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At concentrations achieved following systemic administration, the primary effect of imidazoles and triazoles on fungi is inhibition of 14-α-sterol demethylase, a microsomal cytochrome P450 (CYP) enzyme. Imidazoles and triazoles impair the biosynthesis of ergosterol for the cytoplasmic membrane and lead to the accumulation of 14-α-methyl sterols. The synthetic imidazole miconazole is additionally able to increase intracellular reactive oxygen species, at least in part through inhibition of fungal catalase and peroxidase. This unique feature of miconazole is probably the basis for its fungicidal activity in C. albicans, in addition to the fungistatic mode of action. Studies show that miconazole is superior to nystatin treatment and demonstrate its impact as one of the best options in managing vulvovaginal candidiasis. Regarding recurrent vulvovaginal candidiasis, several new drugs are currently developed to ensure effective treatment also for this group of patients. [ABSTRACT FROM AUTHOR]

Simple Summary: There is a growing demand for molecules of natural origin for biocontrol and biostimulation, given the current trend away from synthetic chemicals. Leachates extracted from plantain stems, obtained after the biodegradation of plant material, were characterized to test their potential role as fungicides, plant defense elicitors, and/or plant biostimulants. The plant extracts induced a slight inhibition of fungal growth of an aggressive strain of Colletotrichum gloeosporioides, responsible for anthracnose. Organic compounds such as cinnamic, ellagic, quinic, and fulvic acids and indole alkaloids such as ellipticine, as well as minerals such as potassium, calcium, and phosphorus, may be responsible for the inhibition of fungal growth. Jasmonic, benzoic, and salicylic acids have also been found. These are known to play a role in plant defense and as biostimulants in tomatoes. Indeed, foliar application of banana leachate induced overexpression of the LOXD, PPOD, and Worky70-80 genes, which are involved in phenylpropanoid metabolism, jasmonic acid biosynthesis, and salicylic acid metabolism, respectively. Leachate also activated root growth in tomato seedlings. However, the main effect of leachate was observed in mature plants, where it reduced leaf area and fresh weight, remodeled stem cell wall glycopolymers, and increased proline dehydrogenase gene expression. There is a growing demand for molecules of natural origin for biocontrol and biostimulation, given the current trend away from synthetic chemical products. Leachates extracted from plantain stems were obtained after biodegradation of the plant material. To characterize the leachate, quantitative determinations of nitrogen, carbon, phosphorus, and cations (K+, Ca2+, Mg2+, Na+), Q2/4, Q2/6, and Q4/6 absorbance ratios, and metabolomic analysis were carried out. The potential role of plantain leachates as fungicide, elicitor of plant defense, and/or plant biostimulant was evaluated by agar well diffusion method, phenotypic, molecular, and imaging approaches. The plant extracts induced a slight inhibition of fungal growth of an aggressive strain of Colletotrichum gloeosporioides, which causes anthracnose. Organic compounds such as cinnamic, ellagic, quinic, and fulvic acids and indole alkaloid such as ellipticine, along with some minerals such as potassium, calcium, and phosphorus, may be responsible for the inhibition of fungal growth. In addition, jasmonic, benzoic, and salicylic acids, which are known to play a role in plant defense and as biostimulants in tomato, were detected in leachate extract. Indeed, foliar application of banana leachate induced overexpression of LOXD, PPOD, and Worky70-80 genes, which are involved in phenylpropanoid metabolism, jasmonic acid biosynthesis, and salicylic acid metabolism, respectively. Leachate also activated root growth in tomato seedlings. However, the main impact of the leachate was observed on mature plants, where it caused a reduction in leaf area and fresh weight, the remodeling of stem cell wall glycopolymers, and an increase in the expression of proline dehydrogenase. [ABSTRACT FROM AUTHOR]

At concentrations achieved following systemic administration, the primary effect of imidazoles and triazoles on fungi is inhibition of 14-α-sterol demethylase, a microsomal cytochrome P450 (CYP) enzyme. Imidazoles and triazoles impair the biosynthesis of ergosterol for the cytoplasmic membrane and lead to the accumulation of 14-α-methyl sterols. The synthetic imidazole miconazole is additionally able to increase intracellular reactive oxygen species, at least in part through inhibition of fungal catalase and peroxidase. This unique feature of miconazole is probably the basis for its fungicidal activity in C. albicans, in addition to the fungistatic mode of action. Studies show that miconazole is superior to nystatin treatment and demonstrate its impact as one of the best options in managing vulvovaginal candidiasis. Regarding recurrent vulvovaginal candidiasis, several new drugs are currently developed to ensure effective treatment also for this group of patients.

The computer program Prediction of Activity Spectra for Substances (PASS), which allows a prediction of the spectrum of biological activity of chemical compounds based on an analysis of their structure(activity relationships, was used to predict the biological activity of new promising derivatives of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2H-pyrido[4,3,2-de]cinnolin-3-ones. Screening of the compounds found that 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2H-pyrido[4,3,2-de]cinnolin-3-ones could exhibit antibacterial and antifungal activity. The antimicrobial activity of the synthesized compounds was studied against Gram-positive and Gram-negative bacteria and yeast and mold fungi. The compounds were shown to have an inhibitory effect on some types of Gram-positive bacteria and fungi. 8,8-Dimethyl-2-p-tolyl-5-p-chlorophenyl-3,7,8,9-tetrahydro-2H-pyrido[4,3,2-de]cinnolin-3-one had a minimum inhibitory concentration of 48 μg/mL for Gram-positive bacteria and possessed the most pronounced antimicrobial activity of the tested compounds. [ABSTRACT FROM AUTHOR]

Propenylbenzenes, including isosafrole, anethole, isoeugenol, and their derivatives, are natural compounds found in essential oils from various plants. Compounds of this group are important and valuable, and are used in the flavour and fragrance industries as well as the pharmaceutical and cosmetic industries. The aim of this study was to develop an efficient process for synthesising oxygenated derivatives of these compounds and evaluate their potential biological activities. In this paper, we propose a two-step chemo-enzymatic method. The first step involves the synthesis of corresponding diols 1b-5b from propenylbenzenes 1a-5a via lipase catalysed epoxidation followed by epoxide hydrolysis. The second step involves the microbial oxidation of a diasteroisomeric mixture of diols 1b-5b to yield the corresponding hydroxy ketones 1c-4c, which in this study was performed on a preparative scale using Dietzia sp. DSM44016, Rhodococcus erythropolis DSM44534, R. erythropolis PCM2150, and Rhodococcus ruber PCM2166. Application of scaled-up processes allowed to obtain hydroxy ketones 1-4c with the following yield range 36-62.5%. The propenylbenzene derivatives thus obtained and the starting compounds were tested for various biological activities, including antimicrobial, antioxidant, haemolytic, and anticancer activities, and their impact on membrane fluidity. Fungistatic activity assay against selected strains of Candida albicans results in MIC50 value varied from 37 to 124 µg/mL for compounds 1a, 3a-c, 4a,b, and 5a,b. The highest antiradical activity was shown by propenylbenzenes 1-5a with a double bond in their structure with EC50 value ranged from 19 to 31 µg/mL. Haemolytic activity assay showed no cytotoxicity of the tested compounds on human RBCs whereas, compounds 2b-4b and 2c-4c affected the fluidity of the RBCs membrane. The tested compounds depending on their concentration showed different antiproliferative activity against HepG2, Caco-2, and MG63. The results indicate the potential utility of these compounds as fungistatics, antioxidants, and proliferation inhibitors of selected cell lines. [ABSTRACT FROM AUTHOR]

This article presents the results of a gas chromatography-mass spectrometry (GC-MS) study of the chemical composition of Cupressus sempervirens L. (Mediterranean cypress) and Thuja occidentalis L. (northern white-cedar) essential oils, as well as their activity against four strains of pathogenic fungi infecting crops. Our observations revealed high concentrations of monoterpenes, sesquiterpenes, monoteppernic and sesquitepernic alcohols, ethers and esters, and flavonoids in the essential oil samples of both plants. Notably, the growth of pathogens was significantly inhibited by α-pinene (44.73% for C. sempervirens and 27.74% for T. occidentalis) and α-terpineol (4.04% and 5.14%, respectively) found at high levels. The selective effect exerted by all the compounds on the strains of the phytopathogenic fungi tested was established. C. sempervirens L. essential oil displayed the highest antifungal activity against fusarial wilt (Fusarium graminearum FG-30) and snow mold (Microdochium nivale) pathogens.

Propenylbenzenes, including isosafrole, anethole, isoeugenol, and their derivatives, are natural compounds found in essential oils from various plants. Compounds of this group are important and valuable, and are used in the flavour and fragrance industries as well as the pharmaceutical and cosmetic industries. The aim of this study was to develop an efficient process for synthesising oxygenated derivatives of these compounds and evaluate their potential biological activities. In this paper, we propose a two-step chemo-enzymatic method. The first step involves the synthesis of corresponding diols 1b–5b from propenylbenzenes 1a–5avia lipase catalysed epoxidation followed by epoxide hydrolysis. The second step involves the microbial oxidation of a diasteroisomeric mixture of diols 1b–5b to yield the corresponding hydroxy ketones 1c–4c, which in this study was performed on a preparative scale using Dietzia sp. DSM44016, Rhodococcus erythropolis DSM44534, R. erythropolis PCM2150, and Rhodococcus ruber PCM2166. Application of scaled-up processes allowed to obtain hydroxy ketones 1-4c with the following yield range 36–62.5%. The propenylbenzene derivatives thus obtained and the starting compounds were tested for various biological activities, including antimicrobial, antioxidant, haemolytic, and anticancer activities, and their impact on membrane fluidity. Fungistatic activity assay against selected strains of Candida albicans results in MIC50 value varied from 37 to 124 μg/mL for compounds 1a, 3a–c, 4a,b, and 5a,b. The highest antiradical activity was shown by propenylbenzenes 1-5a with a double bond in their structure with EC50 value ranged from 19 to 31 μg/mL. Haemolytic activity assay showed no cytotoxicity of the tested compounds on human RBCs whereas, compounds 2b–4b and 2c–4c affected the fluidity of the RBCs membrane. The tested compounds depending on their concentration showed different antiproliferative activity against HepG2, Caco-2, and MG63. The results indicate the potential utility of these compounds as fungistatics, antioxidants, and proliferation inhibitors of selected cell lines.

Trichoderma spp. produce multiple bioactive volatile organic compounds (VOCs). While the bioactivity of VOCs from different Trichoderma species is well documented, information on intraspecific variation is limited. The fungistatic activity of VOCs emitted by 59 Trichoderma sp. "atroviride B" isolates against the pathogen Rhizoctonia solani was investigated. Eight isolates representing the two extremes of bioactivity against R. solani were also assessed against Alternaria radicina, Fusarium oxysporum f. sp. lycopersici and Sclerotinia sclerotiorum. VOCs profiles of these eight isolates were analyzed using gas chromatography–mass spectrometry (GC-MS) to identify a correlation between specific VOCs and bioactivity, and 11 VOCs were evaluated for bioactivity against the pathogens. Bioactivity against R. solani varied among the fifty-nine isolates, with five being strongly antagonistic. All eight selected isolates inhibited the growth of all four pathogens, with bioactivity being lowest against F. oxysporum f. sp. lycopersici. In total, 32 VOCs were detected, with individual isolates producing between 19 and 28 VOCs. There was a significant direct correlation between VOC number/quantity and bioactivity against R. solani. 6-pentyl-α-pyrone was the most abundant VOC produced, but 15 other VOCs were also correlated with bioactivity. All 11 VOCs tested inhibited R. solani growth, some by >50%. Some of the VOCs also inhibited the growth of the other pathogens by >50%. This study demonstrates significant intraspecific differences in VOC profiles and fungistatic activity supporting the existence of biological diversity within Trichoderma isolates from the same species, a factor in many cases ignored during the development of biological control agents. [ABSTRACT FROM AUTHOR]

Vegetal foods are one of the most consumed commodities globally, accounting for more than 40 % of total food wastage. Hydrothermal conversion is an innovative transformation method towards effective utilization for vegetal waste to generate value-added products which are more eco-friendly and sustainable. In this study, the vegetable wastes of Chinese cabbage (C), broccoli (B) and sweet potato (S) were used to prepare humic acids (HAs) by hydrothermal conversion. The KOH concentration was the key factor affecting the preparation of HA. There was a significant difference in S element (p < 0.05), which followed the order of S-HA (1.48 %) > C-HA (0.57 %) > B-HA (0.43 %). The proportions of HA h , HA m , and HA l with molecular weights of > 100, 10–100, and < 10 kDa were 49.89–52.62 %, 23.70–27.92 %, and 18.75–21.13 %, respectively. HAs were rich in oxygen-containing functional groups such as C O, C C, and COOH. The fungistatic activities of Botrytis cinerea and Phytophthora capsici Leonian by S-HA were higher than those of other HAs. Through Mantel analysis and redundancy analysis, it was shown that element S and structure of aliphatic compounds had important effects on the fungistatic activity. In summary, hydrothermal conversion provided a new theory and technical guidance for the high-value utilization of vegetable waste. [Display omitted] [ABSTRACT FROM AUTHOR]

There is a growing demand for molecules of natural origin for biocontrol and biostimulation, given the current trend away from synthetic chemical products. Leachates extracted from plantain stems were obtained after biodegradation of the plant material. To characterize the leachate, quantitative determinations of nitrogen, carbon, phosphorus, and cations (K+, Ca2+, Mg2+, Na+), Q2/4, Q2/6, and Q4/6 absorbance ratios, and metabolomic analysis were carried out. The potential role of plantain leachates as fungicide, elicitor of plant defense, and/or plant biostimulant was evaluated by agar well diffusion method, phenotypic, molecular, and imaging approaches. The plant extracts induced a slight inhibition of fungal growth of an aggressive strain of Colletotrichum gloeosporioides, which causes anthracnose. Organic compounds such as cinnamic, ellagic, quinic, and fulvic acids and indole alkaloid such as ellipticine, along with some minerals such as potassium, calcium, and phosphorus, may be responsible for the inhibition of fungal growth. In addition, jasmonic, benzoic, and salicylic acids, which are known to play a role in plant defense and as biostimulants in tomato, were detected in leachate extract. Indeed, foliar application of banana leachate induced overexpression of LOXD, PPOD, and Worky70-80 genes, which are involved in phenylpropanoid metabolism, jasmonic acid biosynthesis, and salicylic acid metabolism, respectively. Leachate also activated root growth in tomato seedlings. However, the main impact of the leachate was observed on mature plants, where it caused a reduction in leaf area and fresh weight, the remodeling of stem cell wall glycopolymers, and an increase in the expression of proline dehydrogenase.

The aim of conducted research was to devalute the inhibition effect of metabolites secreted by some Rhizospheric bacteria on the growth of two pathogenic fungi: Rhizoctonia solani and Fussarium solani, 330 bacteria isolates were obtained from the rhizosphere of the wheat, tomato, cowpea and Mt. Atlas mastic tree grown in the Sulaimani. Thirty-five isolates were screened for suppression of phytopathogeneic fungus. Results showed that most of these rhizospheric bacteria were have fungistatic potential in different degrees. The highest inhibition of the linear growth of fungi was noted for R. solani and F. solani, by Bacillus cereus LXJ73 (90.41%), Bacillus atropheaus SM-1 (75%) respectively. Six bacterial isolates were selected which have potential effect on the growth of the two studied fungi, five isolates belonging to the Bacillus genus and one isolate belonging to the genus Klebsiella. these isolates were molecularly confirmed by 16SrRNA, and their activity for inhibiting fungal growth were studied. The extracted metabolities analysied by Gas chromatography-Mass spectrometry (GCMS), showing that extracts contain different volatile organic compounds as Pyrrolo[1,2-a]pyrazine-1,4-dione, hexahydro-, 2-Pentanone, 4-hydroxy-4-methyl-, Isosteviol methyl ester,2-methyl-, Butanoic acid, 3-methyl-, 3- Pyrrolidin-2-yl-propionic acid, 9-Octadecenamide, (Z)-, Hexadecane, Tridecane, 2,5-Piperazinedione, 3,6-bis(2- methyl propyl)-, 1,2-Benzenedicarboxylic acid, diisooctyl ester, Acetic acid, Dodecane, beta.-D-Glucopyranose, 1,6-anhydro-, Lauric acid, 2-(hexadecyloxy)-3-(octadecyloxy)propyl ester and cis-Vaccenic acid. The presence of these componuds indicate that all studied Bacillus species and Klebsiella michiganensis M1-3-11having antagonistic activity and they can be used for development of biocontrol agents to reducing the phytopathogenic problems and decreasing mycotoxine in contaminated crops. [ABSTRACT FROM AUTHOR]

The possibility of increasing the biological efficiency of the Vitaplan biological product via the inclusion of chitosan salicylate as an inducer of plant disease resistance against dark-brown spot disease in wheat was studied. It was established that the addition to the medium of chitosan salicylate at a concentration of 0.1% for the submerged cultivation of Bacillus subtilis VKM B-2604D and VKM B-2605D strains (components of the Vitaplan product), as well as to the Vitaplan product, increased its protective effect in the wheat–Cochliobolus sativus pathosystem by 1.5–2 times. The increased biological activity of new formulations of the Vitaplan product is apparently the result of a combination of the fungicidal activity of the biological product and the induction of plant defense reactions by chitosan salicylate. [ABSTRACT FROM AUTHOR]

Fusarium Head Blight (FHB), caused by multiple species of Fusarium in small grain cereals, is a significant and long-standing problem anywhere in the world. Knowing regional Fusarium spp. present on non-symptomatic grains and their potential for mycotoxin production is of concern for identifying novel actions for FHB and mycotoxin management, such as treatments with essential oils. Analyzing the mycotoxin content of grains from non-symptomatic ears of different wheat varieties cultivated in Tunisia, we isolated Fusaria specimens identified as F. culmorum and F. acuminatum using analysis of the partial DNA sequence of the β-tubulin gene and ITS region. Two isolates of the latter species, uncommon in cereal grains in this region until now, were shown to be effective producers of enniatins in vitro, with 1390 and 3089 µg g−1 mycelial biomass (dry) in 11-day-old cultures. The susceptibility of an isolate of F. acuminatum to the fungistatic and antimycotoxin effects of eight essential oils was measured. Essential oils from Ammoides pusilla and Thymus capitatus used at 0.1 µL mL−1 in an agar culture medium, affected the mycelial growth by 55% and 79%, respectively and reduced the accumulation of enniatins per unit of mycelial colony by 26% and 52%, respectively. Finally, F. acuminatum was shown to be a contaminant of wheat grains in Tunisia and it may contribute to the contamination in enniatins. Two essential oils of Tunisian plants could be used for developing a biofungicide limiting both its mycelial growth and its accumulation of mycotoxins in grains. [ABSTRACT FROM AUTHOR]

Surfactants (adjuvants) are the substances often added to the spray tank, besides the pesticide formulation, whose role is to improve the performance of the pesticide or the physical properties of the spray mixture, or both. Adjuvants are not often used as fungicides themselves, however, it is interesting to investigate if they can improve the fungistatic activity of the system they are included in. Therefore the main aim of this work was to determine the effect of the addition of a newly obtained, never investigated before, sulfobetaine type surfactant to the fungicides on their final properties. In the in vitro experiment fungistatic activity of the surfactant and the system of surfactant with strobilurins and benzimidazole fungicides were evaluated. The tested surfactants were added to the liquid medium of Potato Dextrose Agar (PDA) at concentrations: 1, 10, 50, and 100 ppm. The organisms of Fusarium culmorum, Rhizoctonia solani, Microdochium nivale, and Alternaria brassicas were used as indicators. The experiments have shown that the addition of the new surfactant studied to the medium resulted in inhibition of mycelium growth of all the tested fungi. The system with the surfactant and the fungicide was much more effective against the tested fungi than individual fungicides.

Relevance. The use of chemical fungicides in protecting plants from pathogens is the most common way, despite the proven danger of pesticides. The use of biofungicides based on essential oils of medicinal plants, which also have phytoncidal properties, can be a suitable alternative to chemical preparations. In the years favorable for the development of alternariosis or cladosporiosis, spots appear on the plants, leading to necrosis and significant loss of seed productivity. Therefore, the search for new effective and safe means of combating fungal phytopathogens becomes relevant.Methods. Alternaria alternata (2018-1.1) and Cladosporium cladosporioides (2019-11.4) strains were isolated from leaves with signs of alternariosis and cladosporiosis, on which the essential oils Abies alba, Artemisia vulgaris, Caryophyllus aromaticus, Coriandrum sativum, Lavandula officinalis, Ocimum basilicum, Pimpinella anisum, Rosmarinus officinalis, Salvia sclarea, Thymus vulgaris. The antifungal activity of essential oils was evaluated by comparing the diameter of the experimental (with the addition of essential oil to the Petri dish) and control colonies using the author’s scale.Results. All studied essential oils had antifungal properties, but species-specificity was observed. Essential oils of basil, coriander and thyme showed a fungicidal effect on C. cladosporioides and A. alternata. Lavender oil proved to be a fungicide for A. alternata and a strong fungistatic for C. cladosporioides. To create biological products for plant protection against alternariosis, sage essential oil (moderate fungistatic effect) may also be of interest, and cladosporiosis - anise and rosemary oils.

Trichoderma spp. produce multiple bioactive volatile organic compounds (VOCs). While the bioactivity of VOCs from different Trichoderma species is well documented, information on intraspecific variation is limited. The fungistatic activity of VOCs emitted by 59 Trichoderma sp. “atroviride B” isolates against the pathogen Rhizoctonia solani was investigated. Eight isolates representing the two extremes of bioactivity against R. solani were also assessed against Alternaria radicina, Fusarium oxysporum f. sp. lycopersici and Sclerotinia sclerotiorum. VOCs profiles of these eight isolates were analyzed using gas chromatography–mass spectrometry (GC-MS) to identify a correlation between specific VOCs and bioactivity, and 11 VOCs were evaluated for bioactivity against the pathogens. Bioactivity against R. solani varied among the fifty-nine isolates, with five being strongly antagonistic. All eight selected isolates inhibited the growth of all four pathogens, with bioactivity being lowest against F. oxysporum f. sp. lycopersici. In total, 32 VOCs were detected, with individual isolates producing between 19 and 28 VOCs. There was a significant direct correlation between VOC number/quantity and bioactivity against R. solani. 6-pentyl-α-pyrone was the most abundant VOC produced, but 15 other VOCs were also correlated with bioactivity. All 11 VOCs tested inhibited R. solani growth, some by >50%. Some of the VOCs also inhibited the growth of the other pathogens by >50%. This study demonstrates significant intraspecific differences in VOC profiles and fungistatic activity supporting the existence of biological diversity within Trichoderma isolates from the same species, a factor in many cases ignored during the development of biological control agents.

A new idea for the modification of a carboxylic group in phenoxyacetic herbicides is proposed. Common herbicides, 2,4-dichlorophenoxyacetic acid (2,4-D) and 4-chloro-2-methylphenoxyacetic acid (MCPA), and their chalcogen analogs (arylthio and arylselenyl fragments instead of a phenoxy one) were used as carboxylic components in the tricomponent Passerini reaction. Cyclohexyl isocyanide and 4-isocyano-2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO-NC) were used as isocyanides. Acetone, acetaldehyde and formaldehyde were used as carbonyl components. Passerini adducts 4a–4L were obtained in yields of 32–59%. The structures of the Passerini adducts were determined using spectroscopic methods: MS, HR MS, 1H NMR, 13C NMR, 77Se NMR (if appropriate) and IR spectra (MS, HR MS, IR for the nitroxides 4k and 4L). The herbicidal activity of the Passerini adducts synthesized (4a–4L) was tested against ten weed species (at 2 kg/ha using 2,4-D and MCPA as a control). 100% herbicidal post-emergent activity was reported for 4i, 4j, 4k, 4L [a weed black mustard (Brassica nigra)], for 4k, 4L [weeds pale smartweed (Polygonum lapathifolium) and fathen (Chenopodium album)], as well as for 4k (weeds common poppy (Papaver rhoeas) and gallant soldier (Galinsoga parviflora)). The fungistatic activity of the Passerini adducts synthesized (4a–4L) was tested against six phytopathogenic fungi species (at 200 mg/L and procymidone as a control). The tested compounds showed a weak activity (% of inhibition) against: Alternaria alternata:4g (47), 4i (26), 4j (26), 4k (50), Botrytis cinerea4g (38), Fusarium culmorum4g (44), Phytophthora cactorum4i (35), 4j (35), 4k (30), Rhizoctonia solani4g (30), 4i (24), Phytophthora infestans4g (29), 4i (34), 4j (28), 4k (46). [ABSTRACT FROM AUTHOR]

Fusarium Head Blight (FHB), caused by multiple species of Fusarium in small grain cereals, is a significant and long-standing problem anywhere in the world. Knowing regional Fusarium spp. present on non-symptomatic grains and their potential for mycotoxin production is of concern for identifying novel actions for FHB and mycotoxin management, such as treatments with essential oils. Analyzing the mycotoxin content of grains from non-symptomatic ears of different wheat varieties cultivated in Tunisia, we isolated Fusaria specimens identified as F. culmorum and F. acuminatum using analysis of the partial DNA sequence of the β-tubulin gene and ITS region. Two isolates of the latter species, uncommon in cereal grains in this region until now, were shown to be effective producers of enniatins in vitro, with 1390 and 3089 µg g−1 mycelial biomass (dry) in 11-day-old cultures. The susceptibility of an isolate of F. acuminatum to the fungistatic and antimycotoxin effects of eight essential oils was measured. Essential oils from Ammoides pusilla and Thymus capitatus used at 0.1 µL mL−1 in an agar culture medium, affected the mycelial growth by 55% and 79%, respectively and reduced the accumulation of enniatins per unit of mycelial colony by 26% and 52%, respectively. Finally, F. acuminatum was shown to be a contaminant of wheat grains in Tunisia and it may contribute to the contamination in enniatins. Two essential oils of Tunisian plants could be used for developing a biofungicide limiting both its mycelial growth and its accumulation of mycotoxins in grains.

Introduction: Antifungal resistant is one of the causes of high mortality rates during invasive candidiasis. Since development of new antifungal agents is limited, researchers have focused on natural products including essential oils (EOs) with antifungal properties. In immunocompromised patients fungicidal activity is of benefit. This study was designed to evaluate chemical composition and fungicidal/fungistatic activities of five Iranian EOs and against fluconazole resistant Candida species. Methods: To determine chemical composition of EOs gas chromatography-mass spectroscopy (GC/MS) was employed. Fluconazole resistant Candida species were chosen and minimum inhibitory concentration (MIC) values of studied EOs were determined by broth microdilution method. Minimum fungicidal concentration (MFC) was determined as the lowest concentration with no fungal growth on solid media. Fungicidal activity was calculated by MFC/MIC ratio. Results: The results showed that C. albicans and C. tropialis isolates were susceptible to itraconazole (ITC) and voriconazole (VRC) while one species of C. glabrata and C. krusei each was resistant to itraconzaole; and itraconazole resistant C. glabrata isolate was resistance to voriconzaole as well. Among tested EOs, the ones from Cinnamomum cayennense, Origanum majorana var. majoranoides and Andropogon citratus had the highest anti-Candida activity. Artemisia aromatica A. Nelson had the highest MIC value against Candida isolates. All EOs in this study had fungicidal activity. Conclusion: In general, the tested natural compounds are suitable to be used as anti-Candida. However more studies are needed on each chemical compound to evaluate its antifungal activity alone or in combination with other agents.

Objective: To investigate the fungistatic activity and synergistic effects of natural products and their constituents, including traditional oriental medicines (TOMs). Methods: Fungistatic activities of TOMs prepared by hot-water (115 °C) or ethanol (70%; 40 °C) extraction were determined by their minimum inhibitory concentration. To assess possible synergistic effects, minimum inhibitory concentrations of various combinations were evaluated. Results: By evaluating antifungal susceptibility of Trichophyton rubrum, which is a major causative fungus for several types of dermatophytosis, we confirmed that ethanol extracts were more active than hot-water extracts in 25 of the 36 TOMs, suggesting that the constituents with high hydrophobicity tend to contribute significantly to fungistatic activity. We selected four TOMs with high fungistatic activity, including Aucklandiae radix, Gentianae macrophyllae radix, Scutellariae radix, and Galla rhois, and their synergistic effects were investigated through the combination studies between TOMs or TOM-conventional drug terbinafine. In combinations between four TOMs, partial synergistic effects were observed in Aucklandiae radix–Galla rhois and Gentianae macrophyllae radix–Galla rhois combinations, as supported by the lowest fractional inhibitory concentration index value of 0.66 for both combinations. Furthermore, Galla rhois showed the strongest synergistic effect on growth inhibition of Trichophyton rubrum with a fractional inhibitory concentration index value of 0.50 in combination with terbinafine. Conclusions: Our findings indicate that the combination of TOMs and TOM-terbinafine may be effective on treatment for chronic and recurrent dermatophytosis by improving fungistatic activity and led to decrease systemic toxicity in clinical practice.

Instead of chemical fungicides, biological ones should be used, based on which plant essential oils can be used. Plant diseases alternariosis and cladosporiosis cause leaf necrosis and lead to large losses in seed productivity. Therefore, it is important to search for new effective and safe means of protection against phytopathogenic hyphomycetes. The strains of Alternaria alternata and Cladosporium cladosporioides were isolated from the leaves of Vicia faba, and they were tested for the effect of the essential oils Artemisia vulgaris, Caryophyllus aromaticus, Coriandrum sativum, Lavandula officinalis, Ocimum basilicum, Pimpinella anisum, Rosmarinus officinalis, Salvia sclarea, Thymus vulgaris. To compare the antifungal activity of essential oils, the diameter of the experimental colonies (with the addition of essential oil on the Petri dish cover) and control colonies was measured using the author's scale. It was found that all the studied essential oils had antifungal properties, but species-specificity was noted. Essential oils of basil, coriander and thyme showed a fungicidal effect on both strains. The fungicide for A. alternata and the strong fungistatic for C. cladosporioides was lavender oil. When creating a biological product to protect plants from alternariosis, sage essential oil with a medium fungistatic effect can also be used, and anise and rosemary oils can be used to protect plants from cladosporiosis. [ABSTRACT FROM AUTHOR]

BACKGROUND: Humic‐like substances (HULIS) for use in controlling soil‐borne diseases have been a research focus, but obtaining HULIS with high fungistatic activity via different extraction solvents has been challenging. In this work, three solvents were selected to extract HULIS from weathered coal. Inhibition rates against phytopathogens were used to evaluate the fungistatic activities of HULIS. Element contents (C, N, S, and O) and carbon‐13‐cross polarization magic‐angle spinning nuclear magnetic resonance (13C‐CP‐MAS NMR) spectra were used to evaluate the chemical composition. The relationships between the chemical compositions and fungistatic activities were assessed by redundancy analysis (RDA) and partial least squares regression (PLSR). RESULTS: The results showed that HULIS extracted with different solvents varied in the element contents, organic carbon structures and fungistatic activities. HULIS extracted with potassium hydroxide–ethanol had the highest content of C, the lowest contents of N and O, and the highest fungistatic activities (up to 71.86%). Consistent results through RDA and PLSR shows that C and S had positive effects on the fungistatic activity, while N and O had negative effects. Aliphatic C in HULIS had positive effects on the fungistatic activity, while the aromatic fraction and anomeric C had negative effects. CONCLUSION: In summary, different solvents extracted different fractions from weather coal. Mixed solvents with organic and inorganic solvents were more beneficial for extracting active fractions with higher fungistatic activity of HULIS from weather coal. The results of this work provide a good theoretical basis for the application of HULIS extracted from weathered coal. © 2019 Society of Chemical Industry [ABSTRACT FROM AUTHOR]

We determined the chemical composition and explored the hypothesis that the essential oil of the fruits of Pimenta dioica inhibits the mycelial development of fungi Fusarium oxysporum f. sp. lycopersici, F. oxysporum f. sp. passiflorae, F. subglutinans f. sp. ananas, F. oxysporum f. sp. vasinfectum e F. oxysporum f. sp. Cubense. To do this, we extracted the oil by hydrodistillation, identified its components by gas chromatography coupled to mass spectrometry (GC-MS) and determined the fungal activity against five special forms of Fusarium species. The results showed that the oil had 76.88% of eugenol and inhibited the mycelial development of fungi up to 97.78% in an average of 7.2 days. Therefore, oil is a potential natural fungicide. [ABSTRACT FROM AUTHOR]

Enniatins are mycotoxins produced by Fusarium species contaminating cereals and various agricultural commodities. The co-occurrence of these mycotoxins in large quantities with other mycotoxins such as trichothecenes and the possible synergies in toxicity could lead to serious food safety problems. Using the agar dilution method, Ammoides pusilla was selected among eight Tunisian plants for the antifungal potential of its essential oil (EO) on Fusarium avenaceum mycelial growth and its production of enniatins. Two EO batches were produced and analyzed by GC/MS-MS. Their activities were measured using both contact assays and fumigant tests (estimated IC50 were 0.1 µL·mL−1 and 7.6 µL·L−1, respectively). The A. pusilla EOs and their volatiles inhibited the germination of spores and the mycelial growth, showing a fungistatic but not fungicidal activity. The accumulation of enniatins was also significantly reduced (estimated IC50 were 0.05 µL·mL−1 for the contact assays and 4.2 µL·L−1 for the fumigation assays). The most active batch of EO was richer in thymol, the main volatile compound found. Thymol used as fumigant showed a potent fungistatic activity but not a significant antimycotoxigenic activity. Overall, our data demonstrated the bioactivity of A. pusilla EO and its high potential to control F. avenaceum and its enniatins production in agricultural commodities.

Complexes of colchiceine with monovalent cation perchlorates and iodides have been obtained and characterized by spectroscopic methods. DFT and spectroscopic studies reveal that the dihedral angle ω1‐1a‐12‐12a, crucial for colchicine biological mechanism of action, that is, binding to tubulins depends on the diameter of the complexed metal cation. Biological tests indicated no antifungal properties of colchicine (it was active only toward A.pullulans), in contrast to its derivative—(colchiceine). Complexation of colchiceine with metal cations improved significantly the antifungal potency, even below MIC <1 μg/ml. The colchiceine complexes were more potent than colchiceine, and some of them were even more potent than the fungicidal standard IPBC. The highest potency of colchiceine complexes was noted against A. pullulans (MIC = 0.5 μg/ml). In contrast to the findings concerning antifungal potency, the anticancer studies showed complexes of colchicine more active (~IC50 = 2 nM) than those of colchiceine (~IC50 = 6 μM). MDA‐MB‐231 breast cancer cell lines and human lung fibroblasts CCD39Lu were also tested. [ABSTRACT FROM AUTHOR]

Elena Campione,1 Roberta Gaziano,2 Daniele Marino,2 Augusto Orlandi3 1Department of Dermatology, 2Department of Microbiology, 3Department of Anatomic Pathology, University of Rome Tor Vergata, Rome, Italy Purpose: Fungal infections are a major complication in hematologic and neoplastic patients causing severe morbidity and mortality. Aspergillus fumigatus and Candida albicans are among the most invasive opportunistic pathogens in immunocompromised patients, and classic antifungal drugs are frequently unsuccessful in these patients. Recent reports hypothesize that the antifungal efficacy of all-trans retinoic acid (ATRA) is mainly related to its strong capacity to stimulate monocyte-mediated immunity, but no consideration was given to its potential direct fungistatic activity. Moreover, ATRA offers the opportunity for systemic therapy. Methods and results: We investigated the efficacy of ATRA at different concentrations for its antifungal activity against opportunistic A. fumigatus and C. albicans obtained from clinical samples according to standard protocols. A fungistatic activity of ATRA on A. fumigatus and C. albicans at 0.5–1 mM concentration was documented up to 7 days. Conclusion: This is the first evidence of a direct and strong fungistatic activity of ATRA against A. fumigatus and C. albicans. The potential adjuvant therapeutic application of ATRA might be useful in the treatment and/or prevention of systemic mycoses in immunocompromised patients. The discovery of a direct fungistatic activity, in association with its reported immunomodulatory properties, makes ATRA an excellent candidate for new combined antifungal strategies for systemic mycoses in immunocompromised and cancer patients. Keywords: all-trans retinoic acid, fungistatic activity, fungal infections

The aim of the study was to detect the activity and characterize potentially fungistatic chitinases synthesized by rhizosphere bacteria identified as Paenibacillus sp. M4. Maximum chitinolytic activity was achieved on the fifth day of culturing bacteria in a growth medium with 1% colloidal chitin. Analysis of a zymogram uncovered the presence of four activity bands in the crude bacterial extract. The used three-stage protein purification procedure resulted in a single band of chitinase activity on the zymogram. The purified enzyme exhibited maximum activity at pH 6.5 and temperature 45oC, and thermal stability at 40oC for 4 h. In terms of substrate specificity, it is an exochitinase (chitobiose). The amino acid sequence obtained after mass spectrometry showed similarity to chitinase A1 synthesized by Bacillus circulans. The M4 isolate demonstrated the highest growth inhibiting activity against plant pathogens belonging to the genera Fusarium, Rhizoctonia and Alternaria. Fungistatic activity, although to a somewhat lesser degree, was also demonstrated by purified chitinase. The obtained results confirm the participation of the studied exochitinase in antagonism towards pathogenic molds. However, the lower fungistatic effectiveness of the chitinases points to the synergistic action of different metabolites in biocontrol by these bacteria.

The aim of the study was to determine the relationship between the chemical composition of eight commercial essential oils (EsO) (garlic, grapefruit, lemon grass, tea tree, thyme, verbena, cajeput, and Litsea cubeba) and their fungistatic activity in relation to four species of Fusarium: F. avenaceum, F. culmorum, F. graminearum, and F. oxysporum. The species identification of Fusarium isolates was confirmed by matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometer. The determination of qualitative and quantitative chemical composition of the EsO was carried out using the gas chromatography−mass spectrometry (GC−MS) method. The fungistatic activity of EsO was assessed by using the method of poisoned substrates. The data were compiled in the STATISTICA 13.0 program. The chemical composition of the tested oils varied; the dominant fraction, except for grapefruit and garlic oils, were monoterpenoids. The greatest similarity to the action of the synthetic pesticide Funaben T was found in four oils, i.e., thyme, lemongrass, verbena, and Litsea cubeba. The studies showed that F. oxysporum and F. avenaceum were characterized by a higher resistance to low oil concentrations, and F. culmorum and F. graminearum by sensitivity. The fungicidal activity of two EsO-dominant monoterpenoids-thymol and citral—has been confirmed.

Selenium analogs of phenoxyacetic herbicides, namely 2-(2,4-dichlorophenoxy)propionic acid (2,4-DP), 2-(2,4-dichlorophenoxy)acetic acid (2,4-D), 2-(4-chloro-2-methylphenoxy)propionic acid (MCPP), 2-(4-chloro-2-methylphenoxy)acetic acid (MCPA), 2-(2,4,5-trichlorophenoxy)propionic acid (2,4,5-TP), and 2-(2,4,5-trichlorophenoxy)acetic acid (2,4,5-T), were synthesized in two steps. Iodo aryl derivatives were dimerized with elemental selenium in the presence of CuO as catalyst to the corresponding diselenides. Diselenides were reduced with NaBH4 to a selenide anion and condensed with either propionic or chloroacetic acid to achieve the selenium analogs of phenoxyacetic herbicides. These selenium analogs show moderate herbicidal and fungistatic activity. [ABSTRACT FROM AUTHOR]

Objective: To investigate the fungistatic activity and synergistic effects of natural products and their constituents, including traditional oriental medicines (TOMs). Methods: Fungistatic activities of TOMs prepared by hot-water (115 °C) or ethanol (70%; 40 °C) extraction were determined by their minimum inhibitory concentration. To assess possible synergistic effects, minimum inhibitory concentrations of various combinations were evaluated. Results: By evaluating antifungal susceptibility of Trichophyton rubrum, which is a major causative fungus for several types of dermatophytosis, we confirmed that ethanol extracts were more active than hot-water extracts in 25 of the 36 TOMs, suggesting that the constituents with high hydrophobicity tend to contribute significantly to fungistatic activity. We selected four TOMs with high fungistatic activity, including Aucklandiae radix, Gentianae macrophyllae radix, Scutellariae radix, and Galla rhois, and their synergistic effects were investigated through the combination studies between TOMs or TOM-conventional drug terbinafine. In combinations between four TOMs, partial synergistic effects were observed in Aucklandiae radix-Galla rhois and Gentianae macrophyllae radix-Galla rhois combinations, as supported by the lowest fractional inhibitory concentration index value of 0.66 for both combinations. Furthermore, Galla rhois showed the strongest synergistic effect on growth inhibition of Trichophyton rubrum with a fractional inhibitory concentration index value of 0.50 in combination with terbinafine. Conclusions: Our findings indicate that the combination of TOMs and TOM-terbinafine may be effective on treatment for chronic and recurrent dermatophytosis by improving fungistatic activity and led to decrease systemic toxicity in clinical practice. [ABSTRACT FROM AUTHOR]

We analyzed antioxidant and antimicrobial activity of aqueous alcoholic extracts from mycothallus and mycelium of Inonotus rheades. It was found that 70% aqueous alcoholic extracts from mycelium of I. rheades had the biggest antioxidant activity. 30% aqueous alcoholic extracts from mycothallus and mycelium have antimicrobial activity against the variety of microorganisms (Salmonella еnteritidis IMVL, Enterococcus faecalis ATSS 29217, Salmonella Ngor IMVL, Streptococcus spp. 44, Staphylococcus aureus ATSS 209p, Escherichia coli ATSS3 5218, Escherichia coli TI). We determined fungistatic activity of 30% aqueous alcoholic extracts of mycelium against Saccharomyces cerevisiae.

The reactions of 3-isoselenocyanato-2,2,5,5-tetramethylpyrrolidine-1-oxyl, 3-isoselenocyanatomethyl-2,2,5,5-tetramethyl-3-pyrrolidine-1-oxyl, and 4-isoselenocyanato-2,2,6,6-tetramethylpiperidine-1-oxyl with selected amines and alcohols give the corresponding novel nitroxyl selenoureas and selenocarbamates, all bearing a nitroxyl moiety. Synthesized selenoureas and selenocarbamates show significant activity against pathogenic fungi and bacteria. In contrast to piperidine nitroxides, pyrrolidine, five-membered nitroxyl selenoureas and selenocarbamates show excellent antifungal and antibacterial activity against pathogenic fungi and bacteria, respectively.

Aryloxy fluoroacetic acids 3a - 3h – fluorine analogs of phenoxyacetic herbicides 2,4-D, MCPA, 2,4,5-T, and 4-CPA were efficiently synthesized in 29–88% yield, using appropriate phenols and either bromodifluoro- or bromofluoroacetic acid in the presence of sodium hydride as a base and in either dioxane or THF as solvents. Fluorine derivatives of 2,4-D ( 3a , 3b ) show herbicidal activity against three weed species. Parent herbicides 2,4-D, MCPA, 2,4,5-T, 4-CPA, monofluorine derivatives of MCPA ( 3d ) and 2,4,5-T ( 3f ) show fungistatic activity against phytopatogenic fungi species Phytophtora cactorum . [ABSTRACT FROM AUTHOR]

Eysenhardtia polystachya (Fabaceae) is a valuable medicinal plant from Mexico. There have been no cell culture studies of this plant to produce secondary metabolites. The aim of this work was to establish callus and cell suspension cultures of E. polystachya (Ortega) and to evaluate the content of phenols, total flavonoids, and fungicidal activity against Sclerotium cepivorum and Rhizoctonia solani from extracts of wild plant and cell cultures. An efficient protocol for callus induction and cell cultures was established. The maximum percentage of explants inducing callus (100 and 98%) was obtained using 1-naphthaleneacetic acid (8.28 μM) plus kinetin (0.41 μM) or picloram (4.14 μM) plus kinetin (0.41 μM), respectively. Only the cell suspension cultures from callus with picloram plus kinetin grew appropriately and the maximum dry biomass accumulation (14 g L − 1 ) occurred at 12 days of culture. The leaves from wild plants yielded larger amounts of total phenols (155.17 mg gallic acid equivalents g − 1 dry weight) and total flavonoids (124.3 mg quercetin equivalents g − 1 dry weight) compared to cell suspension cultures, which exhibited total phenols amounts of 73.98 mg gallic acid equivalents g − 1 dry weight and total flavonoids of 16.29 mg quercetin equivalents g − 1 dry weight. The fungicide Cercobin® inhibited 100% the S. cepivorum mycelial growth, while 80.0 and 73.0% inhibition was achieved with the ethyl acetate fraction of the dichloromethane extracts from E. polystachya sapwood and heartwood, respectively. However, cell suspension cultures showed only 39% inhibition of S. cepivorum mycelial growth with methanol extracts. The maximum percentage inhibition of R. solani (66.0%) occurred using the hexane fraction of methanolic extracts from cell suspension cultures; however, Cercobin® presented only 33.0% growth inhibition. Extracts of E. polystachya cell suspension cultures can be used as a biotechnological option against phytopathogenic fungi. [ABSTRACT FROM AUTHOR]

Copyright of Progress in Plant Protection is the property of Institute of Plant Protection and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The aim of the work was to determine the usefulness of dried leaves of savoy cabbage, red cabbage, horse radish and fringed cabbage in protection of cucumber against damping-off caused by fungi Rhizoctonia solani and Fusarium culmorum. In the laboratory experiments, pathogens were grown on PDA containing dried leaves (3g·100 cm-3) and in atmosphere containing volatile substances evolved from plant material. The addition of radish horse leaves into PDA caused total inhibition of R. solani development. Remaining plants were also characterized by high fungistatic activity (% of growth inhibition about 85%). F. culmorum was less sensitive. The horse radish leaves showed the strongest activity (65 %), weakest in combination with fringed cabbage leaves (38,9%). The similar regularity in the case of fumigation activity was observed. The effectiveness of dried leaves in protection of cucumber against damping-off was confirmed in greenhouse experiment. The amendment of soil inoculated with R. solani in dose 2 g per 500 cm3 of soil significantly increased the number of cucumber sprouts compared to the control. In the experiment with F. culmorum only in combination with horse radish and red cabbage leaves significant action was observed.

Copyright of Revista Brasileira de Engenharia Agricola e Ambiental - Agriambi is the property of Revista Brasileira de Engenharia Agricola e Ambiental and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The present investigation was carried out to analyse the presence of endophytes in the above-ground parts of Hipericum perforatum and to analyse the biodiversity and enumeration of epiphytes. Plant material was collected in Poland three times during the growing season. Phenotypic and genotypic diversity of all the endophytes and the most abundant epiphytes were researched. We analysed fungistatic activity of this isolates. From the endosphere of tested plant Alcaligenes faecalis and Bacillus licheniformis were isolated. The most numerous epiphytes were the copiotrophs and a bit less numerous were oligotrophs, bacteria cultivated on Bunt and Rovir’s medium and fungi. The least numerous bacteria were Azotobacter sp. Among all the molds dominant were: Cladosporium herbarum, C. cladosporioides and Alternaria consortialis, A. alternata, Clonostachys rosea f. catenulata (Gliocladium catenulatum), Scopulariopsis brevicaulis and Penicillium terrestre. Among phyllobacteria there were found mostly the following species: Burkholderia cepacia, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas fluorescens, P. putida, Pantoea agglomerans, Paenibacillus polymyxa, Bacillus cereus, Rhodococcus sp., R. erythropolis and Cellulosimicrobium cellulans. The broadest spectrum of antifungal activity was examined for the following species: Paenibacillus polymyxa, Pseudomonas putida and Pantoea agglomerans. P. polymyxa limited the growth of over 82% tested molds, so did the other two strains: P. agglomerans over 77% and P. putida over 73%.

Background. 1,3,5-triaryl-2-pyrazolines are organic luminophores with arylic radicals that show a wide biological activity and are used as liquid scintillators and electro-optic materials. Experimental. Eleven 2- pyrazolines were synthesized from phenylhidrazine and chalcones of the 8-hydroxyquinoline series: 3-(8-hydroxyquinolin-5-yl)-1-(3-R)-phenylprop-2-enone and 1-(8-hydroxyquinolin-5-yl)-3-(3-R)-phenylprop-2-enone, where R = H, CH3, OCH3, N(CH3)2, Cl, Br, and NO2. The structures were confirmed by elemental analysis, IR, ¹H-NMR, and electronic spectroscopy. Results and discussion. The 1- and 3- aryl substituents of the pyrazoline ring produced shifts to shorter or longer wavelengths, in absorbance and fluorescence. The electron acceptor hydroxyquinolinic fragment influenced the absorption and luminescence spectra; the possible cause of low quantum yields in pyrazolines 4a-g (1-phenyl-3-(4-R phenyl)-5-(8-hydroxyquinolinil-5)-2-pyrazoline) may be the specific intramolecular fluorescence quenching in bicromophores, characteristic of 5-acceptor substituted pyrazolines, and, in series 5a-g (1-phenyl-5-(4-R phenyl)-3-(8-hydroxyquinolinil-5)-2-pyrazoline) of excited-state intramolecular proton transfer (ESIPT) reactions, and the increasing donor-acceptor intramolecular interaction of their excited molecules; Density functional calculations (method PM6) were used to probe the electronic structure and energy ordering of the emissive and the electron-transfer states; PM6 results agreed with the experimental data. 1-phenyl-3-(4-R phenyl)-5-(8-hydroxyquinolinil-5)-2-pyrazoline showed fungistatic and fungicide activities. Additionally, all our pyrazolines showed wide theoretical biological activities. [ABSTRACT FROM AUTHOR]

The biologically active melanin fraction was isolated from the mushroom chaga and investigated. Terpenic and phenolic compounds were found in it by using mass spectrometry. The total contents of lipids, phenols, and carbohydrates were determined. It was found that the isolated fraction possessed antioxidant, fungicidal, fungistatic, and prebiotic activity for several microorganism groups. [ABSTRACT FROM AUTHOR]

Rhizopus rot is a common postharvest disease that causes devastating economic losses for peach producers around the world. Thus, new alternatives for the control of this disease are required. Herein we report on the obtainment of a new hydrotalcite/shilovite (HT/Sh) composite with in situ fungistatic properties on Rhizopus stolonifer. The protective effect of this composite was studied at the metabolic level by non-targeted 1H NMR metabolomics (coupled to PCA and OPLS-DA models) and RP-HPLC to determine possible changes in the primary and secondary metabolism of peaches. Our results demonstrated that the HT/Sh composite exerted a protective effect on the levels of specific sugars (glucose, ribose, and xylose) amino acids (glutamic acid, glutamine, histidine, isoleucine, leucine threonine, and valine), phenols (chlorogenic and neochlorogenic acids) and carotenoids (neoxanthin, violaxanthin, lutein, zeaxanthin, β-cryptoxanthin, and β-carotene). Our findings demonstrated that the new HT/Sh composite reported in this work was able to retard the emergence of Rhizopus rot in peaches for ten days and promoted the conservation of their nutraceutical content. [Display omitted] • A new antifungal shilovite/hydrotalcite composite was synthesized. • This material avoided side effects of peaches infected with Rhizopus infection. • Changes in the nutraceutical content were determined through NMR and HPLC. [ABSTRACT FROM AUTHOR]

[Display omitted] Zygomycetes are ubiquitous saprophytes in natural environments which transform organic matter. Some zygomycetes of gender Mucor have attracted interest in health sector. Due to its ability as opportunistic microorganisms infecting immuno-compromised people and to the few available pharmacological treatments, the mucormycosis is receiving worldwide attention. Concerning to the pharmacological treatments, some triazole-based compounds such as fluconazole are extensively used. Nevertheless, we focused in the quinolines since they are broadly used models for the design and development of new synthetic antifungal agents. In this study, the fungistatic activity on M. circinelloides of various 2-aryl-4-aryloxyquinoline-based compounds was discovered, and in some cases, it resulted better than reference compound fluconazole. These quinoline derivatives were synthesized via the C sp 2-O bond formation using diaryliodonium(III) salts chemistry. A QSAR study was carried out to quantitatively correlate the chemical structure of the tested compounds with their biological activity. Also, a docking study to identify a plausible action target of our more active quinolines was carried out. The results highlighted an increased activity with the fluorine- and nitro-containing derivatives. In light of the few mucormycosis pharmacological treatments, herein we present some non-described molecules with excellent in vitro activities and potential use in the mucormycosis treatment. [ABSTRACT FROM AUTHOR]