Potential of agricultural fungicides for antifungal drug discovery

Jampílek, Josef

doi:10.1517/17460441.2016.1110142

Cited by 76 publications

(60 citation statements)

References 37 publications

(37 reference statements)

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“…This fact is justified by the reason that they have condensed aromatic groups (lipophilic groups), and carboxyl and carboxylic groups, which can also act on membrane rupture and metabolic inhibition. Anthraquinones of natural origin are attributed innumerable activities, with emphasis on the oxidative potential that favors the triggering of cellular apoptosis (cellular suicide); this effect occurs by intercalation between vicinal nucleotides of the DNA strand, via ionic and van der Waals interactions with the anthraquinones, blocking the polymerases and interfering with protein synthesis (Silva et al, 2003;Jampilek, 2015). Assis (2013), working with ethanolic extracts of P. ramiflora (stem and root peels), showed fungitoxic activity on Candida parapsilosis, with values of minimum inhibitory concentration lower than 3.9 μg/mL.…”

Section: Antifungal Activity Of Ethanolic Extract and Fractionsmentioning

confidence: 99%

Phytochemical analysis and fungicide potential of Pouteria ramiflora against Lasiodiplodia theobromae

et al. 2017

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The use of plant extracts can be an alternative to reduce the use of pesticides, to control diseases and pests that affect agricultural production. The aim of this study was the chemical characterization of the extract and fractions of Pouteria ramiflora leaves and to determine its fungistatic potential on Lasiodiplodia theobromae. The ethanolic extract of dried and crushed leaves was obtained by maceration. Part of this extract was sequentially partitioned and the following fractions were obtained: hexane, dichloromethane, chloroform, ethyl acetate, n-butyl, and hydromethanol for subsequent bioassay, and qualitative and quantitative phytochemical analysis. Experimental development comprises of adding a L. theobromae mycelial disk (5 mm), obtained from pure colonies, in the middle of Petri dishes with PDA culture growth (potato-dextrose-agar) plus the aforementioned substances in different concentrations (800; 1,200; 1,600; 2,000, and 2,400 µg/mL), and a control treatment (PDA). The plates were incubated in B.O.D. (25±2°C), and the assessment was performed by measuring the diameter of the colonies until it reaches the edge of the board. The experimental design was completely randomized with five replications, and the treatments were constituted of a factorial of seven extracts/fractions and six concentrations. For the Mycelial Growth Rate Index (MGRI) obtained, the analysis of variance was performed, and when significant, the regression analysis was performed. All extract/fractions decreased MGRI of L. theobromae, as the concentrations were increased. The best MGRI reduction occurred in n-butanolic fraction, and the efficiency of this fraction may be related to the presence of flavonoids and anthraquinones. The extract and fractions of P. ramiflora, a tree from the Cerrado biome in Mato Grosso do Sul, was effective in the control of L. theobromae, which can be used as a control option in organic farming or in integrated management systems.

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Section: Antifungal Activity Of Ethanolic Extract and Fractionsmentioning

confidence: 99%

Phytochemical analysis and fungicide potential of Pouteria ramiflora against Lasiodiplodia theobromae

et al. 2017

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“…Since different classes of herbicides are able to bind to different mammalian cellular receptors, the majority of pharmaceutical companies have pesticide divisions, and developed biologically active agents are investigated as both pesticides and drugs. Previously, several successful pesticides became pharmaceuticals and vice versa [31,32,33,34,35]. …”

Section: Introductionmentioning

confidence: 99%

Synthesis and Spectrum of Biological Activities of Novel N-arylcinnamamides

Pospíšilová

Kos

Michnová

et al. 2018

IJMS

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A series of sixteen ring-substituted N-arylcinnamamides was prepared and characterized. Primary in vitro screening of all the synthesized compounds was performed against Staphylococcus aureus, three methicillin-resistant S. aureus strains, Mycobacterium tuberculosis H37Ra, Fusarium avenaceum, and Bipolaris sorokiniana. Several of the tested compounds showed antistaphylococcal, antitubercular, and antifungal activities comparable with or higher than those of ampicillin, isoniazid, and benomyl. (2E)-N-[3,5-bis(trifluoromethyl)phenyl]-3-phenylprop-2-enamide and (2E)-3-phenyl-N-[3-(trifluoromethyl)phenyl]prop-2-enamide showed the highest activities (MICs = 22.27 and 27.47 µM, respectively) against all four staphylococcal strains and against M. tuberculosis. These compounds showed an activity against biofilm formation of S. aureus ATCC 29213 in concentrations close to MICs and an ability to increase the activity of clinically used antibiotics with different mechanisms of action (vancomycin, ciprofloxacin, and tetracycline). In time-kill studies, a decrease of CFU/mL of >99% after 8 h from the beginning of incubation was observed. (2E)-N-(3,5-Dichlorophenyl)- and (2E)-N-(3,4-dichlorophenyl)-3-phenylprop-2-enamide had a MIC = 27.38 µM against M. tuberculosis, while a significant decrease (22.65%) of mycobacterial cell metabolism determined by the MTT assay was observed for the 3,5-dichlorophenyl derivative. (2E)-N-(3-Fluorophenyl)- and (2E)-N-(3-methylphenyl)-3-phenylprop-2-enamide exhibited MICs = 16.58 and 33.71 µM, respectively, against B. sorokiniana. The screening of the cytotoxicity of the most effective antimicrobial compounds was performed using THP-1 cells, and these chosen compounds did not shown any significant lethal effect. The compounds were also evaluated for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. (2E)-N-(3,5-dichlorophenyl)-3-phenylprop-2-enamide (IC50 = 5.1 µM) was the most active PET inhibitor. Compounds with fungicide potency did not show any in vivo toxicity against Nicotiana tabacum var. Samsun. The structure–activity relationships are discussed.

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“…Many activities are attributed to anthraquinones found in nature specially their oxidant potential which triggers cellular apoptosis; this effect occurs by intercalation among vicinal nucleotides from DNA, by ionic and Van der Waals interactions with anthraquinones, blocking polymerases and interfering on protein synthesis (Silva et al, 2003;Jampilek, 2016).…”

Section: Resultsmentioning

confidence: 99%

Phytochemistry, antioxidant potential and antifungal of Byrsonima crassifolia on soil phytopathogen control

et al. 2017

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The use of chemical defensives to control fungal diseases has by consequence to impact negatively over the environment and human health, this way, the use of plant extracts with antifungal properties along with proper cultural management makes viable an alternative plant production control, specially for familiar and organic cultures. The objective of this study was to perform phytochemical and antioxidant analysis of Byrsonima crassifolia (canjiqueira) barks and evaluate its antifungal potential over Fusarium solani and Sclerotinia sclerotiorum mycelial growth. The ethanol extract from plants collected in Pantanal, Mato Grosso do Sul, Brazil was submitted to phytochemical prospection, total phenol and flavonoids quantification and antioxidant activiy determination (DPPH). To evaluate antifungal activity concentrations of 800, 1200, 1600, 2000 and 2400 µg 100 mL -1 of ethanol extract were used. Which concentration was separately incorporated in agar (PDA) and shed in Petri dishes, followed by the fungi mycelial disc where the colonies diameter was measured daily. Negatives control with agar without extract and agar with an ethanol solution were used. The B. crassifolia ethanol extract presented inhibitory activity over the fungi studied where concentrations of 800 and 1600 µg 100 mL -1 , inhibited 38% of the mycelial growth of F. solani; to S. sclerotiorum the best concentration was 2400 µg 100 mL 1 , reducing 37.5%. The antifungal bark extract potential of this specie is attributed to phenolic compounds and to triterpenes derivatives.

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Potential of agricultural fungicides for antifungal drug discovery

Cited by 76 publications

References 37 publications

Phytochemical analysis and fungicide potential of Pouteria ramiflora against Lasiodiplodia theobromae

Phytochemical analysis and fungicide potential of Pouteria ramiflora against Lasiodiplodia theobromae

Synthesis and Spectrum of Biological Activities of Novel N-arylcinnamamides

Phytochemistry, antioxidant potential and antifungal of Byrsonima crassifolia on soil phytopathogen control

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