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1.
Avian Pathol ; : 1-12, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38529824

RESUMO

Coccidiosis, caused by parasites of the genus Eimeria, is a significant economic burden to the poultry industry. In this study, we conducted a comprehensive analysis to evaluate the financial losses associated with Eimeria infection in chickens in Algeria, relying on data provided by key stakeholders in the Algerian poultry industry to assess sub-clinical as well as clinical impact. We employed the updated 2020 version of a model established to estimate the cost of coccidiosis in chickens, taking into consideration specific cultural and technical aspects of poultry farming in Algeria. The findings predict economic losses due to coccidiosis in chickens of approximately £86.7 million in Algeria for the year 2022, representing £0.30 per chicken raised. The majority of the cost was attributed to morbidity (74.9%), emphasizing the substantial economic impact of reduced productivity including decreased bodyweight gain and increased feed conversion ratio. Costs associated with control measures made up 20.5% of the total calculated cost, with 4.6% of the cost related to mortality. These figures provide a clear indication of the scope and economic impact of Eimeria infection of chickens in Algeria, illustrating the impact of practices common across North Africa. They underscore the ongoing requirement for effective preventive and control measures to reduce these financial losses while improving productivity and welfare, ensuring the economic sustainability of the Algerian poultry industry.

2.
Bioorg Chem ; 150: 107598, 2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-38959645

RESUMO

A completely green protocol was developed for the synthesis of a series of arylaminonaphthol derivatives in the presence of N-ethylethanolamine (NEEA) as a catalyst under ultrasonic irradiation and solventless conditions. The major assets of this methodology were the use of non-toxic organic medium, available catalyst, mild reaction condition, and good to excellent yield of desired products. All of the synthesized products were screened for their in vitro antioxidant activity using DPPH, ABTS, and Ferric-phenanthroline assays and it was found that most of them are potent antioxidant agents. Also, their butyrylcholinesterase inhibitory activity has been investigated in vitro. All tested compounds exhibited potential inhibitory activity toward BuChE when compared to standard reference drug galantamine, however, compounds 4r, 4u, 4 g and 4x gave higher butyrylcholinesterase inhibitory with IC50 values of 14.78 ± 0.65 µM, 16.18 ± 0.50 µM, 20.00 ± 0.50 µM, and 20.28 ± 0.08 µM respectively. On the other hand, we employed density functional theory (DFT), calculations to analyze molecular geometry and global reactivity descriptors, and MESP analysis to predict electrophilic and nucleophilic attacks. A quantitative structure-activity relationship (QSAR) investigation was conducted on the antioxidant and butyrylcholinesterase properties of 25 arylaminonaphthol derivatives, resulting in robust and satisfactory models. To evaluate their anti-Alzheimer's activity, compounds 4 g, 4q, 4r, 4u, and 4x underwent docking simulations at the active site of the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), revealing why these compounds displayed superior activity, consistent with the biological findings.

3.
Acta Parasitol ; 67(3): 1393-1400, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35869337

RESUMO

PURPOSE: This study aimed to develop a rapid spectrophotometric method for counting coccidian oocysts in broilers feces, based on a standard count method "Malassez cell". METHODS: Therefore, a raw suspension containing purified oocysts of Eimeria known to parasitize broiler chicken was used. Five concentrations of oocyst suspensions were prepared, and three series of counts using the proposed method were compared with the conventional protocol using Malassez cell to quantify oocysts. Calibration curves were drawn to correlate the specific absorbance measurement at 550 nm and the number of coccidian oocysts quantified using Malassez cell counting (oocysts mL-1). RESULTS: The obtained results allowed to establish a formula for an easy estimation of the cell count based on their respective absorbance. The developed method can be used not only for the in vitro evaluation of the anticoccidian activity of natural or synthetic substances, but also for assessing oocysts production and the level of coccidian infection in broilers. CONCLUSION: The estimation formula has been found to be satisfactory and useful for a wide range of Eimeria oocyst suspension, offering a methodology with high potential for automation in anticoccidian tests in vivo and in vitro.


Assuntos
Coccidiose , Eimeria , Doenças das Aves Domésticas , Animais , Galinhas , Coccidiose/diagnóstico , Coccidiose/veterinária , Fezes , Oocistos , Doenças das Aves Domésticas/diagnóstico
4.
AIMS Microbiol ; 8(3): 318-337, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36317006

RESUMO

This study was designed to investigate, at a laboratory scale, the possibility of valorizing the leftover carob fruits to produce the eco-friendly biopolymer polyhydroxybutyrate (PHB) by using the bacterial strain Bacillus paramycoides, which has been isolated from the botanical garden of Skikda University in Algeria. The PHB production was tested under various conditions: a pH of 3-8, temperature range of 30-44 °C, carob extracted molasses concentration of 2-8% v/v, an incubation time of 24-96 h and an agitation speed of 150-300 rpm. The effects of different nitrogen sources and carob extracted molasses treatment types were also investigated. The PHB concentration was determined quantitatively as crotonic acid by measuring the absorbance at 300 nm. Cell growth was quantified by measuring the density of the culture at 600 nm. The presence of PHB was confirmed by applying high-performance liquid chromatography (HPLC) using an Aminex HPX-87H and implementing gas chromatography analysis. The best yield of PHB synthesis was obtained by using 6% v/v of 5 M H2SO4 treated with carob molasses as a carbon source, with peptone as a nitrogen source; incubation was conducted at 37 °C for 96 h at an agitation speed of 300 rpm (114.95 mg/L). The HPLC analysis confirmed the synthesis of PHB by B. paramycoides to have a chromatogram retention time of 22.5 min. Carob waste was successfully valorized to PHB.

5.
Eur J Med Chem ; 184: 111772, 2019 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-31630055

RESUMO

The membrane transporter BCRP/ABCG2 has emerged as a privileged biological target for the development of small compounds capable of abolishing multidrug resistance. In this context, the chromone skeleton was found as an excellent scaffold for the design of ABCG2 inhibitors. With the aims of optimizing and developing more potent modulators of the transporter, we herewith propose a multidisciplinary medicinal chemistry approach performed on this promising scaffold. A quantitative structure-activity relationship (QSAR) study on a series of chromone derivatives was first carried out, giving a robust model that was next applied to the design of 13 novel compounds derived from this nucleus. Two of the most active according to the model's prediction, namely compounds 22 (5-((3,5-dibromobenzyl)oxy)-N-(2-(5-methoxy-1H-indol-3-yl)ethyl)-4-oxo-4H-chromene-2-carboxamide) and 31 (5-((2,4-dibromobenzyl)oxy)-N-(2-(5-methoxy-1H-indol-3-yl)ethyl)-4-oxo-4H-chromene-2-carboxamide), were synthesized and had their biological potency evaluated by experimental assays, confirming their high inhibitory activity against ABCG2 (experimental EC50 below 0.10 µM). A supplementary docking study was then conducted on the newly designed derivatives, proposing possible binding modes of these novel molecules in the putative ligand-binding site of the transporter and explaining why the two aforementioned compounds exerted the best activity according to biological data. Results from this study are recommended as references for further research in hopes of discovering new potent inhibitors of ABCG2.


Assuntos
Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/antagonistas & inibidores , Cromonas/farmacologia , Simulação de Acoplamento Molecular , Proteínas de Neoplasias/antagonistas & inibidores , Relação Quantitativa Estrutura-Atividade , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo , Células Cultivadas , Cromonas/síntese química , Cromonas/química , Relação Dose-Resposta a Droga , Células HEK293 , Humanos , Estrutura Molecular , Proteínas de Neoplasias/metabolismo
6.
Acta Crystallogr C Struct Chem ; 74(Pt 4): 411-417, 2018 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-29620023

RESUMO

Due to their rich structural chemistry and wide variety of applications, borate materials have provided a rich area of research. In a continuation of this research, diethylammonium bis(2-oxidobenzoato-κ2O1,O2)borate, C4H12N+·BO4(C7H4O)2-, (1), and propylammonium bis(2-oxidobenzoato-κ2O1,O2)borate, C3H10N+·BO4(C7H4O)2-, (2), have been synthesized by the reaction of boric acid with salicylic acid under ambient conditions. In both structures, the B atom exhibits a slightly distorted tetrahedral environment formed by the bidentate coordination of two salicylate anions via the O atoms of the central carboxylate and oxide groups. In the crystals of salts (1) and (2), mixed cation-anion layers lying parallel to the (101) plane are formed through N-H...O, C-H...O and C-H...π/N-H...O hydrogen-bonding interactions, resulting, in each case, in a two-dimensional supramolecular architecture in the solid state. The photoluminescence properties of the salts were studied using the as-synthesized samples and reveal that salts (1) and (2) both display a strong blue-light emission, with maxima at 489 and 491 nm, respectively. In DFT/TD-DFT (time-dependent density functional theory) studies, the blue emission appears to be derived from an intramolecular charge transfer (ICT) excited state. In addition, IR and UV-Vis spectroscopies were used to investigate the title salts.

7.
Acta Crystallogr E Crystallogr Commun ; 74(Pt 8): 1042-1048, 2018 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-30116558

RESUMO

The synthesis and characterization of di-aqua-bis-[2-(2-hy-droxy-eth-yl)pyridine-κ2N,O)nickel(II) dinitrate, [Ni(C7H9NO)2(H2O)2](NO3)2, under ambient conditions is reported and compared with catena-poly[[bis-[2-(2-hy-droxy-eth-yl)pyridine-κ2N,O]copper(II)]-µ-sulfato-κ2O:O'], [Cu(C7H9NO)2(SO4)] n [Zegh-ouan et al. (2016 ▸). Private communication (refcode 1481676). CCDC, Cambridge, England]. In the two complexes, the 2-(2-hy-droxy-eth-yl)pyridine ligands coordinate the metal ions through the N atom of the pyridine ring and the O atom of the hy-droxy group, creating a chelate ring. The NiII or CuII ion lies on an inversion centre and exhibits a slightly distorted MO4N2 octa-hedral coordination geometry, build up by O and N atoms from two 2-(2-hy-droxy-eth-yl)pyridine ligands and two water mol-ecules or two O atoms belonging to sulfate anions. The sulfate anion bridges the CuII ions, forming a polymeric chain. The photoluminescence properties of these complexes have been studied on as-synthesized samples and reveal that both compounds display a strong blue-light emission with maxima around 497 nm. From DFT/TDDFT studies, the blue emission appears to be derived from the ligand-to-metal charge-transfer (LMCT) excited state. In addition, the IR spectroscopic properties and thermogravimetric behaviours of both complexes have been investigated.

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