• Title/Summary/Keyword: Anti-obesity drug

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Modulatory Effects of Korean Red Ginseng Extract (Panax ginseng C.A. Meyer) on Cytochrome P450 after Oral Administration to Mice for 14 Days (마우스에 홍삼추출물의 14일간 경구 투여에 따른 약물대사효소 조절능 평가)

  • Kim, Hee-Yeon;Nam, Woong-Shik;Kim, Seong-Hee;Jang, Hye-Ryang;Lee, Mi-Kyoung;Kim, Tae-Wan;Lee, Sang-Kyu
    • Journal of Life Science
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    • v.22 no.8
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    • pp.991-998
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    • 2012
  • Ginseng is one of the most commonly used herbal medicines and health foods. Korean red ginseng (KRG; Panax ginseng C.A. Meyer) extract is known to have potential therapeutic activities, such as anti-viral effects, the amelioration of food allergies, anti-oxidant effects, and obesity reduction. Nevertheless, no reports have been issued the modulatory effects of KRG extract on the activity of cytochrome P450 (CYP). In the present study, we investigated the modulatory effect of KRG extract in vitro and in vivo by using pooled human liver microsomes and male ICR mice. When human liver microsomes were incubated with KRG extract at 0.01-10 mg/ml, CYP1A2, 2B6, 2C19, 2D6, and 3A were not significantly inhibited by KRG extract, although CYP2B6 was slightly inhibited. Mice were orally administered KRG extract at 50, 250, or 500 mg/kg daily for 3, 7, or 14 days. However, the activities of CYPs in mouse livers were not significantly different from those of vehicle-treated controls. In conclusion, no significant ginseng-drug interaction was observed. KRG extract did not significantly modulate the activities of CYPs in vitro or in vivo.

Pharmacokinetic and Pharmacodynamic Interaction between Metformin and (-)-Epigallocatechin-3-gallate

  • Ko, Jeong-Hyeon;Jang, Eun-Hee;Park, Chang-Shin;Kim, Hyoung-Kwang;Cho, Soon-Gu;Shin, Dong-Wun;Yi, Hyeon-Gyu;Kang, Ju-Hee
    • Molecular & Cellular Toxicology
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    • v.5 no.4
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    • pp.298-303
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    • 2009
  • (-)-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.

Inhibitory Effect of Triticum aestivum Ethanol Extract on Lipid Accumulation in 3T3-L1 Preadipocytes (3T3-L1 세포에서 소맥엽 에탄올추출물의 지질생성 억제효과)

  • Lee, Sun-Hee;Xin, Mingjie;Luyen, Bui Thi Thuy;Cha, Ji-Yun;Im, Ji-Young;Kwon, Se-Uk;Lim, Sung-Won;Suh, Joo-Won;Kim, Young-Ho;Kim, Dae-Ki;Lee, Young-Mi
    • YAKHAK HOEJI
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    • v.55 no.6
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    • pp.478-484
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    • 2011
  • Non-alcoholic fatty liver disease is known to be frequently associated with obesity and type 2 diabetes. We examined the effects of EtOH extracts from Triticum aestivum on lipid accumulation during the differentiation of 3T3-L1 preadipocytes to screening the candidate materials in preventing non-alcoholic fatty liver disease. The lipid level in adipocytes was determined by Oil Red O staining. The treatment of 50% ethanol, but not water and 100% ethanol extracts, from Triticum aestivum at concentration of 0.5 $mg/ml$ inhibited lipid accumulation in 3T3-L1 cells, revealing no cell toxicity. Thus, the fractions of $CH_2Cl_2$, EtOAc and BuOH were separated from 50% EtOH extract to characterize anti-adipogenic effect. The $CH_2Cl_2$ fraction at concentration of $50{\mu}g/ml$ effectively inhibited the lipid accumulation in the adipocytes compared to those of EtOAc and BuOH at concentration of $50{\mu}g/ml$. The intracellular triglyceride accumulation also was significantly reduced by treatment of $CH_2Cl_2$ fraction in concentration-dependent manner. Western blot analysis showed that the $CH_2Cl_2$ fraction attenuated the intracelluar level of fatty acid synthase(FAS) accompanied by attenuated expression of Peroxidase proliferator-activated receptor ${\gamma}$ ($PPAR{\gamma}$) adipogenic transcription factor. These results suggest that $CH_2Cl_2$ fraction from 50% EtOH extract of Triticum aestivum may has the potent anti-adipogenic effects by inhibiting the transactivation of $PPAR{\gamma}$.

Preventive Effect of the Water Extract of Agrimonia pilosa Ledeb and Micronucleus Assay-Based Evaluation of Genotoxicity in Gastritis Animal Models (동물모델을 이용한 짚신나물 물 추출물의 위염 예방효과 및 유전독성 평가)

  • Nho, Jong Hyun;Jang, Ji Hun;Lee, Hyun Joo;Yang, Beodul;Woo, Kyeong Wan;Kim, A Hyeon;Seo, Jae Wan;Hwang, Tae Yeon;Cho, Hyun Woo;Jung, Ho Kyung
    • Korean Journal of Medicinal Crop Science
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    • v.27 no.2
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    • pp.136-142
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    • 2019
  • Background: Agrimonia pilosa Ledeb has been used as a traditional medicine for the treatment of hematuresis and uterine bleeding in Korea. It has been reported to have anti-obesity, anti-diabetes and anti-inflammaotry effect by regulating the inflammatory signaling pathway. However, the preventive effect of Agrimonia pilosa Ledeb on gastritis has not been elucidated. Thus, in the present study, we evaluated the effects of the water extract of Agrimonia pilosa Ledeb (APW) using HCl/EtOH-induced gastritis rat models. Method and Results: Gastritis was induced in rats by HCl/EtOH administration. The rats in each group were orally administered with two doses of APW (100 and 500 mg/kg). Omeprazole was used as a positive control drug. An enzyme-linked immunosorbent assay (ELISA) was used to measure the prostaglandin $E_2$ ($PGE_2$) levels in stomach. The treatment with 500 mg/kg APW reduced the gastric ulcer area. The APW treatment prevented a decreased in $PGE_2$ concentration induced by HCl/EtOH in rats. In the micronucleus test, the ratio of micronucleated polychromatic erythrocytes to polychromatic erythrocytes showed no significant change in the APW-treated group compared with the control group. Conclusions: These results indicate that APW could be used to prevent the gastritis caused by the HCl/EtOH-induced damage to stomach lining. In addition, the APW treatment showed no significant change in results of the micronucleus test. However, further experiments are required to determine how APW influenced the secretion of mucus and gastric acid using the chromosome aberration test and bacterial reverse mutation assay.

Development of a Simultaneous Detection and Quantification Method of Anorectics in Human Urine Using GC-MS and its Application to Legal Cases (GC-MS를 이용한 사람 뇨시료 중 비만치료제 분석 및 비만치료제 남용 현황의 법과학적 고찰)

  • Choi, Hyeyoung;Lee, Jaesin;Jang, Moonhee;Yang, Wonkyung;Kim, Eunmi;Choi, Hwakyung
    • YAKHAK HOEJI
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    • v.57 no.6
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    • pp.420-425
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    • 2013
  • Phentermine (PT) and phenmetrazine (PM) have been widely used as anti-obesity drugs. These drugs should be used with caution due to its close relation to amphetamine in its structure and toxicity. PT and PM, amphetamine-type anorectics, have recently been considered as alternatives for methamphetamine abuse in Korea. In addition, the misuse and abuse of PT and PM obtained by illegal sources such as the internet become a serious social problem. In the present study, a simultaneous detection and quantification method for determining PT and PM in human urine was developed and validated according to the international guidelines. The urine samples were screened using a fluorescence polarization immunooassay and analyzed by gas chromatography mass spectrometry (GC-MS) after extraction using automatic solid phase extraction (SPE) with a mixed-mode cation exchange cartridge and derivatization with pentafluoropropionic anhydride (PFPA). The validation results for selectivity, linearity, limits of detection (LOD) and quantification (LOQ), intra- and inter-assay precision and accuracy and recovery were satisfactory. The validated method was successfully applied to authentic urine samples collected from 38 drug abuse suspects. PT and/or PM were identified with or without methamphetamine in urine samples. Abuse of PT and PM have increased continuously in Korea, therefore, closer supervision of the inappropriate use of anoretics is necessary.

Protective Effects of Ethanol Extract from Aster Yomena on Acute Pancreatitis (쑥부쟁이 에탄올 추출물의 급성췌장염 보호 효과)

  • Seo, Sang Wan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.33 no.2
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    • pp.109-115
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    • 2019
  • Aster Yomena (AY) has been used in traditional medicine to treat diseases such as obesity, hyperlipidemia, atherosclerosis, diabetes and osteoarthritis. However, protective effect of AY on acute pancreatitis (AP) has not been reported. The present study examined the anti-inflammatory effects of an ethanol extract of AY on cerulein-induced AP. AP was induced in mice by intraperitoneally injecting cerulein ($50{\mu}g/kg$) hourly for 6 times. 70% ethanol extract of AY (0.1, 0.2, and 0.5 g/kg) was orally administered for 1 week before acute pancreatitis induction. The mouse was killed at 6 hours after the final cerulein injection. The pancreas and lung were rapidly removed for histological examination and myeloperoxidase (MPO) assay. Blood samples were taken to determine serum amylase and lipase activity. In addition real-time reverse transcription-polymerase chain reaction (RT-PCR) was also performed to investigate mRNA expression of proinflammatory cytokines such as $TNF-{\alpha}$. $IL-1{\beta}$, and IL-6. Administration of AY significantly ameliorated pancreatic weight to body weight ratio, histological damages and MPO activity during AP. In addition, AY inhibited the serum amylase and lipase activity during AP. Also, mRNA expression of $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 were inhibited by AY against AP. Our results revealed that pre-treatment of AY reduces the severity of cerulein-induced AP. Therefore, AY may have a protective effect drug against AP.

Inhibitory Activities of Water Extracts of Black Ginseng on HCl/Ethanol-Induced Acute Gastritis through Anti-Oxidant Effect (흑삼 열수 추출물의 항산화 효과를 통한 염산/에탄올로 유발된 위염 억제 작용)

  • Kim, Min Yeong;Kwon, O Jun;Noh, Jeong Sook;Roh, Seong-Soo
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.9
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    • pp.1249-1256
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    • 2016
  • Black ginseng (BG) obtained by a 9-fold steaming process of Panax ginseng has been reported to have anti-oxidative, anti-obesity, and anti-diabetes effects. The current study evaluated the protective effect of BG by steaming time in an HCl/ethanol-induced acute gastritis model. BG was divided into four samples according to steaming-drying processing (Gin1, Gin3, Gin6, and BG). High performance liquid chromatography analysis, free radical scavenging activity, and total phenol and flavonoid contents were examined in ginseng and four BG samples. Compared with ginseng, BG showed a stronger radical scavenging effect and higher contents of total phenol and flavonoids. To evaluate the anti-gastritic effect of BG, mice were distributed into five groups: normal mice (N), acute gastritic mice with distilled water (CON), acute gastritic mice with 100 mg/kg of ginseng (Gin0), acute gastritic mice with 100 mg/kg of BG (BG), and acute gastritic mice with 10 mg/kg of sucralfate (SC). After 1 hour of pre-treatment with water, extracts (Gin0 and BG), or drug (SC), experimental groups except for N were orally administered 0.5 mL of 150 mM HCl/60% ethanol (v/v) mixture. Blood was collected 1 hour later from the heart, and gastric tissue was harvested. Reactive oxygen species (ROS) levels were measured in serum, and related protein expression was examined by Western blot assay. In HCl/ethanol-induced acute gastritic mice, treatment with ginseng or BG improved mucosal damage in the histological evaluation. The serum ROS level significantly decreased in the BG-treated group compared with the CON group. Furthermore, expression of inflammatory cytokines significantly decreased in the BG-treated group compared with the CON group. Based on these results, antioxidant and anti-gastritic activities of ginseng were enhanced by streaming-drying processing, in part due to an increase in biological active compounds.

Adipocyte Differentiation Inhibitor Isolated from the Barks of Phellodendron amurense (황백(Phellodendri Cortex)으로부터 분리한 지방세포 분화 저해물질)

  • Kim, Kyung-Hee;Ahn, Soon-Cheol;Lee, Myung-Sun;Kweon, Oh-Song;Oh, Won-Keun;Kim, Min-Soo;Sohn, Cheon-Bae;Ahn, Jong-Seog
    • Korean Journal of Food Science and Technology
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    • v.35 no.3
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    • pp.503-509
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    • 2003
  • For the development of the anti-obesity natural drug, the inhibitor of adipocyte differentiation was screened from Korean traditional medicinal plants. Phellodendri Cortex was selected as a candidate of adipocyte differentiation inhibitor. An inhibitory compound PC-4 was purified from the methanol (MeOH) extract of Phellodendri Cortex using silica gel and ODS RP-18 column chromatography and HPLC. PC-4 was obtained as yellow powder; UV ${\lambda}_{max}$ (MeOH): 230, 260, 340 and 430 nm. The chemical structure of PC-4 was determined as an isoquionoline alkaloid, berberine, on the basis of various NMR experiments including $^1H-\;and\;^{13}C-NMR$. The PC-4 inhibited the differentiation of preadipocyte NIH-3T3 L1 cells at a concentration of $1\;{\mu}g/mL$.

Comparative Evaluation of Korean Medicine Well-matched with Pork through an Inhibition of Pancreatic Lipase (저육(猪肉)과 잘 어울리는 췌장라이페이즈 억제능을 가진 한약재의 비교평가)

  • Shin, Mi-Rae;Kim, SooHyun;Lee, AhReum;Kim, KyeongJo;Kim, SuJi;Lee, Young Cheol;Roh, Seong-Soo
    • The Korea Journal of Herbology
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    • v.32 no.5
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    • pp.57-63
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    • 2017
  • Objectives : The aim of this study is to search Korean Medicine with the superior inhibitory effect of pancreatic lipase including a possibility as a well-matched sauce material with pork. Methods : We chose 5 samples which have the potent inhibitory effect of pancreatic lipase enzyme among 9 samples. 5 samples were Glycyrrhizae rhizoma, Cinnamomi cortex, Ganoderma lucidum, Syzygium aromaticum, and Schisandra chinensis. Animals were divided into eight groups (n=7). The experimental groups except for normal group were fed 60% high-fat diet. 5 samples were orally administered at a dose of 200 mg/kg body weight and orlistat were orally administrated at a dose of 60 mg/kg body weight for 7 days. Biochemical anaylses of 5 samples were executed based on lipid parameters such as triglyceride (TG) and total cholesterol (TC). Results : Korean Medicines with $IC_{50}$ of below $1mg/m{\ell}$ were Glycyrrhizae rhizoma, Cinnamomi cortex, Ganoderma lucidum, Syzygium aromaticum, and Schisandra chinensis. Body weight change of all drug-treated groups except Glycyrrhizae rhizoma reduced significantly during the experimental period. Orlistat treatment reduced significantly both TG and TC in serum. The significant emission of TG in fece showed in Cinnamomi cortex treatment, whereas Ganoderma lucidum and Syzygium aromaticum showed a tendency to increase without a significance. Besides, Ganoderma lucidum and Schisandra chinensis emitted significantly TC to fece. Conclusions : In conclusion, Cinnamomi cortex may exert anti-obesity effect by directly inhibiting pancreatic lipase, which would prevent the absorption of lipid from the small intestine. Accordingly, Cinnamomi cortex may suggest a high possibility as a well-matched sauce material with pork.