scholarly journals Copper(II) and Zinc(II) Complexes with the Clinically Used Fluconazole: Comparison of Antifungal Activity and Therapeutic Potential

2020 ◽  
Vol 14 (1) ◽  
pp. 24
Author(s):  
Nevena Lj. Stevanović ◽  
Ivana Aleksic ◽  
Jakob Kljun ◽  
Sanja Skaro Bogojevic ◽  
Aleksandar Veselinovic ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Biofilm Formation ◽  
Candida Parapsilosis ◽  
Therapeutic Potential ◽  
A549 Cells ◽  
Candida Krusei ◽  
Strong Inhibition ◽  
Subinhibitory Concentrations ◽  
Pyocyanin Production

Copper(II) and zinc(II) complexes with clinically used antifungal drug fluconazole (fcz), {[CuCl2(fcz)2].5H2O}n, 1, and {[ZnCl2(fcz)2]·2C2H5OH}n, 2, were prepared and characterized by spectroscopic and crystallographic methods. The polymeric structure of the complexes comprises four fluconazole molecules monodentately coordinated via the triazole nitrogen and two chlorido ligands. With respect to fluconazole, complex 2 showed significantly higher antifungal activity against Candida krusei and Candida parapsilosis. All tested compounds reduced the total amount of ergosterol at subinhibitory concentrations, indicating that the mode of activity of fluconazole was retained within the complexes, which was corroborated via molecular docking with cytochrome P450 sterol 14α-demethylase (CYP51) as a target. Electrostatic, steric and internal energy interactions between the complexes and enzyme showed that 2 has higher binding potency to this target. Both complexes showed strong inhibition of C. albicans filamentation and biofilm formation at subinhibitory concentrations, with 2 being able to reduce the adherence of C. albicans to A549 cells in vitro. Complex 2 was able to reduce pyocyanin production in Pseudomonas aeruginosa between 10% and 25% and to inhibit its biofilm formation by 20% in comparison to the untreated control. These results suggest that complex 2 may be further examined in the mixed Candida-P. aeruginosa infections.

scholarly journals Symbiotic NCR Peptide Fragments Affect the Viability, Morphology and Biofilm Formation of Candida Species

2021 ◽  
Vol 22 (7) ◽  
pp. 3666
Author(s):  
Bettina Szerencsés ◽  
Attila Gácser ◽  
Gabriella Endre ◽  
Ildikó Domonkos ◽  
Hilda Tiricz ◽  
...  
Keyword(s):  
Candida Species ◽  
Biofilm Formation ◽  
Therapeutic Potential ◽  
Fungal Infections ◽  
Combined Treatment ◽  
Antimicrobial Activities ◽  
Dilution Method ◽  
Model Legume ◽  
Anticandidal Activity

The increasing rate of fungal infections causes global problems not only in human healthcare but agriculture as well. To combat fungal pathogens limited numbers of antifungal agents are available therefore alternative drugs are needed. Antimicrobial peptides are potent candidates because of their broad activity spectrum and their diverse mode of actions. The model legume Medicago truncatula produces >700 nodule specific cysteine-rich (NCR) peptides in symbiosis and many of them have in vitro antimicrobial activities without considerable toxicity on human cells. In this work we demonstrate the anticandidal activity of the NCR335 and NCR169 peptide derivatives against five Candida species by using the micro-dilution method, measuring inhibition of biofilm formation with the XTT (2,3-Bis-(2-Methoxy-4-Nitro-5-Sulfophenyl)-2H-Tetrazolium-5-Carboxanilide) assay, and assessing the morphological change of dimorphic Candida species by microscopy. We show that both the N- and C-terminal regions of NCR335 possess anticandidal activity as well as the C-terminal sequence of NCR169. The active peptides inhibit biofilm formation and the yeast-hypha transformation. Combined treatment of C. auris with peptides and fluconazole revealed synergistic interactions and reduced 2-8-fold the minimal inhibitory concentrations. Our results demonstrate that shortening NCR peptides can even enhance and broaden their anticandidal activity and therapeutic potential.

scholarly journals Antifungal Activity of SCY-078 and Standard Antifungal Agents against 178 Clinical Isolates of Resistant and Susceptible Candida Species

2017 ◽  
Vol 61 (11) ◽  
Author(s):  
Wiley A. Schell ◽  
A. M. Jones ◽  
Katyna Borroto-Esoda ◽  
Barbara D. Alexander
Keyword(s):  
Candida Glabrata ◽  
Antifungal Agents ◽  
Candida Parapsilosis ◽  
Candida Krusei ◽  
Wild Type ◽  
Content Type ◽  
Clinical Resistance ◽  
Excellent Activity ◽  
Candida Lusitaniae

ABSTRACT SCY-078 in vitro activity was determined for 178 isolates of resistant or susceptible Candida albicans, Candida dubliniensis, Candida glabrata, Candida krusei, Candida lusitaniae, and Candida parapsilosis, including 44 Candida isolates with known genotypic (FKS1 or FKS2 mutations), phenotypic, or clinical resistance to echinocandins. Results were compared to those for anidulafungin, caspofungin, micafungin, fluconazole, and voriconazole. SCY-078 was shown to have excellent activity against both wild-type isolates and echinocandin- and azole-resistant isolates of Candida species.

scholarly journals Inhibitory effect of propafenone derivatives on pseudomonas aeruginosa biofilm and pyocyanin production

2020 ◽  
Vol 148 (3-4) ◽  
pp. 196-202
Author(s):  
Snjezana Petrovic ◽  
Jasmina Basic ◽  
Zoran Mandinic ◽  
Dragana Bozic ◽  
Marina Milenkovic ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Biofilm Formation ◽  
Laboratory Strain ◽  
Inhibitory Effect ◽  
Negative Control ◽  
Clinical Strains ◽  
Control Value ◽  
Essential Components ◽  
Pyocyanin Production

Introduction/Objective. Biofilm and pyocyanin production are essential components of Pseudomonas aeruginosa virulence and antibiotic resistance. Our objective was to examine inhibitory effect of synthetized propafenone derivatives 3-(2-Fluorophenyl)- 1-(2- (2-hydroxy-3-propylamino-propoxy)-phenyl)-propan-1-one hydrochloride (5OF) and3-(2- Trifluoromethyl-phenyl)-1-(2-(2-hydroxy-3-propylamino-propoxy)-phenyl)-propan-1-one hydrochloride (5CF3) on biofilm and pyocyanin in Pseudomonas aeruginosa clinical strains. Methods. Effects were tested on nine clinical isolates and one control laboratory strain of P. aeruginosa. In vitro analysis of biofilm growing was performed by incubating bacteria (0.5 McFarland) with 5OF and 5CF3 (500?31.2 ?g/ml) and measuring optical density (OD) at 570 nm. Bacteria in medium without compounds were positive control. Blank medium (an uninoculated medium without test compounds) was used as negative control. Pyocyanin production was estimated by OD at 520 nm, after bacteria incubated with 5CF3 and 5OF (250 and 500 ?g/ml), treated with chloroform, and chloroform layer mixed with HCl. Results. A total of 500 ?g/ml of 5OF and 5CF3 completely inhibited biofilm formation in 10/10 and 4/10 strains, respectively. A total of 250 ?g/ml of 5OF and 5CF3 strongly inhibited biofilm formation in 7/10 strains, while inhibition with 125 ?g/ml of 5OF and 5CF3 was moderate. Lower concentrations had almost no effect on biofilm production. Pyocyanin production was reduced to less than 40% of the control value in 6/9, and less than 50% of the control in 7/9 strains with 500 ?g/ml of 5OF and 5CF3, respectively. At 250 ?g/ml 5OF and 5CF3, most strains had pyocyanin production above 50% of the control value. Conclusion. Synthetized propafenone derivatives, 5OF and 5CF3, inhibited biofilms and pyocyanin production of Pseudomonas aeruginosa clinical strains. Presented results suggest that propafenone derivatives are potential lead-compounds for synthesis of novel antipseudomonal drugs.

scholarly journals Probiotic Yeasts Inhibit Virulence of Non-albicans Candida Species

mBio ◽  
2019 ◽  
Vol 10 (5) ◽  
Author(s):  
Lohith Kunyeit ◽  
Nawneet K. Kurrey ◽  
K. A. Anu-Appaiah ◽  
Reeta P. Rao
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Candida Tropicalis ◽  
Biofilm Formation ◽  
Candida Glabrata ◽  
Candida Parapsilosis ◽  
Candida Krusei ◽  
Probiotic Properties ◽  
Candida Auris ◽  
Content Type ◽  
Alternative Approach

ABSTRACT Systemic infections of Candida species pose a significant threat to public health. Toxicity associated with current therapies and emergence of resistant strains present major therapeutic challenges. Here, we report exploitation of the probiotic properties of two novel, food-derived yeasts, Saccharomyces cerevisiae (strain KTP) and Issatchenkia occidentalis (strain ApC), as an alternative approach to combat widespread opportunistic fungal infections. Both yeasts inhibit virulence traits such as adhesion, filamentation, and biofilm formation of several non-albicans Candida species, including Candida tropicalis, Candida krusei, Candida glabrata, and Candida parapsilosis as well as the recently identified multidrug-resistant species Candida auris. They inhibit adhesion to abiotic surfaces as well as cultured colon epithelial cells. Furthermore, probiotic treatment blocks the formation of biofilms of individual non-albicans Candida strains as well as mixed-culture biofilms of each non-albicans Candida strain in combination with Candida albicans. The probiotic yeasts attenuated non-albicans Candida infections in a live animal. In vivo studies using Caenorhabditis elegans suggest that exposure to probiotic yeasts protects nematodes from infection with non-albicans Candida strains compared to worms that were not exposed to the probiotic yeasts. Furthermore, application of probiotic yeasts postinfection with non-albicans Candida alleviated pathogenic colonization of the nematode gut. The probiotic properties of these novel yeasts are better than or comparable to those of the commercially available probiotic yeast Saccharomyces boulardii, which was used as a reference strain throughout this study. These results indicate that yeasts derived from food sources could serve as an effective alternative to antifungal therapy against emerging pathogenic Candida species. IMPORTANCE Non-albicans Candida-associated infections have emerged as a major risk factor in the hospitalized and immunecompromised patients. Besides, antifungal-associated complications occur more frequently with these non-albicans Candida species than with C. albicans. Therefore, as an alternative approach to combat these widespread non-albicans Candida-associated infections, here we showed the probiotic effect of two yeasts, Saccharomyces cerevisiae (strain KTP) and Issatchenkia occidentalis (ApC), in preventing adhesion and biofilm formation of five non-albicans Candida strains, Candida tropicalis, Candida krusei, Candida glabrata, Candida parapsilosis, and Candida auris. The result would influence the current trend of the conversion of conventional antimicrobial therapy into beneficial probiotic microbe-associated antimicrobial treatment.

scholarly journals Blue laser light inhibits biofilm formation in vitro and in vivo by inducing oxidative stress

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Katia Rupel ◽  
Luisa Zupin ◽  
Giulia Ottaviani ◽  
Iris Bertani ◽  
Valentina Martinelli ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Biofilm Formation ◽  
Mammalian Cells ◽  
Bacterial Infections ◽  
Laser Light ◽  
Therapeutic Potential ◽  
Blue Laser ◽  
Data Set

Abstract Resolution of bacterial infections is often hampered by both resistance to conventional antibiotic therapy and hiding of bacterial cells inside biofilms, warranting the development of innovative therapeutic strategies. Here, we report the efficacy of blue laser light in eradicating Pseudomonas aeruginosa cells, grown in planktonic state, agar plates and mature biofilms, both in vitro and in vivo, with minimal toxicity to mammalian cells and tissues. Results obtained using knock-out mutants point to oxidative stress as a relevant mechanism by which blue laser light exerts its anti-microbial effect. Finally, the therapeutic potential is confirmed in a mouse model of skin wound infection. Collectively, these data set blue laser phototherapy as an innovative approach to inhibit bacterial growth and biofilm formation, and thus as a realistic treatment option for superinfected wounds.

scholarly journals In Vitro Inhibition of Streptococcus mutans Biofilm Formation on Hydroxyapatite by Subinhibitory Concentrations of Anthraquinones

2007 ◽  
Vol 51 (4) ◽  
pp. 1541-1544 ◽  
Author(s):  
Tom Coenye ◽  
Kris Honraet ◽  
Petra Rigole ◽  
Pol Nadal Jimenez ◽  
Hans J. Nelis
Keyword(s):  
Reactive Oxygen Species ◽  
Streptococcus Mutans ◽  
Biofilm Formation ◽  
Reactive Oxygen ◽  
Oxygen Species ◽  
Membrane Perturbation ◽  
In Vitro Inhibition ◽  
Subinhibitory Concentrations

ABSTRACT We report that certain anthraquinones (AQs) reduce Streptococcus mutans biofilm formation on hydroxyapatite at concentrations below the MIC. Although AQs are known to generate reactive oxygen species, the latter do not underlie the observed effect. Our results suggest that AQs inhibit S. mutans biofilm formation by causing membrane perturbation.

scholarly journals Aspectos micológicos e suscetibilidade in vitro de leveduras do gênero Candida em pacientes HIV-positivos provenientes do Estado de Mato Grosso

2010 ◽  
Vol 43 (6) ◽  
pp. 673-677 ◽  
Author(s):  
Olivia Cometti Favalessa ◽  
Marilena dos Anjos Martins ◽  
Rosane Christine Hahn
Keyword(s):  
Candida Albicans ◽  
Candida Tropicalis ◽  
Candida Glabrata ◽  
Candida Parapsilosis ◽  
Candida Guilliermondii ◽  
Candida Krusei ◽  
Mato Grosso ◽  
Candida Sp

INTRODUÇÃO: A candidíase é uma das infecções fúngicas mais frequentes entre os pacientes infectados pelo vírus da imunodeficiência humana. O presente estudo objetivou a caracterização das leveduras do gênero Candida de distintas amostras clínicas, provenientes de pacientes HIV - positivos, assim como a determinação do perfil de suscetibilidade in vitro a cinco drogas antifúngicas. MÉTODOS: A caracterização dos isolados de Candida sp foi realizada através da metodologia clássica, testes bioquímicos (zimograma e auxanograma) e morfológicos (prova do tubo germinativo e microcultivo em lâmina). Também, foram realizadas a técnica genotípica (PCR) e identificação pelo método comercial API 20C AUX (BioMeriéux). Para a determinação do perfil de suscetibilidade in vitro, foram utilizadas cinco drogas antifúngicas (cetoconazol, fluconazol, itraconazol, voriconazol e anfotericina B), através do método comercialmente disponível - Etest. RESULTADOS: Foram identificados 105 isolados de leveduras do gênero Candida provenientes de 102 pacientes infectados pelo vírus HIV. Destes, foram caracterizadas 82 (78,1%) Candida albicans, 8 (7,6%) Candida parapsilosis, 8 (7,6%) Candida tropicalis, 4 (3,8%) Candida krusei, 2 (1,9%) Candida glabrata e 1 (1%) Candida guilliermondii. CONCLUSÕES: Considerando o perfil geral de sensibilidade, 60% dos isolados foram suscetíveis a todos os antifúngicos testados, porém as espécies C. tropicalis e C. krusei demonstraram uma tendência a valores mais elevados de CIMs para os azóis do que os encontrados paraC. albicans, sugerindo resistência.

scholarly journals Oral Administration of the Broad-Spectrum Antibiofilm Compound Toremifene Inhibits Candida albicans and Staphylococcus aureus Biofilm FormationIn Vivo

2014 ◽  
Vol 58 (12) ◽  
pp. 7606-7610 ◽  
Author(s):  
Kaat De Cremer ◽  
Nicolas Delattin ◽  
Katrijn De Brucker ◽  
Annelies Peeters ◽  
Soña Kucharíková ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Broad Spectrum ◽  
Staphylococcus Epidermidis ◽  
Biofilm Formation ◽  
Candida Krusei ◽  
Content Type ◽  
And Staphylococcus Aureus

ABSTRACTWe here report on thein vitroactivity of toremifene to inhibit biofilm formation of different fungal and bacterial pathogens, includingCandida albicans,Candida glabrata,Candida dubliniensis,Candida krusei,Pseudomonas aeruginosa,Staphylococcus aureus, andStaphylococcus epidermidis. We validated thein vivoefficacy of orally administered toremifene againstC. albicans and S. aureusbiofilm formation in a rat subcutaneous catheter model. Combined, our results demonstrate the potential of toremifene as a broad-spectrum oral antibiofilm compound.

scholarly journals In vitro evaluation of the antifungal activity of Marco (Ambrosia arborescens Mill.) and Matico (Aristeguietia glutinosa Lam.) on the pathogenic fungi that cause dermatomycosis (ringworm)

F1000Research ◽  
2018 ◽  
Vol 7 ◽  
pp. 559
Author(s):  
Tatiana de los Ángeles Mosquera Tayupanta ◽  
Sandra Elizabeth Ayala Valarezo ◽  
Tatiana Alexandra Vasquez Villareal ◽  
María Belén Montaluisa Álvarez
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Therapeutic Potential ◽  
Pathogenic Fungi ◽  
Trichophyton Mentagrophytes ◽  
Microsporum Canis ◽  
The One ◽  
One Way Anova

Background: Currently, there is a trend towards using natural and ethnopharmacological species with therapeutic potential. This investigation evaluated the antifungal activity of two species in the Ecuadorian Andes, which are used in treating dermatomycosis: Ambrosia arborescens Mill. (Marco) and Aristeguietia glutinosa Lam. (Matico). Methods: We worked with seven concentrations (100 to 700ppm) of Ambrosia arborescens Mill. extract and ten concentrations (0.5 to 5%) of essential oil (EO) of Aristeguietia glutinosa Lam. on Trichophyton mentagrophytes ATCC 9533, Trichophyton rubrum ATCC 28188, Microsporum canis ATCC 36299 and Candida albicans ATCC 10231. The methodology used was a modified version of the Kirby-Bauer method, using diffusion in agar wells. Results: The Tukey test, after the one-way Anova, determined effective concentrations of EO: 5% for Trichophyton mentagrophytes, 4.5% for Trichophyton rubrum, 5% for Microsporum canis and 2% for Candida albicans. In the extracts, the concentration of 700ppm was used for Trichophyton mentagrophytes, Trichophyton rubrum, and 600ppm for Microsporum canis and Candida albicans. Conclusions: The evaluation of the antifungal activity of the Ambrosia arborescens extract showed inhibition in the studied dermatophytes in each one of the planted concentrations (100 to 700ppm). The evaluation of the antifungal activity of Aristeguietia glutinosa EO showed inhibition in the studied dermatophytes in each of the planted concentrations (0.5 to 5%).

scholarly journals Atividade antifúngica de isolados clínicos de Candida não-albicans aos óleos essenciais de Syzygium aromaticum (cravo-da-índia) e Eucalyptus globulus (eucalipto-comum)

2021 ◽  
Vol 54 (1) ◽  
pp. e168684
Author(s):  
Aryanna Kelly Pinheiro Souza ◽  
Rita Dâmaris Soares Dantas ◽  
Dálity Keffelen de Barros Rodrigues ◽  
Claudio José dos Santos Júnior
Keyword(s):  
Candida Albicans ◽  
Eucalyptus Globulus ◽  
Candida Glabrata ◽  
Candida Parapsilosis ◽  
Candida Krusei ◽  
Syzygium Aromaticum

Introdução: O gênero Candida infecta o ser humano com alta incidência, sendo a espécie Candida albicans a mais isolada em infecções invasivas e superficiais. Porém, tem sido relatado um aumento considerável de espécies de Candida não-albicans em infecções fúngicas. Os óleos essenciais, por serem voláteis, podem agir como sinais de comunicação química e arma de defesa. Objetivo: Avaliar a eficácia, in vitro, dos óleos essenciais de Syzygium aromaticum e Eucalyptus globulus na inibição do crescimento de espécies de Candida não-albicans. Métodos: Para avaliação da atividade antifúngica de S. aromaticum e de E. globulus e do efeito dos seus óleos essenciais sobre a micromorfologia das espécies Candida krusei, Candida parapsilosis e Candida glabrata, foram empregadas, nesta ordem, as técnicas de difusão em ágar e microcultivo para leveduras. Resultados: Na técnica de difusão, o óleo essencial de S. aromaticum apresentou formação de halo de inibição para Candida krusei, Candida parapsilosis e Candida glabrata. O óleo de E. globulus, por sua vez, não apresentou crescimento de halos de inibição em nenhuma das concentrações testadas frente as três espécies de Candida não-albicans. Todavia, com o microcultivo, ambos os óleos essenciais se provaram, in vitro, eficazes antimicrobianos tendo apresentado estruturas indicativas de atividade antifúngica na maior concentração dos óleos e diferentes graus de destruição celular nas demais concentrações. Conclusão: Nas condições deste estudo, concluiu-se que os produtos avaliados exerceram atividade antifúngica contra cepas de Candida não-albicans, destacando-se o óleo essencial de S. aromaticum que apresentou atividade antimicrobiana em ambas as metodologias.

Sign in / Sign up

Export Citation Format

Share Document