β-lactam substituted polycyclic fused pyrrolidine/pyrrolizidine derivatives eradicate C. albicans in an ex vivo human dentinal tubule model by inhibiting sterol 14-α demethylase and cAMP pathway

Gowri, M.; Beaula, Winfred Sofi; Biswal, Jayashree; Prabhu, Dhamodharan; Raghavan, Saiharish; prasad, Surabi Rohan; Pitani, Ravishankar; Kandaswamy, Deivanayagam; Raghunathan, Ragavachary; Jeyakanthan, Jeyaraman; Rayala, Suresh K.; Venkatraman, Ganesh

doi:10.1016/j.bbagen.2015.12.020

Cited by 20 publications

(9 citation statements)

References 46 publications

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“…and Aspergillus spp. (Gowri et al 2016 ; O'Driscoll et al 2008 ; Mohamadzadeh et al 2020 ). However, studies have indicated that β-lactam antibiotics are unable to inhibit the growth of Candida species, and amoxicillin can increase the virulence of Candida krusei and Candida tropicalis in Caenorhabditis elegans (Aguiar Cordeiro et al 2018 ).…”

Section: Antibacterial Drugsmentioning

confidence: 99%

Drug repurposing strategies in the development of potential antifungal agents

Zhang

Liu

Zeng

et al. 2021

Appl Microbiol Biotechnol

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The morbidity and mortality caused by invasive fungal infections are increasing across the globe due to developments in transplant surgery, the use of immunosuppressive agents, and the emergence of drug-resistant fungal strains, which has led to a challenge in terms of treatment due to the limitations of three classes of drugs. Hence, it is imperative to establish effective strategies to identify and design new antifungal drugs. Drug repurposing is a potential way of expanding the application of existing drugs. Recently, various existing drugs have been shown to be useful in the prevention and treatment of invasive fungi. In this review, we summarize the currently used antifungal agents. In addition, the most up-to-date information on the effectiveness of existing drugs with antifungal activity is discussed. Moreover, the antifungal mechanisms of existing drugs are highlighted. These data will provide valuable knowledge to stimulate further investigation and clinical application in this field. Key points • Conventional antifungal agents have limitations due to the occurrence of drug-resistant strains. • Non-antifungal drugs act as antifungal agents in various ways toward different targets. • Non-antifungal drugs with antifungal activity are demonstrated as effective antifungal strategies.

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Section: Antibacterial Drugsmentioning

confidence: 99%

Drug repurposing strategies in the development of potential antifungal agents

Zhang

Liu

Zeng

et al. 2021

Appl Microbiol Biotechnol

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“…Candida spp. were studied in an ex vivo model of human dentinal tubule as observed in the study of Gowri et al This model closely resembles root canal infection in a human tooth. This ex vivo technique proved to be very effective for the evaluation of the fungal charge eradication by substances with antifungal potential in the dentinal tubules and has promising clinical applications .…”

Section: Alternative Methods That Simulate Fungal Infectionsmentioning

confidence: 99%

“…were studied in an ex vivo model of human dentinal tubule as observed in the study of Gowri et al This model closely resembles root canal infection in a human tooth. This ex vivo technique proved to be very effective for the evaluation of the fungal charge eradication by substances with antifungal potential in the dentinal tubules and has promising clinical applications . Bovine radicular dentine can also be used for the same purpose, as demonstrated in the study by Siqueira et al Spherical cylinders of the dentine were made and, after the experimental infection by C. albicans , were kept in contact with different drugs.…”

Section: Alternative Methods That Simulate Fungal Infectionsmentioning

confidence: 99%

Fungal infection models: Current progress ofex vivomethods

Quatrin

Lana

Kaminski

2019

Mycoses

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| INTRODUC TI ONThe principles developed by Russell and Burch in 1959, concerning the use of animals in research, have been updated in recent decades, and cover the use of tissues from dead animals as alternatives to in vivo methods. 1 In vivo tests generally involve a large number of specimens to obtain representative results, and the well-being of these animals has become an ethical issue to be respected. 2 The term ex vivo refers to the use of living tissues, which are removed from an organism in vivo, for the application in experiments that will be performed in an artificial environment. 3The murine models used to evaluate the therapeutic profile of new antifungal agents are addressed in several studies, such as induction of keratitis, onychomycosis, and systemic, vaginal, pulmonary and cutaneous infections. 4-9 However, it is important to maintain a balance between qualified science and animal well-being, using rational and ethical ways of research. In this scenario, ex vivo models that simulate fungal infections in nails, mucous membranes and skin are promising alternatives that have been showing considerable results. [10][11][12] In order to demonstrate new perspectives in the evaluation of antifungal therapy, we will approach a critical review of the main ex vivo techniques used in the simulation and treatment of mycoses, providing an adaptation of the widely used in vivo methods. | ME THODS | Data source SummaryExperimental alternative ex vivo models that simulate infectious processes in vivo are of fundamental importance for the evaluation of new drugs, since in some cases, their execution does not depend on the approval of an ethics committee in research.Although studies using alternative infectious models to evaluate the efficacy of antifungal molecules have been increasingly described and reported, there is no critical consensus that establishes the most appropriate ones regarding the type of infection. Numerous studies contemplate ex vivo protocols of fungal infections on nails, corneas, dentinal tubules and skin and reveal counterpoints and concordances not yet finely confronted. In this minireview, we propose a critical analysis of the main ex vivo models of fungal infections for the evaluation of new antifungal candidates for both topical and systemic use, as opposed to the advantages and disadvantages of the traditional in vivo models employed in preclinical research. K E Y W O R D S dentinal tubule infections, ex vivo models, mucosal infections, onychomycosis, skin infection, systemic infections | 861 MACIEL QUATRIN ET AL. How to cite this article: Maciel Quatrin P, Flores Dalla Lana D, Andrzejewski Kaminski TF, Meneghello Fuentefria A. Fungal infection models: Current progress of ex vivo methods.

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“…7) has been found to inhibit the 14α-demethylase and cAMP pathway in C. albicans. 89 The compound proved to have MIC values in the mid to high μg mL −1 range. Additionally, the triphenylethylene tamoxifen (12, Fig.…”

Section: Modification Combination and Repurposing Of Current Antifung...mentioning

confidence: 97%

A complex game of hide and seek: the search for new antifungals

2016

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Fungal infections directly affect millions of people each year. In addition to the invasive fungal infections of humans, the plants and animals that comprise our primary food source are also susceptible to diseases caused by these eukaryotic microbes. The need for antifungals, not only for our medical needs, but also for use in agriculture and livestock causes a high demand for novel antimycotics. Herein, we provide an overview of the most commonly used antifungals in medicine and agriculture. We also present a summary of the recent progress (from 2010–2016) in the discovery/development of new agents against fungal strains of medical/agricultural relevance, as well as information related to their biological activity, their mode(s) of action, and their mechanism(s) of resistance.

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β-lactam substituted polycyclic fused pyrrolidine/pyrrolizidine derivatives eradicate C. albicans in an ex vivo human dentinal tubule model by inhibiting sterol 14-α demethylase and cAMP pathway

Cited by 20 publications

References 46 publications

Drug repurposing strategies in the development of potential antifungal agents

Drug repurposing strategies in the development of potential antifungal agents

Fungal infection models: Current progress ofex vivomethods

A complex game of hide and seek: the search for new antifungals

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