Alzheimer's disease (AD), characterised by gradual memory loss and neurodegeneration, is an important risk to global health. Despite the recent advances in the field of neuroscience, the complex biological mechanisms underlying the aetiology and pathology of AD have not been elucidated yet. The development of amyloid-beta plaques, hyperphosphorylation of tau protein, oxidative stress, and neuroinflammation have been identified as important components.
View Article and Find Full Text PDFAim: To identify some novel fatty acid hydrolase (FAAH) inhibitors that may contribute to the treatment of Alzheimer's disease (AD).
Methods: In-silico pharmacophore modelling including ligand-based pharmacophore modelling, virtual screening, molecular docking, molecular dynamics modelling, density functional theory and in-silico pharmacokinetics and toxicological studies were employed for the retrieving of novel FAAH inhibitors. Further, these compounds were evaluated for FAAH inhibitory activity using an in vitro enzymatic assay, and later, an in vivo streptozotocin (STZ)-induced AD model was examined in mice.
Protein tyrosine phosphatase 1b (PTP1b) is a member of the protein tyrosine phosphatase (PTP) enzyme group and encoded as PTP1N gene. Studies have evidenced an overexpression of the PTP1b enzyme in metabolic syndrome, anxiety, schizophrenia, neurodegeneration, and neuroinflammation. PTP1b inhibitor negatively regulates insulin and leptin pathways and has been explored as an antidiabetic agent in various clinical trials.
View Article and Find Full Text PDFSystemic hypertension, a common metabolic disorder, poses significant health risks despite the availability of antihypertensive drugs. Nyctanthes arbor-tristis has garnered increasing attention for its perceived efficacy and safety, though its mechanisms of action and the bioactive compounds responsible for its antihypertensive effects remain elusive. Therefore, this study aims to elucidate the antihypertensive activity of N.
View Article and Find Full Text PDFCell Biochem Funct
December 2024
The renin-angiotensin system (RAS) is crucial for regulating and understanding the pathophysiology of hypertension. However, there has been little focus on the breakdown of the active peptide, angiotensin II (AngII). Given that animals lacking aminopeptidase A (APA) exhibit hypertension, it may be concluded that APA is a crucial enzyme in regulating blood pressure by breaking down AngII.
View Article and Find Full Text PDFAconitum heterophyllum Wall ex Royle. (Ranunculaceae) is a traditional medicinal herb that has shown extensive pharmacological potential to treat cough, diarrhea, and infectious diseases but no scientific evidence is available to validate its antiasthmatic potential. In this study, we have investigated the tracheal relaxation and antiasthmatic activity of the selected bioactive fraction of A.
View Article and Find Full Text PDFAlzheimer's disease (AD) has many etiologies and the impact of gender on AD changes throughout time. As a consequence of advancements in precision medical procedures and methodology, Alzheimer's disease is now better understood and treated. Several risk factors may be addressed to lower one's chances of developing Alzheimer's disease or associated dementia (ADRD).
View Article and Find Full Text PDFAlzheimer's disease (AD) is a multifaceted neurodegenerative condition. The pathogenesis of AD is highly intricate and the disease is apparent in the aged population ~ 50-70 years old. Even after > 100 years of research, the root origin of AD and its pathogenesis is unclear, complex and multifaceted.
View Article and Find Full Text PDFJ Ayurveda Integr Med
November 2023
Background: Decalepis hamiltonii (D. hamiltonii) is Indian folk medicine in herbal preparations, to reduce appetite, and cures dysentery, bronchitis, uterine hemorrhage, and other ailments.
Objective: The current investigation focused on the hepatoprotective effect of D.
Biocatalytic and chemoenzymatic biosynthesis are powerful methods of organic chemistry that use enzymes to execute selective reactions and allow the efficient production of organic compounds. The advantages of these approaches include high selectivity, mild reaction conditions, and the ability to work with complex substrates. The utilization of chemoenzymatic techniques for the synthesis of complicated compounds has lately increased dramatically in the area of organic chemistry.
View Article and Find Full Text PDFAim: We investigated the effect of mitochondria transfer in high fat diet and streptozotocin (HFD + STZ) induced metabolic syndrome (MeS) in rats. The effect of mitochondria transfer in MeS with co-existing hypertension, hyperlipidaemia, diabetes and fatty liver together, has not been reported.
Materials And Methods: Heathy mitochondria was transferred intravenously and the effect on several physiological parameters and biochemical parameters were examined in HFD + STZ rats.
Background: Metabolic syndrome is one of the major non-communicable global health hazards of the modern world owing to its amplifying prevalence. Acetyl coenzyme-A carboxylase 2 (ACC 2) is one of the most crucial enzymes involved in the manifestation of this disease because of its regulatory role in fatty acid metabolism.
Objective: To find novel potent ACC 2 inhibitors as therapeutic potential leads for combating metabolic syndrome.
The glucokinase regulator (GCKR) gene encodes an inhibitor of the glucokinase enzyme (GCK), found only in hepatocytes and responsible for glucose metabolism. A common GCKR coding variation has been linked to various metabolic traits in genome-wide association studies. Rare GCKR polymorphisms influence GKRP activity, expression, and localization.
View Article and Find Full Text PDFAmong the various prominent fungal infections, superficial ones are widespread. A large number of antifungal agents and their formulations for topical use are commercially available. They have some pharmacokinetic limitations which cannot be retracted by conventional delivery systems.
View Article and Find Full Text PDFAkt, a known serine/threonine-protein kinase B has been revealed to be an imperative protein of the PI3K/Akt pathway. Akt is available in three isoforms, Akt1, Akt2, and Akt3. Ubiquitously expressed Akt1 & Akt2 are essential for cell survival and are believed to be involved in regulating glucose homeostasis.
View Article and Find Full Text PDFBackground: Tylophora indica (Burm. f.) Merr is a climbing perennial plant reported in Indian traditional system of medicine for its use in allergy and asthma.
View Article and Find Full Text PDF1H-indol-2,3-dione (isatin) class of biologically active compounds have analgesic, anti-microbial, anti-inflammatory, anti-tubercular, anti-proliferative properties, and is also useful for the treatment of SARS-CoV. Schiff bases containing isatin moiety are known to have broad spectrum of biological activities like anti-viral, anti-tubercular, anti-fungal, and anti-bacterial. In this work, several Schiff base derivatives have been synthesized using two methods (synthetic and microwave) by reacting isatin with -phenylenediamine.
View Article and Find Full Text PDFEmerging and re-emerging illnesses will probably present a new hazard of infectious diseases and have fostered the urge to research new antiviral agents. Most of the antiviral agents are analogs of nucleosides and only a few are non-nucleoside antiviral agents. There is quite a less percentage of marketed/clinically approved non-nucleoside antiviral medications.
View Article and Find Full Text PDFAlzheimer's disease (AD) is the most common form of dementia, having characteristic clinical features of progressive memory loss and visuospatial, language, and cognitive impairment. In addition, patients often suffer from comorbid depression and aggression. Aging is a major contributing factor, though the exact pathophysiological involvement in the disease progression is debatable.
View Article and Find Full Text PDFInflammopharmacology
June 2023
Simvastatin is a semisynthetic inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and is used extensively to treat atherosclerotic cardiovascular disease. Apart from the lipid-lowering effect, simvastatin has been documented to offer impressive vasorelaxant activity. However, the mechanism associated with this vasorelaxant activity has yet not been substantially explored.
View Article and Find Full Text PDFEndocr Metab Immune Disord Drug Targets
September 2023
Background: Metabolic syndrome, also referred to as Syndrome X or obesity syndrome is a cluster of diseases prevalent worldwide in both developed and developing countries. According to WHO, it is referred to as a pathological condition wherein multiple disorders are manifested in the same individual. These include hypertension, hyperglycemia, dyslipidemia and abdominal obesity.
View Article and Find Full Text PDFProc Natl Acad Sci India Sect B Biol Sci
November 2022
Asthma is a disease of the airways that is characterized by chronic inflammation and disordered airway function. The purpose of writing the current review paper is to review the history, current situation, control history, challenges, and ongoing management programs of asthma. Some official websites of known respiratory professional bodies were consulted for asthma guidelines, and information from Google Scholar® and PubMed® was also consulted.
View Article and Find Full Text PDFReserpine is as old as the scientific diagnosis of hypertension. For many years' clinicians have used it for the treatment of high blood pressure, but with the passage of time and introduction of new anti-hypertensive drugs, the usage of reserpine has gone down drastically most probably due to poorly understood mechanism of action and multiple misleading adverse effects precisely due to high dosing of reserpine. With an aim to elucidate the specific mechanism of action, we screened reserpine against various targets associated with regulation of blood pressure.
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