Antifungal properties of the anti-hypertensive drug: Aliskiren

Kathwate, Gunderao Hanumantrao; Karuppayil, Sankunny Mohan

doi:10.1016/j.archoralbio.2013.02.006

Cited by 14 publications

(5 citation statements)

References 22 publications

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“…Here, we anticipated that the adherent Candida cell count would be low. Given the fact that the OD of Candida cell suspension could be recognized at different wavelengths [ 48 , 49 ], we inspected the OD of the adherent Candida at 620 nm and 410 nm wavelengths. Moreover, CFU assay results of the adherent Candida revealed the marked effects of caffeine against Candida biofilm formation at all tested concentrations.…”

Section: Discussionmentioning

confidence: 99%

The Antifungal and Antibiofilm Activities of Caffeine against Candida albicans on Polymethyl Methacrylate Denture Base Material

et al. 2022

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Background: In this study, the effect of pure caffeine was established against Candida albicans (C. albicans) using different microbiological techniques. Methods: Broth microdilution and colony forming units (CFUs) assays were used to detect the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC). The Live/Dead fluorescent dyes were implemented to determine the yeast viability. Polymethyl methacrylate acrylic resin (PMMA) discs were prepared to evaluate caffeine’s effects against adherent C. albicans using microplate reader, CFUs, and scanning electron microscope (SEM). Results: caffeine’s MIC was detected around 30 mg/mL, while the MFC was considered at 60 mg/mL. In an agar-well diffusion test, the inhibition zones were wider in caffeine groups. The Live/Dead viability test verified caffeine’s antifungal effects. The optical density of the adherent C. albicans on PMMA discs were lower at 620 nm or 410 nm in caffeine groups. CFU count was also reduced by caffeine treatments. SEM revealed the lower adherent C. albicans count in caffeine groups. The effect of caffeine was dose-dependent at which the 60 mg/mL dose demonstrated the most prominent effect. Conclusion: The study reinforced caffeine’s antifungal and antibiofilm properties and suggested it as an additive, or even an alternative, disinfectant solution for fungal biofilms on denture surfaces.

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Section: Discussionmentioning

confidence: 99%

The Antifungal and Antibiofilm Activities of Caffeine against Candida albicans on Polymethyl Methacrylate Denture Base Material

et al. 2022

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“…Similarly, C. albicans can utilize alternative Sap proteins when one is compromised, removed or lost (Hube and Naglik, 2001). The Sap expression assays after exposure to antimicrobials are based on the in vitro Sap2 activity, the dominant secreted aspartic protease in vitro (Hube et al, 1994;Kathwate and Karuppayil, 2013;Wu et al, 2000).…”

Section: Discussionmentioning

confidence: 99%

Comparison of anti-Candida albicans activities of halogenomethylsulfonyl derivatives

2014

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A rapidly growing resistance of Candida spp. requires a search for bioactive compounds with fungicidal or fungistatic activity. In this context a characteristics and comparison of antifungal properties of 19 sulfone derivatives were conducted. MICs of the Compounds were determined using the M27-A3 protocol following CLSI recommendations. The SAP expression was analyzed using RT-PCR; relative quantification was normalized against ACT1 in cells grown in YEPD and on Caco-2. 79 % of sulfone derivatives (15 out of 19) exhibited an activity against Candida albicans in the tested concentrations. While the addition of both chlorine and bromine atoms to halogenomethylsulfonyl groups stimulates sulfone's antifungal activity, a chlorine atom more effectively up-regulates antifungal properties of the tested sulfones. The insertion of a fluorine atom has a binary effect on antifungal properties of the tested sulfones. The fluorine atom enhances anti-Candida properties when introduced to the aromatic ring, while its presence in halogenomethylsulfonyl group generally lowers the Compound's efficiency. The deletion of particular SAP genes resulted in an increased susceptibility of C. albicans toward sulfones indicating the role of this gene family in resistance mechanisms. Furthermore, RT-PCR analysis demonstrated that sulfone derivatives inhibit the SAP2 expression but not that of SAP7.

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“…Additionally, the compounds from a group of renin inhibitors, including A-70450 or A-79912, also inhibited the enzymatic activity of Sap2, but in vivo experiments revealed no protective effect [203][204][205][206]. Another renin inhibitor and drug used for hypertension treatment, aliskiren, also significantly reduced Saps activity, especially Sap2 [207]. In addition, in recent studies, structural analysis of compounds from Piper crocatum extract and molecular modeling revealed two potential ligands for Sap5, CHEMBL216163 and MLS000557666, forming bonds with enzymes that are considered important for efficient ligand binding [208].…”

Section: Protease Inhibitors As Prospective Agents Accompanying the T...mentioning

confidence: 99%

Secreted Aspartic Proteinases: Key Factors in Candida Infections and Host-Pathogen Interactions

Bras,

Satala,

Juszczak

et al. 2024

IJMS

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Extracellular proteases are key factors contributing to the virulence of pathogenic fungi from the genus Candida. Their proteolytic activities are crucial for extracting nutrients from the external environment, degrading host defenses, and destabilizing the internal balance of the human organism. Currently, the enzymes most frequently described in this context are secreted aspartic proteases (Saps). This review comprehensively explores the multifaceted roles of Saps, highlighting their importance in biofilm formation, tissue invasion through the degradation of extracellular matrix proteins and components of the coagulation cascade, modulation of host immune responses via impairment of neutrophil and monocyte/macrophage functions, and their contribution to antifungal resistance. Additionally, the diagnostic challenges associated with Candida infections and the potential of Saps as biomarkers were discussed. Furthermore, we examined the prospects of developing vaccines based on Saps and the use of protease inhibitors as adjunctive therapies for candidiasis. Given the complex biology of Saps and their central role in Candida pathogenicity, a multidisciplinary approach may pave the way for innovative diagnostic strategies and open new opportunities for innovative clinical interventions against candidiasis.

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Antifungal properties of the anti-hypertensive drug: Aliskiren

Cited by 14 publications

References 22 publications

The Antifungal and Antibiofilm Activities of Caffeine against Candida albicans on Polymethyl Methacrylate Denture Base Material

The Antifungal and Antibiofilm Activities of Caffeine against Candida albicans on Polymethyl Methacrylate Denture Base Material

Comparison of anti-Candida albicans activities of halogenomethylsulfonyl derivatives

Secreted Aspartic Proteinases: Key Factors in Candida Infections and Host-Pathogen Interactions

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