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Modular mimics of neuroactive alkaloids - design, synthesis, and cholinesterase inhibitory activity of rivastigmine analogs

Yu et al. | Sep 12, 2022

Modular mimics of neuroactive alkaloids - design, synthesis, and cholinesterase inhibitory activity of rivastigmine analogs

Naturally occurring neuroactive alkaloids are often studied for their potential to treat Neurological diseases. This team of students study Rivastigmine, a potent cholinesterase inhibitor that is a synthetic analog of physostigmine, which comes from the Calabar bean plant Physostigma venenosum. By comparing the effects of optimized synthetic analogs to the naturally occurring alkaloid, they determine the most favorable analog for inhibition of acetylcholinesterase (AChE), the enzyme that breaks down the neurotransmitter acetylcholine (ACh) to terminate neuronal transmission and signaling between synapses.

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Computational Structure-Activity Relationship (SAR) of Berberine Analogs in Double-Stranded and G-Quadruplex DNA Binding Reveals Both Position and Target Dependence

Sun et al. | Dec 18, 2020

Computational Structure-Activity Relationship (SAR) of Berberine Analogs in Double-Stranded and G-Quadruplex DNA Binding Reveals Both Position and Target Dependence

Berberine, a natural product alkaloid, and its analogs have a wide range of medicinal properties, including antibacterial and anticancer effects. Here, the authors explored a library of alkyl or aryl berberine analogs to probe binding to double-stranded and G-quadruplex DNA. They determined that the nature of the substituent, the position of the substituent, and the nucleic acid target affect the free energy of binding of berberine analogs to DNA and G-quadruplex DNA, however berberine analogs did not result in net stabilization of G-quadruplex DNA.

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Discovery of the Heart in Mathematics: Modeling the Chaotic Behaviors of Quantized Periods in the Mandelbrot Set

Golla et al. | Dec 14, 2020

Discovery of the Heart in Mathematics: Modeling the Chaotic Behaviors of Quantized Periods in the Mandelbrot Set

This study aimed to predict and explain chaotic behavior in the Mandelbrot Set, one of the world’s most popular models of fractals and exhibitors of Chaos Theory. The authors hypothesized that repeatedly iterating the Mandelbrot Set’s characteristic function would give rise to a more intricate layout of the fractal and elliptical models that predict and highlight “hotspots” of chaos through their overlaps. The positive and negative results from this study may provide a new perspective on fractals and their chaotic nature, helping to solve problems involving chaotic phenomena.

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Mechanistic deconvolution of autoreduction in tetrazolium-based cell viability assays

Tran et al. | Jul 12, 2024

Mechanistic deconvolution of autoreduction in tetrazolium-based cell viability assays

Optical reporters like tetrazolium dyes, exemplified by 5-diphenyl tetrazolium bromide (MTT), are effective tools for quantifying cellular responses under experimental conditions. These dyes assess cell viability by producing brightly-colored formazan dyes when reduced inside active cells. However, certain small molecules, including reducing agents like ascorbic acid, cysteine, and glutathione (GSH), can interfere with MTT assays, potentially compromising accuracy.

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