RESUMO
Dorzagliatin is a new dual action allosteric systemic glucokinase agonist (GKA), which can simultaneously activate the glucokinase (GK) in the pancreas and liver, promote insulin secretion and liver glycogen conversion in patients with type 2 diabetes, and improve pancreatic islets β - Cell function and insulin resistance simultaneously stimulate intestinal GK to regulate the secretion of Glucagon-like peptide-1 to play multiple hypoglycemic effects. As the first marketed GKA drug, it provides a new therapeutic approach for patients with type 2 diabetes. This article reviews the mechanism of action, pharmacokinetics, Drug interaction, clinical research and safety of Dorzagliatin.
RESUMO
A new coronavirus (SARS-CoV-2) has been identified as the etiologic agent for the COVID-19 outbreak. Currently, effective treatment options remain very limited for this disease; therefore, there is an urgent need to identify new anti-COVID-19 agents. In this study, we screened over 6,000 compounds that included approved drugs, drug candidates in clinical trials, and pharmacologically active compounds to identify leads that target the SARS-CoV-2 papain-like protease (PLpro). Together with main protease (M
Assuntos
Humanos , Antivirais/uso terapêutico , Sítios de Ligação , COVID-19/virologia , Proteases Semelhantes à Papaína de Coronavírus/metabolismo , Cristalografia por Raios X , Avaliação Pré-Clínica de Medicamentos , Reposicionamento de Medicamentos , Ensaios de Triagem em Larga Escala/métodos , Imidazóis/uso terapêutico , Concentração Inibidora 50 , Simulação de Dinâmica Molecular , Mutagênese Sítio-Dirigida , Naftoquinonas/uso terapêutico , Inibidores de Proteases/uso terapêutico , Estrutura Terciária de Proteína , Proteínas Recombinantes/isolamento & purificação , SARS-CoV-2/isolamento & purificaçãoRESUMO
Objective To investigate the effect of tadpole extract(T871 3) on tumor cells and its mechanism. Methods We studied the effects of T871 3 on proliferation, differentiation and apoptosis of HL 60 cells by cytomorphological observation, cytochemistry and TUNEL method. We also examined gene expression during the induction of apoptosis and differentiation in tadpole extract treated HL 60 cells by in situ hybridization and intact cell mRNA dot blot techniques. Results 1 T871 3 was able to inhibite HL 60 cells proliferation. 2 T871 3 was able to induce HL 60 cells to differentiate along monocyte macrophage lineage at low concentration, and apoptosis at higher concentration. 3 The differentiation of HL 60 cells was accompanied by downregulations of c myc,c myb gene expression, The apoptosis of HL 60 cells was accompanied by downregulations of c\|myc bcl 2 gene expression, suggesting that these genes may be involved in the apoptosis and differentiation process. Conclusion Tadpole extract may have effects on HL 60 cells through changing the oncogene expression. [