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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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Modulation of VEGF and TGF beta in 5-FU induced inflammation in MCF-7 using an herbal formulation

Vinay Nair et al. | Jun 03, 2022

Modulation of VEGF and TGF beta in 5-FU induced inflammation in MCF-7 using an herbal formulation

Acquired drug resistance is an increasing challenge in treating cancer with chemotherapy. One mechanism
behind this resistance is the increased inflammation that supports the progression and development of
cancer that arises because of the drug’s presence. Integrative oncology is the field that focuses on including natural products alongside traditional therapy to create a treatment that focuses on holistic patient well-being.
In this study, the authors demonstrate that the use of an herbal formulation, consisting of turmeric and green tea, alongside a traditional chemotherapeutic drug, 5-fluorouracil (FU) significantly decreases the level of cytokines produced in breast cancer cells when compared to the levels produced when exposed solely to the chemo drug. The authors conclude that this combination of treatment, based on the principle of integrative oncology, shows potential for reducing the resistance against treatment conferred through increased inflammation. Consequently, this suggests a prospective way forward in improving the efficacy of cancer treatment.

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RNAi-based Gene Therapy Targeting ZGPAT Promotes EGF-dependent Wound Healing

Lee et al. | Nov 15, 2021

RNAi-based Gene Therapy Targeting ZGPAT Promotes EGF-dependent Wound Healing

Wound-healing involves a sequence of events, such as inflammation, proliferation, and migration of different cell types like fibroblasts. Zinc Finger CCCH-type with G-Patch Domain Containing Protein (ZGPAT), encodes a protein that has its main role as a transcription repressor by binding to a specific DNA sequence. The aim of the study was to find out whether inhibiting ZGPAT will expedite the wound healing process by accelerating cell migration. This treatment strategy can provide a key to the development of wound healing strategies in medicine and cellular biology.

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Strain-selective in vitro and in silico structure activity relationship (SAR) of N-acyl β-lactam broad spectrum antibiotics

Poosarla et al. | Oct 19, 2021

Strain-selective <i>in vitro</i> and <i>in silico</i> structure activity relationship (SAR) of N-acyl β-lactam broad spectrum antibiotics

In this study, the authors investigate the antibacterial efficacy of penicillin G and its analogs amoxicillin, carbenicillin, piperacillin, cloxacillin, and ampicillin, against four species of bacteria. Results showed that all six penicillin-type antibiotics inhibit Staphylococcus epidermidis, Escherichia coli, and Neisseria sicca with varying degrees of efficacy but exhibited no inhibition against Bacillus cereus. Penicillin G had the greatest broad-spectrum antibacterial activity with a high radius of inhibition against S. epidermidis, E. coli, and N. sicca.

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The Effects of Ezetimibe on Triglyceride and Alanine Transaminase Reduction in Drosophila Melanogaster Model of Nonalcoholic Fatty Liver Disease (NAFLD)

Dania et al. | Apr 30, 2020

The Effects of Ezetimibe on Triglyceride and Alanine Transaminase Reduction in <i>Drosophila Melanogaster</i> Model of Nonalcoholic Fatty Liver Disease (NAFLD)

Nonalcoholic Fatty Liver Disease (NAFLD) is a condition where a surplus of triglycerides or fat are present in the liver. In this study, ezetimibe, a cholesterol lowering drug, was used to treat flies modeling NAFLD. Compared to the coconut oil fed flies that were transferred to the control medium, the flies transferred to the control medium treated with ezetimibe showed a decrease in their triglyceride and alanine transaminase level.

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Combating Insulin Resistance Using Medicinal Plants as a Supplementary Therapy to Metformin in 3T3-L1 Adipocytes: Improving Early Intervention-Based Diabetes Treatment

Jayram et al. | Apr 08, 2019

Combating Insulin Resistance Using Medicinal Plants as a Supplementary Therapy to Metformin in 3T3-L1 Adipocytes: Improving Early Intervention-Based Diabetes Treatment

A primary cause of diabetes is insulin resistance, which is caused by disruption of insulin signal transduction. The objective of this study was to maximize insulin sensitivity by creating a more effective, early intervention-based treatment to avert severe T2D. This treatment combined metformin, “the insulin sensitizer”, and medicinal plants, curcumin, fenugreek, and nettle.

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The Protective Effects of Panax notoginseng Saponin on the Blood-Brain Barrier via the Nrf2/ARE Pathway in bEnd3 Cells

Yang et al. | Apr 06, 2016

The Protective Effects of <i>Panax notoginseng</i> Saponin on the Blood-Brain Barrier via the Nrf2/ARE Pathway in bEnd3 Cells

Disruption of the blood-brain barrier (BBB) is related to many neurological disorders, and can be caused by oxidative stress to cerebral microvascular endothelial cells (CMECs) composing the BBB. The authors of the paper investigated the protective effects of the total saponins in the leaves of Panax notoginseng (LPNS) on oxidative-stress-induced damage in a mouse cerebral microvascular endothelial cell line.

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