Abstract
In this work, we evaluated the antidermatophytic activities of three resorcinol derivatives that have a history of use in dermo-cosmetic applications to discover molecules with multiple dermatological activities (i.e., multi-target drugs), thereby reducing the cost and time necessary for new drug development. The antidermatophytic activities of the three skin lighteners were evaluated relative to the known antifungal drug fluconazole on nine dermatophytes responsible for the most common dermatomycoses: Microsporum gypseum, Microsporum canis, Trichophyton violaceum, Arthroderma cajetani, Trichophyton mentagrophytes, Epidermophyton floccosum, Nannizzia gypsea, Trichophyton rubrum and Trichophyton tonsurans. Among the three tested resorcinols, only two showed promising properties, with the ability to inhibit the growth of all tested dermatophytes; additionally, the IC50 values of these two resorcinols against the nine dermatophytes confirmed their good antifungal activity, particularly for phenylethyl resorcinol against M. gypseum. Ultrastructural alterations exhibited by the fungus were observed using scanning electron microscopy and transmission electron microscopy and reflected a dose-dependent response to treatment with the activation of defence and self-preservation strategies.
Highlights
We recently initiated a systematic study [1] that utilizes a multi-target drug discovery approach to discover new molecules with antifungal activities among drugs already used for other dermatological applications
In In thethe current study, we we investigated the the fungus using scanning electron microscopy and transmission electron microscopy and fungus using scanning electron microscopy and transmission electron microscopy
The results clearly show that fluconazole was less active than phenylethyl-resorcinol
Summary
We recently initiated a systematic study [1] that utilizes a multi-target drug discovery approach to discover new molecules with antifungal activities among drugs already used for other dermatological applications. The objective of this study is to discover novel antifungals with low toxicity, as proven by their long history of dermatological use. Resorcinol has a long history of therapeutic use for its keratolytic properties [2] and has been included, usually with sulphur, in topical preparations for the treatment of acne and seborrhoeic skin conditions, other treatments are generally preferred [2]. Resorcinol of the components in thein well-known. Resorcinol isisone one of the components the well-known.
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