• Bulletin of the Korean Chemical Society
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• v.32 no.3
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• pp.1000-1006
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• 2011

The discovery of carbohydrate-based bioactive compounds has recently received considerable interest in the drug development. This paper stresses on the application of 1-methoxy-O-glucoside as the central scaffold, whereas salicylic pharmacophores were introduced with diverse spatial orientations probing into the structural preference of an enzymatic target, i.e. protein tyrosine phosphatase 1B (PTP1B). By employing regioselective protection and deprotection strategy, 2,6-, 3,4-, 4,6- and 2,3-di-O-propynyl 1-methoxy-O-glucosides were previously synthesized and then coupled with azido salicylate via click chemistry in forming the desired bidentate salicylic glucosides with high yields. The inhibitory assay of the obtained triazolyl derivatives leads to the identification of the 2,3-disubstituted salicylic 1-methoxy-O-glucoside as the structurally privileged PTP1B inhibitor among this bidentate compound series with micromole-ranged $IC_{50}$ value and reasonable selectivity over other homologous PTPs tested. In addition, docking simulation was conducted to propose a plausible binding mode of this authorized inhibitor with PTP1B. This research might furnish new insight toward the construction of structurally different bioactive compounds based on the monosaccharide scaffold.

• The Journal of Internal Korean Medicine
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• v.11 no.1
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• pp.29-40
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• 1990

In order to study the effect on liver diseases, Saenggan-tang has been applied to 26 patients of chronic hepatitis, 9 patients of liver cirrhosis, 5 patients of acute hepatitis, 8 patients of alcoholic liver diseases, 1 patient of hepatoma total 49 patients visiting the first internal medicine department of the hospital of Oriental Medicine, Kyung Hee University. The Saenggan-tang was taken every 4 weeks (ecept acute hepatitis every 2 weeks). 1. Saenggan-tang had decrease on activity of SGOTF SGPT, with the passage of time, 4, 8, and 12 weeks, showing statistically significant effect. 2. Saenggan-tang revealed sharp decrease on levels of total bilirubin and alkaline phosphatase no showing significance in relation to a few cases 3. Serum protein total and albumin levels were in normal limit before or after Saenggan-tang treatment 4. Triglyceride level was lowered remarkably after Saenggan-tang treatment, showing significance in alcoholic liver disease group whereas no significance in chornic hepatitis Judging from above results, it is proved that Saenggan-tang has curative effect of liver diseases such as acute, chronic hepatitis, liver cirrhosis, alcobolic liver diseases and so on.

• Journal of Microbiology and Biotechnology
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• v.23 no.9
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• pp.1206-1211
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• 2013

The selective inhibition of PTP1B has been widely recognized as a potential drug target for the treatment of type 2 diabetes and obesity. In the course of screening for PTP1B inhibitory fungal metabolites, the organic extracts of several fungal species isolated from marine environments were found to exhibit significant inhibitory effects, and the bioassay-guided investigation of these extracts resulted in the isolation of fructigenine A (1), cyclopenol (2), echinulin (3), flavoglaucin (4), and viridicatol (5). The structures of these compounds were determined mainly by analysis of NMR and MS data. These compounds inhibited PTP1B activity with 50% inhibitory concentration values of 10.7, 30.0, 29.4, 13.4, and 64.0 ${\mu}M$, respectively. Furthermore, the kinetic analysis of PTP1B inhibition by compounds 1 and 5 suggested that compound 1 inhibited PTP1B activity in a noncompetitive manner, whereas compound 5 inhibited PTP1B activity in a competitive manner.

• Nutrition Research and Practice
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• v.4 no.5
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• pp.369-374
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• 2010

Grape is one of the most popular and widely cultivated fruits in the world. Although grape skin and seeds are waste product of the winery and grape juice industry, these wastes contain large amounts of phytochemicals such as flavonoids, phenolic acids, and anthocyanidins, which play an important role as chemopreventive and anticancer agents. We evaluated efficacies of grape skin and seeds on hepatic injury induced by dimethylnitrosamine (DMN) in rats. Treatment with DMN significantly increased levels of serum alanine transaminase, aspartate transaminase, alkaline phosphatase, and bilirubin. Diet supplementation with grape skin or seeds (10% daily for 4 weeks) prevented these elevations. The grape skin and seeds also restored serum albumin and total protein levels, and reduced the hepatic level of hydroxyproline and malondialdehyde. Furthermore, grape skin and seeds reduced DMN-induced collagen accumulation, as estimated by histological analysis of liver tissue stained with Sirius red. Grape skin and seeds also reduced hepatic stellate cell activation, as assessed by ${\alpha}$-smooth muscle actin staining. In conclusion, grape skin and seeds exhibited in vivo hepatoprotective and antifibrogenic effects against DMN-induced liver injury, suggesting that grape skin and seeds may be useful in preventing the development of hepatic fibrosis.

• Korean Journal of Plant Resources
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• v.17 no.3
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• pp.283-288
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• 2004

Effect of Siho (Bupleurum falcatum L.) extracts on liver function were investigated in CCl4 intoxicated rats. Plasma $\alpha$-fetoprotein and total protein concentration showed a tendency to decrease in Siho extracts groups. However plasma albumin concentration showed no significantly different in all treatment groups. Activities of plasma asparate aminotransferase and alanine aminotransferase in Siho extracts groups showed a lower values than control group. Alkan phosphatase and lactate dehydrogenase activities showed a tendency to decrease in Siho extracts groups. However ${\gamma}$-glutamyl transferase activity showed no significantly different in all treatment groups. Concentration of plasma triglyceride and total cholesterol showed no significantly different in all treatment groups.

• Korean Journal of Pharmacognosy
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• v.52 no.2
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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.

• 한국체육학회지인문사회과학편
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• v.55 no.3
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• pp.649-658
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• 2016

This study aimed to analyze PDH(Pyruvate dehydrogenase) and protein expression of PDK4(Pyruvate dehydrogenase kinase 4), PDP1(PDH phosphatase 1), enzymes that are involved in the activation of PDH, in skeletal muscle and to investigate the concentration of thiamine administration in liver and muscle following 4 weeks of endurance training. Methods : 6 weeks old male ICR mice were divided into two groups: sedentary group (CON, n=10; TH, n=10), and exercise group (EX, n=10, THEX, n=10). Thiamine(thiamine tetrahydrofurfuryl disulfide: TTFD) TTFD was orally administrated into TH and THEX groups in 50mg/kg body weight for 4 weeks. Treadmill training was performed in EX and THEX groups at about 70% of VO2max for 5 times a week for 4 weeks. Results : In this study, the concentration of glycogen was significantly increased following 4 weeks of endurance training, but a significant difference was not found following thiamine administration. Similarly, there was a significant effect of the training on PDH and the expression of PDK4 and PDP1 as PDH was increased by about 40% along with the increase in PDK4 and PDP1. However, there was no significant difference found between the groups following thiamine administration. Discussion : This result shows that there was no synergistic effect of thiamine administration, potentially due to adaptation of skeletal muscle from a long-term endurance training. Therefore, it will be necessary to consider the intake timing of thiamine and to analyze proteins that are related to PDH following the administration of complex carbohydrates.

• The Korean Journal of Food And Nutrition
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• v.21 no.1
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• pp.71-78
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• 2008

This study examined the effects of mulberry-leaf powder Tofu(MPT) on the anthropometric measurements, bone mineral density(BMD), biochemical markers of bone turnover, serum lipid levels of and macrominerals status in 30 female university students living in Choongnam with low dietary Ca intake was low(mean daily $intake=524.66{\pm}21.47$ mg/day). The subjects received the MPT supplemented(100 g/day) for 4 weeks. The nutrient content per 100 g MPT was 84.10 kcal(energy), 8.98 g(protein), 0.53 mg(fiber), 211.33 mg(Ca) and 1.59 g(fat). Anthropometric measurements, 24-hour dietary recall, carpus BMD using DEXA, select BMD biomarckers(serum alkaline phophatase activity, osteocalcin, urinary deoxypyridinoline), serum protein levels, albumin, and glucose levels, lipid profiles(cholesterol, triglyceride, HDL-cholesterol, LDL-cholesterol) and serum macrominerals(Ca, Ca/P ratio, Mg) were analyzed before and after MPT supplementation. Following MPT supplementation, there was no significant differences in anthropometric measurements, nutrient intakes, carpus BMD, serum alkaline phosphatase activity, osteocalcin, and urinary deoxypyridinoline, serum levels of protein, albumin, and glucose or lipid profiles with AI, HTR, LHR and CRF. However, there were significant increases in dietary calcium as well as decreases in serum triglycerides with MPT supplementation. Although further research is needed, these results that regular intake MPT could prevent bone and cardiovascular diseases.

• Microbiology and Biotechnology Letters
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• v.33 no.4
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• pp.260-266
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• 2005

IgE-dependent histamine releasing factor (HRF), previously known as P23/P21 or translationally controlled tumor protein (TCTP), induces the degranulation of histamine in mast cell and basophil. Yeast two hybrid results showed that HRF interacts with the alpha subunit of Na, K-ATPase, suggesting that HRF is a regulator for governing the activity of Na, K-ATPase. In this study, we examined the interaction of HRF and Wa,K-ATPase after treatments of various PKC isotype inhibitors. Membrane fractionation, pull-down assay and immunoprecipitation results showed that PKC $\alpha,\;PKC\;\beta,\;\delta$ subunits are involved in the phosphorylation of HRF. However, these results did not correlate with the results of histamine release assay since histamine release assay results suggested that some PKC isotype inhibitors induced the histamine release in RBL-2H3 cell.

• Nutrition Research and Practice
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• v.12 no.1
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• pp.20-28
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• 2018

BACKGROUND/OBJECTIVES: Perilla frutescens (L.) Britton var. (PF) sprout is a plant of the labiate family. We have previously reported the protective effects of PF sprout extract on cytokine-induced ${\beta}-cell$ damage. However, the mechanism of action of the PF sprout extract in type 2 diabetes (T2DM) has not been investigated. The present study was designed to study the effects of PF sprout extract and signaling mechanisms in the T2DM mice model using C57BL/KsJ-db/db (db/db) mice. MATERIALS/METHODS: Male db/db mice were orally administered PF sprout extract (100, 300, and 1,000 mg/kg of body weight) or rosiglitazone (RGZ, positive drug, 1 mg/kg of body weight) for 4 weeks. Signaling mechanisms were analyzed using liver tissues and HepG2 cells. RESULTS: The PF sprout extract (300 and 1,000 mg/kg) significantly reduced the fasting blood glucose, serum insulin, triglyceride and total cholesterol levels in db/db mice. PF sprout extract also significantly improved glucose intolerance and insulin sensitivity, decreased hepatic gluconeogenic protein expression, and ameliorated histological alterations of the pancreas and liver. Levels of phosphorylated AMP-activated protein kinase (AMPK) protein expression also increased in the liver after treatment with the extract. In addition, an increase in the phosphorylation of AMPK and decrease in the phosphoenolpyruvate carboxykinase and glucose 6-phosphatase proteins in HepG2 cells were also observed. CONCLUSIONS: Our results sugges that PF sprout displays beneficial effects in the prevention and treatment of type 2 diabetes via modulation of the AMPK pathway and inhibition of gluconeogenesis in the liver.