TGR5 is a G protein-coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide-1 (GLP-1) and modulates insulin secretion. The 2-thio-imidazole derivative 6g was identified as a novel, potent, and selective TGR5 agonist (hTGR5 EC50 = 57 pM, mTGR5 = 62 pM) with a favorable pharmacokinetic profile. The compound 6g was found to have potent glucose lowering effects in vivo during an oral glucose tolerance test in DIO C57 mice with ED50 of 7.9 mg/kg and ED90 of 29.2 mg/kg.
Nanotechnology developments have resulted in the emergence of many forms of pharmaceutical products like Nanoemulsions, Nano micelles, Nano sponges and Nano niosomes. In recent years, through nanotechnology, Nano sponges (NS) has acquired remarkable strength in drug delivery. Later, as they effectively overcome the problems like increasing the solubility of water-insoluble drugs, increasing bioavailability, reducing drug toxicity, avoiding drug degradation and targeting the drug to a specific site, which offers controlled drug delivery for topical use. They can also be used as a carrier as biocatalysts for vaccines, enzymes, proteins and antibodies. Nano sponges are better than micro sponges because the diameter of Nano sponge is below 1μm and the diameter of the microsponge is 10-25μm with the void size around 5-300μm, thereby decreases side effect and protect the drug from degradation. This review study to expound the characteristics of β-cyclodextrin based Nano sponges like factors affecting the formation of Nano sponges, applications in topical formulation and comparison of different marketed products of Nano sponges along with cyclodextrin in various drug delivery and offer high drug loading compared to other Nanocarriers
Sudden deaths due to natural causes are commonly seen in forensic practice, most of which are attributed to cardiovascular diseases. Cardiac tamponade (CT) is one of the causes of sudden cardiac death, with a fatal outcome usually detected at autopsy. While both trauma and non-traumatic causes are responsible for CT, it is a known complication of acute myocardial infarction leading to cardiac rupture that involves the ventricular wall, septum, and papillary muscles. We report the case of a 50-year-old male who collapsed suddenly and was declared dead in the Trauma and Emergency Unit of the hospital before admission. Autopsy findings revealed 250 mL of blood and a 206 g blood clot in the pericardial cavity with a vertical tear on the posterolateral surface of the left ventricle with focal hemorrhagic myocardium consistent with acute myocardial infarction. The cause of death was CT as a result of myocardial rupture due to acute myocardial infarction. The gross and histopathological findings were diagnostic and revealed thrombosis of the left circumflex artery, transmural myocardial infarction, and ruptured myocardium of the left ventricle.
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