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Heart failure is a condition in which the heart's one or both ventricles are unable to either receive an adequate amount of blood or eject an adequate amount of blood. Diabetes is considered one of the major risk factors for cardiovascular diseases. The current research is designed to evaluate the cardioprotective effects of dapagliflozin in streptozotocin and isoproterenol-induced comorbid rats. The COX-2, TNF-α, NF-Κ B, NLRP3, PPAR-γ, CKMB, TROP-I, AR, GP and SGLT were docked against dapagliflozin, propranolol and metformin. Dapagliflozin restored adequate blood flow and halted myofibril damage. Moreover, it's evident from this study that dapagliflozin significantly decreased serum concentration of various blood markers, decreased relative growth rate and QT interval prolongation, as compared to the negative control group. However, it improved the ventricular ejection fraction in rats of the treatment group. The GST, GSH and CAT levels were increased, as compared to normal. On the contrary, a decrease in LPO concentrations was observed. Evaluation of the coronal section of heart tissues showed the anti-inflammatory expressions evaluated through H & E staining and immunohistochemical techniques and with ELISA and PCR. In a nutshell, dapagliflozin reverses myocardial necrosis and apoptosis. [ABSTRACT FROM AUTHOR]

Pyrimidine 2, 4, 6-trione derivatives are known to have L-type calcium channel blockade activity due to which they are quite effective in cardiovascular diseases along with cancer, epilepsy and inflammatory disorders. The chemoinformatics prediction for test compounds: 5-(3-Hydroxybenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-5), 5-(4-Hydroxybenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-8), 5-(3-Chlorobenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-9) and 5-(4-Chlorobenzylidene)-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione (SR-10) was investigated. The druglikeliness and pharmacokinetic properties (PKs) of test compounds calculated using Molinspiration & Swiss ADME online servers. These test drugs subjected to molecular docking analysis and molecular dynamic (MD) simulation to calculate their binding energies with hypertensive and platelet aggregatory proteinaceous targets and their stability against calcium channel. The druggability and PKs of selected compounds exhibited that these compounds could be represented as potential candidates for further development into antihypertensive-like agents. The docking results indicated that binding energies ranged between -5 and -8.8 kcal/mol. Compounds showed good binding energies against calcium channels (CC) and subjected to molecular dynamic simulation to assess the stability of proteinligand complex. The results showed that all the ligands form stable complexes with the CC, though SR-9 and SR-10 had enhanced stability when compared to SR-5 and SR-8. [ABSTRACT FROM AUTHOR]

In present study hypoglycaemic effects of the crude powdered C. decussata and its methanolic extract (ME) in alloxan diabetic rabbits were evaluated. The hypoglycaemic effect was measured by blood glucose, insulin level, HbA1c and his to pathology of pancreas. Glucose lowering effect of the ME was studied in diabetic rabbits. The effects of extract on blood glucose, body weight, food in take, fluid intake, OGTT were also evaluated. The results showed that 0.5,1 and 2g/kg of the powder significantly decreased blood glucose levels in normal rabbits and diabetic rabbits at the intervals checked. Oral intake of pioglitazone also reduced the levels in these rabbits. Synergistic hypoglycaemic effect of 600mg/kg of ME with different doses of insulin (2 & 3unit/kg, s/c) further reduced blood glucose levels of treated alloxan-diabetic rabbits. The oral glucose tolerance test revealed lowered area under curve values in ME treated rabbits. Treatment with ME (400 and 600 mg/kg) for 30 days showed highly significant decrease in blood glucose level by augmenting insulin secretion, HbA1cand significant increase in body weight, serum insulin levels in treated diabetic rabbits. Histopathology study showed regeneration of β-cells. These studies have, therefore, supported the traditional use of this herb in diabetic patients. [ABSTRACT FROM AUTHOR]