Abstract

Multi-target strategies are directed toward targets that are unrelated (or distantly related) and can create opportunities to address different pathologies. The antidermatophytic activities of nine natural skin lighteners: α-bisabolol, kojic acid, β-arbutin, azelaic acid, hydroquinone, nicotinamide, glycine, glutathione and ascorbyl tetraisopalmitate, were evaluated, in comparison with the known antifungal drug fluconazole, on nine dermatophytes responsible for the most common dermatomycoses: Microsporum gypseum, Microsporum canis, Trichophyton violaceum, Nannizzia cajetani, Trichophyton mentagrophytes, Epidermophyton floccosum, Arthroderma gypseum, Trichophyton rubrum and Trichophyton tonsurans. α-Bisabolol showed the best antifungal activity against all fungi and in particular; against M. gypseum. Further investigations were conducted on this fungus to evaluate the inhibition of spore germination and morphological changes induced by α-bisabolol by TEM.

Highlights

  • The skin is our first line of defense against the outside world

  • For both the lower and higher doses of α-bisabolol, inhibition was greater than 50% for five fungi (M. gypseum, N. cajetani, T. mentagrophytes, T. tonsurans and A. gypseum)

  • IC50 values confirmed the interesting activity of α-bisabolol, in particular on M. gypseum

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Summary

Introduction

The skin is our first line of defense against the outside world. As the body’s border, it is subject to various microbiological attacks. If multi-target strategies are directed toward targets that are unrelated (or distantly related) an opportunity maybe created to target different pathologies In these regards, it is well known that skin hyperpigmentation is a relevant problem, affects a large portion of the world’s population, and is a particular social issue for black and elderly people. Α-bisabolol, kojic acid, β-arbutin, azelaic acid, hydroquinone, nicotinamide, glycine, glutathione and ascorbyl tetraisopalmitate were selected These nine molecules are already known in the literature for their action as skin lighteners [13,14,15,16,17] and are present in several commercial products. Α-bisabolol emerged as the most active compound; the following experiments focused on this molecule and its effects on the most sensitive of the nine fungi, M. gypseum. Investigations were conducted by TEM to confirm whether the mechanism of action for the inhibition of ergosterol synthesis by α-bisabolol, as suggested by Pauli [19] for other fungi, was responsible for its antifungal activity [21]

Antifungal Activity
Effect of Time and Spore Density on Percent Reduction of Resazurin
Inhibition of Spore Germination by Resazurin Assay
Chemicals
Microorganisms
Evaluation of Inhibition of Spore Germination of α-Bisabolol
Spectrophotometric Measurement and Visual Inspection
Conclusions
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