Ecofriendly synthesis of halogenated flavonoids and evaluation of their antifungal activity

2015 ◽  
Vol 39 (4) ◽  
pp. 2980-2987 ◽  
Author(s):  
Roberta Bernini ◽  
Marcella Pasqualetti ◽  
Gianfranco Provenzano ◽  
Sabrina Tempesta

Chlorinated catechin derivative 29 resulted in being the most active compound against Trichoderma koningii and Cladosporium cladosporioides, common saprotrophic soil and seed fungi.

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Kátia Santana Cruz ◽  
Emerson Silva Lima ◽  
Marcia de Jesus Amazonas da Silva ◽  
Erica Simplício de Souza ◽  
Andreia Montoia ◽  
...  

Background. Cryptococcosis is a fungal disease of bad prognosis due to its pathogenicity and the toxicity of the drugs used for its treatment. The aim of this study was to investigate the medicinal potential of carbazole and β-carboline alkaloids and derivatives against Cryptococcus neoformans and C. gattii. Methods. MICs were established in accordance with the recommendations of the Clinical and Laboratory Standards Institute for alkaloids and derivatives against C. neoformans and C. gattii genotypes VNI and VGI, respectively. A single active compound was further evaluated against C. neoformans genotypes VNII, VNIII, and VNIV, C. gattii genotypes VGI, VGIII, and VGIV, Candida albicans ATCC 36232, for cytotoxicity against the MRC-5 lineage of human fibroblasts and for effects on fungal cells (cell wall, ergosterol, and leakage of nucleic acids). Results. Screening of 11 compounds revealed 8-nitroharmane as a significant inhibitor (MIC 40 μg/mL) of several C. neoformans and C. gattii genotypes. It was not toxic to fibroblasts (IC50 > 50 µg/mL) nor did it alter fungal cell walls or the concentration of ergosterol in C. albicans or C. neoformans. It increased leakage of substances that absorb at 260 nm. Conclusions. The synthetic β-carboline 8-nitroharmane significantly inhibits pathogenic Cryptococcus species and is interesting as a lead compound towards new therapy for Cryptococcus infections.


2013 ◽  
Vol 61 (19) ◽  
pp. 4551-4555 ◽  
Author(s):  
Xiaoning Wang ◽  
Mohamed M. Radwan ◽  
Amer H. Taráwneh ◽  
Jiangtao Gao ◽  
David E. Wedge ◽  
...  

2021 ◽  
Vol 57 (1) ◽  
pp. 86-93
Author(s):  
A. E. Kuvarina ◽  
M. L. Georgieva ◽  
E. A. Rogozhin ◽  
A. B. Kulko ◽  
I. A. Gavryushina ◽  
...  

Abstract The ability of alkalophilic micromycetes of the species Sodiomyces alkalinus to produce antimicrobial compounds was studied. As a result of the determination of the spectrum and yield of antibiotic compounds, a promising producer of the antimycotics Sodiomyces alkalinus was selected from the most active strains 8KS17-10. The producer exhibited antifungal activity against opportunistic fungi, as well as pathogenic clinical isolates of molds and yeasts—pathogens of systemic mycoses. The isolated active compound can be attributed to the group of antimicrobial glycopeptides based on the totality of the identified structural features (molecular weight, absorption ratio at certain wavelengths).


2021 ◽  
Vol 22 (8) ◽  
pp. 4175
Author(s):  
Virginia Brighenti ◽  
Ramona Iseppi ◽  
Luca Pinzi ◽  
Annamaria Mincuzzi ◽  
Antonio Ippolito ◽  
...  

Punica granatum L. (pomegranate) fruit is known to be an important source of bioactive phenolic compounds belonging to hydrolysable tannins. Pomegranate extracts have shown antifungal activity, but the compounds responsible for this activity and their mechanism/s of action have not been completely elucidated up to now. The aim of the present study was the investigation of the inhibition ability of a selection of pomegranate phenolic compounds (i.e., punicalagin, punicalin, ellagic acid, gallic acid) on both plant and human fungal pathogens. In addition, the biological target of punicalagin was identified here for the first time. The antifungal activity of pomegranate phenolics was evaluated by means of Agar Disk Diffusion Assay and minimum inhibitory concentration (MIC) evaluation. A chemoinformatic analysis predicted for the first time topoisomerases I and II as potential biological targets of punicalagin, and this prediction was confirmed by in vitro inhibition assays. Concerning phytopathogens, all the tested compounds were effective, often similarly to the fungicide imazalil at the label dose. Particularly, punicalagin showed the lowest MIC for Alternaria alternata and Botrytis cinerea, whereas punicalin was the most active compound in terms of growth control extent. As for human pathogens, punicalagin was the most active compound among the tested ones against Candida albicans reference strains, as well as against the clinically isolates. UHPLC coupled with HRMS indicated that C. albicans, similarly to the phytopathogen Coniella granati, is able to hydrolyze both punicalagin and punicalin as a response to the fungal attack. Punicalagin showed a strong inhibitory activity, with IC50 values of 9.0 and 4.6 µM against C. albicans topoisomerases I and II, respectively. Altogether, the results provide evidence that punicalagin is a valuable candidate to be further exploited as an antifungal agent in particular against human fungal infections.


2019 ◽  
Vol 7 (12) ◽  
pp. 664 ◽  
Author(s):  
María L. De la Cruz-Claure ◽  
Ariel A. Cèspedes-Llave ◽  
María T. Ulloa ◽  
Miguel Benito-Lama ◽  
Enrique Domínguez-Álvarez ◽  
...  

Candida glabrata is one of the most prevalent pathogenic Candida species in dental plaque on tooth surfaces. Candida biofilms exhibit an enhanced resistance against most antifungal agents. Thus, the development of alternative more potent and effective antimicrobials is required to overcome this resistance. In this study, three novel fluorinated derivatives and nine selenoester compounds were screened as novel antifungal and antibiofilm agents against C. krusei, C. parapsilosis, and C. glabrata (N = 81 dental isolates). C. glabrata strains were susceptible only to fluorinated compounds while C. krusei, C. parapsilosis, and C. glabrata were susceptible to the action of the selenoesters. The evaluated symmetrical selenoester compounds presented very good antifungal activity against all the tested C. glabrata dental isolates (1–4 μg/mL of minimum inhibitory concentration-MIC). The most active compound (Se-5) was able to inhibit and disperse C. glabrata biofilms. These results demonstrated that selenoesters may be novel and promising biocide agents against C. glabrata clinical dental isolates.


2018 ◽  
Vol 43 (1) ◽  
pp. 33
Author(s):  
Herlle Aparecido Da Silva ◽  
Lydia Fumiko Yamaguchi ◽  
Maria Cláudia Marx Young ◽  
Clécio Souza Ramos ◽  
André Márcio Araújo Amorim ◽  
...  

The phytochemical study on dichlorometane extracts of leaves, stem and roots of Piper mollicomum Kunth (Piperaceae) led to isolation of the known piperamides tembamide (1), (R)-(-)-tembamide acetate (2) and riparin I (3). Compounds 1 and 2 displayed moderate in vitro antifungal activity against Cladosporium cladosporioides (5.0 μg) and Cladosporium sphaerospermum (1.0 μg) by direct bioautographic analyses and compound 3 was inactive up to 100.0 μg.


2019 ◽  
pp. 96-99
Author(s):  
A. A. Safonov ◽  
Т. V. Panasenko ◽  
E. G. Knysh ◽  
N. M. Polishchuk

For creating a new biologically active compounds are using a system on which already exist medications. One such system is the core of 1,2,4-triazole. The aim of our work was to study the antimicrobial and antifungal activity new 4-((R-iden)amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiols. The study was conducted according to the method of serial dilutions. As a result of studies new synthesized 4-((R-idene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiols exhibit antimicrobial and antifungal activity. The most active compound that exhibits antimicrobial activity against Staphylococcus aureus is 4-((1-(phenyl)ethylidene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiol and 4-((3-nitrobenzylidene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiol, 4-((4-fluorbenzylidene)amino)-5-(thiophene-2-ilmetyl)-4H-1,2,4-triazoles-3-thiol exhibit antifungal activity level of the comparator fluconazole, compound III, VI exceed its performance.


1999 ◽  
Vol 47 (2) ◽  
pp. 584-587 ◽  
Author(s):  
Yasuhiro Iida ◽  
Ki-Bong Oh ◽  
Mikako Saito ◽  
Hideaki Matsuoka ◽  
Hiroshi Kurata ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document