Objective: The objective of the study was to develop new Cyclooxygenase-2 inhibitors as anti-inflammatory agents from synthetic route. Method: The 2-phenyl-4H-chromen-4-one and 2-phenyl-2,3-dihydro-4H-chromen-one hybrids were synthesised and characterised by using UV, IR, 1H-NMR, and mass spectrometry. An attempt was made for consolidated the lead flavones and flavanones scaffolds by determining ADME/T properties. Molecular docking simulations were performed by using Autodock.4. for understanding the binding interaction over the targeted enzyme Cyclooxygenase-2. The titled compounds were evaluated for various in-vitro models for antioxidant and anti-inflammatory activities and based upon the IC50 values, the selected compounds were screened for invivo anti-inflammatory activity by both acute and chronic models. Results: The twenty compounds of titled compounds were synthesised and elucidated their structure for confirmation of their functional groups by various spectroscopic techniques. Among the synthesized compounds, in flavone derivatives such as HFc (7-hydroxy-3-(4-methoxy phenyl)-4H-chromen-4-one), HFd (2-(2,4-di methoxy-phenyl)-7-hydroxy-4H-chromen-4-one) and HFe (7-hydroxy-2-(thiophen-2-yl)-4H-chromen-4-one) were produced higher potency. As like, flavanone derivatives HFAc (7-hydroxy-2-(4-hydroxy-3-methoxy phenyl)-2,3-dihydro-4H-chromen-4-one), HFAb (7-hydroxy-2-(4-methoxy phenyl)-2,3-dihydro-4H-chromen-4-one) and HFAd (7-hydroxy-2-(thiophen-2-yl)-2,3-dihydro-4H-chromen-4-one) showed significant anti-inflammatory activity compared to the standard COX-2 inhibitors. Conclusions: The flavone and flavanone scaffolds were posses their excellent inhibitory action over the Cyclooxygenase-2 and acts as a potential anti-inflammatory agents. The results of computational studies were also significantly correlated and conclude that those naturally mimicking flavonoid analogues were tremendous candidates for fighting against the inflammatory diseases in drug discovery.

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.

Roots of Illupai (Madhuca longifolia) are mentioned for Madhumegam in Gunapadam -Mooligai (Siddha Materia Medica). The disease Madhumegam found in siddha text is correlated with Diabetes mellitus type-II. Madhuca longifolia known as Illupai in Tamil has been widely used for the treatment of diabetes. Hence, the present study aimed to demonstrate the antidiabetic effects of Illupai ver chooranam in normal and streptozotocin (STZ) induced diabetic rats. The qualitative phytochemical analysis of the chooranam showed the presence of flavonoids, glycosides, tannins, triterpenoids, polyphenols, carbohydrates, steroids, saponin and proteins. Acute toxicity studies revealed the nontoxic nature of the illupai ver chooranam up to a dose level 2000 mg/kg body weight until the end of the study period. The illupai ver chooranam (500 and 1000 mg/kg) significantly reduced (P**< 0.01) glucose levels in diabetic rats. The other biochemical parameters like cholesterol, lipid, urea, protein, liver glycogen, serum glutamate pyruvate transaminase (SGPT) and serum glutamate oxaloacetate transaminase (SGOT), were found to be reduced by the illupai ver chooranam. The histopathological results of treated groups showed the regenerative/protective effect on ?-cells of pancreas in diabetic rats. In the oral glucose tolerance test, the illupai ver chooranam increased the glucose tolerance. The current study revealed the antidiabetic potential of illupai ver chooranam effective in hyperglycemia and that it can effectively protect against other metabolic aberrations caused by diabetes in rats, which seems to validate its therapeutic traditional use.

Background: Alzheimer’s disease (AD) is a chronic, and prevalent, neurodegenerative disease that leads to memory loss, especially in the elderly. AD is caused by a lack of acetylcholine in the brain and oxidative stress. The Cyamopsis tetragonoloba also known as Guar or cluster bean is a legume that belongs to the family Fabaceae. It is cheap, widely consumed as a seasoned vegetable, and reported to counteract chronic diseases linked to oxidative stress, such as diabetes, dyslipidemia, inflammation, and ulcer. Objective: The present study was undertaken to assess the anti-alzheimer’s activity of a tender green pod extract of Cyamopsis tetragonoloba on learning and memory impairment induced by scopolamine. Methods: The extract's total phenolic and flavonoid content was determined using a UV-visible spectrophotometer. The Cyamopsis tetragonoloba methanolic pod extract (CTMPE) at a dose of 100 and 200 mg/kg and donepezil 2.5 mg/kg was administered orally for 7 successive days. On the seventh day, a single intraperitoneal injection of scopolamine was used to induce dementia. The behavioral experiments included an elevated plus maze, step-through passive avoidance, radial arm maze, and Y-maze tests were conducted. The mice were sacrificed and acetylcholine, acetylcholinesterase, and oxidative stress markers were measured in brain homogenate. Results: The total phenolic and flavonoid content was found as 12.9 mg of GAE/g and 1.71 mg of QE/g respectively. Scopolamine caused memory deterioration, as well as changes in acetylcholine, acetylcholinesterase, and increased oxidative stress in the brain. Mice pretreatment with CTMPE at both doses attenuated scopolamine-induced behavioral, neurochemical, and oxidative changes in a similar way to donepezil. Conclusion: The CTMPE showed an anti-amnesic effect that makes it a promising candidate targeting multiple events as a potential strategy to curb the progression of cognitive impairment.

Background: Chronic non communicable diseases were interlinked with inflammation and infections should response to starting core of major diseases in both acute and chronic conditions. In drug discovery, development of a drug which acts as anti-infective agents (anti-microbial and anti-inflammatory) must be ideal and challenging for management of many chronic diseases. Objective: In this study, six lead pyrazoline hybrids were synthesized by cyclization of chalcones and characterized by various spectroscopic and elemental analysis. All synthesized compounds were screened for anti-inflammatory and anti-microbial activity by computational tools and biological evaluation. Methods: Synthesized pyrazoline analogues were characterized by various spectroscopic techniques and evaluated for prediction of pharmacokinetics, physicochemical properties and Molecular docking studies of various targeted enzymes on microbial and inflammatory mediators. Those compounds were screened by anti-microbial and anti-inflammatory activities by several in-vitro and in-vivo methods. Results: The synthesized compounds (A1-A6) were screened for anti-inflammatory activity in which compound A2 produced effective percentage inhibition (45.8 %) potent activity compared with that of standard indomethacin (49.7 %) in carrageenan paw edema method were observed. The anti-microbial activity was screened on synthesized compounds, among which A3 [2-(1,3-diphenyl-4,5-dihydro-1H-pyrazol-5-yl) phenol, A2 [5-(4-chlorophenyl)-1,3-diphenyl-4,5-dihydro-1H-pyrazole] produced potential percentage zone of inhibition between 80 - 70 % for bacterial strains and 94 - 89 % for fungal strains were observed. The minimum inhibitory concentration values of those compounds were 1.56 to 6.25 µg/ml for bacterial strains and 1.56 to 12.5 µg/ml for fungal strains were noted compared with the standard gatifloxacin and clotrimazole, respectively. The molecular docking, pharmacokinetics and toxicity predictions on those compounds were supported further for the development of potent anti-infective agents. Conclusion: The hypothesis of this research was correlated with the results of anti-inflammatory and anti-microbial activity. The binding interactions of respective enzymes were coincided with reduction of paw edema in anti-inflammatory model and zone of inhibition in anti-microbial activity were observed.