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1.
Biometals ; 37(2): 357-369, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37945804

RESUMO

Drug-protein interactions are essential since most administered drugs bind abundantly and reversibly to serum albumin and are delivered mainly as a complex with protein. The nature and strength of drug-protein interactions have a big impact on how a drug works biologically. The binding parameters are useful in studying the pharmacological response of drugs and the designing of dosage forms. Serum albumin is regarded as optimal model for in vitro research on drug-protein interaction since it is the main protein that binds medicines and other physiological components. In this perspective, binary complex have been synthesized and characterized, from vanadium metal and acetylacetone(4,4,4-trifluoro-1-(2-theonyl)-1,3-butanedione). Imidazole, 2-Methyl-imidazole, and 2-Ethyl-imidazole auxiliary ligands were employed for the synthesis of ternary complexes. Additionally, UV absorption and fluorescence emission spectroscopy were used to examine the binding interactions between vanadium complexes and Bovine Serum Albumin. The outcomes of the binding studies and spectral approaches were in strong agreement with one another. These complexes upon inoculation into diabetes-induced Wistar rats stabilized their serum glucose levels within 3 days. From various studies, it was discovered that the ordering of glucose-lowering actions of these metal complexes were equivalent. The vanadium ternary metal complex derived from (4,4,4-trifluoro-1-(2-theonyl)-1,3-butanedione) and imidazole as ligands is the best among the other metal vanadium complexes.


Assuntos
Complexos de Coordenação , Diabetes Mellitus , Ratos , Animais , Vanadatos/química , Soroalbumina Bovina/química , Vanádio/farmacologia , Vanádio/química , Ratos Wistar , Complexos de Coordenação/farmacologia , Complexos de Coordenação/química , Albumina Sérica , Espectrometria de Fluorescência , Glucose , Imidazóis/farmacologia
2.
Biol Trace Elem Res ; 201(10): 5037-5052, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36652102

RESUMO

The medical field now needs more novel drugs to treat obesity and type-2 diabetes mellitus (T2D) than ever before. Obesity and T2D are both characterized by resistance to the hormones leptin and insulin. PTP-1B is a promising target for drug growth, as strong genetic, pharmacological, and biochemical evidence points to the possibility of treating diabetes and obesity by blocking the PTP-1B enzyme. Studies have also found that PTP-1B is overexpressed in patients with diabetes and obesity, suggesting that inhibiting PTP-1B may be a useful technique in their care. There are no clinically used PTP-1B inhibitors, despite the fact that numerous naturally occurring PTP-1B inhibitors have demonstrated great therapeutic promise. This is most likely due to their low activity or lack of selectivity. It is still important to look for more effective and focused PTP-1B inhibitors. A few organovanadium metal complexes were synthesized and characterized, and binding studies on vanadium complexes with PTP-B were also performed using fluorescence emission spectroscopy. Additionally, we theoretically (molecular modeling) and experimentally (enzyme kinetics) examined the PTP-1B inhibitory effects of these vanadium metal complexes and found that they have excellent PTP-1B inhibitory properties.


Assuntos
Complexos de Coordenação , Diabetes Mellitus Tipo 2 , Humanos , Vanádio/farmacologia , Complexos de Coordenação/farmacologia , Cinética , Diabetes Mellitus Tipo 2/tratamento farmacológico , Obesidade/tratamento farmacológico , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/uso terapêutico
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