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1.
Bratisl Lek Listy ; 114(6): 303-7, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23731039

RESUMO

BACKGROUND AND AIM: Under physiological conditions, maintenance of skeletal mass is the result of a tightly coupled process of bone formation and bone resorption. Disease states, osteoporosis included, arise when this delicate balance is disrupted, such as in menopause. The aim of the present work was to study the effect of leptin supplementation on bone metabolism in ovariectomized adult female rats by measuring indices of bone biomarkers. METHODS: Forty adult female albino rats were chosen as an animal model for this study and divided into the four equal groups (n=10/group): Group I (control SHAM-operated group) received a single dose of buffer solution i.p. daily for eight weeks. Group II (ovariectomy group) received a single dose of buffer solution i.p. daily for eight weeks. Group III (alendronate group): Ovariectomized rats that received alendronate 0.1 mg/kg body weight i.p. daily for eight weeks. Group IV (leptin group): Ovariectomized rats that received leptin (10 µg/kg body weight) i.p. daily for eight weeks. The obtained serum is required for determination of: Serum osteocalcin, alkaline phosphatase, calcium and phosphorous levels. RESULTS: The obtained data revealed that treatment with alendronate or leptin caused a significant decrease of serum osteocalcin, specific bone alkaline phosphatase and urinary deoxypyridinoline levels compared to ovariectomy group, and there was no significant difference between both drugs. CONCLUSION: Leptin prevents ovariectomy induced increases in bone turnover in rats. Leptin therapy has a significant effect in treatment of ovariectomy induced osteoporosis in rats (Tab. 1, Ref. 32).


Assuntos
Alendronato/farmacologia , Alendronato/uso terapêutico , Biomarcadores/sangue , Osso e Ossos/efeitos dos fármacos , Osso e Ossos/metabolismo , Leptina/farmacologia , Leptina/uso terapêutico , Ovariectomia , Animais , Feminino , Ratos , Ratos Sprague-Dawley
2.
J Enzyme Inhib Med Chem ; 23(4): 483-92, 2008 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-18665995

RESUMO

Quinazolinone derivatives have been studied as both in vitro and in vivo inhibitors of aspartate transcarbamylase (ATCase). In vitro treatment of mammalian ATCase with four compounds revealed that they inhibited enzyme activity and that 2-phenyl-1,3-4(H)benzothiazin-4-thione was the most potent one. This compound acts as a noncompetitive inhibitor towards both aspartate and carbamoyl phosphate. The values of the inhibition constant (K(i)) indicate that this compound exerts a potent inhibitory effect upon ATCase activity. Moreover, in vivo treatment with different doses of these derivatives showed also an inhibitory effect upon ATCase, the relative activity being decreased by 40%-58% with a 1 mg dose. These data support the inhibition of ATCase by quinazolinone derivatives as a new type of inhibitor for the enzyme.


Assuntos
Antifúngicos/farmacologia , Aspartato Carbamoiltransferase/antagonistas & inibidores , Quinazolinonas/farmacologia , Animais , Antifúngicos/síntese química , Aspartato Carbamoiltransferase/metabolismo , Células Cultivadas , Cinética , Quinazolinonas/síntese química
3.
J Biochem Mol Biol ; 37(2): 223-8, 2004 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-15469699

RESUMO

The levels of arylsulfatases A and B, alpha-amylase, aspartate transcarbamylase, and gamma-glutamyl transpeptidase were investigated during the infection of mice with schistosoma mansoni. This infection caused a significant (p < 0.001) increase in the activity of hepatic arylsulfatase B (ASB), aspartate transcarbamylases and gamma-glutamyl transpeptidase. A non-significant difference occurred for alpha-amylase (p < 0.3) and arylsulfatase A (p > 0.5) when compared to the control. The specific activity of hepatic ASB was progressively increased with the progression of the Schistosoma-infection. Moreover, the kinetic studies of hepatic ASB in Schistosoma-infection showed that a slight decrease in the value of K(m) and about a 40% increase in V(max) when compared to the control. In addition, the pH optimum of hepatic ASB was altered from 6 to 7 as a result of schistosomiasis. These observations suggest that there are schistosomiasis-associated changes of the catalytic and kinetic properties of hepatic ASB.


Assuntos
Aspartato Carbamoiltransferase/metabolismo , Cerebrosídeo Sulfatase/metabolismo , N-Acetilgalactosamina-4-Sulfatase/metabolismo , Esquistossomose/enzimologia , alfa-Amilases/metabolismo , gama-Glutamiltransferase/metabolismo , Animais , Catálise , Estabilidade Enzimática , Concentração de Íons de Hidrogênio , Cinética , Fígado/enzimologia , Hepatopatias Parasitárias/enzimologia , Masculino , Camundongos , Schistosoma mansoni/parasitologia , Temperatura
4.
J Environ Sci Health B ; 37(5): 475-84, 2002 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-12369764

RESUMO

The effect of three species of hypoglycemic herbs (Termis, Halfa barr, or Kammun Quaramany) on the lipid profile was investigated in plasma and liver tissues of diabetic and herbs-treated diabetic rats. This profile includes total lipids (TL), triglycerides (TG), cholesterol, high-density lipoprotein (HDL) and low-density lipoprotein (LDL). A dose of 1.5 ml of aqueous suspension of each herb/100 g body weight (equivalent to 75 mg/100 g body weight) was orally administered daily to alloxan-diabetic rats for four weeks. The present study showed 2-fold increase (p<0.05) in the plasma glucose level of diabetic rats, which received alloxan as a single dose of 120 mg/kg body weight, relative to the mean value of control group. This elevated glucose level was restored to its normal level after treatment with any one of the three herbs. Furthermore, the levels of TL, TG, cholesterol, LDL and VLDL were significantly (p<0.05) increased in the plasma and the liver tissues of diabetic rats compared to the control group, whereas HDL level was significantly (p<0.05) decreased. The plasma levels of all above parameters were normalized after treatment of the diabetic rats with Kammun Quaramany. Treatment of diabetic rats with Tennis normalized TG, cholesterol, LDL and VLDL levels, but Halfa barr restored the induced levels of plasma cholesterol, LDL and HDL to their normal levels. On the other hand, treatment with any of the three herbal suspensions could not restore the concentrations of the all tested parameters in the liver. These data demonstrated that the glycemic control of any of the three herbal suspensions was associated with their hypocholesterolemic effects on the hypercholesterolemia of the alloxan-induced diabetic rats. Moreover, the Kammun Quaramany showed the most potent effect.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Lipídeos/sangue , Fígado/química , Fitoterapia , Extratos Vegetais/uso terapêutico , Plantas Medicinais , Animais , Glicemia/análise , Glicemia/efeitos dos fármacos , Lipídeos/análise , Fígado/metabolismo , Lupinus , Masculino , Poaceae , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Zygophyllum
5.
Toxicology ; 170(3): 221-8, 2002 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-11788159

RESUMO

The present study was carried out to investigate the effects of Lupinus albus, L. (Lupinus termis), family L. leguminosae, Cymbopogon proximus, (Halfa barr), family Gramineae, and Zygophyllum coccineum L. (Kammun quaramany), family L. Zygophyllacae on biochemical parameters in alloxan-induced diabetic rats. A dose of 1.5 ml of aqueous suspension of each herb/100 g body weight (equivalent to 75 mg/100 g b.wt.) was orally administered daily to alloxan-diabetic rats for 4 weeks. The levels of glucose, urea, creatinine and bilirubin were significantly (P<0.05) increased in plasma of alloxan-diabetic rats compared with the control group. In contrast, total protein and albumin were significantly decreased by 25 and 46%, respectively, versus control. Treatment of the diabetic rats with repeated doses of any one of the three herb suspensions could restore the changes of the above parameters to their normal levels after 4 weeks of treatment. Aspartate aminotransferase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) and alkaline phosphatase (AlP) activities were significantly (P<0.05) increased in the plasma of alloxan-diabetic rats. However, acetylcholinesterase activity was significantly (P<0.05) decreased in the plasma compared with the control group, whereas, such activity did not change in brain. The activities of AST, ALT and LDH were significantly (P<0.05) decreased in the liver of alloxan-diabetic rats by 58, 21 and 40%, respectively, and such activities increased in testes by 39, 26 and 26%, respectively, compared with the control group. Also, brain LDH was significantly (P<0.05) increased. Treatment of the diabetic rats with the aqueous suspension of the tested herbs restored the activities of the above enzymes to their normal level in plasma, liver and testes. The present results showed that the herb suspensions exerted antihyperglycemic effects and consequently may alleviate liver and renal damage caused by alloxan-induced diabetes.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Plantas Medicinais/química , Animais , Glicemia/metabolismo , Proteínas Sanguíneas/metabolismo , Encéfalo/enzimologia , Diabetes Mellitus Experimental/enzimologia , Egito , Fígado/enzimologia , Testes de Função Hepática , Masculino , Ratos , Ratos Sprague-Dawley , Testículo/enzimologia
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