The synthesis and synergistic antifungal effects of chalcones against drug resistant Candida albicans

Wang, Yuanhua; Dong, Huai-Huai; Zhao, Fei; Jie, Wang; Fang, Yan; Jiang, Yuanying; Jin, Yong‐Sheng

doi:10.1016/j.bmcl.2016.05.013

Cited by 62 publications

(37 citation statements)

References 14 publications

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“…Natural source molecules with antifungal activity are also described as having in vitro synergistic activity with traditional antifungal drugs, reducing the concentration of both substances (Soares et al, 2014; Sardi et al, 2016; Wang et al, 2016). Use of the natural substance beauvericin with traditional antifungals was able to inhibit eﬄux pumps and morphogenesis in FLZ-resistant C. albicans and potentiate the action of this azole (Shekhar-Guturja et al, 2016).…”

Section: Drug Combinationsmentioning

confidence: 99%

Antifungal Therapy: New Advances in the Understanding and Treatment of Mycosis

et al. 2017

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The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of eﬄux pump proteins and biofilm formation, emphasizing the importance of understanding these mechanisms. To address these problems, different approaches to preventing and treating fungal diseases are described in this review, with a focus on the resistance mechanisms of fungi, with the goal of developing efficient strategies to overcoming and preventing resistance as well as new advances in antifungal therapy. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, and the synergistic effect obtained by the combination of antifungals contributes to reducing toxicity and could be an alternative for treatment. Another important issue is the development of new formulations for antifungal agents, and interest in nanoparticles as new types of carriers of antifungal drugs has increased. In addition, modifications to the chemical structures of traditional antifungals have improved their activity and pharmacokinetic parameters. Moreover, a different approach to preventing and treating fungal diseases is immunotherapy, which involves different mechanisms, such as vaccines, activation of the immune response and inducing the production of host antimicrobial molecules. Finally, the use of a mini-host has been encouraging for in vivo testing because these animal models demonstrate a good correlation with the mammalian model; they also increase the speediness of as well as facilitate the preliminary testing of new antifungal agents. In general, many years are required from discovery of a new antifungal to clinical use. However, the development of new antifungal strategies will reduce the therapeutic time and/or increase the quality of life of patients.

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Section: Drug Combinationsmentioning

confidence: 99%

Antifungal Therapy: New Advances in the Understanding and Treatment of Mycosis

et al. 2017

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“…For example, Palanco et al [48] tested the efficacy of 3 -hydroxychalcone. Chalcones, which are abundant in plants, have numerous pharmacological activities including antifungal action [80]. The efficacy of this compound was evaluated on groups of larvae infected by one isolate of C. gattii (collected from a psittacine bird) or the strain C. gattii ATCC 56990 (collected from a human).…”

Section: Cryptococcus Sppmentioning

confidence: 99%

Galleria mellonella for the Evaluation of Antifungal Efficacy against Medically Important Fungi, a Narrative Review

et al. 2020

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The treatment of invasive fungal infections remains challenging and the emergence of new fungal pathogens as well as the development of resistance to the main antifungal drugs highlight the need for novel therapeutic strategies. Although in vitro antifungal susceptibility testing has come of age, the proper evaluation of therapeutic efficacy of current or new antifungals is dependent on the use of animal models. Mammalian models, particularly using rodents, are the cornerstone for evaluation of antifungal efficacy, but are limited by increased costs and ethical considerations. To circumvent these limitations, alternative invertebrate models, such as Galleria mellonella, have been developed. Larvae of G. mellonella have been widely used for testing virulence of fungi and more recently have proven useful for evaluation of antifungal efficacy. This model is suitable for infection by different fungal pathogens including yeasts (Candida, Cryptococcus, Trichosporon) and filamentous fungi (Aspergillus, Mucorales). Antifungal efficacy may be easily estimated by fungal burden or mortality rate in infected and treated larvae. The aim of the present review is to summarize the actual data about the use of G. mellonella for testing the in vivo efficacy of licensed antifungal drugs, new drugs, and combination therapies.

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“…5 In chalcones, two aromatic rings are fused together through a three-carbon a,b-unsaturated carbonyl system. 6 Chalcones and avones containing various functional groups possess a wide range of biological and pharmacological activities such as antitumor, 7 antitubercular, 8 antiviral, 9 antiplatelet, 10 antifungal, 11 and cytotoxic 12 properties as well as enzyme inhibition. 13 1,2,3-Triazoles are nitrogen-rich ve-membered heterocycles and are preferred as structural components in various biologically active molecules due to their chemotherapeutic value.…”

Section: Introductionmentioning

confidence: 99%