In vitro and in vivo Activity of Phibilin Against Candida albicans

Li, Zhongjie; Jing, Xiaoyuan; Yuan, Yaping; Shui, Yingbin; Li, Shasha; Zhao, Zhuoran; Deng, Bo; Zhang, Wenlu

doi:10.3389/fmicb.2022.862834

Cited by 7 publications

(3 citation statements)

References 67 publications

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“…The plates were then incubated in aerobic conditions at 37 °C for 24 h. Later, the growth inhibition was assessed by measuring OD 595 using an Elisa plate reader (BioRad i-Mark). The MIC www.nature.com/scientificreports/ of acarbose is defined as the lowest concentration that inhibits the growth by ≥ 90% (for MIC90) or ≥ 50% (for MIC50) when compared to the control (untreated) using the formula ((control-test)/(control-blank)) *100 [46][47][48] .…”

Section: Susceptibility Of Planktonic Cellsmentioning

confidence: 99%

Mitigating candidiasis with acarbose by targeting Candida albicans α-glucosidase: in-silico, in-vitro and transcriptomic approaches

David,

Vasudevan,

Solomon

2024

Sci Rep

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Biofilm-associated candidiasis poses a significant challenge in clinical settings due to the limited effectiveness of existing antifungal treatments. The challenges include increased pathogen virulence, multi-drug resistance, and inadequate penetration of antimicrobials into biofilm structures. One potential solution to this problem involves the development of novel drugs that can modulate fungal virulence and biofilm formation, which is essential for pathogenesis. Resistance in Candida albicans is initiated by morphological changes from yeast to hyphal form. This transition triggers a series of events such as cell wall elongation, increased adhesion, invasion of host tissues, pathogenicity, biofilm formation, and the initiation of an immune response. The cell wall is a critical interface for interactions with host cells, primarily through various cell wall proteins, particularly mannoproteins. Thus, cell wall proteins and enzymes are considered potential antifungal targets. In this regard, we explored α-glucosidase as our potential target which plays a crucial role in processing mannoproteins. Previous studies have shown that inhibition of α-glucosidase leads to defects in cell wall integrity, reduced adhesion, diminished secretion of hydrolytic enzymes, alterations in immune recognition, and reduced pathogenicity. Since α-glucosidase, primarily converts carbohydrates, our study focuses on FDA-approved carbohydrate mimic drugs (Glycomimetics) with well-documented applications in various biological contexts. Through virtual screening of 114 FDA-approved carbohydrate-based drugs, a pseudo-sugar Acarbose, emerged as a top hit. Acarbose is known for its pharmacological potential in managing type 2 diabetes mellitus by targeting α-glucosidase. Our preliminary investigations indicate that Acarbose effectively inhibits C. albicans biofilm formation, reduces virulence, impairs morphological switching, and hinders the adhesion and invasion of host cells, all at very low concentrations in the nanomolar range. Furthermore, transcriptomic analysis reveals the mechanism of action of Acarbose, highlighting its role in targeting α-glucosidase.

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Section: Susceptibility Of Planktonic Cellsmentioning

confidence: 99%

Mitigating candidiasis with acarbose by targeting Candida albicans α-glucosidase: in-silico, in-vitro and transcriptomic approaches

David,

Vasudevan,

Solomon

2024

Sci Rep

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“…Phibilin was investigated in a mouse cutaneous infection model, in which C. albicans was injected subcutaneously and 1 h later phibilin was directly injected subcutaneously into the infected area, once daily for 3 days. Phibilin significantly reduced skin abscesses and total yeast numbers [ 57 ].…”

Section: Antimicrobial Peptides In Preclinical and Clinical Trialsmentioning

confidence: 99%

“…LL-III/43 alone prevented C. albicans biofilm formation on a material used in orthopedic surgeries (Ti-6Al-4 V alloy), but only the combination of LL-III/43 with clotrimazole prevented the formation of biofilms on urinary catheters [ 154 ]. Phibilin displayed in vitro synergistic effects with clotrimazole against C. albicans , but not with amphotericin B, nystatin or anidulafungin [ 57 ]. In a mouse model of Candida vaginitis, in which yeast biofilms were first established in mouse vaginas and then drugs were administered daily for 8 consecutive days, HPRP-A2 presented a synergistic effect when combined with chlorhexidine acetate.…”

Section: Antimicrobial Peptides In Combination Therapiesmentioning

confidence: 99%

Antimicrobial Peptides: Avant-Garde Antifungal Agents to Fight against Medically Important Candida Species

et al. 2023

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Expanding the antifungal drug arsenal for treating Candida infections is crucial in this era of the rising life expectancy of patients with immunosuppression and comorbidities. Infections caused by Candida species are on the rise, including those caused by multidrug-resistant strains or species, and the list of antifungals approved for the treatment of these infections is still limited. Antimicrobial peptides (AMPs) are short cationic polypeptides whose antimicrobial activity is under intense investigation. In this review, we present a comprehensive summary of the AMPs with anti-Candida activity that have undergone successful preclinical or clinical trials. Their source, mode of action, and animal model of infection (or clinical trial) are presented. In addition, as some of these AMPs have been tested in combination therapy, the advantages of this approach, as well as the studied cases that have used AMPs and other drugs concomitantly to fight Candida infections, are described.

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Buforins: A Potential Antimicrobial Peptide Explored With Its Anticancer Efficacy‐A Review

Adhikari,

Jena,

Kar

et al. 2024

Peptide Science

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Antimicrobial peptides (AMPs), derived from numerous life forms, is being recognised as favourable contenders in today's era to overcome the multi drug resistance of cancer cells. Despite of their diverse structural orientations (β‐sheet, α‐helical, loop and extended peptides), they are immensely involved in immune defences and potentially involved for combating cancers and other types of infections via cellular membrane depolarization. Buforins (Bf), the histone H2A derived AMPs along with their analogues (like Bf‐I, Bf‐II and Bf‐IIb) demonstrated substantial anticancer efficacy despite of numerous challenges. They are quite effective in controlling the apoptosis in various cancer cell lines like breast, HeLa, ovarian, lung, liver and prostate cancers. Bf conjugated with bioconjugates were explored for enhancing the bioavailability, drug resistance and stability of these super giants in cancer therapy. The functionalized nanoparticles could possibly help to overwhelm the shortcomings of AMPs, towards cancer therapy. However, the success of in vivo approach may lead to the clinical translation of such therapeutics. In this review, we emphasized on the characteristic features, mechanisms of action, numerous anticancer approaches of Bf. Further discussion was continued with the challenges and their overcoming, advancement and future directions of Bf towards their success in chemotherapy.

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In vitro and in vivo Activity of Phibilin Against Candida albicans

Cited by 7 publications

References 67 publications

Mitigating candidiasis with acarbose by targeting Candida albicans α-glucosidase: in-silico, in-vitro and transcriptomic approaches

Mitigating candidiasis with acarbose by targeting Candida albicans α-glucosidase: in-silico, in-vitro and transcriptomic approaches

Antimicrobial Peptides: Avant-Garde Antifungal Agents to Fight against Medically Important Candida Species

Buforins: A Potential Antimicrobial Peptide Explored With Its Anticancer Efficacy‐A Review

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