RESUMO
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease mainly caused by insulin resistance, which can lead to a series of complications such as cardiovascular disease, retinopathy, and its typical clinical symptom is hyperglycaemia. Glucosidase inhibitors, including Acarbose, Miglitol, are commonly used in the clinical treatment of hypoglycaemia. In addition, Protein tyrosine phosphatase 1B (PTP1B) is also an important promising target for the treatment of T2DM. Gynostemma pentaphyllum is a well-known oriental traditional medicinal herbal plant, and has many beneficial effects on glucose and lipid metabolism. In the present study, three new and nine known dammarane triterpenoids isolated from G. pentaphyllum, and their structures were elucidated by spectroscopic methods including HR-ESI-MS,1H and 13C NMR and X-ray crystallography. All these compounds were evaluated for inhibitory activity against α-glucosidase, α-amylase and PTP1B. The results suggested that compounds 7â¼10 were potential antidiabetic agents with significantly inhibition activity against PTP1B in a dose-dependent manner.
Assuntos
Relação Dose-Resposta a Droga , Inibidores Enzimáticos , Gynostemma , Proteína Tirosina Fosfatase não Receptora Tipo 1 , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo , Gynostemma/química , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Estrutura Molecular , Relação Estrutura-Atividade , alfa-Glucosidases/metabolismo , Humanos , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Modelos Moleculares , Cristalografia por Raios X , Triterpenos/farmacologia , Triterpenos/química , Triterpenos/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificaçãoRESUMO
WHAT IS ALREADY KNOWN ABOUT THIS TOPIC?: Rabies is fatal while preventable. More than 99% of human rabies cases were caused by dog bites worldwide. Mass dog vaccination could interrupt dog-mediated rabies if achieving and maintaining a minimum coverage rate of 70%. WHAT DOES THIS REPORT CONTRIBUTE?: The results of this study show that roughly 23.7% of households owned dogs in Guangxi Zhuang Autonomous Region, China but only about 19.1% of these households reported having their dogs vaccinated. Possible positive factors were injury history of dog bites, awareness of the necessity, and policy help for the costs of dog vaccination, but negative factors were negative attitude and inaccessibility. WHAT ARE THE IMPLICATIONS FOR PUBLIC HEALTH PRACTICES?: Much more effort should be made to improve dog vaccination coverage in rural areas in Guangxi Zhuang Autonomous Region, China. Well-designed free mass vaccination campaigns with more accessibility and awareness campaigns are important to improve coverage.
RESUMO
WHAT IS ALREADY KNOWN ABOUT THIS TOPIC?: Although fatal once clinical signs appear, rabies is preventable through three proven, effective interventions including mass dog vaccination, post-exposure prophylaxis (PEP), and, though sometimes neglected, awareness of rabies. WHAT IS ADDED BY THIS REPORT?: The total awareness rate of rabies-related knowledge among rural residents was only 57.9% in Guangxi Zhuang Autonomous Region, one of the provincial-level administrative divisions (PLADs) with endemic rabies in China, and the exposure rate of dog-bite injuries was as high as 7.2% in the past year. In addition, 14.8% of bite victims failed to seek PEP service. WHAT ARE THE IMPLICATIONS FOR PUBLIC HEALTH PRACTICE?: This study can provide evidence for the targeted prevention and control program of rabies in rural areas and help realize the international goals of eliminating dog-mediated rabies by 2030.