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In vitro Comparison of Anticancer and Immunomodulatory Activities of Resveratrol and its Oligomers

Zhang et al. | Sep 02, 2020

<em>In vitro</em> Comparison of Anticancer and Immunomodulatory Activities of Resveratrol and its Oligomers

Resveratrol is a type of stillbenoid, a phenolic compound produced in plants, that is known for its anti-inflammatory and anticancer effects. Many oligomers of resveratrol have recently been isolated their bioactivities remain unknown. Here, authors compared the bioactivities of resveratrol with natural dimers (ε-viniferin and gnetin H) and trimers (suffruticosol B and C). Results provide preliminary evidence that resveratrol oligomers could be potential preventive or therapeutic agents for cancers and other immune-related diseases

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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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Determining the Effects of Voice Pitch on Adolescent Perception, Subconscious Bias, and Marketing Success Using Electroencephalography

Guan et al. | Apr 28, 2021

Determining the Effects of Voice Pitch on Adolescent Perception, Subconscious Bias, and Marketing Success Using Electroencephalography

Voice pitch affects perceived authoritativeness, competency, and leadership capacity. In this study, the authors suggest that examining certain measures of brain activity collected using an affordable EEG could predict advertising effectiveness, which may be invaluable in future neuromarketing research. Understanding voice pitch and other factors that cause implicit bias may allow significant advances in marketing, facilitating business success.

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How has California’s Shelter-in-Place Order due to COVID-19 and the Resulting Reduction in Human Activity Affected Air and Water Quality?

Everitt et al. | Feb 15, 2021

How has California’s Shelter-in-Place Order due to COVID-19 and the Resulting Reduction in Human Activity Affected Air and Water Quality?

As the world struggled to grapple with the emerging COVID-19 pandemic in 2020, many countries instated policies to help minimize the spread of the virus among residents. This inadvertently led to a decrease in travel, and in some cases, industrial output, two major sources of pollutants in today's world. Here, the authors investigate whether California's shelter-in-place policy was associated with a measurable decrease in water and air pollution in that state between June and July of 2020, compared to the preceeding five years. Their findings suggest that, by some metrics, air quality improved within certain areas while water quality was relatively unchanged. Overall, these findings suggest that changing human behavior can, indeed, help reduce the level of air pollutants that compromise air quality.

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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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High-throughput virtual screening of novel dihydropyrimidine monastrol analogs reveals robust structure-activity relationship to kinesin Eg5 binding thermodynamics

Shern et al. | Jan 20, 2021

High-throughput virtual screening of novel dihydropyrimidine monastrol analogs reveals robust structure-activity relationship to kinesin Eg5 binding thermodynamics

As cancer continues to take millions of lives worldwide, the need to create effective therapeutics for the disease persists. The kinesin Eg5 assembly motor protein is a promising target for cancer therapeutics as inhibition of this protein leads to cell cycle arrest. Monastrol, a small dihydropyrimidine-based molecule capable of inhibiting the kinesin Eg5 function, has attracted the attention of medicinal chemists with its potency, affinity, and specificity to the highly targeted loop5/α2/α3 allosteric binding pocket. In this work, we employed high-throughput virtual screening (HTVS) to identify potential small molecule Eg5 inhibitors from a designed set of novel dihydropyrimidine analogs structurally similar to monastrol.

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