The in vitro study of interaction between antacids and anti-diabetic drug sitagliptin in the treatment of type II diabetes.

Hyperglycemia is a long-lasting syndrome that occurs either when the pancreas cannot produce enough insulin, or the body cannot effectively utilize that insulin to regulate blood sugar levels. Non-insulin-dependent hyperglycemia, also known as type II diabetes, causes a common consequence of severe damage to many of the body's organs mainly the blood vessels and nerves. The majority of people around the world are suffering from non-insulin-dependent diabetes.

The LC-QTOF-MS/MS analysis of acid degradation products of Rifaximin, an antibiotic.

The present research aims to propose a simple and accurate technique for the analysis of Rifaximin in the presence of its stress degradation products and analysis of degradation products by LC-MS/MS analysis. Rifaximin was submitted to forced degradation under the acid hydrolysis condition as prescribed by the ICH. The extract was prepared by firstly treated with HCl and heated about 4 to 8 h.

Role of Cys-Cys Disulfide Bond on the Structure and Activity of α-Conotoxins at Human Neuronal Nicotinic Acetylcholine Receptors.

α-Conotoxins preferentially antagonize muscle and neuronal nicotinic acetylcholine receptors (nAChRs). Native α-conotoxins have two disulfide links, C-C and C-C, and owing to the inherent properties of disulfide bonds, α-conotoxins have been systematically engineered to improve their chemical and biological properties. In this study, we explored the possibility of simplifying the disulfide framework of α-conotoxins Vc1.

Molecular Determinants Conferring the Stoichiometric-Dependent Activity of α-Conotoxins at the Human α9α10 Nicotinic Acetylcholine Receptor Subtype.

α9α10 nicotinic acetylcholine receptors (nAChRs) putatively exist at different stoichiometries. We systematically investigated the molecular determinants of α-conotoxins Vc1.1, RgIA#, and PeIA inhibition at hypothetical stoichiometries of the human α9α10 nAChR.

Exploring the binding energy profiles of full agonists, partial agonists, and antagonists of the α7 nicotinic acetylcholine receptor.

Nicotinic acetylcholine receptors (nAChRs) belong to the Cys-loop receptor family and are important drug targets for the treatment of neurological diseases. However, the precise determinants of the binding efficacies of ligands for these receptors are unclear. Therefore, in this study, the binding energy profiles of various ligands (full agonists, partial agonists, and antagonists) were quantified by docking those ligands with structural ensembles of the α7 nAChR exhibiting different degrees of C-loop closure.

Investigation of α-conotoxin unbinding using umbrella sampling.

α-Conotoxins, a class of short and disulfide rich peptide toxins, specifically and potently block nicotinic acetylcholine receptors (nAChRs). In this study umbrella sampling was performed to study the unbinding pathways and potential of mean force (PMF) of α-conotoxin ImI and PNIA(A10L,D14K). Our results suggest that (i) the unbinding pathways of ImI and PNIA(A10L,D14K) are similar despite of their different disulfide framework and structure, and (ii) α-conotoxin unbinding requires large conformation perturbation of the C-loop and the backbone flexibility of the C-loop can affect the binding or unbinding kinetics of the α-conotoxins.