(-)-Epigallocatechin-3-gallate (EGCG), a major flavonoid in green tea has multiple health benefits including chemoprevention, anti-inflammatory, anti-diabetic, and anti-obesity effects. In connection with these effects, EGCG can be a candidate to help the treatment of metabolic diseases. Metformin is a widely used anti-diabetic drug regulating cellular energy homeostasis via AMP-activated protein kinase (AMPK) activation. Therefore, the combination of metformin with EGCG may have additive or synergistic effects on treatment of type 2 diabetes. Nevertheless, there is no report for the pharmacokinetic and/or pharmacodynamic interaction of EGCG with metformin. Here, we evaluated the pharmacokinetic and pharmacodynamic interaction between metformin and EGCG in rats. Pharmacokinetics parameters of metformin were measured after oral administration of metformin in rats pre-treated with EGCG (10 mg/kg) or saline for 7 days. The results showed that there is no significant difference in pharmacokinetic parameters between saline control and EGCG-treated group. In addition, the hepatic AMPK activation by metformin in EGCG-treated rats was also similar to the control. The lack of additive effects of EGCG on AMPK activation or intracellular uptake of metformin was also evaluated in cells in the presence or absence of EGCG. Treatment of HepG2 cells with EGCG inhibited the metformin-induced AMPK activation. Combined results suggested that EGCG has no effect on the pharmacokinetics of metformin but may contribute to metformin action.
This study investigates the antioxidant and anti-adipogeneic effects of fermented Rhus verniciflua., evaluating the total phenol, total flavonoids contents and antioxidant activity of the fermented Rhus verniciflua as well as assessing the lipid accumulation during adipogenesis of 3T3-L1 cells. Our results demonstrate that the total phenolic and flavonoids contents of fermented Rhus verniciflua were $29.2{\pm}0.12$ GAE mg/g and $20.4{\pm}1.52$ RE mg/g, respectively. The antioxidative activities of fermented Rhus verniciflua were significantly increased in a dose dependent manner on DPPH (1,1-Diphenyl-2-picrylhydrazyl) radical scavenging, ABTS(2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) radical scavenging, FRAP(ferric reducing antioxidant power)activity, reducing power. In addition, the fermented Rhus verniciflua did not show any cytotoxicity up to 300 ug/mL. However, the anti-adipogenic effect of fermented Rhus verniciflua extract was barely detectable.
Purpose: Neuroinflammation is mediated by activation of microglia implicated in the pathogenesis of neurodegenerative disorders such as Alzheimer's disease and Parkinson's disease. Inhibition of neuroinflammation may be an effective solution to treat these brain disorders. Petalonia binghamiae is known as a traditional food, based on multiple biological activities such as anti-oxidant and anti-obesity. In present study, the anti-neuroinflammatory potential of Petalonia binghamiae was investigated in LPS-stimulated BV2 microglial cells. Methods: Cell viability was measured by MTT assay. Production of nitric oxide (NO) was examined using Griess reagent. Expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) was detected by Western blot analysis. Activation of nuclear factor ${\kappa}B$ ($NF-{\kappa}B$) signaling was examined by nuclear translocation of $NF-{\kappa}B$ p65 subunit and phosphorylation of $I{\kappa}B$. Results: Extract of Petalonia binghamiae significantly inhibited LPS-stimulated NO production and iNOS/COX-2 protein expression in a dose-dependent manner without cytotoxicity. Pretreatment with Petalonia binghamiae suppressed LPS-induced $NF-{\kappa}B$ p65 nuclear translocation and phosphorylation of $I{\kappa}B$. Co-treatment with Petalonia binghamiae and pyrrolidine duthiocarbamate (PDTC), an $NF-{\kappa}B$ inhibitor, reduced LPS-stimulated NO release compared to that in PB-treated or PDTC-treated cells. Conclusion: The present results indicate that extract of Petalonia binghamiae exerts anti-neuroinflammation activities, partly through inhibition of $NF-{\kappa}B$ signaling. These findings suggest that Petalonia binghamiae might have therapeutic potential in relation to neuroinflammation and neurodegenerative diseases.
This study aimed to evaluate the anti-adipogenic and anti-inflammation effects of extract from Maclura tricuspidata twig fermented with Ganoderma lucidum mycelium (EMFG) in 3T3-L1 preadipocytes. 3T3-L1 adipocytes were treated with 100, 200, 300 ㎍/mL of EMFG. The result showed that EMFG dose-dependently inhibited the accumulation of intracellular lipid content in differentiated 3T3-L1 adipocytes and enhanced increase of adiponectin release and inhibition of leptin release. EMFG treatment reduced expression of adipogenic transcriptional factor such as peroxisome proliferator-activated receptor γ (PPARγ), CCAAT-enhancer-binding protein α (C/EBPα). EMFG also decreased production of lipopolysaccharide (LPS)-induced inflammatory cytokine [tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and monocyte chemoattractant protein-1 (MCP-1)] and the protein expression of cyclooxygenase-2 (COX-2) and inducible NOS (iNOS) in differentiated 3T3-L1 adipocytes. The study demonstrated that EMFG inhibited adipogenesis and inflammation in a dose-dependent manner. These findings suggest that EMFG may have potential as an anti-obesity and anti-metabolic disease agent that works by inhibiting adipogenesis and inflammation.
Journal of the Korean Society of Food Science and Nutrition
/
v.38
no.3
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pp.309-318
/
2009
This study was conducted to investigate the cholesterol lowering and anti-obesity effects of an ethanol extract of broccoli sprouts (BS) in rats fed high fat diet. Male Sprague-Dawley rats weighing $150{\sim}155g$, were divided into 6 groups; a normal diet group (ND), a high fat diet group (HFD), a normal diet and BS with 200 mg/kg treated group (ND-BSL), a normal diet and BS with 400 mg/kg treated group (ND-BSH), a high fat diet and BS with 200 mg/kg treated group (HFD-BSL), and a high fat diet and BS with 400 mg/kg treated group (HFD-BSH). The body weight gain and mesenteric adipose tissue weight were increased by high fat diet, but gradually decreased to the corresponding level of ND group after administration of BS extract. The liver and epididymal adipose tissue weights of HFD group were the highest among the six groups, although the difference was not significant. Food intake was lower in high fat diet groups compared with normal diet groups. The serum ALT and AST activities that were elevated by the high fat diet were significantly decreased after BS administration. Levels of serum total cholesterol, LDL-cholesterol, triglyceride and the atherogenic index tended to be decrease in the BS administered groups compared with HFD group. However, HDL-cholesterol level in serum decreased in HFD group and markedly increased in BS administered groups. There were no differences in the contents of serum triglyceride, LDL-cholesterol and HDL-cholesterol between normal diet groups. Levels of total cholesterol and triglyceride in liver and adipose tissues were also lower in BS administrated groups than in HFD group. The activities of heparin-releasable lipoprotein lipase (HR-LPL) and total-extractable LPL (TE-LPL) in adipose tissue were increased in HFD group compared with the BS administered groups, but those of the ND-BSL group and ND-BSH group were similar to ND group. These results suggest that BS ethanol extract may exert cholesterol-lowering effect and potentially reduce lipid storage.
Journal of the Korean Society of Food Science and Nutrition
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v.43
no.6
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pp.814-821
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2014
As a natural plant ingredients, glasswort (Salicornia herbacea L.) contains various physiological activities, mainly anti-oxidative and anti-diabetic activities. However, only a few studies have been carried out on its anti-adipogenic effect. This study investigated the anti-obesity effects of Salicornia herbacea L. on 3T3-L1 adipocytes. As adipogenesis of preadipocytes to adipocytes involves proliferation and differentiation of cells, we treated three concentrations (125, 250, and $500{\mu}g/mL$) of Salicornia herbacea L. water extracts (SLW) in both pre-processing and post-processing stages. When 3T3-L1 adipocytes were differentiated and dyed with Oil Red O, adipocytes size and the value of relative Oil Red O staining were reduced by all concentrations of SLW in post-processing stage. Following adipogenic differentiation, the concentration of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) in the cell supernatant significantly increased upon treatment with $125{\mu}g/mL$ of SLW and further rose at concentrations of 250 and $500{\mu}g/mL$ during post-processing stage. There was no significant difference in glycerol production upon SLW treatment. Leptin production significantly decreased at all SLW concentrations during post-processing stage, whereas peroxisome proliferator activated receptor-${\gamma}$ (PPAR-${\gamma}$) and adiponectin secretions were significantly enhanced. Overall results showed that SLW might have an anti-adipogenic effect via enhancement of TNF-${\alpha}$ production, which causes dedifferentiation and inhibits lipid accumulations in adipocyte. Furthermore, SLW might prevent diabetes and cardiovascular disease, as it reduces leptin secretion and enhances production of both PPAR-${\gamma}$ and adiponectin. However, further research is needed to elucidate the exact mechanism and bioactive compounds of glasswort.
Purpose: Aster glehnii (AG) and Aster yomena (AY) are medicinal plants that belong to the family Compositea and grow widely in Korea. Plants in the genus Aster have been used to treat snakebite wounds or bruises in oriental medicine. This study compared the effects of anti-oxidants and anti-adipocyte differentiation according to the species (the aerial parts of AG and AY). Methods: AG and AY were extracted using 70% ethanol (-E) and water (-W) at room temperature. The anti-oxidant activities were measured by total phenol contents (TPC), total flavonoid contents (TFC), DPPH and $ABTS^+$ assay. In addition, correlation analysis was performed for the anti-oxidant compounds and effect. The level of anti-adipocyte differentiation was assessed using an oil red O assay on pre-adipocytes. Results: AG-W showed higher TPC ($6.92{\mu}g/mL$) and AG-E presented higher TFC ($8.22{\mu}g/mL$) than the other extracts. Furthermore, AG-E exhibited higher radical scavenging activity in the DPPH and $ABTS^+$ assay ($IC_{50}$: 104.88 and $30.06{\mu}g/mL$). In the cytotoxicity assay, AG and AY extracts at concentrations less than $100{\mu}g/mL$ were non toxic. AG-W reduced the lipid accumulation of 3T3-L1 cells significantly after differentiation (70.49%) compared to the other extracts. Conclusion: These results show that the water extract of AG has anti-oxidant effects and reduces the differentiation of 3T3-L1 cells. Therefore, AG has utility as a functional food material for its anti-oxidant activities and ability to prevent lipid accumulation.
Journal of the Korean Applied Science and Technology
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v.35
no.3
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pp.654-666
/
2018
This study was determined the effects of dietary omega-6 and 3 fatty acid ratios (n-6/n-3, 0, 4:1, 15:1, 30:1) on lipid metabolism in obese model animal rats. Blood triacylglycerol, total cholesterol, LDL-C, glucose, ALT, AST, insulin, and leptin concentrations in n-6/n-3 group were decreased by 22.21, 20.60, 52.96, 15.71, 11.97, 9.13, 37.57, 45.98%, respectively, while HDL-C and phospholipid concentrations were increased by 28.38, 80.39% respectively, compared with control group, as especially in 4:1 group showed the greatest effect. SREPB-$1{\alpha}$ and SREPB-2 mRNA in liver tissues were down-regulated in n-6/n-3 group, but LPL-mRNA of PPARs in adipose tissue was up-regulated compared with control group. The adipocyte size in liver tissues was decreased in the order of n-6/n-3 ratio of 30:1, control, 15:1 groups, and the adipocyte size in adipose tissues was decreased in the order of n-6/n-3 ratio of control, 30:1, 15:1, 4:1 groups.
Park Jung-Mi;Kim Ho-Jun;Kim Jin-Ah;Kim Su-Jin;Ko Byeong-Pyo
The Journal of Korean Medicine
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v.26
no.3
s.63
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pp.249-262
/
2005
Backgrounds : As obesity prevails as an epidemic. diet programs including low-calorie diets are developed continuously. It is generally believed that a low-calorie diet is commonly followed by resting metabolic rate decrease and ultimate weight regain. Ephedra and Evodia are known to have sympathomimetic and anti-obesity effect. Objectives : This study was a prospective, double-blinded, randomized md placebo-controlled clinical trial to evaluate the effects of Ephedra sinica and Evodia rutaecarpa on resting metabolic rate (RMR), weight, body composition, and short-term safety in obese women on low-calorie diet. Methods : 125 otherwise healthy obese women (body mass Index ${\geq}\;25kg/m^2$) were recruited and randomly assigned to three groups: Ephedra group (n=41), Evodia group (n =45), and placebo group (n=39). Subjects were administered Ephedra extract in capsules (pseudo-ephedrine 31.52mg) or Evodia extract in capsules (evodiamine 6.75mg, rutaecarpine 0.66mg) or placebo capsules as well as participating in a low-calorie diet for 8 weeks, Resting metabolic rate and body composition were measured at baseline,4 and 8 weeks. Basic serum exams were performed to evaluate the short-term safety of the herbs and changes of lipid variables. Results : All three groups showed significant BMI decreases probably due to low-calorie diet. Among them, the Ephedra group manifested most prominent BMI-reducing effect and towered total cholesterol and triglycerides significantly. The RMR was not changed during the 8-week diet in all groups. No significant difference among the groups was found in RMR, either. Stbject with higher RMR than the mean at the baseline showed a tendency to keep their RMR more stable during the diet program. Conclusions : Ephedra with a low-calorie diet was effective in reducing BMI. RMR change was not compensated by herbal medicines. RMR change seemed to be affected rather by constitution and body composition than medicine. Ephedra and Evodia were proven to be safe for sort-term use in herbal form. Especially, Ephedra was effective in lowering total cholesterol and triglycerides during the 8 weeks.
Objectives : This study evaluated activities and ingredient contents concerning extracts according to extraction solvents of Insampaedok-san (IS, Renshen bai du-san). Methods : The herbal constituents of IS were extracted with water and 70% ethanol at $100^{\circ}C$ for 2 hr. Using the HPLC system, the six ingredient contents of different solvent extracts of IS were analyzed. The nitric oxide (NO), prostaglandin $E_2$ ($PGE_2$) production and proinflammatory cytokines were measured in RAW264.7 cells stimulated with lipopolysaccharide (LPS). The macrophage-derived chemokine (MDC/CCL22) and regulated on activation normal T-cell expression and secreted (RANTES/CCL5) production were measured in HaCaT and BEAS-2B cells stimulated tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) and interferon-${\gamma}$ (IFN-${\gamma}$). The activities of glycerol-3-phosphate dehydrogenase (GPDH) and leptin level were measured in 3T3-L1 cells. Results : The calibration curves showed good linearity ($r^2$=1.0000) for different concentration ranges. The contents of liquiritin, naringin, hesperidin, neohesperirin and glycyrrizin in 70% ethanol extracts of IS were relatively higher than that of water extract, however the content of ferulic acid in 70% ethanol and water extract of IS were similar. The extraction solvents of water and 70% ethanol were evaluated inhibitory effect on the production of NO, $PGE_2$, TNF-${\alpha}$ and IL-6 in RAW 264.7 cells. Their extractions were inhibitory effect on production of MDC/CCL22 and RANTES/CCL5 in HaCaT cell and BEAS-2B cell, respectively. In addition, evaluated reduced on GPDH activity and leptin level in 3T3-L1 preadipocyte cell. Conclusions : Our results suggest that IS extracts were inhibitory effects of disease such as inflammation, allergies and obesity.
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