• Bulletin of the Korean Chemical Society
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• 제33권7호
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• pp.2365-2368
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• 2012

The $11{\beta}$-hydroxysteroid dehydrogenase type 1 ($11{\beta}$-HSD1) enzyme is involved in modulation of glucocorticoid activity within target tissues. This enzyme may contribute to obesity and/or metabolic disease through its action in adipose or liver tissue. Inhibition of $11{\beta}$-HSD1 has major therapeutic potential for glucocorticoid-associated diseases, including obesity, diabetes (wound healing), and muscle atrophy. To develop such therapeutics, we performed a pharmacophore-based virtual screening (VS) for identification of novel $11{\beta}$-HSD1 inhibitors and found that the VS hit compounds show potent inhibition of $11{\beta}$-HSD1 enzyme activity. Further, we present a binding model for active compounds. The proposed pharmacophore may serve as a useful guideline for future design of new chemical entities as $11{\beta}$-HSD1-targeted antidiabetic agents.

• Archives of Pharmacal Research
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• 제24권3호
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• pp.214-218
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• 2001

The mechanisms responsible for the antidiabetic activity of both the white ginseng radix (Ginseng Radix Alba, GRA) and the rootlet (Cinseng Radix Palva, GRP) were investigated. After a four week oral administration, the fasting blood glucose levels in the GRA- and GRP-treated groups were lower when compared to the control group. To elucidate the hypoglycemic mechanism(s) of the ginseng radices, glucose absorption from the small intestine, hepatic hexokinase and glucose-6-phosphatase activities, in addition to PPAR-${\gamma}$ expression in adipose tissue were examined. The results strongly suggest that GRA can improve hyperglycemia in KKAy mice, possibly by blocking intestinal glucose absorption and inhibiting hepatic glucose-6-phosphatase, and GRP through the upregulation of adipocytic PPAR-$\gamma$ protein expression as well as inhibiting intestinal glucose absorption.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.97.1-97.1
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• 2003

Antidiabetic activity of formular containing an Euonymus alata (EA) and Mori Foluim (MF) was investigated in oral glucose tolerance test (OGTT) and multiple low dose Streptozotocin (MLDSTZ)-induced rats. Optimum ratio between EA and MF was found to be 1:1 in OGTT, and two strengths (250 and 500 mg/kg for each medicinal plant) were coadministered with 20 mg/kg of STZ in 5 consecutive days. At 3rd week, water and food intakes were compared between groups and polydipsia and polyphagia shown in diabetic control were markedly improved in dose dependent manner. (omitted)

• Biomolecules & Therapeutics
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• 제29권2호
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• pp.154-165
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• 2021

This study aimed to investigate whether the antidiabetic drugs dipeptidyl peptidase 4 (DPP4) inhibitors such as evogliptin and sitagliptin affect the membrane DPP4 (mDPP4) enzymatic activity and immune function of T helper1 (Th1) cells in terms of cytokine expression and cell profiles. The mDPP4 enzymatic activity, cytokine expression, and cell profiles, including cell counts, cell viability, DNA synthesis, and apoptosis, were measured in pokeweed mitogen (PWM)-activated CD4+CD26+ H9 Th1 cells with or without the DPP4 inhibitors, evogliptin and sitagliptin. PWM treatment alone strongly stimulated the expression of mDPP4 and cytokines such as interleukin (IL)-2, IL-10, tumor necrosis factor-alpha, interferon-gamma, IL-13, and granulocyte-macrophage colony stimulating factor in the CD4+CD26+ H9 Th1 cells. Evogliptin or sitagliptin treatment potently inhibited mDPP4 activity in a dose-dependent manner but did not affect either the cytokine profile or cell viability in PWM-activated CD4+CD26+ H9 Th1 cells. These results suggest that, following immune stimulation, Th1 cell signaling pathways for cytokine expression function normally after treatment with evogliptin or sitagliptin, which efficiently inhibit mDPP4 enzymatic activity in Th1 cells.

• 고려인삼연구와산업
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• 제3권1호
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• pp.19-26
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• 2009

• 생명과학회지
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• 제27권5호
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• pp.579-583
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• 2017

번행초는 주요 화합물인 수용성 다당류와 cerebroside의 작용에 기인하여 기대되는 항궤양성 약용작물이다. 스트렙토조토신 유도 당뇨마우스에서 번행초의 다당 추출물(TPE)의 항당뇨 효과는 이전에 보고된 바가 없다. 본 연구는 체중 1 kg 당 65 mg의 스트렙토조토신을 복강에 주사하여 확립된 당뇨 마우스에서 TPE의 항당뇨 효과를 측정하기 위해 실시하였다. 100 mg 농도의 TPE를 3주간 투여했을 때, 당뇨 마우스의 체중은 유지되었으며, 혈당, 중성지방, 그리고 lactate dehydrogenase, alkaline phosphatase 및 glutamic pyruvic transaminase가 낮은 수준으로 감소함이 관찰되었다. 또한 내당능 실험에서도 TPE의 투여는 대조군인 당뇨 마우스에 비해 혈당 수준을 현저하게 감소시켰으며, 실험 가능한 거의 모든 생화학적 요인을 당뇨마우스에 비해 낮은 수준으로 회복시켰다. 따라서 전통적인 약용작물인 번행초의 잠재적인 항당뇨 효능을 본 연구에서 처음으로 증명하였다.

• 생약학회지
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• 제50권2호
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• pp.141-147
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• 2019

The aim of this study was to investigate the potential of Acanthopanax sieboldianum (Makino) Koidz (ACS) as a potent antioxidant and antidiabetic agent. The antioxidative and alpha-glucosidase inhibitory activities were examined using the methanol extracts and solvent fractions from ACS-leaf and ACS-stem. Antioxidative activities were measured by in vitro methods such as DPPH and ABTS radical scavenging activity and superoxide dismutase (SOD) activity. When the chloroform and ethyl acetate fractions of ACS-leaf and ethyl acetate fractions of ACS-stem were compared with the control, the SOD-like activity was impaired even at the low treatment concentrations. In addition, the ethyl acetate fractions of ACS-leaf and ACS-stem showed alpha-glucosidase inhibition activities at low treatment concentrations. Analysis of the major components in the fractions of ACS-leaf and ACS-stem was also performed using HPLC. Finally, astragalin, isoqurecetin, chlorogenic acid and caffeic acid contents were measured. Based on this work, we propose that ACS-leaf and ACS-stem have great potential as natural antioxidant and antidiabetic materials related to health benefits.

• 생명과학회지
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• 제34권6호
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• pp.385-392
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• 2024

고추(Capsicum annuum L.)는 전 세계적으로 식용 및 의약용으로 널리 사용되는 향신 식물이다. 본 연구에서는 한국 재래종 5종(유월초, 수비초, 수미향, 고운빛, 및 칠성초)과 개량종 5종(다복, 청양, 충성, 올복합 및 신홍길동)의 에탄올 추출물을 조제하고, 추출물의 색차, polyphenol 함량, 항산화, 항당뇨 및 항응고 활성을 비교하였다. 개량종 고추 추출물은 재래종 고추 추출물에 비해 높은 적색과 낮은 황색을 보였다. 고추 추출물의 polyphenol 및 flavonoid 함량 분석결과, 유월초와 수미향 추출물에서 유의하게 높았으며, 이들은 우수한 DPPH 음이온 소거 활성, ABTS 양이온 소거 활성 및 환원력을 보였다. Nitrite 소거능의 경우 칠성초, 유월초 및 다복 품종에서 유의하게 높게 나타났다. 또한 항당뇨 활성은 수비초, 수미향 및 고운빛 추출물에서 우수하였다. 항혈전 활성 평가에서, 유월초 추출물은 5 mg/ml 농도에서 용매대조군과 비교하여 thrombin time을 1.61배 연장시켰으며, 다복 추출물은 prothrombin time 및 activated partial thromboplastin time을 각각 1.33배 및 2.21배 연장시켜 항혈전 활성을 확인하였다. 또한 모든 고추 추출물은 5 mg/ml 농도까지 적혈구 용혈 활성을 나타내지 않았다. 이러한 결과는 국내 재래종 고추를 이용한 항산화, 항당뇨 및 항혈전 소재 개발이 가능함을 제시하고 있으며, 향후 국내 재래종 고추 품종이 나고야 의정서 발효에 대응하면서 막대한 종자 사용료를 지불하고 있는 개량종 고추를 대치할 수 있음을 제시하고 있다.

• 한국축산식품학회지
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• 제35권6호
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• pp.847-858
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• 2015

The study aimed to evaluate the effect of kefir combination from goat milk and soy milk on lipid profile, plasma glucose, glutathione peroxidase (GPx) activity and the improvement of pancreatic β-cell in diabetic rats. Male rats were divided into five treatments: normal control, diabetic control, goat milk kefir, combination of goat milk-soy milk kefir and soy milk kefir. All rats were induced by streptooztocin-nicotinamide (STZ-NA), except for normal control. After 35 d experiment, the rats were sampled for blood, sacrificed and sampled for pancreatic tissues. Results showed that diabetic rats fed kefir combination had higher (p<0.05) triglyceride than the rats fed goat milk or soy milk kefir. Decreasing of plasma glucose in diabetic rats fed kefir combination was higher (p<0.05) than rats fed goat millk kefir. The activity of GPx in diabetic rats fed three kinds of kefir were higher (p<0.01) than untreated diabetic rats. The average number of Langerhans and β-cells in diabetic rats fed kefir combination was the same as the normal control, but it was higher than diabetic control. It was concluded that kefir combination can be used as antidiabetic through maintaining in serum triglyceride, decreasing in plasma glucose, increasing in GPx activity and improving in pancreatic β-cells.

• 생약학회지
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• 제52권2호
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• pp.77-83
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• 2021

The number of people suffering from diabetes have been increased around the world. In this study, we investigated the antidiabetic and antioxidant effects of Anthriscus sylvestris(L.) Hoffm and its main compounds. It was divided into root(R) and aerial part(AP) for comparative analysis. Total polyphenol, total flavonoid content was higher in AP extract, but nodakenin content was higher in R(1169.13 ± 6.00 mg/g) extract. Antioxidant activity was also higher in AP extract. To compare antidiabetic efficacy, we analyzed the effects of R and AP extracts on ɑ-glucosidase inhibition(AGI), dipeptidyl peptidase-4(DPP-4) and protein tyrosine phosphatase(PTP)1B activity. R and AP extracts showed similar effects on AGI and DPP-4 activity in a concentration dependent manner, and there was no effect on PTP1B activation. Glucose uptake(139.51 ± 3.19%) in 3T3-L1 cells was more effective in the AP extract-treated group than the positive control, rosiglitazone, group. Both R and AP extracts were effective in protecting against pancreatic beta cell damage caused by hyperglycemia. These results suggest that Anthriscus sylvestris(L.) Hoffm. could be used as a candidate for diabetes treatment.