scholarly journals Cytosporone B as a Biological Preservative: Purification, Fungicidal Activity and Mechanism of Action against Geotrichum citri-aurantii

Biomolecules ◽  
2019 ◽  
Vol 9 (4) ◽  
pp. 125 ◽  
Author(s):  
Chunxiao Yin ◽  
Hongxin Liu ◽  
Yang Shan ◽  
Vijai Gupta ◽  
Yueming Jiang ◽  
...  
Keyword(s):  
Gene Ontology ◽  
Cell Membrane ◽  
Fungicidal Activity ◽  
Inhibitory Concentration ◽  
Membrane Integrity ◽  
Action Mechanism ◽  
Fungal Cell ◽  
Effect Concentration ◽  
Biological Preservative

To prevent citrus decay caused by Geotrichum citri-aurantii, 12 natural products were isolated from two endophytic fungi, in which cytosporone B was shown to have excellent bioactivity for control of G. citri-aurantii with median effect concentration (EC50) of 26.11 μg/mL and minimum inhibitory concentration (MIC) of 105 μg/mL, and also significantly reduced the decay of sugar orange during the in vivo trials. In addition, cytosporone B could alter the morphology of G. citri-aurantii by causing distortion of the mycelia and loss of membrane integrity. Differentially expressed genes (DEGs) between cytosporone B-treated and -untreated samples were revealed by Illumina sequencing, including 3540 unigenes. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses showed that most DEGs were related to metabolic production and cell membrane. These findings suggest cytosporone B is a promising biological preservative to control citrus decay and reveal the action mechanism of cytosporone B in relation to the destruction of the fungal cell membrane at both morphological and molecular levels.

scholarly journals Fungicidal Activity of a Safe 1,3,4-Oxadiazole Derivative Against Candida albicans

Pathogens ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 314
Author(s):  
Daniella Renata Faria ◽  
Raquel Cabral Melo ◽  
Glaucia Sayuri Arita ◽  
Karina Mayumi Sakita ◽  
Franciele Abigail Vilugron Rodrigues-Vendramini ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Fungicidal Activity ◽  
Inhibitory Concentration ◽  
Therapeutic Potential ◽  
Bloodstream Infections ◽  
Common Species ◽  
Future Application ◽  
Chemical Similarity ◽  
Preclinical Trials

Candida albicans is the most common species isolated from nosocomial bloodstream infections. Due to limited therapeutic arsenal and increase of drug resistance, there is an urgent need for new antifungals. Therefore, the antifungal activity against C. albicans and in vivo toxicity of a 1,3,4-oxadiazole compound (LMM6) was evaluated. This compound was selected by in silico approach based on chemical similarity. LMM6 was highly effective against several clinical C. albicans isolates, with minimum inhibitory concentration values ranging from 8 to 32 µg/mL. This compound also showed synergic effect with amphotericin B and caspofungin. In addition, quantitative assay showed that LMM6 exhibited a fungicidal profile and a promising anti-biofilm activity, pointing to its therapeutic potential. The evaluation of acute toxicity indicated that LMM6 is safe for preclinical trials. No mortality and no alterations in the investigated parameters were observed. In addition, no substantial alteration was found in Hippocratic screening, biochemical or hematological analyzes. LMM6 (5 mg/kg twice a day) was able to reduce both spleen and kidneys fungal burden and further, promoted the suppresses of inflammatory cytokines, resulting in infection control. These preclinical findings support future application of LMM6 as potential antifungal in the treatment of invasive candidiasis.

scholarly journals Effect of Bacoside A on growth and biofilm formation by Staphylococcus aureus and Pseudomonas aeruginosa

2017 ◽  
Vol 63 (2) ◽  
pp. 169-178 ◽  
Author(s):  
Debaprasad Parai ◽  
Ekramul Islam ◽  
Jayati Mitra ◽  
Samir Kumar Mukherjee
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Cell Membrane ◽  
Extracellular Polymeric Substances ◽  
Inhibitory Concentration ◽  
Membrane Integrity ◽  
Bacterial Biofilm ◽  
Antibiofilm Activity ◽  
Bacoside A ◽  
Microscopic Studies

The goal of this study was to evaluate the antibiofilm and antimicrobial activities of Bacoside A, a formulation of phytochemicals from Bacopa monnieri, against Staphylococcus aureus and Pseudomonas aeruginosa, which are known to form biofilms as one of their virulence traits. The antimicrobial effects of Bacoside A were tested using the minimum inhibitory concentration and minimum bactericidal concentration assays. A cell membrane disruption assay was performed to find its possible target site. MTT assay, crystal violet assay, and microscopic studies were performed to assess the antibiofilm activity. Bacoside A showed antimicrobial activity against both test organisms in their planktonic and biofilm states. At a subminimum inhibitory concentration of 200 μg·mL−1, Bacoside A significantly removed ∼88%–93% of bacterial biofilm developed on microtiter plates. Biochemical and microscopic studies suggested that the eradication of biofilm might be due to the loss of extracellular polymeric substances and to a change in cell membrane integrity of the selected bacterial strains treated with Bacoside A. These results indicate that Bacoside A might be considered as an antimicrobial having the ability to disrupt biofilms. Thus, either alone or in combination with other therapeutics, Bacoside A could be useful to treat biofilm-related infections caused by opportunistic bacterial pathogens.

scholarly journals ECHINOCANDINS VERSUS DATED ANTIFUNGALS IN COMBINATION AGAINST OPPORTUNISTIC MYCOTIC INFECTIONS

2017 ◽  
Vol 10 (8) ◽  
pp. 54
Author(s):  
Mrridula Dangi Narwal ◽  
Meenakshi Balhara ◽  
Renu Chaudhary ◽  
Chhillar Ak
Keyword(s):  
Fungal Pathogens ◽  
Fungicidal Activity ◽  
Major Constituent ◽  
Laboratory Studies ◽  
Candida Spp ◽  
Fungal Cell ◽  
Development Of Resistance ◽  
Mycotic Infections

Scientific and clinical reports globally demonstrated that the opportunistic mycotic infections are at major risk to the human fitness. In past few decades, development of resistance in microbes to existing antifungals, has emphasized on the search of new antimycotic drugs. As a matter of fact "echinocandins" are new categories of broad-spectrum antifungal enlighten a hope in this direction. Echinocandins are bulky lipopeptides that inhibits the production of β-[1,3]-glucan "a major constituent of fungal cell wall" which ultimately leads to the death of fungal pathogens. In vitro as well as in vivo published reports have demonstrated that the echinocandins exhibit fungicidal activity against most Candida spp while fungistatic against Aspergillus spp and exclusively found to be more effective when tested in combination with polyenes/azoles. Present article is an expert views on the recent and historical literature available on the antifungal therapies with accessing their impact on the human health. Emphasis is given on the utility of the echinocandins as potential antifungal agent by discussing recent examples of clinical and laboratory studies including the use of improved proteomics approaches to know a bit more about the interaction of human host and fungal pathogens.

scholarly journals Lovastatin Has Significant Activity against Zygomycetes and Interacts Synergistically with Voriconazole

2006 ◽  
Vol 50 (1) ◽  
pp. 96-103 ◽  
Author(s):  
Georgios Chamilos ◽  
Russell E. Lewis ◽  
Dimitrios P. Kontoyiannis
Keyword(s):  
Fungicidal Activity ◽  
Inhibitory Concentration ◽  
Effective Concentration ◽  
Significant Activity ◽  
In Vitro Activity ◽  
Testing Methods ◽  
Disk Diffusion Testing ◽  
Dye Staining

ABSTRACT Zygomycetes are emerging opportunistic molds resistant to most conventional antifungals. We evaluated the in vitro activity of lovastatin (LOV), a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, against seven clinical isolates of Zygomycetes by using standard microdilution methods in three different media, disk diffusion testing, and viability dye staining. To further study the in vivo efficacy of LOV against zygomycetes, we developed a Drosophila melanogaster model of zygomycosis. In different experiments, groups of Toll-deficient (Tl) flies fed LOV-containing food were subsequently injected with two representative Zygomycetes isolates (Mucor and Rhizopus spp.). Finally, we examined the effects of LOV on voriconazole (VRC) activity against zygomycetes in vitro by checkerboard dilution, Epsilometer test-based methods, and bis-(1,3-dibutylbarbituric acid) trimethine oxonol staining and in vivo in Tl flies fed food containing LOV plus VRC and infected with zygomycetes. LOV exhibited significant, medium, and strain-independent fungicidal activity against all Zygomycetes isolates in vitro by all testing methods (MIC50, 48.0 μg/ml; 50% minimal fungicidal concentration, 56.0 μg/ml; 50% effective concentration, 29.4 μg/ml [6.6 to 38.9 μg/ml]). Tl flies fed LOV-containing food and infected with Mucor had a significantly better 6-day survival rate than did infected Tl flies fed regular food (P = 0.0005). LOV displayed in vitro synergy with VRC against all Zygomycetes isolates (fractional inhibitory concentration index, 0.104 to 0.290) by all methods used. LOV also displayed synergy with VRC in the Drosophila model of zygomycosis (P < 0.01). LOV is significantly active against zygomycetes and synergizes with triazoles inherently resistant to them, such as VRC. The clinical significance of these findings needs to be further explored.

scholarly journals Novel 2,4-Disubstituted-1,3-Thiazole Derivatives: Synthesis, Anti-Candida Activity Evaluation and Interaction with Bovine Serum Albumine

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1079 ◽  
Author(s):  
Andreea-Iulia Pricopie ◽  
Monica Focșan ◽  
Ioana Ionuț ◽  
Gabriel Marc ◽  
Laurian Vlase ◽  
...  
Keyword(s):  
Bovine Serum ◽  
Membrane Integrity ◽  
Antifungal Drugs ◽  
Thiazole Derivatives ◽  
Molecular Docking Study ◽  
Binding Interaction ◽  
Fungal Cell ◽  
Broth Microdilution Method

Herein we report the synthesis of two novel series of 1,3-thiazole derivatives having a lipophilic C4-substituent on account of the increasing need for novel and versatile antifungal drugs for the treatment of resistant Candida sp.-based infections. Following their structural characterization, the anti-Candida activity was evaluated in vitro while using the broth microdilution method. Three compounds exhibited lower Minimum Inhibitory Concentration (MIC) values when compared to fluconazole, being used as the reference antifungal drug. An in silico molecular docking study was subsequently carried out in order to gain more insight into the antifungal mechanism of action, while using lanosterol-C14α-demethylase as the target enzyme. Fluorescence microscopy was employed to further investigate the cellular target of the most promising molecule, with the obtained results confirming its damaging effect towards the fungal cell membrane integrity. Finally, the distribution and the pharmacological potential in vivo of the novel thiazole derivatives was investigated through the study of their binding interaction with bovine serum albumin, while using fluorescence spectroscopy.

scholarly journals Internalization and membrane activity of the antimicrobial peptide CGA-N12

2021 ◽  
Author(s):  
Ruifang Li ◽  
Mengke Tao ◽  
Shang Li ◽  
Xueqin Wang ◽  
Yanhui Yang ◽  
...  
Keyword(s):  
Cell Membrane ◽  
Fungicidal Activity ◽  
Membrane Integrity ◽  
Antimicrobial Activities ◽  
Antagonist Activity ◽  
Cell Membrane Integrity ◽  
Membrane Activity ◽  
Dependent Inhibition ◽  
Energy Dependent ◽  
Time Dependent Inhibition

Antimicrobial peptides (AMPs) are conventional antibiotic alternatives due to their broad-spectrum antimicrobial activities and special mechanisms of action against pathogens. The antifungal peptide CGA-N12 was originally derived from human chromogranin A (CGA) and consists of the 65th to 76th amino acids of the CGA N-terminal region. In the present study, we found that CGA-N12 had fungicidal activity and exhibited time-dependent inhibition activity against Candida tropicalis. CGA-N12 entered the cells to exert its antagonist activity. The internalization of CGA-N12 was energy-dependent and accompanied by actin cytoskeleton-, clathrin-, sulfate proteoglycan-, endosome-, and lipid-depleting agent-mediated endocytosis. Moreover, the CGA-N12 internalization pathway was related to the peptide concentration. The effects of CGA-N12 on the cell membrane were investigated. CGA-N12 at low concentration less than 4×MIC100 did not destroy the cell membrane. While with increasing concentration, the damage to the cell membrane caused by CGA-N12 became more serious. At concentrations greater than 4×MIC100, CGA-N12 destroyed the cell membrane integrity. Therefore, the membrane activity of CGA-N12 is concentration dependant.

Conventional Versus Natural Alternative Treatments for Leishmaniasis: A Review

2018 ◽  
Vol 18 (15) ◽  
pp. 1275-1286 ◽  
Author(s):  
Luiz Felipe Domingues Passero ◽  
Lucas Antal Cruz ◽  
Gabriela Santos-Gomes ◽  
Eliana Rodrigues ◽  
Márcia Dalastra Laurenti ◽  
...  
Keyword(s):  
Side Effects ◽  
Visceral Leishmaniasis ◽  
Traditional Knowledge ◽  
Conventional Therapy ◽  
Pathogenic Species ◽  
Action Mechanism ◽  
In Vivo Assays ◽  
Clinical Forms

Leishmaniasis is a neglected disease caused by protozoan belonging to the Leishmania genus. There are at least 16 pathogenic species for humans that are able to cause different clinical forms, such as cutaneous or visceral leishmaniasis. In spite of the different species and clinical forms, the treatment is performed with few drug options that, in most cases, are considered outdated. In addition, patients under classical treatment show serious side effects during drug administration, moreover parasites are able to become resistant to medicines. Thus, it is believed and well accepted that is urgent and necessary to develop new therapeutic options to overpass these concerns about conventional therapy of leishmaniasis. The present review will focus on the efficacy, side effects and action mechanism of classic drugs used in the treatment of leishmaniasis, as well as the importance of traditional knowledge for directing a rational search toward the discovery and characterization of new and effective molecules (in vivo assays) from plants to be used against leishmaniasis.

Light Chain LC and TAT-EGFP-HCS of Botulinum Toxin Expression and Biological Function in vitro and in vivo

2019 ◽  
Vol 16 (3) ◽  
pp. 175-180
Author(s):  
Fengjin Hao ◽  
Yueqin Feng ◽  
Yifu Guan
Keyword(s):  
Biological Activity ◽  
Botulinum Toxin ◽  
Cell Membrane ◽  
Western Blot ◽  
Biological Function ◽  
C6 Cells ◽  
Green Fluorescence ◽  
Bv2 Cells

Objective: To verify whether the botulinum toxin heavy chain HCS has specific neuronal targeting function and to confirm whether TAT-EGFP-LC has hydrolyzable SNAP-25 and has transmembrane biological activity. Methods: We constructed the pET-28a-TAT-EGFP-HCS/LC plasmid. After the plasmid is expressed and purified, we co-cultured it with nerve cells or tumors. In addition, we used Western-Blot to identify whether protein LC and TAT-EGFP-LC can digest the protein SNAP-25. Results: Fluorescence imaging showed that PC12, BV2, C6 and HeLa cells all showed green fluorescence, and TAT-EGFP-HCS had the strongest fluorescence. Moreover, TAT-EGFP-LC can hydrolyze intracellular SNAP-25 in PC12 cells, C6 cells, BV2 cells and HeLa, whereas LC alone cannot. In addition, the in vivo protein TAT-EGFP-HCS can penetrate the blood-brain barrier and enter mouse brain tissue. Conclusion: TAT-EGFP-HSC expressed in vitro has neural guidance function and can carry large proteins across the cell membrane without influencing the biological activity.

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