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1.
An. acad. bras. ciênc ; 90(1): 401-414, Mar. 2018. tab
Artigo em Inglês | LILACS | ID: biblio-886923

RESUMO

ABSTRACT Two experiments (E) were carried out to evaluate the effects of fumaric acid and an acidifier blend [composed by calcium formate, calcium lactate and medium-chain fatty acids (capric and caprylic)] in piglet diets containing colistin (40 ppm) or halquinol (120 ppm) on performance, diarrhea incidence (E1), organs relative weight, pH values, intestinal morphometry and microbiota (E2). In E1, 192 and E2, 24 piglets weaned at 21-day-old were randomly assigned to blocks with 2x2 factorial arrangement of treatments [absence or presence of fumaric acid x absence or presence of acidifier blend], six replicates of eight (E1) and one piglet per pen (E2). For E1, the treatments were control (CD): no acidifier product + 40 ppm of colistin, FA: fumaric acid in absence of acidifier blend, AB: acidifier blend in absence of fumaric acid and, AF+AB: presence of fumaric acid and acidifier blend. For E2, the pre-starter I diet were used and the same treatments as E1 evaluated. No treatment effects (P>0.05) were observed on performance, diarrhea incidence (E1), gut pH values and duodenum morphometry of piglets (E2). However, the addition of AB increased (P<0.05) large intestine relative weight and, FA addition decreased (P<0.05) pancreas relative weight, jejunum villi height and, total coliform and E. coli counts in cecum. The inclusion of FA and AB in diets containing colistin or halquinol did not improve performance, although FA exerted an inhibitory effect on cecum microbiota.


Assuntos
Animais , Masculino , Suínos/crescimento & desenvolvimento , Cloroquinolinóis/administração & dosagem , Colistina/administração & dosagem , Suplementos Nutricionais/análise , Trato Gastrointestinal/fisiologia , Diarreia/veterinária , Ração Animal/análise , Suínos/fisiologia , Cloroquinolinóis/efeitos adversos , Colistina/efeitos adversos , Suplementos Nutricionais/efeitos adversos , Diarreia/induzido quimicamente , Fumaratos/administração & dosagem , Mucosa Intestinal/efeitos dos fármacos , Ração Animal/efeitos adversos , Antibacterianos/administração & dosagem
2.
An Acad Bras Cienc ; 90(1): 401-414, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29466480

RESUMO

Two experiments (E) were carried out to evaluate the effects of fumaric acid and an acidifier blend [composed by calcium formate, calcium lactate and medium-chain fatty acids (capric and caprylic)] in piglet diets containing colistin (40 ppm) or halquinol (120 ppm) on performance, diarrhea incidence (E1), organs relative weight, pH values, intestinal morphometry and microbiota (E2). In E1, 192 and E2, 24 piglets weaned at 21-day-old were randomly assigned to blocks with 2x2 factorial arrangement of treatments [absence or presence of fumaric acid x absence or presence of acidifier blend], six replicates of eight (E1) and one piglet per pen (E2). For E1, the treatments were control (CD): no acidifier product + 40 ppm of colistin, FA: fumaric acid in absence of acidifier blend, AB: acidifier blend in absence of fumaric acid and, AF+AB: presence of fumaric acid and acidifier blend. For E2, the pre-starter I diet were used and the same treatments as E1 evaluated. No treatment effects (P>0.05) were observed on performance, diarrhea incidence (E1), gut pH values and duodenum morphometry of piglets (E2). However, the addition of AB increased (P<0.05) large intestine relative weight and, FA addition decreased (P<0.05) pancreas relative weight, jejunum villi height and, total coliform and E. coli counts in cecum. The inclusion of FA and AB in diets containing colistin or halquinol did not improve performance, although FA exerted an inhibitory effect on cecum microbiota.


Assuntos
Ração Animal/análise , Cloroquinolinóis/administração & dosagem , Colistina/administração & dosagem , Diarreia/veterinária , Suplementos Nutricionais/análise , Trato Gastrointestinal/fisiologia , Suínos/crescimento & desenvolvimento , Ração Animal/efeitos adversos , Animais , Antibacterianos/administração & dosagem , Cloroquinolinóis/efeitos adversos , Colistina/efeitos adversos , Diarreia/induzido quimicamente , Suplementos Nutricionais/efeitos adversos , Fumaratos/administração & dosagem , Mucosa Intestinal/efeitos dos fármacos , Masculino , Suínos/fisiologia
3.
Bioorg Med Chem Lett ; 26(2): 545-550, 2016 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-26642767

RESUMO

A self-immolative γ-aminopropylsulfonate linker was investigated for use in the development of prodrugs that are reactive to various chemical or biological stimuli. To demonstrate their utility, a leucine-conjugated prodrug of 5-chloroquinolin-8-ol (5-Cl-8-HQ), which is a potent inhibitor against aminopeptidase from Aeromonas proteolytica (AAP), was synthesized. The sulfonate prodrug was considerably stable under physiological conditions, with only enzyme-mediated hydrolysis of leucine triggering the subsequent intramolecular cyclization to simultaneously release 5-Cl-8-HQ and form γ-sultam. It was also confirmed that this γ-aminopropylsulfonate linker was applicable for prodrugs of not only 8-HQ derivatives but also other drugs bearing a phenolic hydroxy group.


Assuntos
Aeromonas/enzimologia , Alcanossulfonatos/metabolismo , Aminopeptidases/antagonistas & inibidores , Cloroquinolinóis/metabolismo , Pró-Fármacos/metabolismo , Alcanossulfonatos/administração & dosagem , Alcanossulfonatos/síntese química , Aminopeptidases/metabolismo , Animais , Cloroquinolinóis/administração & dosagem , Ciclização , Humanos , Hidrólise , Leucina/análogos & derivados , Leucina/síntese química , Leucina/metabolismo , Fígado/metabolismo , Camundongos , Pró-Fármacos/administração & dosagem , Pró-Fármacos/síntese química , Propilaminas/síntese química , Propilaminas/metabolismo , Ratos , Sulfonamidas/química
4.
J Basic Clin Physiol Pharmacol ; 19(1): 15-27, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-19024792

RESUMO

The aim of the present study was to evaluate the effect of halquinol, an antimicrobial used as a growth promotor in poultry, on the fresh water fish Catla catla in terms of growth promotion, protein profile, and physiology as the rate of oxygen consumption. A synergic increment in the free amino acid level and total protein concentration suggested enhanced anabolic metabolism resulting in weight gain. When compared with an untreated control group, fishes treated with 0.1% halquinol (T1) showed a higher weight gain than those treated with 0.2% halquinol (T2). Variations in the rate of oxygen consumption among the three groups (control, T1, T2) expressed the physiological response of the animals toward the chemical along the time factor. After 7 days of treatment, the absence of halquinol revealed by post-withdrawal residual HPLC studies suggests its biosafety.


Assuntos
Carpas/metabolismo , Cloroquinolinóis/farmacologia , Consumo de Oxigênio/efeitos dos fármacos , Aumento de Peso/efeitos dos fármacos , Aminoácidos/efeitos dos fármacos , Aminoácidos/metabolismo , Animais , Carpas/crescimento & desenvolvimento , Cloroquinolinóis/administração & dosagem , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Resíduos de Drogas/análise , Resíduos de Drogas/metabolismo , Proteínas de Peixes/efeitos dos fármacos , Proteínas de Peixes/metabolismo , Índia , Fatores de Tempo
8.
Gynecol Invest ; 9(4): 166-9, 1978.
Artigo em Inglês | MEDLINE | ID: mdl-750325

RESUMO

The systemic absorption and the plasma concentrations of chloroquinaldol have been determined after local application of one vaginal tablet of Sterosan. A peak plasma concentration of 33 ng/ml was determined 12 h after application. A mean absorption of 6.0% of the applied dose was estimated.


Assuntos
Cloroquinolinóis/sangue , Hidroxiquinolinas/sangue , Absorção , Cloroquinolinóis/administração & dosagem , Cloroquinolinóis/metabolismo , Feminino , Humanos , Comprimidos , Vagina
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