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
We developed a molecular marker for MAS of mungbean resistant varieties against CLS from the consensus sequence(MB-CLsRG)of identified RGAs(MB-ClsRCaG1 and MB-ClsRCaG2).The MB-CLsRG sequence-specific primer pair was u...We developed a molecular marker for MAS of mungbean resistant varieties against CLS from the consensus sequence(MB-CLsRG)of identified RGAs(MB-ClsRCaG1 and MB-ClsRCaG2).The MB-CLsRG sequence-specific primer pair was used to screen Cercospora leaf spot(CLS)resistant varieties of mungbean in genomic analysis that showed congruency with phenotypic screening.Validation of molecular marker linkage with CLS resistance was performed using rtPCR in transcriptomic analysis.The sequenced PCR products showed 100%homology with MB-CLsRG sequence and putative disease resistance proteins that confirmed the linkage of molecular marker with CLS resistance in mungbean.The antifungal potential of MB-CLsRG gene encoding protein was assessed.The MB-CLsRG gene sequence was cloned in the E.coli expression vector for recombinant protein production.The recombinant protein was then investigated for its in vitro antifungal potential against Cercospora canescens.The in vitro investigation showed strong antifungal activity of recombinant protein as it restricted the growth of fungal mycelial mass.The results validated the linkage of developed marker with CLS-resistant mungbean varieties;therefore,it can be used to screen resistant varieties from a large population in MAS.Moreover,the recombinant protein of the MB-CLsRG gene sequence revealed antifungal potential,which proved the gene sequence could be suitable to use in transgenic plants technology to develop fungal-resistant transgenic crops.展开更多
Puccinia triticina(Pt), as the causal agent of wheat leaf rust, employs a plethora of effector proteins to modulate wheat immunity for successful colonization. Understanding the molecular mechanisms underlying Pt effe...Puccinia triticina(Pt), as the causal agent of wheat leaf rust, employs a plethora of effector proteins to modulate wheat immunity for successful colonization. Understanding the molecular mechanisms underlying Pt effector-mediated wheat susceptibility remains largely unexplored. In this study, an effector Pt_21 was identified to interact with the apoplast-localized wheat thaumatin-like protein TaTLP1 using a yeast two-hybrid assay and the Pt_21-TaTLP1 interaction was characterized. The interaction between Pt_21 and TaTLP1 was validated by in vivo co-immunoprecipitation assay. A TaTLP1 variant,TaTLP1C71A, that was identified by the site-directed mutagenesis failed to interact with Pt_21. Pt_21was able to suppress Bax-mediated cell death in leaves of Nicotiana benthamiana and inhibit TaTLP1-mediated antifungal activity. Furthermore, infiltration of recombinant protein Pt_21 into leaves of transgenic wheat line overexpressing TaTLP1 enhanced the disease development of leaf rust compared to that in wild-type leaves. These findings demonstrate that Pt_21 suppresses host defense response by directly targeting wheat TaTLP1 and inhibiting its antifungal activity, which broadens our understanding of the molecular mechanisms underlying Pt effector-mediated susceptibility in wheat.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 crystallizes...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
A new coordination compound, [Co(L^(223))_2(H_2O)_2]·H_2pm(1, L^(223) = 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(L^(223))_2(H_2O)_2]·H_2pm(1, L^(223) = 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
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,1H-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,1H-NMR and elementary analysis. Most of these compounds showed excellent antifungal activity.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
Background: Nigeria is plagued with a variety of socioeconomic problems mainly poverty, poor access to quality healthcare and poor hygienic conditions resulting in the myriad of fungal infections that are frequently e...Background: Nigeria is plagued with a variety of socioeconomic problems mainly poverty, poor access to quality healthcare and poor hygienic conditions resulting in the myriad of fungal infections that are frequently encountered in clinical practice. Method: The antifungal activity of aqueous, methanolic, propanolic and benzyl alcohol extracts of Capsicum annuum fruits and seeds, Capsicum chinense fruits and seeds, Aframomum melegueta pods and seeds, Allium sativum bulbs, Allium cepa bulbs and Zingiber officinale rhizomes on Candida albicans (yeast), Aspergillus niger (mould) and Trichophyton rubrum (dermatophyte) were evaluated by the agar well diffusion method. The aqueous and alcoholic filtered plant extracts were obtained by maceration, and also methanolic extracts were also obtained by Soxhlet extraction. The results were obtained by measuring the inhibition zone diameter in millimeters and were presented by subtracting the activity of the control. Results: Aqueous and methanolic extracts of Allium sativum gave the highest inhibition of the growth of Candida albicans (22 mm), followed closely by its propanolic extract with inhibition zone diameter of 15 mm, and also, propanolic extracts of Aframomum melegueta and Allium cepa gave inhibition zone diameters of 12 mm each. Soxhlet methanolic extract of Allium sativum had the highest inhibition of the growth of Aspergillus niger with an inhibition zone diameter of 25 mm, followed closely by Zingiber officinale Soxhlet methanolic extract with an inhibition zone diameter of 22 mm, also, the propanolic extract of Allium sativum gave an inhibition zone diameter of 21 mm, whereas Soxhlet methanolic extracts of Aframomum melegueta and Allium cepa gave an inhibition zone diameter of 19 mm each. The highest activity against Trichophyton rubrum was obtained with the Soxhlet methanolic extract of Allium sativum (39 mm), followed closely by its propanolic extract with an inhibition zone diameter of 27 mm. An inhibition zone diameter of 22 mm was recorded with the benzyl alcohol extract of Allium cepa, 22 mm with the Soxhlet methanolic extract of Aframomum melegueta and 19mm with the aqueous extract of Capsicum chinense seeds. Conclusion: The in-vitro inhibitory effects of these spice extracts indicated that the test spices could serve as potential candidates for developing new systemic and topical antifungal drugs against the wide range of pathogenic fungal strains, and they could also serve as natural prophylaxis against the fungal infections.展开更多
Microorganism resistance to the existing products is yet another difficulty that agriculturalists have to deal with. In this context, the search for new agricultural products that can fight phytopathogens has become i...Microorganism resistance to the existing products is yet another difficulty that agriculturalists have to deal with. In this context, the search for new agricultural products that can fight phytopathogens has become increasingly important. Plants have played an important role in this process, because they can serve as a source of new compounds for drug discovery. Plants belonging to the genus Pinus produce an oleoresin that protects the plant against herbivores and pathogens. With a view to developing products that can combat fungal pathogens without harming the environment, this work aimed to evaluate the antifungal activity of the oleoresins and fractions of Pinus elliottii Engelm and Pinus tropicalis against phytopathogens. The methodology based on NCCLS M38-A standards aided antifungal activity assessment. The microdilution method helped to determine the Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC). The oleoresins of P. elliottii and P. tropicalis afforded the most significant results—they displayed fungicidal activity against all the tested species. MIC values were promising, especially the MIC of the oleoresin of P. elliottii against S. rolfsii (1.95 μg·mL-1). The MIC values of the oleoresins of P. elliottii and P. tropicalis ranged from 1.95 to 1000 μg·mL-1 and from 31.25 to 250 μg·mL-1, respectively. Fraction PT2 of P. tropicalis furnished the best results among all the assayed fractions: MIC values lay between 125 and 500 μg·mL-11. In conclusion, the oleoresin of P. tropicalis is a promising source of new antifungal agents for application in the treatment of phytopathogenic infections.展开更多
Objective:To evaluate the in vitro antifungal activity of Aegle marmelos leaf extracts and fractions on the clinical isolates of dermatophytic fungi like Trichophyton mentagrophytes,Trichophyton rubrum,Microsporum can...Objective:To evaluate the in vitro antifungal activity of Aegle marmelos leaf extracts and fractions on the clinical isolates of dermatophytic fungi like Trichophyton mentagrophytes,Trichophyton rubrum,Microsporum canis,Microsporum gypseum and Epidermophyton floccosum.Methods:The minimum inhibitory concentration(MIC) and minimum fungicidal concentration(MFC) of various extracts and fractions of the leaves of Aegle marmelos were measured using method of National Committee for Clinical Laboratory Standards(NCCLS).Results:Aegle marmelos leaf extracts and fractions were found to have fungicidal activity against various clinical isolates of dermatophytic fungi.The MIC and MFC was found to be high in water and ethyl alcohol extracts and methanol fractions(200μg/mL) against dermatophytic fungi studied.Conclusions:Aegle marmelos leaf extracts significantly inhibites the growth of all dermatophytic fungi studied.If this activity is confirmed by in vivo studies and if the compound is isolated and identified,it could be a remedy for dermatophytosis.展开更多
Twenty-three 1 -(1H-1,2,4-triazole-1 -y1)-2-(2,4-difluorophenyl)-3-(iV-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase. In vitro...Twenty-three 1 -(1H-1,2,4-triazole-1 -y1)-2-(2,4-difluorophenyl)-3-(iV-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase. In vitro antifungal activities showed that some of the title compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.展开更多
Objective:To evaluate the antifungal activity of four honeys of different types from Algeria against pathogenic yeast i.e.Candida albicans(C.albicans) and Rhoddtorula sp.Methods:Four Algeria honeys of different botani...Objective:To evaluate the antifungal activity of four honeys of different types from Algeria against pathogenic yeast i.e.Candida albicans(C.albicans) and Rhoddtorula sp.Methods:Four Algeria honeys of different botanical origin were analvzed to test anlilungal effect against C.albicans,and Rhodotorula sp.Different concentrations(undiluted,10%,30%,50%and 70%w/v) of honey were studied in vitro for their antifugal aclivity using C.albicans and Rhodotorula sp.as fungal strains.Results:The range of the c liameter of zone of inhibition of various concentrations ol tested honeys was(7-23 mm) for Rhodotorula sp.,while C.albicans showed clearly resistance towards all concentrations used.The MICs of tested honey concentrations against C.albicans and Rhodotorula sp.were(70.09-93.48)%and(4.90-99.70)%v/v,respectively.Conclusions:This study demonstrales that,in vitro,these natural products have clearly an antifungal activity against Rhodotorula sp.and C.albicans.展开更多
Objective:To assess antifungal activity of Ocimum sanctum leaves against dermatophytic fungi. Methods:Antifungal activity of Ocimum sanctum leaves was measured by 38 A NCCLS method. Minimum inhibitory concentration(MI...Objective:To assess antifungal activity of Ocimum sanctum leaves against dermatophytic fungi. Methods:Antifungal activity of Ocimum sanctum leaves was measured by 38 A NCCLS method. Minimum inhibitory concentration(MIC) and minimum fungicidal concentration(MFC) of various extracts and fractions of Ocimum sanctum leaves were also determined.Results:Ocimum sanctum leaves possessed antifungal activity against clinically isolated dermatophytes at the concentration of 200μg/mL.MIC and MFC were high with water fraction(200μg/mL) against dermatophytic fungi used.Conclusions:Ocimum sanctum has antifungal activity,and the leaf extracts may be a useful source for dermatophytic infections.展开更多
Essential oils (EOs) are the volatile lipophilic components extracted from plants. Many EOs have demonstrated strong antimicrobial properties when tested in in vitro experiments. The commercial applications of these E...Essential oils (EOs) are the volatile lipophilic components extracted from plants. Many EOs have demonstrated strong antimicrobial properties when tested in in vitro experiments. The commercial applications of these EOs require a suitable formulation constituted by biodegradable compounds that protect them from degradation and evaporation at the same time that allows for a sustained release. The objective of this study was therefore to reduce the rate of evaporation of the oil via microencapsulation. Alginate microspheres (AMSs) were prepared using emulsion extrusion method. The AMSs were hardened with a cross-linking agent, calcium chloride. The effects of the three variables: alginate concentration (0.5% - 8%), the amount of cross-linking agent (0.125% - 2%) and time of cross-linking (5 - 30 min.) on loading capacity and encapsulation efficiency (EE, %) were studied. The effect of the amount of cross-linker was significant on loading capacity (%) and EE (%). The AMSs under the optimized conditions provided loading capacity of 22% - 24% and EE of 90% - 94% based on type of EO. The antifungal activity of vapors of microencapsulated and non-microencapsulated oils were evaluated against two of pathogenic fungi species for stored grains: Aspergillus niger and Fusarium verticillioides. The optimized MSs were observed to have a sustained in vitro release profile (50% of the antifungal activity was maintained at the 8th day of the study). In conclusion, encapsulation in Ca-alginate microspheres may effectively reduce the evaporation rate of essential oils, thus?increase the potential antifungal activity.展开更多
Root rot disease caused by Fusarium solani is the most devastating disease of the tomato and legume crops in China.The metabolites of Bacillus species can inhibit many fungal diseases.In this study,the metabolites of ...Root rot disease caused by Fusarium solani is the most devastating disease of the tomato and legume crops in China.The metabolites of Bacillus species can inhibit many fungal diseases.In this study,the metabolites of deep-sea-derived bacterium Bacillus subtilis 2 H11 can significantly inhibit the growth of F.solani.The metabolite C_(17)-fengycin B,one of the cyclic lipopeptides,was identified by the combination of silica column chromatography,high-performance liquid chromatography(HPLC),high-energy collision induced dissociation mass spectrometry(HCD-MS)and tandem mass spectrometry(HCD-MS/MS).The results of scanning electron microscopy(SEM)and transmission electron microscopy(TEM)showed that C_(17)-fengycin B could destroy the structure of the hyphae and spores of F.solani.The antifungal activities of C_(17)-fengycin B against F.solani were tested at concentrations ranging from 0.05 mg/mL to 0.20 mg/mL.The results indicated that C_(17)-fengycin B inhibited the growth of F.solani with antifungal index of 89.80%at 0.20 mg/mL,and the antifungal activity of C_(17)-fengycin B was further verified by the pot experiment.In addition,the cytotoxicity experiment showed that C_(17)-fengycin B had good biocompatibility and was a potential candidate for the development of biocontrol pesticide in the future.展开更多
A Streptomyces isolate having antifungal activity against Pyricularia oryzae, the causal agent of rice blast disease, was isolated from soil collected in rice fields of Tanjung Karang Selangor, peninsula Malaysia.The ...A Streptomyces isolate having antifungal activity against Pyricularia oryzae, the causal agent of rice blast disease, was isolated from soil collected in rice fields of Tanjung Karang Selangor, peninsula Malaysia.The aim of the study was to determine the antifungal activity of Streptomyces sp. isolate UPMRS4 extracts against P. oryzae and to identify bioactive antifungal compounds produced by UPMRS4. Various solvents were used for extraction of antifungal compounds and well diffusion method was used to determine the antifungal activity of the extracts. The ethyl acetate extract demonstrated the highest activity against mycelial growth of P. oryzae, with an effective inhibitory concentration (EIC) of 1.562 μg/ml significantly higher compared to that of chloroform, diethyl ether, methanol, acetone, ethanol and water. Based on GC-MS and LC-MS/MSanalyses,compounds with antifungal activity were detected such as (Pyrrolo[1,2-a] pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl);Pyrrolo[1,2-a] pyrazine-1,4-dione, hexahydro-3-(phenylmethyl);ergotamine;amicomacin;fungichromin;rapamycin and N-Acetyl-D, L-phenylalanine. These compounds had good general antifungal activity and might have potential future agricultural applications.展开更多
The title compound N-((2,6-difluorophenyl)carbamoyl)-1,3-dimethyl-1 H-pyrazole-4-carboxamide(C_(13)H_(12)F_2N_4O_2) was synthesized, and its structure was confirmed by ~1H NMR,HRMS and X-ray diffraction. It crystalliz...The title compound N-((2,6-difluorophenyl)carbamoyl)-1,3-dimethyl-1 H-pyrazole-4-carboxamide(C_(13)H_(12)F_2N_4O_2) was synthesized, and its structure was confirmed by ~1H NMR,HRMS and X-ray diffraction. It crystallizes in the monoclinic system, space group P2_(1/c) with a = 9.50(2), b = 10.11(2), c = 14.07(3) ?, β = 102.15(3)°, Dc = 1.480 g/cm^3, Z = 4, V = 1320(5) ?~3, the final R = 0.0789 and wR = 0.1860 for 1054 observed reflections with I > 2σ(I). The preliminary biological test shows that the title compound has weak antifungal activities.展开更多
BACKGROUND(-)-Fenchone is a bicyclic monoterpene present in essential oils of plant species,such as Foeniculum vulgare and Peumus boldus,used to treatment of gastrointestinal diseases.Pharmacological studies report it...BACKGROUND(-)-Fenchone is a bicyclic monoterpene present in essential oils of plant species,such as Foeniculum vulgare and Peumus boldus,used to treatment of gastrointestinal diseases.Pharmacological studies report its anti-inflammatory,antioxidant,and antinociceptive activity.AIM To investigate antidiarrheal activity related to gastrointestinal motility,intestinal secretion and antimicrobial activity.METHODS A castor oil-induced diarrhea model was used to evaluate antidiarrheal activity.Intestinal transit and gastric emptying protocols were used to assess a possible antimotility effect.Muscarinic receptors,presynaptic α2-adrenergic and tissue adrenergic receptors,KATP channels,nitric oxide were investigated to uncover antimotility mechanisms of action and castor oil-induced enteropooling to elucidate antisecretory mechanisms.The antimicrobial activity was evaluated in the minimum inhibitory concentration model,the fractional inhibitory concentration index using the(-)-fenchone association method with standard antifungal agents.RESULTS(-)-Fenchone(75,150 and 300 mg/kg)showed antidiarrheal activity,with a significant decrease in the evacuation index.This activity is possibly related to a percentage of reduced intestinal transit(75,150 and 300 mg/kg).The antimotility effect of(-)-fenchone decreased in the presence of pilocarpine,yohimbine,propranolol,L-NG-nitroarginine methyl ester or glibenclamide.In the enteropooling model,no reduction in intestinal fluid weight was observed.(-)-Fenchone did not show antibacterial activity;on the other hand,inhibits the growth of strains of fungi with a minimum fungicide concentration of 32μg/mL.However,when it was associated with amphotericin B,no synergism was observed.CONCLUSION The antidiarrheal effect of(-)-fenchone in this study involves antimotility effect and not involve antisecretory mechanisms.(-)-Fenchone presents antifungal activity;however,it did not show antibacterial activity.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The Higher Education Commission(HEC)funded this work under“Transcriptomics Based Understanding of Cercospora Leaf Spot Resistance in Mungbean and Disease Management through Nanotechnology,”Project No.7425.
文摘We developed a molecular marker for MAS of mungbean resistant varieties against CLS from the consensus sequence(MB-CLsRG)of identified RGAs(MB-ClsRCaG1 and MB-ClsRCaG2).The MB-CLsRG sequence-specific primer pair was used to screen Cercospora leaf spot(CLS)resistant varieties of mungbean in genomic analysis that showed congruency with phenotypic screening.Validation of molecular marker linkage with CLS resistance was performed using rtPCR in transcriptomic analysis.The sequenced PCR products showed 100%homology with MB-CLsRG sequence and putative disease resistance proteins that confirmed the linkage of molecular marker with CLS resistance in mungbean.The antifungal potential of MB-CLsRG gene encoding protein was assessed.The MB-CLsRG gene sequence was cloned in the E.coli expression vector for recombinant protein production.The recombinant protein was then investigated for its in vitro antifungal potential against Cercospora canescens.The in vitro investigation showed strong antifungal activity of recombinant protein as it restricted the growth of fungal mycelial mass.The results validated the linkage of developed marker with CLS-resistant mungbean varieties;therefore,it can be used to screen resistant varieties from a large population in MAS.Moreover,the recombinant protein of the MB-CLsRG gene sequence revealed antifungal potential,which proved the gene sequence could be suitable to use in transgenic plants technology to develop fungal-resistant transgenic crops.
基金supported by the National Natural Science Foundation of China (32172384 and 31501623)the Natural Science Foundation of Hebei (C2020204028)+1 种基金the Key Research and Development Project of Hebei Province (20326505D)the “Hundred Talents Program” for the Introduction of High-level Overseas Talents in Hebei Province (E2020100004)。
文摘Puccinia triticina(Pt), as the causal agent of wheat leaf rust, employs a plethora of effector proteins to modulate wheat immunity for successful colonization. Understanding the molecular mechanisms underlying Pt effector-mediated wheat susceptibility remains largely unexplored. In this study, an effector Pt_21 was identified to interact with the apoplast-localized wheat thaumatin-like protein TaTLP1 using a yeast two-hybrid assay and the Pt_21-TaTLP1 interaction was characterized. The interaction between Pt_21 and TaTLP1 was validated by in vivo co-immunoprecipitation assay. A TaTLP1 variant,TaTLP1C71A, that was identified by the site-directed mutagenesis failed to interact with Pt_21. Pt_21was able to suppress Bax-mediated cell death in leaves of Nicotiana benthamiana and inhibit TaTLP1-mediated antifungal activity. Furthermore, infiltration of recombinant protein Pt_21 into leaves of transgenic wheat line overexpressing TaTLP1 enhanced the disease development of leaf rust compared to that in wild-type leaves. These findings demonstrate that Pt_21 suppresses host defense response by directly targeting wheat TaTLP1 and inhibiting its antifungal activity, which broadens our understanding of the molecular mechanisms underlying Pt effector-mediated susceptibility in wheat.
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 Natural Science Foundation of Ningxia(No.NZ15015)
文摘A new coordination compound, [Co(L^(223))_2(H_2O)_2]·H_2pm(1, L^(223) = 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.
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,1H-NMR and elementary analysis. Most of these compounds showed excellent antifungal activity.
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.
文摘Background: Nigeria is plagued with a variety of socioeconomic problems mainly poverty, poor access to quality healthcare and poor hygienic conditions resulting in the myriad of fungal infections that are frequently encountered in clinical practice. Method: The antifungal activity of aqueous, methanolic, propanolic and benzyl alcohol extracts of Capsicum annuum fruits and seeds, Capsicum chinense fruits and seeds, Aframomum melegueta pods and seeds, Allium sativum bulbs, Allium cepa bulbs and Zingiber officinale rhizomes on Candida albicans (yeast), Aspergillus niger (mould) and Trichophyton rubrum (dermatophyte) were evaluated by the agar well diffusion method. The aqueous and alcoholic filtered plant extracts were obtained by maceration, and also methanolic extracts were also obtained by Soxhlet extraction. The results were obtained by measuring the inhibition zone diameter in millimeters and were presented by subtracting the activity of the control. Results: Aqueous and methanolic extracts of Allium sativum gave the highest inhibition of the growth of Candida albicans (22 mm), followed closely by its propanolic extract with inhibition zone diameter of 15 mm, and also, propanolic extracts of Aframomum melegueta and Allium cepa gave inhibition zone diameters of 12 mm each. Soxhlet methanolic extract of Allium sativum had the highest inhibition of the growth of Aspergillus niger with an inhibition zone diameter of 25 mm, followed closely by Zingiber officinale Soxhlet methanolic extract with an inhibition zone diameter of 22 mm, also, the propanolic extract of Allium sativum gave an inhibition zone diameter of 21 mm, whereas Soxhlet methanolic extracts of Aframomum melegueta and Allium cepa gave an inhibition zone diameter of 19 mm each. The highest activity against Trichophyton rubrum was obtained with the Soxhlet methanolic extract of Allium sativum (39 mm), followed closely by its propanolic extract with an inhibition zone diameter of 27 mm. An inhibition zone diameter of 22 mm was recorded with the benzyl alcohol extract of Allium cepa, 22 mm with the Soxhlet methanolic extract of Aframomum melegueta and 19mm with the aqueous extract of Capsicum chinense seeds. Conclusion: The in-vitro inhibitory effects of these spice extracts indicated that the test spices could serve as potential candidates for developing new systemic and topical antifungal drugs against the wide range of pathogenic fungal strains, and they could also serve as natural prophylaxis against the fungal infections.
基金CNPq(Brazilian National Research Council)which has awarded us a grant for this research
文摘Microorganism resistance to the existing products is yet another difficulty that agriculturalists have to deal with. In this context, the search for new agricultural products that can fight phytopathogens has become increasingly important. Plants have played an important role in this process, because they can serve as a source of new compounds for drug discovery. Plants belonging to the genus Pinus produce an oleoresin that protects the plant against herbivores and pathogens. With a view to developing products that can combat fungal pathogens without harming the environment, this work aimed to evaluate the antifungal activity of the oleoresins and fractions of Pinus elliottii Engelm and Pinus tropicalis against phytopathogens. The methodology based on NCCLS M38-A standards aided antifungal activity assessment. The microdilution method helped to determine the Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC). The oleoresins of P. elliottii and P. tropicalis afforded the most significant results—they displayed fungicidal activity against all the tested species. MIC values were promising, especially the MIC of the oleoresin of P. elliottii against S. rolfsii (1.95 μg·mL-1). The MIC values of the oleoresins of P. elliottii and P. tropicalis ranged from 1.95 to 1000 μg·mL-1 and from 31.25 to 250 μg·mL-1, respectively. Fraction PT2 of P. tropicalis furnished the best results among all the assayed fractions: MIC values lay between 125 and 500 μg·mL-11. In conclusion, the oleoresin of P. tropicalis is a promising source of new antifungal agents for application in the treatment of phytopathogenic infections.
文摘Objective:To evaluate the in vitro antifungal activity of Aegle marmelos leaf extracts and fractions on the clinical isolates of dermatophytic fungi like Trichophyton mentagrophytes,Trichophyton rubrum,Microsporum canis,Microsporum gypseum and Epidermophyton floccosum.Methods:The minimum inhibitory concentration(MIC) and minimum fungicidal concentration(MFC) of various extracts and fractions of the leaves of Aegle marmelos were measured using method of National Committee for Clinical Laboratory Standards(NCCLS).Results:Aegle marmelos leaf extracts and fractions were found to have fungicidal activity against various clinical isolates of dermatophytic fungi.The MIC and MFC was found to be high in water and ethyl alcohol extracts and methanol fractions(200μg/mL) against dermatophytic fungi studied.Conclusions:Aegle marmelos leaf extracts significantly inhibites the growth of all dermatophytic fungi studied.If this activity is confirmed by in vivo studies and if the compound is isolated and identified,it could be a remedy for dermatophytosis.
文摘Twenty-three 1 -(1H-1,2,4-triazole-1 -y1)-2-(2,4-difluorophenyl)-3-(iV-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase. In vitro antifungal activities showed that some of the title compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.
基金supported by project CNEPRU,Institute of Veterinary Sciences(IVS),University Ibn-Khaldoun(TIARET),Algeria(grant No.F023 2009/0009)
文摘Objective:To evaluate the antifungal activity of four honeys of different types from Algeria against pathogenic yeast i.e.Candida albicans(C.albicans) and Rhoddtorula sp.Methods:Four Algeria honeys of different botanical origin were analvzed to test anlilungal effect against C.albicans,and Rhodotorula sp.Different concentrations(undiluted,10%,30%,50%and 70%w/v) of honey were studied in vitro for their antifugal aclivity using C.albicans and Rhodotorula sp.as fungal strains.Results:The range of the c liameter of zone of inhibition of various concentrations ol tested honeys was(7-23 mm) for Rhodotorula sp.,while C.albicans showed clearly resistance towards all concentrations used.The MICs of tested honey concentrations against C.albicans and Rhodotorula sp.were(70.09-93.48)%and(4.90-99.70)%v/v,respectively.Conclusions:This study demonstrales that,in vitro,these natural products have clearly an antifungal activity against Rhodotorula sp.and C.albicans.
文摘Objective:To assess antifungal activity of Ocimum sanctum leaves against dermatophytic fungi. Methods:Antifungal activity of Ocimum sanctum leaves was measured by 38 A NCCLS method. Minimum inhibitory concentration(MIC) and minimum fungicidal concentration(MFC) of various extracts and fractions of Ocimum sanctum leaves were also determined.Results:Ocimum sanctum leaves possessed antifungal activity against clinically isolated dermatophytes at the concentration of 200μg/mL.MIC and MFC were high with water fraction(200μg/mL) against dermatophytic fungi used.Conclusions:Ocimum sanctum has antifungal activity,and the leaf extracts may be a useful source for dermatophytic infections.
文摘Essential oils (EOs) are the volatile lipophilic components extracted from plants. Many EOs have demonstrated strong antimicrobial properties when tested in in vitro experiments. The commercial applications of these EOs require a suitable formulation constituted by biodegradable compounds that protect them from degradation and evaporation at the same time that allows for a sustained release. The objective of this study was therefore to reduce the rate of evaporation of the oil via microencapsulation. Alginate microspheres (AMSs) were prepared using emulsion extrusion method. The AMSs were hardened with a cross-linking agent, calcium chloride. The effects of the three variables: alginate concentration (0.5% - 8%), the amount of cross-linking agent (0.125% - 2%) and time of cross-linking (5 - 30 min.) on loading capacity and encapsulation efficiency (EE, %) were studied. The effect of the amount of cross-linker was significant on loading capacity (%) and EE (%). The AMSs under the optimized conditions provided loading capacity of 22% - 24% and EE of 90% - 94% based on type of EO. The antifungal activity of vapors of microencapsulated and non-microencapsulated oils were evaluated against two of pathogenic fungi species for stored grains: Aspergillus niger and Fusarium verticillioides. The optimized MSs were observed to have a sustained in vitro release profile (50% of the antifungal activity was maintained at the 8th day of the study). In conclusion, encapsulation in Ca-alginate microspheres may effectively reduce the evaporation rate of essential oils, thus?increase the potential antifungal activity.
基金the National Key R&D Program of China(No.2018YFC0310800)the China Ocean Mineral Resources R&D Association Grant(No.DY135-B2-14)+3 种基金the Strategic Priority Research Program of the Chinese Academy of Sciences(No.XDA22050301)the Taishan Young Scholar Program of Shandong Province(No.tsqn20161051)the Qingdao Innovation Leadership Program(No.18-1-2-7-zhc)for Chaomin SUNthe China Postdoctoral Science Foundation(No.2019M652492)。
文摘Root rot disease caused by Fusarium solani is the most devastating disease of the tomato and legume crops in China.The metabolites of Bacillus species can inhibit many fungal diseases.In this study,the metabolites of deep-sea-derived bacterium Bacillus subtilis 2 H11 can significantly inhibit the growth of F.solani.The metabolite C_(17)-fengycin B,one of the cyclic lipopeptides,was identified by the combination of silica column chromatography,high-performance liquid chromatography(HPLC),high-energy collision induced dissociation mass spectrometry(HCD-MS)and tandem mass spectrometry(HCD-MS/MS).The results of scanning electron microscopy(SEM)and transmission electron microscopy(TEM)showed that C_(17)-fengycin B could destroy the structure of the hyphae and spores of F.solani.The antifungal activities of C_(17)-fengycin B against F.solani were tested at concentrations ranging from 0.05 mg/mL to 0.20 mg/mL.The results indicated that C_(17)-fengycin B inhibited the growth of F.solani with antifungal index of 89.80%at 0.20 mg/mL,and the antifungal activity of C_(17)-fengycin B was further verified by the pot experiment.In addition,the cytotoxicity experiment showed that C_(17)-fengycin B had good biocompatibility and was a potential candidate for the development of biocontrol pesticide in the future.
文摘A Streptomyces isolate having antifungal activity against Pyricularia oryzae, the causal agent of rice blast disease, was isolated from soil collected in rice fields of Tanjung Karang Selangor, peninsula Malaysia.The aim of the study was to determine the antifungal activity of Streptomyces sp. isolate UPMRS4 extracts against P. oryzae and to identify bioactive antifungal compounds produced by UPMRS4. Various solvents were used for extraction of antifungal compounds and well diffusion method was used to determine the antifungal activity of the extracts. The ethyl acetate extract demonstrated the highest activity against mycelial growth of P. oryzae, with an effective inhibitory concentration (EIC) of 1.562 μg/ml significantly higher compared to that of chloroform, diethyl ether, methanol, acetone, ethanol and water. Based on GC-MS and LC-MS/MSanalyses,compounds with antifungal activity were detected such as (Pyrrolo[1,2-a] pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl);Pyrrolo[1,2-a] pyrazine-1,4-dione, hexahydro-3-(phenylmethyl);ergotamine;amicomacin;fungichromin;rapamycin and N-Acetyl-D, L-phenylalanine. These compounds had good general antifungal activity and might have potential future agricultural applications.
基金funded by Natural Science Foundation of Zhejiang Province(No.LY16C140007)National Natural Science Foundation of China(No.31401691)
文摘The title compound N-((2,6-difluorophenyl)carbamoyl)-1,3-dimethyl-1 H-pyrazole-4-carboxamide(C_(13)H_(12)F_2N_4O_2) was synthesized, and its structure was confirmed by ~1H NMR,HRMS and X-ray diffraction. It crystallizes in the monoclinic system, space group P2_(1/c) with a = 9.50(2), b = 10.11(2), c = 14.07(3) ?, β = 102.15(3)°, Dc = 1.480 g/cm^3, Z = 4, V = 1320(5) ?~3, the final R = 0.0789 and wR = 0.1860 for 1054 observed reflections with I > 2σ(I). The preliminary biological test shows that the title compound has weak antifungal activities.
文摘BACKGROUND(-)-Fenchone is a bicyclic monoterpene present in essential oils of plant species,such as Foeniculum vulgare and Peumus boldus,used to treatment of gastrointestinal diseases.Pharmacological studies report its anti-inflammatory,antioxidant,and antinociceptive activity.AIM To investigate antidiarrheal activity related to gastrointestinal motility,intestinal secretion and antimicrobial activity.METHODS A castor oil-induced diarrhea model was used to evaluate antidiarrheal activity.Intestinal transit and gastric emptying protocols were used to assess a possible antimotility effect.Muscarinic receptors,presynaptic α2-adrenergic and tissue adrenergic receptors,KATP channels,nitric oxide were investigated to uncover antimotility mechanisms of action and castor oil-induced enteropooling to elucidate antisecretory mechanisms.The antimicrobial activity was evaluated in the minimum inhibitory concentration model,the fractional inhibitory concentration index using the(-)-fenchone association method with standard antifungal agents.RESULTS(-)-Fenchone(75,150 and 300 mg/kg)showed antidiarrheal activity,with a significant decrease in the evacuation index.This activity is possibly related to a percentage of reduced intestinal transit(75,150 and 300 mg/kg).The antimotility effect of(-)-fenchone decreased in the presence of pilocarpine,yohimbine,propranolol,L-NG-nitroarginine methyl ester or glibenclamide.In the enteropooling model,no reduction in intestinal fluid weight was observed.(-)-Fenchone did not show antibacterial activity;on the other hand,inhibits the growth of strains of fungi with a minimum fungicide concentration of 32μg/mL.However,when it was associated with amphotericin B,no synergism was observed.CONCLUSION The antidiarrheal effect of(-)-fenchone in this study involves antimotility effect and not involve antisecretory mechanisms.(-)-Fenchone presents antifungal activity;however,it did not show antibacterial activity.
