scholarly journals Mechanochemical synthesis of antifungal bis(benzoxaboroles)

RSC Advances ◽  
2020 ◽  
Vol 10 (61) ◽  
pp. 37187-37193 ◽  
Author(s):  
Krzysztof M. Borys ◽  
Dorota Wieczorek ◽  
Magdalena Tarkowska ◽  
Agnieszka Jankowska ◽  
Jacek Lipok ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Mechanochemical Synthesis ◽  
High Antifungal Activity

Several piperazine bis(benzoxaboroles) have been obtained mechanochemically – two of them have been shown to display high antifungal activity.

scholarly journals The newly synthesized thiazole derivatives as potential antifungal compounds against Candida albicans

2021 ◽  
Author(s):  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Gumieniczek ◽  
Maria Malm ◽  
Krzysztof Z. Łączkowski ◽  
...  
Keyword(s):  
Cell Wall ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Cell Membrane ◽  
Mode Of Action ◽  
Thiazole Derivatives ◽  
Fungal Cell ◽  
Erythrocyte Lysis ◽  
Low Cytotoxicity ◽  
High Antifungal Activity

Abstract Recently, the occurrence of candidiasis has increased dramatically, especially in immunocompromised patients. Additionally, their treatment is often ineffective due to the resistance of yeasts to antimycotics. Therefore, there is a need to search for new antifungals. A series of nine newly synthesized thiazole derivatives containing the cyclopropane system, showing promising activity against Candida spp., has been further investigated. We decided to verify their antifungal activity towards clinical Candida albicans isolated from the oral cavity of patients with hematological malignancies and investigate the mode of action on fungal cell, the effect of combination with the selected antimycotics, toxicity to erythrocytes, and lipophilicity. These studies were performed by the broth microdilution method, test with sorbitol and ergosterol, checkerboard technique, erythrocyte lysis assay, and reversed phase thin-layer chromatography, respectively. All derivatives showed very strong activity (similar and even higher than nystatin) against all C. albicans isolates with minimal inhibitory concentration (MIC) = 0.008–7.81 µg/mL Their mechanism of action may be related to action within the fungal cell wall structure and/or within the cell membrane. The interactions between the derivatives and the selected antimycotics (nystatin, chlorhexidine, and thymol) showed additive effect only in the case of combination some of them and thymol. The erythrocyte lysis assay confirmed the low cytotoxicity of these compounds as compared to nystatin. The high lipophilicity of the derivatives was related with their high antifungal activity. The present studies confirm that the studied thiazole derivatives containing the cyclopropane system appear to be a very promising group of compounds in treatment of infections caused by C. albicans. However, this requires further studies in vivo. Key points • The newly thiazoles showed high antifungal activity and some of them — additive effect in combination with thymol. • Their mode of action may be related with the influence on the structure of the fungal cell wall and/or the cell membrane. • The low cytotoxicity against erythrocytes and high lipophilicity of these derivatives are their additional good properties. Graphical abstract

N-(5-Amino-9H-benzo[a]phenoxazin-9-ylidene)propan-1-aminium chlorides as antifungal agents and NIR fluorescence probes

2021 ◽  
Author(s):  
Rui P. C. L. Sousa ◽  
João C. C. Ferreira ◽  
Maria João Sousa ◽  
M Sameiro Sameiro T T Gonçalves
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Nile Blue ◽  
Fluorescence Probes ◽  
Cell Labelling ◽  
Nir Fluorescence ◽  
High Antifungal Activity

The search for benzo[a]phenoxazines, Nile Blue derivatives, with high antifungal activity and cell labelling capacity based on our previously published works in this type of compounds, led us to the...

scholarly journals Development of Antidandruff Shampoo from the Fermented Product of Ocimum sanctum Linn.

Cosmetics ◽  
2018 ◽  
Vol 5 (3) ◽  
pp. 43 ◽  
Author(s):  
Chanun Punyoyai ◽  
Sasithorn Sirilun ◽  
Panuwan Chantawannakul ◽  
Wantida Chaiyana
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Activity ◽  
Total Soluble Protein ◽  
Diffusion Method ◽  
Ocimum Sanctum ◽  
Level Of Satisfaction ◽  
Fermented Product ◽  
Inhibition Zones ◽  
High Level ◽  
High Antifungal Activity

This study aimed to investigate Malassezia furfur inhibitory activity of the fermented product from Ocimum sanctum and develop an antidandruff shampoo. The fermented product was obtained by the fermentation process of the aerial part of O. sanctum. Total soluble protein was detected in the fermented product with the amount of 65.32 ± 0.14 mg/100 mL, whereas there was no organic acid. The inhibitory activity against four strains of M. furfur (No. 133, 656, 6000, and 7966) of the fermented product and shampoos containing the fermented product were investigated by broth dilution and agar diffusion method, respectively. The fermented product possessed high antifungal activity with the minimum inhibitory concentrations for 50% (MIC50) of M. furfur 133, 656, 6000, and 7966 of 0.125, 0.25, 0.125, and 0.125 mg/mL, respectively. Interestingly, the antifungal activity against M. furfur 656 was comparable to that of ketoconazole. Shampoo formulation C, which was the best formulation in terms of characteristics and stability, obtained a high level of satisfaction scores in terms of hair smoothness, hair shine, ease in combing, frizz reduction, and triboelectric reduction while brushing. Additionally, the shampoo containing 2% (w/w) of the fermented product of O. sanctum also possessed inhibitory activity against M. furfur 133, 656, 6000, and 7966 with inhibition zones of 13.2 ± 1.6, 12.8 ± 1.1, 18.7 ± 0.3, and 17.0 ± 1.1 mm respectively. Therefore, this shampoo was suggested for use as an antidandruff shampoo.

Syntheses of Halophenyl-γ-iodopropargyl Ethers Having High Antifungal Activity

1963 ◽  
Vol 27 (2) ◽  
pp. 150-151
Author(s):  
Shigeo Seki ◽  
Ken Nishihata ◽  
Tadayuki Nakayama ◽  
Hiroshi Ogawa
Keyword(s):  
Antifungal Activity ◽  
High Antifungal Activity

scholarly journals Structure-Antifungal Activity Relationships of Polyene Antibiotics of the Amphotericin B Group

2013 ◽  
Vol 57 (8) ◽  
pp. 3815-3822 ◽  
Author(s):  
Anna N. Tevyashova ◽  
Evgenia N. Olsufyeva ◽  
Svetlana E. Solovieva ◽  
Svetlana S. Printsevskaya ◽  
Marina I. Reznikova ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Cooh Group ◽  
Hydroxyl Groups ◽  
Activity Data ◽  
Oh Groups ◽  
Polyene Antibiotics ◽  
High Antifungal Activity

ABSTRACTA comprehensive comparative analysis of the structure-antifungal activity relationships for the series of biosynthetically engineered nystatin analogues and their novel semisynthetic derivatives, as well as amphotericin B (AMB) and its semisynthetic derivatives, was performed. The data obtained revealed the significant influence of the structure of the C-7 to C-10 polyol region on the antifungal activity of these polyene antibiotics. Comparison of positions of hydroxyl groups in the antibiotics andin vitroantifungal activity data showed that the most active are the compounds in which hydroxyl groups are in positions C-8 and C-9 or positions C-7 and C-10. Antibiotics with OH groups at both C-7 and C-9 had the lowest activity. The replacement of the C-16 carboxyl with methyl group did not significantly affect thein vitroantifungal activity of antibiotics without modifications at the amino group of mycosamine. In contrast, the activity of the N-modified derivatives was modulated both by the presence of CH3or COOH group in the position C-16 and by the structure of the modifying substituent. The most active compounds were testedin vivoto determine the maximum tolerated doses and antifungal activity on the model of candidosis sepsis in leukopenic mice (cyclophosphamide-induced). Study of our library of semisynthetic polyene antibiotics led to the discovery of compounds, namely,N-(l-lysyl)-BSG005 (compound 3n) and, especially,l-glutamate of 2-(N,N-dimethylamino)ethyl amide of S44HP (compound 2j), with high antifungal activity that were comparable inin vitroandin vivotests to AMB and that have better toxicological properties.

Bombyx mori cecropin A has a high antifungal activity to entomopathogenic fungus Beauveria bassiana

Gene ◽  
2016 ◽  
Vol 583 (1) ◽  
pp. 29-35 ◽  
Author(s):  
Dingding Lu ◽  
Tao Geng ◽  
Chengxiang Hou ◽  
Yuxia Huang ◽  
Guangxing Qin ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Bombyx Mori ◽  
Beauveria Bassiana ◽  
Entomopathogenic Fungus ◽  
Cecropin A ◽  
Fungus Beauveria Bassiana ◽  
High Antifungal Activity

scholarly journals Antimicrobial Activity of Lipopeptide Biosurfactants Against Foodborne Pathogen and Food Spoilage Microorganisms and Their Cytotoxicity

2021 ◽  
Vol 11 ◽  
Author(s):  
Konstantina Kourmentza ◽  
Xavier Gromada ◽  
Nicholas Michael ◽  
Charlotte Degraeve ◽  
Gaetan Vanier ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Foodborne Pathogen ◽  
Food Spoilage ◽  
Food Preservatives ◽  
Byssochlamys Fulva ◽  
Lipopeptide Biosurfactants ◽  
First Time ◽  
High Antifungal Activity ◽  
Spoilage Microorganisms

Lipopeptide biosurfactants produced by Bacillus sp. were assessed regarding their antimicrobial activity against foodborne pathogenic and food spoilage microorganisms. Both Gram-positive and Gram-negative bacteria were found not to be susceptible to these lipopeptides. However, mycosubtilin and mycosubtilin/surfactin mixtures were very active against the filamentous fungi Paecilomyces variotti and Byssochlamys fulva, with minimum inhibitory concentrations (MICs) of 1–16 mg/L. They were also active against Candida krusei, MIC = 16–64 mg/L. Moreover it was found that the antifungal activity of these lipopeptides was not affected by differences in isoform composition and/or purity. Furthermore their cytotoxicity tested on two different cell lines mimicking ingestion and detoxification was comparable to those of approved food preservatives such as nisin. Overall, for the first time here mycosubtilin and mycosubtilin/surfactin mixtures were found to have high antifungal activity against food relevant fungi at concentrations lower than their toxicity level hence, suggesting their application for extending the shelf-life of products susceptible to these moulds. In addition combining nisin with mycosubtilin or mycosubtiliin/surfactin mixtures proved to be an effective approach to produce antimicrobials with broader spectrum of action.

scholarly journals Elucidation and Identification of an Antifungal Compound from Pseudomonas aeruginosa DA3.1 Isolated from Soil in Vietnam

2020 ◽  
Vol 13 (10) ◽  
Author(s):  
Nguyen Thi Trung ◽  
Nguyen Tien Cuong ◽  
Nguyen Thi Thao ◽  
Dao Thi Mai Anh ◽  
Do Thi Tuyen
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Pseudomonas Aeruginosa ◽  
Antifungal Activity ◽  
Carboxylic Acid ◽  
Magnetic Resonance ◽  
13C Nmr ◽  
Bacterial Strain ◽  
Antifungal Compound ◽  
Fusarium Sp ◽  
High Antifungal Activity

Background: Fusarium sp. and Rhizoctonia sp. fungi have been always threats to short-term crops. In Vietnam, corn and soybean suffer serious losses annually. Therefore, it is necessary to utilize an environmentally friendly antifungal compound that is highly effective against phytopathogenic fungi. Pseudomonas sp. is a popular soil bacterial strain and well known for its high antifungal activity. Objectives: This study was carried out to evaluate and assess the antifungal activity of a local bacterial strain namely DA3.1 that was later identified as Pseudomonas aeruginosa. This would be strong scientific evidence to develop an environmentally friendly biocide from a local microorganism strain for commercial use. Methods: The antifungal compound was purified from ethyl acetate extraction of deproteinized cell culture broth by a silica gel column (CH2Cl2/MeOH (0% - 10% MeOH)). The purity of the isolated compound was determined by HPLC, and its molecular structure was elucidated using spectroscopic experiments including one-dimensional (1D) (1H NMR, 13C NMR, DEPT) and two-dimensional (2D) (HMBC and HSQC) spectra. The activity of the purified compound against Fusarium sp. and Rhizoctonia sp. fungi was measured using the PDA-disk diffusion method, and its growth-promoting ability was evaluated using the seed germination test of corn and soybean. Results: The results showed that the antifungal compound produced by Pseudomonas aeruginosa DA3.1 had a retention factor (Rf) of 0.86 on thin layer chromatography (TLC). Based on the evidence of spectral data including proton nuclear magnetic resonance (1H NMR), carbon nuclear magnetic resonance (13C NMR), distortionless enhancement by polarization transfer (DEPT), heteronuclear multiple bond correlation (HMBC), and heteronuclear single quantum coherence (HSQC), the chemical structure was elucidated as phenazine-1-carboxylic. The purified compound showed inhibitory activity against F. oxysporum and R. solani and exhibited the ability of the germination of corn and soybean seeds. The results revealed the benefit of native P. aeruginosa DA3.1 and phenazine-1-carboxylic acid for use as a biocontrol agent, as well as a plant growth promoter. Conclusions: The antifungal compound isolated from local Pseudomonas DA3.1 was identified as phenazine-1-carboxylic acid that posed high antifungal activity and was a plant germination booster.

The antifungal strobilurins and their possible ecological role

1995 ◽  
Vol 73 (S1) ◽  
pp. 940-945 ◽  
Author(s):  
T. Anke
Keyword(s):  
Antifungal Activity ◽  
Key Words ◽  
Phytopathogenic Fungi ◽  
Ecological Role ◽  
Natural Substrate ◽  
Lead Compounds ◽  
Low Toxicity ◽  
Respiration Inhibitors ◽  
Nutrient Resources ◽  
High Antifungal Activity

The strobilurins and the closely related oudemansins are new respiration inhibitors, binding to the Qp centre of cytochrome b. Their high antifungal activity against phytopathogenic fungi and their low toxicity towards mammals make them attractive lead compounds for the synthesis of agricultural fungicides. The strobilurins have been isolated from a great number of Basidiomycetes belonging to the genera Strobilurus, Oudemansiella, Xerula, Hydropus, Mycena, Filoboletus, Crepidotus, and Cyphellopsis as well as one Ascomycete, Bolinea lutea. Strobilurin-producing species occur in Europe, the Americas, Africa, and Australia. Most of the producing fungi grow on wood. Since under sterile conditions strobilurin production could be detected in the natural substrate it appears that the strobilurins play a role in securing nutrient resources for the producers from competing fungi. Key words: strobilurins, oudemansins, antibiotics, antifungal, Basidiomycetes.

scholarly journals Effect of N-chlorotaurine on Aspergillus, with particular reference to destruction of secreted gliotoxin

2006 ◽  
Vol 55 (7) ◽  
pp. 913-918 ◽  
Author(s):  
Emer P. Reeves ◽  
Markus Nagl ◽  
Joseph O'Keeffe ◽  
Judy Kelly ◽  
Kevin Kavanagh
Keyword(s):  
Antifungal Activity ◽  
Aspergillus Fumigatus ◽  
Clinical Isolate ◽  
Topical Treatment ◽  
Therapeutic Efficacy ◽  
Fungicidal Activity ◽  
Immunosuppressive Agent ◽  
Good Choice ◽  
Disulphide Bridge ◽  
High Antifungal Activity

The fungistatic and fungicidal activity of N-chlorotaurine (NCT), a long-lived oxidant produced by stimulated neutrophils, was investigated. Physiological concentrations (75–100 μM) of NCT showed clear fungicidal activity against a range of Aspergillus isolates. Moreover, killing by NCT was significantly increased in the presence of ammonium chloride, explained by the formation of monochloramine by halogenation of ammonium. One clinical isolate of Aspergillus fumigatus was characterized for the production of the immunosuppressive agent gliotoxin, and NCT was shown to cause destruction of gliotoxin, possibly via reduction of the disulphide bridge. Because of its endogenous nature and its high antifungal activity, NCT appears to be a good choice for topical treatment of Aspergillus infections, and the results of this study further substantiate its therapeutic efficacy.

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