Antifungal efficiency of miconazole and econazole and the interaction with transport protein: A comparative study

Abstract

Context: Miconazole (MIZ) and econazole (ECZ) are clinically used as antifungal drugs. Objective: The drug effect and binding property with transport protein human serum albumin of MIZ and ECZ were studied. Materials and methods: The antifungal efficiency was investigated by microdiluting drug solutions from 0 to 48 mmol L À1 through microcalorimetry and voltammetry studies. Transmission electron microscopy was used for morphological observations of C. albicans. The interaction with HSA was studied by electrochemical methods, fluorescence spectrometry, electron microscopy, and molecular simulation. , the peak currents increased to 4.887 and 6.024 mA. The peak currents of C. albicans in the presence of 20 and 48 mmol L À1 ECZ were 4.701 and 5.544 mA. The docking scores for MIZ and ECZ of the best binding conformation in site I and site II were 5.60, 4.79, 5.63, and 5.85. Discussion and conclusion: Strong inhibition to the metabolism of C. albicans and destructive effect was proved for both drugs. The lower IC 50 , growth rate constant of C. albicans, and higher peak current, reveal stronger antifungal activity of MIZ. Both drugs show an efficient quenching effect to intrinsic fluorescence residues of protein. MIZ mainly binds on site I while ECZ on site II. Molecular modeling experiments give further insight of the binding mechanism.

Action of econazole on Ca2+ levels and cytotoxicity in OC2 human oral cancer cells

“…1 It seemed econazole bound serum proteins, and was inappropriate for systemic application. 2 The cellular effect of econazole was similar to that of miconazole. 3 The mechanism of action of econazole is unclear.…”

Enhanced Antifungal and Wound Healing Efficacy of Statistically Optimized, Physicochemically Evaluated Econazole-Triamcinolone Loaded Silica Nanoparticles

“…Moreover, the emergence of resistant infections requires treatment with a combination of drugs ( Fotouhi et al, 2009 ). It was intended to develop a formulation to provide long-lasting benefits of an antimycotic, particularly azoles such as econazole nitrate ( Mangas-Sánchez et al, 2011 ) and a corticosteroid such as triamcinolone acetonide, used to treat multiple skin diseases but their use is limited used due to their poor aqueous solubility, poor penetration, and skin itching that eventually limits compliance with patient guidelines ( Agrawal et al, 2010 ; Hu et al, 2015 ).…”

Drug Enhancement, Synergism and Antifungal Activity of Miconazole Associated Polygodial Against Candida Albicans

“…An increase incidence of fungal infections is associated with some predisposing factors as the use of dentures, xerostomia, prolonged therapy with antibiotics, local trauma, malnutrition, endocrine disorders, increased longevity of people, among other states that diminish the quality of individual defense [1][2][3][4]. Oral candidiasis is one of the most common clinical features of those patients infected with the human immunodeficiency virus -HIV [5,6].Oral candidiasis treatment is based on four fundaments: making an early and accurate diagnosis of the infection; correcting the predisposing factors or underlying diseases; evaluating the type of Candida infection; appropriate use of antifungal drugs [7][8][9][10].Miconazole (MCZ) is a time-honored antifungal of the imidazole class. MCZ exerts a multipronged effect on fungi.…”