Arenobufagin-loaded PEG-PLA nanoparticles for reducing toxicity and enhancing cancer therapy.

Arenobufagin (ArBu) is a natural anticancer drug with good anti-tumor effects, but its clinical applications and drug development potential are limited due to its toxicity. The purpose of this study is to reduce the toxic side effects of ArBu and improve the efficacy of tumor treatment by incorporating it into poly(ethylene glycol)-b-poly (lactide) co-polymer (PEG-PLA). ArBu@PEG-PLA micelles were prepared by a thin film hydration method. The optimized micelles were characterized by size, stability, drug loading, encapsulation rate, and drug release. The tumor-inhibition efficacy of the micelles was evaluated on A549 cells and tumor-bearing mice. The ArBu@PEG-PLA micelles have good drug-loading capacity, release performance, and stability. They can accumulate at the tumor site through the EPR effect. The micelles induce apoptosis through a mitochondrial apoptosis pathway. Compared with the free ArBu, the ArBu@PEG-PLA micelles had lower toxicity and higher safety in the acute toxicity evaluation experiment. The in vivo anti-tumor experiment with tumor-bearing mice showed that the tumor-inhibition rate of ArBu@PEG-PLA micelles was 72.9%, which was 1.28-fold higher than that of free ArBu (57.1%), thus showing a good tumor treatment effect. This study indicates that ArBu@PEG-PLA polymeric micelles can significantly improve the toxicity and therapeutic efficacy of ArBu. These can lead to a new therapeutic strategy to reduce the toxicity of ArBu and enhance tumor treatment.

Research progress of active ingredients of Scutellaria baicalensis in the treatment of type 2 diabetes and its complications.

Diabetes mellitus is a common disorder of endocrine and metabolic disorders. Long term hyperglycemia can lead to a variety of serious chronic complications, such as diabetic nephropathy, diabetic retinopathy, diabetes cardiovascular disease, and so on, threatening human life, health and safety. Scutellaria baicalensis Georgi is one of the most commonly used traditional Chinese medicine. Flavonoids are the main effective components of Scutellaria baicalensis Georgi. The flavonoids are mainly baicalin, baicalein, wogonoside and wogonin. The four have the effects of improving the renal function, insulin resistance and retinopathy of type 2 diabetic patients. The aim of this review is to summarize the pathogenesis and clinical research progress of baicalin, baicalein, wogonoside and wogonin in Scutellaria baicalensis Georgi in the treatment of type 2 diabetes mellitus and its complications.

Association of plasma leptin levels and complexity of the culprit lesion in patients with unstable angina.

BACKGROUND: Angiographically visible complex lesions which are associated with plaque vulnerability have been shown to correlate strongly with clinical severity of unstable angina (UA). By activating different immune/inflammatory cells or directly acting on the vessel wall leptin has been shown to play a potential role in the development of acute coronary syndrome. However, the relationship between leptin and simple or complex lesion morphology in UA has not been investigated. Therefore, we designed this study to determine the association between plasma leptin level and simple or complex lesions in patients with UA and to see any correlation between leptin and other inflammatory markers in these patients. METHODS: Plasma concentrations of leptin, interleukin (IL)-6, IL-10 and high-sensitivity C-Reactive Protein (hsCRP) were analyzed in 47 patients with UA. These patients were also angiographically studied and divided into two groups: simple lesion (n=18) and complex lesion (n=29) based on the coronary plaque morphology. We further compared them with 20 control subjects having no evidence of coronary artery diseases. RESULTS: Plasma leptin concentrations were higher in patients having complex lesions compared to those having simple lesions as well as normal controls. Similarly IL-6 and hsCRP were also higher in complex lesion group compared to simple lesion group and controls, and leptin was positively correlated with IL-6 and hsCRP. Concentrations of IL-10 were lower in simple and complex lesion groups compared to the controls and leptin was negatively correlated with IL-10, but no significant difference between simple and complex lesions was found. Furthermore, leptin was found to be an independent predictor for the complex lesion morphology in UA patients. CONCLUSION: These findings suggested that angiographically visible complex lesions are associated with increased concentrations of leptin, and thus leptin can be a useful biomarker for risk stratification in UA.