Synthesis, antifungal activity of caffeic acid derivative esters, and their synergism with fluconazole and nystatin against Candida spp.

Sardi, Janaína de Cássia Orlandi; Gullo, Fernanda Patrícia; Freires, Irlan Almeida; Pitangui, Nayla de Souza; Segalla, Maicon Petrônio; Fusco‐Almeida, Ana Marisa; Rosalen, Pedro Luiz; Regasini, Luís Octávio; Mendes-Giannini, María José Soares

doi:10.1016/j.diagmicrobio.2016.08.002

Cited by 45 publications

(23 citation statements)

References 42 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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“…Three large families group the most commonly used anti- Nystatin perficial mycoses, such as flucytosine, griseofulvin and terbinafine, are not used commonly in oral candidiasis (7,8,11,(14)(15)(16)(17). Finally, other therapeutic alternatives under development involve the use of new antifungal drugs, terpens, probiotics, peptides with antifungal activity, sera with polyclonal or monoclonal antibodies or cocktails of cytokines (18)(19)(20)(21)(22)(23)(24)(25). The main mechanisms of antifungal action consist in the alteration of the membrane or the fungal cell wall by inhibition of molecules essential for these, such as ergosterol (azoles) or 1,3-ß-D-glucan (echinocandins), or by binding to ergosterol (polyenes), causing the formation of pores and altering the integrity and permeability of the cell membrane (Fig.…”

Section: Discussionmentioning

confidence: 99%

“…There are other pharmacological preparations that have antifungal activity and can be used in combination with antifungal drugs. These formulations include chlorhexidine, povidone iodine, solutions of gentian violet, potassium permanganate, methylene blue or sodium hyposulfite, propylene glycol, selenium sulphide, boric acid, and caffeic acid derivatives (17,21). Several investigational agents are currently under development against old targets, such as ergosterol (tetrazoles VT-1129, VT-1161, and VT-1598) or 1,3-β-D-glucan (extended half-life echinocandin CD101 or ibrexafungerp -SCY-078-) that may offer advantages over currently available drugs.…”

Section: Discussionmentioning

confidence: 99%

Therapeutic tools for oral candidiasis: Current and new antifungal drugs

Quindós

Gil-Alonso²,

Marcos‐Arias³

et al. 2019

Med Oral

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Background: Candidiasis is one of the most common opportunistic oral infections that presents different acute and chronic clinical presentations with diverse diagnostic and therapeutic approaches. The present study carries out a bibliographic review on the therapeutic tools available against oral candidiasis and their usefulness in each clinical situation. Material and Methods: Recent studies on treatment of oral candidiasis were retrieved from PubMed and Cochrane Library. Results: Nystatin and miconazole are the most commonly used topical antifungal drugs. Both antifungal drugs are very effective but need a long time of use to eradicate the infection. The pharmacological presentations of miconazole are more comfortable for patients but this drug may interact with other drugs and this fact should be assessed before use. Other topical alternatives for oral candidiasis, such as amphotericin B or clotrimazole, are not available in many countries. Oral fluconazole is effective in treating oral candidiasis that does not respond to topical treatment. Other systemic treatment alternatives, oral or intravenous, less used are itraconazole, voriconazole or posaconazole. Available novelties include echinocandins (anidulafungin, caspofungin) and isavuconazole. Echinocandins can only be used intravenously. Isavuconazole is available for oral and intravenous use. Other hopeful alternatives are new drugs, such as ibrexafungerp, or the use of antibodies, cytokines and antimicrobial peptides. Conclusions: Nystatin, miconazole, and fluconazole are very effective for treating oral candidiasis. There are systemic alternatives for treating recalcitrant infections, such as the new triazoles, echinocandins, or lipidic presentations of amphotericin B.

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“…But in our opinion, A. scaber which contains five important secondary metabolites namely, Caffeoyl quinic acid, (-) 3, 5-dicaffeoyl-muco-quinic acid, (-) 3, 5-dicaffeoyl quinic acid, (-) 4, 5-dicaffeoyl quinic acid, (-) 5-caffeoyl quinic acid with anti-fungal property, and A. dubia composed of caffeic acid, gallic acid, catechin, coumarin, and camphor could act against fungus. Nosema's place in the fungi kingdom lead us to speculate that both A. scaber and A. dubia could have anti nosemosis activity (Kwon.et al, 2000;Rhimi et al, 2017;Sardi et al, 2016;Li et al, 2017;Hirasawa & Takada, 2004;Montagner et al, 2008;Mahilrajan et al, 2014;Kiani et al, 2016). Fumagillin, isolated from the microbial organism A. fumigatus, has been used against a variety of microsporidial parasites in both bee and human medicine.…”

Section: Discussionmentioning

confidence: 99%

Anti-Nosemosis Activity of Aster scaber and Artemisia dubia Aqueous Extracts

Lee

Kim

Mi-Na

et al. 2018

Journal of Apicultural Science

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In our previous study, we demonstrated that the ethanol extracts of Artemisia dubia (A. dubia) and Aster scaber (A. scaber) have anti-nosemosis activity. In our present study, we intend to establish the anti-nosemosis activity of aqueous, ethyl acetate (EA), and butanol (BuOH) extracts of A. dubia and A. scaber. In order to determine the optimal dose, we performed both in vitro and in vivo toxicity for all the extracts and also carried out anti-nosemosis experiments. Although all of the extracts (aqueous, EA, and BuOH) showed in vitro and in vivo anti-nosemosis activity in a dose-dependent manner, the aqueous extracts of A. dubia and A. scaber showed more potent anti-nosemosis activity than the EA and BuOH extracts. Moreover, an aqueous extract of A. dubia + A. scaber demonstrated stronger anti-nosemosis activity compared with the aqueous extracts of either A. dubia or A. scaber alone. Although the main ingredients in A. dubia and A. scaber remain unclear, our results suggest that the active components of A. dubia and A. scaber could dissolve in the aqueous fraction.

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Synthesis, antifungal activity of caffeic acid derivative esters, and their synergism with fluconazole and nystatin against Candida spp.

Cited by 45 publications

References 42 publications

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

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

Therapeutic tools for oral candidiasis: Current and new antifungal drugs

Anti-Nosemosis Activity of Aster scaber and Artemisia dubia Aqueous Extracts

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