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Neonatal hypoxic-ischemic encephalopathy (HIE) is one of the main causes of death and nervous system damage in neonates. The aim of the present study was to investigate the effect of the Toll‑like receptor 4 (TLR4) antagonist TAK‑242 on HIE. The Rice‑Vannucci method was used for ligation of the left common carotid artery, followed by hypoxic treatment for 2.5 h to establish a neonatal HIE rat model. Rats were intraperitoneally injected with 7.5 ml/kg TAK‑242 after hypoxia‑ischemia. It was demonstrated that TAK‑242 significantly reduced the infarct volume and cerebral edema content of neonatal rats after HIE, alleviating neuronal damage and neurobehavioral function deficits. Furthermore, TAK‑242 decreased the protein expression levels of TLR4, MyD88, TIR‑domain‑containing adapter‑inducing interferon‑β (TRIF), NF‑κB, tumor necrosis factor α (TNF‑α) and interleukin‑1β in the hippocampus. The present results suggested that TAK‑242 may exert a neuroprotective effect after HIE by inhibiting the TLR4/MyD88/TRIF/NF‑κB signaling pathway, and reducing the release of downstream inflammatory cytokines.

Aim To compare the blood glucose control of patients with type 2 diabetes mellitus (T2DM) with different treatment methods, oral hypoglycemic agents (OHA) monotherapy, insulin injection and combined therapy (OHA + insulin injection) and evaluate their satisfaction with the medical care. Methods A total of 1512 T2DM patients were assessed, to compare the effects of different treatment methods on glycemic control in T2DM patients, the influencing factors of patients’ satisfaction with medical care measures and their relationship with glycemic control. Fasting plasma glucose (FPG), 2 hrs postprandial plasma glucose (2hPG) and HbA1c were measured as the standard of the glycemic control. Satisfaction was defined using the simplified version of DAWN of chronic disease care patient scale (PACIC - DSF). Results In this study, the FPG compliance rate, 2hPG compliance rate and HbA1c compliance rate were 25.5%, 22.7% and 19.5%, respectively. The differences in the glycemic control compliance rates of different treatment methods were not statistically significant. The total score of PACIC - DSF was 34.54±11.65(p>0.05), and the influencing factors included fast blood glucose (FBG) and 2hPG, 2hPG and PACIC - DSF were negatively correlated. Conclusions The T2DM glycemic control rate in China is currently low. From the score of the PACIC - DSF, there is no significant difference in general satisfaction with medical care measures in different treatments. What is more, education level, occupation and exercise of patients with type 2 diabetes had influence on PACIC - DSF score. Different treatment methods have no influence on the glycemic control of patients with T2DM. FPG value and the 2hPG value are negative correlation with the satisfaction of patients in medical care measures.

An α-alkyldiazoacetate-involved three-component reaction has been developed via the suppression of intramolecular α-H shift and 1,2-proton transfer by Rh(i) complexes., Metal-associated carbenes from diazo compounds promote many useful chemistry transformations in modern organic chemistry. However, compared to α-aryldiazoacetate-derived carbenes (ArDCs), the synthetic application of α-alkyldiazoacetate-derived carbenes (AlDCs) is greatly limited due to intramolecular α-H transfer (elimination) that results in alkenes as the main by-products. An intriguing α-alkyldiazoacetate-involved three-component reaction has been developed following DFT calculation inspiration to provide β-hydroxyl α-alkyl-α-amino acid derivatives in good yields. The intramolecular α-H shift of an α-alkyldiazoacetate-derived carbene was successfully suppressed by the association of a Rh(i) complex to form the corresponding active ammonium ylide, which was trapped before the fast 1,2-H transfer process. A Rh(i)-chiral diene complex was identified as an effective catalyst to give an asymmetric version of the reaction with good enantioselectivity. This reaction provides insight into extending the efficient transformation of α-alkyldiazoacetate-derived carbenes and their synthetic application.