Effect of natural products on commercial oral antidiabetic drugs in enhancing 2-deoxyglucose uptake by 3T3-L1 adipocytes
01 Jun 2011-Therapeutic Advances in Endocrinology and Metabolism (SAGE Publications)-Vol. 2, Iss: 3, pp 103-114
TL;DR: The current study suggests that berberine and arecoline could allow dosage reduction of OHDs, which could also lead to a reduction in the toxicity and side effects caused by O HDs.
Abstract: Objective:
The management of diabetes with insulin and synthetic oral hypoglycemic drugs (OHDs) can produce serious side effects and in addition fails to prevent diabetes-related complications in many patients. A new diabetes management strategy is needed that is more effective and has fewer side effects.
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TL;DR: Ferulic acid interacts synergistically with both the drugs and might be a good supplement with the OHDs to manage diabetic complications as well as reduces the use of the later.
102 citations
TL;DR: The observed synergy and mechanism of action between phytochemicals and synthetic drugs in effectively combating differs significantly than that of the drugs alone; hence isolating a single component may lose its importance thereby simplifying the task of pharma industries.
78 citations
TL;DR: The effects of phytochemicals and their action on insulin signaling pathways accelerating GLUT4 translocation based on the current literature will be summarized.
Abstract: Diabetes is associated with obesity, generally accompanied by a chronic state of oxidative stress and redox imbalances which are implicated in the progression of micro- and macro-complications like heart disease, stroke, dementia, cancer, kidney failure and blindness. All these complications rise primarily due to consistent high blood glucose levels. Insulin and glucagon help to maintain the homeostasis of glucose and lipids through signaling cascades. Pancreatic hormones stimulate translocation of the glucose transporter isoform 4 (GLUT4) from an intracellular location to the cell surface and facilitate the rapid insulin-dependent storage of glucose in muscle and fat cells. Malfunction in glucose uptake mechanisms, primarily contribute to insulin resistance in type 2 diabetes. Plant secondary metabolites, commonly known as phytochemicals, are reported to have great benefits in the management of type 2 diabetes. The role of phytochemicals and their action on insulin signaling pathways through stimulation of GLUT4 translocation is crucial to understand the pathogenesis of this disease in the management process. This review will summarize the effects of phytochemicals and their action on insulin signaling pathways accelerating GLUT4 translocation based on the current literature.
58 citations
Cites background from "Effect of natural products on comme..."
...Berberine and vanillic acid significantly improve GLUT4 translocation via AMPK-dependent pathway, whereas arecoline does the same via the PPAR-γ pathway [33] Besides, the fungal metabolite, demethylasterrriquinone-B, could directly stimulate IRTK, AKT and ERK pathways, apply glucotropic effects of insulin with no mitogenic effect exertion [79,80]....
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...Berberine and vanillic acid Berberis aristata and numerous plants Improves the translocation of GLUT4 via AMPK-dependent pathway [33]...
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TL;DR: The article reviews the mechanisms of action of available anti-diabetic drugs with in-depth mechanistic analysis of each therapy and identifies multiple targets from different signaling pathways that may be manipulated simultaneously to treat or manage T2DM effectively.
54 citations
TL;DR: It is reported that polyphenols and phenolic acids inhibit adipogenesis in 3T3-L1 with different intensity depending on the family and the stage of differentiation, which might suggest a crucial role for these amino acids modulating the activity of the receptor.
Abstract: Phenolic compounds might modulate adiposity. Here, we report our observation that polyphenols and phenolic acids inhibit adipogenesis in 3T3-L1 with different intensity depending on the family and the stage of differentiation. While quercetin and resveratrol inhibited lipid accumulation along the whole process of differentiation, apigenin and myricetin were active during the early and latest stages, but not intermediate, contrary to hesperidin. The activity of phenolic acids was limited to the early stages of the differentiation process, except p-coumaric and ellagic acids. This anti-adipogenic effect was accompanied by down-regulation of Scd1 and Lpl. Molecular docking analysis revealed that the inhibitory activity of these phenolic compounds over the early stages of adipogenesis exhibits a significant correlation (r = 0.7034; p = 0.005) with their binding affinity to the ligand-binding domain of PPARγ. Results show that polyphenols and phenolic acids would interact with specific residues of the receptor, which could determine their potential anti-adipogenic activity during the early stages of the differentiation. Residues Phe264, His266, Ile281, Cys285 and Met348 are the most frequently involved in these interactions, which might suggest a crucial role for these amino acids modulating the activity of the receptor. These data contribute to elucidate the possible mechanisms of phenolic compounds in the control of adipogenesis.
52 citations
References
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TL;DR: A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation and is used to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis.
50,114 citations
"Effect of natural products on comme..." refers methods in this paper
...The MTT assay (method supplied in the online Supplementary Material), which measures the activity of the mitochondrial reductase enzyme, is an estimate of the number of viable cells [Mosmann, 1983]....
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TL;DR: The method can be applied to most laboratory animals in the conscious state and is based on the use of 2‐deoxy‐D‐[14C]glucose as a tracer for the exchange of glucose between plasma and brain and its phosphorylation by hexokinase in the tissues.
Abstract: — A method has been developed for the simultaneous measurement of the rates of glucose consumption in the various structural and functional components of the brain in vivo. The method can be applied to most laboratory animals in the conscious state. It is based on the use of 2-deoxy-D-[14C]glucose ([14C]DG) as a tracer for the exchange of glucose between plasma and brain and its phosphorylation by hexokinase in the tissues. [14C]DG is used because the label in its product, [14C]deoxyglucose-6-phosphate, is essentially trapped in the tissue over the time course of the measurement. A model has been designed based on the assumptions of a steady state for glucose consumption, a first order equilibration of the free [14C]DG pool in the tissue with the plasma level, and relative rates of phosphorylation of [14C]DG and glucose determined by their relative concentrations in the precursor pools and their respective kinetic constants for the hexokinase reaction. An operational equation based on this model has been derived in terms of determinable variables. A pulse of [14C]DG is administered intravenously and the arterial plasma [14C]DG and glucose concentrations monitored for a preset time between 30 and 45min. At the prescribed time, the head is removed and frozen in liquid N2-chilled Freon XII, and the brain sectioned for autoradiography. Local tissue concentrations of [14C]DG are determined by quantitative autoradiography. Local cerebral glucose consumption is calculated by the equation on the basis of these measured values.
The method has been applied to normal albino rats in the conscious state and under thiopental anesthesia. The results demonstrate that the local rates of glucose consumption in the brain fall into two distinct distributions, one for gray matter and the other for white matter. In the conscious rat the values in the gray matter vary widely from structure to structure (54-197 μmol/100 g/min) with the highest values in structures related to auditory function, e.g. medial geniculate body, superior olive, inferior colliculus, and auditory cortex. The values in white matter are more uniform (i.e. 33–40 μmo1/100 g/min) at levels approximately one-fourth to one-half those of gray matter. Heterogeneous rates of glucose consumption are frequently seen within specific structures, often revealing a pattern of cytoarchitecture. Thiopental anesthesia markedly depresses the rates of glucose utilization throughout the brain, particularly in gray matter, and metabolic rate throughout gray matter becomes more uniform at a lower level.
5,988 citations
"Effect of natural products on comme..." refers background in this paper
...Assaying the uptake of the latter is more convenient than assaying with the former because 2DG is converted into a stable and impermeable derivative, 2DG6P, through phosphorylation by hexokinase or glucokinase [Sokoloff et al. 1977]....
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TL;DR: Patients should caution patients against mixing herbs and pharmaceutical drugs, as many reports of herb-drug interactions are sketchy and lack laboratory analysis of suspect preparations.
1,246 citations
"Effect of natural products on comme..." refers background in this paper
...Many phytochemicals and pharmaceuticals are therapeutic at one dose and toxic at another and synergistic interactions can complicate dosing during long-term medication but experimental data on herb drug interactions are limited [Fugh-Berman, 2000]....
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TL;DR: This review describes many examples of how modern molecular-biological methods can enable us to understand the various synergistic mechanisms underlying these effects of herbal drug combinations.
1,004 citations
TL;DR: Positive and negative aspects of interactions are discussed together with the methods used to identify and measure synergy, and the evidence is divided into experimental, in vitro instances, as well as clinical examples where available.
806 citations
"Effect of natural products on comme..." refers background in this paper
...It is generally believed that the use of herbs with pharmaceuticals enhances the effect of the latter and reduces their adverse effects [Williamson, 2001]....
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