• 약학회지
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• 제42권6호
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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.

• 약학회지
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• 제43권6호
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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.

• 한국식품영양과학회지
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• 제38권11호
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• pp.1528-1534
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• 2009

구기자는 식용가능하고 제2형 당뇨병 합병증인 지방간분해, 고혈압 및 고혈당에 효능이 있다고 알려져 있다. 하지만 당 대사 및 지질 대사에 작용하는 정확한 기작에 대한 연구는 아직 미비하기에 탄수화물 소화효소인 ${\alpha}$-amylase와 ${\alpha}$-glucosidase의 저해활성 및 정상생쥐를 이용한 혈당강하 효과와 3T3-L1 adipocyte를 통하여 비만축적 억제효과를 보았다. 구기자 추출은 80% MeOH, 70% EtOH 및 열수추출하였으며 이들 중 ${\alpha}$-amylase 50% 저해 활성($IC_{50}$)은 saliva ${\alpha}$-amylase에서 acarbose, 80% MeOH, 70% EtOH, aqueous(7.04, 3.19, 3.20, 3.66 mg/mL), pacreas ${\alpha}$-amylase acarbose, 80% MeOH, 70% EtOH, aqueous(10.97, 4.16, 3.07, 3.55 mg/mL)로 saliva ${\alpha}$-amylase에선 acarbose보다 80% MeOH, 70% EtOH 추출물이 가장 낮은 농도에서 $IC_{50}$값을 나타냈고 pacreas ${\alpha}$-amylase에서는 70% EtOH 추출물이 가장 낮은 농도에서 $IC_{50}$값을 나타냈다. 또한 10 ${\mu}g/mL$ 농도에서 yeast ${\alpha}$-glucosidase 활성저해 $IC_{50}$값은 80% MeOH, 70% EtOH, aqueous(5.01, 4.98, 4.80 ${\mu}g/mL$)로 구기자 추출물 모두 acarbose(5.05)보다 우수한 $IC_{50}$값을 나타냈다. 정상생쥐에게 탄수화물 소화효소의 저해활성이 높은 70% EtOH 추출물을 전분과 함께 경구투여 한 후 내당능을 측정한 결과, 전분과 함께 100, 200 mg/kg body weight를 경구투여 한 경우, 대조군에 비해 투여 후 30, 60, 90, 120분에 혈당 증가가 낮았다. 또한 추출물을 100 mg보다 200 mg 투여하였을 경우 대조군에 비해 각각 19% 및 40%씩 저하되었으며, 120분에는 대조군 수준이 되었다. 그리고 3T3-L1 adipocyte에서 비만축적 억제효과를 측정한 결과 70% EtOH 추출물 농도가 증가함에 따라 leptin, 중성지방 농도가 감소하였고 유리지방산 농도는 증가하였다. 이상의 연구 결과 구기자 추출물 중 70% EtOH는 acarbose보다 높은 ${\alpha}$-glucosidase, ${\alpha}$-amylase 저해활성을 나타냈으며, 정상생쥐를 통해 식후 혈당증가를 저하시키는 효과를 확인하였고 GLUT4 발현 역시 증가함을 확인했다. 이를 통해 구기자 추출물이 지방축적 억제와 인슐린 저항성 억제 및 혈당강하 기전을 확인하여 제2형 당뇨병 개선에 효과적인 것으로 판단, 추후 더 연구하여 보다 더 정확한 성분을 조사할 필요성이 있다고 사료된다.

• 대한한방내과학회지
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• 제30권2호
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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.

• 생명과학회지
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• 제28권4호
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• pp.421-428
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• 2018

식후고혈당은 제 2형 당뇨병의 발병에 부정적인 영향을 미치고 미세혈관 및 대혈관 질환 등의 당뇨병 합병증 유발과 밀접한 관계가 있다. 따라서 식후고혈당을 조절하는 것이 당뇨병 합병증의 위험을 줄이는 가장 중요한 요소이다. 식후고혈당은 소장에서 ${\alpha}$-글루코시다아제와 같은 탄수화물 소화 효소를 저해함으로써 조절될 수 있다. 이에 본 연구는 쇠비름 에탄올 추출물(PEE)과 물 추출물(PWE)이 탄수화물 소화 효소를 저해하고, 당뇨병 마우스에서 식후 고혈당을 강하시키는 효과에 대해 조사하였다. ${\alpha}$-글루코시다아제와 ${\alpha}$-아밀라아제에 대한 저해효과는 두 추출물 모두 양성대조군인 acarbose보다 더 효과적이었으며, PEE에 의한 ${\alpha}$-글루코시다아제 저해 효과가 PWE 보다 더 효과적이었다. Diabetic mice에 전분(2 g/kg)을 투여한 후의 혈당 증가는 30, 60, 120분에 각각 383.7, 429.3, 360.2 mg/dL로 나타났고, 전분(2 g/kg)과 PEE 또는 PWE 추출물(300 mg/Kg)을 투여한 후의 혈당 증가는 30, 60, 120분에 각각 337.0, 368.5, 290.1 mg/dL과 365.8, 379.2, 324.3 mg/dL로 나타나, PEE 추출물 투여군이 대조군에 비해 식후 혈당 강하가 효과적으로 나타남을 알 수 있었다. 이러한 결과는 쇠비름 추출물이 탄수화물 소화효소를 저해함으로써 식후 고혈당을 완화시키고, 특히 쇠비름 에탄올 추출물(PEE)이 쇠비름 물 추출물(PWE) 보다 식후 고혈당을 완화시키는데 더욱 효과가 있는 것으로 나타났다.

• 보험의학회지
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• 제17권
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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.

• 한국약용작물학회지
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• 제17권5호
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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.

• Nutrition Research and Practice
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• 제11권3호
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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.

• 대한한의학회지
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• 제29권1호
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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.

• Journal of Microbiology and Biotechnology
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• 제13권6호
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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.