Plant-derived compounds as a tool for the control of gastrointestinal nematodes: Modulation of abamectin pharmacological action by carvone

The combination of synthetic anthelmintics and bioactive phytochemicals may be a pharmacological tool for improving nematode control in livestock. Carvone (R-CNE) has shown in vitro activity against gastrointestinal nematodes; however, the anthelmintic effect of bioactive phytochemicals either alone or combined with synthetic drugs has been little explored in vivo. Here, the pharmacological interaction of abamectin (ABM) and R-CNE was assessed in vitro and in vivo. The efficacy of this combination was evaluated in lambs naturally infected with resistant gastrointestinal nematodes. Additionally, the ligand and molecular docking of both molecules to P-glycoprotein (P-gp) was studied in silico. The presence of R-CNE produced a significant (p 90%. In vitro/in vivo pharmacoparasitological studies are relevant for the knowledge of the interactions and the efficacy of bioactive natural products combined with synthetic anthelmintics. While ADMET (absorption, distribution, metabolism, excretion, and toxicity) predictions and the molecular docking study showed a good interaction between ABM and P-gp, R-CNE does not appear to modulate this efflux protein. Therefore, the pharmacokinetic–pharmacodynamic effect of R-CNE on ABM should be attributed to its effect on membrane permeability. The development of pharmacology-based information is critical for the design of successful strategies for the parasite control.Fil: Miró, María Victoria. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; ArgentinaFil: Luque, Sonia Elisabet. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; ArgentinaFil: Cardozo, Patricia Alejandra. Instituto Nacional de Tecnología Agropecuaria. Centro Regional Buenos Aires Sur. Estación Experimental Agropecuaria Balcarce. Agencia de Extensión Rural Balcarce; ArgentinaFil: Lloberas, Maria Mercedes. Instituto Nacional de Tecnología Agropecuaria. Centro Regional Buenos Aires Sur. Estación Experimental Agropecuaria Balcarce. Agencia de Extensión Rural Balcarce; ArgentinaFil: Sousa, Dauana Mesquita. Universidade Federal Do Maranhao; BrasilFil: Soares, A.M.S.. Universidade Federal Do Maranhao; BrasilFil: Costa Junior, Livio Martins. Universidade Federal Do Maranhao; BrasilFil: Virkel, Guillermo Leon. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; ArgentinaFil: Lifschitz, Adrian Luis. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentin

Chromone derivatives and other constituents from cultures of the marine sponge-associated fungus penicillium erubescens KUFA0220 and their antibacterial activity

A previously unreported chromene derivative, 1-hydroxy-12-methoxycitromycin (1c), and four previously undescribed chromone derivatives, including pyanochromone (3b), spirofuranochromone (4), 7-hydroxy-6-methoxy-4-oxo-3-[(1E)-3-oxobut-1-en-1-yl]-4H-chromene-5-carboxylic acid (5), a pyranochromone dimer (6) were isolated, together with thirteen known compounds: β-sitostenone, ergosterol 5,8-endoperoxide, citromycin (1a), 12-methoxycitromycin (1b), myxotrichin D (1d), 12-methoxycitromycetin (1e), anhydrofulvic acid (2a), myxotrichin C (2b), penialidin D (2c), penialidin F (3a), SPF-3059-30 (7), GKK1032B (8) and secalonic acid A (9), from cultures of the marine sponge- associated fungus Penicillium erubescens KUFA0220. Compounds 1a-e, 2a, 3a, 4, 7-9, were tested for their antibacterial activity against Gram-positive and Gram-negative reference and multidrug-resistant strains isolated from the environment. Only 8 exhibited an in vitro growth inhibition of all Gram-positive bacteria whereas 9 showed growth inhibition of methicillin-resistant Staphyllococus aureus (MRSA). None of the compounds were active against Gram-negative bacteria tested. © 2018 MDPI. All Rights Reserved.Funding: This research was funded by Fundação para a Ciências e Tecnologia (FCT) (grant number POCI-01-0145-FEDER-016790) and North Portugal Regional Operational Programme (NORTE 2020)(grant number NORTE-01-0145-FEDER-000035). Acknowledgments: This work was partially supported through national funds provided by FCT/MCTES-Foundation for Science and Technology from the Minister of Science, Technology and Higher Education (PIDDAC) and European Regional Development Fund (ERDF) through the COMPETE—Programa Operacional Factores de Competitividade (POFC) programme, under the project PTDC/MAR-BIO/4694/2014 (reference POCI-01-0145-FEDER-016790; Project 3599-Promover a Produção Científica e Desenvolvimento Tecnológico e a Constituição de Redes Temáticas (3599-PPCDT)) in the framework of the programme PT2020 as well as by the project INNOVMAR-Innovation and Sustainability in the Management and Exploitation of Marine Resources (reference NORTE-01-0145-FEDER-000035, within Research Line NOVELMAR), supported by North Portugal Regional Operational Programme (NORTE 2020), under the PORTUGAL 2020 Partnership Agreement, through the European Regional Development Fund (ERDF). Decha Kumla thanks the Alfabet Project of the Erasmus Mundus for a PhD’s scholarship. We thank Júlia Bessa and Sara Cravo for technical support

Bis-indolyl benzenoids, hydroxypyrrolidine derivatives and other constituents from cultures of the marine sponge-associated fungus aspergillus candidus KUFA0062

A previously unreported bis-indolyl benzenoid, candidusin D (2e) and a new hydroxypyrrolidine alkaloid, preussin C (5b) were isolated together with fourteen previously described compounds: palmitic acid, clionasterol, ergosterol 5,8-endoperoxides, chrysophanic acid (1a), emodin (1b), six bis-indolyl benzenoids including asterriquinol D dimethyl ether (2a), petromurin C (2b), kumbicin B (2c), kumbicin A (2d), 2”-oxoasterriquinol D methyl ether (3), kumbicin D (4), the hydroxypyrrolidine alkaloid preussin (5a), (3S, 6S)-3,6-dibenzylpiperazine-2,5-dione (6) and 4-(acetylamino) benzoic acid (7), from the cultures of the marine sponge-associated fungus Aspergillus candidus KUFA 0062. Compounds 1a, 2a–e, 3, 4, 5a–b, and 6 were tested for their antibacterial activity against Gram-positive and Gram-negative reference and multidrug-resistant strains isolated from the environment. Only 5a exhibited an inhibitory effect against S. aureus ATCC 29213 and E. faecalis ATCC29212 as well as both methicillin-resistant S. aureus (MRSA) and vancomycin-resistant enterococci (VRE) strains. Both 1a and 5a also reduced significant biofilm formation in E. coli ATCC 25922. Moreover, 2b and 5a revealed a synergistic effect with oxacillin against MRSA S. aureus 66/1 while 5a exhibited a strong synergistic effect with the antibiotic colistin against E. coli 1410/1. Compound 1a, 2a–e, 3, 4, 5a–b, and 6 were also tested, together with the crude extract, for cytotoxic effect against eight cancer cell lines: HepG2, HT29, HCT116, A549, A 375, MCF-7, U-251, and T98G. Except for 1a, 2a, 2d, 4, and 6, all the compounds showed cytotoxicity against all the cancer cell lines tested. © 2018 by the authorsAcknowledgments: This work was partially supported through national funds provided by the FCT/MCTES-Foundation for Science and Technology from the Minister of Science, Technology and Higher Education (PIDDAC) and European Regional Development Fund (ERDF) through the COMPETE—Programa Operacional Factores de Competitividade (POFC) programme, under the project PTDC/MAR-BIO/4694/2014 (reference POCI-01-0145-FEDER-016790; Project 3599-Promover a Produção Científica e Desenvolvimento Tecnológico e a Constituição de Redes Temáticas (3599-PPCDT)) in the framework of the program PT2020 as well as by the project INNOVMAR-Innovation and Sustainability in the Management and Exploitation of Marine Resources (reference NORTE-01-0145-FEDER-000035, within Research Line NOVELMAR), supported by North Portugal Regional Operational Program (NORTE 2020), under the PORTUGAL 2020 Partnership Agreement, through the European Regional Development Fund (ERDF). We thank Júlia Bessa and Sara Cravo for technical support

Kaon properties in (proto)neutron stars

The modification on kaon and antikaon properties of in the interior of (proto-)neutron stars is investigated using a chiral SU(3) model. The parameters of the model are fitted to nuclear matter saturation properties, baryon octet vacuum masses, hyperon optical potentials and low energy a kaon-nucleon scattering lengths. We study the kaon/antikaon medium modification and explore the possibility of antikaon condensation in (proto-)neutron star matter at zero as well as finite temperature/entropy and neutrino content. The effect of hyperons on kaon and antikaon optical potentials is also investigated at different stages of the neutron star evolution.Comment: 17 pages including 4 figure

Photosynthesis, stomatal conductance and leaf water potential in crabwood (Carapa guianensis)

Leaf water potential is one of the most important factors affecting stomatal functioning. The aim of this study was to assess the effect of variation in diurnal irradiance and vapour pressure deficit on photosynthesis (A), stomatal conductance (g s) and leaf water potential (psi) in Carapa guianensis (Aubl.). Data were collected from 07:00 to 17:00 h. Photosynthetic rates reached a maximum (2.5 µmol m-2 s-1) at 10:00 h, thereafter declined to a minimum of 1 µmol m-2 s-1 at 16:00 h. Stomatal conductance oscillated during the day, from 0.04 mol m-2 s-1 (at midday) to 0.02.mol.m-2.s-1 at the end of the afternoon. Leaf water potential was higher early in the morning (-0.3 MPa) and lower (-0.75 MPa) at mid-afternoon (14:30 -15:00 h). After reaching a minimum, psi increased up to -0.64 MPa at sunset. Photosynthetic rates increased linearly as a function of g s (P < 0.01). Also there was a positive relationship between psi and g s (P< 0.01). Photosynthetic rates declined during the day after reaching a peak early in the morning, which makes clear that environmental factors that influence psi greatly affect carbon assimilation of C. guianensis.O potencial hídrico da folha é um dos fatores mais importantes que afetam o funcionamento dos estômatos. O objetivo deste trabalho foi avaliar o efeito da variação diurna na irradiância e déficit de pressão de vapor (DPV) na fotossíntese (A), condutância estomática (g s) e potencial hídrico da folha (psi) em Carapa guianensis (Aubl.). Os dados foram coletados de 07:00 às 17:00 h. A taxa fotossintética atingiu um valor máximo (2,5 µmol m-2 s-1) às 10:00 h, depois declinou até atingir um mínimo de 1 µmolm-2 s-1 às 16:00 h. A condutância estomática oscilou durante o dia, de 0,04 molm-2s-1 (ao meio dia) para 0,02 molm-2s- 1 no final da tarde. O potencial hídrico da folha foi máximo nas primeiras horas do dia (-0,3 MPa) e mínimo (-0,75 MPa) no meio da tarde (14:30 a 15:00 h). Após ter alcançado um mínimo, o psi aumentou até -0,64 MPa no fim da tarde. A taxa fotossintética aumentou linearmente em função do g s (P < 0,01). Também houve uma relação positiva entre psi e g s (P < 0,01). A taxa fotossintética declinou durante o dia após ter alcançado um pico no início da manhã, demonstrando que os fatores ambientais que afetam o psi têm efeito significativo na assimilação do carbono de C. guianensis