• Title/Summary/Keyword: Acarbose

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Antidiabetic Activity of Mori Folium Ethanol Soluble Fraction in db/db mice (db/db 마우스에서 상엽 에탄올가용분획의 항당뇨활성)

  • Ryu, Jeong-Wha;Seo, Seong-Hoon;Chung, Sung-Hyun
    • YAKHAK HOEJI
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    • v.42 no.6
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    • pp.613-620
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    • 1998
  • Antidiabetic activity of Mori folium ethanol soluble fraction (MFESF) was examined in db/db mice, which is a spontaneously hyperglycemic, hyperinsulinemic and obese animal model . 500 and 1000mg/kg dose for MFFSF (designated by SY 500 and SY 1000, respectively) and 5mg/kg dose for acarbose were administered for 6 weeks. Body weight gain, fasting and non-fasting serum glucose, glycated hemoglobin and triglyceride were all reduced dose dependently when compared between db/db control group and MFESF treated group. At 11th and 13th week after birth, MFESF increased an insulin secretion which may result in lowering serum glucose level. Total activities of sucrase and maltase in SY 500 treated group were decreased when compared to db/db control. On the other hand, those in SY 1000 and acarbose treated groups were increased. This result may suggest that proteins for sucrase and maltase were compensatorily induced due to significant inhibition of glycosidase-catalyzed reaction at doses administered in this study.

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Blood Glucose Lowering Activity and Mechanism of Sangbackpitang (SBPT) in db/db Mouse (db/db 마우스에서 상백피탕의 혈당강하 활성 및 기전연구)

  • 이성현;안세영;두호경;정성현
    • YAKHAK HOEJI
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    • v.43 no.6
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    • pp.818-826
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    • 1999
  • Antidiabetic activity and mechanism of Sangbackpitang (SBPT) was examined in db/db mice, which is a spontaneously hyperglycemic, hyperinsulinemic and obese animal model. SBPT and acarbose were administered orally for 4 weeks. Fasting and non-fasting serum glucose, glycated hemoglobin and triglyceride were all reduced when compared between db/db control group and SBPT treated group. At 12th week after birth, SBPT increased an insulin secretion although statistic significance was not seen. Total activities of sucrase, maltase and lactase in SBPT treated group were all decreased when compared to db/db control. On the other hand, sucrase and maltase activities in acarbose treated groups were increased. Effect of SBPT on mRNA expression of glucose transporter(GLUT-4) was also examined. Quantitation of glucose transporter was performed by RT-PCR and in vitro transcription with co-amplification of rat-action gene as an internal standard. Muscular GLUT-4 mRNA expression in SBPT treated group was increased significantly. These results may suggest that SBPT lowered blood glucose ascribing to inhibition of glycosidase-catalyzed reaction and upregulation of muscular GLUT-4 mRNA expression.

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Study on Anti-obesity and Hypoglycemic Effects of Lycium chinense Mill Extracts (구기자 추출물의 항비만 및 혈당강하 효과)

  • Hwang, Eun-Young;Hong, Jung-Hee;Choi, Jun-Hyeok;Choi, Eun-Jung;Lee, In-Seon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.11
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    • pp.1528-1534
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    • 2009
  • This study was designed to evaluate the anti-obesity and hypoglycemic effects of Gugija (Lycium chinense Mill) extracts in 3T3-L1 adipocytes. We investigated the $\alpha$-amylase and $\alpha$-glucosidase inhibitory activities of extracts from Gugija. Gugija was extracted by 70% EtOH and 80% MeOH and aqueous, respectively. A single oral dose of Gugija extract inhibited the increase of blood glucose levels significantly at 0, 30, 60, 90 and 120 min and decreased incremental response areas under the glycemic response curve. These results suggest that Gugija 70% EtOH extracts may delay carbohydrate digestion and reduce postprandial hyperglycemia. In addition, triglyceride content in 3T3-L1 adipocytes decreased at higher concentrations of Gugija 70% EtOH extract. Free fatty acid content in 3T3-L1 adipocytes was increased at higher concentrations of Gugija 70% EtOH extract. Also, glucose transporter 4 (GLUT4), the key insulin signaling pathway transcription factor, was remarkably increased by the Gugija 70% EtOH extract when compared to those of control cells in protein expression levels. Therefore, Gugija can be developed as an effective anti-obesity and hypoglycemic agent.

The Effects of Supungsunki-hwan on High Fat, High Carbohydrate Diet-induced Obese Type 2 Diabetic Mouse Model (수풍순기환 투여가 고지방, 고탄수화물 식이로 유발된 비만형 제2형 당뇨병 동물모델에 미치는 영향)

  • Park, Jong-Seol;Lee, Byung-Cheol;Doo, Ho-Kyung;Ahn, Young-Min;Ahn, Se-Young
    • The Journal of Internal Korean Medicine
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    • v.30 no.2
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    • pp.257-269
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    • 2009
  • Objective : Obesity is an important cause of diabetes, and lipotoxicity causes insulin resistance. Recently a lot of research is being done on PPAR-${\alpha}$. TNF-${\alpha}$. adiponectin, and leptin, which are important obesity related factors. In this study, we investigated the effects of Supungsunki-hwan on high fat. high carbohydrate diet-induced obese type 2 diabetic mouse models. Methods: Diabetes was induced in ICR male mouse (30${\pm}$5g) with Surwit's high fat, high sucrose diet. Mice were divided into 4 groups(n=10) of Normal. Control. Supungsunkj-hwan group. and acarbose group. The Supungsunki-hwsn group was given 10% Supungsunkj-hwan in their diet. and the acarbose group was given 0.5% acarbose in their diet. After 6 weeks. body weight. food intake, FBS and OGTT. lipid profile and liver enzymes, epididymal fat weight, and gene expression of leptin, adiponectin, TNF-${\alpha}$ and PPAR-${\alpha}$ were measured. Leptin. adiponectin. tumor necrosis factor(TNF)-${\alpha}$ and peroxisome proliferator-activated receptor (PPAR)-${\alpha}$ were evaluated by reverse transcription-polymerase chain reaction. Results : Supungsunkj-hwan increased the gene expression of PPAR-${\alpha}$, which reduces lipotoxicity and insulin resistance. Supungsunkj-hwan also significantly reduced triglyceride. AST. ALT serum levels. and 1 hour oral glucose tolerance levels. Conclusion : These results show that Supungsunkj-hwan improves insulin resistance in the liver and muscles, by reducing triglyceride levels and lipotoxicity through increased PPAR-${\alpha}$ gene expression. This is supported by the fact that Supungsunkj-hwan significantly reduces 1 hour oral glucose tolerance levels. Therefore we suggest that Supungsunkj-hwan would be an effective treatment for obese type 2 diabetic patients.

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Portulaca oleracea L. Extract Lowers Postprandial Hyperglycemia by Inhibiting Carbohydrate-digesting Enzymes (쇠비름(Portulaca oleracea L.) 추출물의 탄수화물 소화 효소 저해와 식후 고혈당 완화 효과)

  • Park, Jae-Eun;Han, Ji-Sook
    • Journal of Life Science
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    • v.28 no.4
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    • pp.421-428
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    • 2018
  • Postprandial hyperglycemia plays an important role in the development of Type 2 Diabetes and diabetic complications. Controlling postprandial hyperglycemia is the most important factor for reducing the risks of diabetic complications in Type 2 diabetic patients. This study was designed to determine whether Portulaca oleracea L. extract suppresses the activation of carbohydrate-digesting enzymes, and lowers postprandial hyperglycemia in diabetic mice through streptozotocin. P. oleracea was extracted with either 80% ethanol (PEE) or water (PWE), and the extract solutions were concentrated. The ${\alpha}$-glucosidase and ${\alpha}$-amylase inhibition assays were performed using the chromogenic method. Normal mice and STZ-induced diabetic mice were orally treated with PEE, PWE (300 mg/kg of body weight) or acarbose (100 mg/kg of body weight), with soluble starch (2 g/kg of body weight). The ${\alpha}$-glucosidase and ${\alpha}$-amylase inhibitory effectiveness by PEE were markedly more effective than PWE, and both extracts indicated a higher effectiveness than the acarbose (positive control). The rise in postprandial blood glucose due to starch loading was markedly inhibited in the PEE group when compared to the control group in diabetic and normal mice. Furthermore, the area under the concentration-time curve values were markedly declined by the PEE injection in the diabetic group when compared to that exerted for the control group. These results demonstrate that P. oleracea extracts lower postprandial hyperglycemia by inhibiting carbohydrate-digesting enzymes, and that the ethanol extract is more efficacious than the water extract.

Clinical Use of Oral Hypoglycemic Agents (경구혈당강하제의 사용법)

  • Lee, Tai-Hee
    • The Journal of the Korean life insurance medical association
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    • v.17
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    • pp.21-30
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    • 1998
  • 인슐린의존형당뇨병 환자의 혈당조절의 방법으로 먼저 식이요법과 운동이 권장되며, 이러한 방법으로 혈당조절이 만족스럽지 않을 때 경구혈당강하제를 사용하는 것은 혈당조절과 합병증 예방에 중요한 역할을 할 수 있다. 국내에서는 경구혈당강하제로 설폰요소제, 비구아나이드제인 메트포르민(metformin) 및 알파글루코시다제(${\alpha}$-glucosidase) 억제제인 아카보스(acarbose) 등이 사용되고 있다. 새로 개발중인 트로글리타존, 지방산 산화 억제제 등의 약제는 아직 임상에서 널리 사용되고 있지는 않다.

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$\alpha$-Glucosidase and $\alpha$-Amylase Inhibitory Activity of Compounds from Roots Extract of Pueraria thunbergiana (갈근에서 분리한 화합물의 $\alpha$-glucosidase와 $\alpha$-amylase 활성 저해 효과)

  • Park, Jee-Hee;Baek, Mok-Ryeon;Lee, Byung-Hoi;Yon, Gyu-Hwan;Ryu, Shi-Yong;Kim, Young-Sup;Park, Sang-Un;Hong, Kyung-Sik
    • Korean Journal of Medicinal Crop Science
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    • v.17 no.5
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    • pp.357-362
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    • 2009
  • Compounds of isolated from roots extract of Pueraria thunbergiana were tested their inhibitory effects on $\alpha$-glucosidase and $\alpha$-amylase. Inhibitory activity of methylene chloride (MC) fraction and ethyl acetate (EA) fraction against $\alpha$-glucosidase showed more than 60% at a concentration of $500{\mu}g/m{\ell}$. Among the nine compounds tested on $\alpha$-glucosidase, biochanin A, (-)-tuberosin and calycosin from MC fraction and daidzein from EA fraction were stronger inhibitors than acarbose ($IC_{50}=530{\mu}g/m{\ell}$), and their $IC_{50}$ were 9, 144, 328 and $20{\mu}g/m{\ell}$, respectively. Biochanin A and (-)-tuberosin also inhibited $\alpha$-amylase activity as like as acarbose $IC_{50}=20.5{\mu}g/m{\ell}$), and their $IC_{50}$ were 22 and $348{\mu}g/m{\ell}$, respectively. Although daidzein was already known $\alpha$-glucosidase inhibitory effects, it was newly evaluated that biochanin A and (-)-tuberosin inhibited $\alpha$-glucosidase as well as $\alpha$-amylase, and that calycosin did $\alpha$-glucosidase.

Increased glucose metabolism and alpha-glucosidase inhibition in Cordyceps militaris water extract-treated HepG2 cells

  • Kim, Dae Jung;Kang, Yun Hwan;Kim, Kyoung Kon;Kim, Tae Woo;Park, Jae Bong;Choe, Myeon
    • Nutrition Research and Practice
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    • v.11 no.3
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    • pp.180-189
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    • 2017
  • BACKGROUND/OBJECTIVES: Recent living condition improvements, changes in dietary habits, and reductions in physical activity are contributing to an increase in metabolic syndrome symptoms including diabetes and obesity. Through such societal developments, humankind is continuously exposed to metabolic diseases such as diabetes, and the number of the victims is increasing. This study investigated Cordyceps militaris water extract (CMW)-induced glucose uptake in HepG2 cells and the effect of CMW treatment on glucose metabolism. MATERIALS/METHODS: Colorimetric assay kits were used to determine the glucokinase (GK) and pyruvate dehydrogenase (PDH) activities, glucose uptake, and glycogen content. Either RT-PCR or western blot analysis was performed for quantitation of glucose transporter 2 (GLUT2), hepatocyte nuclear factor 1 alpha ($HNF-1{\alpha}$), phosphatidylinositol 3-kinase (PI3k), protein kinase B (Akt), phosphorylated AMP-activated protein kinase (pAMPK), phosphoenolpyruvate carboxykinase, GK, PDH, and glycogen synthase kinase 3 beta ($GSK-3{\beta}$) expression levels. The ${\alpha}-glucosidase$ inhibitory activities of acarbose and CMW were evaluated by absorbance measurement. RESULTS: CMW induced glucose uptake in HepG2 cells by increasing GLUT2 through $HNF-1{\alpha}$ expression stimulation. Glucose in the cells increased the CMW-induced phosphorylation of AMPK. In turn, glycolysis was stimulated, and glyconeogenesis was inhibited. Furthermore, by studying the mechanism of action of PI3k, Akt, and $GSK-3{\beta}$, and measuring glycogen content, the study confirmed that the glucose was stored in the liver as glycogen. Finally, CMW resulted in a higher level of ${\alpha}-glucosidase$ inhibitory activity than that from acarbose. CONCLUSION: CMW induced the uptake of glucose into HepG2 cells, as well, it induced metabolism of the absorbed glucose. It is concluded that CMW is a candidate or potential use in diabetes prevention and treatment.

Study of Effects and Optimum Concentrations of Medical Herb Extracts on Blood Glucose and Serum Lipid in Streptozotocin-Induced Diabetic Rats (Streptozotocin 유발 당뇨 쥐의 혈당 및 혈청 지질에 미치는 한방추출물의 효과와 최적 농도에 관한 연구)

  • Chong, Myong-Soo;Kim, Hae-Ja;Cho, Hwa-Eun;Choi, Yun-Hee;Lee, Kin-Am
    • The Journal of Korean Medicine
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    • v.29 no.1
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    • pp.85-94
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    • 2008
  • Objectives : The purpose of this study was to investigate effects of extract from mixed culture with Tricholoma matsutake mycelium and Cordyceps militaris mycelium in oriental medicine and cereal midium (OCM) considered effective for the treatment of diabetes. Methods : We examined antioxidant activity and $\alpha$-glucosidase inhibit activity of OCM and orally administered OCM extracts to Streptozotocin-induced diabetic ratsat the dose of 100mg/kg, 200mg/kg and 300mg/kg body weight. Results : Total polyphenol content of extracts of OCM was 26.41 mg/g, DPPH radical scavenging activity was 32.24% and SOD-like activity was 31.43%. $\alpha$-glucosidase inhibit activity showed 85.3% of acarbose. Blood glucose levels of the OCM extracts-treated groups were lower than those of the diabetic control group (DC), total cholesterol and triglyceride contents were similar to the acarbose-treated group (PC) and ALT, AST were lower than the DC and PC groups. The 300 mg/kg body weight administered group (UM-300) were superior to other OCM-treated groups (UM-100, UM-200). Conclusions : These results showed extract from mixed culture with Tricholoma matsutake mycelium and Cordyceps militaris mycelium in oriental medicine and cereal midium has potentiality to beused in pharmaceutical products and medicinal food for preventive and treatment diabetes mellitus.

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Role of Dipeptide at Extra Sugar-Binding Space of Thermus Maltogenic Amylase in Transglycosylation Activity

  • Baek, Jin-Sook;Kim, Tae-Jip;Kim, Young-Wan;Cha, Hyun-Ju;Kim, Jung-Wan;Kim, Yong-Ro;Lee, Sung-Joon;Moon, Tae-Wha;Park, Kwan-Hwa
    • Journal of Microbiology and Biotechnology
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    • v.13 no.6
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    • pp.969-975
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    • 2003
  • Two conserved amino acid residues in the extra sugar-binding space near the catalytic site of Thermus maltogenic amylase (ThMA) were analyzed for their role in the hydrolysis and transglycosylation activity of the enzyme. Site-directed mutagenesis was carried out by replacing N33l with a lysine (N331K), E332 with a histidine (E332H), or by replacing both residues at the same time (N331K/E332H). The measured $K_m$ values indicated that affinities toward all substrates tested, including starch, pullulan, ${\beta}-cyclomaltodextrin$, and acarbose, were lower in all the mutants compared to that of wild-type ThMA, leading to reduced hydrolysis activity. In addition, the lower ratio of transglycosylation to hydrolysis in the mutants compared to that in the wild-type ThMA indicated that these mutants preferred hydrolysis to the transglycosylation reaction. These results demonstrated that the conserved dipeptide at 331 and 332 of ThMA is directly involved in the formation and accumulation of transfer products by accommodating acceptor sugar molecules.