ABSTRACT
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.
Subject(s)
Aedes/physiology , Culex/physiology , Life History Traits , Animals , Color , Feeding BehaviorABSTRACT
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.
ABSTRACT
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.
Subject(s)
Adhesives/chemistry , Disulfides/chemistry , Dopamine/chemistry , Indoles/chemistry , Nanotechnology/methods , Polymers/chemistry , Proteins/chemistry , Animals , Biocompatible Materials/chemistry , Bivalvia , Buffers , Coated Materials, Biocompatible/chemistry , Doxorubicin/chemistry , Drug Delivery Systems , Glutathione/chemistry , Levodopa/chemistry , Spectroscopy, Fourier Transform Infrared , Surface Properties , Tissue Engineering/methods , Water/chemistryABSTRACT
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.
Subject(s)
Indenes/chemistry , Indenes/pharmacology , PPAR gamma/agonists , Structure-Activity RelationshipABSTRACT
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.
Subject(s)
Chemistry, Pharmaceutical/methods , Dipeptidyl-Peptidase IV Inhibitors , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Hydrazines/chemical synthesis , Animals , Crystallography, X-Ray , Drug Design , Glucagon-Like Peptide 1/metabolism , Hydrazines/pharmacology , Inhibitory Concentration 50 , Kinetics , Mice , Mice, Inbred C57BL , Models, Chemical , Molecular Conformation , Protein Structure, TertiaryABSTRACT
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.
Subject(s)
Dopamine Antagonists/chemical synthesis , Dopamine Antagonists/pharmacology , Isoxazoles/chemical synthesis , Isoxazoles/pharmacology , Receptors, Dopamine/metabolism , Dopamine Antagonists/metabolism , Isoxazoles/metabolism , Models, Molecular , Protein Binding , Receptors, Dopamine/chemistry , Structure-Activity RelationshipABSTRACT
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.
Subject(s)
Indenes/chemical synthesis , PPAR gamma/agonists , PPAR gamma/chemistry , Animals , Crystallography, X-Ray , Humans , Indenes/chemistry , Indenes/pharmacology , Ligands , Mice , Models, Molecular , Molecular Structure , NIH 3T3 CellsABSTRACT
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).
Subject(s)
Dipeptidyl Peptidase 4/drug effects , Protease Inhibitors/pharmacology , Pyrazoles/pharmacology , Animals , Magnetic Resonance Spectroscopy , Mass Spectrometry , Mice , Mice, Inbred C57BL , Protease Inhibitors/chemistry , Pyrazoles/chemistryABSTRACT
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.
Subject(s)
Dipeptidyl-Peptidases and Tripeptidyl-Peptidases/antagonists & inhibitors , Hypoglycemic Agents/chemical synthesis , Protease Inhibitors/chemical synthesis , Pyrazoles/chemical synthesis , Animals , Caco-2 Cells , Dipeptidyl-Peptidases and Tripeptidyl-Peptidases/metabolism , Humans , Hypoglycemic Agents/pharmacology , Mice , Mice, Inbred C57BL , Protease Inhibitors/pharmacology , Pyrazoles/pharmacology , Rats , SwineABSTRACT
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.
Subject(s)
Dopamine Antagonists/pharmacology , Dopamine D2 Receptor Antagonists , Isoxazoles/pharmacology , Thiophenes/pharmacology , Animals , Antipsychotic Agents/pharmacology , Benzamides/metabolism , Binding, Competitive , Body Temperature/drug effects , Catalepsy/chemically induced , Cell Line , Clozapine/pharmacology , Cocaine/pharmacology , Dopamine Agonists/pharmacology , Dose-Response Relationship, Drug , Haloperidol/pharmacology , Humans , Hypothermia/chemically induced , Isoxazoles/chemistry , Isoxazoles/metabolism , Male , Mice , Motor Activity/drug effects , Prolactin/blood , Psychomotor Performance/drug effects , Radioligand Assay , Rats , Rats, Sprague-Dawley , Receptors, Dopamine D2/genetics , Receptors, Dopamine D2/metabolism , Receptors, Dopamine D3 , Tetrahydronaphthalenes/pharmacology , Thiophenes/chemistry , Thiophenes/metabolism , TritiumABSTRACT
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.
