RÉSUMÉ
Abstract Background: Organic acids and ammonium salts added to drinking water can optimize productivity of broiler chickens. Objective: To evaluate the effect of acidifying drinking water on productive performance, blood and intestinal pH, and intestinal morphology of broilers. Methods: 1,400 one-day-old broiler chicks were used to evaluate two pH levels (4 and 6) of drinking water during three periods (1-21, 1-28, and 1-42 days of age). The treatments consisted of water added with a blend of formic acid (31%), propionic acid (19%), and their salts ammonium formate (26%), and ammonium propionate (6%) compared to a control group (pH 8). Results: Compared to the control, the groups consuming water at pH 6 (0.038 moles) continuously for 42 days improved (p≤0.01) live weight (2.785 vs 2.691 kg), feed conversion ratio (1.430 vs 1.463 kg/kg), and increased the number of intestinal villi (59.0 vs 55.7). Additionally, blood and intestinal pH was reduced vs the control group (7.75 vs 7.89; 6.32 vs 6.41, respectively). Conclusion: The blend of formic and propionic acids and their ammonium salts in drinking water at pH 6 during the complete production cycle of broilers improves performance, increases the number of intestinal villi, and reduces the pH of blood, duodenum, and ileum.
Resumen Antecedentes: Agregar ácidos orgánicos y sus sales amoniacales en el agua de bebida de pollos de engorde puede optimizar su productividad. Objetivo: Evaluar el efecto de la acidificación del agua de bebida sobre el rendimiento productivo, pH sanguíneo e intestinal, y morfología intestinal del pollo de engorde. Métodos: Se utilizaron 1.400 pollos de engorde de un día de edad para evaluar dos niveles de pH (4 y 6) en agua de bebida durante tres períodos (1-21, 1-28 y 1-42 días de edad). Los tratamientos consistieron en agua con una mezcla de ácido fórmico (31%), ácido propiónico (19%) y sus sales formiato de amonio (26%) y propionato de amonio (6%) en comparación con un grupo control (pH 8). Resultados: En comparación con el control, los grupos que recibieron agua a pH 6 (0,038 moles) continuamente durante 42 días tuvieron mejor (p≤0,01) rendimiento en términos de peso vivo (2,785 vs 2,691 kg) y conversión alimenticia (1,430 vs 1,463 kg/kg) así como un mayor número de vellosidades intestinales (59,0 vs 55,7). Adicionalmente, el pH sanguíneo e intestinal disminuyó vs el grupo control (7,75 vs 7,89; 6,32 vs 6,41, respectivamente). Conclusión: La mezcla de ácidos fórmico y propiónico y sus sales de amonio en el agua de bebida a pH 6 durante todo el ciclo productivo mejora los parámetros productivos en pollos de engorde, aumenta el número de vellosidades intestinales y reduce el pH de la sangre, duodeno e íleon.
Resumo Antecedentes: Recomendações para a aplicação de mistura de ácidos orgânicos e sais de amônio na água potável são necessárias para otimizar a produtividade em frangos de corte. Objetivo: Avaliar o efeito da acidificação da água de bebida no desempenho produtivo, pH sanguíneo e intestinal e morfologia intestinal. Métodos: 1.400 pintos de corte entre 1 e 42 dias de idade foram utilizados para avaliar dois níveis de pH (4 e 6) na água de beber entre três períodos (1-21, 1-28 e 1-42 dias de idade) de tratamentos em água com uma mistura de ácido fórmico 31%, ácido propiônico 19%, e seus sais formato de amônio 26% e propionato de amônio 6% em relação ao controle (pH 8). Resultados: Os grupos que receberam água continuamente pH 6 (0,038 mols), por 42 dias tiveram melhor desempenho em relação ao controle (p≤0,01) em termos de peso vivo (2,785 vs 2,691 kg) e conversão alimentar (1,430 vs 1,463 kg/kg), bem como aumento do número de vilosidades intestinais (59,0 vs 55,7), sangue e pH intestinal reduzidos vs controle (7,75 vs 7,89; 6,32 vs 6,41). Conclusão: A mistura dos ácidos fórmico e propiônico e seus sais de amônio na água de bebida em pH 6 durante o ciclo completo de produção melhorou os parâmetros de produção em frangos de 42 dias de idade e aumentou o número de vilosidades intestinais e uma redução no sangue, duodeno, e pH do íleo.
RÉSUMÉ
@#To optimize the process of hydrogenation reduction in the synthesis of apremilast (APST), 3-nitrophthalic anhydride (4) and (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl) ethanamine-(S)-2-acetamido-4-methylpentanoate (7) were used as starting materials to synthesize (S)-2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-4-nitroisoindoline-1,3-dione (8) by amination.Then compound 8 was reduced to (S)-4-amino-2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl) ethyl) isoindoline-1,3-dione (9) with ammonium formate as hydrogen source and palladium hydroxide as catalyst.Finally, apremilast was obtained by the acetylation reaction with acetic anhydride.The structure of the products were verified by optical rotation, 1H NMR, 13C NMR, MS and elemental analysis.And the total yield of three steps was increased to 67.0%.The improved reduction process can avoid the special reaction of hydrogenation and pressurization, and reduce the safety risk and production costs with high commercial value.
RÉSUMÉ
The sigma-1 receptor (R) is a unique intracellular protein. R plays a major role in various pathological conditions in the central nervous system (CNS), implicated in several neuropsychiatric disorders. Imaging of R in the brain using positron emission tomography (PET) could serve as a noninvasively tool for enhancing the understanding of the disease's pathophysiology. Moreover, R PET tracers can be used for target validation and quantification in diagnosis. Herein, we describe the radiosynthesis, PET/CT imaging of novel R C-labeled radioligands based on 6-hydroxypyridazinone, [C]HCC0923 and [C]HCC0929. Two radioligands have high affinities to R, with good selectivity. In mice PET/CT imaging, both radioligands showed appropriate kinetics and distributions. Additionally, the specific interactions of two radioligands were reduced by compounds and (self-blocking). Of the two, [C]HCC0929 was further investigated in positive ligands blocking studies, using classic R agonist SA 4503 and R antagonist PD 144418. Both R ligands could extensively decreased the uptake of [C]HCC0929 in mice brain. Besides, the biodistribution of major brain regions and organs of mice were determined . These studies demonstrated that two radioligands, especially [C]HCC0929, possessed ideal imaging properties and might be valuable tools for non-invasive quantification of R in brain.