Dihydrochelerythrine(DHCHE)is an isoquinoline compound,which has distinct antifungal activity and can induce apoptosis.The antifungal activity of DHCHE against five rice pathogenic fungi was studied in vitro.At the co...Dihydrochelerythrine(DHCHE)is an isoquinoline compound,which has distinct antifungal activity and can induce apoptosis.The antifungal activity of DHCHE against five rice pathogenic fungi was studied in vitro.At the concentration of 7.5 mg/L,DHCHE exhibited the highest efficacy among tested compounds in inhibiting mycelium growth,with an inhibition rate of 68.8%in Ustilaginoidea virens,which was approximately 2.4 times of that of validamycin(28.7%).After exposure to DHCHE,transmission electron micrographs revealed spores showed incomplete organelles,malformed cell walls and nuclear membranes,as well as irregular lipid spheres.Reactive oxygen species accumulation in treated spores was markedly higher than that in control spores.DHCHE induced cell damage increased in a dose-dependent manner,as indicated by the decrease in mitochondrial membrane potential and initiation of apoptosis.The differences of expression levels of Fip1,ACP1,PMS2 and COX13 that are important for oxidative phosphorylation and mismatch repair pathway were significant,which may be some of the reasons for the induction of apoptosis in DHCHE-treated U.virens.The protein levels of Fip1,ACP1,PMS2 and COX13 agreed with protein fold change ratio from parallel reaction monitoring Gene Ontology terms and Kyoto Encyclopedia of Genes and Genomes pathway of differentially expressed proteins were further analyzed.These findings will help to elucidate the mechanisms associated with antifungal and pro-apoptotic effects of DHCHE on U.virens,thereby aiding the potential development of novel pesticides.展开更多
The present work was aimed to the study of the antifungal activity of essential oils of two aromatic plants against three strains of Sclerotinia sclerotiorum responsible for white rot of bean. The two essential oils (...The present work was aimed to the study of the antifungal activity of essential oils of two aromatic plants against three strains of Sclerotinia sclerotiorum responsible for white rot of bean. The two essential oils (EO) of the studied plants: Thymus vulgaris (HET) and Cymbopogon citratrus (HEC), used at different concentrations: C1 (0.75 ml/ml), C2 (1.5 ml/ml) and C3 (3 ml/ml) presented significant inhibitory activities on the three tested fungal strains namely Bia 1, Bia 2, and Njo 2. Two control treatments (T-: containing no antifungal substance and T+: synthetic fungicide) were also used. The antifungal activity here is related to the inhibition of mycelial growth especially with high concentrations of essential oils. Thus, against S. sclerotiorum, HET showed the highest activity comparable to that of T+ (100% inhibition) at all concentrations on the Bia 1 and Bia 2 strains and at concentration C3 on the Njo 2 strain compared to that of HEC, which certainly inhibited the mycelial growth of the different strains considerably (with a maximum of 78.15% on the Njo 2 strain) but not completely. According to their sensitivity, the Bia 2 strain showed a higher sensitivity to essential oils than the others while the Njo 2 strain was more aggressive. On the basis of MIC<sub>50</sub> and MIC<sub>90</sub> obtained on the Njo 2 strain, the HET turns out to be the most efficient with respective lower values of (1.73 and 23.34 ml/ml) against (4.76 and 26.03 ml/ml) for the HEC. These EO could thus be exploited as biodegradable antifungal substances, likely to control white rot of bean.展开更多
The test was undertaken to reveal the antifungal activity of extracts from Clerodendrum bungei leaves against Pestalotia and Rhizoctonia solani, the results showed that optimal condition for best antifungal activity o...The test was undertaken to reveal the antifungal activity of extracts from Clerodendrum bungei leaves against Pestalotia and Rhizoctonia solani, the results showed that optimal condition for best antifungal activity of extracts against pestalotia and Rhizoctonia solani are as follows： material-liquid ratio of 1：6,75% ethanol as extracting solvent, reflux at 90℃ for 1.5 h. The substances with good dissolubility in ethanol and water solution such as organic acid, bioflavonoid and alkaloid are main antifungal bioactive substances in Clerodendrun bungei.展开更多
[ Objective] The paper was to screen myxobacteria with antifungal activity, and identify its species. [ Method] 237 myxobacteria were isolated and pu- rified from 200 copies of soil samples collected from 23 provinces...[ Objective] The paper was to screen myxobacteria with antifungal activity, and identify its species. [ Method] 237 myxobacteria were isolated and pu- rified from 200 copies of soil samples collected from 23 provinces in China. The strains were fermented in four different media, and the fermentation products were extracted by methanol to obtain metabolites. With Candida albicans as the model, the secondary metabolites were carried out high-throughput screening. [ Result ] A strain of myxohacteria numbered ZJ2 was obtained after secondary screening, its secondary metabolites had activities against G. albicans. 16S rDNA cloning and sequencing results showed that ZJ2 was Myxococcus fidvus. [ Conclusion ] The secondary metabolites of ZJ2 strain had bioactive substances with significant inhibi- tion effect against the growth of C. albicans, which had potential pharmaceutical research and development value.展开更多
[Objective] The antifungal activity of the extracts from,Atractylodes macracephal Koidz and Pulsatilla chinensis Bunge Regel,against Botrytis cinerea and Alternaria solani were studied under the condition of laborator...[Objective] The antifungal activity of the extracts from,Atractylodes macracephal Koidz and Pulsatilla chinensis Bunge Regel,against Botrytis cinerea and Alternaria solani were studied under the condition of laboratory,in order to develop and utilize these two plants.[Method] The mycelium growth rate test was applied to measure the antifungal activities of extracts against fungi.[Result] the extracts of all the two plants showed strong antifungal activity against the target pathogenic fungi,especially the antifungal activity of the extract from Pulsatilla chinensis Bunge Regel was stronger and more stable.The inhibition rate to the mycelium growth of Botrytis cinerea was 80.25%.At the same concentration,the extract from Atractylodes macracephal Koidz showed little inhibition to Botrytis cinerea and Alternaria solani.The petrolelum ether extract of Atractylodes macracephal Koidz showed stronger antifungal activities and the EC50 was 5.31 mg/ml,and the n-butanol extract of Pulsatilla chinensis Bunge Regel showed stronger antifungal activities and the EC50 was 2.93 mg/ml.[Conclusion] The extracts from Pulsatilla chinensis Bunge Regel showed the stronger antifungal activity against Botrytis cinerea and Alternaria solani.展开更多
5-（4-Cyclopropyl-5-（（3-fluorobenzyl）sulfonyl）-4H-1,2,4-triazol-3-yl）-4-methyl-1,2,3-thiadiazole was synthesized and recrystallized from Et OH. The compound was characterized by ^1H NMR,MS,elemental analysis and ...5-（4-Cyclopropyl-5-（（3-fluorobenzyl）sulfonyl）-4H-1,2,4-triazol-3-yl）-4-methyl-1,2,3-thiadiazole was synthesized and recrystallized from Et OH. The compound was characterized by ^1H NMR,MS,elemental analysis and X-ray diffraction. The structure-active relationship and the antifungal activity based on density functional theory calculation（DFT） and antifungal activities were investigated. The compound crystallizes in the monoclinic space group P121/n1 with a = 8.929（3）,b=12.715（4）,c=15.161（5） A°,β = 106.142（3）o,V = 1653.3（9） A°3,Z = 4 and R = 0.0393 for 3930 observed reflections with I 〉 2σ（I）. Theoretical calculation of the title compound was carried out with B3LYP/6-31G（d,p）. The full geometry optimization was carried out using the 6-31G（d,p） basis set.The frontier orbital energy and atomic net charges were discussed. The observed results of the compound have been compared with theoretical results and the experimental data show good agreement with the calculated values. The compound exhibits good antifungal activity.展开更多
A new coordination compound, [Co（L223）2（H2O）2]·H2pm（1, L223 = 3,4-bis（2-pyridyl）-5-（3-pyridyl）-1,2,4-triazole and H4 pm = pyromellitic acid）, has been synthesized. The structure of complex 1 has been ch...A new coordination compound, [Co（L223）2（H2O）2]·H2pm（1, L223 = 3,4-bis（2-pyridyl）-5-（3-pyridyl）-1,2,4-triazole and H4 pm = pyromellitic acid）, has been synthesized. The structure of complex 1 has been characterized by X-ray single-crystal diffraction, elemental analysis, IR spectrum analysis and thermogravimetric analysis. Single-crystal X-ray diffraction analysis reveals that complex 1 belongs to the triclinic system, space group P1 with a = 10.2470（8）, b = 10.2879（9）, c = 10.2951（11） ？, α = 109.398（2）, β = 97.6590（10）, γ = 95.3260（10）°, V = 1003.60（16） ？3, Z = 1, Dc = 1.565 g/cm^3, μ = 0.508 mm%^-1, Mr = 945.73, F（000） = 485, the final R = 0.0562 and w R = 0.0783 with I 〉 2σ（I）. Two L223 as chelating ligands link one Co（II） ion to form a 0D motif. Furthermore, the 0D motifs are linked into a 2D coordination pattern with hydrogen bonds. In addition, the antifungal effects of the ligand and the complex were evaluated by the disc diffusion method against Colletotrichum gloeosporioides Penz. 1 represents antifungal activity with high levels of inhibitory potency which is larger than the corresponding ligand.展开更多
The title compound 8-chloro-3-（（4-chlorobenzyl）thio）-[1,2,4]triazolo[4,3-a]pyridine was prepared from 1-chloro-4-（chloromethyl）benzene and 8-chloro-[1,2,4]triazolo[4,3-a]pyridine-3（2H）-thione in the presence o...The title compound 8-chloro-3-（（4-chlorobenzyl）thio）-[1,2,4]triazolo[4,3-a]pyridine was prepared from 1-chloro-4-（chloromethyl）benzene and 8-chloro-[1,2,4]triazolo[4,3-a]pyridine-3（2H）-thione in the presence of Na OH, and its structure was determined by X-ray diffraction analysis. The crystal is of triclinic system, space group P1 with a = 6.8264（6）, b = 7.5890（4）, c = 13.0960（7） A, α = 93.447（4）, β = 98.772（6）, γ = 92.615（6）o, V = 668.26（8） A3, Z = 2, the final R = 0.035 and wR = 0.09 for 2259 observed reflections with I 〉 2σ（I）. The preliminary biological test showed that the title compound has activities against Stemphylium lycopersici（Enjoji） Yamamoto, Fusarium oxysporum. sp. cucumebrium, and Botrytis cinerea with inhibitory to be 51.19%, 62.02% and 15.56%, respectively.展开更多
A series of derivatives were synthesized from trichodermin（1） which was an antifungal metabolite produced by Trichoderma taxi sp.nov.Their structures were confirmed by ~1H NMR,MS spectrum.Their antifungal activities...A series of derivatives were synthesized from trichodermin（1） which was an antifungal metabolite produced by Trichoderma taxi sp.nov.Their structures were confirmed by ~1H NMR,MS spectrum.Their antifungal activities were evaluated in vitro.The preliminary structure activity relationships（SAR） results indicated that the double bond,epoxide moiety and ester group were main pharmacophore elements,the stereochemistry of C4 position played a key role as well,and the compounds 1e-1g displayed stronger antifungal activity against Magnaporthe grisea than 1.展开更多
The economic losses and the health hazards of the mycotoxins produced by spoilage fungi are the main concerns of the food industry. The spoilage of bakery products by fungi is more common in countries with a high humi...The economic losses and the health hazards of the mycotoxins produced by spoilage fungi are the main concerns of the food industry. The spoilage of bakery products by fungi is more common in countries with a high humidity and temperature. About 5-10% of food production is spoiled by the growth of yeast and fungi in food materials. Similarly, in Western Europe, the growth of the spoilage fungi of bread is estimated to reach more than 200 million Euros per year. The history conditions of the food can be a major factor in determining any fungal spoilage--for example, stored and processed foods are more sensitive to spoilage when compared with fresh and prepared foods. Lactic acid bacteria isolated from Bulgarian wheat and rye flour were used in the present study to check their antifungal properties against pathogenic yeast and fungi imperfecta using standard disc diffusion method in vitro. A broad spectrum of antifungal activity of the six newly identified as L. plantarum strains e Tsl, Ts2, Ts3,Ts4 and Ts5, and L. helveticus Ts6 was estimated. Our in vitro studies were performed with wheat and rye sourdough, in order to simulate a real product and to assess the bio-protective potential of the tested lactobacilli. The used test-cultures are representatives of carcinogenic, toxigenic, deteriorative and allergenic fungi from the genera .4spergillus and Penicillium. The all tested strains completely suppress the growth of against C. glabrata 72. Strains L. plantarum Tsl and Ts3 completely suppress the growth against S. cerevisae. While, in the sample with L. plantarum strains e Tsl, Ts2, Ts3,Ts4 and Ts5, and L. helveticus Ts6, a retarded and weak growth of A. niger and P. claviforme was observed. However, the spore germination and the colony growth started only on the fifth day of the mould lactobacilli co-cultivation, which also should be considered as a good result. In this study six isolates Tsl,Ts2, Ts3, Ts4, Ts5 and Ts6, from the traditional Bulgarian wheat and rye flour have been identified as L. plantarum and L. helveticus and characterized as cultures with promising antifungal activity. Obtained results from the combined molecular identification （16S rRNA gene sequencing） approach contribute to give new data on the microbial biodiversity of this not well-studied niche. The antifungal activity of our new isolates, identified as L. plantarum and L. helveticus, seems to be a promising advantage of these six strains, suggesting their potential applications in different food technologies. However, more experiments have to be conducted to clarify the nature and the mechanisms of the reported antifungal activity and they are still in progress. The combination of dairy origin and strong inhibitory activity of the lactobacillus strains is a prerequisite for their possible application as starters and/or bioprotective antifungal adjuncts.展开更多
A new lanthanide coordination polymer, [Ho（sba）（H2O）2（DMF）2]？H2O？DMF？Cl （1） based on the versatile ligand H2sba （H2sba = 4,4？-dicarboxybiphenyl sulfone）, was prepared and characterized by single-crystal ...A new lanthanide coordination polymer, [Ho（sba）（H2O）2（DMF）2]？H2O？DMF？Cl （1） based on the versatile ligand H2sba （H2sba = 4,4？-dicarboxybiphenyl sulfone）, was prepared and characterized by single-crystal X-ray diffraction, elemental analysis, IR spectroscopy and thermogravimetric analysis. Single-crystal X-ray diffraction indicates that complex 1 belongs to the triclinic system, space group P with a = 10.6942（6）, b = 11.8452（7）, c = 13.1814（8） ？, α = 94.854（2）, ？ = 96.649（2）, γ = 91.663（2）o, V = 1651.30（17） ？3, Z = 2, Dc = 1.565 g？cm-3, μ = 2.597 mm-1, Mr = 777.98, F（000） = 780, the final R = 0.0446 and wR = 0.1116 with I 〉 2？（I）. In the title complex, the Ho（III） ions exhibit 1D ∞-like double chains. The DMF molecules not only make the structure more stable, but also act as hydrogen bond acceptors making the 1D double chains into a three-dimensional （3D） supramolecular framework. In addition, the antifungal effects of the ligand, metal salt and Ho（III） complex have also been studied by the disc diffusion method against Colletotrichum gloeosporioides Penz. It was found that the antifungal activity of complex 1 was better than the corresponding ligand and the metal salt. Complex 1 has potential applications in the antifungal activity.展开更多
The title compound 2-（（2-fluorobenzyl）thio）-5-（pyridin-4-yl）-1,3,4-oxadiazole（C_（14）H_（10）FN_3OS） was synthesized,and its structure was confirmed by ~1H NMR,MS,elemental analyses and X-ray diffraction. It ...The title compound 2-（（2-fluorobenzyl）thio）-5-（pyridin-4-yl）-1,3,4-oxadiazole（C_（14）H_（10）FN_3OS） was synthesized,and its structure was confirmed by ~1H NMR,MS,elemental analyses and X-ray diffraction. It crystallizes in the monoclinic system,space group P21/n with a = 11.541（16）,b = 8.226（12）,c = 13.683（19） ？,β = 94.872（17）o,V = 1294（3） ？~3,Z = 4 and R = 0.0648 for 2198 observed reflections with I 〉 2σ（I）. The preliminary biological test shows that the title compound has good activity against Pythium ultimum with inhibitory to be 100%.展开更多
The aim of this study was to determine the extraction technique of supercritical fluid carbon dioxide（SF-CO 2） for the essential oil from Inula britannica flowers and its antifungal activities against plant pathogen...The aim of this study was to determine the extraction technique of supercritical fluid carbon dioxide（SF-CO 2） for the essential oil from Inula britannica flowers and its antifungal activities against plant pathogenic fungi for its potential application as botanical fungicide.The effects of factors,including extraction temperature,extraction pressure,SF-CO 2 flow rate,flower powder size,and time on the essential oil yield were studied using the single factor experiment.An orthogonal experiment was conducted to determine the best operating conditions for the maximum extraction oil yield.Adopting the optimum conditions,the maximum yield reached 10.01% at 40°C temperature,30 MPa pressure,60 mesh flower powder size,20 L h-1SF-CO 2 flow rate,and 90 min extraction time.The antifungal activities of I.britannica essential oil using the SF-CO 2 against the most important plant pathogenic fungi were also examined through in vitro and in vivo tests.Sixteen plant pathogenic fungi were inhibited to varying degrees at 1 mg mL-1concentration of the essential oil.The mycelial growth of Gaeumannomyces graminis var.tritici was completely inhibited.The radial growths of Phytophthora capsici and Fusarium monilifome were also inhibited by 83.76 and 64.69%,respectively.In addition,the essential oil can inhibit the spore germination of Fusarium oxysporum f.sp.vasinfectum,Phytophthora capsici,Colletotrichum orbiculare,and Pyricularia grisea,and the corresponding inhibition rates were 98.26,96.54,87.89,and 87.35% respectively.The present study has demonstrated that the essential oil of I.britannica flowers extracted through the SF-CO 2 technique is one potential and promising antifungal agent that can be used as botanical fungicide to protect crops.展开更多
The polar and nonpolar extracts of Colpomenia sinuosa, Padina pavonia, Cystoseira barbata and Sargassum vulgare collected during spring, summer and autumn were evaluated for their antifungal activities. The phytochem...The polar and nonpolar extracts of Colpomenia sinuosa, Padina pavonia, Cystoseira barbata and Sargassum vulgare collected during spring, summer and autumn were evaluated for their antifungal activities. The phytochemicals of unexplored seaweeds were analyzed by gas chromatography and mass spectrometric （GC/MS）. The algal extracts were tested for their antifungal activities against Aspergillus niger, A. flavus, Penicillium parasiticus, Candida utilis and Fusarium solani. Phytochemicals were extracted from the four seaweeds with various solvents including methanol, ethanol, acetone, chloroform and dimethyl ether. Among the various extracts, methanolic extract showed the highest inhibition activity on all fungal species. Seasonal variation in antifungal activity was studied, while methanol extracts showed the best antifungal activity in spring. Cystoseira barbata was the most effective seaweed, having anatifungal activity throughout the whole year. The UV-Vis phytochemical procedure and GC-MS analysis of the methanol extracts from tested species indicated the existence of different constituents. In conclusions, the compounds with antifungal activity were identified as indoles, terpenes, acetogenins, phenols, and volatile halogenated hydrocarbons.展开更多
In this study, three hymexazol-linked chitosan derivatives （HML-CS） were synthesized and their structures confirmed by Fourier transform infrared and elemental analysis. Linkage ratios were measured by high performa...In this study, three hymexazol-linked chitosan derivatives （HML-CS） were synthesized and their structures confirmed by Fourier transform infrared and elemental analysis. Linkage ratios were measured by high performance liquid chromatography. The derivatives＇ antifungal activity against the plant pathogenic fimgi Rhizoctonia solani CGMCC 3.28 and Gibberella zeae CGMCC 3.42 were investigated at concentrations of 100, 200, and 400 mg/L. These HML-CS derivatives exhibited stronger antifungal activity than CS alone. HML-CS-1 showed the best antifizngal activity against G. zeae, whose antifimgal index was 65.9% at 400 mg/L, and also showed the best antifungal activity against R. solani, whose antifimgal index was 52.7% at 400 mg/L. This conjugation of CS and HML suggested the presence of synergistic effects between the moieties and indicated that these derivatives possessed great potential as novel fungicides and require further research for the development of applications in crop protection.展开更多
A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized fr...A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry（MS） and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.展开更多
In this paper nine New Mannich bases of 6-fluoro-thiochromanone and eight new 3-substituted-6.8-dichloro thiochromanones were synthesized and their structures were confirmed by IR, H-1-NMR and elementary analysis. Mos...In this paper nine New Mannich bases of 6-fluoro-thiochromanone and eight new 3-substituted-6.8-dichloro thiochromanones were synthesized and their structures were confirmed by IR, H-1-NMR and elementary analysis. Most of these compounds showed excellent antifungal activity.展开更多
Objective: To study the effect of fluconzole derivatives from a side chain containing 4-substituted acyl piperazin-1-yl on antifungal activity. Methods: Fourteen title compounds were synthesized and confirmed by the e...Objective: To study the effect of fluconzole derivatives from a side chain containing 4-substituted acyl piperazin-1-yl on antifungal activity. Methods: Fourteen title compounds were synthesized and confirmed by the elementary analysis, 1HNMR and IR spectra. Five deep fungal strains and 3 shallow fungal strains were chosen as the experimental strains.Minimum inhibitory concentrations(MICs) of all title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards (NCCLS) using RPMI 1640 test medium. Results: Among the 14 title compounds, 12 were first reported. The results of preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. The activity of 4 compounds were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro(MIC 80 value≤0.125 μg/ml). Conclusion: Introduction of a side chain containing 4-substituted acyl piperazin-1-yl into the main part of fluconazole has important influence on antifungal activities of title compounds.展开更多
Antifungal activity and mode of action of nine essential oils(EOs)against S.cerevisiae cells were examined.Antifungal effects of commercial lemon peel,orange peel,tea tree,turpentine,rosemary,peppermint,thyme,oregano ...Antifungal activity and mode of action of nine essential oils(EOs)against S.cerevisiae cells were examined.Antifungal effects of commercial lemon peel,orange peel,tea tree,turpentine,rosemary,peppermint,thyme,oregano and clove oils were determined through Minimum Inhibitory Concentration(MIC),Minimum Fungicidal Concentration(MFC)and inhibition zone measurements.The most effective oil was turpentine oil.Orange peel,thyme and oregano oils were also effective,according to MIC and MFC.Inhibition zone measurements,also revealed oregano,orange peel,thyme,turpentine and clove oils as most efficient ones.Later,membrane damage of yeast cells was studied by measuring the extracellular pH and conductivity in a concentration dependent manner.Orange peel,turpentine,thyme and oregano oils caused a clear increase in extracellular pH of glucose-induced yeast cells and induced an increase in extracellular conductivity.These results point to the deterioration of yeast cell membrane integrity upon exposure to EOs.Since these oils can be used as food preservatives and pharmaceutical agents,it is very important to understand their mode of action and their main target sites in the cell.Thus this research not only opens new perspectives to understand antifungal activity mechanisms of EOs,but also help widen their use.展开更多
Wood is mainly made up of cellulose, hemicelluloses, lignin polymers and other organic and inorganic substances, making it susceptible to deteriorate by various biological agents. Tectona grandis L.f. (Teak) is a timb...Wood is mainly made up of cellulose, hemicelluloses, lignin polymers and other organic and inorganic substances, making it susceptible to deteriorate by various biological agents. Tectona grandis L.f. (Teak) is a timberspecies with high resistance to biological deterioration, valued for its durability, beauty, and mechanical resistance.The purpose of this work was to evaluate the antifungal activity of crude extracts from teak on various fungi thatcause wood deterioration. For this, Teak heartwood was obtained, then fragmented and pulverized until obtaininga flour which was used for compounds extraction using the Soxhlet technique coupled to a rotary evaporatorthrough solvents of increasing polarity (hexane, dichloromethane, tetrahydrofuran, and acetone). The extractsobtained were tested against fungal organisms collected in the field, and the LC50 was determined using teak crudeextracts on Artemia salina as a biological model. The results obtained showed that a high flour yield was obtainedwith hexane (0.951 g), followed by tetrahydrofuran (0.446 g), dichloromethane (0.348 g), and acetone (0.152 g). Byusing nine fungal organisms that predominantly correspond to the genus Aspergillus, the extractable compoundswere tested, inhibiting 25% of mycelial growth with tetrahydrofuran (T. versicolor), and 40.9% with dichloromethane(G. trabeum). Likewise, the biological model of A. salina showed an LC50 of 84.9 μg/mL with hexane, 43.3 μg/mLwith dichloromethane, 59.6 μg/mL with tetrahydrofuran, and 54.7 μg/mL with acetone. For this reason, it is concluded that Teak wood contains many extractable compounds in relation to its weight, besides having antimicrobialactivity when extracted through polar compounds such as dichloromethane and tetrahydrofuran.展开更多
基金financially supported by the National Natural Science Foundation of China(Grant No.51678120).
文摘Dihydrochelerythrine(DHCHE)is an isoquinoline compound,which has distinct antifungal activity and can induce apoptosis.The antifungal activity of DHCHE against five rice pathogenic fungi was studied in vitro.At the concentration of 7.5 mg/L,DHCHE exhibited the highest efficacy among tested compounds in inhibiting mycelium growth,with an inhibition rate of 68.8%in Ustilaginoidea virens,which was approximately 2.4 times of that of validamycin(28.7%).After exposure to DHCHE,transmission electron micrographs revealed spores showed incomplete organelles,malformed cell walls and nuclear membranes,as well as irregular lipid spheres.Reactive oxygen species accumulation in treated spores was markedly higher than that in control spores.DHCHE induced cell damage increased in a dose-dependent manner,as indicated by the decrease in mitochondrial membrane potential and initiation of apoptosis.The differences of expression levels of Fip1,ACP1,PMS2 and COX13 that are important for oxidative phosphorylation and mismatch repair pathway were significant,which may be some of the reasons for the induction of apoptosis in DHCHE-treated U.virens.The protein levels of Fip1,ACP1,PMS2 and COX13 agreed with protein fold change ratio from parallel reaction monitoring Gene Ontology terms and Kyoto Encyclopedia of Genes and Genomes pathway of differentially expressed proteins were further analyzed.These findings will help to elucidate the mechanisms associated with antifungal and pro-apoptotic effects of DHCHE on U.virens,thereby aiding the potential development of novel pesticides.
文摘The present work was aimed to the study of the antifungal activity of essential oils of two aromatic plants against three strains of Sclerotinia sclerotiorum responsible for white rot of bean. The two essential oils (EO) of the studied plants: Thymus vulgaris (HET) and Cymbopogon citratrus (HEC), used at different concentrations: C1 (0.75 ml/ml), C2 (1.5 ml/ml) and C3 (3 ml/ml) presented significant inhibitory activities on the three tested fungal strains namely Bia 1, Bia 2, and Njo 2. Two control treatments (T-: containing no antifungal substance and T+: synthetic fungicide) were also used. The antifungal activity here is related to the inhibition of mycelial growth especially with high concentrations of essential oils. Thus, against S. sclerotiorum, HET showed the highest activity comparable to that of T+ (100% inhibition) at all concentrations on the Bia 1 and Bia 2 strains and at concentration C3 on the Njo 2 strain compared to that of HEC, which certainly inhibited the mycelial growth of the different strains considerably (with a maximum of 78.15% on the Njo 2 strain) but not completely. According to their sensitivity, the Bia 2 strain showed a higher sensitivity to essential oils than the others while the Njo 2 strain was more aggressive. On the basis of MIC<sub>50</sub> and MIC<sub>90</sub> obtained on the Njo 2 strain, the HET turns out to be the most efficient with respective lower values of (1.73 and 23.34 ml/ml) against (4.76 and 26.03 ml/ml) for the HEC. These EO could thus be exploited as biodegradable antifungal substances, likely to control white rot of bean.
基金Supported by Doctor Startup Foundation of Yibin College(2005B02)~~
文摘The test was undertaken to reveal the antifungal activity of extracts from Clerodendrum bungei leaves against Pestalotia and Rhizoctonia solani, the results showed that optimal condition for best antifungal activity of extracts against pestalotia and Rhizoctonia solani are as follows： material-liquid ratio of 1：6,75% ethanol as extracting solvent, reflux at 90℃ for 1.5 h. The substances with good dissolubility in ethanol and water solution such as organic acid, bioflavonoid and alkaloid are main antifungal bioactive substances in Clerodendrun bungei.
基金Supported by Agriculture Public Relation Projects of Science and Technology Department of Shaanxi Province"Utilization of Specific Biological Resources and New Product Development in Southern Shaanxi"(2009K01-25)Industrial Pilot Projects of Education Department of Shaanxi Province"Industrializa-tion of Additives of Green Pollution-free Microbial Fermentation Feed"(2010JC22)~~
文摘[ Objective] The paper was to screen myxobacteria with antifungal activity, and identify its species. [ Method] 237 myxobacteria were isolated and pu- rified from 200 copies of soil samples collected from 23 provinces in China. The strains were fermented in four different media, and the fermentation products were extracted by methanol to obtain metabolites. With Candida albicans as the model, the secondary metabolites were carried out high-throughput screening. [ Result ] A strain of myxohacteria numbered ZJ2 was obtained after secondary screening, its secondary metabolites had activities against G. albicans. 16S rDNA cloning and sequencing results showed that ZJ2 was Myxococcus fidvus. [ Conclusion ] The secondary metabolites of ZJ2 strain had bioactive substances with significant inhibi- tion effect against the growth of C. albicans, which had potential pharmaceutical research and development value.
基金Supported by Talent Introduction Grantin Anhui Science and Technology University(ZRC2007102)Outstanding Young Talets Project of Anhui Provincal Universities(2009SQRZ11)~~
文摘[Objective] The antifungal activity of the extracts from,Atractylodes macracephal Koidz and Pulsatilla chinensis Bunge Regel,against Botrytis cinerea and Alternaria solani were studied under the condition of laboratory,in order to develop and utilize these two plants.[Method] The mycelium growth rate test was applied to measure the antifungal activities of extracts against fungi.[Result] the extracts of all the two plants showed strong antifungal activity against the target pathogenic fungi,especially the antifungal activity of the extract from Pulsatilla chinensis Bunge Regel was stronger and more stable.The inhibition rate to the mycelium growth of Botrytis cinerea was 80.25%.At the same concentration,the extract from Atractylodes macracephal Koidz showed little inhibition to Botrytis cinerea and Alternaria solani.The petrolelum ether extract of Atractylodes macracephal Koidz showed stronger antifungal activities and the EC50 was 5.31 mg/ml,and the n-butanol extract of Pulsatilla chinensis Bunge Regel showed stronger antifungal activities and the EC50 was 2.93 mg/ml.[Conclusion] The extracts from Pulsatilla chinensis Bunge Regel showed the stronger antifungal activity against Botrytis cinerea and Alternaria solani.
基金funded by National Natural Science Foundation of China(No.21002090)the National Key Technologies R&D Program(2011BAE06B03-01)
文摘5-（4-Cyclopropyl-5-（（3-fluorobenzyl）sulfonyl）-4H-1,2,4-triazol-3-yl）-4-methyl-1,2,3-thiadiazole was synthesized and recrystallized from Et OH. The compound was characterized by ^1H NMR,MS,elemental analysis and X-ray diffraction. The structure-active relationship and the antifungal activity based on density functional theory calculation（DFT） and antifungal activities were investigated. The compound crystallizes in the monoclinic space group P121/n1 with a = 8.929（3）,b=12.715（4）,c=15.161（5） A°,β = 106.142（3）o,V = 1653.3（9） A°3,Z = 4 and R = 0.0393 for 3930 observed reflections with I 〉 2σ（I）. Theoretical calculation of the title compound was carried out with B3LYP/6-31G（d,p）. The full geometry optimization was carried out using the 6-31G（d,p） basis set.The frontier orbital energy and atomic net charges were discussed. The observed results of the compound have been compared with theoretical results and the experimental data show good agreement with the calculated values. The compound exhibits good antifungal activity.
基金Supported by the Natural Science Foundation of Ningxia(No.NZ15015)
文摘A new coordination compound, [Co（L223）2（H2O）2]·H2pm（1, L223 = 3,4-bis（2-pyridyl）-5-（3-pyridyl）-1,2,4-triazole and H4 pm = pyromellitic acid）, has been synthesized. The structure of complex 1 has been characterized by X-ray single-crystal diffraction, elemental analysis, IR spectrum analysis and thermogravimetric analysis. Single-crystal X-ray diffraction analysis reveals that complex 1 belongs to the triclinic system, space group P1 with a = 10.2470（8）, b = 10.2879（9）, c = 10.2951（11） ？, α = 109.398（2）, β = 97.6590（10）, γ = 95.3260（10）°, V = 1003.60（16） ？3, Z = 1, Dc = 1.565 g/cm^3, μ = 0.508 mm%^-1, Mr = 945.73, F（000） = 485, the final R = 0.0562 and w R = 0.0783 with I 〉 2σ（I）. Two L223 as chelating ligands link one Co（II） ion to form a 0D motif. Furthermore, the 0D motifs are linked into a 2D coordination pattern with hydrogen bonds. In addition, the antifungal effects of the ligand and the complex were evaluated by the disc diffusion method against Colletotrichum gloeosporioides Penz. 1 represents antifungal activity with high levels of inhibitory potency which is larger than the corresponding ligand.
基金funded by the National Natural Science Foundation of China(No.21002090)the Natural Science Foundation of Zhejiang Province(No.LY16C140007)the public program of Science and Technology of Zhejiang Province(2014C31127,2013C32SA700134)
文摘The title compound 8-chloro-3-（（4-chlorobenzyl）thio）-[1,2,4]triazolo[4,3-a]pyridine was prepared from 1-chloro-4-（chloromethyl）benzene and 8-chloro-[1,2,4]triazolo[4,3-a]pyridine-3（2H）-thione in the presence of Na OH, and its structure was determined by X-ray diffraction analysis. The crystal is of triclinic system, space group P1 with a = 6.8264（6）, b = 7.5890（4）, c = 13.0960（7） A, α = 93.447（4）, β = 98.772（6）, γ = 92.615（6）o, V = 668.26（8） A3, Z = 2, the final R = 0.035 and wR = 0.09 for 2259 observed reflections with I 〉 2σ（I）. The preliminary biological test showed that the title compound has activities against Stemphylium lycopersici（Enjoji） Yamamoto, Fusarium oxysporum. sp. cucumebrium, and Botrytis cinerea with inhibitory to be 51.19%, 62.02% and 15.56%, respectively.
基金supported by National Natural Science Foundation of China(No.30700532)the Science and Technology Project of Zhejiang province(No.2008C02007-3)
文摘A series of derivatives were synthesized from trichodermin（1） which was an antifungal metabolite produced by Trichoderma taxi sp.nov.Their structures were confirmed by ~1H NMR,MS spectrum.Their antifungal activities were evaluated in vitro.The preliminary structure activity relationships（SAR） results indicated that the double bond,epoxide moiety and ester group were main pharmacophore elements,the stereochemistry of C4 position played a key role as well,and the compounds 1e-1g displayed stronger antifungal activity against Magnaporthe grisea than 1.
文摘The economic losses and the health hazards of the mycotoxins produced by spoilage fungi are the main concerns of the food industry. The spoilage of bakery products by fungi is more common in countries with a high humidity and temperature. About 5-10% of food production is spoiled by the growth of yeast and fungi in food materials. Similarly, in Western Europe, the growth of the spoilage fungi of bread is estimated to reach more than 200 million Euros per year. The history conditions of the food can be a major factor in determining any fungal spoilage--for example, stored and processed foods are more sensitive to spoilage when compared with fresh and prepared foods. Lactic acid bacteria isolated from Bulgarian wheat and rye flour were used in the present study to check their antifungal properties against pathogenic yeast and fungi imperfecta using standard disc diffusion method in vitro. A broad spectrum of antifungal activity of the six newly identified as L. plantarum strains e Tsl, Ts2, Ts3,Ts4 and Ts5, and L. helveticus Ts6 was estimated. Our in vitro studies were performed with wheat and rye sourdough, in order to simulate a real product and to assess the bio-protective potential of the tested lactobacilli. The used test-cultures are representatives of carcinogenic, toxigenic, deteriorative and allergenic fungi from the genera .4spergillus and Penicillium. The all tested strains completely suppress the growth of against C. glabrata 72. Strains L. plantarum Tsl and Ts3 completely suppress the growth against S. cerevisae. While, in the sample with L. plantarum strains e Tsl, Ts2, Ts3,Ts4 and Ts5, and L. helveticus Ts6, a retarded and weak growth of A. niger and P. claviforme was observed. However, the spore germination and the colony growth started only on the fifth day of the mould lactobacilli co-cultivation, which also should be considered as a good result. In this study six isolates Tsl,Ts2, Ts3, Ts4, Ts5 and Ts6, from the traditional Bulgarian wheat and rye flour have been identified as L. plantarum and L. helveticus and characterized as cultures with promising antifungal activity. Obtained results from the combined molecular identification （16S rRNA gene sequencing） approach contribute to give new data on the microbial biodiversity of this not well-studied niche. The antifungal activity of our new isolates, identified as L. plantarum and L. helveticus, seems to be a promising advantage of these six strains, suggesting their potential applications in different food technologies. However, more experiments have to be conducted to clarify the nature and the mechanisms of the reported antifungal activity and they are still in progress. The combination of dairy origin and strong inhibitory activity of the lactobacillus strains is a prerequisite for their possible application as starters and/or bioprotective antifungal adjuncts.
基金Supported by the Natural Science Foundation of Ningxia Province(No.NZ15006)
文摘A new lanthanide coordination polymer, [Ho（sba）（H2O）2（DMF）2]？H2O？DMF？Cl （1） based on the versatile ligand H2sba （H2sba = 4,4？-dicarboxybiphenyl sulfone）, was prepared and characterized by single-crystal X-ray diffraction, elemental analysis, IR spectroscopy and thermogravimetric analysis. Single-crystal X-ray diffraction indicates that complex 1 belongs to the triclinic system, space group P with a = 10.6942（6）, b = 11.8452（7）, c = 13.1814（8） ？, α = 94.854（2）, ？ = 96.649（2）, γ = 91.663（2）o, V = 1651.30（17） ？3, Z = 2, Dc = 1.565 g？cm-3, μ = 2.597 mm-1, Mr = 777.98, F（000） = 780, the final R = 0.0446 and wR = 0.1116 with I 〉 2？（I）. In the title complex, the Ho（III） ions exhibit 1D ∞-like double chains. The DMF molecules not only make the structure more stable, but also act as hydrogen bond acceptors making the 1D double chains into a three-dimensional （3D） supramolecular framework. In addition, the antifungal effects of the ligand, metal salt and Ho（III） complex have also been studied by the disc diffusion method against Colletotrichum gloeosporioides Penz. It was found that the antifungal activity of complex 1 was better than the corresponding ligand and the metal salt. Complex 1 has potential applications in the antifungal activity.
基金funded by the Natural Science Foundation of Zhejiang Province(No.LY16C140007)the program of Science and Technology of Jiangsu Province(BY2014108-14)
文摘The title compound 2-（（2-fluorobenzyl）thio）-5-（pyridin-4-yl）-1,3,4-oxadiazole（C_（14）H_（10）FN_3OS） was synthesized,and its structure was confirmed by ~1H NMR,MS,elemental analyses and X-ray diffraction. It crystallizes in the monoclinic system,space group P21/n with a = 11.541（16）,b = 8.226（12）,c = 13.683（19） ？,β = 94.872（17）o,V = 1294（3） ？~3,Z = 4 and R = 0.0648 for 2198 observed reflections with I 〉 2σ（I）. The preliminary biological test shows that the title compound has good activity against Pythium ultimum with inhibitory to be 100%.
基金supported by the Scientific and Technological Key Project of Henan Province, China (082102350006 and 102102310242)the College Young Teachers Projects of Henan Province, China (2010GGJS046)
文摘The aim of this study was to determine the extraction technique of supercritical fluid carbon dioxide（SF-CO 2） for the essential oil from Inula britannica flowers and its antifungal activities against plant pathogenic fungi for its potential application as botanical fungicide.The effects of factors,including extraction temperature,extraction pressure,SF-CO 2 flow rate,flower powder size,and time on the essential oil yield were studied using the single factor experiment.An orthogonal experiment was conducted to determine the best operating conditions for the maximum extraction oil yield.Adopting the optimum conditions,the maximum yield reached 10.01% at 40°C temperature,30 MPa pressure,60 mesh flower powder size,20 L h-1SF-CO 2 flow rate,and 90 min extraction time.The antifungal activities of I.britannica essential oil using the SF-CO 2 against the most important plant pathogenic fungi were also examined through in vitro and in vivo tests.Sixteen plant pathogenic fungi were inhibited to varying degrees at 1 mg mL-1concentration of the essential oil.The mycelial growth of Gaeumannomyces graminis var.tritici was completely inhibited.The radial growths of Phytophthora capsici and Fusarium monilifome were also inhibited by 83.76 and 64.69%,respectively.In addition,the essential oil can inhibit the spore germination of Fusarium oxysporum f.sp.vasinfectum,Phytophthora capsici,Colletotrichum orbiculare,and Pyricularia grisea,and the corresponding inhibition rates were 98.26,96.54,87.89,and 87.35% respectively.The present study has demonstrated that the essential oil of I.britannica flowers extracted through the SF-CO 2 technique is one potential and promising antifungal agent that can be used as botanical fungicide to protect crops.
文摘The polar and nonpolar extracts of Colpomenia sinuosa, Padina pavonia, Cystoseira barbata and Sargassum vulgare collected during spring, summer and autumn were evaluated for their antifungal activities. The phytochemicals of unexplored seaweeds were analyzed by gas chromatography and mass spectrometric （GC/MS）. The algal extracts were tested for their antifungal activities against Aspergillus niger, A. flavus, Penicillium parasiticus, Candida utilis and Fusarium solani. Phytochemicals were extracted from the four seaweeds with various solvents including methanol, ethanol, acetone, chloroform and dimethyl ether. Among the various extracts, methanolic extract showed the highest inhibition activity on all fungal species. Seasonal variation in antifungal activity was studied, while methanol extracts showed the best antifungal activity in spring. Cystoseira barbata was the most effective seaweed, having anatifungal activity throughout the whole year. The UV-Vis phytochemical procedure and GC-MS analysis of the methanol extracts from tested species indicated the existence of different constituents. In conclusions, the compounds with antifungal activity were identified as indoles, terpenes, acetogenins, phenols, and volatile halogenated hydrocarbons.
基金Supported by the National Natural Science Foundation of China(No.41306071)the Public Science and Technology Research Funds Projects of Ocean(No.201305016-2)the Science and Technology Development Program of Shandong Province(No.2012GHY11530)
文摘In this study, three hymexazol-linked chitosan derivatives （HML-CS） were synthesized and their structures confirmed by Fourier transform infrared and elemental analysis. Linkage ratios were measured by high performance liquid chromatography. The derivatives＇ antifungal activity against the plant pathogenic fimgi Rhizoctonia solani CGMCC 3.28 and Gibberella zeae CGMCC 3.42 were investigated at concentrations of 100, 200, and 400 mg/L. These HML-CS derivatives exhibited stronger antifungal activity than CS alone. HML-CS-1 showed the best antifizngal activity against G. zeae, whose antifimgal index was 65.9% at 400 mg/L, and also showed the best antifungal activity against R. solani, whose antifimgal index was 52.7% at 400 mg/L. This conjugation of CS and HML suggested the presence of synergistic effects between the moieties and indicated that these derivatives possessed great potential as novel fungicides and require further research for the development of applications in crop protection.
基金Supported by the National Science and Technology Major Projects of China(No.2009ZX09301-012)
文摘A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry（MS） and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.
文摘In this paper nine New Mannich bases of 6-fluoro-thiochromanone and eight new 3-substituted-6.8-dichloro thiochromanones were synthesized and their structures were confirmed by IR, H-1-NMR and elementary analysis. Most of these compounds showed excellent antifungal activity.
文摘Objective: To study the effect of fluconzole derivatives from a side chain containing 4-substituted acyl piperazin-1-yl on antifungal activity. Methods: Fourteen title compounds were synthesized and confirmed by the elementary analysis, 1HNMR and IR spectra. Five deep fungal strains and 3 shallow fungal strains were chosen as the experimental strains.Minimum inhibitory concentrations(MICs) of all title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards (NCCLS) using RPMI 1640 test medium. Results: Among the 14 title compounds, 12 were first reported. The results of preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. The activity of 4 compounds were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro(MIC 80 value≤0.125 μg/ml). Conclusion: Introduction of a side chain containing 4-substituted acyl piperazin-1-yl into the main part of fluconazole has important influence on antifungal activities of title compounds.
文摘Antifungal activity and mode of action of nine essential oils(EOs)against S.cerevisiae cells were examined.Antifungal effects of commercial lemon peel,orange peel,tea tree,turpentine,rosemary,peppermint,thyme,oregano and clove oils were determined through Minimum Inhibitory Concentration(MIC),Minimum Fungicidal Concentration(MFC)and inhibition zone measurements.The most effective oil was turpentine oil.Orange peel,thyme and oregano oils were also effective,according to MIC and MFC.Inhibition zone measurements,also revealed oregano,orange peel,thyme,turpentine and clove oils as most efficient ones.Later,membrane damage of yeast cells was studied by measuring the extracellular pH and conductivity in a concentration dependent manner.Orange peel,turpentine,thyme and oregano oils caused a clear increase in extracellular pH of glucose-induced yeast cells and induced an increase in extracellular conductivity.These results point to the deterioration of yeast cell membrane integrity upon exposure to EOs.Since these oils can be used as food preservatives and pharmaceutical agents,it is very important to understand their mode of action and their main target sites in the cell.Thus this research not only opens new perspectives to understand antifungal activity mechanisms of EOs,but also help widen their use.
基金Thanks to CONACYT for the scholarship granted(2019-000002-01NACF-13536).
文摘Wood is mainly made up of cellulose, hemicelluloses, lignin polymers and other organic and inorganic substances, making it susceptible to deteriorate by various biological agents. Tectona grandis L.f. (Teak) is a timberspecies with high resistance to biological deterioration, valued for its durability, beauty, and mechanical resistance.The purpose of this work was to evaluate the antifungal activity of crude extracts from teak on various fungi thatcause wood deterioration. For this, Teak heartwood was obtained, then fragmented and pulverized until obtaininga flour which was used for compounds extraction using the Soxhlet technique coupled to a rotary evaporatorthrough solvents of increasing polarity (hexane, dichloromethane, tetrahydrofuran, and acetone). The extractsobtained were tested against fungal organisms collected in the field, and the LC50 was determined using teak crudeextracts on Artemia salina as a biological model. The results obtained showed that a high flour yield was obtainedwith hexane (0.951 g), followed by tetrahydrofuran (0.446 g), dichloromethane (0.348 g), and acetone (0.152 g). Byusing nine fungal organisms that predominantly correspond to the genus Aspergillus, the extractable compoundswere tested, inhibiting 25% of mycelial growth with tetrahydrofuran (T. versicolor), and 40.9% with dichloromethane(G. trabeum). Likewise, the biological model of A. salina showed an LC50 of 84.9 μg/mL with hexane, 43.3 μg/mLwith dichloromethane, 59.6 μg/mL with tetrahydrofuran, and 54.7 μg/mL with acetone. For this reason, it is concluded that Teak wood contains many extractable compounds in relation to its weight, besides having antimicrobialactivity when extracted through polar compounds such as dichloromethane and tetrahydrofuran.
