Toxicological Profiling of Potential Shikimate Kinase Inhibitors Against .

Over the last decade, has mutated into a putative 'superbug', as treatments against it have failed due to increasing antimicrobial resistance. As a result, the rising incidence of multidrug-resistant tuberculosis (MDR-TB) is posing a significant public health threat, thus, the need to develop effective drugs for MDR-TB has become an urgent priority. To identify new drug candidates for the treatment of MDR-TB, the present study was based on mycobacterial shikimate kinase (MtSK) as the pharmacological target.

Facile green synthesis and characterization of bark phenolic-selenium nanogel: a biocompatible and green nano-biomaterial for multifaceted biological applications.

Biogenic nanoparticle production is in demand as it is secure, has great promise, and is environmental friendly. This study aimed at green synthesis, characterization, and evaluation of selenium nanoparticles (TA-SeNPs) for their antioxidant, antibacterial, anticancer activities, and their incorporation in gel for biomedical applications. The bio-reduction attributes of the (TA) bark extract were utilized to fabricate selenium nanoparticles.

Comparative clinical evaluation of a local drug delivery of cranberry and garcinia fruit gel with tetracycline fibers for amelioration of periodontitis: A split mouth study.

Background: The present study formulates and evaluates a polyberry gel comprising extracts of cranberry () and brindle berry () in patients suffering from chronic periodontitis.

Materials And Methods: The polyberry gel was evaluated for various physicochemical parameters, permeability and stability, and the active phytoconstituents were quantified by High-performance thin layer chromatography (HPTLC). Total phenolic content, total antioxidants, and ascorbic acid were estimated in the two extracts by assays.

Synthesis and biological evaluation of benzamide-chalcone hybrids as potential c-Met kinase and COX-2 inhibitors.

c-Met kinase and cyclooxygenase 2 (COX-2) enzymes are two significant targets in tumor progression. Chalcone and benzamide moieties were combined using molecular hybridization to assess their potential as c-Met kinase and COX-2 inhibitors. 4-Methylbenzamide and 4-chlorobenzamide chalcone analogs were synthesized, characterized, and evaluated for antiproliferative activity on Michigan Cancer Foundation-7 (MCF-7), HT-29, MDA-MB-231, COLO-205, and A549 cell lines by sulforhodamine-B stain (SRB) assay.

Effect of and in combination with Metformin and Enalapril in streptozotocin induced diabetic nephropathy in rats.

Aim: The present study was designed to investigate the effect of methanolic extract of (MECP) and in combination with drugs (Metformin and Enalapril) used in clinical practice in streptozotocin (STZ) induced diabetic nephropathy (DN) in rats.

Methods: Diabetes was induced in male Wistar rats by a single injection of STZ (50 mg/kg ). After 28 days diabetic rats were divided into six groups.

Analgesic Action of Catechin on Chronic Constriction Injury-Induced Neuropathic Pain in Sprague-Dawley Rats.

Chronic neuropathy is a common and debilitating problem that poses a significant challenge to health care worldwide. Natural compounds have received considerable attention as potential sources of new drugs for the treatment of neuropsychiatric pain. Catechin is a well-known novel flavonoid with several therapeutic properties, notably in neurodegenerative diseases.

Effect of Withania somnifera hydroalcoholic extract and other dietary interventions in improving muscle strength in aging rats.

Background: Aging leads to loss of skeletal muscle, diminished muscle strength, and decline in physical functions.

Objective: This study evaluates Withania somnifera and some dietary interventions to combat muscle weakness in aging rats.

Materials And Methods: Rats (12-13 months old) corresponding to a human age of 60-65 years were assigned to various groups and given orally a standardized W.

Diabetic Neuropathy: Review on Molecular Mechanisms.

Diabetic mellitus is a worldwide endocrine and metabolic disorder with insulin insensitivity or deficiency or both whose prevalence could rise up to 592 million by 2035. Consistent hyperglycemia leads to one of the most common comorbidities like Diabetic Peripheral Neuropathy (DPN). DPN is underlined with unpleasant sensory experience, such as tingling and burning sensation, hyperalgesia, numbness, etc.

An Ayurvedic formulation of Emblica officinalis and Curcuma longa alleviates insulin resistance in diabetic rats: Involvement of curcuminoids and polyphenolics.

Background: Nishamalaki is an Ayurvedic herbal formulation used to treat type 2 diabetes mellitus (T2DM), comprises Emblica officinalis and Curcuma longa.

Objective(s): One of the main cause of T2DM is Insulin Resistance (IR) hence, this study was planned to evaluate IR lowering effect of a standardized Nishamalaki extract "EmbliQur" in high-fat diet (HFD) and streptozotocin (STZ) induced T2DM rats.

Materials And Methods: Curcuminoids (23.

In quest of small-molecules as potent non-competitive inhibitors against influenza.

A series of scaffolds namely aurones, 3-indolinones, 4-quinolones and cinnamic acid-piperazine hybrids, was designed, synthesized and investigated in vitro against influenza A/H1N1pdm09 virus. Designed molecules adopted different binding mode i.e.

Formulation, Evaluation, and Clinical Assessment of Novel Solid Lipid Microparticles of Tetracycline Hydrochloride for the Treatment of Periodontitis.

The novel solvent-free process to formulate long-acting microparticles of tetracycline hydrochloride (TH) using hot melt extrusion granulation process coupled with size reduction using comil for the treatment of periodontitis was investigated using hydrogenated castor oil (HCO) as hydrophobic matrix former. The microparticles were characterized for micromeritics, drug diffusion, SEM studies, and stability analysis by DSC, FTIR, and proton NMR. Xanthan gum gel was used as delivery vehicles to administer microparticles inside periodontal pockets.

Evaluation of Benzamide-Chalcone Derivatives as EGFR/CDK2 Inhibitor: Synthesis, In-Vitro Inhibition, and Molecular Modeling Studies.

Background: EGFR (Epidermal Growth Factor Receptor) and CDK2 (Cyclin Dependent Kinase 2) are important targets in the treatment of many solid tumors and different ligands of these receptors share many common structural features.

Objective: The study involved the synthesis of benzamide-substituted chalcones and determination of their antiproliferative activity as well as a preliminary evaluation of EGFR and CDK2 inhibitory potential using both receptor binding and computational methods.

Methods: We synthesized 13 benzamide-substituted chalcone derivatives and tested their antiproliferative activity against MCF-7, HT-29 and U373MG cell lines using Sulforhodamine B Assay.

Nanotechnology-based approaches applied to nutraceuticals.

Nutraceuticals and food industries are opening to a tremendously upcoming technology in the field of "Nano science". A new prospect has been defined by nanotechnology by conferring modified properties of nanomaterials and its application in the development of nanoformulations, nutritional supplements and food industry. Nanomaterials reveal exclusive properties because of their small size and high surface/volume ratio; thus, they have a complete application in nutraceuticals and food sector.

Fighting Strategies Against the Novel Coronavirus Pandemic: Impact on Global Economy.

Sudden outbreak of a new pathogen in numbers of pneumonic patients in Wuhan province during December 2019 has threatened the world population within a short period of its occurrence. This respiratory tract-isolated pathogen was initially named as novel coronavirus 2019 (nCoV-2019), but later termed as SARS-CoV-2. The rapid spreading of this infectious disease received the label of pandemic by the World Health Organization within 4 months of its occurrence, which still seeks continuous attention of the researchers to prevent the spread and for cure of the infected patients.

Anti-atherogenic effect of Nepitrin-7-O-glucoside: A flavonoid isolated from Nepeta hindostana via acting on PPAR - α receptor.

Atherogenic dyslipidemia is a condition and responsible for the induction of major cardiovascular diseases. Traditionally, Nepeta hindostana a medicinal plant commonly used as cardioprotective in Indo-Pak regions has gained importance because of its therapeutic active flavonoid Nepitrin-7-O-glucoside. Flavonoid-glycosides are steroids having the ability to exert specific, decisive action on the cardiac muscle.

Studies in molecular modeling, in-vitro CDK2 inhibition and antimetastatic activity of some synthetic flavones.

Naturally occurring flavonoids have been shown to possess anticancer activity. We have previously shown that certain synthetic flavonoids also exert significant antiproliferative potential in MOLT-4, MCF-7, and HepG2 cell lines. To this end, we evaluated eight synthetic flavones for their CDK2 binding by molecular docking.

Protective effect of a polyherbal bioactive fraction in propylthiouracil-induced thyroid toxicity in ratsby modulation of the hypothalamic-pituitary-thyroid and hypothalamic-pituitary-adrenal axes.

Hypothyroidism is the most frequent consequence of the interaction of a large variety of drugs, environmental pollutants and industrial chemicals with the thyroid gland. It is associated with diminished endocrine function which may lead to hyperlipidemia, diabetes, Alzheimer's disease, weight gain, and other metabolic disorders. The present study evaluates the pro-thyroid activity of a bioactive fraction from a polyherbal teabag in rats with hypothyroidism induced by propylthiouracil.

Comparative distribution of somatostatin and somatostatin receptors in PTU-induced hypothyroidism.

Purpose: Propylthiouracil (PTU)-induced hypothyroidism is a well-established model for assessing hormonal and morphological changes in thyroid as well as other central and peripheral tissues. Somatostatin (SST) is known to regulate hormonal secretion and synthesis in endocrine tissues; however, nothing is currently known about the distribution of SST and its receptor in hypothyroidism.

Method: In the present study, the comparative immunohistochemical distribution of SST and somatostatin receptors (SSTRs) were analyzed in PTU-induced hypothyroid rats.

Design, synthesis and biological evaluation of substituted flavones and aurones as potential anti-influenza agents.

We designed a series of substituted flavones and aurones as non-competitive H1N1 neuraminidase (NA) inhibitors and anti-influenza agents. The molecular docking studies showed that the designed flavones and aurones occupied 150-cavity and 430-cavity of H1N1-NA. We then synthesized these compounds and evaluated these for cytotoxicity, reduction in H1N1 virus yield, H1N1-NA inhibition and kinetics of inhibition.

Cardioprotective potential of (Spinach) against isoproterenol-induced myocardial infarction in rats.

Context: is rich in antioxidant phyto-constituents, termed as the natural antioxidant mixture (NAO).

Objective: This study investigates the cardioprotective effect of an antioxidant-rich extract of (NAOE) and its phytoconstituent rutin in isoproterenol (ISO)-induced myocardial infarction in rats.

Methods: Rats were treated with NAOE (400 and 800 mg/kg), rutin (50 mg/kg) and the reference drug gemfibrozil (50 mg/kg) daily for 30 days and were administered ISO (85 mg/kg, s.

A herbal premix containing , ginger, and whey curtails obesity in rats fed a high-fat diet by a novel mechanism.

The present study designed and evaluated a polyherbal premix comprising , whey protein, , and . Animals were fed a high-fat diet (HFD) for 30 days and were daily administered the premix (1.5 g/kg) in milk (PM) and water (PW), aerobic exercise (AE), premix in milk and water along with AE (PMAE and PWAE), ferulic acid (100 mg/kg), and the reference drug fluoxetine (6 mg/kg).

Structure-aided drug development of potential neuraminidase inhibitors against pandemic H1N1 exploring alternate binding mechanism.

The rate of mutability of pathogenic H1N1 influenza virus is a threat. The emergence of drug resistance to the current competitive inhibitors of neuraminidase, such as oseltamivir and zanamivir, attributes to a need for an alternative approach. The design and synthesis of new analogues with alternate approach are particularly important to identify the potential neuraminidase inhibitors which may not only have better anti-influenza activity but also can withstand challenge of resistance.

Consumption of (spinach) and aerobic exercise controls obesity in rats by an inhibitory action on pancreatic lipase.

(spinach) is abundant in antioxidant phytoconstituents, termed as the natural antioxidant mixture (NAO). This study evaluates the anti-hyperlipidemicand anti-obesity effects of an antioxidant-rich extract of (NAOE) and aerobic exercise (AE) in rats fed with high fat diet (HFD). Rats received NAOE (200 and 400 mg/kg), the standard drug orlistat (10 mg/kg), AE and NAOEAE (NAOE 400 mg/kg + AE) daily with HFD for 21 d.

In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.

Alzheimer's disease (AD) is a progressive neurodegenerative disorder with multiple factors associated with its pathogenesis. Our strategy against AD involves design of multi-targeted 2-substituted-4,5-diphenyl-1H-imidazole analogues which can interact and inhibit AChE, thereby, increasing the synaptic availability of ACh, inhibit BuChE, relieve induced oxidative stress and confer a neuroprotective role. Molecular docking was employed to study interactions within the AChE active site.

A comparative study of the antacid effect of some commonly consumed foods for hyperacidity in an artificial stomach model.

Objectives: The incorporation of certain alkalinizing vegetables, fruits, milk and its products in the diet has been known to alleviate hyperacidity. These foods help to restore the natural gastric balance and function, curb acid reflux, aid digestion, reduce the burning sensation due to hyperacidity and soothe the inflamed mucosa of the stomach. The present study evaluates and compares the antacid effect of broccoli, kale, radish, cucumber, lemon juice, cold milk and curd in an artificial stomach model.