Biological assessment of the lower Boise River, October 1995 through January 1998, Ada and Canyon Counties, Idaho

Background: Diabetes mellitus is a chronic metabolic disorder, characterized by hyperglycemia over a prolonged period, disturbance of fat, protein and carbohydrate metabolism, resulting from defective insulin secretion, insulin action or both. Dipeptidyl peptidase-IV (DPP-IV) inhibitors are relatively a new class of oral hypoglycemic agents that reduces the deterioration of gut-derived endogenous incretin hormones that are secreted in response to food ingestion to stimulate the secretion of insulin from beta cells of pancreas. Objective: In this study, synthesis, characterization, and biological assessment of twelve novel phenanthridine sulfonamide derivatives 3a-3l as potential DPP-IV inhibitors was carried out. The target compounds were docked to study the molecular interactions and binding affinities against DPP-IV enzyme. Methods: The synthesized molecules were characterized using 1H-NMR, 13C-NMR, IR, and MS. Quantum-polarized ligand docking (QPLD) was also performed. Results: In vitro biological evaluation of compounds 3a-3l reveals comparable DPP-IV inhibitory activities ranging from 10%-46% at 100 µM concentration, where compound 3d harboring ortho-fluoro moiety exhibited the highest inhibitory activity. QPLD study shows that compounds 3a-3l accommodate DPP-IV binding site and form H-bonding with the R125, E205, E206, S209, F357, R358, K554, W629, S630, Y631, Y662, R669 and Y752 backbones. Conclusion: In conclusion, phenanthridine sulfonamides could serve as potential DPP-IV inhibitors that require further structural optimization in order to enhance their inhibitory activity.

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Evidences of Brain Plasticity and Motor Control Modulation after Hemodialysis Session by Helixone Membrane: BOLD-fMRI Study

CNS & Neurological Disorders - Drug Targets ◽

10.2174/1871527319666200902133343 ◽

2020 ◽

Vol 19 (6) ◽

pp. 466-477

Author(s):

Saïd Boujraf ◽

Rachida Belaïch ◽

Abdelkhalek Housni ◽

Badreeddine Alami ◽

Tariq Skalli ◽

...

Keyword(s):

Oxidative Stress ◽

Functional Activity ◽

Brain Plasticity ◽

Biological Assessment ◽

Bold Fmri ◽

Before And After ◽

Total Antioxidant ◽

Inflammatory State ◽

Functional Control ◽

The Impact

Objective: The aim of this paper is to demonstrate the impact of hemodialysis (HD) using synthetic Helixone membrane on brain functional control reorganization and plasticity in the cortical area generated while Oxidative Stress (OS) would be the main impacting agent. Methods: Indeed, 9 chronic HD patients underwent identical brain BOLD-fMRI assessment using the motor paradigm immediately before and after the same HD sessions. To assess the oxidative stress, the same patients underwent biological-assessment, including Malondialdehyde (MDA) and Total- Antioxidant-Activity (TAOA) reported in earlier papers. Results: BOLD-fMRI maps of motor areas obtained from HD-patients before and after HD sessions revealed a significant enhancement of activation volume of the studied motor cortex after HD reflecting brain plasticity. Results were correlated with OS assessed by the measurement of MDA and TAOA; this correlation was close to 1. Conclusion: Indeed, HD enhances the inflammatory state of brain tissues reflected by the increased OS. The functional brain reaction demonstrated a functional activity reorganization to overcome the inflammatory state and OS enhanced by HD process. This functional activity reorganization reveals brain plasticity induced by OS originated by HD.

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The Molecular Characterization and Biological Assessment of the Leaves Extracts of Loofah Reveal their Nutraceutical Potential

Recent Patents on Food Nutrition & Agriculturee ◽

10.2174/2212798411999201110211931 ◽

2020 ◽

Vol 11 ◽

Author(s):

Takoua Ben Hlel ◽

Feten Belhadj ◽

Fatih Gül ◽

Muhammed Altun ◽

Ayşe Şahin Yağlıoğlu ◽

...

Keyword(s):

Fatty Acids ◽

Phenolic Compounds ◽

Hela Cell ◽

Arid Region ◽

Biological Properties ◽

Biological Assessment ◽

Omega 3 ◽

Hela Cell Lines ◽

Semi Arid Region ◽

Semi Arid

Background:: Luffa cylindrica is a plant that is widely distributed in Africa and Asia and it can be grown in regions with tropical or subtropical climates. Few patents dealt with Loofah biological properties, including some functional foods formulated from its leaves. Objective:: This study aimed to structurally and functionally characterize the bioactive compounds of L. cylindrica leaves grown in two different environments. Methods:: The extracts of L. cylindrica leaves collected from two Tunisian locations: Essouasi (LE), a semi-arid region and Medenine (LM) an arid region, were investigated for their phenolic compounds and fatty acids using HPLC/TOF-MS and GCMS techniques respectively. Furthermore, the antioxidant capacity was evaluated with DPPH, Chelating effect, Hydroxyl radical and Superoxide anion scavenging activities while the anticancer activity against HeLa cell lines was assessed using xCELLigence real time cell analyzer and lactate dehydrogenase cytotoxicity assay. Results:: The antiproliferative capacity of both extracts was time and dose-dependent with LE presenting the lowest HeLa cell index (CI = 0.035 ± 0.018, 250 μg/ml). LE also showed the best cytotoxic capacity (56.49 ± 0.8%) and antioxidant potential (IC50 = 54.41 ± 1.12 μg/ml for DPPH and 12.12 ± 0.07 μg/ml for chelating effet). 14 phenolic compounds were detected in LE with ferulic acid being the major compound (5128.5 ± 4.09 μg Phenols/g) while LM had only 6 phenolics. GCMS analysis showed the presence of omega-3 fatty acids in LE. Conclusions:: Our findings suggest that L. cylindrica leaves, especially when collected from semi-arid regions, are promising for formulating nutraceuticals of interest.

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New Antimicrobials Based on the Adarotene Scaffold with Activity against Multi-Drug Resistant Staphylococcus aureus and Vancomycin-Resistant Enterococcus

Antibiotics ◽

10.3390/antibiotics10020126 ◽

2021 ◽

Vol 10 (2) ◽

pp. 126

Author(s):

Salvatore Princiotto ◽

Stefania Mazzini ◽

Loana Musso ◽

Fabio Arena ◽

Sabrina Dallavalle ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Anticancer Activity ◽

Bactericidal Effect ◽

Biological Assessment ◽

Drug Resistant ◽

Vancomycin Resistant Enterococcus ◽

Vancomycin Resistant ◽

Global Increase ◽

Common Infections

The global increase in infections by multi-drug resistant (MDR) pathogens is severely impacting our ability to successfully treat common infections. Herein, we report the antibacterial activity against S. aureus and E. faecalis (including some MDR strains) of a panel of adarotene-related synthetic retinoids. In many cases, these compounds showed, together with favorable MICs, a detectable bactericidal effect. We found that the pattern of substitution on adarotene could be modulated to obtain selectivity for antibacterial over the known anticancer activity of these compounds. NMR experiments allowed us to define the interaction between adarotene and a model of microorganism membrane. Biological assessment confirmed that the scaffold of adarotene is promising for further developments of non-toxic antimicrobials active on MDR strains.

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Bioactive potential of natural biomaterials: identification, retention and assessment of biological properties

Signal Transduction and Targeted Therapy ◽

10.1038/s41392-021-00512-8 ◽

2021 ◽

Vol 6 (1) ◽

Author(s):

Kieran Joyce ◽

Georgina Targa Fabra ◽

Yagmur Bozkurt ◽

Abhay Pandit

Keyword(s):

Tissue Engineering ◽

Therapeutic Potential ◽

Biological Properties ◽

Biological Assessment ◽

Cross Linking ◽

Natural Polymers ◽

Drug Delivery Device ◽

Biomedical Device ◽

Wide Range ◽

Bioactive Potential

AbstractBiomaterials have had an increasingly important role in recent decades, in biomedical device design and the development of tissue engineering solutions for cell delivery, drug delivery, device integration, tissue replacement, and more. There is an increasing trend in tissue engineering to use natural substrates, such as macromolecules native to plants and animals to improve the biocompatibility and biodegradability of delivered materials. At the same time, these materials have favourable mechanical properties and often considered to be biologically inert. More importantly, these macromolecules possess innate functions and properties due to their unique chemical composition and structure, which increase their bioactivity and therapeutic potential in a wide range of applications. While much focus has been on integrating these materials into these devices via a spectrum of cross-linking mechanisms, little attention is drawn to residual bioactivity that is often hampered during isolation, purification, and production processes. Herein, we discuss methods of initial material characterisation to determine innate bioactivity, means of material processing including cross-linking, decellularisation, and purification techniques and finally, a biological assessment of retained bioactivity of a final product. This review aims to address considerations for biomaterials design from natural polymers, through the optimisation and preservation of bioactive components that maximise the inherent bioactive potency of the substrate to promote tissue regeneration.

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Design, synthesis and biological assessment of novel CDK4 inhibitor with potent anticancer activity

Bioorganic Chemistry ◽

10.1016/j.bioorg.2021.104717 ◽

2021 ◽

Vol 109 ◽

pp. 104717

Author(s):

Yongtao Li ◽

Renle Du ◽

Yongwei Nie ◽

Tianqi Wang ◽

Yakun Ma ◽

...

Keyword(s):

Anticancer Activity ◽

Biological Assessment ◽

Design Synthesis ◽

Cdk4 Inhibitor

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