• The Korea Journal of Herbology
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• v.20 no.2
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• pp.91-102
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• 2005

Objectives : By examining the effects of Jwa Kum-Whan composed of Coptidis Rhizoma and Evodiae Fructus by the ratio of 6:1 the effects of Soo Ryeon-Whan and composed of Coptidis Rhizoma and Evodiae Fructus by the ratio of 1:1 on hyperlipidemia, the present study attempted to reveal the change of effects based on the ratio of combination. Methods : Jwa Kum-Whan and Soo Ryeon-Whan were injected to rats suffered from induced hyperlipidemia, and then its influence on lipid. During the cultivation of hepatocytes, Jwa Kum-Whan and Soo Ryeon-Whan were added to culture media, and the expression of the enzymes relevant to fat metabolism of hepatocytes was examined. Results : 1. Jwa Kum-Whan significantly decreased total cholesterol(Tc), triglyceride(TG), and LDL-cholesterol(LDLc) of rats suffering from hyperlipidemia induced by high cholesterol diet. Soo Ryeon-Whan decreased LDLc, but had no significant on Tc and TG. 2. Jwa Kum-Whan increased the expression of cholesterol esterase, LDL-receptor, diacylglycerol acyltransferase (DGAT), acylCoA-cholesterol-acyltransferase (ACAT), peroxisome proliferator activated receptor gamma $(PPAR{\gamma})$, peroxisome proliferator activated receptor alpha $(PPAR{\alpha})$ of cultivated hepatocytes. In addition, Soo Ryeon-Whan increased the expression of cholesterol esterase, LDL-Receptor, DGAT, $PPAR{\gamma},\;PPAR{\alpha}$ of cultivated hepatocytes, but had no significant effects on the expression of ACAT. Conclusion : Both Jwa Kum-Whan and Soo Ryeon-Whan were composed of Coptidis Rhizoma and Evodiae Fructus, but the fonner is more effective in hyperlipidemia.

• KSBB Journal
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• v.31 no.3
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• pp.145-150
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• 2016

Boehmeria nivea (L.) Gaud., a flowering plant, has been widely cultivated in Asian countries including Korea. It has been reported that B. nivea exhibits health beneficial effects for the prevention of inflammation, oxidative stress, and virus-related diseases. In this study, we evaluated the inhibitory effect of B. nivea on adipocyte differentiation and angiogenesis. DPPH radical scavenging activities of 70% ethanol extract of B. nivea (EBN) and water extract of B. nivea (WBN) were $90.8{\pm}1.1%$ and $20{\pm}6.9%$, respectively. EBN was also effective in the reduction of adipocyte differentiation in 3T3-L1 cells. We next examined the transcriptional activity of peroxisome proliferator-activated receptor gamma ($PPAR-{\gamma}$), a pivotal target for anti-obesity. We found that treatment with rosiglitazone induced the transactivation of $PPAR-{\gamma}$. Under the same condition, $800{\mu}g/mL$ EBN reduced the transactivation of $PPAR-{\gamma}$ in rosiglitazone-induced cells. These results demonstrate that EBN-inhibited adipocyte differentiation was accompanied by $PPAR-{\gamma}$ inhibition. The study also tested whether EBN exhibits an anti-angiogenic effect by inhibiting tube formation in HUVECs. We found that EBN effectively inhibits tube formation, suggesting that EBN exhibited an anti-angiogenic effect. Taken together, B. nivea can be used as a functional food for the prevention of obesity and angiogenesis-related diseases including cancer.

• Toxicological Research
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• v.29 no.1
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• pp.7-14
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• 2013

Betaine supplementation has been shown to alleviate altered glucose and lipid metabolism in mice fed a high-fat diet or a high-sucrose diet. We investigated the beneficial effects of betaine in diabetic db/db mice. Alleviation of endoplasmic reticulum (ER) and oxidative stress was also examined in the livers and brains of db/db mice fed a betaine-supplemented diet. Male C57BL/KsJ-db/db mice were fed with or without 1% betaine for 5 wk (referred to as the db/db-betaine group and the db/db group, respectively). Lean non-diabetic db/+ mice were used as the control group. Betaine supplementation significantly alleviated hyperinsulinemia in db/db mice. Betaine reduced hepatic expression of peroxisome proliferator-activated receptor gamma coactivator 1 alpha, a major transcription factor involved in gluconeogenesis. Lower serum triglyceride concentrations were also observed in the db/db-betaine group compared to the db/db group. Betaine supplementation induced hepatic peroxisome proliferator-activated receptor alpha and carnitine palmitoyltransferase 1a mRNA levels, and reduced acetyl-CoA carboxylase activity. Mice fed a betaine-supplemented diet had increased total glutathione concentrations and catalase activity, and reduced lipid peroxidation levels in the liver. Furthermore, betaine also reduced ER stress in liver and brain. c-Jun N-terminal kinase activity and tau hyperphosphorylation levels were lower in db/db mice fed a betaine-supplemented diet, compared to db/db mice. Our findings suggest that betaine improves hyperlipidemia and tau hyperphosphorylation in db/db mice with insulin resistance by alleviating ER and oxidative stress.

• Preventive Nutrition and Food Science
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• v.18 no.2
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• pp.85-91
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• 2013

Recent studies have shown that Rosa canina L. and tiliroside, the principal constituent of its seeds, exhibit anti-obesity and anti-diabetic activities via enhancement of fatty acid oxidation in the liver and skeletal muscle. However, the effects of rosehip, the fruit of this plant, extract (RHE), or tiliroside on lipid accumulation in adipocytes have not been analyzed. We investigated the effects of RHE and tiliroside on lipid accumulation and protein expression of key transcription factors in both in vitro and in vivo models. RHE and tiliroside inhibited lipid accumulation in a dose-dependent manner in 3T3-L1 cells. We also analyzed the inhibitory effect of RHE on white adipose tissue (WAT) in high-fat diet (HFD)-induced obesity mice model. Male C57BL/6J mice were fed HFD or HFD supplemented with 1% RHE (HFDRH) for 8 weeks. The HFDRH-fed group gained less body weight and had less visceral fat than the HFD-fed group. Liver weight was significantly lower in the HFDRH-fed group and total hepatic lipid and triglyceride (TG) content was also reduced. A significant reduction in the expression of peroxisome proliferator-activated receptor gamma (PPAR${\gamma}$) was observed in epididymal fat in the HFDRH-fed group, in comparison with controls, through Western blotting. These results suggest that downregulation of PPAR${\gamma}$ expression is involved, at least in part, in the suppressive effect of RHE on lipid accumulation in WAT.

• The Korean Journal of Physiology and Pharmacology
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• v.15 no.3
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• pp.157-162
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• 2011

Vascular inflammation process has been suggested to be an important risk factor in the development of atherosclerosis. Recently we reported that induction of peroxisome proliferator-activated receptor-${\gamma}$ (PPAR-${\gamma}$) selectively inhibits vascular cell adhesion molecule-1 (VCAM-1) but not intercellular cell adhesion molecule-1 (ICAM-1) in tumor necrosis factor (TNF)-${\alpha}$-activated human umbilical vein endothelial cells (HUVEC). In this study, we investigated whether genipin inhibits expression of cellular adhesion molecules, which is relevant to inflammation. Pretreatment with genipin reduced reactive oxygen species (ROS) production and expression of VCAM-1, but not ICAM-1 in TNF-${\alpha}$-activated HUVEC. Genipin dose- and time-dependently increased PPAR-${\gamma}$ expression and inhibited TNF-${\alpha}$-induced phosphorylation of Akt and PKC with different degrees. Finally, genipin prevented TNF-${\alpha}$-induced adhesion of U937 monocytic cells to HUVEC. Taken together, these results indicate that upregualtion of PPAR-${\gamma}$ by genipin selectively inhibits TNF-${\alpha}$-induced expression of VCAM-1, in which regulation of Akt and/or PKC play a key role. We concluded that genipin can be used for the treatment of cardiovascular disorders such as atherosclerosis.

• YAKHAK HOEJI
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• v.53 no.4
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• pp.184-188
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• 2009

Fluorouracil (5-FU) is one of the most widely used chemotherapeutic drugs in the treatment of advanced colorectal cancer patients. Capsaicin (N-vanillyl-8-methyl-alpha-nonenamide), a spicy component of hot pepper, is a homovanillic acid derivative that preferentially induces cancer cells to undergo apoptosis. The purpose of the present study is to examine whether capsaicin enhances the anticancer effect of 5-fluorouracil in HT-29 human colon cancer cells by inducing apoptosis, and whether PPARgamma is involved in the capsaicin action in combination treatment with 5-FU. Treatment of the cells with either 5-FU or capsaicin alone for 48 h had little effect on the cell viability up to $50{\mu}M$ concentration, whereas co-treatment of the cells with capsaicin in the presence of 5-FU for 48 h significantly decreased the cell viability in a concentration-dependent manner. In addition, caspase-3 activity, a marker enzyme for apoptosis, was significantly increased by the combined treatment with 5-FU and capsaicin compared to the 5-FU or capsaicin alone treatment. Also, treatment with troglitazone, a peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) agonist, further enhanced the effect of the combination treatment on the cell viability and caspase-3 activity, and bisphenol A diglycidyl ether (BADGE), a $PPAR{\gamma}$ antagonist, blocked the effect of the combination treatment. These results suggest that the combination treatment of HT-29 cells with 5-FU and capsaicin induces apoptotic cell death at relatively low concentration than each drug alone, and the combination treatment may be associated with the $PPAR{\gamma}$ pathway activation.

• Bulletin of the Korean Chemical Society
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• v.33 no.7
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• pp.2219-2223
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• 2012

Human peroxisome proliferator-activated receptor gamma ($hPPAR{\gamma}$) has been implicated in numerous pathologies, including obesity, diabetes, and cancer. Previously, we verified that amentoflavone is an activator of $hPPAR{\gamma}$ and probed the molecular basis of its action. In this study, we investigated the mechanism of action of amentoflavone in cancer cells and demonstrated that amentoflavone showed strong cytotoxicity against MCF-7 and HeLa cancer cell lines. We showed that $hPPAR{\gamma}$ expression in MCF-7 and HeLa cells is specifically stimulated by amentoflavone, and suggested that amentoflavone-induced cytotoxic activities are mediated by activation of $hPPAR{\gamma}$ in these two cancer cell lines. Moreover, amentoflavone increased PTEN levels in these two cancer cell lines, indicating that the cytotoxic activities of amentoflavone are mediated by increasing of PTEN expression levels due to $hPPAR{\gamma}$ activation.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.1
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• pp.1-8
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• 2008

Epidermis is one of the most dynamic organs in the human body. Multiple layers of keratinocytes in the epidermis continuously undergo proliferation, differentiation, and desquamation cycles, which is the bases of maintaining the epidermal homeostasis. Epidermal homeostasis eventually leads to establish and maintain permeability barrier homeostasis, the most important function of the epidermis. The permeability barrier is located in the stratum corneum. Tightly coordinated regulations are required for the sustained normal barrier function. Extensive studies have established that several nuclear hormone liposensors, including peroxisome proliferator-activated receptor a PPARa, PPARb/d, PPARg and LXRs are expressed in keratinocyte. Activation of PPARs and LXRs could provide a mechanism to coordinate the formation of the corneocytes and extracellular lipid membranes that constitute the stratum corneum. Topical application of PPAR/LXR ligands to murine skin results in the increased expression of keratinocyte differentiation-related proteins, such as involucrin, loricrin, profilaggrin, and trans-glutaminase 1, which would stimulate cornified envelope formation. In conclusion, topical application of ligands or activators of PPAR/LXR as an epidermotherapy would be a promising option to deal dry skin conditions such as atopy.

• Journal of Ginseng Research
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• v.41 no.3
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• pp.240-246
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• 2017

Background: Korean Red Ginseng (KRG) is a traditional herbal medicine made by steaming and drying fresh ginseng. It strengthens the endocrine and immune systems to ameliorate various inflammatory responses. The cyclooxygenase-2 (COX-2)/prostaglandin E2 pathway has important implications for inflammation responses and tumorigenesis. Peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) is a transcription factor that regulates not only adipogenesis and lipid homeostasis, but also angiogenesis and inflammatory responses. Methods: The effects of the KRG on inhibition of hypoxia-induced COX-2 via $PPAR{\gamma}$ in A549 cells were determined by luciferase assay, Western blot, and/or quantitative reverse transcription-polymerase chain reaction (qRT-PCR). The antimigration and invasive effects of KRG were evaluated on A549 cells using migration and matrigel invasion assays. Results and conclusion: We previously reported that hypoxia-induced COX-2 protein and mRNA levels were suppressed by KRG. This study examines the possibility of $PPAR{\gamma}$ as a cellular target of KRG for the suppression of hypoxia-induced COX-2. $PPAR{\gamma}$ protein levels and $PPAR{\gamma}$-responsive element (PPRE)-driven reporter activities were increased by KRG. Reduction of hypoxia-induced COX-2 by KRG was abolished by the $PPAR{\gamma}$ inhibitor GW9662. In addition, the inhibition of $PPAR{\gamma}$ abolished the effect of KRG on hypoxia-induced cell migration and invasion. Discussion: Our results show that KRG inhibition of hypoxia-induced COX-2 expression and cell invasion is dependent on $PPAR{\gamma}$ activation, supporting the therapeutic potential for suppression of inflammation under hypoxia. Further studies are required to demonstrate whether KRG activates directly $PPAR{\gamma}$ and to identify the constituents responsible for this activity.

• Journal of Ginseng Research
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• v.44 no.1
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• pp.123-134
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• 2020

Background: The lepidopteran Asiatic corn borer (ACB), Ostrinia furnacalis (Guenee), has caused huge economic losses throughout the Asian-Western Pacific region. Usually, chemical pesticides are used for the control, but excessive use of pesticides has caused great harm. Therefore, the inartificial ecotypic pesticides to ACB are extremely essential. In our previous study, we found that panaxadiol saponins (PDS) can effectively reduce the harm of ACB by causing antifeedant activity. Therefore, it is necessary to reveal the biological molecular changes in ACB and the functionary mechanism of PDS. Methods: We analyzed the global transcription of ACB with different PDS concentration treatment (5 mg/mL, 10 mg/mL, and 25 mg/mL) by high-throughput sequencing and de novo transcriptome assembly method. Results: PDS treatment could cause the changes of many gene expressions which regulate its signal pathways. The genes in peroxisome proliferator-activated receptor (PPAR) signaling pathway were significantly downregulated, and then, the downstream fatty acid degradation pathway had also been greatly affected. Conclusion: Through this experiment, we hypothesized that the occurrence of antifeedant action of ACB is because the PDS brought about the downregulation of FATP and FABP, the key regulators in the PPAR, and the downregulation of FATP and FABP exerts further effects on the expression of SCD-1, ACBP, LPL, SCP-X, and ACO, which leads to the disorder of PPAR signaling pathway and the fatty acid degradation pathway. Not only that, PDS treatment leads to enzyme activity decrease by inhibiting the expression of genes associated with catalytic activity, such as cytochrome P450 and other similar genes.