• 한국미생물·생명공학회지
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• 제45권4호
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• pp.311-315
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• 2017

화살나무 가지로부터 activity based fractionation에 의해 ${\alpha}$-glucosidase 저해 활성 물질 compound 1-4을 분리하였고, $^1H$ NMR, $^{13}C$ NMR, $^1H-^1H$ COSY와 HMBC 등의 spectral data에 의해 구조를 결정하였다. Compound 1-4는 모두 flavonol 물질로 ${\alpha}$-glucosidase에 대해 $IC_{50}$ 값이 각각 25.3, 17.1, 47.3과 $35.1{\mu}M$로 positive control로 사용한 acarbose 보다 강한 활성을 나타내었다. 화살나무의 혈당 저하 기능의 유효성분으로 처음 동정된 Compound 1-4는 ${\alpha}$-glucosidase에만 특이적 활성을 갖는 물질로 당뇨병 치료제로의 개발 가능성이 높은 물질로 사료된다.

• 동의생리병리학회지
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• 제18권1호
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• pp.58-62
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• 2004

The effects of herbal medicine on type 2 diabetic animal model were investigated. Herbal medicine were composed with the addition of Coicis Semen into Okchun-san (OCS). Commelinae Herba into Gangsim-tang (GST). Scrophulariae Radix into Hyunsamsunki-san (HSK). and Erythrinae Cortex into Yukmijihuang-hwan (YMH). We evaluated anti-hyperglycemic and body weight reduction activity in diabetic db/db mice. The experimental animals were divided into six groups. as control group and five sample groups. Each 200mg/kg/day of OCS, GST, HSK and YMH was administered with orally for 14days long. 5mg/kg/day of acarbose was administered with orally for 14days long. On day 14, OCS-treated db/db mice had significantly lower fasting blood glucose levels compared to control group(296±25.9 versus 593±16.4mg/dl. p<0.001). During the 2 h intraperitoneal glucose tolerance test (IPGTT), all the sample groups were improved compared to control group but insignificantly. After 14days of extract treatment. body weight in control. YMH and acarbose groups were increased. but OCS. GST and HSK groups reduced. However. it did not significantly lower hemoglobin Alc(HbAlc) in blood of db/db mice. These result suggest that OCS could be effective on insulin-independent type 2 diabetes.

• 약학회지
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• 제42권6호
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• pp.589-597
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• 1998

Effects of Mori Folium Ethanol Soluble Fraction (MFESF) on mRNA expression of glucose transporters, acetyl-CoA carboxylase (ACC) and leptin were examined in db/db mice. 500 and 1000mg/kg dose for MFESF (designated by SY 500 and SY 1000, respectively) and 5mg/kg dose for acarbose were administered for 6 weeks. Quantitations of glucose transporters (GLUT-2 and GLUT-4), ACC and leptin mRNA were performed by RT-PCR and in vitro transcription with co-amplification of rat ${\beta}$-actin gene as an internal standard. Muscular GLUT-4 mRNA expression in MFESF-treated groups were increased dose dependently. On the other hand, MFESF caused the GLLT-4 and leptin mRNA expressions in adipose tissue to decrease dose dependently, which means that triglyceride synthesis in adipocytes might be decreased and consequently signals adipocytes to inhibit the synthesis and release of leptin. Hepatic ACC mRNA expression in MFESF-treated groups was also decreased. and this may result in lowering of serum triiglyceride level. In contrast, liver GLUT-2 mRNA expressions in MFESF-treated and acarbose groups were increased. Higher rate of glucose uptake into hepatocytes is known to inhibit a phosphoenolpyruvate carboxykinase (PEPCK)-catalyzed reaction, which is a rate-limiting step in gluconeogenesis.

• 생약학회지
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• 제46권2호
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• pp.105-108
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• 2015

To establish the anti-diabetic(α-glucosidase inhibitory) activity of D. lotus leaf extract, isolate and identify the constituents responsible for the activity. The methanolic extract of leaves was partitioned between water, n-butanol and ethyl acetate. Bio-assay guided fractionation, based on inhibition of ;${\alpha}$-glucosidase, allowed isolation and identification of the active components. Liquid chromatography/mass spectrometry(LC/MS), ¹ H-NMR and ¹³ C-NMR spectra analyses demonstrated that the active compound was myricetin-3-O-;${\alpha}$-L-rhamnoside(1). Compound 1 demonstrated a strong inhibition on the α-glucosidase, in vitro and ;${\alpha}$-glucosidase inhibitory value was calculated as 98.08%, when that of a reference drug, acarbose was estimated as 83.03%. The present study indicates compound 1 could be considered as an ;${\alpha}$-glucosidase inhibitor and developed as an important antidiabetes agent for type II diabetes therapy.

• Mycobiology
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• 제51권1호
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• pp.60-66
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• 2023

In this study, the α-amylase inhibitory activity, α-glucosidase inhibitory activity, pancreatic lipase inhibitory activity, and Xanthine Oxidase inhibitory activity of the fruiting body extracts of 5 varieties of Agaricus bisporus (AB) were confirmed. First, the α-amylase inhibitory activity of AB12, AB13, AB18, AB34, and AB40 methanol extracts was lower than that of acarbose, a positive control, in all concentration ranges. The α-glucosidase inhibitory activity of the AB40, AB13, and AB12 methanol extracts at the extract concentration of 1.0 mg/mL was 80.5%, 81.3%, and 78.5%, respectively, similar to that of acarbose, a positive control. The pancreatic lipase inhibitory activity of the methanol extract of Agaricus bisporus fruiting body was significantly lower than that of the positive control orlistat in the concentration range of 50~1.000 (mg/mL). The Xanthine Oxidase inhibitory activity was 0.5~8.0 mg/mL of each extract, which was significantly lower than that of the positive control allopurinol in the same concentration range. However, the Xanthine Oxidase inhibitory activity of AB13 and AB40 at 8.0 mg/mL was about 70%, which was higher than that of other mushrooms. In conclusion, five kinds of Agaricus bisporus fruiting bodies seem to have inhibitory effects on enzymes such as α-amylase, α-glucosidase, pancreatic lipase, and Xanthine Oxidase that degrade starch and protein. In particular, it has an inhibitory effect and a reduction effect on xanthine oxidase that causes gout, so it is expected that it can be developed and used as a food or health supplement with health functional properties through future research.

• 한국식품영양과학회지
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• 제40권2호
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• pp.321-326
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• 2011

본 연구는 제2형 당뇨모델 쥐에서 조각자 추출물의 항당뇨 효과를 알아보기 위해 SD계 수컷 흰쥐에 streptozotocin (STZ)을 복강주사 15분 후 nicotineamide(NA)로 복강에 재주사하여 제2형 당뇨를 유발시켰다. 그리고 당뇨대조군(DC), 당뇨 유발군+acarbose 4 mg/kg(AC), 당뇨유발군+조각자 추출물(Gleditschiae Spina ethanol extract) 50 mg/kg (GSE), 그리고 정상군(NC)으로 나누어 10주간 식이와 함께 물을 자유 급여하였다. 10주 동안 매일 식이 섭취량과 음료섭취량 및 매주 체중과 공복혈당을 측정하고, 마지막 주에 경구포도당 부하검사(OGTT)를 실시하였으며, 부검 시 혈액을 채취하여 혈장 TRAP 수준을 측정하였다. 정상군에 비해 당뇨그룹(DC, AC, GSE)의 체중 증가는 유의적으로 감소하였고, 당뇨 유발군들 간에는 유의적 차이가 없었다. 식이섭취량, 음료섭취량 및 식이이용효율은 정상군에 비해 당뇨그룹 DC, AC, GSE에서 유의적으로 높게 나타났으나, 음료섭취량은 DC에 비해 AC, GSE군에서 유의적으로 감소하였다. 정상군은 10주 동안 정상 수준 공복혈당을 나타내었고, acarbose는 8주부터 공복혈당이 유의적으로 감소하였으며, 9주까지 GSE군은 DC군보다 공복혈당은 낮았지만 유의적 차이는 보이지 않다가 마지막 10주에서는 DC군보다 공복혈당이 유의적으로 감소하였다. 경구 당부하 검사 결과에서는 포도당 투여 30분 후부터 혈당이 상승되기 시작하여 정상군보다 당뇨군들에서 유의적으로 상승하였고, 당뇨군들에서는 DC군에 비해 AC와 GSE군에서 유의적으로 혈당상승이 억제되었다. 10주간의 GSE 보충은 DC군에 비해 혈장 내총항산화(TRAP) 수준을 유의적으로 증가시키는 것으로 나타났다. 따라서 제2형 당뇨병에서 조각자 추출물을 장기간 투여한다면 혈당증가 억제에 있어 확연한 효과를 보일 것으로 생각된다. 이는 조각자 추출물의 항산화 활성과도 연관이 있을 것으로 추측되며, 향후 조각자 추출물의 혈당강하작용 효과를 가지는 물질의 분리 및 정제에 대한 연구가 이루어져야 할 것으로 사료된다.

• Preventive Nutrition and Food Science
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• 제17권1호
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• pp.8-13
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• 2012

This study was designed to investigate whether Sargassum ringgoldianum extract may inhibit ${\alpha}$-glucosidase and ${\alpha}$-amylase activities, and alleviate postprandial hyperglycemia in streptozotocin-induced diabetic mice. The $IC_{50}$ values of Sargassum ringgoldianum extract against ${\alpha}$-glucosidase and ${\alpha}$-amylase were 0.12 mg/mL and 0.18 mg/mL, respectively, which evidenced higher activities than those of acarbose. The blood glucose levels of the Sargassum ringgoldianum extract administered group were significantly lower compared to the control group in the streptozotocin-induced diabetic mice. Moreover, the area under the two-hour blood glucose response curve was significantly reduced and the absorption of dietary carbohydrates was delayed after administration of Sargassum ringgoldianum extract in the diabetic mice. Therefore, these results indicated that Sargassum ringgoldianum extract may help decrease the postprandial blood glucose level via inhibiting ${\alpha}$-glucosidase.

• 한국식품영양학회지
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• 제11권6호
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• pp.629-634
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• 1998

1-Deoxynojirimycin which is a potent intestinal ${\alpha}$-glucosidase inhibitor was purified from the culture broth by ion exchange chromatography, Sephadex LH20 column chromatography, TSK gel chromatography and HPLC respectively. Acute toxicity of 1-deoxynojirimycin, which was loaded through the oral as dose of 200mg/kg, was investigated in IRC mouse. None of the tested IRC mice were not dead and increase of body weight showed also the same results in comparison with control mice. The antimicrobial susceptibility of 20 pathogenic strains against 3 antidiabetic compounds (1-deoxynojirimycin, AO-128, acarbose) were obtained by agar dilution method. All of the three antidiabetic compounds has very weak antimicrobial activity (MIC>100$\mu\textrm{g}$/ml).

• Asian-Australasian Journal of Animal Sciences
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• 제23권5호
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• pp.672-679
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• 2010

Diabetes mellitus is a worldwide epidemic with high mortality. As concern over this disease rises, the number and value of research grants awarded by the National Research Foundation of Korea (NRF) have increased. Diabetes mellitus is classified into two groups. Type 1 diabetes requires insulin treatment, whereas type 2 diabetes, which is characterized by insulin resistance, can be treated using a variety of therapeutic approaches. Hyperglycemia is thought to be a primary factor in the onset of diabetes, although hyperlipidemia also plays a role. The major organs active in the regulation of blood glucose are the pancreas, liver, skeletal muscle, adipose tissue, intestine, and kidney. Diabetic complications are generally classified as macrovascular (e.g., stroke and heart disease) or microvascular (i.e., diabetic neuropathy, nephropathy, and retinopathy). Several animal models of diabetes have been used to develop oral therapeutic agents, including sulfonylureas, biguanides, thiazolidinediones, acarbose, and miglitol, for both type 1 and type 2 diseases. This review provides an overview of diabetes mellitus, describes oral therapeutic agents for diabetes and their targets, and discusses new developments in diabetic drug research.

• 미생물학회지
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• 제38권2호
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• pp.139-143
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• 2002

탄수화물분해 효소인 $\alpha$-glucosidase의 활성을 저해하는 물질을 생성하는 미생물을 검색하기 위하여 토양시료로 부터 수종의 미생물을 검색하였다. 토양 시료에서 강력한 $\alpha$-glucosidase 저해제를 생성하는 방선균PM718을 분리하였고 그 저해제의 활성을 기지물질인 acarbose와 비교 측정한 결과 우수한 활성을 나타냄을 확인하였다. 또한 그 활성은 pH 변화에도 안정된 활성을 유지하는 것을 확인하였다.