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Developing anticholinergic drugs for the treatment of asthma with improved efficacy

Wong et al. | Jul 05, 2023

Developing anticholinergic drugs for the treatment of asthma with improved efficacy
Image credit: Wong et al.

Anticholinergics are used in treating asthma, a chronic inflammation of the airways. These drugs block human M1 and M2 muscarinic acetylcholine receptors, inhibiting bronchoconstriction. However, studies have reported complications of anticholinergic usage, such as exacerbated eosinophil production and worsened urinary retention. Modification of known anticholinergics using bioisosteric replacements to increase efficacy could potentially minimize these complications. The present study focuses on identifying viable analogs of anticholinergics to improve binding energy to the receptors compared to current treatment options. Glycopyrrolate (G), ipratropium (IB), and tiotropium bromide (TB) were chosen as parent drugs of interest, due to the presence of common functional groups within the molecules, specifically esters and alcohols. Docking score analysis via AutoDock Vina was used to evaluate the binding energy between drug analogs and the muscarinic acetylcholine receptors. The final results suggest that G-A3, IB-A3, and TB-A1 are the most viable analogs, as binding energy was improved when compared to the parent drug. G-A4, IB-A4, IB-A5, TB-A3, and TB-A4 are also potential candidates, although there were slight regressions in binding energy to both muscarinic receptors for these analogs. By researching the effects of bioisosteric replacements of current anticholinergics, it is evident that there is a potential to provide asthmatics with more effective treatment options.

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Who is at Risk for a Spinal Fracture? – A Comparative Study of National Health and Nutrition Examination Survey Data

He et al. | Mar 01, 2018

Who is at Risk for a Spinal Fracture? – A Comparative Study of National Health and Nutrition Examination Survey Data

One common age-related health problem is the loss of bone mineral density (BMD), which can lead to a variety of negative health outcomes, including increased risk of spinal fracture. In this study, the authors investigate risk factors that may be predictive of an individual's risk of spinal fracture. Their findings provide valuable information that clinicians can use in patient evaluations.

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Use of yogurt bacteria as a model surrogate to compare household cleaning solutions

Shukla et al. | May 07, 2023

Use of yogurt bacteria as a model surrogate to compare household cleaning solutions
Image credit: CDC

While resources on the safety of household cleaning products are plentiful, measures of efficacy of these cleaning chemicals against bacteria and viruses remain without standardization in the consumer market. The COVID pandemic has exasperated this knowledge gap, stoking the growth of misinformation and misuse surrounding household cleaning chemicals. Arriving at a time dire for sanitization standardization, the authors of this paper have created a quantifying framework for consumers by comparing a wide range of household cleaning products in their efficacy against bacteria generated by a safe and easily replicable yogurt model.

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The Effect of Cooking Method on the Amount of Fat in an Egg

Srinivasan et al. | Dec 01, 2014

The Effect of Cooking Method on the Amount of Fat in an Egg

Fat can be chemically altered during cooking through a process called lipid oxidation, which can have a negative impact on health. In this study, the authors measured the extracted fat in raw, fried and hard-boiled eggs and found that cooking eggs to a higher temperature resulted in a lower amount of extracted fat, indicating a greater amount of oxidized fat.

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Combating Insulin Resistance Using Medicinal Plants as a Supplementary Therapy to Metformin in 3T3-L1 Adipocytes: Improving Early Intervention-Based Diabetes Treatment

Jayram et al. | Apr 08, 2019

Combating Insulin Resistance Using Medicinal Plants as a Supplementary Therapy to Metformin in 3T3-L1 Adipocytes: Improving Early Intervention-Based Diabetes Treatment

A primary cause of diabetes is insulin resistance, which is caused by disruption of insulin signal transduction. The objective of this study was to maximize insulin sensitivity by creating a more effective, early intervention-based treatment to avert severe T2D. This treatment combined metformin, “the insulin sensitizer”, and medicinal plants, curcumin, fenugreek, and nettle.

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Phospholipase A2 increases the sensitivity of doxorubicin induced cell death in 3D breast cancer cell models

Lee et al. | Mar 30, 2022

Phospholipase A2 increases the sensitivity of doxorubicin induced cell death in 3D breast cancer cell models

Inefficient penetration of cancer drugs into the interior of the three-dimensional (3D) tumor tissue limits drugs' delivery. The authors hypothesized that the addition of phospholipase A2 (PLA2) would increase the permeability of the drug doxorubicin for efficient drug penetration. They found that 1 mM PLA2 had the highest permeability. Increased efficiency in drug delivery would allow lower concentrations of drugs to be used, minimizing damage to normal cells.

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Kinetic Monitoring and Fourier-Transform Infrared (FTIR) Spectroscopy of the Green Oxidation of (-)-Menthol to (-)-Menthone

Surapaneni et al. | Aug 06, 2020

Kinetic Monitoring and Fourier-Transform Infrared (FTIR) Spectroscopy of the Green Oxidation of (-)-Menthol to (-)-Menthone

In an effort to reduce the production of hazardous substances, green chemistry aims to make chemical processes more sustainable. One way to do so is changing solvents in chemical reactions. Here, authors assessed different “green” solvents on the oxidation of (-)-menthol to (-)-menthone using Fourier-transform infrared (FTIR) spectroscopy, optimizing the solvent system for this reaction.

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Do Attractants Bias the Results of Malaise Trap Research?

Martinez et al. | Jan 22, 2020

Do Attractants Bias the Results of Malaise Trap Research?

Malaise traps are commonly used to collect flying insects for a variety of research. In this study, researchers hypothesized the attractants used in these traps may create bias in insect studies that could lead to misinterpreted data. To test this hypothesis two different kinds of attractant were used in malaise traps, and insect diversity was assessed. Attractants were found to alter the dispersion of insects caught in traps. These findings can inform future malaise traps studies on insect diversity.

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Glyphosate Levels in American Food Products Meet Government Safety Levels Yet Exceed Concentrations Associated with Negative Effects

Lee et al. | Mar 25, 2019

Glyphosate Levels in American Food Products Meet Government Safety Levels Yet Exceed Concentrations Associated with Negative Effects

Glyphosate is the active ingredient in the herbicide Roundup, frequently used in the agricultural industry worldwide. Current literature reveals contradictory findings regarding the effects of glyphosate on vertebrates, leading to concerns about human consumption and differing views on safety levels. Here, authors sought to measure glyphosate levels in common commercially available food products. While some product levels exceed the thresholds at which negative effects have been observed, none exceed government limits.

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