Literature DB >> 33533668

Phenols from Origanum dictamnus L. and Thymus vulgaris L. and their activity against Malassezia globosa carbonic anhydrase.

Charikleia Paloukopoulou1, Sofia Govari1, Athina Soulioti1, Ilias Stefanis1, Andrea Angeli2, An Matheeussen3, Clemente Capasso4, Paul Cos3, Claudiu T Supuran2, Anastasia Karioti1.   

Abstract

Malassezia spp. are lipophilic fungi that are part of the normal flora of the human skin and are the etiological agents of dandruff and seborrheic dermatitis. β-Carbonic Anhydrases (CAs; EC 4.2.1.1) expressed from the pathogenic fungi are an alternative/complementary drug target. Previous work by our groups demonstrated that flavonoids and depsides can effectively inhibit Malassezia globosa β-CA (MgCA). In continuation of this study herein we report the inhibitory activity of a variety of phenols from Origanum dictamnus L. and Thymus vulgaris L. against β-MgCA, among them I4-II7-di-carvacrol, a new natural product. Structure elucidation of the compounds was performed by 1 D, 2 D NMR and spectrometric analyses. Xanthomicrol and rosmarinic acid were active in the (sub)micromolar range (KIS 0.6 and 2.2 μM, respectively vs 40.0 μM of the standard inhibitor acetazolamide). Finally, the compounds were not cytotoxic, but showed in vitro no activity against Malassezia furfur.

Entities:  

Keywords:  I4-II7-di-carvacrol; Malassezia globosa; Origanum dictamnus L; Thymus vulgaris L. Varico 3; carbonic anhydrase; rosmarinic acid; xanthomicrol

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Year:  2021        PMID: 33533668     DOI: 10.1080/14786419.2021.1880406

Source DB:  PubMed          Journal:  Nat Prod Res        ISSN: 1478-6419            Impact factor:   2.861


  4 in total

Review 1.  A Highlight on the Inhibition of Fungal Carbonic Anhydrases as Drug Targets for the Antifungal Armamentarium.

Authors:  Claudiu T Supuran; Clemente Capasso
Journal:  Int J Mol Sci       Date:  2021-04-21       Impact factor: 5.923

2.  Inhibitory Effects of Sulfonamide Derivatives on the β-Carbonic Anhydrase (MpaCA) from Malassezia pachydermatis, a Commensal, Pathogenic Fungus Present in Domestic Animals.

Authors:  Viviana De Luca; Andrea Angeli; Valeria Mazzone; Claudia Adelfio; Fabrizio Carta; Silvia Selleri; Vincenzo Carginale; Andrea Scaloni; Claudiu T Supuran; Clemente Capasso
Journal:  Int J Mol Sci       Date:  2021-11-22       Impact factor: 5.923

3.  Heterologous expression and biochemical characterisation of the recombinant β-carbonic anhydrase (MpaCA) from the warm-blooded vertebrate pathogen malassezia pachydermatis.

Authors:  Viviana De Luca; Andrea Angeli; Valeria Mazzone; Claudia Adelfio; Vincenzo Carginale; Andrea Scaloni; Fabrizio Carta; Silvia Selleri; Claudiu T Supuran; Clemente Capasso
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.051

4.  Inhibition studies of the protozoan α-carbonic anhydrase from Trypanosoma cruzi with phenols.

Authors:  Alessandro Bonardi; Seppo Parkkila; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

  4 in total

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