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The goal of the work is to determine the bioactive pharmaceutical metabolites produced by the Fusarium oxysporum YP9B isolate. Ten new natural compounds were isolated from the ethyl acetate extract of the F. oxysporum YP9B strain. Their structures were elucidated by spectroscopic methods using 1D and 2D NMR, UV, FT-IR, and mass spectra (LC-QTOF MS and GC-FID/MS). Identified compounds were named as; (1-benzyl-2-methoxy-2-oxoethyl)-2-hydroxy-3-methylbutanoate (1), 2-oxo-8-azatricyclo[9.3.1.13,7]-hexadeca-1(15),3(16),4,6,11,13-hexaen-10-one (2), 2,3-dihydroxypropanoic, hexadecanoic anhydride (3a), 2,3-dihydroxypropanoic (9Z)-octadecenoic anhydride (3b), 2,3-dihydroxy-propanoic (9Z,12Z)-octadecadienoic anhydride (3c), 2,3-dihydroxypropanoic (11Z)-octadecenoic anhydride (4a), 2,3-dihydroxypropanoic, (9E,12E)-octadecadienoic anhydride (4b), 3-hydroxy-1,2,6,10-tetramethylundecyl hexzadecanoate (5a), 3-hydroxy-1,2,6,10-tetramethylundecyl (9E)-octadecaenoate (5b), and 3-hydroxy-1,2,6,10-tetramethylundecyl octadecanoate (5c). Antimicrobial activities of the isolates obtained from the YP9B strain were determined. Cytotoxic and antiviral activities were tested for the isolates against VERO, MCF-7, PC-3, and A549. Compounds 5a-c, 1, and 3a-c showed bacteriostatic activity at low concentrations, and 4a-b and 2 were found to be bactericides. MIC and MBC values against Mycobacterium smegmatis for the compounds 5a-c and 1 were determined to be ​​

BACKGROUND Owing to their strong antimicrobial properties, Helichrysum arenarium (HA), Anzer thyme (AT), and Stevia rebaudiana (SR) have been commonly used in medicine. AIM This study aimed to evaluate antimicrobial activities of HA, AT, and SR against S. mutans and S. wiggsiae in biofilms formed on primary teeth. DESIGN Fifty enamel samples were divided into two groups: mono-species biofilm and two-species biofilm. Each biofilm group was divided into five subgroups (n = 5): group 1, HA; group 2, AT; group 3, SR; group 4, CHX (positive control); and group 5, distilled water (negative control). Minimum inhibitory concentration and minimum bactericidal concentration were determined. The number of viable microorganisms was counted. The presence of microorganisms was examined using a scanning electron microscope, and mineral analysis was performed using energy-dispersive X-ray analysis. RESULTS In the mono-species biofilm, CHX was significantly more effective against S. mutans than other groups (p

In this work, due to the biological activity evaluation, a series of hydroxy methoxy benzoins (1-8), benzils (10-16) and methoxy benzoin/benzil-O-beta-D-glucosides (17-28) were synthesized. Antioxidant (FRAP, CUPRAC, DPPH), antimicrobial (16 microorganisms, and two yeast), enzyme inhibition (alpha-amylase, alpha-glucosidase, AChE, BChE, and tyrosinase) of all synthesized benzoin/benzil analogs were investigated. Benzoins (1-8) showed the most effective antioxidant properties compared to all three methods. Compound 28 against alpha-amylase, compound 9 against alpha-glucosidase, compound 11 against AChE, compound 2 against BChE, and compound 13 against tyrosinase showed the best activities with the better or similar IC50 values as used standards. Hydroxy methoxy benzoin compounds (1-8) among all four groups were seen as the most effective against the tested microorganism. Molecular docking analysis showed that all tested compounds 1-28 (0.01-2.22 mu M) had the best binding affinity against AChE enzyme. Cytotoxic effects of the many of compounds (1-16, 21, and 24) also investigated and it was found that they caused different effects in different cells. The LDH tests of compounds 1a + b, 4, 7, 8, 9, 11, 12, 21, and 24, seemed to be effective compared to the positive control cisplatin. The cytotoxicity of compounds 6 (9.24%) for MCF7 cancer cells, 8 (5.16%) and 4 (8.26%) for HT29 cancer cells, 24 (9.84%) for Hep3B cells and 8 (8.52%), 7 (5.70%), 4 (6.94) and 9 (7.22%) for C6 cells were at normal values. And also cytotoxic activity of four compounds (5, 9, 21, and 24) among the all synthetic groups, were evaluated to the HeLa and RPE. Compound 5 showed anticancer activity on HeLa and RPE cancer cells as much as or better than cisplatin which was used as standard.

Volatile constituents of the essential oil which was obtained by hydrodistillation (HD) in a Clevenger-type apparatus from the air-dried Salvia staminea Montbret & Aucher ex Bentham (Lamiaceae) collected from Bayburt (North East Part of Black Sea Reagan of Turkey), were analyzed by GC-FID and GC-MS. Additionally, volatiles for the whole part of S. staminea were analyzed by two different methods which are headspace (HS)-GC-FID/MS and headspace solid-phase micro extraction (HS-SPME)-GC-FID/MS. As results of this study, thirty compounds from hydrodistillation, fifteen constituents from HS-SPME and two components from headspace of S. staminea were identified with GC-FID/MS. The major compounds identified in the essential oil, SPME and HS of S. staminea were linalyl acetate (23.30%, 85.07%, and 87.55%) and linalool (22.05%, 9.02%, and 12.44%), respectively. The antimicrobial activities of the essential oil of S. staminea were screened against seven microorganisms (Escherichia coli, Yersinia pseudotuberculosis, Staphylococcus aureus, Enterococcus faecalis, Bacillus cereus, Listeria monocytogenes , and Candida albican ) and showed good antimicrobial activity against Gram-positive bacteria which is consistent with the literature with the other types of Salvia species. The essential oil of S. staminea showed good antioxidant activity with IC 50 60.4 µg/mL.

7th EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry -- AUG 27-31, 2017 -- Vienna, AUSTRIA Ture, Asli/0000-0003-3422-7425; Birgul, Kaan/0000-0003-3963-4687; Kucukguzel, Ilkay/0000-0002-7188-1859; Vagolu, Siva Krishna/0000-0003-1540-9995; BOZDEVECI, ARIF/0000-0002-0729-9143; kulabas, necla/0000-0003-2273-5094; Alpay Karaoglu, Sengul/0000-0003-1047-8350 WOS:000475378400058 PubMed: 31085371 Twenty-one novel alkyl/acyl/sulfonyl substituted fluoroquinolone derivatives were designed, synthesized and evaluated for their anti-tuberculosis and antibacterial activity. The targeted compounds were synthesized by the introduction of alkyl, acyl or sulfonyl moieties to the basic secondary amine moiety of moxifloxacin. Structures of the compounds were enlightened by FT-IR, H-1 NMR, C-13 NMR and HRMS data besides elemental analysis. Compounds were initially tested in vitro for their anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv using microplate alamar blue assay. Minimal inhibitory concentration (MIC) values of all compounds were found between > 25.00-0.39 mu g/mL while compounds 1, 2 and 13 revealed an outstanding activity against M. tuberculosis H37Rv with MIC values of 0.39 mu g/mL. Activities of compounds 1-21 against to a number of Gram-positive and Gram-negative bacteria and fast growing mycobacterium strain were also investigated by agar well diffusion and microdilution methods. According to antimicrobial activity results, compound 13 was found the most potent derivative with a IC50 value of < 1.23 mu g/mL against Staphylococcus aureus and clinical strain of methicillin-resistant clinical strain of S. aureus. EFMC

Paenibacillus larvae cause an American foulbrood disease (AFB) that is responsible for the extinction of honeybee colonies and is a honeybee bacterial disease that has to be obligatory notified worldwide. Recently, bacteriophage studies targeting Paenibacillus larvae have emerged as a promising alternative treatment method. The inability of bacteria to create resistance against bacteriophages makes this method advantageous. As a consequence, this study was conducted to describe the genome and biological characteristics of a novel phage capable of lysing Paenibacillus larvae samples isolated from honeybee larva samples in Turkey. The Paenibacillus phage SV21 (vB_PlaP_SV21) was isolated by inducing Paenibacillus larvae strain SV21 with Mitomycin-C. Whole-genome sequencing, comparative genomics, and phylogenetic analysis of vB_PlaP_SV21 were performed. Transmission electron microscopy images showed that vB_PlaP_SV21 phage was a Podovirus morphology. The vB_PlaP_SV21 phage specific for Paenibacillus larvae was determined to belong to the Podoviridae family. Host range and specificity, burst size, lytic activity, and morphological characteristics of the phage were determined. Bioinformatic analysis of the Paenibacillus phage SV21 showed 77 coding sequences in its linear 44,949 bp dsDNA genome with a GC content of 39.33%. In this study, we analysed the genomes of all of the currently sequenced P. larvae phage genomes and classified them into five clusters and a singleton. According to molecular, morphological, and bioinformatics results, it was observed that API480 (podovirus), which was reported as a singleton in previous studies and public databases, and Paenibacillus phage SV21 phage could form a new cluster together

Sellitepe, Hasan Erdinc/0000-0001-5339-6940; Pannecouque, Christophe/0000-0002-1254-4473; Tatar, Esra/0000-0003-3490-8597; Kucukguzel, Ilkay/0000-0002-7188-1859; senkardes, sevil/0000-0002-0523-459X; BOZDEVECI, ARIF/0000-0002-0729-9143 WOS: 000376305300013 A series of 38 new acylhydrazones [3-40], derived from (2S)-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl] amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV and antimicrobial activity with the further aim to develop acylhydrazones carrying an amino acid side chain. All tested compounds possess stronger activity against gram (+) bacteria. Compound 23 was found active against methicillin-resistant Staphylococcus aureus (MRSA) with a MIC value of 3.9 mu g/mL. the MIC value of compound 30 against Enterococcus faecalis, Listeria monocytogenes, and Bacillus cereus was 8 mu g/mL. A computational study for prediction of ADME and drug-like properties (solubility, drug-likeness, and drug score) as well as potential toxicity profiles of compounds 2-40 was performed using the Molinspiration online property calculation toolkit and Osiris Property Explorer. As most of our compounds meet Lipinski's rule of five, they promise good solubility and permeability. According to Osiris calculations, the majority of our compounds are supposed to be nonmutagenic and nonirritating. Research Fund of Marmara UniversityMarmara University [SAG-A-060510-0109] This work was supported by the Research Fund of Marmara University, project number: SAG-A-060510-0109.

Enlightening effects of biocontrol agents as Trichoderma spp. to provide disease control by combating pathogens is an important alternative in agricultural crop production. To that end, 9 species of Hypocrea/ Trichoderma having green ascospores isolated from the soil that tea plants cultivated in are identified by ITS sequences and were found to be close relative of Trichoderma sect. Pachybasium (77%). Ethyl acetate extracts of fungal isolates exhibited the antimicrobial activity against to Vibrio sp, Serratia marcescens, Mycobacterium smegmatis and Bacillus cereus but no antifungal activity was detected. The highest level of inhibitory activity was observed against to M. smegmatis by Trichoderma harzianum ID4A, ID4B and ID6B. In dual culture test, all Trichoderma strains were found to be showing the highest inhibitory activity against to the plant pathogens Botrytis cinerea, Sclerotonia sclerotiorum and Rhizoctonia solani (AG3), but relatively low activity against to the entomopathogen fungi. Volatile metabolites of Trichoderma spp. caused maximum reduction in mycelial growth and sclerotial production. Tested strains showed the highest tolerance to the fungicide Dikozin, whereas the lowest tolerance was against to the Captan regardless of the dosage.

Maize is an agro-economically important crop and its global scale cultivation dates back to ancient times. It is vital to find organic solutions for the agricultural sustainability of maize. Trichoderma spp. is a cheap bio-control candidate having favorable effects on plant growth and enhances resistance to abiotic stresses. Herein, the effect of the endophytic fungus Trichoderma atroviride, our local isolate named ID20G (TaID20G), was evaluated in maize (Zea mays L.) seedlings under drought stress. The fungal strain was characterized based on the internal transcribed spacer (ITS) sequence of 5.8S rDNA. Relative water content, phenotypic characters of roots, antioxidant enzyme activity, hydrogen peroxide content, lipid peroxidation and chlorophyll fluorescence (Fv/Fm ratio) were recorded. Root colonization of TaID20G increased fresh and dry weight of maize roots under drought stress. Chlorophyll and carotenoid contents of seedlings were reduced by drought stress and membrane damage was high in uninoculated plants. Root colonization of TaID20G almost totally prevented increase in lipid peroxidation and reversed the changes caused by drought in pigment contents and photosystem efficiency. Antioxidant enzyme activity was induced and hydrogen peroxide (H2O2) content was less in response to drought stress in inoculated plants. Taken together, these data indicate that TaID20G inoculation could diminish the injurious effects of drought and might have a function in arranging resilience against stress by inducing antioxidant machinery. Low cost and effortless nature of Trichoderma-based formulas might be developed as crop protectors in drought-affected lands around the world, leading to an eco-friendly insight into the plant stress tolerance.