• Title/Summary/Keyword: Anti-obesity drug

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Analysis and management of new hazard chemicals in foods (식품 중 신종유해물질의 관리 및 분석)

  • Choi, Dongmi;Hu, Soojung;Suh, Junghyuck;Yoon, Taehyung;Kim, Eunju;Choi, Jangduck;Park, Sung-Kug;Lee, Kwangho
    • Analytical Science and Technology
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    • v.22 no.2
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    • pp.172-185
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    • 2009
  • To help understanding about hazard chemicals occurring newly in food, it has been reviewed characteristics, mechanism, food standards and analytical trend of the hazard chemicals occurring avoidably in food manufacturing process. The new hazard chemicals in food are classified by 4 regarding mechanism such as heat, fermentation, additives and unknowns. The new hazard chemicals by heat process are acrylamide, furan, HCAs and PAHs. By the fermentation, ethylcarbamate and biogenic amines are occurred. According to food additives, 3-MCPD, benzene and nitrosamines can be produced. And the last group is the illegal compounds including anti-impotence drug analogues and anti-obesity drug analogues. To analyze the new hazard chemicals in food, GC or LC with UVD, FLD or MSD are used mainly after sample pretreatment by LLE, SPE or headspace method.

Pancreatic lipase inhibitory activity of taraxacum officinale in vitro and in vivo

  • Zhang, Jian;Kang, Min-Jung;Kim, Myung-Jin;Kim, Mi-Eun;Song, Ji-Hyun;Lee, Young-Min;Kim, Jung-In
    • Nutrition Research and Practice
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    • v.2 no.4
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    • pp.200-203
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    • 2008
  • Obesity has become a worldwide health problem. Orlistat, an inhibitor of pancreatic lipase, is currently approved as an anti-obesity drug. However, gastrointestinal side effects caused by Orlistat may limit its use. In this study the inhibitory activities of dandelion (Taraxacum officinale) against pancreatic lipase in vitro and in vivo were measured to determine its possible use as a natural anti-obesity agent. The inhibitory activities of the 95% ethanol extract of T. officinale and Orlistat were measured using 4-methylumbelliferyl oleate (4-MU oleate) as a substrate at concentrations of 250, 125, 100, 25, 12.5 and $4\;{\mu}g/ml$. To determine pancreatic lipase inhibitory activity in vivo, mice (n=16) were orally administered with com oil emulsion (5 ml/kg) alone or with the 95% ethanol extract of T. officinale (400 mg/kg) following an overnight fast. Plasma triglyceride levels were measured at 0, 90, 180, and 240 min after treatment and incremental areas under the response curves (AUC) were calculated. The 95% ethanol extract of T. officinale and Orlistat, inhibited, porcine pancreatic lipase activity by 86.3% and 95.7% at a concentration of $250\;{\mu}g/ml$, respectively. T. officinale extract showed dose-dependent inhibition with the $IC_{50}$ of $78.2\;{\mu}g/ml$. A single oral dose of the extract significantly inhibited increases in plasma triglyceride levels at 90 and 180 min and reduced AVC of plasma triglyceride response curve (p<0.05). The results indicate that T. officinale exhibits inhibitory activities against pancreatic lipase in vitro and in vivo. Further studies to elucidate anti-obesity effects of chronic consumption of T. officinale and to identify the active components responsible for inhibitory activity against pancreatic lipase are necessary.

Screening of Protein Tyrosine Phosphatase 1B Inhibitory Activity from Some Vietnamese Medicinal Plants

  • Hoang, Duc Manh;Trung, Trinh Nam;Hien, Phan Thi Thu;Ha, Do Thi;Van Luong, Hoang;Lee, Myoung-Sook;Bae, Ki-Hwan
    • Natural Product Sciences
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    • v.16 no.4
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    • pp.239-244
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    • 2010
  • Protein tyrosine phosphatase 1B (PTP1B), a negative regulator of insulin signaling, has served as a potential drug target for the treatment of type 2 diabetes. The MeOH extracts of twenty-nine medicinal plants, traditionally used in Vietnam as anti-diabetes agents, were investigated for PTP1B inhibitory activity in vitro. The results indicated that, most materials showed moderate to strong inhibitory activity with $IC_{50}$ values ranging from $3.4\;{\mu}g/mL$ to $35.1\;{\mu}g/mL$; meanwhile, eleven extracts (37.9%) could demonstrate PTP1B activity with $IC_{50}$ values less than $15.5\;{\mu}g/mL$; sixteen extracts (55.2%) could demonstrate PTP1B activity with $IC_{50}$ values ranging from $15.5\;{\mu}g/mL$ to $35.1\;{\mu}g/mL$. The study may provide a proof, at least in a part, for the ethno-medical use in diabetes disease of these plants.

Investigating the Status of WHO VigiAccess Adverse Drug Event Reporting and Exploring its Potential for Application Using Anti-Obesity Agents as Examples (VigiAccess를 통한 WHO의 약물 이상사례 보고 현황 검색과 그 활용 가능성 탐색 : 비만 치료제를 중심으로)

  • Mikyung Kim
    • The Journal of Internal Korean Medicine
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    • v.45 no.1
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    • pp.55-74
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    • 2024
  • Objectives: This study reviewed the status of adverse event (AE) reporting in VigiAccess using anti-obesity agents as examples and explored the possibility of its use and future challenges. Methods: AE reports related to some representative drugs among herbal medicines (HMs), complex HM prescriptions, ingredients of supplements, and over-the-counter and prescription medicines were investigated using VigiAccess on February 1, 2024. Results: AE reports on prescription drugs were overwhelmingly higher than those on HMs or supplements. Although most reports were submitted from North America, reports on Ephedra sinica and green tea extract (GTE) were more from Asia and Europe, respectively. The female population reported more, and the difference in the sex ratio was the smallest for Ephedra spp. The age group was concentrated on young adults, but many older patients reported GLP-1 receptor agonist-related AEs. Symptoms related to the gastrointestinal and nervous systems were most commonly reported, but mental and cardiac disorders were common in Ephedra-type HMs. Hepatobiliary disorders are also commonly found in GTE-related reports. Conclusions: VigiAccess was useful for easily checking the global status of AE reporting for prescription drugs. However, several limitations were observed in using VigiAccess for HMs because of the few reports. Thus, it is necessary to increase the number of reports by education and to promote AE reporting among HM prescribers and users. The full range of HMs should be included in the pharmacovigilance system, and the coding and classification of HMs should be revised.

Revisiting PPARγ as a target for the treatment of metabolic disorders

  • Choi, Sun-Sil;Park, Jiyoung;Choi, Jang Hyun
    • BMB Reports
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    • v.47 no.11
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    • pp.599-608
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    • 2014
  • As the prevalence of obesity has increased explosively over the last several decades, associated metabolic disorders, including type 2 diabetes, dyslipidemia, hypertension, and cardiovascular diseases, have been also increased. Thus, new strategies for preventing and treating them are needed. The nuclear peroxisome proliferator-activated receptors (PPARs) are involved fundamentally in regulating energy homeostasis; thus, they have been considered attractive drug targets for addressing metabolic disorders. Among the PPARs, $PPAR{\gamma}$ is a master regulator of gene expression for metabolism, inflammation, and other pathways in many cell types, especially adipocytes. It is a physiological receptor of the potent anti-diabetic drugs of the thiazolidinediones (TZDs) class, including rosiglitazone (Avandia). However, TZDs have undesirable and severe side effects, such as weight gain, fluid retention, and cardiovascular dysfunction. Recently, many reports have suggested that $PPAR{\gamma}$ could be modulated by post-translational modifications (PTMs), and modulation of PTM has been considered as novel approaches for treating metabolic disorders with fewer side effects than the TZDs. In this review, we discuss how PTM of $PPAR{\gamma}$ may be regulated and issues to be considered in making novel anti-diabetic drugs that can modulate the PTM of $PPAR{\gamma}$.

Hypocholesterolemic Effect of Ginkgo Biloba Seeds Extract from High Fat Diet Mice

  • Kang, Hyun
    • Biomedical Science Letters
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    • v.23 no.2
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    • pp.138-143
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    • 2017
  • To investigate the efficacy of extract of Ginkgo Biloba seeds in high fat diet (HFD) in mice, the Ginkgo Biloba seeds extract (GSE) was orally administered to mice with a HFD at 300 mg/kg/day for 4 weeks. Our results show that GSE significantly inhibited fat accumulation. Moreover, GSE markedly reduced the final body weight with a decrease in epididymal adipose tissue mass and adipocyte size compared with the untreated HFD-induced group. Additionally, GSE ameliorated serum high-density lipoprotein cholesterol levels. The results show that Ginkgo Biloba seeds possesses hypocholesterolemic effect through down regulating lipid metabolism. Further studies are required in this area to strengthen the anti-obesity effects of GSE with active component, and it can be used a pro-drug instead of whole extract.

Hypocholesterolemic Effect of Tartary Buckwheat (F. tataricum Gaertn.) Extract from High Fat Diet Mice

  • Lee, Sung-Gyu;Lee, Dongsup;Kang, Hyun
    • Biomedical Science Letters
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    • v.23 no.1
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    • pp.34-38
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    • 2017
  • To investigate the efficacy of extract of Tartary buckwheat (F. tataricum Gaertn.) in high fat diet (HFD) in mice, the F. tataricum Gaertn. extract (FTE) was orally administered to mice with a HFD at 300 mg/kg/day for 4 weeks. Our results show that FTE significantly inhibited fat accumulation. Moreover, FTE markedly reduced the final body weight with a decrease in epididymal adipose tissue mass and adipocyte size compared with the untreated HFD-induced group. Additionally, FTE ameliorated serum total cholesterol, triglyceride, and low-density lipoprotein cholesterol levels. The results show that Tartary buckwheat possesses hypocholesterolemic effect through downregulating lipid metabolism. Further studies are required in this area to strengthen the anti-obesity effects of FTE with active component, and it can be used a pro-drug instead of whole extract.

Determination of Novel Synthetic 5HT2C Agonist KOPC20010 by Gas-Chromatography/Mass Spectrometry and its Bioavailability in Sprague-Dawley Rats

  • Im, Hye-Yeon;Pae, Ae-Nim;Yang, Ha-Yun;Park, Woo-Kyu;Seo, Ji-Eun;Haque, Md. Mamunul;Kwon, Oh-Seung
    • Journal of Pharmaceutical Investigation
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    • v.41 no.1
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    • pp.31-36
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    • 2011
  • $5HT_{2C}$ receptor among fourteen 5-HT subtypes plays important roles in several disorders such as depression, anxiety, epilepsy, schizophrenia and sleep disorders. The purpose of the study is to investigate pharmacokinetic parameters and bioavailability of a newly synthesized selective agonist of $5-HT_{2C}$ receptor, KOPC-20010 (KP10) in rats after intravenous and oral administration for the development of therapeutic anti-obesity agents. KP10 was administered orally (40 mg/kg) or intravenously (20 mg/kg), blood was collected via a catheter, and analyzed by GC/MSD. The calibration curve of KP10 in plasma and urine showed high linearity ($r^2$ >0.999). The retention times of KP10 in plasma and urine were 8.7 and 9.7 min, respectively. After oral administration of 40 mg/kg, pharmacokinetic parameters were calculated as follows; $C_{max}$ value was $1242.9{\pm}1195.5$ ng/mL at $1.1{\pm}0.6$ hr ($T_{max}$). $AUC_{0->24hr}$ and $AUC_{0>{\infty}}$ were $8034.2{\pm}960.7$ and $10464.1{\pm}681.5\;ng{\cdot}hr/mL$, respectively. The terminal half-life was $21.9{\pm}7.6$ hr. $AUC_{0->24hr}$ and $AUC_{0>{\infty}}$ were $4292.4{\pm}523.0$ and $6111.2{\pm}756.2\;ng{\cdot}hr/mL$, respectively, after 20 mg/kg of intravenous administration. The terminal half-life after intravenous administration was $25.1{\pm}9.4$ hr. Bioavailability of KP10 was determined to 86%. The excretion amount into the urine within 48 hr was approximately 4.7 to 6.7% of the dose administered. These data may be beneficial to the anti-obesity drug development of KP10.

Effects of Gami-Handayeolso-Tang on Body Fat Reduction in High Fat Diet-Fed Obese Mice (가미한다열소탕(加味寒多熱少湯)이 고지방식이 비만생쥐의 체지방감소에 미치는 영향)

  • Lee, Ha-Il;Lee, Jong-Ha;Kwon, Young-Mi;Song, Yung-Sun
    • Journal of Korean Medicine Rehabilitation
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    • v.26 no.1
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    • pp.13-31
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    • 2016
  • Objectives In this study, it was investigated whether Gami-Handayeolso-Tang (HDYST) medication has anti-obesity effects in high fat diet (HFD)-fed obese mice. Methods The experimental animals were divided into five groups-normal diet-fed (ND), high fat diet-fed control (HFD), HFD+HDYST 150, HFD+HDYST 300, and HFD+orlistat as a positive drug. The obese markers such as body weight, diet efficiency ratio, serum levels of total cholesterol, triglyceride, lipid contents, leptin, adiponectin, and GOT/GPT were measured. Also, white adipose tissue, liver weight, abdominal fat mass, hepatic lipid contents, and mRNA expression of obese-associating genes were examined in obese mice. Results In high fat diet-fed mice, HDYST administration significantly decreased body weight, diet efficiency ratio, serum levels of total cholesterol, triglyceride, LDL-cholesterol, as well as leptin and GOT/GPT, compared to the HFD group in a dose-dependent manner. HDYST increased significantly the serum levels of HDL-cholesterol and adiponectin. It also reduced the accumulation of lipids, such as total lipid and triglycerides, in organs such as liver and abdominal adipose tissue. Moreover, HDYST administration significantly decreased the expression levels of fatty acid synthetic genes, such as sterol regulatory element-binding protein-1c (SREBP-1c), FAS and Stearoyl-Coenzyme A desaturase 1 (SCD-1), in the liver tissues, while it increased the messenger RAN (mRNA) levels of fatty acid catalytic genes, such as Peroxisome proliferator activated receptor alpha (PPAR-${\alpha}$), acyl-COA oxidase (ACO), and Carnitine palmitoyltransferase-1a (CPT-1a). Conclusions Based on the results above, HDYST reveals anti-obesity effects declining body fat accumulation through the regulation of fatty acid metabolism and leptin/adiponectin serum levels. It therefore suggests that HDYST can be clinically useful for the treatment of obesity.

The Effects of Whole Body Vibration in the Aspect of Reducing Abdominal Adipose Tissue in High-Fat Diet Mice Model (고지방 식이 섭취 소동물 모델을 활용한 전신진동 자극의 복부 지방 감소 효능 평가)

  • Hwang, Donghyun;Kim, Seohyun;Lee, Hana;lee, Sangyeob;Seo, Donghyun;Cho, Seungkwan;Chen, Seulgi;Han, Taeyoung;Kim, Han Sung
    • Journal of Biomedical Engineering Research
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    • v.38 no.1
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    • pp.49-55
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    • 2017
  • The prevalence of obesity has noticeably increased worldwide over several decades with various complication. Even though anti-obesity drug treatments have been spotlighted by resulting in effective mean weight losses, its adverse effects cannot be overlooked. Thus, this study aimed to evaluate the effects of multi-frequency whole body vibration, one of the mechanical stimulus, as a countermeasure against obesity. Thirty-two-6-week-old C57BL/6J male mice were equally assigned to four groups: the Control group (CON, n = 8), the Sham group (Sham, n = 8), the sham with single frequency whole body vibration (S+V, n = 8), and the sham with multi frequency whole body vibration (S+MV, n = 8). After 4 weeks, morphologic changes in the adipose tissue were evaluated from three-dimensional images using in vivo micro-computed tomography. At 4 weeks, the volume of the abdominal adipose tissue, which had the highest value in Sham group, noticeably reduced in S+MV group compared to it in S+V group. These results implied that the accumulation of abdominal adipose tissue can be effectively reduced through applying multi-frequency whole body vibration.