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Testing Simarouba amara’s therapeutic effects against weedicide-induced tumor-like morphology in planarians

Thiagarajan et al. | Apr 26, 2024

Testing Simarouba amara’s therapeutic effects against weedicide-induced tumor-like morphology in planarians

According to the World Health Organization, cancer is a leading cause of death globally. The disease’s prevalence is rapidly increasing in association with factors including the increased use of pesticides and herbicides, such as glyphosate, which is one of the most widely used herbicide ingredients. Natural antioxidants and phytochemicals are being tested as anti-cancer agents due to their antiproliferative, antioxidative, and pro-apoptotic properties. Thus, we aimed to investigate the potential role of S. amara extract as a therapeutic agent against glyphosate-induced toxicity and tumor-like morphologies in regenerating and homeostatic planaria (Dugesia dorotocephala).

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A Novel Alzheimer's Disease Therapeutic Model: Attenuating Hyperphosphorylated Tau and Amyloid β (Aβ) Aggregates by Characterizing Antioxidative, Anti-Inflammatory, and Neuroprotective Properties of Natural Extracts

Pokkunuri et al. | Jul 25, 2022

A Novel Alzheimer's Disease Therapeutic Model: Attenuating Hyperphosphorylated Tau and Amyloid β (Aβ) Aggregates by Characterizing Antioxidative, Anti-Inflammatory, and Neuroprotective Properties of Natural Extracts

Oxidative damage and neuro-inflammation were the key pathways implicated in the pathogenesis of Alzheimer’s disease. In this study, 30 natural extracts from plant roots and leaves with extensive anti-inflammatory and anti-oxidative properties were consumed by Drosophila melanogaster. Several assays were performed to evaluate the efficacy of these combinational extracts on delaying the progression of Alzheimer’s disease. The experimental group showed increased motor activity, improved associative memory, and decreased lifespan decline relative to the control group.

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Quantitative NMR spectroscopy reveals solvent effects in the photochemical degradation of thymoquinone

Mandava et al. | Dec 16, 2023

Quantitative NMR spectroscopy reveals solvent effects in the photochemical degradation of thymoquinone

Thymoquinone is a compound of great therapeutic potential and scientific interest. However, its clinical administration and synthetic modifications are greatly limited by its instability in the presence of light. This study employed quantitative 1H nuclear magnetic resonance (NMR) spectroscopy to identify the effect of solvation on the degradation of thymoquinone under ultraviolet light (UV). It found that the rate of degradation is highly solvent dependent occurs maximally in chloroform.

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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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Reactivity-informed design, synthesis, and Michael addition kinetics of C-ring andrographolide analogs

Zhou et al. | Nov 17, 2022

Reactivity-informed design, synthesis, and Michael addition kinetics of C-ring andrographolide analogs

Here, based on the identification of androgapholide as a potential therapeutic treatment against cancer, Alzheimer's disease, diabetes, and multiple sclerosis, due to its ability to inhibit a signaling pathway in immune system function, the authors sought ways to optimize the natural product human systems by manipulating its chemical structure. Through the semisynthesis of a natural product along with computational studies, the authors developed an understanding of the kinetic mechanisms of andrographolide and semisynthetic analogs in the context of Michael additions.

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