scholarly journals α-Mangostin Improves Glucose Uptake and Inhibits Adipocytes Differentiation in 3T3-L1 Cells via PPARγ, GLUT4, and Leptin Expressions

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Muhammad Taher ◽  
Mohamed Zaffar Ali Mohamed Amiroudine ◽  
Tengku Muhamad Faris Syafiq Tengku Zakaria ◽  
Deny Susanti ◽  
Solachuddin J. A. Ichwan ◽  
...  

Obesity has been often associated with the occurrence of cardiovascular diseases, type 2 diabetes, and cancer. The development of obesity is also accompanied by significant differentiation of preadipocytes into adipocytes. In this study, we investigated the activity ofα-mangostin, a major xanthone component isolated from the stem bark ofG. malaccensis, on glucose uptake and adipocyte differentiation of 3T3-L1 cells focusing on PPARγ, GLUT4, and leptin expressions.α-Mangostin was found to inhibit cytoplasmic lipid accumulation and adipogenic differentiation. Cells treated with 50 μM ofα-mangostin reduced intracellular fat accumulation dose-dependently up to 44.4% relative to MDI-treated cells. Analyses of 2-deoxy-D-[3H] glucose uptake activity showed thatα-mangostin significantly improved the glucose uptake (P<0.05) with highest activity found at 25 μM. In addition,α-mangostin increased the amount of free fatty acids (FFA) released. The highest glycerol release level was observed at 50 μM ofα-mangostin. qRT-PCR analysis showed reduced lipid accumulation via inhibition ofPPARγgene expression. Induction of glucose uptake and free fatty acid release byα-mangostin were accompanied by increasing mRNA expression ofGLUT4andleptin. These evidences propose thatα-mangostin might be possible candidate for the effective management of obesity in future.

2014 ◽  
Vol 223 (2) ◽  
pp. 119-132 ◽  
Author(s):  
M van de Vyver ◽  
E Andrag ◽  
I L Cockburn ◽  
W F Ferris

Chronic administration of the insulin-sensitising drugs, thiazolidinediones (TZDs), results in low bone mineral density and ‘fatty bones’. This is thought to be due, at least in part, to aberrant differentiation of progenitor mesenchymal stem cells (MSCs) away from osteogenesis towards adipogenesis. This study directly compared the effects of rosiglitazone, pioglitazone, and netoglitazone treatment on osteogenesis and adipogenesis in MSCs derived from subcutaneous (SC) or visceral (PV) white adipose tissue. MSCs were isolated from adipose tissue depots of male Wistar rats and characterised using flow cytometry. The effects of TZD treatment on osteogenic and adipogenic differentiation were assessed histologically (day 14) and by quantitative PCR analysis (Pparγ2(Pparg2),Ap2(Fabp4), Adipsin(Adps),Msx2, Collagen I(Col1a1), andAlp) on days 0, 7, and 10. Uniquely, lipid droplet formation and mineralisation were found to occur concurrently in response to TZD treatment during osteogenesis. Compared with SC MSCs, PV MSCs were more prone to lipid accumulation under controlled osteogenic and adipogenic differentiation conditions. This study demonstrated that the extent of lipid accumulation is dependent on the nature of thePparligand and that SC and PV MSCs respond differently toin vitroTZD treatment, suggesting that metabolic status can contribute to the adverse effects associated with TZD treatment.


Metabolism ◽  
1992 ◽  
Vol 41 (10) ◽  
pp. 1146-1149 ◽  
Author(s):  
Brunella Capaldo ◽  
Raffaele Napoli ◽  
Lucrezia Di Marino ◽  
Luigi Saccà

2018 ◽  
Vol 104 (3) ◽  
pp. 647-657 ◽  
Author(s):  
Johan Onslev ◽  
Jørgen Jensen ◽  
Jens Bangsbo ◽  
Jørgen Wojtaszewski ◽  
Morten Hostrup

Nutrients ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 2788 ◽  
Author(s):  
Federica Geddo ◽  
Rosaria Scandiffio ◽  
Susanna Antoniotti ◽  
Erika Cottone ◽  
Giulia Querio ◽  
...  

Trans-β-caryophyllene (BCP) is a natural sesquiterpene hydrocarbon with several important pharmacological activities, including antioxidant, anti-inflammatory, anticancer, and cardioprotective functions. These properties are mainly due to its selective interaction with the peripherally expressed cannabinoid receptor 2. In addition, BCP activates peroxisome proliferated activator receptors α and γ and inhibits the Toll-like receptor signaling pathway. Given the growing scientific interest in BCP, the aim of our study was to investigate the metabolic effects of a black pepper extract (PipeNig®-FL), containing a high standardized content of BCP. In particular our interest was focused on its potential activity on lipid accumulation and glucose uptake. The extract PipeNig®-FL was chemically characterized by gas chromatography–mass spectrometry (GC–MS) and gas chromatography with flame-ionization detection (GC–FID), confirming a high content (814 mg/g) of BCP. Experiments were performed on 3T3-L1 preadipocytes and on C2C12 myotubes. Lipid content following 3T3-L1 adipogenic differentiation was quantified with AdipoRed fluorescence staining. Glucose uptake and GLUT4 membrane translocation were studied in C2C12 myotubes with the fluorescent glucose analog 2-NBDG and by immunofluorescence analysis. Here we show that PipeNig®-FL reduces 3T3-L1 adipocyte differentiation and lipid accumulation. Moreover, acute exposure of C2C12 myotubes to PipeNig®-FL improves glucose uptake activity and GLUT4 migration. Taken together, these results reveal interesting and novel properties of BCP, suggesting potential applications in the prevention of lipid accumulation and in the improvement of glucose uptake.


Author(s):  
Ninon G.E.R. Etsassala ◽  
Kadidiatou O. Ndjoubi ◽  
Thilly J. Mbira ◽  
Brendon Pearce ◽  
Keenau Pearce ◽  
...  

The prevalence of diabetes mellitus (DM), considered one of the most common metabolic disorders, has dramatically increased and resulted in higher rate of morbidity and mortality around the world, in the past decade. It is well known that insulin resistance in target tissues and a deficiency in insulin secretion from pancreatic &beta;-cells are the main characteristic of type 2 diabetes. The aim of this study was the bio-evaluation of compounds isolated from three selected plant species; namely, Salvia africana-lutea, Leonotis ocymifolia and Plectranthus madagascariensis, for their glucose uptake ability. Methanolic extracts were produced from the arterial part of each plant. Compounds were identified using different spectroscopic techniques. The glucose uptake ability of each compound was then evaluated in mammalian cells using 2-deoxyglucose-6-phosphate. The cytotoxicity of each compound was established via the MTT assay. Chromatographic purification of the three plant species yielded fifteen pure terpenoids. Compounds 1 (p = 0.0031), 8 (p = 0.0053), and 6 (p = 0.0086), showed a marked increase in glucose uptake, with p values of p=0.0031, p=0.0053 and p=0.0086, respectively. Additionally, 1, 4 and 6 exhibited cytotoxicity toward mammalian tissue with a decrease in cell viability of ~70%, ~68% and ~67%, respectively. The results suggested that several compounds demonstrated a marked increase in glucose uptake while two of the compounds exhibited signs of cytotoxicity. It may, therefore, be suggested that these compounds be considered as potential candidates for novel plant-derived alternative therapies in the treatment of type 2 diabetes.


Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4129
Author(s):  
Ninon G. E. R. Etsassala ◽  
Kadidiatou O. Ndjoubi ◽  
Thilly J. Mbira ◽  
Brendon Pearce ◽  
Keenau Pearce ◽  
...  

The prevalence of diabetes mellitus (DM), considered one of the most common metabolic disorders, has dramatically increased and resulted in higher rates of morbidity and mortality around the world in the past decade. It is well known that insulin resistance in target tissues and a deficiency in insulin secretion from pancreatic β-cells are the main characteristics of type 2 diabetes. The aim of this study was the bio-evaluation of compounds isolated from three selected plant species: namely, Salvia africana-lutea, Leonotis ocymifolia, and Plectranthus madagascariensis, for their glucose-uptake ability. Methanolic extracts were produced from the aerial parts of each plant. Compounds were identified using different spectroscopic techniques. The glucose-uptake ability of each compound was then evaluated in mammalian cells using 2-deoxyglucose-6-phosphate. The cytotoxicity of each compound was established via the MTT assay. Chromatographic purification of the three plant species yielded sixteen pure terpenoids. Compounds 1 (p = 0.0031), 8 (p = 0.0053), and 6 (p = 0.0086) showed a marked increase in glucose uptake, respectively. Additionally, 1, 4, and 6 exhibited cytotoxicity toward mammalian tissue with a decrease in cell viability of ~70%, ~68%, and ~67%, respectively. The results suggested that several compounds demonstrated a marked increase in glucose uptake, while two of the compounds exhibited signs of cytotoxicity. It may, therefore, be suggested that these compounds be considered as potential candidates for novel plant-derived alternative therapies in the treatment of type 2 diabetes.


2020 ◽  
Vol 17 (7) ◽  
pp. 840-849
Author(s):  
Mahendra Gowdru Srinivas ◽  
Prabitha Prabhakaran ◽  
Subhankar Probhat Mandal ◽  
Yuvaraj Sivamani ◽  
Pranesh Guddur ◽  
...  

Background: Thiazolidinediones and its bioisostere, namely, rhodanines have become ubiquitous class of heterocyclic compounds in drug design and discovery. In the present study, as part of molecular design, a series of novel glitazones that are feasible to synthesize in our laboratory were subjected to docking studies against PPAR-γ receptor for their selection. Methods and Results: As part of the synthesis of selected twelve glitazones, the core moiety, pyridine incorporated rhodanine was synthesized via dithiocarbamate. Later, a series of glitazones were prepared via Knovenageal condensation. In silico docking studies were performed against PPARγ protein (2PRG). The titled compounds were investigated for their cytotoxic activity against 3T3-L1 cells to identify the cytotoxicity window of the glitazones. Further, within the cytotoxicity window, glitazones were screened for glucose uptake activity against L6 cells to assess their possible antidiabetic activity. Conclusion: Based on the glucose uptake results, structure activity relationships are drawn for the title compounds.


2020 ◽  
Vol 16 (2) ◽  
pp. 137-142
Author(s):  
Ali Alshahrani

Background: Smoking is an established predictor of type 2 diabetes. However, the link between smoking cessation and diabetes progression remains a subject of scholarly investigation. Objective: The objective of this systematic review is to establish the link between smoking cessation and diabetes. Data Sources: The study utilized conference abstracts and peer-reviewed journals that reported randomized controlled trials smoking cessation interventions for diabetes patients. Results: Results from the review were inconclusive on the link between smoking cessation and diabetes. On one hand, several researchers have confirmed a positive correlation between smoking cessation and decreased risk of diabetes. On the other hand, some researchers have demonstrated that immediate withdrawal of nicotine resulted in increased risk of diabetes; however, this risk reduces with time. Conclusion: The result of this review did not estblish a clear relationship between smoking cessation and diabates. Limitations: Compared to other studies examining the implication of smoking on chronic diseases, this study identified a very small number of trials evaluating the effect of smoking cessation on diabetes. The small number of studies implies that the results may not be suitable for generalization. Implication: Results from the review can help in the development of a tailored intervention for effective management of diabetes in smoking patients.


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