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

Paloukopoulou, Charikleia; Govari, Sofia; Soulioti, Athina; Stefanis, I; Angeli, Andrea; Matheeussen, An; Capasso, Clemente; Cos, Paul; Karioti, Anastasia

doi:10.1080/14786419.2021.1880406

Cited by 13 publications

(9 citation statements)

References 22 publications

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“…MgCA and MreCA showed a catalytic activity very similar to that of MpaCA. In particular, MreCA showed a k cat value = 1.06 × 10 6 s −1 and k cat /K M value = 1.07 x 10 8 M −1 s −1 [25], while MgCA exhibited a k cat value of 9.2 × 10 5 s −1 and k cat /K M value of 8.3 × 10 7 M −1 s −1 [27][28][29][30][31][32][33].…”

Section: Biochemical Characterization Of Mpacamentioning

confidence: 96%

“…The series AAZ-EPA (see Table 1 for their identification) involves classical CA inhibitors (CAIs) used in clinics for managing and treating glaucoma, idiopathic intracranial hypertension, altitude sickness, congestive heart failure, epilepsy, and other diseases [4,[36][37][38]43,45]. Recently, we reported the inhibition profiles of sulfonamides against MreCA and MgCA [26][27][28][29][30][31][32][33]. Since these two fungal CAs have been proposed as new pharmacological targets for combatting fungal infection and showed a different inhibition pattern toward CAIs [26][27][28][29][30][31][32][33], we decided to explore the in effect of the above-mentioned compounds on the activity of MpaCA.…”

Section: Inhibition Profile Of Mpaca With Sulfonamidesmentioning

confidence: 99%

“…Recently, we reported the inhibition profiles of sulfonamides against MreCA and MgCA [26][27][28][29][30][31][32][33]. Since these two fungal CAs have been proposed as new pharmacological targets for combatting fungal infection and showed a different inhibition pattern toward CAIs [26][27][28][29][30][31][32][33], we decided to explore the in effect of the above-mentioned compounds on the activity of MpaCA. The data of the other two Malassezia enzymes (MreCA and MgCA) are here provided for comparison purposes.…”

Section: Inhibition Profile Of Mpaca With Sulfonamidesmentioning

confidence: 99%

“…When the skin microenvironment or the host's defenses are compromised, this opportunistic commensal has the potential to become a disease-causing pathogen [21,22]. In this context, we determined that the genome of the M. pachydermatis contains a single gene encoding a β-CA (acronym MpaCA) that is closely related to β-CAs previously identified by our groups in two other Malassezia species, namely M. globosa and M. restricta, which are responsible for dandruff and seborrheic dermatitis [20,[25][26][27][28][29][30][31][32][33][34].…”

Section: Introductionmentioning

confidence: 97%

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

Luca

Angeli

Mazzone

et al. 2021

IJMS

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Fungi are exposed to various environmental variables during their life cycle, including changes in CO2 concentration. CO2 has the potential to act as an activator of several cell signaling pathways. In fungi, the sensing of CO2 triggers cell differentiation and the biosynthesis of proteins involved in the metabolism and pathogenicity of these microorganisms. The molecular machineries involved in CO2 sensing constitute a promising target for the development of antifungals. Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial enzymes in the CO2 sensing systems of fungi, because they catalyze the reversible hydration of CO2 to proton and HCO3-. Bicarbonate in turn boots a cascade of reactions triggering fungal pathogenicity and metabolism. Accordingly, CAs affect microorganism proliferation and may represent a potential therapeutic target against fungal infection. Here, the inhibition of the unique β-CA (MpaCA) encoded in the genome of Malassezia pachydermatis, a fungus with substantial relevance in veterinary and medical sciences, was investigated using a series of conventional CA inhibitors (CAIs), namely aromatic and heterocyclic sulfonamides. This study aimed to describe novel candidates that can kill this harmful fungus by inhibiting their CA, and thus lead to effective anti-dandruff and anti-seborrheic dermatitis agents. In this context, current antifungal compounds, such as the azoles and their derivatives, have been demonstrated to induce the selection of resistant fungal strains and lose therapeutic efficacy, which might be restored by the concomitant use of alternative compounds, such as the fungal CA inhibitors.

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Section: Biochemical Characterization Of Mpacamentioning

confidence: 96%

Section: Inhibition Profile Of Mpaca With Sulfonamidesmentioning

confidence: 99%

Section: Inhibition Profile Of Mpaca With Sulfonamidesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 97%

See 2 more Smart Citations

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

Luca

Angeli

Mazzone

et al. 2021

IJMS

Self Cite

View full text Add to dashboard Cite

show abstract

“…The OH moiety of the inhibitor was anchored to the zinc-coordinated water, making hydrogen bonds with Ser48 and Asp49 in the catalytic pocket [ 122 ]. MgCA was also investigated for its inhibition profile with various natural phenols, such as xanthomicrol and rosmarinic acid, which inhibited MgCA with a K IS = 0.6 and 2.2 µM, respectively [ 123 ].…”

Section: Kinetic Parameters and Inhibition Profiles Of Various Fungal Casmentioning

confidence: 99%

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

Supuran

Capasso

2021

IJMS

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Carbon dioxide (CO2), a vital molecule of the carbon cycle, is a critical component in living organisms’ metabolism, performing functions that lead to the building of compounds fundamental for the life cycle. In all living organisms, the CO2/bicarbonate (HCO3−) balancing is governed by a superfamily of enzymes, known as carbonic anhydrases (CAs, EC 4.2.1.1). CAs catalyze the pivotal physiological reaction, consisting of the reversible hydration of the CO2 to HCO3− and protons. Opportunistic and pathogenic fungi can sense the environmental CO2 levels, which influence their virulence or environmental subsistence traits. The fungal CO2-sensing is directly stimulated by HCO3− produced in a CA-dependent manner, which directly activates adenylyl cyclase (AC) involved in the fungal spore formation. The interference with CA activity may impair fungal growth and virulence, making this approach interesting for designing antifungal drugs with a novel mechanism of action: the inhibition of CAs linked to the CO2/HCO3−/pH chemosensing and signaling. This review reports that sulfonamides and their bioisosteres as well as inorganic anions can inhibit in vitro the β- and α-CAs from the fungi, suggesting how CAs may be considered as a novel “pathogen protein” target of many opportunistic, pathogenic fungi.

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Antimicrobial Properties of Selected Native Greek Aromatic Plants: An Ethnopharmacological Overview

Ganos

Gortzi

Chinou

et al. 2022

Promising Antimicrobials From Natural Products

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

Cited by 13 publications

References 22 publications

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

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

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

Antimicrobial Properties of Selected Native Greek Aromatic Plants: An Ethnopharmacological Overview

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