Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations.

Nine compounds () containing the morpholine moiety were assessed for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). Most of the compounds potently inhibited MAO-B; most potently inhibited with an IC value of 0.030 µM, followed by (0.

Fast and efficient degradation of water pollutant dyes and fungicide by novel sulfur-doped graphene oxide-modified AgPO nanocomposite.

The sulfur-doped graphene oxide (sGO)-integrated AgPO composite displayed very high catalytic activity toward prominent water pollutants like textile dyes and fungicide under sunlight. The optimum amount of sGO doping was found as 5% for degradation. The novel composite degraded 99% of methylene blue (MB) in only 5 min of sunlight exposure, which is 16 and 8 times faster than AgPO and 5% GO-AgPO.

Can Cancer Diagnosis Help in Quitting Tobacco? Barriers and Enablers to Tobacco Cessation Among Head and Neck Cancer Patients from a Tertiary Cancer Center in South india.

Background: Tobacco use contributes to almost 40% of the cancers in India. Considering the potential threat, many preventive measures have been instigated in the country. However, tobacco cessation for hospitalized cancer patients is an unexplored territory in India.

Integrating psycho-oncology services in cancer care in India.

Psychological distress is often an under-diagnosed problem in cancer care. Addressing psychosocial issues would enhance treatment compliance, physician-patient relationship, treatment efficacy and quality of life. This article emphasizes the importance of integrating psycho-oncology services in cancer care and attempts to define the various roles that a psycho-oncologist can play across the entire trajectory.

Cell fate clusters in ICM organoids arise from cell fate heredity and division: a modelling approach.

During the mammalian preimplantation phase, cells undergo two subsequent cell fate decisions. During the first decision, the trophectoderm and the inner cell mass are formed. Subsequently, the inner cell mass segregates into the epiblast and the primitive endoderm.

Natural Products Database Screening for the Discovery of Naturally Occurring SARS-Cov-2 Spike Glycoprotein Blockers.

SARS-CoV-2 coronavirus has been recognized the causative agent of the recent and ongoing pandemic. Effective and specific antiviral agents or vaccines are still missing, despite a large plethora of compounds have been proposed and tested worldwide. New compounds are requested urgently and virtual screening can offer fast and robust predictions to investigate.

An Integrated Approach to Selecting a Prepared Medical Decision-Maker.

Background: We implemented a systematic multidisciplinary process to engage new outpatients with cancer in selecting and preparing a medical decision-maker.

Measures: Templated advance care planning notes and medical power of attorney documents were used in the electronic health record by the third office visit.

Intervention: Patients were coached to meet with social work from a "culture of yes," viewed a video about the importance of selecting a prepared medical a decision-maker in English or in Spanish, and referenced cards containing simple explanations of advance directives when responding to advance directive questions.

COVID-19 and Domestic Animals: Exploring the Species Barrier Crossing, Zoonotic and Reverse Zoonotic Transmission of SARS-CoV-2.

Background: To date, more than thirty animals have been tested positive for SARS-CoV-2; all of them infected by humans with COVID-19. Some animal experiments suggested the possibility of animal to animal transmission of SARS-CoV-2 that was seen in some cases of infected animals. Animal to human transmission was considered unlikely until investigations revealed the possibility of mink to human transmission of SARS-CoV-2 in the Netherlands.

Design, Synthesis, and Biological Evaluation of Pyridazinones Containing the (2-Fluorophenyl) Piperazine Moiety as Selective MAO-B Inhibitors.

Twelve pyridazinones (-) containing the (2-fluorophenyl) piperazine moiety were designed, synthesized, and evaluated for monoamine oxidase (MAO) -A and -B inhibitory activities. was found to be the most potent MAO-B inhibitor with an IC value of 0.013 µM, followed by (IC = 0.

Neuroprotective Effects of Ellagic Acid in Alzheimer's Disease: Focus on Underlying Molecular Mechanisms of Therapeutic Potential.

Neurodegeneration is a multifactorial process involved the different cytotoxic pathways that lead to neuronal cell death. Alzheimer's disease (AD) is a persistent neurodegenerative disorder that normally has a steady onset and gradually worsens. Neuropathology, AD is characterized by the presence of neuroinflammation, mitochondrial dysfunction, increased oxidative stress, decreased antioxidant defense as well as increased acetylcholinesterase activity.

A Workflow of Integrated Resources to Catalyze Network Pharmacology Driven COVID-19 Research.

Motivation: In the event of an outbreak due to an emerging pathogen, time is of the essence to contain or to mitigate the spread of the disease. Drug repositioning is one of the strategies that has the potential to deliver therapeutics relatively quickly. The SARS-CoV-2 pandemic has shown that integrating critical data resources to drive drug-repositioning studies, involving host-host, hostpathogen and drug-target interactions, remains a time-consuming effort that translates to a delay in the development and delivery of a life-saving therapy.

Educational Status, Cancer Stage, and Survival in South India: A Population-Based Study.

Purpose: Lower socioeconomic status is associated with more advanced cancer at the time of cancer diagnosis. It is unknown whether this leads to inferior survival in low- and middle-income countries. Here, we explore the association between educational level and survival in South India.

Structure-activity relationship (SAR) studies of N-(3-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine (SRI-22819) as NF-ҡB activators for the treatment of ALS.

ALS is a rare type of progressive neurological disease with unknown etiology. It results in the gradual degeneration and death of motor neurons responsible for controlling the voluntary muscles. Identification of mutations in the superoxide dismutase (SOD) 1 gene has been the most significant finding in ALS research.

A Comprehensive Overview of Colon Cancer- A Grim Reaper of the 21st Century.

A few decades ago, the incidence of colorectal cancer (CRC) was low and is now the fourth in the list of deadly cancers producing nearly a million deaths annually. A population that is aging along with risk factors such as smoking, obesity, sedentary lifestyle with little or no physical activity, and non-healthy food habits of developed countries can increase the risk of colorectal cancer. The balance in gut microbiota and the metabolites produced during bacterial fermentation within the host plays a significant role in regulating intestinal diseases as well as colorectal cancer development.

(Hetero-)(arylidene)arylhydrazides as Multitarget-Directed Monoamine Oxidase Inhibitors.

Fourteen (hetero-)(arylidene)arylhydrazide derivatives (-) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound most potently inhibited MAO-B with an IC value of 0.025 ± 0.

An Agathokakological Tale of Δ-THC: Exploration of Possible Biological Targets.

Δ-Tetrahydrocannabinol (Δ-THC), the active phytocannabinoid in cannabis, is virtually an adjunct to the endogenous endocannabinoid signaling system. By interacting with G-proteincoupled receptors CB1 and CB2, Δ-THC affects peripheral and central circulation by lowering sympathetic activity, altering gene expression, cell proliferation, and differentiation, decreasing leukocyte migration, modulating neurotransmitter release, thereby modulating cardiovascular functioning, tumorigenesis, immune responses, behavioral and locomotory activities. Δ-THC effectively suppresses chemotherapy-induced vomiting, retards malignant tumor growth, inhibits metastasis, and promotes apoptosis.

Natural compounds from Leea macrophylla enhance phagocytosis and promote osteoblasts differentiation by alkaline phosphatase, type 1 collagen, and osteocalcin gene expression.

The current study investigated the immunomodulating and osteoblast differentiation potential of the natural compounds from Leea macrophylla (LMN). Immunomodulatory effects have been investigated by the phagocytosis of Candida albicans using polymorphonuclear neutrophil cells in the in vitro slide method. A bioactivity-guided fractionation technique was used to evaluate the stimulating effect of L.

Evaluation of pooled sample analysis strategy in expediting case detection in areas with emerging outbreaks of COVID-19: A pilot study.

Timely diagnosis of COVID-19 infected individuals and their prompt isolation are essential for controlling the transmission of SARS-CoV-2. Though quantitative reverse transcriptase PCR (qRT-PCR) is the method of choice for COVID-19 diagnostics, the resource-intensive and time-consuming nature of the technique impairs its wide applicability in resource-constrained settings and calls for novel strategies to meet the ever-growing demand for more testing. In this context, a pooled sample testing strategy was evaluated in the setting of emerging disease outbreak in 3 central Indian districts to assess if the cost of the test and turn-around time could be reduced without compromising its diagnostic characteristics and thus lead to early containment of the outbreak.

Exploring the Therapeutic Potentials of Highly Selective Oxygenated Chalcone Based MAO-B Inhibitors in a Haloperidol-Induced Murine Model of Parkinson's Disease.

Parkinson's disease (PD) is a neurodegenerative disorder of dopaminergic, noradrenergic, and serotonergic systems, in which dopamine, noradrenaline, and serotonin levels are depleted and lead to the development of motor and non-motor symptoms such as tremor, bradykinesia, weight changes, fatigue, depression, and visual hallucinations. Therapeutic strategies place much focus on dopamine replacement and the inhibition of dopamine metabolism. The present study was based on the known abilities of chalcones to act as molecular scaffolds that selectively inhibit MAO-B with the added advantage of binding reversibly.

Comparison of predicted postoperative forced expiratory volume in the first second (FEV1) using lung perfusion scintigraphy with observed forced expiratory volume in the first second (FEV1) post lung resection.

Lung perfusion scintigraphy is done as a part of preoperative evaluation in lung cancer patients for the prediction of postoperative forced expiratory volume in the first second (FEV1). This study was performed to see the accuracy of prediction of postoperative FEV1 by perfusion scintigraphy for patients undergoing lobectomy/pneumonectomy by comparing it with actual postoperative FEV1 obtained by spirometry 4-6 months after surgery. We retrospectively reviewed 50 surgically resected lung cancer patients who underwent preoperative spirometry, lung perfusion study, and postoperative spirometry.

Transcriptome profiling at osmotic and ionic phases of salt stress response in bread wheat uncovers trait-specific candidate genes.

Background: Bread wheat is one of the most important crops for the human diet, but the increasing soil salinization is causing yield reductions worldwide. Improving salt stress tolerance in wheat requires the elucidation of the mechanistic basis of plant response to this abiotic stress factor. Although several studies have been performed to analyze wheat adaptation to salt stress, there are still some gaps to fully understand the molecular mechanisms from initial signal perception to the onset of responsive tolerance pathways.

Selected 1,3-Benzodioxine-Containing Chalcones as Multipotent Oxidase and Acetylcholinesterase Inhibitors.

Chalcones are considered effective templates for the development of monoamine oxidase (MAO) and cholinesterase (ChE) inhibitors. The present work describes the syntheses of selected 1,3-benzodioxine-containing chalcones (CD3, CD8 and CD10), and their inhibitory activities against MAO-A, MAO-B, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Compound CD8 most potently inhibited MAO-B with an IC value of 0.