RESUMO
A cue for long-range vision allows mosquitoes to identify hosts and differentiate the ecological niches (e.g., habitats). However, the visual factors involved in attracting mosquitoes to a host are complex and have not been fully understood. Therefore, we assessed color preference to Aedes albopictus (Skuse) and Culex pipiens (Conquillett) as diurnal and nocturnal species, respectively, using seven fundamental colors including black, white, red, yellow, green, blue, and purple with each trap at 100 lux in a laboratory. We used a binary behavioral assay using the Mosquito Preference Index (MPI) as a preference ratio with a range of 0-1. Our analyses showed that Ae. albopictus had a greater response to black (MPIs, 0.7), followed closely by red, blue, and purple (MPIs, 0.6). We also found that red, blue, and purple were significantly higher (P < 0.05) than those of green (MPI, 0.5), white (MPI, 0.3), and yellow (MPI, 0.2). Similarly, the MPIs for Cx. pipiens were significantly higher at black and red (MPIs, 0.7; P < 0.05) compare to those of white and yellow (MPIs, 0.3; P < 0.05). The color preference of Ae. albopictus showed significant correlation to luminous intensities (L-value) (r = -0.640; P = 0.000) and blue intensities (b-value) (r = -0.372; P = 0.000) for all seven colors. In addition, Cx. pipiens negatively correlated (r = -0.703; P = 0.000) between color preference and L-value. Our analyses provide a greater understanding of how color plays a role in visual sensory stimuli, and how that could potentially affect mosquito host-seeking behavior.
Assuntos
Aedes/fisiologia , Culex/fisiologia , Características de História de Vida , Animais , Cor , Comportamento AlimentarRESUMO
To clarify the microscopic effects of solvents on the formation of the Li(+)-O2() process of a LiO2 battery, we studied the kinetics and thermodynamics of these ions in dimethyl sulfoxide (DMSO) and 1-ethyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide (EMI-TFSI) using classical molecular dynamics simulation. The force field for ionssolvents interactions was parametrized by force matching first-principles calculations. Despite the solvation energies of the ions are similar in both solvents, their mobility is much higher in DMSO. The free-energy profiles also confirm that the formation and decomposition rates of Li(+)-O2() pairs are greater in DMSO than in EMI-TFSI. Our atomistic simulations point out that the strong structuring of EMI-TFSI around the ions is responsible for these differences, and it explains why the LiO2 clusters formed in DMSO during the battery discharge are larger than those in EMI-TFSI. Understanding the origin of such properties is crucial to aid the optimization of electrolytes for LiO2 batteries.
RESUMO
Although the programmed degradation of biocompatible films finds applications in various fields including biomedical and bionanotechnological areas, coating methods have generally been limited to be substrate-specific, not applicable to any kinds of substrates. In this paper, we report a dopamine derivative, which allows for both universal coating of various substrates and stimuli-responsive film degradation, inspired by mussel-adhesive proteins. Two dopamine moieties are linked together by the disulfide bond, the cleavage of which enables the programmed film degradation. Mechanistic analysis of the degradable films indicates that the initial cleavage of the disulfide linkage causes rapid uptake of water molecules, hydrating the films, which leads to rapid degradation. Our substrate-independent coating of degradable films provides an advanced tool for drug delivery systems, tissue engineering, and anti-fouling strategies.
Assuntos
Adesivos/química , Dissulfetos/química , Dopamina/química , Indóis/química , Nanotecnologia/métodos , Polímeros/química , Proteínas/química , Animais , Materiais Biocompatíveis/química , Bivalves , Soluções Tampão , Materiais Revestidos Biocompatíveis/química , Doxorrubicina/química , Sistemas de Liberação de Medicamentos , Glutationa/química , Levodopa/química , Espectroscopia de Infravermelho com Transformada de Fourier , Propriedades de Superfície , Engenharia Tecidual/métodos , Água/químicaRESUMO
A series of novel indene N-oxide derivatives were prepared by various synthetic methods and evaluated for their ability to activate PPARgamma. The best PPARgamma agonist in this series was 9h, which showed an EC(50) value of 15 nM.
Assuntos
Indenos/química , Indenos/farmacologia , PPAR gama/agonistas , Relação Estrutura-AtividadeRESUMO
Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of beta-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3-amino-1-(2-benzoyl-1,2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography.
Assuntos
Química Farmacêutica/métodos , Inibidores da Dipeptidil Peptidase IV , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Hidrazinas/síntese química , Animais , Cristalografia por Raios X , Desenho de Fármacos , Peptídeo 1 Semelhante ao Glucagon/metabolismo , Hidrazinas/farmacologia , Concentração Inibidora 50 , Cinética , Camundongos , Camundongos Endogâmicos C57BL , Modelos Químicos , Conformação Molecular , Estrutura Terciária de ProteínaRESUMO
The asymmetric synthesis of chiral piperazinylpropylisoxazoline analogues, (R)-(+)-1, 2 and (S)-(-)-1, 2 was accomplished through a seven-step sequence of reactions, which involved asymmetric 1,3-dipolar cycloaddition, alkyl chain extension, and reductive amination as key reactions. Chiral ligands (R)-(+)-1, 2 exhibited the higher binding affinity and selectivity for the D(3) receptor over the D(4) receptor than (S)-(-)-1, 2 ligands.
Assuntos
Antagonistas de Dopamina/síntese química , Antagonistas de Dopamina/farmacologia , Isoxazóis/síntese química , Isoxazóis/farmacologia , Receptores Dopaminérgicos/metabolismo , Antagonistas de Dopamina/metabolismo , Isoxazóis/metabolismo , Modelos Moleculares , Ligação Proteica , Receptores Dopaminérgicos/química , Relação Estrutura-AtividadeRESUMO
Agonists of peroxisome proliferator-activated receptor gamma (PPAR gamma) are of interest as a treatment for diabetes, which prompted the identification of a new class of non-TZD PPAR gamma agonist. Moreover, compound 14c has displayed the most active agonistic activity with an EC50 value of 50 nM, in addition to exhibiting a new binding mode in the X-ray cocrystal structure.
Assuntos
Indenos/síntese química , PPAR gama/agonistas , PPAR gama/química , Animais , Cristalografia por Raios X , Humanos , Indenos/química , Indenos/farmacologia , Ligantes , Camundongos , Modelos Moleculares , Estrutura Molecular , Células NIH 3T3RESUMO
In the continuation of efforts to modify the structure of our novel DP-IV inhibitors, a series of pyrazolidine derivatives with heteroaryl urea was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV).
Assuntos
Dipeptidil Peptidase 4/efeitos dos fármacos , Inibidores de Proteases/farmacologia , Pirazóis/farmacologia , Animais , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Camundongos , Camundongos Endogâmicos C57BL , Inibidores de Proteases/química , Pirazóis/químicaRESUMO
A new series of cyano-pyrazoline derivatives with secondary amine at P-2 site was synthesized through achiral and chiral synthetic methods and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 5i revealed good in vivo efficacy (ED50: 4.1 mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent.
Assuntos
Dipeptidil Peptidases e Tripeptidil Peptidases/antagonistas & inibidores , Hipoglicemiantes/síntese química , Inibidores de Proteases/síntese química , Pirazóis/síntese química , Animais , Células CACO-2 , Dipeptidil Peptidases e Tripeptidil Peptidases/metabolismo , Humanos , Hipoglicemiantes/farmacologia , Camundongos , Camundongos Endogâmicos C57BL , Inibidores de Proteases/farmacologia , Pirazóis/farmacologia , Ratos , SuínosRESUMO
1-(2-ethoxy-phenyl)-4-[3-(3-thiophen-2-yl-isoxazolin-5-yl)-propyl]-piperazine (KCH-1110), has a high affinity for human dopamine D3 (hD3) receptor (Ki=1.28 nM) with about 90-fold selectivity over the human dopamine D2L (hD2L) receptor. Antipsychotic or antidopaminergic activity of KCH-1110 was investigated in the models for the positive symptoms of schizophrenia, apomorphine-induced climbing and cocaine-induced hyperlocomotion, in mice. Intraperitoneal (i.p.) or oral (p.o.) administration of KCH-1110 potently inhibited the apomorphine-induced cage climbing without any rotarod ataxia in mice. Cocaine-induced hyperactivity was also antagonised by KCH-1110. In addition, KCH-1110 attenuated the hypothermia induced by a selective dopamine D3 agonist, 7-OH-DPAT in mice. KCH-1110 did not induce catalepsy in mice, but at much higher doses only a slight catalepsy response was shown. Although high doses of KCH-1110 significantly enhanced serum prolactin secretion in rats, low dose of KCH-1110 did not increase prolactin levels in rats. The present studies, therefore, suggest that KCH-1110 is a potent and relatively selective dopamine D3 receptor antagonist with antipsychotic actions.
Assuntos
Antagonistas de Dopamina/farmacologia , Antagonistas dos Receptores de Dopamina D2 , Isoxazóis/farmacologia , Tiofenos/farmacologia , Animais , Antipsicóticos/farmacologia , Benzamidas/metabolismo , Ligação Competitiva , Temperatura Corporal/efeitos dos fármacos , Catalepsia/induzido quimicamente , Linhagem Celular , Clozapina/farmacologia , Cocaína/farmacologia , Agonistas de Dopamina/farmacologia , Relação Dose-Resposta a Droga , Haloperidol/farmacologia , Humanos , Hipotermia/induzido quimicamente , Isoxazóis/química , Isoxazóis/metabolismo , Masculino , Camundongos , Atividade Motora/efeitos dos fármacos , Prolactina/sangue , Desempenho Psicomotor/efeitos dos fármacos , Ensaio Radioligante , Ratos , Ratos Sprague-Dawley , Receptores de Dopamina D2/genética , Receptores de Dopamina D2/metabolismo , Receptores de Dopamina D3 , Tetra-Hidronaftalenos/farmacologia , Tiofenos/química , Tiofenos/metabolismo , TrítioRESUMO
A new series of 1,2-naphthoquinone derivatives was synthesized by various synthetic methods and evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B). 1,2-Naphthoquinone derivatives with substituent at R(4) position showed submicromolar inhibitory activity, and compound 24 demonstrated 10- to 60-fold selectivity against the tested phosphatases. Also, several 4-aryl-1,2-naphthoquinone derivatives with substituents at R(3), R(6), R(7), or/and R(8) showed submicromolar inhibitory activity and good plasma stability.