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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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Can essential oils be allelopathic to Lolium multiforum without harming Solanum lycopersicum?

Madan et al. | Nov 13, 2021

 Can essential oils be allelopathic to <em>Lolium multiforum</em> without harming <em>Solanum lycopersicum</em>?

Seeking to investigate eco-friendly biological methods to control weeds and enhance food crop yields, here the authors considered the effects of three essential oils on seed germination and radicle length of both a weed and a common crop. They found that treatment with turmeric oil had phytotoxic potential, leading to a reduction in both seed germination and radicle length of the weed. In contrast, ginger oil possessed allelopathic properties towards both. The authors suggest that essential oils could be used as eco-friendly bio-herbicides.

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Failure of colony growth in probiotic Lactobacillus casei Shirota as result of preservative sorbic acid

Raymond et al. | May 07, 2023

Failure of colony growth in probiotic <i>Lactobacillus casei</i> Shirota as result of preservative sorbic acid

This study tested the proficiency of different concentrations of the antimicrobial sorbic acid to inhibit the probiotic Lactobacillus casei Shirota. It was hypothesized that sorbic acid’s use as a bacterial deterrent would also target this bacterial strain of Lactobacillus. The results supported the hypothesis, with the colony count of L. casei Shirota having significant decreases at all concentrations of sorbic acid. These results additionally suggest that even under the FDA sorbic acid restrictions of 0.03% concentration, damaging effects could be seen in L. casei Shirota.

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Culturally Adapted Assessment Tool for Autism Spectrum Disorder and its Clinical Significance

Das et al. | Apr 19, 2021

Culturally Adapted Assessment Tool for Autism Spectrum Disorder and its Clinical Significance

Diagnosing of Autism Spectrum Disorder (ASD) using tools developed in the West is challenging in the Indian setting due to a huge diversity in sociocultural and economic backgrounds. Here, the authors developed a home-based, audiovisual game app (Autest) suitable for ASD risk assessment in Indian children under 10 years of age. Ratings suggested that the tool is effective and can reduce social inhibition and facilitate assessment. Further usage and development of Autest can improve risk assessment and early intervention measures for children with ASD in India.

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Blue light blocking glasses: do they do what they promise?

Lee et al. | Dec 13, 2023

Blue light blocking glasses: do they do what they promise?
Image credit: nacer eddine

With increased screen time and exposure to blue light, an increasing number of people have sleep deprivation. Blue light suppresses the release of melatonin and hinders sleep at night. We hypothesized that people could get a greater amount of sleep by controlling the blue light exposure from screen time before bedtime. BBG’s effect on reducing time to fall asleep was significant within the teenage group, but not significant in the adult group. This indicated that BBG could improve the time taken to sleep for young teenagers post screen time in the evening.

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In silico modeling of emodin’s interactions with serine/threonine kinases and chitosan derivatives

Suresh et al. | Jan 10, 2022

<i>In silico</i> modeling of emodin’s interactions with serine/threonine kinases and chitosan derivatives

Here, through protein-ligand docking, the authors investigated the effect of the interaction of emodin with serine/threonine kinases, a subclass of kinases that is overexpressed in many cancers, which is implicated in phosphorylation cascades. Through molecular dynamics theyfound that emodin forms favorable interactions with chitosan and chitosan PEG (polyethylene glycol) copolymers, which could aid in loading drugs into nanoparticles (NPs) for targeted delivery to cancerous tissue. Both polymers demonstrated reasonable entrapment efficiencies, which encourages experimental exploration of emodin through targeted drug delivery vehicles and their anticancer activity.

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