Posted by admin on May 31, 2023 in |
Serotonin plays a crucial role in various cognitive and behavioral functions. The serotonin signaling is mediated by binding of serotonin to specific receptors on the cell surface. Serotonin 5-HT6 receptors turned out to be promising biological targets for the modulation of central nervous system dysfunctions. Several classes of serotonin 5-HT6 receptor ligands have been discovered. Among them, many aryl sulphonamides derivatives as 5-HT6 antagonists were reported to have better affinity towards the receptor. In the present study, a quantitative structure-activity relationship (QSAR) study of forty derivatives of aryl sulphonamide and sulfone based 5-HT6antagonists has been made with the help of topological parameters. The descriptors that have been used are valence connectivity indices of order 0, 1 & 2 and shape indices of order 1, 2 & 3. The biological activities of compounds have been taken from the literature. The study indicates that the valence connectivity index (order-0) appears an important descriptor for the QSAR study of aryl sulphonamides which alone gives a QSAR model with reliable predictive power. The...
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Posted by admin on May 31, 2023 in |
A peptic ulcer is an excoriated area of the stomach or intestinal mucosa caused principally by the digestive action of gastric juice or small upper intestinal secretions. A peptic ulcer is a conglomerate of heterogeneous disorders that manifests as a lesion in the lining of the gastrointestinal mucosa bathed by acid and pepsin. Peptic ulcers frequently occur along the lesser curvature of the antral end of the stomach or, more rarely, in the lower end of the esophagus, where stomach juices frequently reflux. It occurs because of an imbalance between aggressive factors (gastric acid and pepsin) and defensive factors (gastric mucus, bicarbonate, prostaglandins). The white mulberry tree (M. alba L.) is a deciduous tree originating from Asia but currently cultivated in subtropical, tropical, and moderate environments. M. alba leaves contain triterpenoid and steroidal saponin (lupeol, β- Sitosterol), bioflavonoids (rutin, moracetin, quercetin-3-triglucoside and isoquercitrin), coumarins, volatile oil, alkaloids, amino acids and organic acids, rutin, quercetin. M. alba leaves have various pharmacological properties such as anti-cancer, Anti- dopaminergic, and Hepatoprotective activity....
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Posted by admin on May 31, 2023 in |
Healthy diet has been known to play a key role in managing and preventing diseases. The health benefits of consuming common beans (Phaseolus vulgaris) are widely acknowledged and are ascribed mostly to their high dietary fiber contents and polyphenols. Various animal experimental studies have shown that polyphenol in common beans has antioxidant properties and other biological activities. This study was designed to evaluate the antilipidemic potentials of Phaseolus vulgaris on experimentally-induced diabetic rats. 20 male rats of the Wistar strain were divided into 4 groups (n=5). Group A was the normal control; group B was the diabetic control; while groups C and D were diabetic and treated with 400mg and 800mg/kg body weight of aqueous extract of Phaseolus vulgaris seed, respectively. Blood samples were collected on the last day of the experiment for biochemical assay. Results showed a significant increase (p<0.05) in total cholesterol (TC), triglyceride (TG), and low-density lipoprotein (LDL-c) levels of diabetic rats when compared to the control group. Treatment of diabetic rats with Phaseolus vulgaris showed...
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Posted by admin on May 31, 2023 in |
Solubility and stability are the limiting steps for almost all drugs in the pharmaceutical field toward bioavailability. In the present investigation, microwave reacts with the crystallization solvent to change their crystalline state to stable and highly soluble nanocrystals. Microwave Assisted Grinding Nanotechnology (MAGN) was used to prepare stable nanocrystals of Valsartan, BCS class II, by treating them with Chitosan and neusiline US2. Ternary crystalline particles were designed using 32 level full factorial design using Design Expert Software version 12. The optimized batch showed a nano-size range with about a 3.2 times increase in saturation solubility and 2.89 times enhanced cumulative drug release than pure valsartan. Compatibility with excipients, crystallinity and particle size study was confirmed from FTIR, DSC, XRD, and particle analyzer. Physical interactions from FTIR and NMR results also confirmed intermolecular hydrogen bond interaction. The accelerated stability study showed a confirmed stable product due to the absence in any interactions from FTIR and variation of drug content. Formulation of microwave-treated nanocrystals is a novel technique to enhance bioavailability...
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Posted by admin on May 31, 2023 in |
Pyrazole and its derivatives are pharmacologically active and are being used in various disorders and diseases with a few side effects. The wide distribution of pyrazole compounds in nature with fascinating pharmacological action is key in the application of this development of newer derivatives. The main structure has a great variety of compounds that have essential pharmaceutical and agrochemical activities in addition to biological activity like anti-inflammatory, antifungal, antitumor, antiviral, antibacterial, anti-tubercular, and antiphrastic. Protection against various substances that causes oxidative stress in the body is needed in the modernizing world in this direction intermediate obtained from the Vilsmeier Haack reaction (4) was treated with aromatic amines to obtain N-[3-(naphthalen-1-yl)-1-phenyl-1H-pyrazol-4-yl] methylene) derivatives (5a-5l). The in-vitro antioxidant activity of newly synthesized compounds was determined by the Nitric oxide scavenging...
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