scholarly journals Antifungal Activity and DNA Topoisomerase Inhibition of Hydrolisable Tannins from Punica granatum L.

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.

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3853 ◽  
Author(s):  
Eftichia Kritsi ◽  
Minos-Timotheos Matsoukas ◽  
Constantinos Potamitis ◽  
Anastasia Detsi ◽  
Marija Ivanov ◽  
...  

The prevalence of invasive fungal infections has been dramatically increased as the size of the immunocompromised population worldwide has grown. Aspergillus fumigatus is characterized as one of the most widespread and ubiquitous fungal pathogens. Among antifungal drugs, azoles have been the most widely used category for the treatment of fungal infections. However, increasingly, azole-resistant strains constitute a major problem to be faced. Towards this direction, our study focused on the identification of compounds bearing novel structural motifs which may evolve as a new class of antifungals. To fulfil this scope, a combination of in silico techniques and in vitro assays were implemented. Specifically, a ligand-based pharmacophore model was created and served as a 3D search query to screen the ZINC chemical database. Additionally, molecular docking and molecular dynamics simulations were used to improve the reliability and accuracy of virtual screening results. In total, eight compounds, bearing completely different chemical scaffolds from the commercially available azoles, were proposed and their antifungal activity was evaluated using in vitro assays. Results indicated that all tested compounds exhibit antifungal activity, especially compounds 1, 2, and 4, which presented the most promising minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values and, therefore, could be subjected to further hit to lead optimization.


Author(s):  
Shahindokht Bassiri-Jahromi ◽  
Farzad Katiraee ◽  
Mannan Hajimahmoodi ◽  
Ehsan Mostafavi ◽  
Malihe Talebi. ◽  
...  

2019 ◽  
Vol 9 (1) ◽  
pp. 21-28
Author(s):  
Nisha Sharma ◽  
Shashikiran Misra

Background and Objectives: Dermatophytosis (topical fungal infection) is the 4th common disease in the last decade, affecting 20-25% world’s population. Patients of AIDS, cancer, old age senescence, diabetes, cystic fibrosis become more vulnerable to dermatophytosis. The conventional topical dosage proves effective as prophylactic in preliminary stage. In the advanced stage, the therapeutics interacts with healthy tissues before reaching the pathogen site, showing undesirable effects, thus resulting in pitiable patient compliance. The youngest carbon nano-trope “Graphene” is recently used to manipulate bioactive agents for therapeutic purposes. Here, we explore graphene via smart engineering by virtue of high surface area and high payload for therapeutics and developed graphene–ketoconazole nanohybrid (Gn-keto) for potent efficacy towards dermatophytes in a controlled manner. </P><P> Methods: Polymethacrylate derivative Eudragit (ERL100 and ERS 100) microspheres embedded with keto and Gn-keto nanohybrid were formulated and characterized through FTIR, TGA, and SEM. In vitro drug release and antifungal activity of formulated Gn-keto microspheres were assessed for controlled release and better efficacy against selected dermatophytes. </P><P> Results: Presence of numerous pores within the surface of ERL100 microspheres advocated enhanced solubility and diffusion at the site of action. Controlled diffusion across the dialysis membrane was observed with ERS100 microspheres owing to the nonporous surface and poor permeability. Antifungal activity against T. rubrum and M. canis using microdilution method focused on a preeminent activity (99.785 % growth inhibition) of developed nanohybrid loaded microspheres as compared to 80.876% of keto loaded microspheres for T. rubrum. The culture of M. canis was found to be less susceptible to formulated microspheres. Conclusion: Synergistic antifungal activity was achieved by nanohybrid Gn-Keto loaded microspheres against selected topical fungal infections suggesting a vital role of graphene towards fungi.


Author(s):  
Maria-Dimitra Tsolakidou ◽  
Ioannis A Stringlis ◽  
Natalia Fanega-Sleziak ◽  
Stella Papageorgiou ◽  
Antria Tsalakou ◽  
...  

Abstract Composts represent a sustainable way to suppress diseases and improve plant growth. Identification of compost-derived microbial communities enriched in the rhizosphere of plants and characterization of their traits, could facilitate the design of microbial synthetic communities (SynComs) that upon soil inoculation could yield consistent beneficial effects towards plants. Here, we characterized a collection of compost-derived bacteria, previously isolated from tomato rhizosphere, for in vitro antifungal activity against soil-borne fungal pathogens and for their potential to change growth parameters in Arabidopsis. We further assessed root-competitive traits in the dominant rhizospheric genus Bacillus. Certain isolated rhizobacteria displayed antifungal activity against the tested pathogens and affected growth of Arabidopsis, and Bacilli members possessed several enzymatic activities. Subsequently, we designed two SynComs with different composition and tested their effect on Arabidopsis and tomato growth and health. SynCom1, consisting of different bacterial genera, displayed negative effect on Arabidopsis in vitro, but promoted tomato growth in pots. SynCom2, consisting of Bacilli, didn't affect Arabidopsis growth, enhanced tomato growth and suppressed Fusarium wilt symptoms. Overall, we found selection of compost-derived microbes with beneficial properties in the rhizosphere of tomato plants, and observed that application of SynComs on poor substrates can yield reproducible plant phenotypes.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 3032 ◽  
Author(s):  
Suresh Mickymaray ◽  
Wael Alturaiki

Fungal sensitization is very common in bronchial asthmatic cases, and the connection with airway colonization by fungi remains uncertain. Antifungal therapy failure is a significant fraction of the cost and morbidity and mortality in the majority of the asthmatic cases. Hence, the present study aimed to investigate the antifungal activity of five marine macroalgae—Acanthaophora specifera, Cladophoropsis sp., Laurencia paniculata, Tydemania sp., and Ulva prolifera—which were tested on selected fungal pathogens isolated from 15 sputum of 45 bronchial asthmatic patients. The highest antifungal activity was observed in ethanol fractions of L. paniculata followed by U. prolifera, Cladophoropsis sp., A. specifera, and Tydemania sp. The minimum fungicidal concentration and minimum inhibitory concentration values of the ethanolic fractions of algal species were found to be 125–1000 µg/mL and 125–500 µg/mL, respectively. The algal extracts contained terpene alcohol, diterpene, steroids, sesquiterpene, and sesquiterpene alcohol, as determined by GC–MS/MS analyses. The present study shows that the marine macroalgae containing bioactive compounds had excellent inhibitory activity against a variety of fungal pathogens, which may be useful for combating fungal infections and recovering from chronic asthmatic states.


2018 ◽  
Author(s):  
Maria-Dimitra Tsolakidou ◽  
Ioannis A. Stringlis ◽  
Natalia Fanega-Sleziak ◽  
Stella Papageorgiou ◽  
Antria Tsalakou ◽  
...  

AbstractComposts represent a sustainable way to suppress diseases and improve plant growth. Identification of compost-derived microbial communities enriched in the rhizosphere of plants and characterization of their traits, could facilitate the design of microbial synthetic communities (SynComs) that upon soil inoculation could yield consistent beneficial effects towards plants. Here, we characterized a collection of compost-derived bacteria, previously isolated from tomato rhizosphere, forin vitroantifungal activity against soil-borne fungal pathogens and for their potential to change growth parameters inArabidopsis. We further assessed root-competitive traits in the dominant rhizospheric genusBacillus. Certain isolated rhizobacteria displayed antifungal activity against the tested pathogens and affected growth ofArabidopsis, and Bacilli members possessed several enzymatic activities. Subsequently, we designed two SynComs with different composition and tested their effect onArabidopsisand tomato growth and health. SynCom1, consisting of different bacterial genera, displayed negative effect onArabidopsis in vitro, but promoted tomato growth in pots. SynCom2, consisting of Bacilli, didn’t affectArabidopsisgrowth, enhanced tomato growth and suppressed Fusarium wilt symptoms. Overall, we found selection of compost-derived microbes with beneficial properties in the rhizosphere of tomato plants, and observed that application of SynComs on poor substrates can yield reproducible plant phenotypes.


2018 ◽  
Vol 73 (7-8) ◽  
pp. 313-318 ◽  
Author(s):  
Rose Vanessa Bandeira Reidel ◽  
Simona Nardoni ◽  
Francesca Mancianti ◽  
Claudia Anedda ◽  
Abd El-Nasser G. El Gendy ◽  
...  

Abstract The objective of the present paper was the assessment of the chemical composition of the essential oils from four Asteraceae species with a considerable food, medicinal, and agricultural value, collected in Egypt, together with their in vitro inhibitory activity against molds and yeasts. The essential oil of Launaea cornuta flowers was also evaluated for the first time, but because of its very low yield (<0.01%), no antifungal test was performed.


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