Antifungal therapy with an emphasis on biofilms

Pierce, Christopher G.; Srinivasan, Anand; Uppuluri, Priya; Ramasubramanian, Anand K.; López-Ribot, José L.

doi:10.1016/j.coph.2013.08.008

Cited by 133 publications

(130 citation statements)

References 64 publications

(76 reference statements)

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“…The essential oils and their components, such as linalool, can interfere in the biosynthesis of the cell wall and/or can increase the ionic permeability of the fungal cell membrane (Pierce et al, 2013;Sookto et al, 2013). They may represent an important source of new molecules capable of controlling oral fungal infections.…”

Section: Discussionmentioning

confidence: 99%

Antifungal activity of linalool in cases of Candida spp. isolated from individuals with oral candidiasis

et al. 2017

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This study analyzed the antifungal activity of phytoconstituents from linalool on Candida spp. strains, in vitro, isolated from patients with clinical diagnoses of oral candidiasis associated with the use of a dental prosthesis. Biological samples were collected from 12 patients using complete dentures or removable partial dentures and who presented mucous with diffuse erythematous or stippled features, indicating a clinical diagnosis of candidiasis. To identify fungal colonies of the genus Candida, samples were plated onto CHROMagar Candida  . The antifungal activity of linalool, a monoterpene unsaturated constituent of basil oil, was performed using the broth microdilution technique. Then, the minimum inhibitory concentration (MIC), the two subsequent stronger concentrations and the positive controls were subcultured on Sabouraud Dextrose Agar plates to determine the minimum fungicidal concentration (MFC). The experiments were performed in triplicate and nystatin was used as a positive control in all tests. Diagnoses of oral candidiasis were verified in eight patients (66.6%) and the most prevalent fungal species was Candida albicans (37.5%), followed by Candida krusei (25.0%); and Candida tropicalis (4.2%). The best antifungal activity of linalool was observed on Candida tropicalis (MIC = 500 mg/mL), followed by Candida albicans (MIC = 1.000 mg/mL), and Candida krusei (MIC = 2.000 mg/mL).Under the study conditions and based on the results obtained, it can be concluded that the Candida strains tested were susceptible to linalool.Keywords: candidiasis, linalool, phytotherapy. Atividade antifúngica do linalol em casos de Candida spp. isolados de indivíduos com candidíase oral ResumoEste estudo analisou a atividade antifúngica do fitoconstituinte linalol em cepas de Candida ssp, in vitro, isolados de pacientes com o diagnóstico clínico de candidíase oral associado ao uso de prótese dentária. As amostras biológicas foram coletadas de 12 pacientes portadores de próteses totais ou próteses parciais removíveis e que apresentavam características de mucosa eritematosa difusa ou pontilhadas, indicando um diagnóstico clínico de candidíase. Para identificar colônias de fungos do gênero Candida, as amostras foram semeadas em CHROMagar Candida  . A atividade antifúngica do linalol, um componente insaturado monoterpene de óleo de manjericão, foi realizada através da técnica de microdiluição em caldo. Em seguida, a concentração inibitória mínima (MIC), as duas concentrações consecutivas mais fortes e os controles positivos foram subcultivados em placas de Agar Sabouraud Dextrose para determinar a concentração fungicida mínima (MFC). Os experimentos foram realizados em triplicata e a nistatina foi usada como controle positivo em todos os testes. O diagnóstico de candidíase oral foi comprovado em oito pacientes (66,6%) e as espécies de fungos mais prevalentes foram Candida albicans (37,5%), seguido por Candida krusei (25,0%); e Candida tropicalis (4,2%). A melhor atividade antifúngica do linalol foi observada em Candi...

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Section: Discussionmentioning

confidence: 99%

Antifungal activity of linalool in cases of Candida spp. isolated from individuals with oral candidiasis

et al. 2017

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“…The clinical treatment of candidiasis caused by C. albicans relies on limited drugs, which are usually composed of three major classes: polyenes, azoles and echinocandins (Odds et al ., 2003; Pierce et al ., 2013). However, problems such as selectivity, toxicity and the development of resistance have led to an emergent need for new strategies and novel drugs to efficiently treat C. albicans infections (Chandra et al ., 2001; Ramage et al ., 2002; Tobudic et al ., 2010).…”

Section: Introductionmentioning

confidence: 99%

(1‐aryloxy‐2‐hydroxypropyl)‐phenylpiperazine derivatives suppress Candida albicans virulence by interfering with morphological transition

Zhao

Huang

Sun

et al. 2018

Microbial Biotechnology

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SummaryClinical treatment of Candida albicans infections has become more difficult due to the limited development of antifungal agents and the rapid emergence of drug resistance. In this study, we demonstrate the synthesis of a series of piperazine derivatives and the evaluation of their inhibitory activity against C. albicans virulence. Thirty‐four (1‐aryloxy‐2‐hydroxypropyl)‐phenylpiperazine derivatives, including 25 new compounds, were synthesized and assessed for their efficacy against the physiology and pathogenesis of C. albicans. Several compounds strongly inhibited the morphological transition and virulence of C. albicans cells, although they did not influence the growth rate of the fungal pathogen. A leading novel compound, (1‐(4‐ethoxyphenyl)‐4‐(1‐biphenylol‐2‐hydroxypropyl)‐piperazine), significantly attenuated C. albicans virulence by interfering with the process of hyphal development, but it showed no cytotoxicity against human cells at a micromolar level. These findings suggest that (1‐aryloxy‐2‐hydroxypropyl)‐phenylpiperazine derivatives could potentially be developed as novel therapeutic agents for the clinical treatment of C. albicans infections by interfering with morphological transition and virulence.

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“…There are still a limited number of antifungal classes commercially available, many of which have the same mechanism of action, as a result of the few targets so far known in the fungal cell (Pierce et al 2013). Not surprisingly, this non-diverse arsenal is sometimes ineffective upon microbial resistance (Ramage et al 2012) leading to either persistent or recurrent fungal infections in the clinical setting.…”

Section: Introductionmentioning

confidence: 99%

Antifungal potential ofSideroxylon obtusifoliumandSyzygium cuminiand their mode of action againstCandida albicans

Pereira

Freires

Castilho

et al. 2016

Pharmaceutical Biology

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Context The emergence of resistant pathogens and toxicity of antifungals have encouraged an active search for novel candidates to manage Candida biofilms. Objective In this study, the little known species Sideroxylon obtusifolium T.D. Penn (Sapotacea) and Syzygium cumini (L.) Skeels (Myrtaceae), from the Caatinga biome in Brazil were chemically characterized and explored for their antifungal potential against C. albicans. Materials and methods We determined the effects of hydroalcoholic extracts/fractions upon fungal growth (minimum inhibitory and fungicidal concentrations, MIC/MFC), biofilm morphology (scanning electron microscopy) and viability (confocal laser scanning microscopy), proposed their mode of action (sorbitol and ergosterol assays), and finally investigated their effects against macrophage and keratinocyte cells in a cell-based assay. Data were analysed using one-way analysis of variance with Tukey-Kramer post-test (a ¼ 0.05). Results The n-butanol (Nb) fraction from S. obtusifolium and S. cumini extract (Sc) showed flavonoids (39.11 6 6.62 mg/g) and saponins (820.35 6 225.38 mg/g), respectively, in their chemical composition and demonstrated antifungal activity, with MICs of 62.5 and 125 lg/mL, respectively. Nb and Sc may complex with ergosterol as there was a 4-16-fold increase in MICs in the presence of exogenous ergosterol, leading to disrupted permeability of cell membrane. Deleterious effects were observed on morphology and viability of treated biofilms from concentrations as low as their MICs and higher. Sc was not toxic to macrophages and keratinocytes at these concentrations (p > 0.05), unlike Nb. Conclusions Nb and Sc demonstrated considerable antifungal activity and should be further investigated as potential alternative candidates to treat Candida biofilms. ARTICLE HISTORY

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Antifungal therapy with an emphasis on biofilms

Cited by 133 publications

References 64 publications

Antifungal activity of linalool in cases of Candida spp. isolated from individuals with oral candidiasis

Antifungal activity of linalool in cases of Candida spp. isolated from individuals with oral candidiasis

(1‐aryloxy‐2‐hydroxypropyl)‐phenylpiperazine derivatives suppress Candida albicans virulence by interfering with morphological transition

Antifungal potential ofSideroxylon obtusifoliumandSyzygium cuminiand their mode of action againstCandida albicans

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