SYNTHESIS, BIOLOGICAL EVALUATION, AND DOCKING STUDY OF NOVEL 2-PHENYL-1- BENZOPYRAN-4-ONE DERIVATIVES - AS A POTENT CYCLOOXYGENASE-2 INHIBITOR

Objective: The inflammation and oxidative stress were related together in the generation of reactive oxygen species, which is responsible for the enhancement of inflammation associated with various chronic diseases. Methods: The aim of this study is to synthezise and characterizes the flavones (2-phenyl-1-benzopyran-4-one) derivatives and analyzed by their docking hypothetical data as an effective anti-inflammatory mediator against cyclooxygenase-2 (COX-2) enzyme. Further, the evaluation of various in vitro antioxidant and anti-inflammatory studies was carried out. Results: The 10 compounds were synthesized and characterized by ultraviolet, infrared, nuclear magnetic resonance, and mass spectroscopic techniques. The docking data results of these 10 flavones derivatives against COX-2 enzymes (Protein Data Bank ID: 3LN1) showed the binding energy ranging between −5.53 kcal/mol and −7.02 kcal/mol when compared with that of the standard diclofenac (−6.34 kcal/mol). The in vitro studies suggest that the lipophilic character of the side chain donor, along with the hydroxyl substituted flavones found to have significant half maximal inhibitory concentration values. Conclusion: Based on these in silico and in vitro evaluation results, these synthesized compounds could act as a promising inhibitor to target the COX- 2 enzyme. Hence, those compounds were effective in the management of chronic diseases by exhibits free radical scavenging and anti-inflammatory property

Antihyperglycemic activity of Trichosanthes tricuspidata root extract

To evaluate the anti-diabetic activity of ethanolic extract of Trichosanthes tricuspidata root in alloxan induced diabetic rats and to perform the phytochemical screening. The extraction, preliminary phytochemical screening, anti-diabetic activity in alloxan induced diabetic rats  by oral administration of  extract (200 and 400 mg/kg b.w.), the blood glucose level and biochemical parameters like cholesterol, triglyceride, serum protein, SGPT, SGOT, and ALP were estimated. Phytochemical studies shows the presence of carbohy-drates, proteins, glycosides and terpenoids and the ethanolic extract of T. tricuspidata root significantly lowered the blood sugar level. The above findings justified the traditional claim of anti-diabetic activity in this plant

Anti-hyperglycemic activity of Trichosanthes tricuspidata root extract

To evaluate the anti-diabetic activity of ethanolic extract of Trichosanthes tricuspidata root in alloxan induced diabetic rats and to perform the phyto-chemical screening. The extraction, preliminary phytochemical screening, anti-diabetic activity in alloxan induced diabetic rats by oral administration of extract (200 and 400 mg/kg b.w.), the blood glucose level and biochemical parameters like cholesterol, triglyceride, serum protein, SGPT, SGOT, and ALP were estimated. Phytochemical studies shows the presence of carbohy-drates, proteins, glycosides and terpenoids and the ethanolic extract of T. tricuspidata root significantly lowered the blood sugar level. The above findings justified the traditional claim of anti-diabetic activity in this plant

<i>p</i>-Coumaric Acid Nanoparticles Ameliorate Diabetic Nephropathy via Regulating mRNA Expression of KIM-1 and GLUT-2 in Streptozotocin-Induced Diabetic Rats

Diabetic nephropathy (DN) has become a leading cause of end-stage renal failure worldwide. The goal of the current study was to examine the protective effects of chitosan-loaded p-Coumaric acid nanoparticles (PCNPs) in nephrotoxicity induced by streptozotocin (STZ). Because of the antidiabetic, anti-inflammatory, and antioxidant properties of PCNPs, the development of DN may be considerably decreased. In this study, the rats received a single intraperitoneal injection (i.p.) of STZ (45 mg/kg) to induce DN. PCNPs were given orally 80 mg/kg b.w to the rats for a duration of four weeks. Body weight, kidney weight, blood glucose, and insulin levels were measured at the end of the experiment. Serum and urine parameters were also examined, along with the histological, immunobiological, and tumor necrosis factor (TNF) and interleukin-6 (IL-6) expression of the nephrotic rats. To comprehend the impact of PCNPs, the expression patterns of the kidney injury molecule (KIM-1) and glucose transporter-2 (GLUT-2) were evaluated. Administration of PCNPs significantly increased body weight, decreased kidney weight and also ameliorated blood glucose levels in the nephropathic rats. The administration of PCNPs also reverted the levels of urea, serum creatinine, urinary NAG, β-glucuronidase and albumin to near-normal levels. The administration of PCNPs also caused the levels of serum and urine parameters to return to near-normal levels. Additionally, the PCNP-treated rats had markedly reduced TNF-α, IL-6, and KIM-1 expressions as well as enhanced GLUT-2 mRNA expression. Our findings clearly showed that PCNP administration prevents the onset of DN in rats by lowering hyperglycemia, decreasing inflammation, and improving the expression of GLUT-2 mRNA in nephropathic rats