Heterocycles in a one-pot fashion starting by catalytic formation of a three-carbon building block

What is it about?

Heterocycles are usually assembled from more than two starting materials. For making heterocycle formation smoothly and in a one-pot fashion we established the catalytic generation of alkynones, i.e. reactive Michael systems, before adding further components to the reaction mixture to selectively form the compound class of choice. By the substitution pattern of the starting materials the structural and functional diversity of these efficiently formed heterocycles are varied in a wide range.

Why is it important?

Heterocycles are the most important small molecules, since the contain functionality that is of utmost importance for their biological or materials properties. Concise, diversity-oriented heterocycle synthesis in a one-pot fashion enhance the establishing of substance libraries, which are very important to establish structure-property-function relationships of molecular materials, ranging from life sciences over molecular electronics to materials sciences. Read more about the article here: https://bit.ly/3ADAjvC

Lead finding from selected flavonoids with antiviral (SARS-CoV-2) potentials against COVID-19

What is it about?

In silico molecular docking studies can be useful to predict the binding affinity between the selected flavonoids and the target protein and play a vital role in finding an inhibitor through structure-based drug design.

Why is it important?

COVID-19 is a pandemic respiratory contagious viral (SARS-CoV-2) disease associated with high morbidity and mortality worldwide. Currently, there are no effective preventive or treatment strategies for COVID-19 and it has been declared as a global health emergency by WHO. Read more about the article here: https://bit.ly/3ys8vsq

Metabolite Profiling of Different Solvent Extracts of the Microalgae Chlorella vulgaris Via 1H NMR-Based Metabolomics

What is it about?

Metabolomics

Why is it important?

Extraction from microalgae

Read more about the article here: https://bit.ly/3wfyYaV

Search for new inhibitors of MurA

What is it about?

Research for new antibacterial agents is ongoing because of the resistance of bacteria to current antibiotics. In this research, we tried to find new antibacterial agents by starting with a bioinformatic method “virtual screening” targeting MurA, and then we completed with a biological test on bacteria.

Why is it important?

As result, four compounds had antibacterial activity, one of them carried out its activity with MIC 457μg/ml against Staphylococcus aureus. Read more about the article here: https://bit.ly/3wiXuIv

Editors Choice: The Emergence of Immune-checkpoint Inhibitors in Colorectal Cancer Therapy

Graphical Abstract:

Abstract:

Immunotherapy has revolutionized the treatment landscape in a number of solid tumors. In colorectal cancer, evidence suggests that microsatellite high (MSI-H) tumors are the most responsive to immune checkpoint blockade due to increased neo-antigen load and a favorable tumor microenvironment. Indeed, Pembrolizumab now represents a first-line option in such patients. However, MSI-H tumors represent the minority and a proportion of patients’ progress despite initially responding. Trials are investigating different immunotherapy combinatorial strategies to enhance immune response in less immunogenic colorectal tumors. Such strategies include dual immune checkpoint blockade, combining immune checkpoint inhibitors with other treatment modalities such as radiotherapy, chemotherapy or other biological or targeted agents. Moreover, there is an increasing drive to identify biomarkers to better select patients most likely to respond to immunotherapy and understand intrinsic and acquired resistance mechanisms. Apart from MSI-H tumors, there is a strong rationale to suggest that tumors with alterations in DNA polymerase epsilon and DNA polymerase delta are also likely to respond to immunotherapy and trials in this subpopulation are underway. Other strategies such as priming O6-methylguanineDNA methyltransferase silenced tumors with alkylating agents to make them receptive to immune checkpoint blockade are also being investigated. Here we discuss different colorectal subpopulations together with their likelihood of response to immune checkpoint blockade and strategies to overcome barriers to a successful clinical outcome. We summarize evidence from published clinical trials and provide an overview of trials in progress whilst discussing newer immunotherapy strategies such as adoptive cell therapies and cancer vaccines. Read more here: https://www.eurekaselect.com/191176/article

Press Release: Potato and rice protein shakes may be a viable vegan alternative to whey protein shakes

A study from the Centre for Nutraceuticals at the University of Westminster found that plant-based protein shakes may be potential viable alternatives to milk-based whey protein shakes, particularly in people with need of careful monitoring of glucose levels.

The study, published in the journal Nutrients, is the first to show potato and rice proteins can be just as effective at managing your appetite and can help better manage blood glucose levels and reduce spikes in insulin compared to whey protein.

During the study the blood metabolic response of participants was measured after drinking potato, rice and whey protein shakes. Appetite was also monitored in the following three hours to understand how these drinks may affect the participants’ hunger and their desire to eat.

The research observed that vegan protein shakes led to a lower rise in blood insulin compared to whey, while potato protein prevented any rise in insulin. This may explain the better blood glucose control following consumption of the plant-based protein and poses the question of whether vegan protein shakes are more suitable for individuals who need to need control their blood glucose levels such as diabetic and obese individuals.

Interestingly, release of the key appetite regulating hormone GLP-1 was greater after drinking the whey protein shake. However, the greater GLP-1 response did not translate to an increased feeling of fullness as there were no differences observed in appetite perception between the three different protein shakes.

Consumer trends in protein intake are on the rise with milk protein derivatives such as whey extensively used in consumer products such as protein shakes, fortified food and beverage products.

There are alternative protein products available for vegetarians and vegans such as soy, rice, wheat and pea proteins but there is a relative lack of evidence on their health benefits in comparison to milk proteins. Potato protein is a novel plant-based protein product that is obtained from the waste material from potato starch production and is a sustainable economic protein source. This study provides the first evidence to suggest that it may be an alternative to whey protein sources.

Professor M Gulrez Zariwala, corresponding author and Director of the Centre for Nutraceuticals at the University of Westminster, said: “Global concerns on sustainability have led to consumer shifts towards ethical eating and a change in dietary habits with increased adoption of vegetarian and vegan diets.

“However, research in this area is still lacking and it would be interesting to clarify whether proteins from plant sources can provide identical metabolic health benefits as those with traditional sources such as milk.

“Our results shed new light in this area and improves our understanding of how plant source proteins can be a more sustainable yet nutritionally beneficial food source. We plan to conduct follow-up studies further research this exciting area.”

Read the full Press Release to find out more: https://www.eurekalert.org/pub_releases/2021-06/uow-par062421.php

N-substituted 5-(oxoindolinyl)-2-thioxo- thiazolidinone

What is it about?

Background & Objectives: New N-substituted 5-(oxoindolinyl)-2-thioxo- thiazolidinone derivatives were synthesized.

Methods: The C2 -substituted thiazolidinone derivatives with piperidinyl and morpholinyl moieties in addition to the tetracyclic [(oxindolo)pyrazino]thiazolidine, the chloro- and amino- derivatives of the (indolyl) thiazolidinone ring system were also prepared.

Results: The COX-2 inhibition activity of the synthesized compounds was investigated by studying their ability to inhibit the conversion of arachidonic acid to prostaglandin H2 (PGH2). Five of the tested candidates, substituted (oxonidolyl)thiazolidine derivatives (3a, 6f, 8b, 10 and 12) showed significant COX-2 inhibitory activity exhibiting IC50 values better than or close to the reference celecoxib. The anti-inflammatory activity was studied revealing that a number of compounds have shown good activities and compound 10 produced no significant mucosal injury.

Conclusion: Molecular docking study was implemented to interpret the variable inhibitory activity of the newly synthesized compounds against COX enzyme.The results suggested that some of these derivatives could be active COX inhibitors possessing a high preference for COX-2.

Why is it important?

Conclusion: Molecular docking study was implemented to interpret the variable inhibitory activity of the newly synthesized compounds against COX enzyme.The results suggested that some of these derivatives could be active COX inhibitors possessing a high preference for COX-2. Read more about the article here: https://bit.ly/3xm6sWo

Pregnancy complicated with ruptured membrane prior to labor’s onset

What is it about?

Prelabor rupture of membrane (PROM) refers to the breakage of fetal membranes before the onset of labor, resulting in the leakage of amniotic fluid. PROM affects approximately 3% and 8% of preterm and term pregnancies. Because of associated high maternal and perinatal mortality, correct and timely diagnosis together with effective management is highly recommended to prevent adverse fetal and maternal outcomes. The article reviews the possible pathophysiological mechanisms and novel therapeutic modalities in PROM.

Why is it important?

The correct and timely diagnosis of PROM is essential for efficacious management. Such an approach can reduce avoidable emergent health care visits and related costs in a clinical setting subjected to pregnancy with suspected PROM. Read more about the article here: https://bit.ly/35ZNitF

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