Screening of Two Biocontrol Strains of Bacillus subtilis against Ginseng Soil-borne Disease and Their Antifungal Activities

[ Objective] The paper was to obtain biocontrol strains with good control effects against ginseng soil-borne disease through screening. [ Method] Dilu- tion plate method and plate confrontation culture method were used to isolate and screen biocontrol bacteria from the rhizosphere soil of diseased ginseng. The strains were identified through morphology, physiological and biochemical characteristics and 16S rDNA. [ Result ] With Rhizoctonia solani, Fusarium oxysporum and Fu- sarium solani as the indicator strains, two biocontrol strains B59 and X1 with strong antagonistic effects were screened from the rhizosphere soil of diseased ginseng in Tieli farm of Heilongjiang Province, and they were identified to be Bacillus subtilis. The inhibition rates of two biocontrol strains against eight different fungi were all greater than 90%. The primary study indicated that B59 and X1 strains could secrete antifungal active substances. [ Conclusion] Two biocontrol Bacillus subti- lis strains 1359 and X1 all had strong antagonistic effect against ginseng soil-borne disease, which had certain potential for development and utilization.

Syntheses, Crystal Structures and Antifungal Activities of Two Compounds Containing Pyrazole and Pyrethroid Units

Compounds 1 （C15H17C1F3N303, Mr = 379） and 2 （C14H14C1F3N4OS, Mr = 378） have been synthesized and their crystal structures were determined by single-crystal X-ray diffraction. Crystal 1 belongs to the triclinic system, space group P1 with a = 6.0223（19）, b = 9.324（3）, c = 15.936（5） A, a = 80.687（5）, β= 87.289（5）, ）, = 86.097（5）°, V= 880.4（5） A3, Z = 2, Dc = 1.433 g/cm3,μ（MoKa） = 0.266 mm^-1, F（000） = 392, R = 0.0861 and wR = 0.1999 for 2022 observed reflections with I 〉 2o（/）. Crystal 2 belongs to the triclinic system, space group PI with a = 7.7029（15）, b = 8.3371（16）, c = 14.410（3） A, a = 100.672（3）, β= 103.168（3）, ？ = 98.726（3）°, V = 876.1（3） A3, Z = 2, Dc= 1.451 g/cm^3,μ（MoKa） = 0.379 mm^-1, F（000） = 388, R = 0.0672 and wR = 0.2105 for 2725 observed reflections with I 〉 2σ（I）. Although the two compounds are similar with the same pyrazole and pyrethroid units, X-ray analysis reveals that their structures are completely different.

Study on the Antifungal Activities of Mikania micrantha Extracts

The stems and leaves of Mikania micrantha were successively extracted with petroleum ether, ethyl acetate and ethanol. In vitro and in vivo test method was adopted to deten＇nine the inhibition activity of three solvent extracts against three plant pathogens. Growth rate method showed that ethyl acetate extract could significantly inhibit the mycelial growth of Botrytis circrea, Gtomerclla ciugulata and Fusarium bulbigeuum under the given concentration of 0.09 g/ml in dry sam- ple, and the inhibition rates were all greater than 90%. Organization test showed that the curative effect of petroleum ether extract against B. cirerea was 63.55% under the given concentration of 0.18 g/ml in dry sample, and the curative effect of ethanol extract was 71.47%. In the potting test against Erysiphe gramiuis, the curative effect of petroleum ether extract was 81.26%, while the curative effect of ethyl acetate extract was 62.07%.

Crystal Structure and Antifungal Activities of a New Zn(Ⅱ) Complex Based on Triadimenol

A new Zn（II） complex, [ZnL2Br2] （L = triadimenol） was synthesized by the reaction of ZnBr2 with the commercial fungicide of triadimenol, then characterized by elemental analysis, IR spectroscopy and single-crystal X-ray diffraction. The crystal structure shows that the complex [ZnL2Br2] crystallizes in orthorhombic, Pnam space group with a = 11.263（2）, b = 8.4478（15）, c = 36.125 （7） A, V = 3437.2 （11 ） ,A Z = 4, C28H36Br2C12N604Zn, Mr = 816.72, Dc = 1.578 g/cm3, F（000） = 1648,μ = 3.236 mm-1, the final R = 0.0388 and wR = 0.0879 for 2399 observed reflections with I 〉 2σ（/）. The central metals adopt square plane coordination geometry. And intermolecular hydrogen bonds connect Zn（Ⅱ） into a one-dimensional chain. In addition, the title complex and triadimenol were screened for antifungal activities against four selected fungi using the mycelial growth rate method. The results indicate that the complex synthesized shows better antifungal activities than the ligand triadimenol.

Antifungal Activities of Ethanol Extracts from 30 Kinds of Chinese Herbs against Powdery Mildew of Pumpkin

With Sphaerotheca fuliginea as test object, the indoor antifungal activities of ethanol extracts from 30 kinds of Chinese herbs were measured by leaf disc method. The results showed that the extracts from Stellera chamaejasma, Datura stramonium, Pericarpium zanthoxyli and Tetradium ruticarpum had the best control effect; when the concentration of extract was 10 g/L, the control effect of these four plants was greater than 90% ; when the concentration was 5 g/L, the control effect of S. chamaejasma was 90.3%, and the control effects of D. stramonium, P. zanthoxyli and T. ruticarpum were also greater than 85%.

SCREENING FOR ANTIBACTERIAL AND ANTIFUNGAL ACTIVITIES IN SOME MARINE ALGAE FROM THE FUJIAN COAST OF CHINA WITH THREE DIFFERENT SOLVENTS

Three different solvents viz ethanol, acetone and methanol toluene (3:1) were used to extract antibiotics from 23 species of marine algae belonging to the Chlorophyta, Phaeophyta and Rhodophyta. Their crude extracts were tested for antibacterial and antifungal activities. Among them, the ethanol extract showed the strongest activity against the bacteria and fungi tested. Four species of the Rhodophyta ( Laurencia okamurai, Dasya scoparia, Grateloupia filicina and plocamium telfairiae ) showed a wide spectrum of antibacterial activity. Every solvent extract from the four species was active against all the bacteria tested. The test bacterium Pseudomonas solancearum and the fungus Penicilium citrinum were most sensitive to the extracts of marine algae. In general, the extracts of seaweeds inhibited bacteria more strongly than fungi and species of the Rhodophyta showed the greatest activity against the bacteria and fungi tested.

One-pot synthesis,antibacterial and antifungal activities of novel 2,5-disubstituted-1,3,4-oxadiazoles

A series of novel 2,5-disubstituted-1,3,4-oxadiazoles have been synthesized from long-chain alkanoic and alkenoic acids. The structures of these compounds have been elucidated by elemental and spectral （IR, ^1H NMR, ^13C NMR, MS） analysis. Furthermore, compounds were screened for in vitro antibacterial activity against the representative panel of two Gram-positive and two Gram- negative bacteria. All the synthesized compounds were also tested for their inhibitory action against five strains of fungus. The various compounds show potent inhibitory action against test organisms. 2007 Abdul Rauf. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

Antitumor and Antifungal Activities of Organic Extracts of Seacucumber Holothuria atra from the Southeast Coast of India

In phylum Echinodermata, the family Holothuridae is distinguished by its capacity of bioactive compounds. Sea cu- cumber Holothuria atra is commonly known as the lollyfish. The antifimgal activity was detected using agar well diffusion method against the various fungal strains such as Trichoderma viride, Aspergillus niger, Aspergillus flavis, Candida albicans and Penicillium chrysogenum. Relatively high antifungal activity was seen against Candida albicans at 100 μL-1 concentration of extracts. Zone of inhibition was measured at 18 mm of diameter. The anti-tumor activities were detected against the Vero and Hep2 cell lines using MTT assay. The cells were treated with H. atra extract at concentrations 0.078-10mg mL-1. The extract showed high proliferative activity against the Hep2 cells. The body wall extracts of sea cucumber （H. atra） showed effective antifungal and antitumor activities All these findings suggest that the extracts could be used for the development of drugs.

Synthesis,Crystal Structure and Antifungal Activities of 3-Methyl-1-(4-methylphenyl)-4-(N-4-trifluoromethylphenyl)-aminomethyl-5-(4-methoxyphenylthio)-1H-pyrazole

The title compound 3-methyl-l-（4-methylphenyl）-4-（N-4-trifluoromethylphenyl） aminomethyl-5-（4-methoxyphenylthio）-lH-pyrazole has been synthesized via a four-step reaction and characterized by IR, 1H NMR, elemental analysis and X-ray crystallography. The compound crystallizes in monoclinic, space group P21/c with a = 8.7170（15）, b = 18.355（3）, c = 15.292（3） A, fl = 103.445（3）°, V= 2379.7（7） A3, Dc = 1.350 g/cm3, Z = 4, p = 0.184, F（000） = 1008, and the final R = 0.0491 and wR = 0.1339 for 4160 observed reflections （I 〉 2a（/））. The results demonstrate that there is a face-to-face π-π stacking interaction between one benzene ring （C（19）-C（24）） and another （C（I 3）-C（! 8）） at a plane-plane distance of 3.3539 A. The ring normal and vector between the ring centroids form an angle of 18.2° up to the centroid-to-centroid distance of 3.5273 A. The crystal structure is stabilized by the intermolecular hydrogen bond of N（3）-H（3A）...N（2） （symmetry code： A -x＋l, -y＋l, -z）. The preliminary biological test shows that the title compound has a moderate antifungal activity.

Solvent-and Catalyst-free Synthesis and Antifungal Activities of α-Aminophosphonate Containing Cyclopropane Moiety

Nine new a-aminophosphonate derivatives containing cyclopropane moiety have been synthesized via conventional and microwave irradiation methods under solvent- and catalyst-free condition. The structures of the title compounds have been confirmed by ^1H NMR, ^31p NMR FTIR, EI-MS and FTICR-MS. Their antifungal activities were evaluated in vivo and some of the compounds were found to exhibit excellent antifungal activities against Corynespora cassiicola, Pseudomonas syringae pv. Lachrymans, Pseudoperonospora cubensis and Sclerotinia sclerotiorum.

Scoping Antifungal Activities of Various Forms of Chitosan Oligomers and Their Potential Fixation in Wood

Chitosan oligomers （average Dp-4） are known for their antifungal activity and wood decay resistance. These oligomers are susceptible to moisture, and promote yeast growth upon air exposure after a sufficient length of time. Chitosan oligomers of three different states viz. completely dried, freshly prepared and highly viscous form, were prepared to compare their in-vitro antifungal activities against three brown-rot fungi, two sapstain and one mould fungus using agar nutrient medium. Additionally, a mixture of chitosan oligomers and boric acid was used for wood treatment. The nutrient medium bioassay results show that all states of chitosan oligomers inhibited the growth of tested basidiomycetes fungi, but not sapstain and mould fungi. Subsequently, wood decay results confirm antifungal activity of chitosan oligomers plus boron against basidiomycetes, but highlighted their leachability upon water exposure.

Preliminary Study on Antifungal Activities of 30 Kinds of Plant Extracts

[Objective]The paper was to screen the plant extracts with strong antifungal activity. [Method] With R. solani as the test object, the antifungal activities of 30 kinds of plant extracts were carried out primary screening by mycelial growth rate method. [Result] Twelve kinds of plant extracts including Pinus yunnanensis （leaf）, Phryma leptostachya （stem and leaf）, Pueraria peduncularis （root, stem and leaf）, Pinus armandiifruit （fruit）, Aconitum brachypodum （stem and leaf）, Phellodendron amurense （stem and leaf）, Rhaponticum uniflorum （root）, Alnus cremastogyne （leaf）, Rehmannia glutinosa （root）, Cryptomeria fortunei （stem and leaf） and Berberis pruinosa （stem and leaf） had strong activities against R. solani with growth inhibition rates over 80% as the concentration was 10 mg/ml,among which the extracts of P. yunnanensis （leaf）, P. leptostachya （stem and leaf）, P. peduncularis （root, stem and leaf） and P. armandiifruit （fruit） showed the inhibition rate above 95%, significantly higher than other plant extracts. The secondary screening results of antifungal activities of the above 12 plant extracts were consistent with the primary screening. [Conclusion] The study laid foundation for further development of high efficient, safe and environmental-friendly new fungicides.

Synthesis, Characterization, Antibacterial, and Antifungal Activities of Cobalt(II), Nickel(II) and Copper(II) Complexes with 3-thioacetyl-2-amino-1,4-naphthoquinone and 2-benzoyl-3-amino-1,4-naphthoquinone Ligands

The aim of this work is to synthesize, characterize and evaluate the biological activity of 1,4-naphthoquinone derivatives ligands and their metal—Co(II), Ni(II) and Cu(II) chelates. Continuing our work with another derivatives of 1,4-naphthoquinone ligands, this work had been constructed for synthesis of new ligands derived from 1,4-naphthoquinone such as 3-thioacetyl-2-amino-1,4-naphthoquinone and 2-benzoyl-3-amino-1,4-naphthoquinone (L1-L2) which characterized on the basis of elemental analysis, electronic, IR, mass, 1H-NMR spectral data. The synthesized ligands have been carried out to achieve the coordination behavior towards bi-valent metal ions like cobalt, nickel and copper. The solid chelates of the different ligands were prepared and subjected to analytical techniques such as elemental analyses, spectroscopic techniques including mass, 1H-NMR, and IR spectroscopy, and thermal analyses techniques. The chelates were found to have octahedral geometry. The biological activity of the prepared ligands and their binary metals complexes were also screened against different antifungal and antibacterial organisms.

Antifungal Activities of Commercial Rice Wine Extracts of Taiwan Residents Allium fistulosum

Antifungal activities of the commercial rice wine extracts of Allium fistulosum were analyzed. Antifungal activities were tested against 7 pathogenic fungi by using agar disc diffusion and tube dilution tests. The results show that the commercial rice wine extracts of Allium fistulosum have strong antifungal activity against Aspergillus brasiliensis ATCC 16404, Candida albicans ATCC 10231, Microsporumcanis ATCC 36299, M. gypseum ATCC 24102, Trichophyton mentagrophytes ATCC 9533, T. rubrum ATCC 28188, and T. tonsurans ATCC 28942. The commercial rice wine extracts of different A. fistulosum parts were found to exhibit significant antifungal activities with the minimal inhibitory concentration (MIC) in the range of 0.2 - 1.0 mg/mL. The antifungal activity of the extracts of different A. fistulosum parts was in the order of AFS (stem) > AFI (plant body) > AFL (leaf) > AFR (root).

Antifungal Activities of Eight Fungicides against Fusarium oxysporum Schlecht

[Objective]The paper was to screen fungicides with strong antifungal activities against Fusarium oxysporum Schlecht,and to provide a theoretical basis for controlling root-rot of Rhodiola sachalinensis A. Bor. [Method]Using mycelial growth rate method,the indoor antifungal activities of eight fungicides against F. oxysporum were studied. [Result]Eight fungicides at different concentrations performed different antifungal activities. Toxicity test results showed that the EC_（50） value of Difenoconazole was the smallest（ 4. 267 4 mg/L）,followed by Mancozeb（ 6. 952 5 mg/L）,and the EC_（50） of Thiram,Captan and Procymidone were relatively small from 25 to 50 mg/L. [Conclusion]Among eight fungicides,Difenoconazole had the best antifungal effect against F. oxysporum,while Mancozeb,Thiram,Captan and Procymidone had good control effects as well.

Synthesis and Antifungal Activities of New Type β-Methoxyacrylate-Based StrobUurin Analogues

Strobilurins have become one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel fl-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, 1H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds 1 exhibited potent antifungal activity against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 μg/mL. Exhilaratingly, compound 1 a （R= methyl） showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.

Mechanisms,clinically curative effects,and antifungal activities of cinnamon oil and pogostemon oil complex against three species of Candida

The anti-fungus mechanisms and curative effects of cinnamon oil and pogostemon oil complexes to wards intestinal Candida infections were investigat ed.We measured the minimal inhibitory concentra tion(MIC) values of the complexes against Candida using proportionally-diluted test-tube medium and examined the evolution of the morphology and structures of Candida albicans using scanning electronic microscopy(SEM) and transmission elec tronic microscopy(TEM).We found that the aver age MIC values of the complexes against the fung were 0.064 mg/mL(cinnamon oil),0.032 mg/mL(pogostemon oil) for Candida albicans,0.129 mg/mL(cinnamon oil),0.064 mg/mL(pogostemon oil for Candida tropicalis,and 0.129 mg/mL(cinnamon oil),0.064 mg/mL(pogostemon oil),for Candida krusei.SEM examination over a 24-48 h period showed that the morphology of Candida albicans cells changed significantly.Irregular hollows ap peared on the surfaces,inside organelles were destroyed and the cells burst after treatment.TEM examination over a 48-72 h period indicated that the cell walls were damaged,organelles were destroyed and most cytoplasms became empty bubbles.Sixty intestinal Candida-infected patients were treated with a capsule containing cinnamon and pogostemon oil.The curative ratio was 71.67%(43/60),and the improvement ratio was 28.33%(17/60),giving a to talratio of 100%.Thus,the cinnamonoil and pogostemon oil complexes had strong anti-funguseffectsag ainst Candida albicans,Candidatropicalis,and Candidakrusei.They impacted the morphology and sub-micro structures of the fungus within48-72h,and eventually denatured and killed the cells.The complexes have also shown considerable curative effects to intestinal Candida infections.

Design, Synthesis, Antifungal Activities and SARs of （R）-2-Aryl-4,5-dihydrothiazole-4-carboxylic Acid Derivatives

Based on the structure of natural product 2-aryl-4,5-dihydrothiazole-4-carboxylic acid, a series of novel （R）-2-aryl-4,5-dihydrothiazole-4-carboxylic acid derivatives were designed and synthesized. Their structures were characterized by ^1H NMR, ^13C NMR and HRMS. The single crystal structure of compound 9b was determined by X-ray diffraction analysis. The antifungal activities were evaluated for the first time. The bioassay results indicated that most compounds exhibited moderate to good antifungal activities. The antifungal activities of compound 13a （against Cercospora arachidicola Hori）, 13d （against Alternaria solani）, and 16e （against Cercospora arachidieola Hori） were 61.9%, 67.3% and 61.9%, respectively, which are higher than those of the commercial fungicides chlorothalonil and carbendazim. Moreover, compound 13d exhibited excellent antifungal activities against 7 kinds of the fungi tested （66.7%, 77.3%, 63.0%, 87.9%, 70.0%, 70.0% and 80.0% at 50 μg/mL）. Therefore, 13d can be used as a new lead structure for the development of antifungal agents.

In Vitro Antifungal Activity of Dihydrochelerythrine and Proteomic Analysis in Ustilaginoidea virens

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.

The antifungal properties of terpenoids from the endophytic fungus Bipolaris eleusines

A series of terpenoids(1-17),comprising six new compounds designated bipolariterpenes A-F(1-6)and eleven rec-ognized compounds(7-17),were isolated from the wheat culture of the potato endophytic fungus Bipolaris eleusines.Their structures and stereochemistry were clarified by HRESIMS,NMR,DP4+probability analyses,and computations for electronic circular dichroism(ECD).All compounds are made up of six meroterpenoids,four sesterterpenes and seven sesquiterpenes.Among them,four sesterterpenes(4,5,10,11)were investigated for their antifungal,antibacterial and cytotoxic properties,and six meroterpenoids(1-3,7-9)were evaluated for their antifungal properties.The compounds 7,9,and 10 had substantial antifungal activity against Epidermophyton floccosum at a concentration of 100μM.No antibacterial and cytotoxic activities were observed.