β-Resorcylidene aminoguanidine (RAG) dilates coronary arteries in an endothelium-independent manner.

Background: β-Resorcylidene aminoguanidine (RAG), a highly reactive derivative of aminoguanidine, possesses antithrombotic activity which involves the activation of the vascular COX-2/PGI2 pathway. This endothelium-dependent effect suggests that RAG may demonstrate vasomotor activity in arterial vessels. The aim of the present study was to investigate a possible vasoactive action of RAG in coronary arteries of rat heart.

Influence of pyridoxylidene aminoguanidine on biomarkers of the oxidative stress and selected metabolic parameters of rats with diabetes mellitus.

Oxidative damage is considered to play an important role in the pathogenesis of several diseases, such as diabetes mellitus (DM), atherosclerosis, cardiovascular complications and chronic renal failure. DM is associated with the oxidative stress and formation of advanced glycation end products (AGEs). Different drugs inhibit oxidative stress and formation of advanced glycation end products.

Resorcylidene aminoguanidine induces antithrombotic action that is not dependent on its antiglycation activity.

There is good evidence supporting the notion that aminoguanidine(AG)-derived compounds prevent glycation/glycooxidation-dependent processes and therefore inhibit late diabetic complications. The aim of the present work was to analyse the antithrombotic action and antiglycation activity of beta-resorcylidene aminoguanidine (RAG) in comparison with another commonly used aminoguanidine (AG)-derived compound, pyridoxal aminoguanidine (PAG). In vitro RAG and PAG prevented exhaustive glycation and glycooxidation of BSA to a similar extent.

Effects of resorcylidene aminoguanidine (RAG) on selected parameters of isolated rat liver mitochondria.

In the present investigation, we attempted to study possible mechanisms of the interactions of resorcylidene aminoguanidine (RAG), the agent with a recognized anti-glycation and antioxidative activity, with rat liver mitochondria. We hypothesized that RAG affects organization of the lipid bilayer in mitochondrial membranes and thus impairs transmembrane Ca(2+) redistribution, transmembrane potential, and respiration capacity. Isolated mitochondria were exposed to RAG (50-200 microM) and several parameters of their function monitored employing spectrofluorimetric, cytometric, and respirometric techniques.

Effect of pyridoxylidene aminoguanidine on human diploid cells B-HEF-2: in vitro cytotoxicity test and cytogenetic analysis.

Background: Pyridoxylidene aminoguanidine is an appropriate inhibitor of protein glycation, respectively formation of advanced glycation products, which are connected with mechanism of pathogenesis in chronic diabetic complications. Moreover, it was found that in comparison with aminoguanidine, pyridoxylidene aminoguanidine does not influence the level of vitamin B6 in liver and kidneys in vivo. The aim of this study was to test cytotoxic effect of pyridoxylidene aminoguanidine in vitro, in regard to its potential use as inhibitor of advance protein glycation in diabetic patients.

Remodelling of the sarcolemma in diabetic rat hearts: the role of membrane fluidity.

The hyperglycaemia and oxidative stress, that occur in diabetes mellitus, cause impairment of membrane functions in cardiomyocytes. Also reduced sensitivity to Ca-overload was reported in diabetic hearts (D). This enhanced calcium resistance is based on remodelling of the sarcolemmal membranes (SL) with down-regulated, but from the point of view of kinetics relatively well preserved Na,K-ATPase and abnormal Mg- and Ca-ATPase (Mg/Ca-ATPase) activities.

Fluidity gradient of erythrocyte membranes in diabetics: the effect of resorcylidene aminoguanidine.

We estimated in vitro membrane fluidity gradient in erythrocytes (RBC) from diabetic patients, using a fluorescent dye 1,6-diphenyl-1,3,5-hexatriene (DPH). The rate constant of DPH incorporation (k) into the membranes was determined by fitting experimental data to an exponential equation. Four important findings were made.