• Title/Summary/Keyword: Anti-diabetic drugs

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$^{18}F$-FDG Colonic Uptake by Oral Anti-Diabetic Drugs Including Metfomin in PET/CT Scan (PET/CT 검사에서 Metformin 성분의 항 당뇨약제에 의한 대장에서의 $^{18}F$-FDG 섭취에 관한 연구)

  • Kim, Sang-Gyu;Park, Hoon-Hee;Kim, Jung-Yul;Bahn, Young-Kag;Lim, Han-Sang;Kim, Jae-Sam;Lee, Chang-Ho
    • The Korean Journal of Nuclear Medicine Technology
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    • v.14 no.2
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    • pp.50-54
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    • 2010
  • Purpose: The uptake of $^{18}F$-FDG is often observed in normal cell of colon to patients who have non-insulin-dependent diabetes mellitus and had taken anti-diabetic drugs including Metformin in PET/CT scan. In this study, the region of colon was compared between the patients who took anti-diabetic drugs including Metfomin and other patients who took the other anti-diabetic drugs through SUV measurements. Materials and Methods: A hundred eighty patients were studied. 120 patients who have non-insulin-dependent diabetes mellitus (Including Metformin: 60, Excluding Metformin: 60) and 60 patients as a control group were composed. The patient fasted at least 6 hours before receiving an intravenous injection of 370-592 MBq (10-16 mCi) of $^{18}F$-FDG. Scanning from the base of the skull though the mid thigh was performed using the Discovery STe PET/CT Equipment (GE Healthcare, Milwaukee, WI, USA). The highest uptake region was measured SUV among ascending, transverse and descending colon. Results: The values of patients who took the anti-diabetic drugs including Metformin were $6.16{\pm}3.64$ g/mL, $4.41{\pm}2.94$ g/mL, and $5.46{\pm}2.44$ g/mL. The patients who took the anti-diabetic drugs which does not have Metformin were $3.05{\pm}1.39$ g/mL, $2.08{\pm}0.97$ g/mL and $3.15{\pm}1.85$ g/mL. The control group were $2.02{\pm}0.88$ g/mL, $1.68{\pm}0.87$ g/mL and $2.19{\pm}1.88$ g/mL. Conclusion: The effect of the intake of Metformin was observed from the SUV on region of large bowel in this study. Thus, it could be helpful for the results by identifying the ingredient of anti-diabetic drug before the examination and the possibility of interpretation of false positive will be reduced.

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15-Hydroxyprostaglandin Dehydrogenase Is Associated with the Troglitazone-Induced Promotion of Adipocyte Differentiation in Human Bone Marrow Mesenchymal Stem Cells

  • Noh, Min-Soo;Lee, Soo-Hwan
    • Biomolecules & Therapeutics
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    • v.18 no.1
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    • pp.16-23
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    • 2010
  • Adipocyte differentiation in human bone marrow mesenchymal stem cells (hBM-MSCs) is not as efficient as that in murine pre-adipocytes when induced by adipogenic agents including insulin, dexamethasone, and 3-isobutyl-1-methylxanthine (IDX condition). Therefore, the promotion of adipocyte differentiation in hBM-MSCs has been used as a cell culture model to evaluate insulin sensitivity for anti-diabetic drugs. In hBM-MSCs, $PPAR{\gamma}$ agonists or sulfonylurea anti-diabetic drugs have been added to IDX conditions to promote adipocyte differentiation. Here we show that troglitazone, a peroxisome proliferator-activated receptor-gamma ($PPAR{\gamma}$) agonist, significantly reduced the levels of anti-adipogenic $PGE_2$ in IDX-conditioned hBM-MSC culture supernatants when compared to $PGE_2$ levels in the absence of $PPAR{\gamma}$ agonist. However, there was no difference in the mRNA levels of cyclooxygenases (COXs) and the activities of COXs and prostaglandin synthases during adipocyte differentiation in hBM-MSCs with or without troglitazone. In hBM-MSCs, troglitazone significantly increased the mRNA level of 15-hydroxyprostaglandin dehydrogenase (HPGD) which can act to decrease $PGE_2$ levels in culture. These results suggest that the role of $PPAR{\gamma}$ activation in promoting adipocyte differentiation in hBM-MSCs is to reduce anti-adipogenic $PGE_2$ levels through the up-regulation of HPGD expression.

Repaglinide, but Not Nateglinide Administered Supraspinally and Spinally Exerts an Anti-Diabetic Action in D-Glucose Fed and Streptozotocin-Treated Mouse Models

  • Sim, Yun-Beom;Park, Soo-Hyun;Kang, Yu-Jung;Kim, Sung-Su;Kim, Chea-Ha;Kim, Su-Jin;Lim, Su-Min;Jung, Jun-Sub;Ryu, Ohk-Hyun;Choi, Moon-Gi;Suh, Hong-Won
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.6
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    • pp.493-497
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    • 2013
  • We have recently demonstrated that some anti-diabetic drugs such as biguanide and thizolidinediones administered centrally modulate the blood glucose level, suggesting that orally administered anti-diabetic drugs may modulate the blood glucose level by acting on central nervous system. The present study was designed to explore the possible action of another class of anti-diabetic drugs, glinidies, administered centrally on the blood glucose level in ICR mice. Mice were administered intracerebroventricularly (i.c.v.) or intrathecally (i.t.) with 5 to $30{\mu}g$ of repaglinide or nateglinide in D-glucose-fed and streptozotocin (STZ)-treated models. We found that i.c.v. or i.t. injection with repaglinide dose-dependently attenuated the blood glucose level in D-glucose-fed model, whereas i.c.v. or i.t. injection with nateglinide showed no modulatory action on the blood glucose level in D-glucose-fed model. Furthermore, the effect of repaglinide administered i.c.v. or i.t. on the blood glucose level in STZ-treated model was studied. We found that repaglinide administered i.c.v. slightly enhanced the blood glucose level in STZ-treated model. On the other hand, i.t. injection with repaglinide attenuated the blood glucose level in STZ-treated model. The plasma insulin level was enhanced by repaglinide in D-glucose-fed model, but repaglinide did not affect the plasma insulin level in STZ-treated model. In addition, nateglinide did not alter the plasma insulin level in both D-glucose-fed and STZ-treated models. These results suggest that the anti-diabetic action of repaglinide appears to be, at least, mediated via the brain and the spinal cord as revealed in both D-glucose fed and STZ-treated models.

Anti-diabetic Activity of Herbal Drugs (수종 생약의 혈당강하작용)

  • Kim, Bak-Kwang;Park, Man-Ki;Cho, Sool-Yeon;Lee, Jae-Shin;Han, Hye-Kyung;Jeong, Choon-Sik;Jung, Ki-Hwa;Park, Jeong-Hill
    • Korean Journal of Pharmacognosy
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    • v.28 no.2
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    • pp.72-74
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    • 1997
  • Antidiabetic activity of several herbal drugs, which are used as antidiabetics in folkmedicine, was evaluated. Among tested herbal drugs, extract of Astragali Radix significantly lowered blood glucose level in streptozotocin-induced diabetic model rat.

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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 $PPAR{\gamma}$.

Anti-diabetic Mechannism Study of Korean Red Ginseng by Transcriptomics (전사체 프로파일을 이용한 고려 홍삼의 항당뇨 기전 연구)

  • Yuan, Hai-Dan;Shin, En-Jung;Chung, Sung-Hyun
    • YAKHAK HOEJI
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    • v.52 no.5
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    • pp.345-354
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    • 2008
  • This study was designed to investigate the anti-diabetic effect and mechanism of Korean red ginseng extract through transcriptomics in C57BL/KsJ db/db mice. The db/db mice were randomly divided into six groups: diabetic control group (DC), red ginseng extract low dose group (RGL, 100 mg/kg), red ginseng extract high dose group (RGH, 200 mg/kg), metformin group (MET, 300 mg/kg), glipizide group (GPZ, 15 mg/kg) and pioglitazone group (PIO, 30 mg/kg), and treated with drugs once per day for 10 weeks. At the end of treatment, we measured blood glucose, insulin, hemoglobin A1c (HbA1c), triglyceride (TG), adiponectin, leptin, non-esterified fatty acid (NEFA). RGL-treated group lowered the blood glucose and HbA1c levels by 19.6% and 11.4% compared to those in diabetic control group. In addition, plasma adiponectin and leptin levels in RGL-treated groups were increased by 20% and 12%, respectively, compared to those in diabetic control. Morphological analyses of liver, pancreas and epidydimal adipose tissue were done by hematoxylin-eosin staining, and pancreatic islet insulin and glucagon levels were detected by double-immunofluorescence staining. RGL-treated group revealed higher insulin contents and lower glucagon contents compared to diabetic control. To elucidate an action mechanism of Korean red ginseng, DNA microarray analyses were performed in liver and fat tissues, and western blot and RT-PCR were conducted in liver for validation. According to hierarchical clustering and principal component analysis of gene expression Korean red ginseng treated groups were close to metformin treated group. In summary, Korean red ginseng lowered the blood glucose level through protecting destruction of islet cells and shifting glucose metabolism from hepatic glucose production to glucose utilization and improving insulin sensitivity through enhancing plasma adiponectin and leptin levels.

Anti-diabetic Effect and Mechanism of Korean Red Ginseng in C57BL/KsJ db/db Mice

  • Yuan, Hai-Dan;Shin, Eun-Jung;Chung, Sung-Hyun
    • Journal of Ginseng Research
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    • v.32 no.3
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    • pp.187-193
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    • 2008
  • The present study was designed to investigate the anti-diabetic effect and mechanism of Korean red ginseng in C57BL/KsJ db/db mice. The db/db mice were divided into three groups: diabetic control group (DC), Korean red ginseng group (KRG, 100 mg/kg) and metformin group (MET, 300 mg/kg), and treated with drugs once per day for 10 weeks. Compared to the DC group, fasting blood glucose levels were decreased by 19.8% in KRG-, 67.7% in MET-treated group. With decreased plasma glucose and insulin levels, the insulin resistance index of the KRG-treated group was reduced by 27.6% compared to the DC group. The HbA1c levels in KRG and MET-treated groups were also decreased by 11.0% and 18.9% compared to that of DC group, respectively. Plasma triglyceride and non-esterified fatty acid levels were decreased by 18.8% and 16.8%, respectively, and plasma adiponectin and leptin levels were increased by 20.6% and 12.1%, respectively, in the KRG-treated group compared to those in DC group. Histological analyses of the liver and fat tissue of mice treated with KRG revealed significantly decreased number of lipid droplets and decreased size of adipocytes compared to the DC group. From the pancreatic islet double-immunofluorescence staining, we observed KRG has increased insulin contents, but decreased glucagon production. To elucidate action mechanism of KRG, effects on AMP-activated protein kinase (AMPK) and its downstream target proteins responsible for fatty acid oxidation and gluconeogenesis were explored in the liver. KRG activated AMPK and acetyl-coA carboxylase (ACC) phosphorylations, resulting in stimulation of fatty acid oxidation. KRG also caused to down regulation of SREBP1a and its target gene expressions such as FAS, SCD1 and GPAT. In summary, our results suggest that KRG exerted the anti-diabetic effect through AMPK activation in the liver of db/db mice.

Inhibitory effects of extract from the Schizandra chinensis on rat small intestinal ${\alpha}-amylase$ activity and postprandial blood glucose

  • Chae, Hee-Jin;Heo, Ye-Na;Moon, Hae-Yeon
    • 한국생물공학회:학술대회논문집
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    • 2005.10a
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    • pp.821-826
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    • 2005
  • Postprandial hyperglycemia plays an important role in the development of type 2 diabetes and complications associated with the disease such micro-and macro-vascular disease. The present study investigated the effect and action mechanism of a ethanolic extract from the Schizandra chinensis(SC-E) on hypeglycemia in vivo and in vitro. In vitro, SE-E demonstrated a potent inhibitory effects on ${\alpha}-amylase$ activity ($IC_{50}$ : 4 ${\mu}g/ml$). Its inhibition on ${\alpha}-amylase$ was determined to be competitive type. Oral administration of SE-E markedly lowered plasma glucose levels in non-fasted streptozotocin induced diabetic rats (45 mg/kg BW). In addition when it was orally administrated to rats with starch (2g/kg BW), SC-E (50 and 100 mg/kg BW) significantly suppressed the increase of blood glucose levels after starch loading . These results suggest that some edible plants merit further evaluation for clinical usefulness as anti-diabetic drugs.

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Studies on the Efficacy of Combined Preparation of Crude Drugs (XIII) -Effects of ‘Daeshiho-Tang’ on the Blood Vessels, Activities of the Liver Enzyme, Biliary Secretory and Anti-Diabetic Actions- (생약복합제제(生藥複合製劑)의 약효연구(藥效硏究) 제13보(第13報) -대시호탕(大柴胡湯)이 혈관(血管), 간독성(肝毒性), 이담(利膽) 및 항당뇨효과(抗糖尿效果)에 대(對)하여-)

  • Hong, N.D.;Chang, I.K.;Kim, N.J.;Shon, J.G.
    • Korean Journal of Pharmacognosy
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    • v.14 no.1
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    • pp.30-38
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    • 1983
  • These studies were conducted in an attempt to investigate effects of 'Daeshiho-Tang' on the blood vessels, activities of liver enzyme and excretory action of bile juice in serum of $CCl_4-intoxicated$ rabbits, glucose and total cholesterol levels in serum of alloxan-induced diabetic rabbits. The result of these studies were summarized as follows; 1. Hypotensive ind vaso-dilatating actions due to vascular smooth muscle relaxation were noted in frogs, rabbits and dogs. 2. GOT, GPT and total cholesterol in serum of $CCl_4-intoxicated$ rabbits showed significant depressive effects. 3. Significantly increased biliary secretary effect was noted in $CCl_4-intoxicated$ rabbits. 4. Glucose and total cholesterol levels showed markedly decraese in alloxan-induced diabetic rabbits. Considering the experimental studies results, it is suggested that 'Daeshiho-Tang' has therapeutic efficacy to treat febrile diseses and metabolic diseases.

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Anti-diabetic efficacy of the alcoholic extracts in Ganoderma sp. and Phellinus Baumi (영지, 상황버섯 주정추출물의 항당뇨 효능)

  • Cho, Jae-Han;Park, Hye-Sung;Han, Jae-Gu;Lee, Kang-Hyo;Jhune, Chang-Sung
    • Journal of Mushroom
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    • v.13 no.4
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    • pp.326-329
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    • 2015
  • This study was carried out to anti-diabetic efficacy of alcoholic extracts in Ganoderma species and Phellinus Baumi. Ganoderma species and Phellinus Baumi. showed inhibitory activity of PTP1B, which acts as negative regulator of diabetes. The ${\alpha}-amylase$ is an important enzyme in the digestion of carbohydrates in the saliva and pancreatic. If inhibition of the enzyme Delaying the digestion rate of the carbohydrate can be reduced postprandial rise in blood glucose levels. The results of the tests the active level that showed a similar inhibition ${\alpha}-amylase$ inhibitory activity and a positive control. Phellinus Baumi. showed the inhibitory activity to 89%, Acarbose as positive control. ${\alpha}-glucosidase$ is an essential enzyme in the digestion and absorption of carbohydrates that break down carbohydrates into simple sugars polysaccharides. The results of the tests the active level that showed a low inhibitory activity. It is thought to be able to complement the shortcomings of conventional anti-diabetic drugs.