• Journal of Ginseng Research
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• 제38권1호
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• pp.28-33
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• 2014

Background: Panax notoginseng has been used as a general tonic agent to invigorate human body for millennia in China and continued to be used until present. Methods: Some chromatographic methods were performed to isolate pure triterpenoids, and their structures were determined by nuclear magnetic resonance (NMR) experiments. Anti-diabetes activities of isolated compounds were evaluated through their inhibitory activity of protein tyrosine phosphatase 1B (PTP1B) enzyme. Results and Conclusion: Three new dammarane-type triterpenoids, notoginsenoside-LX (1), notoginsenoside-LY (2), and notoginsenoside-FZ (3) together with eighteen known compounds were isolated from the Panax notoginseng leaves. The structure-activity relationship of the compounds with dammaranetype triterpenoids and their PTP1B inhibitory activity were also reported. Results showed that compounds 2, 15, 20, and 21 can significantly inhibit the enzyme activity of PTP1B in a dose-dependent manner, with inhibitory concentration 50 ($IC_{50}$) values of $29.08{\mu}M$, $21.27{\mu}M$, $28.12{\mu}M$, and $26.59{\mu}M$, respectively. The results suggested that Panax notoginseng leaves might have potential as a new therapeutic agent for the treatment of diabetes.

• Natural Product Sciences
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• 제13권4호
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• pp.311-316
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• 2007

In this study, the twenty-four ethyl acetate extracts of twenty-two medicinal plants, traditionally used in Vietnam as anti-diabetes agents, were investigated for ${\alpha}$-amylase and protein tyrosine phosphatase 1B (PTP1B) enzymes inhibitory activity in vitro. The results indicated that, twelve materials (50.0%) showed moderate to strong inhibitory activity in ${\alpha}$-amylase inhibitory activity with $IC_{50}$ values ranging from 2.5 to $48.8{\mu}g/mL$; meanwhile, ten extracts (41.6%) could demonstrate PTP1B activity with $IC_{50}$ values less than $30.5{\mu}g/mL$. Some plants presented interesting activities against both of ${\alpha}$-amylase and PTP1B enzymes such as Catharanthus roseus, Carthamus tinctorius, Momordica charantia, Gynostemma pentaphyllum, Glycyrrhiza glabra, Smilax glabra, Psidium guajava (leave), and Rehmannia glutinosa. The study may provide a proof, at least in a part, for the ethno-medical use in diabetes disease of these plants.

• Bulletin of the Korean Chemical Society
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• 제24권10호
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• pp.1455-1464
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• 2003

Several series of compounds (benzoic acids, pyrazolecarboxylic acids, phenoxyacetic acids, and quinolinoxyacetic acids) were prepared and evaluated for their inhibitory activity against PTP-1B. Several compounds showed submicromolar inhibitory activity.

• BMB Reports
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• 제46권11호
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• pp.533-538
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• 2013

The expression of matrix metalloproteinases (MMPs) produced by cancer cells has been associated with the high potential of metastasis in several human carcinomas, including breast cancer. Several pieces of evidence demonstrate that protein tyrosine phosphatases (PTP) have functions that promote cell migration and metastasis in breast cancer. We analyzed whether PTP inhibitor might control breast cancer invasion through MMP expression. Herein, we investigate the effect of 4-hydroxy- 3,3-dimethyl-2H benzo[g]indole-2,5(3H)-dione (BVT948), a novel PTP inhibitor, on 12-O-tetradecanoyl phorbol-13-acetate (TPA)-induced MMP-9 expression and cell invasion in MCF-7 cells. The expression of MMP-9 and cell invasion increased after TPA treatment, whereas TPA-induced MMP-9 expression and cell invasion were decreased by BVT948 pretreatment. Also, BVT948 suppressed NF-${\kappa}B$ activation in TPA-treated MCF-7 cells. However, BVT948 didn't block TPA-induced AP-1 activation in MCF-7 cells. Our results suggest that the PTP inhibitor blocks breast cancer invasion via suppression of the expression of MMP-9.

• Bulletin of the Korean Chemical Society
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• 제31권11호
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• pp.3359-3365
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• 2010

The incorporation of microwave irradiation with the prevalent "click chemistry" is currently of considerable synthetic interest. We describe here the introduction of such laboratorial shortcut into carbohydrate-based drug discovery, resulting in the rapid formation of a series of triazole-linked salicylic $\beta$-D-O-glycosides with biological activities. All "clicked" products were achieved in excellent yields ($\approx$ 90%) within only a quarter. In addition, based on the structural characteristics of the afforded glycomimetics, their inhibitory activities were evaluated toward protein tyrosine phosphatases 1B (PTP1B) and a panel of homologous protein tyrosine phosphatases (PTPs). Docking simulation was also conducted to plausibly propose binding modes of this glycosyl salicylate series with the enzymatic target.

• Bulletin of the Korean Chemical Society
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• 제34권10호
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• pp.2861-2862
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• 2013

• Bulletin of the Korean Chemical Society
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• 제25권9호
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• pp.1303-1304
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• 2004

• 한국식품영양과학회지
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• 제42권2호
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• pp.175-181
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• 2013

표고버섯, 표고버섯균사체배양쌀 추출물의 항당뇨와 항비만 효과를 규명하고자 본 연구에서는 표고버섯 80% ethanol 추출물(LE), 표고버섯균사체배양쌀 80% ethanol 추출물(LEM)에서 3T3-L1 preadipocyte cell line을 이용하여 세포의 분화에 미치는 영향을 확인할 수 있었다. 분화유도후 8일 째에 Oil Red O 염색을 통해 세포내 형성된 지방구(lipid droplet)를 isopropanol에 용출하여 500 nm에서 흡광도를 측정한 결과, LE 100 ${\mu}g/mL$에서 p<0.05 수준에서 유의한 억제 효과가 나타났으며, LE 300 ${\mu}g/mL$에서는 p<0.01 수준에서 유의한 억제 효과가 나타났다. LEM은 대조군에 비하여 LEM을 10 ${\mu}g/mL$에서 p<0.05 수준에서 유의한 억제 효과가 나타났으며, LEM 30, 100, 300 ${\mu}g/mL$에서는 p<0.01 수준에서 유의한 억제 효과가 나타났다. CETP 저해 활성을 측정한 결과 LE 300 ${\mu}g/mL$에서 p<0.01 수준에서 유의한 저해효과가 나타났다. LEM을 농도별로 처리하였을 때 대조군에 비하여 농도 의존적으로 억제 효과가 있었으며, LEM 30 ${\mu}g/mL$에서 p<0.05 수준에서 유의한 저해효과가 나타났고 LEM 100, 300 ${\mu}g/mL$에서는 p<0.01 수준에서 유의한 저해효과가 나타났다. PTP1B 저해 활성을 측정한 결과, LE는 대조군에 비하여 LE 10, 30, 100, 1,000 ${\mu}g/mL$에서 통계적으로 p<0.05 수준에서의 유의한 저해효과가 나타났으며, LEM은 대조군에 비하여 농도 의존적으로 통계적으로 p<0.01 수준에서의 유의한 저해효과가 나타났다. 또한 고지방식이에 LE, LEM을 28일간 경구투여 하였을 때 흰쥐의 혈청 총콜레스테롤은 HFD군에 비해 LE군, LEM군에서 모두 유의적인 감소를 나타내었고(p<0.05), 혈청의 중성지방(triglyceride) 농도는 HFD군에 비해 LE, LEM군 모두 감소하는 경향을 나타내었으며 특히 LEM군은 통계적으로 p<0.05 수준에서 유의적인 감소를 나타내었다. 혈청의 HDL-cholesterol은 HFD군과 시료처리군에서 유의적인 차이는 나타나지 않았으며, LDL-cholesterol은 HFD군에 비해 LEM군에서 유의적인 감소를 나타내었다(p<0.01). 이상의 결과로 보아 표고버섯과 표고버섯균사체배양쌀은 지방세포의 분화를 억제시키며, 혈중 지질 조성을 개선시키는 효과가 있음을 알 수 있다.

• 대한화학회지
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• 제46권3호
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• pp.296-300
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• 2002

• 대한약학회:학술대회논문집
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• 대한약학회 2005년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.208-209
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• 2005