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1.
Med Vet Entomol ; 35(3): 333-351, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-33452827

RESUMO

Ticks are important vectors of emerging health problems in humans and animals. We conducted several field surveillances to investigate the fauna of hard ticks on domestic animals in seven governorates of Egypt during 2018-2019. A total of 3265 individual tick specimens were collected and identified to the species level; the specimens belong to 11 species within three genera (Amblyomma, Hyalomma, and Rhipicephalus). Tick infestation was highest in dromedary camels (70%), followed by dogs (52.5%), cattle (50%), buffaloes (38%), and horses (12%). Ten species were collected from dromedary camels, 2 from cattle, and one species from dogs, buffaloes, and horses. Diagnostic characters with high-quality photographic images of the 11 tick species were provided. New measurements of the body regions such as spiracles and body grooves were also obtained to provide further details on morphological variations among the diverse tick species. This study provided detailed descriptions of the genital apertures of five Hyalomma species. Morphological variations of male Hyalomma impeltatum, and genital apertures of female Hyalomma dromedarii and Hyalomma excavatum were also examined in this study. Finally, we provided additional details on local geographic distributions, hosts, endemicity status, and disease relationships of the eleven tick species.


Assuntos
Doenças dos Bovinos , Doenças do Cão , Doenças dos Cavalos , Ixodidae , Rhipicephalus , Infestações por Carrapato , Animais , Animais Domésticos , Bovinos , Doenças do Cão/epidemiologia , Cães , Egito , Feminino , Cavalos , Masculino , Infestações por Carrapato/epidemiologia , Infestações por Carrapato/veterinária
2.
Bioorg Chem ; 85: 349-356, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30658234

RESUMO

A series of dimeric melatonin analogues 3a-e obtained by connecting two melatonin molecules through the methoxy oxygen atoms with spacers spanning 16-24 atoms and the agomelatine dimer 7 were synthesized and characterized in 2-[125-I]-iodomelatonin binding assays, bioluminescence resonance energy transfer (BRET) experiments, and in functional cAMP and ß-arrestin recruitment assays at MT1 and MT2 receptors. The binding affinity of 3a-e generally increased with increasing linker length. Bivalent ligands 3a-e increased BRET signals of MT1 dimers up to 3-fold compared to the monomeric control ligand indicating the simultaneous binding of the two pharmacophores to dimeric receptors. Bivalent ligands 3c and 7 exhibited important changes in functional properties on the Gi/cAMP pathway but not on the ß-arrestin pathway compared to their monomeric counterparts. Interestingly, 3c (20 atoms spacer) shows inverse agonistic properties at MT2 on the Gi/cAMP pathway. In conclusion, these findings indicate that O-linked melatonin dimers are promising tools to develop signaling pathway-based bivalent melatonin receptor ligands.


Assuntos
Melatonina/análogos & derivados , Melatonina/farmacologia , Receptor MT1 de Melatonina/agonistas , Receptor MT2 de Melatonina/agonistas , Técnicas de Transferência de Energia por Ressonância de Bioluminescência , AMP Cíclico/metabolismo , Agonismo Inverso de Drogas , Células HEK293 , Humanos , Ligantes , Melatonina/metabolismo , Estrutura Molecular , Multimerização Proteica/efeitos dos fármacos , Receptor MT1 de Melatonina/metabolismo , Receptor MT2 de Melatonina/metabolismo , beta-Arrestinas/metabolismo
3.
Environ Sci Pollut Res Int ; 20(3): 1719-26, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22864756

RESUMO

Heavy metal contamination of agricultural soils has received great concern due to potential risk to human health. Cadmium and Pb are largely released from abandoned or closed mines in Korea, resulting in soil contamination. The objective of this study was to evaluate the effects of eggshell waste in combination with the conventional nitrogen, phosphorous, and potassium fertilizer (also known as NPK fertilizer) or the rapeseed residue on immobilization of Cd and Pb in the rice paddy soil. Cadmium and Pb extractabilities were tested using two methods of (1) the toxicity characteristics leaching procedure (TCLP) and (2) the 0.1 M HCl extraction. With 5 % eggshell addition, the values of soil pH were increased from 6.33 and 6.51 to 8.15 and 8.04 in combination with NPK fertilizer and rapeseed residue, respectively, compared to no eggshell addition. The increase in soil pH may contribute to heavy metal immobilization by altering heavy metals into more stable in soils. Concentrations of TCLP-extracted Cd and Pb were reduced by up to 67.9 and 93.2 % by addition of 5 % eggshell compared to control. For 0.1 M HCl extraction method, the concentration of 0.1 M HCl-Cd in soils treated with NPK fertilizer and rapeseed residue was significantly reduced by up to 34.01 and 46.1 %, respectively, with 5 % eggshell addition compared to control. A decrease in acid phosphatase activity and an increase in alkaline phosphatase activity at high soil pH were also observed. Combined application of eggshell waste and rapeseed residue can be cost-effective and beneficial way to remediate the soil contaminated with heavy metals.


Assuntos
Brassica rapa/química , Casca de Ovo/química , Recuperação e Remediação Ambiental/métodos , Metais Pesados/química , Poluentes do Solo/química , Animais , Cádmio/química , Poluição Ambiental , Concentração de Íons de Hidrogênio , Chumbo/química , Mineração
4.
Chemosphere ; 85(4): 677-82, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21764102

RESUMO

Rapeseed (Brassica napus L.) has been cultivated for biodiesel production worldwide. Winter rapeseed is commonly grown in the southern part of Korea under a rice-rapeseed double cropping system. In this study, a greenhouse pot experiment was conducted to assess the effects of rapeseed residue applied as a green manure alone or in combinations with mineral N fertilizer on Cd and Pb speciation in the contaminated paddy soil and their availability to rice plant (Oryza sativa L.). The changes in soil chemical and biological properties in response to the addition of rapeseed residue were also evaluated. Specifically, the following four treatments were evaluated: 100% mineral N fertilizer (N100) as a control, 70% mineral N fertilizer+rapeseed residue (N70+R), 30% mineral N fertilizer+rapeseed residue (N30+R) and rapeseed residue alone (R). The electrical conductivity and exchangeable cations of the rice paddy soil subjected to the R treatment or in combinations with mineral N fertilizer treatment, N70+R and N30+R, were higher than those in soils subjected to the N100 treatment. However, the soil pH value with the R treatment (pH 6.3) was lower than that with N100 treatment (pH 6.9). Use of rapeseed residue as a green manure led to an increase in soil organic matter (SOM) and enhanced the microbial populations in the soil. Sequential extraction also revealed that the addition of rapeseed residue decreased the easily accessible fraction of Cd by 5-14% and Pb by 30-39% through the transformation into less accessible fractions, thereby reducing metal availability to the rice plant. Overall, the incorporation of rapeseed residue into the metal contaminated rice paddy soils may sustain SOM, improve the soil chemical and biological properties, and decrease the heavy metal phytoavailability.


Assuntos
Brassica rapa/química , Cádmio/metabolismo , Chumbo/metabolismo , Metais Pesados/metabolismo , Oryza/metabolismo , Poluentes do Solo/metabolismo , Cádmio/análise , Produtos Agrícolas , Fertilizantes , Chumbo/análise , Metais Pesados/análise , Oryza/química , Folhas de Planta/química , Caules de Planta/química , Microbiologia do Solo , Poluentes do Solo/análise
5.
Drug Discov Ther ; 4(2): 77-84, 2010 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22491164

RESUMO

The aim of the present study was to improve the solubility, and therefore the dissolution of poorly water-soluble allopurinol. Solid dispersions of allopurinol were prepared with different polymers or carriers such as polyvinylpyrrolidone (PVP K30 and PVP K90), polyethylene glycol (PEG 4000 and PEG 6000), urea and mannitol at two drug : carrier ratios (1:1) and (1:2). Different methods such as melting and solvent evaporation methods were used to improve dissolution characteristics and solubility of allopurinol. The solid dispersions were characterized using a differential scanning calorimeter (DSC) and X-ray diffraction (XRD) while the interactions which took place were identified with fourier transform infrared (FTIR) spectroscopy. Due to formation of hydrogen bonds between allopurinol and urea and mannitol, a transition of allopurinol from the crystalline to amorphous state was achieved. The DSC thermograms of the solid dispersions indicated the potential of heat induced interactions between allopurinol and the carriers used could influence dissolution rate of the drug. The dissolution amount (%) of pure allopurinol was 80% at 45 min. F5, F3, F6, F7, and F1 showed better dissolution percentages of 100, 93, 92.4, 90.6, and 89%, respectively, at 45 min.


Assuntos
Alopurinol , Solubilidade , Varredura Diferencial de Calorimetria , Polietilenoglicóis/química , Povidona , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
6.
Drug Discov Ther ; 4(5): 380-7, 2010 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22491243

RESUMO

Ketoconazole (KZ), an imidazole antifungal, was formulated into inclusion complexes via coprecipitation and kneading with ß-cyclodextrin (ß-CD) as a carrier in 1:1 and 1:2 drug to carrier ratios. The KZ-ß-CD solid complexes were characterized by X-ray diffraction and differential scanning calorimetry (DSC). The diffraction pattern of the pure drug revealed the drug to be highly crystalline in nature, as indicated by numerous distinctive peaks. The lack of numerous distinctive peaks of the drug in KZ-ß-CD complexes prepared by the two methods revealed that a large number of the drug molecules were dissolved in a solid-state carrier matrix with an amorphous structure. The thermograms of the KZ-ß-CD complexes showed a strong reduction in the intensity and broadening of drug peaks somewhat in both kneading and coprecipitation systems, suggesting that the drug is monomolecularly dispersed in the ß-CD cavity. The prepared tablets of KZ-ß-CD solid complexes prepared by the two methods were evaluated for their quality control testing, and an in vitro release study and the results of quality control complied with pharmacopeial requirements and the release profiles indicated complete drug release after 30 min. The kinetic parameters obtained from release data were analyzed in order to explain the mechanism of drug release and revealed non-Fickian transport. Accelerated stability testing at 35°C, 45°C, and 55°C and at 75% relative humidity was carried out for six months and revealed somewhat stable systems as indicated by a t(90) of about 2 years for both KZ-ß-CD systems. A microbiological in vitro assay of KZ from the prepared tablets was performed using Candida albicans as a model fungus, and KZ had improved microbiological activity when administered as an inclusion complex with ß-CD. The results confirmed the benefit of using CDs as a useful tool to enhance the dissolution and hence bioavailability of poorly water-soluble drugs by forming solubilizing systems when exposed to gastrointestinal fluid.


Assuntos
Cetoconazol , beta-Ciclodextrinas , Varredura Diferencial de Calorimetria , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Comprimidos , Difração de Raios X
7.
Int J Pharm ; 279(1-2): 3-7, 2004 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-15234788

RESUMO

The purpose of this investigation was to evaluate the bioavailability of three salbutamol sulfate suppository formulations. The formulations were; 2 mg salbutamol sulfate in Suppocire NA base containing 6% Eudispert gel (F1), 2mg salbutamol sulfate in Witepsol H15 base containing 3% methyl cellulose gel (F2), and 2 mg salbutamol sulfate in Witepsol W25 base containing 3% methyl cellulose gel (F3). The formulations were administered via rectal route in six healthy male adult volunteers. The bioavailability of the three suppository formulations was compared with the oral bioavailability of salbutamol sulfate 2mg tablets (F4). Six volunteers participated in a four-way crossover study, where each study was separated from the other by an interval of 1 weak. Venous blood samples of 5 ml were taken immediately before dosing and after predetermined time intervals of 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6 and 8 h. The result showed that Cmax +/- S.D. observed were 12.96 +/- 2.11, 14.78 +/- 2.33, 10.02 +/- 1.42 and 11.51 +/- 1.22 ng ml(-1) for F1, F2, F3 and F4, respectively. The Tmax +/- S.D. were found to be 1.91 +/- 0.20, 1.83 +/- 0.26, 2.50 +/- 0.00 and 2.67 +/- 0.24 h for F1, F2, F3 and F4, respectively. AUC +/- S.D. values were 40.25 +/- 1.88, 42.16 +/- 1.55, 28.62 +/- 1.98 and 37.63 +/- 1.44 ng h per ml for F1, F2, F3 and F4, respectively. The relative bioavailabilities of the investigated formulations were 112.04, 106.96 and 76.06 for formula F2, F1 and F3, respectively, when compared with the oral preparation (F4). The finding indicates that the bioavailability of salbutamol sulfate can be enhanced by delivering it rectally with Suppocire NA base containing 6% Eudispert gel or with Witepsol W25 base containing 3% methyl cellulose to match that of oral tablets. Salbutamol sulfate can be rectally administered in patients who are less compliant with the oral administration.


Assuntos
Albuterol/administração & dosagem , Albuterol/farmacocinética , Adulto , Área Sob a Curva , Disponibilidade Biológica , Estudos Cross-Over , Humanos , Masculino , Pessoa de Meia-Idade , Veículos Farmacêuticos , Supositórios , Comprimidos
8.
Histopathology ; 14(2): 151-60, 1989 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-2468597

RESUMO

In this study using a panel of anticytokeratin antibodies and an indirect immunoperoxidase method, we examined cervical squamous epithelia including mature stratified epithelium, immature squamous metaplasia, CIN 1, 2 and 3, wart virus infection and squamous carcinoma. Changes from the normal patterns of staining were inconsistently seen in CIN 1 and 2, but in CIN 3 the changes were more marked, and consisted of a loss of stratification of the staining pattern and a patchy reduction in staining. Invasive carcinomas showed a similar staining pattern to CIN 3 lesions.


Assuntos
Carcinoma de Células Escamosas/metabolismo , Colo do Útero/metabolismo , Queratinas/metabolismo , Infecções Tumorais por Vírus/metabolismo , Doenças do Colo do Útero/metabolismo , Neoplasias do Colo do Útero/metabolismo , Carcinoma de Células Escamosas/patologia , Colo do Útero/patologia , Feminino , Humanos , Imuno-Histoquímica , Papillomaviridae , Infecções Tumorais por Vírus/patologia , Doenças do Colo do Útero/patologia , Neoplasias do Colo do Útero/patologia
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