• 대한화장품학회지
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• 제35권2호
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• pp.117-123
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• 2009

후박추출물은 중국 원산인 당후박에서 제조되며, 항산화 및 항염증 효과로 알려져 있다. 후박의 성분으로는 폴레페놀인 honokiol 및 magnolol 등이 알려져 있다. 이 연구에서, 우리는 후박추출물이 triglyceride (TG)의 축척을 감소시킴으로써 지방세포 분화를 억제한다는 표면적인 결과를 얻었다. 또한, 후박 추출물이 hormone sensitive lipase (HSL) 단백질 수준을 증가시키고 adipocyte에 specific한 transcription factors로 peroxisome proliferator activated receptor (PPAR)-${\gamma}$의 단백질과 mRNA 수준을 억제하였다. 결과적으로, 후박추출물이 항비만제로서 adipogenic transcription factor와 그들의 특이적인 유전자의 발현을 억제함으로써 지방세포 분화를 억제한다고 사료된다.

• Journal of Animal Science and Technology
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• 제46권1호
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• pp.23-30
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• 2004

지방세포분화 과정에서 중추적인 역할을 한다고 보고되어지고 있는 PPAR$\gamma$ 유전자를 cloning 하기 위하여 한우 12개월 지방조직을 이용하여 Total RNA를 추출하고 RT-PCR을 수행하여 1515bp, 505 아미노산 서열을 가진 PPAR$\gamma$ 유전자를 cloning 하였다. bovine을 제외한 4종의 다른 동물과의 아미노산 서열을 비교한 결과 모두 90% 이상의 상동성을 나타내었다. 특히 NCBl에 보고된 Norwegian cattle PPAR$\gamma$ (NCBI Accession No. O18971)의 아미노산 서열과 비교한 결과 99.2%의 상동성을 나타내었으며 아미노산 서열중 81번째 이소루신, 140번째 아르기닌, 157번째 글루탐산, 486번째 리신이 각각 트레오닌, 트립토판, 글리신, 이소루신으로 치환된 상태의 아미노산 서열을 나타내었다. 특히 nuclear hormone receptor의 DNA binding domain 영역에 포함 되는 140번째, 157번째 아미노산의 치환은 앞으로 한우PPAR$\gamma$ 유전자가 조절하는 다른 유전자와의 관계를 밝히는데 매우 중요한 점이 될 것으로 사료되어진다. 한우 PPAR$\gamma$ 의 발현은 지방조직에서 매우 높은 발현을 보였으며, 한우 12개월령과 30개월령 지방조직에서의 PPAR$\gamma$ 발현을 비교 분석하였을 때 12개월령에서보다 30개월령 지방조직에서 PPAR$\gamma$ 발현이 약 6배정도 높았다. 이와 같은 결과는 한우 PPAR$\gamma$ 유전자도 사람과 생쥐에서와 같이 지방분화에 관여하고 있다는 보고와 일치하는 결과라고 사료된다.

• Journal of Applied Biological Chemistry
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• 제60권1호
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• pp.23-28
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• 2017

본 연구에서는 초과 에탄올 추출물을 이용하여 3T3-L1 지방전구세포에서 지방세포로의 분화 연구를 통해 항비만 활성을 확인하고자 하였다. 초과 에탄올 추출물에 의한 지방세포 분화 억제 활성 및 지방형성에 미치는 영향을 확인하기 위해 3T3-L1 지방전구세포에 분화를 유도하면서 추출물을 농도별로 처리하였고, 그 결과 초과 에탄올 추출물은 3T3-L1 지방전구세포에서 지방세포로의 분화를 농도에 의존적으로 감소시켰다. 이 같은 활성에 대한 작용기전을 알아보기 위해 지방세포 분화에 중요한 역할을 담당하고 있는 peroxisome proliferator-activated receptor ${\gamma}$ ($PPAR{\gamma}$)와 CCAAT-enhancer-binding protein ${\alpha}$ ($C/EBP{\alpha}$), 그리고 지방세포 분화에 관여하는 유전자들의 활성을 확인해 보았다. 실험 결과 초과 에탄올 추출물은 $PPAR{\gamma}$와 $C/EBP{\alpha}$의 유전자 및 단백질 발현을 유의적으로 감소시켰고 지방세포 분화에 관여하는 adipogenesis marker 유전자들의 발현을 억제 시켰다. 따라서 초과 에탄올 추출물은 지방분화 및 adipogenesis 억제 활성을 통해 항비만 소재로의 가능성이 있을 것으로 기대한다.

• The Korean Journal of Physiology and Pharmacology
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• 제21권3호
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• pp.293-300
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• 2017

Prostaglandin $D_2$ ($PGD_2$) may act against myocardial ischemia-reperfusion (I/R) injury and play an anti-inflammatory role in the heart. Although the effect of $PGD_2$ in regulation of ANP secretion of the atrium was reported, the mechanisms involved are not clearly identified. The aim of the present study was to investigate whether $PGD_2$ can regulate ANP secretion in the isolated perfused beating rat atrium, and its underlying mechanisms. $PGD_2$ (0.1 to $10{\mu}M$) significantly increased atrial ANP secretion concomitantly with positive inotropy in a dose-dependent manner. Effects of $PGD_2$ on atrial ANP secretion and mechanical dynamics were abolished by AH-6809 ($1.0{\mu}M$) and AL-8810 ($1.0{\mu}M$), $PGD_2$ and prostaglandin $F2{\alpha}$ ($PGF2{\alpha}$) receptor antagonists, respectively. Moreover, $PGD_2$ clearly upregulated atrial peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) and the $PGD_2$ metabolite 15-deoxy-${\Delta}12$, 14-$PGJ_2$ (15d-$PGJ_2$, $0.1{\mu}M$) dramatically increased atrial ANP secretion. Increased ANP secretions induced by $PGD_2$ and 15d-$PGJ_2$ were completely blocked by the $PPAR{\gamma}$ antagonist GW9662 ($0.1{\mu}M$). PD98059 ($10.0{\mu}M$) and LY294002 ($1.0{\mu}M$), antagonists of mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) and phosphatidylinositol-3-kinase (PI3K)/protein kinase B (Akt) signaling, respectively, significantly attenuated the increase of atrial ANP secretion by $PGD_2$. These results indicated that $PGD_2$ stimulated atrial ANP secretion and promoted positive inotropy by activating $PPAR{\gamma}$ in beating rat atria. MAPK/ERK and PI3K/Akt signaling pathways were each partially involved in regulating $PGD_2$-induced atrial ANP secretion.

• 대한본초학회지
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• 제20권2호
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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.

• Archives of Pharmacal Research
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• 제29권5호
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• pp.394-399
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• 2006

Benzothiazole derivatives of thiazolidinediones (TZD) were synthesized using a modified Mitsunobu reaction of 2-(benzothiazol-2-ylmethylamino)ethanol (2) with 5-(4-hydroxybenzyl)-3-triphenylmethylthiazolidine-2,4-dione and assayed for activity on peroxisome proliferator-activated receptor (PPAR) subtypes and inhibitory activity of NO production in lipopolysaccharide-activated macrophages. Most of the tested compounds were identified as potent $PPAR_\gamma$ agonists, indicating their potential as drug candidates for diabetes.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2003년도 추계학술대회
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• pp.180-180
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• 2003

Peroxisome proliferator-activated receptor gamma (PPAR-gamma), a member of the nuclear hormone receptor superfamily, is involved in the suppression of growth of several types of tumors such as liposarcoma, cancers of breast, prostate, and colon, possibly through induction of cell cycle arrest and/or apoptosis.(omitted)

• Asian Pacific Journal of Cancer Prevention
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• 제15권5호
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• pp.2313-2318
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• 2014

Peroxisome proliferator-activated receptor gamma (PPAR-${\gamma}$), a ligand-dependent nuclear transcription factor, has been found to widely exist in tumor tissues and plays an important role in affecting tumor cell growth. In this study, we investigated the effect of PPAR-${\gamma}$ on aspects of the cervical cancer malignant phenotype, such as cell proliferation and apoptosis. Cell growth assay, Western blotting, Annexin V and flow cytometry analysis consistently showed that treatment with troglitazone (TGZ, a PPAR-${\gamma}$ agonist) led to dose-dependent inhibition of cervical cancer cell growth through apoptosis, whereas T0070907 (another PPAR-${\gamma}$ antagonist) had no effect on Hela cell proliferation and apoptosis. Furthermore, we also detected the protein expression of p53, p21 and Mdm2 to explain the underlying mechanism of PPAR-${\gamma}$ on cellular apoptosis. Our work, finally, demonstrated the existence of the TGZ-PPAR-${\gamma}$-p53 signaling pathway to be a critical regulator of cell apoptosis. These results suggested that PPAR-${\gamma}$ may be a potential therapeutic target for cervical cancer.

• Asian Pacific Journal of Cancer Prevention
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• 제16권13호
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• pp.5219-5223
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• 2015

Helicobacter pylori (H. pylori) infection as a serious problem in both adults and children can induce chronic gastritis, peptic ulcer disease (PUD), and possibly gastric cancer. The aim of the current study was to survey antibiotic resistance and also to determine influence of PPAR$\gamma$ polymorphism in patients with H. pylori infection. During an 11-month-period, 98 H. pylori isolates were collected from 104 biopsy specimens. In vitro susceptibility of H. pylori isolates to 4 antimicrobial agents metronidazole, clarithromycin, amoxicillin and tetracycline were assessed by quantitative method according to European Committee on Antimicrobial Susceptibility Testing (EUCAST) guideline. PPAR$\gamma$ polymorphism was determined using polymerase chain reaction-restriction fragment length polymorphism assay. The frequency of H. pylori infection in our study was 94.2%. In vitro susceptibility data showed that highest level of resistance was related to metronidazole (66.3%), and the majority of H. pylori isolates were highly susceptible to amoxicillin and tetracycline (94.9% and 96.9%, respectively). Genotypic frequencies were 25.5% for CC (Pro12Pro), 40.8% for GC (Pro12Ala) and 33.7% for GG (Ala12Ala). In our study, CG genotype had highest distributions among infected patients with H. pylori. The study suggests that the PPAR-$\gamma$ Pro12Ala polymorphism could be evaluated as a potential genetic marker for susceptibility to gastric cancer in the presence of H. pylori infection.

• Preventive Nutrition and Food Science
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• 제18권2호
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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.