• Journal of Applied Biological Chemistry
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• 제58권1호
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• pp.1-3
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• 2015

This study investigated the inhibitory activities of 2-hydroxyquinoline and its analogs against ${\alpha}$-glucosidase and ${\alpha}$-amylase. Based on the $IC_{50}$ values of 2-hydroxyquinoline analogs tested against ${\alpha}$-glucosidase and ${\alpha}$-amylase, 2-hydroxyquinoline had potent inhibitory activity (64.4 and $130.5{\mu}g/mL$, respectively), while 2-methyl-8-hydroxyquinoline showed weakly inhibitory activity (90.7 and $215.4{\mu}g/mL$, respectively). 2-Methylquinoline demonstrated no activity against ${\alpha}$-glucosidase and ${\alpha}$-amylase. In conclusion, 2-hydroxyquinoline analogs, with the existence of a methyl group and hydroxyl on quinoline, can be useful as a new diabetes treatment.

• Bulletin of the Korean Chemical Society
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• 제33권11호
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• pp.3772-3776
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• 2012

Mitogen-activated protein kinase phosphatase 4 (MKP4) has proved to be a promising target for the development of therapeutics for the treatment of diabetes and the other metabolic diseases. Here, we report an example for a successful application of the structure-based virtual screening to identify three novel inhibitors of MKP4. These inhibitors have desirable physicochemical properties as a drug candidate and reveal a moderate potency with $IC_{50}$ values ranging from 4.9 to $32.3{\mu}M$. Therefore, they deserve consideration for further development by structure-activity relationship studies to optimize the inhibitory and antidiabetic activities. Structural features relevant to the stabilization of the newly identified inhibitors in the active site of MKP4 are discussed in detail.

• 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.

• Journal of Applied Biological Chemistry
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• 제44권1호
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• pp.1-5
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• 2001

The methanol extracts of 25 leguminous seeds in vitro was evaluated for inhibitory activities against the small intestinal $\alpha$-glucosidase of Sprague Dawley male rats. The responses varied both with leguminous seed types and concentrations used. At the concentration of 0.5 mg/ml, the methanol extracts of Cassia obtusifolia, Glycine max var. yagkong, Glycine max var. hooktae, Glycine max var. geumdu, Glycine max var. mejukong, Glycine soja, Phaseolus multiflorus, Pisum sativum, and Vigna sinensis inhibited over 50% of the enzyme activity. The extracts of G. max var. yagkong and V. sinensis showed relatively strong inhibitory activities against $\alpha$-glucosidase at the concentration of 0.1 mg/ml. The activity of each solvent fraction from G. max var. yagkong and V. sinensis was determined, and potent activities were detected from chloroform and butanol fractions, respectively. $IC_{50}$ values of G. max var. yagkong and V. sinensis were 0.06 and 0.19 mg/ml, respectively. As a naturally occurring therapeutic agents, leguminous seeds examined could be useful for developing new types of antidiabetic agents.

• Journal of Ginseng Research
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• 제20권4호
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• pp.389-415
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• 1996

Panax ginseng C.A. Meyer(Araliaceae) has been traditionally used as an expensive and precious medicine in oriental countries for more than 5, 000 years. Ginseng saponin isolated from the root of Panax ginseng have been regarded as the main effective components responsible for the pharmacological and biological activities. Such as antiaging effects. antidiabetic effects anticancer effects. Protection against physical and chemical stress. Analgesic and antipyretic effects. Effects on the central nervous system, tranquilizing action and others. Thirty kinds of ginsenosides have been so far isolated from ginseng saponin and their chemical structures have been elucidated since 1960's. Among which protopanaxadiol type is 19 kinds. protopanaxatriol type. 10 kinds and oleanane type, one. Since ginsenosides are generally labile under acidic conditions ordinary acid hydrolysis is always accompanied by many side reactions, such as epimerization. hydroxylation and cyclization of side chain of the sapogenins Especially. it is well known that C-20 glycosyl linkage of ginsenoside was hydrolysed on heating with acetic acid to give an equilibrated mixture of 20(S) and 20(R) epimers. And also, the chemical transformations of the secondary metabolites have appeared during the steaming process to prepare red ginseng. Indicating demalonylation of malonyl ginsenosides, elimination of glycosyl residue at C-20 and isomerization of hydroxyl configuration at C-20. But these studies have not provided a comprehensive picture in explaning how these ginsenosides showed val'iotas pharmacological activities of ginseng. Though some of them have been involved in the mechanism of pharmacological actions. Recently, non-saponin components have received a great deal of attention for their antioxidant, anticancer antidiabetic, immunomodulating. anticomplementary activities and so on. To meet the demand for such wide applications, studies on the non-saponin components play an important role in providing a good evidence of pharmacological and biol ogical activities. Among the non-saponin constituents of Korean ginseng, polyacetylenes, phenols. Sesquiterpenes, alkaloids. polysaccharides oligosaccharides, oligopeptides and aminoglycosides together with ginsenosides of terrestrial part are mainly described.

• 동아시아식생활학회지
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• 제25권2호
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• pp.270-277
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• 2015

장미과에 속한 낙엽교목인 산사나무의 열매인 산사의 항산화 및 항당뇨 관련 활성을 검토하고, 추출 용매에 따른 차이를 비교하기 위하여 총 페놀 함량, DPPH 라디칼 소거능, ABTS 라디칼 소거능, 최종당화산물 억제능, ${\alpha}$-glucosidase 억제능, aldose reductase 억제능을 측정하였다. 수율은 70% 에탄올 추출물이 33.16%로 가장 높았고, 50% 에탄올 추출물이 27.79%로 그 다음 높았으며, 물, 30% 에탄올, 100% 에탄올은 각각 21.71%, 21.88%, 19.03%를 나타내었다. 총 페놀함량은 50% 에탄올 추출물이 $41.83{\pm}0.07mg$ GAE/g으로 가장 높았고, DPPH와 ABTS 라디칼 소거능도 50% 에탄올 추출물이 각각 $80.79{\pm}0.83%$, $34.92{\pm}0.97%$로 가장 높았다. 최종 당화산물 억제능과 ${\alpha}$-glucosidase 억제능도 50% 에탄올 추출물이 $27.09{\pm}2.27%$와 $58.87{\pm}0.70%$로 가장 높게 나타난 반면에 AR은 물 추출물이 $30.68{\pm}1.41%$로 가장 높게 나타나면서 상이한 경향을 보였다. 이상의 결과를 종합해 보면, 알코올 농도에 따른 산사의 추출물 중 50% 에탄올 추출물이 천연 항산화제로서 가치가 있으며, 당뇨병 예방을 위한 천연물로서의 가능성도 보였으나 당뇨병 합병증 치료에 대한 효과는 미흡한 것으로 나타났다. 향후 좀 더 다양한 fraction에서의 연구와 in vivo 시험 등을 통한 추가적인 연구가 필요할 것으로 사료된다.

• KSBB Journal
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• 제27권6호
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• pp.361-366
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• 2012

We investigated the anti-diabetic activity and enzymatic activity of 24 commercial doenjang samples certified for traditional foods. Twenty four doenjang samples showed the wide ranges in enzymatic activities (protease activities 0-50.45 unit/g, ${\alpha}$-amylase activities 0-675.9 unit/g, ${\beta}$-amylase 13.6-308.6 unit/g), and there were no difference in enzymatic activity by the producing region. To evaluate the potential anti-diabetic activity of 24 doenjang samples, we examined the effect of doenjang methanol extract (DME) on 2-[n-(7-nitrobenz-2-oxa-1, 3-diazol-4-yl) amyno]-2-deoxy-d-glucose (2-NBDG) uptake. Ten samples among 24 samples significantly stimulated the uptake of 2-NBDG. When the cells were treated with DME at 400 ug/mL, No. 17 and 23 specially stimulated 2-NBDG uptake by 1.23-fold and 1.25-fold, respectively, compared with untreated control cell. And there were no cytotoxicity in the C2C12 cells treated with DME at concentration of 500 ug/mL. Among 24 samples, No. 6, 7, 12, 21 and 24 showed the ${\alpha}$-glucosidase inhibitor activity at concentration of 10 mg/mL; however, they were less effective than acarbose which is a commercial ${\alpha}$-glucosidase inhibitor.

• 한국식품영양과학회지
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• 제34권10호
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• pp.1531-1535
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• 2005

C. militaris 동충하초의 기능성을 규명하기 위하여 당대사 관련 효소인 GK, PDH 및 ACC 활성을 측정하였다. C. militaris에서 추출된 CM-A와 CM-B는 GK와 PDH 및 ACC 효소에 대하여 대조군에 비해 높은 활성을 나타냈으며, CM-B 보다는 CM-A에서 유의적으로 높은 활성 증가를 나타냈다(p < 0.05). 간세포내 당질 관련 호소의 활성은 CM-A와 CM-B 분획물의 혼합 비율에 영향을 받는 것으로 나타났는데 활성이 높은 CM-A의 비율이 커질수록유의적으로 높은 활성 증가를 나타냈다. GK와 ACC는 단일 상태의 CM-A 보다는 혼합된 상태일 때 활성이 증가하였지만, PDH는 혼합된 상태보다는 CM-A 단독일 때 가장 높은 활성을 나타냈다. 결론적으로 C. miliaris는 GK, PDH 및 ACC 등의 효소 활성을 증가시킴으로써 혈중 포도당의 상승을 억제하며 이로 인해 항당뇨 작용을 한다고 판단된다.

• 생명과학회지
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• 제25권6호
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• pp.638-645
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• 2015

본 연구는 ice plant (Mesembryanthemum crystallinum)의 생리활성을 분석하여 기능성 식품으로서의 가능성을 조사하였다. Ice plant는 아프리카와 서유럽, 북미, 남미 그리고 호주에서 서식하는 다육식물로 항당뇨, 항산화, 지질 대사 활성에 효능이 있다고 알려져 있다. Ice plant를 methanol (MCM), ethanol (MCE), 열수(MCHW), 열수 추출 후 methanol (MCHM)로 추출하여, mushroom tyrosinase, pancreatic lipase, DPPH free radical 소거 활성, NO 생성, α-glucosidase에 대한 저해 활성을 측정 하였다. MCM, MCE, MCHW, MCHM 추출물의 추출 수율은 0.37%, 0.33%, 0.5%, 0.07%로 나타났다. MCHW 추출물은 DPPH free radical 소거능에 높은 효과를 보였고, MCM, MCE 추출물은 lipase 저해 활성, α-glucosidase 저해 활성, NO 생성 저해활성을 보였다. 그러나 mushroom tyrosinase 저해 활성은 모든 추출물에서 매우 낮았다. 이러한 결과를 통해 ice plant는 항산화 물질로서 비만, 당뇨, 염증 치료용 기능성 식품으로서의 가능성이 매우 높음을 확인할 수 있었다.

• 한국산학기술학회논문지
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• 제22권4호
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• pp.483-492
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• 2021

곽향은 식욕부진, 메스꺼움 등의 치료에 사용될 뿐만 아니라 최근에는 항당뇨 효능도 알려졌다. 본 연구에서는 곽향의 항산화력과 주요 성분들을 조사한 다음, in-silico 방법론을 적용하여 타겟 단백질들을 예측하였다. 먼저 메탄올 추출물의 DPPH와 ABTS 라디칼 소거능의 EC50 값은 각각 78.6 ㎍/mL과 31.0 ㎍/mL이었다. 이것은 ascorbic acid의 값(9.9 ㎍/mL, 5.2 ㎍/mL)과 비교할 때 항산화력이 뛰어나다고 할 수 있다. HPLC-PDA-MS/MS를 이용하여 성분들을 정성 분석한 결과, 추출물의 주요 화합물로 rosmarinic acid, tilianin, agastachoside 그리고 acacetin을 확인하였다. 이들 성분들의 항당뇨 작용 타겟 단백질을 DIA-DB 서버를 사용하여 구조 유사도와 inverse doking 방법론을 적용하여 예측하였다. 본 가상 탐색 결과, 주요 타겟 단백질들은 PPAR-γ, DPP IV, glucokinase, α-glucosidase, SGLT2, aldose reductase, corticosteroid 11-beta-dehydrogenase로 예측되었다. 그리고 이들 단백질들 중 일부는 이미 실험적으로 검증된 타겟 단백질이었다. 따라서 in silico 검색 방법이 유효하다고 생각할 수 있다. 마지막으로 활성성분들의 최적의 추출 조건을 결정하기 위하여 여러 추출 용매들로 곽향을 추출하였다. 여러 유기 용매들 중에는 메탄올이 그리고 에탄올-물 혼합용매에서는 80% 에탄올이 가장 효과적인 추출 용매로 확인되었다.