scholarly journals The Antimicrobial Peptides P-113Du and P-113Tri Function against Candida albicans

2016 ◽  
Vol 60 (10) ◽  
pp. 6369-6373 ◽  
Author(s):  
Guan-Yu Lin ◽  
Hsueh-Fen Chen ◽  
Yao-Peng Xue ◽  
Ying-Chieh Yeh ◽  
Chia-Lu Chen ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Antimicrobial Peptides ◽  
Antifungal Agents ◽  
Low Ph ◽  
Planktonic Cells ◽  
Content Type ◽  
Peptide Derivatives ◽  
Helix Conformation ◽  
Α Helix

ABSTRACTTwo antimicrobial P-113 peptide derivatives, P-113Du and P-113Tri, were investigated in this study. Notably, P-113Du and P-113Tri contained significant fractions of α-helix conformation and were less sensitive to high salt and low pH than P-113. Moreover, compared to P-113, these peptides exhibited increased antifungal activity against planktonic cells, biofilm cells, and clinical isolates ofCandida albicansand non-albicans Candidaspp. These results suggest that P-113Du and P-113Tri are promising candidates for development as novel antifungal agents.

scholarly journals In VitroAnalyses of the Effects of Heparin and Parabens on Candida albicans Biofilms and Planktonic Cells

2011 ◽  
Vol 56 (1) ◽  
pp. 148-153 ◽  
Author(s):  
Marisa H. Miceli ◽  
Stella M. Bernardo ◽  
T. S. Neil Ku ◽  
Carla Walraven ◽  
Samuel A. Lee
Keyword(s):  
Candida Albicans ◽  
Metabolic Activity ◽  
Biofilm Formation ◽  
High Dose ◽  
Dependent Manner ◽  
Planktonic Cells ◽  
Content Type ◽  
Heparin Sodium ◽  
The Individual

ABSTRACTInfections and thromboses are the most common complications associated with central venous catheters. Suggested strategies for prevention and management of these complications include the use of heparin-coated catheters, heparin locks, and antimicrobial lock therapy. However, the effects of heparin onCandida albicansbiofilms and planktonic cells have not been previously studied. Therefore, we sought to determine thein vitroeffect of a heparin sodium preparation (HP) on biofilms and planktonic cells ofC. albicans. Because HP contains two preservatives, methyl paraben (MP) and propyl paraben (PP), these compounds and heparin sodium without preservatives (Pure-H) were also tested individually. The metabolic activity of the mature biofilm after treatment was assessed using XTT [2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] reduction and microscopy. Pure-H, MP, and PP caused up to 75, 85, and 60% reductions of metabolic activity of the mature preformedC. albicansbiofilms, respectively. Maximal efficacy against the mature biofilm was observed with HP (up to 90%) compared to the individual compounds (P< 0.0001). Pure-H, MP, and PP each inhibitedC. albicansbiofilm formation up to 90%. A complete inhibition of biofilm formation was observed with HP at 5,000 U/ml and higher. When tested against planktonic cells, each compound inhibited growth in a dose-dependent manner. These data indicated that HP, MP, PP, and Pure-H havein vitroantifungal activity againstC. albicansmature biofilms, formation of biofilms, and planktonic cells. Investigation of high-dose heparin-based strategies (e.g., heparin locks) in combination with traditional antifungal agents for the treatment and/or prevention ofC. albicansbiofilms is warranted.

scholarly journals Low In Vitro Antifungal Activity of Tavaborole against Yeasts and Molds from Onychomycosis

2018 ◽  
Vol 62 (12) ◽  
Author(s):  
Mahdi Abastabar ◽  
Iman Haghani ◽  
Tahereh Shokohi ◽  
Mohammad Taghi Hedayati ◽  
Seyed Reza Aghili ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Antifungal Drug ◽  
Content Type ◽  
Fungal Isolates ◽  
Yeasts And Molds ◽  
Low Activity ◽  
In Vitro Antifungal Activity

ABSTRACT The in vitro activity of tavaborole, an FDA-approved antifungal drug, was compared to that of four antifungal agents against 170 clinical fungal isolates originating from patients with onychomycosis. Tavaborole had low activity against all isolates compared to itraconazole, terbinafine, and fluconazole, the principal choices for treatment of onychomycosis. Thus, it appears that tavaborole is not a candidate for the treatment of onychomycosis due to Candida species, Aspergillus species, and dermatophytes.

scholarly journals Differential Activities of Newer Antifungal Agents against Candida albicans and Candida parapsilosis Biofilms

2007 ◽  
Vol 52 (1) ◽  
pp. 357-360 ◽  
Author(s):  
Αspasia Katragkou ◽  
Athanasios Chatzimoschou ◽  
Maria Simitsopoulou ◽  
Maria Dalakiouridou ◽  
Eudoxia Diza-Mataftsi ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Agents ◽  
Candida Parapsilosis ◽  
Planktonic Cells

ABSTRACT The activities of voriconazole, posaconazole, caspofungin, and anidulafungin against Candida albicans and Candida parapsilosis biofilms were evaluated. In contrast to planktonic cells, the MICs for voriconazole and posaconazole for the biofilms of the two species were high (≥256 and >64 mg/liter, respectively) but relatively low for the echinocandins caspofungin and anidulafungin (≤1 and ≤2 mg/liter, respectively).

scholarly journals In VitroInteractions of Antifungal Agents and Tacrolimus against Aspergillus Biofilms

2015 ◽  
Vol 59 (11) ◽  
pp. 7097-7099 ◽  
Author(s):  
Lujuan Gao ◽  
Yi Sun
Keyword(s):  
Antifungal Activity ◽  
Aspergillus Fumigatus ◽  
Amphotericin B ◽  
Aspergillus Flavus ◽  
Inhibitory Activity ◽  
Aspergillus Terreus ◽  
Antifungal Agents ◽  
Broth Microdilution ◽  
Content Type ◽  
Antagonistic Effects

ABSTRACTAspergillusbiofilms were prepared fromAspergillus fumigatus,Aspergillus flavus, andAspergillus terreusvia a 96-well plate-based method, and the combined antifungal activity of tacrolimus with azoles or amphotericin B againstAspergillusbiofilms was investigated via a broth microdilution checkerboard technique system. Our results suggest that combinations of tacrolimus with voriconazole or amphotericin B have synergistic inhibitory activity againstAspergillusbiofilms. However, combinations of tacrolimus with itraconazole or posaconazole exhibit no synergistic or antagonistic effects.

scholarly journals Candida albicans Adhesion to and Invasion and Damage of Vaginal Epithelial Cells: Stage-Specific Inhibition by Clotrimazole and Bifonazole

2011 ◽  
Vol 55 (9) ◽  
pp. 4436-4439 ◽  
Author(s):  
Betty Wächtler ◽  
Duncan Wilson ◽  
Bernhard Hube
Keyword(s):  
Candida Albicans ◽  
Epithelial Cells ◽  
Antifungal Agents ◽  
Vaginal Epithelium ◽  
Specific Inhibition ◽  
Content Type ◽  
Vaginal Epithelial Cells ◽  
Specific Activities ◽  
Low Levels ◽  
Adhesion And Invasion

ABSTRACTClotrimazole and bifonazole are highly effective antifungal agents against mucosalCandida albicansinfections. Here we examined the effects of low levels of clotrimazole and bifonazole on the ability ofC. albicansto adhere, invade, and damage vaginal epithelial cells. Although adhesion and invasion were not affected, damage was greatly reduced upon azole treatment. This clearly indicates that low levels of azoles influence specific activities ofC. albicansduring distinct stages of vaginal epithelium infections.

scholarly journals Effect of pH onIn VitroSusceptibility of Candida glabrata and Candida albicans to 11 Antifungal Agents and Implications for Clinical Use

2012 ◽  
Vol 56 (3) ◽  
pp. 1403-1406 ◽  
Author(s):  
Claire S. Danby ◽  
Dina Boikov ◽  
Rina Rautemaa-Richardson ◽  
Jack D. Sobel
Keyword(s):  
Amphotericin B ◽  
Candida Glabrata ◽  
Antifungal Agents ◽  
Susceptibility Testing ◽  
Low Ph ◽  
Clinical Use ◽  
Effect Of Ph ◽  
Content Type ◽  
Clinical Observations

ABSTRACTThe treatment of vulvovaginal candidiasis (VVC) due toCandida glabratais challenging, with limited therapeutic options. Unexplained disappointing clinical efficacy has been reported with systemic and topical azole antifungal agents in spite ofin vitrosusceptibility. Given that the vaginal pH of patients with VVC is unchanged at 4 to 4.5, we studied the effect of pH on thein vitroactivity of 11 antifungal agents against 40C. glabrataisolates and compared activity against 15 fluconazole-sensitive and 10 reduced-fluconazole-susceptibilityC. albicansstrains.In vitrosusceptibility to flucytosine, fluconazole, voriconazole, posaconazole, itraconazole, ketoconazole, clotrimazole, miconazole, ciclopirox olamine, amphotericin B, and caspofungin was determined using the CLSI method for yeast susceptibility testing. Test media were buffered to pHs of 7, 6, 5, and 4. Under conditions of reduced pH,C. glabrataisolates remained susceptible to caspofungin and flucytosine; however, there was a dramatic increase in the MIC90for amphotericin B and every azole drug tested. Although susceptible to other azole drugs tested at pH 7,C. albicansstrains with reduced fluconazole susceptibility also demonstrated reduced susceptibility to amphotericin B and all azoles at pH 4. In contrast, fluconazole-sensitiveC. albicansisolates remained susceptible at low pH to azoles, in keeping with clinical observations. In selecting agents for treatment of recurrentC. glabratavaginitis, clinicians should recognize the limitations ofin vitrosusceptibility testing utilizing pH 7.0.

Synthesis of New Bis-pyrazolines Endowed with Potent Antifungal Activity against Candida albicans and Aspergillus niger

2020 ◽  
Vol 17 ◽  
Author(s):  
Belgin Sever ◽  
Mehlika Dilek Altıntop ◽  
Ahmet Özdemir
Keyword(s):  
Candida Albicans ◽  
Molecular Docking ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Mtt Assay ◽  
Active Site ◽  
Antifungal Agents ◽  
Docking Studies ◽  
Antifungal Effects ◽  
Nih 3T3

Background: Due to the increasing number of cases of invasive fungal infections (IFIs), there is an urgent need to identify potent antifungal agents capable of combating IFIs. Pyrazolines are one such class of therapeutically active agents that could be considered to fulfil this need. Objective: In this context, this paper aims to identify two new series of bis-pyrazolines endowed with potent antifungal activity against Candida albicans and Aspergillus niger. Methods: Two new series of bis-pyrazolines (4a-i, 5a-e) were synthesized through an efficient and and versatile synthetic procedure. The compounds were screened for their antifungal effects on C. albicans and A. niger using a broth microdilution method. Their cytotoxic effects on NIH/3T3 mouse embryonic fibroblast cell line were determined using MTT assay. Molecular docking studies were performed in the active site of lanosterol 14α-demethylase (CYP51) to shed light on their antifungal effects using Schrödinger’s Maestro molecular modeling package. Results And Discussion: 5,5'-(1,4-Phenylene)bis[1-(2-(5-phenyl-1,3,4-oxadiazol-2-yl)thio)acetyl)-3-(2-thienyl)-4,5- dihydro-1H-pyrazole] (4a) and 5,5'-(1,4-phenylene)bis[1-(2-(4-(2-hydroxyethyl)-1-piperazinylthiocarbamoyl)thio)acetyl)-3- (2-thienyl)-4,5-dihydro-1H-pyrazole] (5a) were found as the most promising antifungal agents in this series. Compounds 4a and 5a showed pronounced antifungal activity against C. albicans (MIC= 0.016 mg/mL) and A. niger (MIC= 0.008 mg/mL). Based on MTT assay, their antifungal effects were selective (IC50 > 0.500 mg/mL for NIH/3T3 cell line). Molecular docking studies suggested that compounds 5a-e might show their anticandidal effects via CYP51 inhibition in regard to their stronger interactions in the active site of CYP51. Conclusion: Compounds 4a and 5a stand out as potential antifungal agents for the management of IFIs caused by C. albicans and A. niger.

scholarly journals Candida albicans Mucin Msb2 Is a Broad-Range Protectant against Antimicrobial Peptides

2013 ◽  
Vol 57 (8) ◽  
pp. 3917-3922 ◽  
Author(s):  
Marc Swidergall ◽  
Andreas M. Ernst ◽  
Joachim F. Ernst
Keyword(s):  
Candida Albicans ◽  
Antimicrobial Peptides ◽  
Tight Binding ◽  
Surface Protein ◽  
Protective Effects ◽  
Content Type ◽  
Histatin 5 ◽  
Growth Environment ◽  
Corynebacterium Pseudodiphtheriticum ◽  
Lipopeptide Antibiotic

ABSTRACTThe human fungal pathogenCandida albicansreleases a large glycofragment of the Msb2 surface protein (Msb2*) into the growth environment, which protects against the action of human antimicrobial peptides (AMPs) LL-37 and histatin-5. Quantitation of Msb2*/LL-37 interactions by microscale thermophoresis revealed high-affinity binding (dissociation constant [KD] = 73 nM), which was lost or greatly diminished by lack ofO-glycosylation or by Msb2* denaturation. Msb2* also interacted with human α- and β-defensins and protectedC. albicansagainst these AMPs. In addition, the lipopeptide antibiotic daptomycin was bound and inactivated by Msb2*, which prevented the killing of bacterial pathogensStaphylococcus aureus,Enterococcus faecalis, andCorynebacterium pseudodiphtheriticum. In coculturings or mixed biofilms ofS. aureuswithC. albicanswild-type but notmsb2mutant strains, the protective effects of Msb2* on the bactericidal action of daptomycin were demonstrated. These results suggest that tight binding of shed Msb2* to AMPs that occurs during bacterial coinfections withC. albicanscompromises antibacterial therapy by inactivating a relevant reserve antibiotic.

scholarly journals In vitroactivities of antifungals alone and in combination with tigecycline againstCandida albicansbiofilms

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e5263 ◽  
Author(s):  
Mayram Hacioglu ◽  
Ayse Seher Birteksoz Tan ◽  
Sibel Dosler ◽  
Nese Inan ◽  
Gulten Otuk
Keyword(s):  
Candida Albicans ◽  
Amphotericin B ◽  
Biofilm Formation ◽  
Antifungal Agents ◽  
Synergistic Effects ◽  
Planktonic Cells ◽  
Effective Agent ◽  
Highly Active ◽  
Highly Effective ◽  
Anti Fungal

BackgroundCandidamay form biofilms, which are thought to underlie the most recalcitrant infections.MethodsIn this study, activities of antifungal agents alone and in combination with tigecycline against planktonic cells and mature and developing biofilms ofCandida albicansisolates were evaluated.ResultsAmphotericin B and echinocandins were found to be the most effective agents against mature biofilms, whereas the least effective agent was fluconazole. Furthermore, the most effective anti-fungal monotherapies against biofilm formation were amphotericin B and anidulafungin, and the least effective monotherapy was itraconazole. The combination of tigecycline and amphotericin B yielded synergistic effects, whereas combinations containing itraconazole yielded antagonist effects against planktonic cells. The combination of tigecycline and caspofungin exhibited maximum efficacy against mature biofilms, whereas combinations containing itraconazole exhibited minimal effects. Combinations of tigecycline with amphotericin B or anidulafungin were highly effective againstC. albicansbiofilm formation.DiscussionIn summary, tigecycline was highly active againstC. albicansparticularly when combined with amphotericin B and echinocandins.

scholarly journals Toxoflavin Produced byBurkholderia gladiolifromLycoris aureaIs a New Broad-Spectrum Fungicide

2019 ◽  
Vol 85 (9) ◽  
Author(s):  
Xiaodan Li ◽  
Yikui Li ◽  
Ren Wang ◽  
Qizhi Wang ◽  
Ling Lu
Keyword(s):  
Antifungal Activity ◽  
Broad Spectrum ◽  
Fungal Pathogens ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Endophytic Bacterium ◽  
Content Type ◽  
Burkholderia Gladioli ◽  
Lycoris Aurea ◽  
Resistant Mutants

ABSTRACTFungal infections not only cause extensive agricultural damage but also result in serious diseases in the immunodeficient populations of human beings. Moreover, the increasing emergence of drug resistance has led to a decrease in the efficacy of current antifungals. Thus, screening of new antifungal agents is imperative in the fight against antifungal drug resistance. In this study, we show that an endophytic bacterium,Burkholderia gladioliHDXY-02, isolated from the medicinal plantLycoris aurea, showed broad-spectrum antifungal activity against plant and human fungal pathogens. An antifungal ability assay indicated that the bioactive component was produced from strain HDXY-02 having an extracellular secreted component with a molecular weight lower than 1,000 Da. In addition, we found that this new antifungal could be produced effectively by liquid fermentation of HDXY-02. Furthermore, the purified component contributing to the antifungal activity was identified to be toxoflavin, a yellow compound possessing a pyrimido[5,4-e][1,2,4]triazine ring.In vitrobioactivity studies demonstrated that purified toxoflavin fromB. gladioliHDXY-02 cultures had a significant antifungal activity against the human fungal pathogenAspergillus fumigatus, resulting in abolished germination of conidia. More importantly, the growth inhibition by toxoflavin was observed in both wild-type and drug-resistant mutants (cyp51Aand non-cyp51A) ofA. fumigatus. Finally, an optimized protocol for the large-scale production of toxoflavin (1,533 mg/liter) has been developed. Taken together, our findings provide a promising biosynthetic resource for producing a new antifungal reagent, toxoflavin, from isolates of the endophytic bacteriumB. gladioli.IMPORTANCEHuman fungal infections are a growing problem associated with increased morbidity and mortality. Moreover, a growing number of antifungal-resistant fungal isolates have been reported over the past decade. Thus, the need for novel antifungal agents is imperative. In this study, we show that an endophytic bacterium,Burkholderia gladioli, isolated from the medicinal plantLycoris aurea, is able to abundantly secrete a compound, toxoflavin, which has a strong fungicidal activity not only against plant fungal pathogens but also against human fungal pathogensAspergillus fumigatusandCandida albicans,Cryptococcus neoformans, and the model filamentous fungusAspergillus nidulans. More importantly, toxoflavin also displays an efficacious inhibitory effect against azole antifungal-resistant mutants ofA. fumigatus. Consequently, our findings provide a promising approach to abundantly produce toxoflavin, which has novel broad-spectrum antifungal activity, especially against those currently problematic drug-resistant isolates.

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