Keyword(s):  
Membrane Trafficking ◽  
Membrane Damage ◽  
Fungal Growth ◽  
Luciferase Reporter ◽  
Ergosterol Biosynthesis ◽  
Endosomal Trafficking ◽  
Calcium Dependent ◽  
Plasma Membrane Damage ◽  
Trafficking Defects ◽  
Azole Tolerance

The azole antifungals arrest fungal growth through inhibition of ergosterol biosynthesis. We recently reported that avps21Δ/Δmutant, deficient in membrane trafficking through the late endosome/pre-vacuolar compartment (PVC), continues to grow in the presence of the azoles, despite depletion of cellular ergosterol. Herein, we report that thevps21Δ/Δmutant exhibits less plasma membrane damage upon azole treatment than wild-type, as measured by the release of a cytoplasmic luciferase reporter into the culture supernatant. Our results also reveal that thevps21Δ/Δmutant has abnormal levels of intracellular Ca2+, and in the presence of fluconazole, enhanced expression of a calcineurin responsiveRTA2-GFPreporter. Furthermore, the azole tolerance phenotype of thevps21Δ/Δmutant is dependent upon both extracellular calcium levels and calcineurin activity. These findings underscore the importance of endosomal trafficking in determining the cellular consequences of azole treatment, and indicate that this may occur through modulation of calcium and calcineurin dependent responses.

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