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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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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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Enhancing activity of antibiotics against Staphylococcus aureus with Shuang-Huang-Lian

Liu et al. | Sep 29, 2022

Enhancing activity of antibiotics against Staphylococcus aureus with Shuang-Huang-Lian

Staphylococcus aureus is a major pathogen in both hospitals and the community and can cause systemic infections such as pneumonia. Multi-drug resistant strains, such as Methicillin-resistant S. aureus (MRSA) are particularly worrisome. In order to reduce the development of bacterial resistance, we hypothesized that two selected traditional Chinese medicines, Shuang-Huang-Lian (SHL) and Lan-Qin, would be effective against S. aureus. The results showed that SHL had a synergistic effect with gentamicin as well as additive effects with penicillin and cefazolin against S. aureus compared with using antibiotics alone.

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