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1.
Vet Med Sci ; 10(3): e1466, 2024 05.
Artigo em Inglês | MEDLINE | ID: mdl-38695249

RESUMO

BACKGROUND: In this study, we investigated the effects of swimming activity and feed restriction on digestion and antioxidant enzyme activities in juvenile rainbow trout (average body weight of 26.54 ± 0.36 g). METHODS: The stomach, liver and kidney tissues were obtained from four distinct groups: the static water group (fish were kept in static water and fed to satiation), the feeding restricted group (fish were kept in static water with a 25% feed restriction), the swimming exercised group (fish were forced to swimming at a flow rate of 1 Body Length per second (BL/s)) and the swimming exercised-feed restricted group (subjected to swimming exercise at a 1 BL/s flow rate along with a 25% feed restriction). We determined the levels of glutathione, lipid peroxidation and the activities of catalase, superoxide dismutase, glutathione peroxidase, glutathione reductase, glucose-6-phosphate dehydrogenase and lactate dehydrogenase, as well as the presence of reactive oxygen species in the tissues obtained from the fish. Additionally, the activities of pepsin, protease, lipase and arginase in these tissues were measured. RESULTS: Swimming activity and feed restriction showed different effects on the enzyme activities of the fish in the experimental groups. CONCLUSION: It can be concluded that proper nutrition and exercise positively influence the antioxidant system and enzyme activities in fish, reducing the formation of free radicals. This situation is likely to contribute to the fish's development.


Assuntos
Antioxidantes , Oncorhynchus mykiss , Natação , Animais , Oncorhynchus mykiss/fisiologia , Oncorhynchus mykiss/metabolismo , Natação/fisiologia , Antioxidantes/metabolismo , Aquicultura , Condicionamento Físico Animal/fisiologia , Privação de Alimentos/fisiologia , Fenômenos Fisiológicos da Nutrição Animal , Digestão/fisiologia , Ração Animal/análise , Fígado/enzimologia , Fígado/metabolismo
2.
Artigo em Inglês | MEDLINE | ID: mdl-38689532

RESUMO

Glutamate dehydrogenase (GDH) participates in the energy metabolism of proteins and the synthesis of metabolites important for the organism. In this study, GDH enzyme was purified from the liver of rainbow trout (Oncorhynchus mykiss) by 2',5'-ADP Sepharose 4B affinity chromatography in one step. As a result of this purification process, GDH enzyme was purified 171-fold with 5.83 U/mg protein-specific activity. The characterization experiments presented that the storage stability of the purified GDH enzyme was determined as -80°C; optimum temperature 40°C; it was determined that the optimum ionic strength was 100 mM phosphate buffer and the optimum pH was 8.00. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) and PAGE studies showed that the natural molar mass of the purified GDH enzyme was 346.74 kDa, and the molar mass of its subunits was 53.71 kDa. Km and Vmax values for substrates and coenzymes of GDH enzyme purified from rainbow trout liver were calculated, and the lowest Km value was found in NAD+ (1.86 mM) and the highest Vmax value in NH4 + (1.79 U/mL). The effects of some metal ions, vitamins, and solvents on the activity of the purified GDH enzyme were investigated and also IC50 values and inhibition types. The metal ion with the lowest IC50 value is Ag+ (8.65 ± 1.68 µM), and the vitamin is B6 (0.77 ± 0.04 mM). The binding affinities of inhibitors were investigated with molecular docking, based on the conformational state of GDH.

3.
Biol Trace Elem Res ; 202(5): 2085-2099, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-37603267

RESUMO

Diabetic people have a much higher rate of cardiovascular disease than healthy people. Therefore, heart and aortic tissues are target tissues in diabetic research. In recent years, the synthesis of new vanadium complexes and investigation of their antidiabetic/lowering effect on the blood glucose levels and antioxidant properties are increasing day by day. Our study aimed to examine the effects of synthesized oxovanadium (IV) complex of 2-[(2,4-dihydroxybenzylidene]hydrazine-1-[(N-(2-hydroxybenzylidene)](S-methyl)carbothioamide [VOL] on diabetic heart and aortic tissues, as well as in vitro lactate dehydrogenase (LDH) and myeloperoxidase (MPO) inhibition, antioxidant properties, and reducing power. Electrochemical characterization of the VOL was carried out by using Cyclic Voltammetry (CV) and Linear Sweep Voltammetry (LSV) methods. In addition, in silico drug-likeness and ADME prediction were also investigated. For in vivo study, male Swiss albino rats were randomly selected and separated into four groups which are control, control + VOL, diabetic and diabetic + VOL. After the experimental procedure, biochemical parameters were investigated in homogenates of heart and aorta tissues. The results showed that VOL has a protective effect on heart and aortic tissue against oxidative stress. According to electrochemical experiments, one reversible oxidative couple and one irreversible reductive response were observed for the complex. In addition, in vitro LDH and MPO inhibition of VOL was examined. It was found that VOL had a protective effect on heart and aortic tissues of diabetic rats, and caused the inhibition of LDH and MPO in in vitro studies. On the other hand, evaluating the synthesized VOL according to in silico drug-likeness and absorption, distribution, metabolism, and excretion (ADME) prediction, it was found that VOL has drug-like properties and exhibited high gastrointestinal absorption. The VOL had a therapeutic impact on the heart and aortic tissues of diabetic rats, according to the findings.


Assuntos
Antioxidantes , Diabetes Mellitus Experimental , Humanos , Ratos , Masculino , Animais , Antioxidantes/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Coração , Hipoglicemiantes/uso terapêutico , Estresse Oxidativo , Aorta , Glicemia/metabolismo
4.
Chem Biodivers ; 21(2): e202301634, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38156512

RESUMO

Clostridium perfringens (C. perfringens) is a bacterium that causes serious problems in humans and animals such as food poisoning, gas gangrene and infections. C. perfringens has three sialidases (NanH, NanI, NanJ) and inhibition of NanI constitutes an approach in the treatment of C. perfringens since NanI provides the carbohydrate source necessary for the growth of bacteria. In our study, the inhibition effect of some drugs belonging to different drug groups on NanI activity was investigated. Among these drugs, orlistat (0.21±0.05 µM) was determined to have a lower IC50 value than the positive control quercetin (15.58±1.59 µM). It was determined in vitro by spectrofluorometric method. Additionally, NanI molecular docking studies with orlistatand quercetin were performed using iGemdock, DockThor and SwissDock. Orlistat (-93.93, -8.649 and -10.03 kcal/mol, respectively) was found to have a higher binding affinity than quercetin (-92.68, -7.491 and -8.70 kcal/mol, respectively), and the results were in line with in vitro studies. The results may suggest that orlistat is a molecule with drug potential for C. perfringens because it inhibits the drug target NanI, and that the inhibition efficiency can be increased by studies with orlistat derivatives.


Assuntos
Clostridium perfringens , Neuraminidase , Humanos , Animais , Clostridium perfringens/metabolismo , Orlistate/farmacologia , Orlistate/metabolismo , Simulação de Acoplamento Molecular , Quercetina/farmacologia
5.
Acta Chim Slov ; 70(4): 574-587, 2023 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-38124650

RESUMO

Men with diabetes have a higher risk of prostate cancer and people with prostate cancer are prone to stomach metastases. Therefore, researchers are continuing in order to find new approaches in the treatment of individuals with both diseases at the same time. The protective effect of metformin (which is used in the treatment of diabetes) on cancer continues to be supported by studies. The present study aimed that the protective effect of metformin in the stomach tissue of diabetic and/or prostate cancer rats was investigated through biochemical parameters. In the study, it was determined that the biochemical parameters studied showed a protective effect on stomach tissues with the administration of metformin to cancer and diabetic+cancer groups, and as a result of the principal component analysis, it was determined that the biochemical parameters studied in the stomach tissue showed a correlation.


Assuntos
Diabetes Mellitus Tipo 2 , Metformina , Neoplasias da Próstata , Humanos , Masculino , Ratos , Animais , Metformina/farmacologia , Metformina/uso terapêutico , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Estresse Oxidativo , Estômago/patologia
6.
Chem Biodivers ; 20(11): e202300776, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37811911

RESUMO

Alzheimer's disease (AD) is a neurodegenerative disease that occurs especially in advanced ages. It reduces the quality of life of both the patient and their relatives. In addition to its primary effects, AD causes metabolic defects and tissues are damaged due to these effects. Oxidative stress damages cells by disrupting antioxidant/oxidant balance in many tissues, especially due to AD. In individuals with AD and the elderly, lens tissue is damaged due to oxidative stress and may cause vision loss. Therefore, it is very important to investigate herbal products that both prevent/cure AD and reduce AD-related oxidative stress, as they may have fewer side effects. In this study, the protective effects of parsley (Petroselinum crispum) extract on lens tissues of an experimental AD model induced by scopolamine were examined and evaluated through biochemical parameters. The result of biochemical experiments and principal component analysis, was observed that parsley extract had a therapeutic effect by reducing oxidative stress in lens tissues of experimentally induced AD rats. It can be suggested that the phenolic and flavonoid-rich content of parsley extract may have caused the reduction of oxidative damage in lens tissues and can be used to protect lens tissue against oxidative stress due to AD disease.


Assuntos
Doenças Neurodegenerativas , Petroselinum , Humanos , Ratos , Animais , Idoso , Petroselinum/química , Extratos Vegetais/metabolismo , Doenças Neurodegenerativas/tratamento farmacológico , Qualidade de Vida , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Estresse Oxidativo , Derivados da Escopolamina/metabolismo , Derivados da Escopolamina/farmacologia
7.
J Diabetes Metab Disord ; 22(1): 591-602, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37255817

RESUMO

Purpose: Melatonin (Mel) is an indolamine mainly synthesized by the pineal gland and many other organs. It plays an important role in scavenging free radicals and stimulating antioxidant enzymes. The goal of this study was to investigate the effect of Mel and/or insulin treatment on oxidative liver and pancreas injuries in diabetic rats. Methods: Male Wistar albino rats were assigned into 5 groups. Group I: control animals. Group II: diabetes was induced via a single dose of STZ (60 mg/kg) administered intraperitoneally. Group III: diabetic rats treated with Mel (10 mg/kg/day). Group IV: diabetic rats given insulin (6U/kg) subcutaneously. Group V: diabetic rats that received insulin and Mel at the same dose and time. After 12 weeks of the experiment, the animals were decapitated, liver and pancreas tissues were collected. Results: The results indicated that reduced glutathione levels in liver and pancreatic tissue decreased, while protein carbonyl, advanced oxidized protein products and lipid peroxidation levels were elevated in diabetic group. Antioxidant enzyme activities decreased in liver tissues but increased in pancreatic tissues of the diabetic group. Administration of Mel, insulin or Mel + insulin reversed these biochemical changes in the diabetic animals. Conclusion: This work shows that in long-term oxidative stress conditions caused by STZ-induced diabetes, either Mel or Mel + insulin administration may improve the deteriorated oxidant/antioxidant system in both the liver and pancreas tissues. These results suggested that Mel alone or Mel + insulin treatments might have a significant role in protecting against liver and pancreatic damage in STZ diabetic rats via different antioxidant effects.

8.
Drug Chem Toxicol ; 46(6): 1212-1222, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36373188

RESUMO

Valproic acid (VPA) is a drug used for the treatment of epilepsy worldwide. Depending on usage, it can cause complications such as coagulopathies, hepatotoxicity, and encephalopathy. Moringa oleifera has been shown to have antitumor, anti-inflammatory, antiulcer, antispasmodic, diuretic, antihypertensive, antidiabetic, and hepatoprotective activities. The current study investigated the effects of Moringa leaves extract (70% ethanol) on antioxidant systems against valproate-induced oxidative damage in muscle tissues of rats. Female Sprague Dawley rats were randomly divided into four groups. Group I: control group; Group II: animals given only Moringa extract; Group III: animals that received only sodium valproate; Group IV: animals administered with sodium valproate + Moringa extract. Moringa extract and sodium valproate were administered orally. Muscle tissues were collected after sacrificing the animals. Biochemical analysis of muscle tissue homogenates of the valproate group revealed elevated levels/activities of lipid peroxidation, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, catalase, glutathione reductase, glutathione-S-transferase, reactive oxygen species, total oxidant status, oxidative stress index, glucose-6-phosphate dehydrogenase, sialic acid, protein carbonyl, nitric oxide, and myeloperoxidase. While glutathione, superoxide dismutase, glutathione peroxidase, total antioxidant status, aryl esterase and sodium/potassium ATPase were decreased. The administration of Moringa extract reversed these biochemical changes. These results indicate that Moringa leaves extract had a protective effect on muscle tissues against valproate-induced damage.


Assuntos
Antioxidantes , Moringa oleifera , Ratos , Feminino , Animais , Antioxidantes/metabolismo , Ácido Valproico/toxicidade , Ácido Valproico/metabolismo , Extratos Vegetais , Ratos Sprague-Dawley , Estresse Oxidativo , Glutationa/metabolismo , Músculos/metabolismo , Folhas de Planta , Fígado
9.
J Biochem Mol Toxicol ; 37(3): e23268, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36527249

RESUMO

In this present study, the duration of melatonin (Mel) administered to diabetic rats was prolonged so as to examine its effects on the biochemical liver parameters of diabetic rats. In the experiment, Male Sprague Dawley rats were divided randomly into five groups; the control, diabetic + Mel, diabetic, diabetic + insulin, and diabetic + Mel + insulin. Diabetes mellitus was induced by administration of a single dose of streptozotocin (60 mg/kg) intraperitoneally and rats were given vehicle as a solvent for Mel every day for 12 weeks. In the diabetic + Mel group, diabetic rats were administered Mel (10 mg/kg/day) for 12 weeks to treat diabetes. The diabetic + insulin group were diabetic rats given insulin (6 U/kg) subcutaneously for 12 weeks. The diabetic + Mel + insulin rats received insulin and Mel at the same dose and time. At the end of the experiment, the animals were decapitated and liver tissues were taken. The protective effect of Mel on liver tissue of diabetic rats was investigated, total antioxidant status, total oxidant status, reactive oxygen species, oxidative stress index, adenosine deaminase, xanthine oxidase, paraoxonase 1, sodium/potassium ATPase, myeloperoxidase, γ-glutamyl transferase, sorbitol dehydrogenase, tumor necrosis factor-alpha, homocysteine, nitric oxide, glucose-6-phosphate dehydrogenase, and glycoprotein levels were determined in liver tissues. Treatment with Mel and/or insulin has been found to have a protective effect on biochemical parameters. The results showed that administration of Mel to diabetic rats prevented the distortion of the studied biochemical parameters of liver tissues.


Assuntos
Diabetes Mellitus Experimental , Insulinas , Melatonina , Animais , Masculino , Ratos , Antioxidantes/farmacologia , Diabetes Mellitus Experimental/metabolismo , Glicoproteínas/metabolismo , Glicoproteínas/farmacologia , Glicoproteínas/uso terapêutico , Insulinas/metabolismo , Fígado/metabolismo , Melatonina/farmacologia , Estresse Oxidativo , Ratos Sprague-Dawley
10.
Arab J Gastroenterol ; 24(1): 45-51, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36379859

RESUMO

BACKGROUND AND STUDY AIMS: This study aimed to investigate the possible protective effects of parsley extract (Petroselinum Crispum; PC) against oxidative liver damage caused by bile obstruction in rats. MATERIAL AND METHODS: Bile duct ligation (BDL) method was used to induce liver injury in rats. The rats were divided into the three groups each consisting of 8 rats; Sham-operated control (C), bile duct ligated + saline treated (BDL), and BDL + PC treated groups. PC extract was given at a dose of 2 g/kg orally for 28 days. Aspartate amino transferase (AST), alanin amino transferase (ALT), and bilirubin levels were analyzed in sera. In order to determine free radicals in liver injury, luminol and lucigenin chemiluminescence tests used. Oxidative stress was evaluated through superoxide dismutase, glutathione, malondialdehyde, Na+/K+-ATPase and 8-hydroxy guanosine levels. Furthermore, inflammation marker myeloperoxidase, apoptosis marker caspase-3, and fibrosis markers TGF- ß and hydoxyproline were investigated. The liver tissues were also examined for histological evaluations. RESULTS: While PC treatment decreased AST and ALT levels which increased with BDL, oxidant damage parameters also decreased with this treatment. CONCLUSION: The present study, which is the first research for PC extract on cholestasis induced liver damage, demonstrated that PC extract could be a potential therapeutic agent against liver fibrosis and need further studies.


Assuntos
Colestase , Hepatopatias , Ratos , Animais , Petroselinum , Fígado/patologia , Ductos Biliares/cirurgia , Ductos Biliares/patologia , Colestase/tratamento farmacológico , Cirrose Hepática/patologia , Hepatopatias/complicações , Ligadura/efeitos adversos
11.
Chem Biol Interact ; 351: 109757, 2022 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-34848165

RESUMO

New thiosemicarbazone-based zinc(II) complexes were synthesized to study their cytotoxicity on A375 malignant melanoma cells. The complexes containing salicylidene (Zn1a), 3-methoxy-salicylidene (Zn1b) or 4-methoxy-salicylidene (Zn1c) moiety were characterized by analytical and spectroscopic methods. Anticancer potential of the complexes was determined by MTT test and HUVEC endothelial cells line was used to comprehend the effect on normal cells. Zn1b with an IC50 of 13 µM was found to be highly cytotoxic against A375 cancer cells, more effective than cisplatin (IC50: 37 µM). Zn1a and Zn1c did not have a negative effect on cell viability in the normal cells and gave the impression that they are more advantageous than cisplatin in this respect. Further, the ability of Zn1a-c to inhibit neuraminidase enzyme and its role in cytotoxicity was discussed. The test revealed that the Zn1b with 3-methoxy substituent exhibited higher inhibition activity against the neuraminidase than the Zn1a and Zn1c as analogical to the cytotoxicity results. In neuraminidase inhibition, IC50 values of Zn1b and Zn1c were 14 and 66 µM, respectively. These concentrations were very close to the cytotoxicity concentrations for Zn1b and Zn1c. The findings may indicate the role of neuraminidase enzyme inhibition in cell death for Zn1b and Zn1c.


Assuntos
Antineoplásicos/farmacologia , Cisplatino/farmacologia , Complexos de Coordenação/farmacologia , Inibidores Enzimáticos/farmacologia , Neuraminidase/antagonistas & inibidores , Tiossemicarbazonas/farmacologia , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Complexos de Coordenação/síntese química , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/síntese química , Células Endoteliais da Veia Umbilical Humana , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Tiossemicarbazonas/síntese química , Zinco/química
12.
Invest New Drugs ; 37(6): 1187-1197, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-30874940

RESUMO

In vitro cytotoxicity and xanthine oxidase inhibition capabilities were investigated for five palladium (II) chelate complexes. The palladium complexes were synthesized by starting from S-alkyl-thiosemicarbazones where the alkyl component is methyl, ethyl, propyl or butyl. The solid complexes are characterized by elemental analysis and spectroscopic techniques (UV-visible, IR and 1H NMR). In order to be able to verify the N2O2-type thiosemicarbazidato ligand (L2-) structure in the square planar geometry, complex 1 has been studied as a representative by using single crystal X-ray crystallography. The in vitro cytotoxic activity measurements were carried out in HepG2 and Hep3B hepatocellular carcinomas, HCT116 colorectal carcinoma, and 3 T3 mouse fibroblast cell lines. The palladium complexes exhibited notable cytotoxic activities in all cell lines at lower µM concentrations compared to the standard chemicals, cisplatin and allopurinol. IC50 values were determined between 0.42 ± 0.01 and 12.01 ± 0.37 µg/ml in examining the antixanthine oxidase abilities of the complexes. Two complexes with S-methyl group exhibited a high inhibition activity on the xanthine oxidase. The results indicated that these complexes could be used as active pharmaceutical ingredients.


Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Paládio/farmacologia , Tiossemicarbazonas/farmacologia , Xantina Oxidase/antagonistas & inibidores , Células 3T3 , Animais , Antineoplásicos/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Complexos de Coordenação/química , Humanos , Camundongos , Paládio/química , Tiossemicarbazonas/química
13.
J Biochem Mol Toxicol ; 32(2)2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29243863

RESUMO

In this study, three substituted polyhalogenated nitrobutadiene derivatives were synthesized. Compound 1-[(2,3-dibromopropyl)sulfanyl]-1,3,4,4-tetrachloro-2-nitrobuta-1,3-diene (4) was synthesized before by our group. Compounds 8-{[1-[(2,3-dibromopropyl)sulfany]-3,4,4-trichloro-2-nitrobuta-1,3-butadien-1-yl}-1,4-dioxa-8-azaspiro[4.5]decane (5) and 1-[(2,3-dibromopropyl)sulfanyl]-3,4,4-trichloro-N-(4-methylpiperazin-1-yl)-2-nitrobuta-1,3-diene-1-amine (6) were synthesized in this work as original compounds. Xanthine oxidase, elastase inhibition abilities, and antioxidant activities were investigated in this work for compounds 4, 5, and 6. In this study, compounds 4, 5, and 6 exhibited antixanthine oxidase, antielastase, and antioxidant activities. Among the compounds screened, compound 4 exhibited xanthine oxidase and elastase inhibitor effect similar to the standard compound. Among the three tested compounds, compound 6 showed potent DPPH radical scavenging and reducing power activities. Therefore, these three compounds (4, 5, and 6) may be useful as an antixanthine oxidase, antielastase, and antioxidant agent in pharmaceutical and cosmetic industry.


Assuntos
Antioxidantes/farmacologia , Butadienos/farmacologia , Inibidores Enzimáticos/farmacologia , Hidrocarbonetos Halogenados/farmacologia , Elastase de Leucócito/antagonistas & inibidores , Inibidores de Serina Proteinase/farmacologia , Xantina Oxidase/antagonistas & inibidores , Antioxidantes/síntese química , Antioxidantes/química , Butadienos/síntese química , Butadienos/química , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Supressores da Gota/síntese química , Supressores da Gota/química , Supressores da Gota/farmacologia , Humanos , Hidrocarbonetos Halogenados/síntese química , Hidrocarbonetos Halogenados/química , Cinética , Elastase de Leucócito/metabolismo , Estrutura Molecular , Nootrópicos/síntese química , Nootrópicos/química , Nootrópicos/farmacologia , Inibidores de Serina Proteinase/síntese química , Inibidores de Serina Proteinase/química , Temperatura de Transição , Xantina Oxidase/metabolismo
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