scholarly journals Exploration of Novel TOSMIC Tethered Imidazo[1,2-a]pyridine Compounds for the Development of Potential Antifungal Drug Candidate.

2021 ◽  
Author(s):  
Pratibha Shukla ◽  
Deepa Deswal ◽  
Mansi Pandit ◽  
N Latha ◽  
Divyank Mahajan ◽  
...  
Keyword(s):  
Fungal Growth ◽  
Drug Candidate ◽  
Fluorescent Properties ◽  
Fungal Cell ◽  
Antifungal Effect ◽  
Antifungal Potential ◽  
Confocal Images ◽  
Fungal Growth Inhibition

Abstract New candidates of imidazo [1, 2-a] pyridine were designed by combining 2-amino pyridine, TOSMIC isocyanide and various assorted aldehydes were synthesized to explore their antioxidant and antifungal potential. The design of these derivatives was based on utilizing the antifungal potential of azoles and TOSMIC moiety. These derivatives were synthesized by adopting multi-component reaction methodology, as it serves as a rapid and efficient tool to target structurally diverse heterocyclic compounds in quantitative yield. The resulting imidazo [1, 2-a] pyridine derivatives were structurally verified by 1HNMR and 13CNMR. The compounds were analyzed for their antioxidant and fluorescent properties and it was observed that compound 15 depicted good fluorescence and antioxidant potential. Additionally, the compounds were evaluated for their antifungal potential against both Aspergillus fumigatus 3007 & Candida albicans 3018 and it was observed that all the compounds had moderate to significant antifungal effect. Confocal images depicted the porous nature of compound treated fungal cell membranes leading to fungal growth inhibition. Molecular docking was performed to establish the interaction with the target enzyme (Lanosterol 14 alpha demethylase) which also corroborated with the in vitro results. In silico tools were employed to determine drug-likeliness of the compounds along with determination of ADME properties.

scholarly journals Antifungal activity of components used for decontamination of dental prostheses on the growth of Candida albicans

2014 ◽  
Vol 43 (2) ◽  
pp. 137-142 ◽  
Author(s):  
Cíntia Lima Gouveia ◽  
Isabelle Cristine Melo Freire ◽  
Maria Luísa de Alencar e Silva Leite ◽  
Rebeca Dantas Alves Figueiredo ◽  
Leopoldina de Fátima Dantas de Almeida ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Sodium Bicarbonate ◽  
Fungal Growth ◽  
Antifungal Effect ◽  
Dental Prostheses ◽  
Diffusion Technique ◽  
Zones Of Inhibition ◽  
And Control

Introduction: The effectiveness of antimicrobial solutions employed in dental prosthesis decontamination is still uncertain. Aim: To evaluate the antifungal activity of cleaners used in the decontamination of dental prostheses on the growth of Candida albicans. Material and method: The evaluated products were: Corega Tabs(r) (S1), Sodium Hypochlorite 1% (S2), Sodium Bicarbonate 1% (S3), Hydrogen Peroxide 1% (S4), Chlorhexidine Digluconate 0.12% - Periogard (r) (S5), Mouthrinse based on essential oils - Listerine(r) (S6), essential oil from Rosmarinus officinalis (rosemary) at concentrations of 1% (S7) and 2% (S8). The antifungal activity of the products was evaluated by agar diffusion technique and the determination of microbial death curve of samples of C. albicans (ATCC 90028) in concentration 1.5 × 106 CFU/mL. The tests were performed in triplicate and statistical analysis was made by ANOVA Two-Way and Tukey tests, with the confidence level of 95%. Result: The average of the zones of inhibition growth, in millimeters, obtained for the products were: 0.0 (S1), 44.7 (S2), 0.0 (S3), 21.6 (S4), 10.0 (S5), 6.1 (S6), 0.0 (S7) and 2.4 (S8). Considering the determination of microbial death curve, all products showed a statistical difference (p<0.01) from control (0.85% sodium chloride) and S3 groups. Fungal growth less than 2×104 CFU/mL and an accentuation of the microbial death curve were observed after 30 minutes, with exception for S3 and control groups. Conclusion: The studied compounds, with the exception of Sodium Bicarbonate, have antifungal effect against C. albicans, which contribute for dental prostheses hygiene.

Secondary metabolites from endophytic Streptomyces aureofaciens CMUAc130 and their antifungal activity

Microbiology ◽  
2005 ◽  
Vol 151 (5) ◽  
pp. 1691-1695 ◽  
Author(s):  
Thongchai Taechowisan ◽  
Chunhua Lu ◽  
Yuemao Shen ◽  
Saisamorn Lumyong
Keyword(s):  
Culture Filtrate ◽  
Fungal Growth ◽  
Zingiber Officinale ◽  
Phytopathogenic Fungi ◽  
Active Ingredients ◽  
Streptomyces Aureofaciens ◽  
Mass Spectral ◽  
Causative Agents ◽  
Fungal Growth Inhibition

Streptomyces aureofaciens CMUAc130 was isolated from the root tissue of Zingiber officinale Rosc. (Zingiberaceae). It was an antagonist of Colletotrichum musae and Fusarium oxysporum, the causative agents of anthracnose of banana and wilt of wheat, respectively. Evidence for the in vitro antibiosis of S. aureofaciens CMUAc130 was demonstrated by the zone of fungal-growth inhibition. Microscopic observations showed thickness and bulbous structures at the edges of the inhibited fungal hyphae. The culture filtrate and crude extract from this strain were all inhibitory to tested phytopathogenic fungi. The major active ingredients from the culture filtrate of S. aureofaciens CMUAc130 were purified by silica gel-column chromatography and identified to be (i) 5,7-dimethoxy-4-p-methoxylphenylcoumarin and (ii) 5,7-dimethoxy-4-phenylcoumarin by NMR and mass-spectral data, respectively. Bioassay studies showed that compounds (i) and (ii) had antifungal activities against tested fungi, and their MICs were found to be 120 and 150 μg ml−1, respectively. This is the first report of compounds (i) and (ii) from micro-organisms as active ingredients for the control of phytopathogenic fungi.

scholarly journals Human Antibodies against a Purified Glucosylceramide from Cryptococcus neoformans Inhibit Cell Budding and Fungal Growth

2000 ◽  
Vol 68 (12) ◽  
pp. 7049-7060 ◽  
Author(s):  
Marcio L. Rodrigues ◽  
Luiz R. Travassos ◽  
Kildare R. Miranda ◽  
Anderson J. Franzen ◽  
Sonia Rozental ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Cell Wall ◽  
Cryptococcus Neoformans ◽  
High Performance ◽  
Fungal Growth ◽  
Fungal Cell ◽  
Human Antibodies ◽  
Different Strains ◽  
Immunofluorescence Labeling

ABSTRACT A major ceramide monohexoside (CMH) was purified from lipidic extracts of Cryptococcus neoformans. This molecule was analyzed by high-performance thin-layer chromatography (HPTLC), gas chromatography coupled with mass spectrometry, and fast atom bombardment-mass spectrometry. The cryptococcal CMH is a β-glucosylceramide, with the carbohydrate residue attached to 9-methyl-4,8-sphingadienine in amidic linkage to 2-hydroxyoctadecanoic acid. Sera from patients with cryptococcosis and a few other mycoses reacted with the cryptococcal CMH. Specific antibodies were purified from patients' sera by immunoadsorption on the purified glycolipid followed by protein G affinity chromatography. The purified antibodies to CMH (mainly immunoglobulin G1) bound to different strains and serological types of C. neoformans, as shown by flow cytofluorimetry and immunofluorescence labeling. Transmission electron microscopy of yeasts labeled with immunogold-antibodies to CMH and immunostaining of isolated cell wall lipid extracts separated by HPTLC showed that the cryptococcal CMH predominantly localizes to the fungal cell wall. Confocal microscopy revealed that the β-glucosylceramide accumulates mostly at the budding sites of dividing cells with a more disperse distribution at the cell surface of nondividing cells. The increased density of sphingolipid molecules seems to correlate with thickening of the cell wall, hence with its biosynthesis. The addition of human antibodies to CMH to cryptococcal cultures of both acapsular and encapsulated strains of C. neoformans inhibited cell budding and cell growth. This process was complement-independent and reversible upon removal of the antibodies. The present data suggest that the cryptococcal β-glucosylceramide is a fungal antigen that plays a role on the cell wall synthesis and yeast budding and that antibodies raised against this component are inhibitory in vitro.

scholarly journals Evaluation of Antifungal Activity of Chitosan Nanoparticles Against Fusarium Solani Phytopathogenic Fungi in in Vitro and in Vivo Assays

2021 ◽  
Author(s):  
Pamela R. Avila ◽  
Graciela Juez Castillo ◽  
Carel E. Carvajal
Keyword(s):  
Antifungal Activity ◽  
Fusarium Solani ◽  
Plant Root ◽  
Chitosan Nanoparticles ◽  
Fungal Growth ◽  
Fungal Cell ◽  
Tomato Root ◽  
Root Cells

Abstract Fungal diseases are a current problem in agriculture causing significant losses in several crops whereby its prevention and treatment is of utmost importance. The Chitosan nanoparticles (ChNPs) were evaluated for their antimicrobial activity against the phytopathogen Fusarium solani. The chitosan concentration in nanoparticles that showed antifungal activity was 2.0 µg/mL. ChNPs showed to be a potential antifungal candidate with applications in phytosanitary control. Transmission electron microscopy (TEM) results showed damage to the fungal cell wall and membrane caused by the nanoparticles interaction with these structures affecting fungal growth and development in in vitro as in in vivo assay where microscopy demonstrated the internalization of nanoparticles aggregates within plant root cells cytoplasm up to 45 days. Therefore ChNPs nanoparticles could be an alternative method for diseases caused by Fusarium solani instead of chemical fungicides commonly used for treating tomato root rot.

scholarly journals Antifungal effects of ZnO, TiO2 and ZnO-TiO2 nanocomposite on Aspergillus flavus

2020 ◽  
Author(s):  
nasrollah najibi ilkhechi ◽  
Mahdi Mozammel ◽  
Ahmad Yari Khoroushahi
Keyword(s):  
Aspergillus Flavus ◽  
Sol Gel ◽  
Fungal Growth ◽  
Titanium Isopropoxide ◽  
Morphological Characterization ◽  
Antifungal Compound ◽  
Inhibition Concentration ◽  
Stress Oxidative ◽  
Fungal Growth Inhibition

Abstract This study aimed to synthesis ZnO, TiO2 and ZnO–TiO2 (ratio weight of 1/1 for Zn/Ti) nanoparticles using zinc acetate and titanium isopropoxide through the sol-gel method. Physicochemical and morphological characterization and antifungal properties evaluation like minimum inhibition concentration (MIC) and minimum fungicide concentration (MFC) of nanopowders were investigated against Aspergillus flavus at in vitro. All synthesized nanoparticles (50 µg/ml) showed fungal growth inhibition while ZnO-TiO2 showed higher antifungal activity against A. flavus than pure TiO2 and ZnO. TiO2 and ZnO-TiO2 (300 µg/ml) inhibited 100% of spur production. Pure ZnO and TiO2 showed pyramidal and spherical shapes, respectively whereas ZnO-TiO2 nanopowders illustrated both spherical and pyramidal shapes with grown particles on the surface. Based on our findings, low concentration (150 µg/ml) of ZnO-TiO2 showed higher ROS production and stress oxidative induction thus fungicide effect as compared to alone TiO2 and ZnO. In conclusion, ZnO-TiO2 nanostructure can be utilized as an effective antifungal compound but more studies need to be performed to understand the antifungal mechanism of the nanoparticles rather than ROS inducing apoptosis.

The MTT [3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide] Assay Is a Fast and Reliable Method for Colorimetric Determination of Fungal Cell Densities

1999 ◽  
Vol 65 (8) ◽  
pp. 3727-3729 ◽  
Author(s):  
Florian M. Freimoser ◽  
Claude A. Jakob ◽  
Markus Aebi ◽  
Urs Tuor
Keyword(s):  
Colorimetric Method ◽  
Medium Composition ◽  
Colorimetric Determination ◽  
Fungal Cell ◽  
Diphenyltetrazolium Bromide ◽  
Hyphal Bodies ◽  
Growth Promoting ◽  
Cell Densities

ABSTRACT The entomopathogenic fungus Neozygites parvispora(Entomophthorales: Zygomycetes) grows in vitro as irregularly rod-shaped hyphal bodies in a complex medium. In order to simplify the medium composition and determine growth-promoting compounds for the cultivation of this fungus, we were looking for a rapid and quantitative method to estimate the number of living cells in small volumes of liquid culture. A colorimetric method for the determination of cell densities using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] proved to be more accurate and timesaving than conventional hemocytometer counting.

scholarly journals Sphingolipid biosynthetic pathway is crucial for growth, biofilm formation and membrane integrity of Scedosporium boydii

2019 ◽  
Vol 11 (22) ◽  
pp. 2905-2917 ◽  
Author(s):  
Rodrigo Rollin-Pinheiro ◽  
Victor Pereira Rochetti ◽  
Mariana Ingrid Dutra da Silva Xisto ◽  
Livia Cristina Liporagi-Lopes ◽  
Beatriz Bastos ◽  
...  
Keyword(s):  
Cell Biology ◽  
Pathogenic Fungus ◽  
Membrane Integrity ◽  
Fungal Growth ◽  
Antifungal Drugs ◽  
Wide Range ◽  
Antifungal Potential ◽  
Sphingolipid Biosynthesis ◽  
Increased Susceptibility

Aim: Glycosphingolipids are conserved lipids displaying a variety of functions in fungal cells, such as determination of cell polarity and virulence. They have been considered as potent targets for new antifungal drugs. The present work aimed to test two inhibitors, myriocin and DL-threo-1-Phenyl-2-palmitoylamino-3-morpholino-1-propanol, in Scedosporium boydii, a pathogenic fungus which causes a wide range of disease. Materials & methods: Mass spectrometry, microscopy and cell biology approaches showed that treatment with both inhibitors led to defects in fungal growth and membrane integrity, and caused an increased susceptibility to the current antifungal agents. Conclusion: These data demonstrate the antifungal potential of drugs inhibiting sphingolipid biosynthesis, as well as the usefulness of sphingolipids as promising targets for the development of new therapeutic options.

scholarly journals Identification of sulfur components enhancing the anti-Candida effect of Lactobacillus rhamnosus Lcr35

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Caroline Dausset ◽  
Stéphanie Bornes ◽  
Sylvie Miquel ◽  
Nathalie Kondjoyan ◽  
Magaly Angenieux ◽  
...  
Keyword(s):  
Sulfur Compound ◽  
Sodium Thiosulfate ◽  
Lactobacillus Rhamnosus ◽  
Active Metabolites ◽  
Fungal Cell ◽  
Functional Link ◽  
Antifungal Effect ◽  
Highly Active ◽  
First Time

Abstract GYNOPHILUS (Lcr REGENERANS) is a live biotherapeutic product (LBP) aimed at restoring the vaginal microbiome and contains the live biotherapeutic microorganism Lactobacillus rhamnosus Lcr35. In this study, the LBP formulation and manufacturing process significantly enhanced the anti-Candida activity of L. rhamnosus Lcr35, with a complete loss of viability of the yeast after 48 h of coincubation. Sodium thiosulfate (STS), one excipient of the product, was used as a potentiator of the anti-Candida spp. activity of Lactobacilli. This contact-independent phenomenon induced fungal cell disturbances, as observed by electron microscopy observations. Nonverbal sensory experiments showed clear odor dissimilarities between cocultures of L. rhamnosus Lcr35 and C. albicans in the presence and absence of STS, suggesting an impact of odor-active metabolites. A volatolomic approach allowed the identification of six odor-active compounds, including one sulfur compound that was identified as S-methyl thioacetate (MTA). MTA was associated with the antifungal effect of Lcr35, and its functional link was established in vitro. We show for the first time that the LBP GYNOPHILUS, which is a highly active product in the reduction of vulvovaginal candidiasis, requires the presence of a sulfur compound to fully achieve its antifungal effect.

In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans

2020 ◽  
Vol 15 (6) ◽  
pp. 648-655
Author(s):  
Gabriel O. de Azambuja ◽  
Laura Svetaz ◽  
Itamar L. Gonçalves ◽  
Patricia F. Corbelini ◽  
Gilsane L. von Poser ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Drug Design ◽  
Cryptococcus Neoformans ◽  
Biginelli Reaction ◽  
Fungal Growth ◽  
Chemical Library ◽  
Antifungal Effect ◽  
In Vitro Antifungal Activity

Background: Since the Monastrol discovery in 1999 as the first inhibitor of Eg5, functionalized dihydropyrimidinones/thiones (DHPMs) have emerged as prototypes for drug design in different targets. The present work aimed to evaluate the antifungal activity of a chemical library of DHPMs. Methods: The compounds were obtained employing Biginelli reaction. Their antifungal activities were assessed against C. neoformans and C. albicans. Results: The compounds 1-i and 1-k inhibited moderately the fungal growth of C. neoformans, with compound 2-k presenting MIC80 values of 62.5-125 µg·mL-1. Considering activity against C. albicans, the compounds 1-i and 1-n present an MIC50 value of 125-250 µg·mL-1. Conclusion: The changes performed in DHPM scaffold appear to be valuable for generating compounds with potential antifungal effect.

scholarly journals Efficacy of botanicals and fungicides against Rhizoctonia solani inciting sheath blight disease on Rice (Oryza sativa L.)

2017 ◽  
Vol 9 (4) ◽  
pp. 1916-1920
Author(s):  
Vipin Kumar ◽  
V.P. Chaudhary ◽  
Dharmendra Kumar ◽  
Ajay Kumar ◽  
Sushma Sagar ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
Mycelial Growth ◽  
Allium Sativum ◽  
Oryza Sativa L ◽  
Fungal Growth ◽  
Sheath Blight ◽  
Ocimum Sanctum ◽  
Sheath Blight Disease ◽  
Fungal Growth Inhibition

Among the fungal diseases, sheath blight, caused by multinucleate Rhizoctoniasolani Kuhn (teleomorph: Thanatephorus cucumeris Donk), a ubiquitous pathogen, is an important fungal disease of rice ranking only after blast and often rivalling it. The potential losses due to sheath blight alone in India has been up to 51.3%. In this study an attempt was made to investigate the antifungal efficacy of botanicals viz., neem (Azadirachtaindica), tulsi (Ocimum sanctum), garlic (Allium sativum), onion (Allium cepa), ginger (Zingiberofficinale) and various fungicides namely mancozeb, propiconazole, hexaconazole, carbendazim, and copper oxychlorideagainst Rhizoctoniasolani in vitro by poison food technique. R. solani was allowed to grow at 5%, 10% concentrations of botanicals and at 200, 500, 1000ppm of fungicides amended potato dextrose agar (PDA) medium. The effect of botanicals and fungicides on mycelial growth inhibition was recorded after 36, 48 and 72 post hrs inoculation (phi). It was observed that bulb extract of Allium sativum and rhizome extract of Zingier officinal suppressed the mycelial growth (80.19 and 76.32, respectively) @ 10% followed by leaf extract of Azadirachtaindica (72.78 %) after 72 phi. Among the fungicides, the complete fungal growth inhibition was observed in propiconazole and carbendazim fungicides amended medium.

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