A5091050812- Natural Antidiabetic Agents Studies
- Synthesis of Organic Compounds
- Diet, Metabolism, and Disease
- Phytochemicals and Antioxidant Activities
- Synthesis and biological activity
- Enzyme Catalysis and Immobilization
- Pharmacology and Obesity Treatment
- Biological Activity of Diterpenoids and Biflavonoids
- Inflammatory mediators and NSAID effects
- Metabolism, Diabetes, and Cancer
- Protein Tyrosine Phosphatases
- Enzyme Production and Characterization
- Peptidase Inhibition and Analysis
- Computational Drug Discovery Methods
- Eicosanoids and Hypertension Pharmacology
- Flavonoids in Medical Research
- Cancer Cells and Metastasis
- Carbohydrate Chemistry and Synthesis
- Pharmacological Effects of Natural Compounds
- Advanced Glycation End Products research
- Diabetes Treatment and Management
- Adipokines, Inflammation, and Metabolic Diseases
- Lipid metabolism and biosynthesis
- Cell death mechanisms and regulation
- Multicomponent Synthesis of Heterocycles
Universidade do Porto
2016-2025
Rede de Química e Tecnologia
2016-2025
α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used management of type 2 diabetes mellitus. As flavonoids promising modulators this enzyme's activity, a panel 44 flavonoids, organised five groups, was screened for their inhibitory activity α-glucosidase, based on vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied...
α-Amylase has been considered an important therapeutic target for the management of type 2 diabetes mellitus (T2DM), decreasing postprandial hyperglycaemia (PPHG). In present work, a panel 40 structurally related flavonoids was tested, concerning their ability to inhibit α-amylase activity, using microanalysis screening system, inhibitory kinetic analysis and molecular docking calculations. From obtained results, it possible observe that flavone with -Cl ion at 3-position C-ring, -OH group...
Abstract Opuntia ficus-indica fruits have been widely used due to their nutritional composition and beneficial effects on health, particularly against chronic diseases such as diabetes, obesity, cardiovascular cancer, among others. In recent years, prickly pear peel pulp extracts characterised, a high number of bioactive compounds identified. This study aimed analyse the triglyceride-lowering effect obtained from three varieties (Pelota, Sanguinos, Colorada) in 3T3-L1 maturing mature...
Xanthones are oxygen-containing heterocyclic compounds that exhibit a wide range of biological and pharmacological properties. Some natural synthetic derivatives have been identified for their antidiabetic profile, mainly as α-glucosidase inhibitors. However, studies concerning the inhibition both carbohydrate-hydrolyzing enzymes α-amylase scarce. Thus, in order to identify some these dual-target agents, series new xanthones were evaluated together with commercial parents mangiferin (4),...
Osteosarcoma (OS) is a common childhood sarcoma, and its treatment hindered by adverse effects, chemoresistance, recurrence. Interleukin (IL)-6 production tumors plays significant role in inflammation, carcinogenesis, metastasis. This study aimed to investigate the antiproliferative potential of luteolin derivatives OS evaluate interleukin production. MG-63, Saos-2, HOS, 143B human cell lines were incubated with eight containing hydroxy, chlorine, or alkyl substitutions. The viability growth...
Background/Objectives: Obesity has reached pandemic proportions, with predictions suggesting that, by 2030, over 1.5 billion people will be affected. Pancreatic lipase (PL), the enzyme primarily responsible for absorption of dietary lipids, presents a potential target obesity management. However, while porcine pancreatic (PPL) is commonly used as source screening inhibitors, its effect on human (HPL) rarely reported. This work aimed to screen inhibitory effects library flavonoids different...
Abstract This study aimed to identify new compounds capable of decreasing pancreatic lipase (PL) catalytic activity. A panel structurally related chalcones with hydroxy and chloro substituents was chosen, their inhibitory effects on the targeted enzyme were assessed. work also optimized conditions for UV/Vis spectrophotometric fluorimetric microanalysis systems and, whenever possible, a structure–activity relationship analysis performed. The obtained results showed effectiveness both...
Abstract α-amylase and α-glucosidase are key enzymes implicated in carbohydrate digestion their inhibition has been suggested as a powerful approach for regulating blood glucose levels. The present work describes the first time by group of twelve hydroxylated 2-styrylchromones (2-SC). Our findings revealed that 2-SC display strong systematic rather than activity. number position hydroxy groups chromone moiety further modulate inhibitory profile studied compounds, derivatives bearing one...
Dipeptidyl peptidase-4 (DPP-4) inhibitors present a unique approach for the management of type 2 diabetes (T2D). In study, inhibition DPP-4 was evaluated large panel flavonoids, important components human diet, using in vitro and ex vivo models. The activity isolated enzyme assayed vitro. Subsequently, most active flavonoids were tested whole blood plasma. this contrary to fluorometric tests, did not show inhibitory against DPP-4. Due discrepancy results between approaches, plasma protein...
Liver fructose 1,6-bisphosphatase (FBPase) is a recognized regulatory enzyme of the gluconeogenesis pathway, which has emerged as valid target to control gluconeogenesis-mediated overproduction glucose. As such, management diabetes with FBPase inhibitors represents potential alternative for currently used antidiabetic agents. In this study, inhibition panel 55 structurally related flavonoids was tested, through microanalysis screening system. Then, subset seven active and their close...
Enzymes, enzymatic kinetics, and enzyme inhibition are topics covered in undergraduate biochemistry textbooks, having perceptible relevance to everyday life. The experimental use of enzymes involved basic physiologic processes may be utmost pedagogic interest because they bring evidence on how a significant number drugs used control illnesses. Salivary pancreatic α-amylases essential digestive responsible for the partial hydrolysis starch, primary source calories human diet. As structures...
Type 2 diabetes (T2D) is the most common form of diabetes, and number people with this metabolic disease steadily increasing worldwide. Among available antidiabetic agents, α-glucosidase inhibitors are effective at reducing postprandial hyperglycaemia (PPHG), one main characteristics T2D. However, studies that have been performed used more readily rat intestinal preparations or yeast as enzyme source, which despite being useful cost effective, a questionable physiological value. The present...