scholarly journals Prenylated Trans-Cinnamic Esters and Ethers against Clinical Fusarium spp.: Repositioning of Natural Compounds in Antimicrobial Discovery

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 658
Author(s):  
Safa Oufensou ◽  
Stefano Casalini ◽  
Virgilio Balmas ◽  
Paola Carta ◽  
Wiem Chtioui ◽  
...  

Onychomycosis is a common nail infection mainly caused by species belonging to the F. oxysporum, F. solani, and F. fujikuroi species complexes. The aim of this study was to evaluate the in vitro susceptibility of six representative strains of clinically relevant Fusarium spp. toward a set of natural-occurring hydroxycinnamic acids and their derivatives with the purpose to develop naturally occurring products in order to cope with emerging resistance phenomena. By introducing a prenylated chain at one of the hydroxy groups of trans-cinnamic acids 1–3, ten prenylated derivatives (coded 4–13) were preliminarily investigated in solid Fusarium minimal medium (FMM). Minimal inhibitory concentration (MIC) and lethal dose 50 (LD50) values were then determined in liquid FMM for the most active selected antifungal p-coumaric acid 3,3′-dimethyl allyl ester 13, in comparison with the conventional fungicides terbinafine (TRB) and amphotericin B (AmB), through the quantification of the fungal growth. Significant growth inhibition was observed for prenylated derivatives 4–13, evidencing ester 13 as the most active. This compound presented MIC and LD50 values (62–250 µM and 7.8–125 µM, respectively) comparable to those determined for TRB and AmB in the majority of the tested pathogenic strains. The position and size of the prenylated chain and the presence of a free phenol OH group appear crucial for the antifungal activity. This work represents the first report on the activity of prenylated cinnamic esters and ethers against clinical Fusarium spp. and opens new avenues in the development of alternative antifungal compounds based on a drug repositioning strategy.

2019 ◽  
Vol 64 (2) ◽  
Author(s):  
A. Broutin ◽  
J. Bigot ◽  
Y. Senghor ◽  
A. Moreno-Sabater ◽  
J. Guitard ◽  
...  

ABSTRACT To evaluate the in vitro susceptibility of Fusarium to isavuconazole, 75 clinical isolates were identified using matrix-assisted laser desorption ionization–time of flight mass spectrometry and then tested with a broth microdilution method (EUCAST) and the gradient concentration strip (GCS) technique. The activity of isavuconazole overall was shown to be limited, with an MIC50 of >16 μg/ml, without significant differences between the species complexes. The categorical agreement between GCS and EUCAST was 97.4% to 100%, making the GCS as a valuable alternative.


Mycoses ◽  
1999 ◽  
Vol 42 (1‐2) ◽  
pp. 97-101 ◽  
Author(s):  
Rai ◽  
S. Qureshi ◽  
A. K. Pandey

2018 ◽  
Vol 101 (5) ◽  
pp. 1534-1541 ◽  
Author(s):  
Medhat A El-Naggar ◽  
Aisha M Alrajhi ◽  
Moustafa M Fouda ◽  
Eman M Abdelkareem ◽  
Tamer M Thabit ◽  
...  

Abstract Background: Deoxynivalenol (DON) is one of the most important fungal mycotoxins excreted by different Fusarium species in many types of grains and food commodities. It has high damage impact on human and animal immune systems. Objective: This in vitro study aimed to evaluate the influence of silver nanoparticles (Ag-NPs) as an inhibitor for the DON toxin excreted from some Fusarium spp., which were isolated from barely, wheat, and corn grains. Methods: Ag-NPs were estimated on Minimum Inhibitory Concentration, using levels of 5, 25, 50, 75, and 100 ppm, while the effect on DON was conducted with ELISA. Tri13 and Tri7 primers were used to evaluate the impact of Ag-NPs on the DNA of tested toxigenic Fusarium isolates. Results: Results revealed that the relative density values (Rd, %) of the isolated Fusarium from barley, wheat, and corn grains were 41.27, 26.47, and 30.76%, respectively. The predominant fungus was F. graminearum and F. culmorum in wheat and barley, respectively. The maximum inhibition diameters used for concentrations were 0.5, 2.8, 3.2, 3.3, and 3.31 mm, respectively. The impact of Ag-NPs on genomic structure was limited. Results demonstrated that Ag-NPs have the ability to reduce the linear growth of Fusarium spp. and eliminate the DON toxin to 34.44, 34.60, and 34.89% at 50, 75, and 100 ppm. Conclusions: Ag-NPs are considered nontransgenic substances, and their impact on Fusarium DNA under tested concentrations has been neglected. Ag-NPs may work as an alternative to fungicides to reduce fungal growth and eliminate DON mycotoxins.


Author(s):  
Nurgozhin T. ◽  
Sergazy S. H. ◽  
Adilgozhina G. ◽  
Gulyayev A. ◽  
Shulgau Z. ◽  
...  

Objective:This study investigates the hepatoprotective effect and the antioxidant role of polyphenol concentrate in the experimental model of carbon tetrachloride (CCl4) induced toxicity. Methods: Antioxidant activity of Cabernet Sauvignon grape polyphenol were evaluated by radical scavenging of 1,1-diphenyl-2-picryl hydrazyl radical (DPPH), 2,2’-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS.+). In addition, the effects of polyphenol concentrate on the survival of Wistar rats in the toxicity model, was also investigated. The polyphenol concentrate was administered for 5 five days prior to injection of carbon tetrachloride in a sub-lethal dose of 300 mg/kg of animal body weight in order to perform histological examinations of the liver and kidney, and detect the levels of AST, ALT and bilirubin. Results: Administration of polyphenol concentrate increased animal survival in the experimental model. Moreover, the intragastric administration of polyphenol concentrate prior to the initiation of the experimental model of toxicity, which was caused by a sub-lethal CCl4 dose, reduced morphological injuries in the liver and kidney, decreased the AST and ALT levels of the blood serum. Discussion and conclusion: Our data demonstrate that polyphenol concentrate possesses an antioxidant potential both in vitro and in vivo by reducing antioxidant stress that was caused by CCl4 administration into rats.


2020 ◽  
Vol 14 (4) ◽  
pp. 295-311
Author(s):  
Ada Gabriel ◽  
Mamman Mohammed ◽  
Mohammed G. Magaji ◽  
Yusuf P. Ofemile ◽  
Ameh P. Matthew ◽  
...  

Background: Snakebite envenomation is a global priority ranked top among other neglected tropical diseases. There is a folkloric claim that Uvaria chamae is beneficial for the management of snakebite and wounds in African ethnobotanical surveys. Besides, there are many registered patents asserting the health benefits of U. chamae. Objective: This study aimed to investigate U. chamae’s potentials and identify candidates for the development of tools for the treatment and management of N. nigricollis envenomation. Methods: Freshly collected U. chamae leaves were air-dried, powdered, and extracted in methanol. The median lethal dose of the extract was determined and further fractionated with n-hexane, n-butanol and ethyl acetate. Each fraction was tested for neutralizing effect against venom-induced haemolytic, fibrinolytic, hemorrhagic, and cytotoxic activities. Results: U. chamae fractions significantly (p<0.05) neutralized the haemolytic activity of N. nigricollis venom in n-butanol; 31.40%, n-hexane; 33%, aqueous residue; 39.60% and ethyl acetate; 40.70% at the concentration of 100mg/ml of each fraction against 10mg/ml of the snake venom when compared to the positive control. The fibrinolytic activity of N. nigricollis venom was significantly (p<0.05) neutralized in n-hexane at 73.88%, n-butanol; 72.22% and aqueous residue; 72.22% by the fractions of U. chamae. In addition, haemorrhagic activity of N. nigricollis venom was significantly (p<0.05) neutralized by U. chamae fractions at the concentrations of 100mg/ml, 200mg/ml and 400mg/ml except for n-butanol and aqueous residues at 400 mg/ml. Conclusion: U. chamae leaves fractions possess a high level of protection against N. nigricollis venoms-induced lethality and thus validate the pharmacological rationale for its usage in the management of N. nigricollis envenomation.


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