• Korean Journal of Pharmacognosy
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• v.52 no.3
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• pp.127-133
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• 2021

Platelet activation plays a major role in cardiovascular disorders (CVDs). Thus, disrupting platelet activation represents an attractive therapeutic target on CVDs. Esculetin, a bioactive 6,7-dihydroxy derivative of coumarin, possesses pharmacological activities against obesity, diabetes, renal failure, and CVDs. In other report, the effect of esculetin has been examined in human platelet activation and experimental mouse models, and esculetin inhibited collagen- and arachidonic acid-induced platelet aggregation in washed human platelets. However, it had no effects on other agonists such as thrombin and U46619, and its mechanism is not also clearly known. This study investigated the effect of esculetin on collagen-induced human platelet aggregation, and we clarified the mechanism. Esuletin has effects on the down regulation of PI3K/Akt and MAPK, phosphoproteins that act in the signaling process in platelet aggregation. The effects of esculetin reduced of TXA₂ production and phospholipase A₂ activation, and intracellular granule secretion including ATP and serotonin, leading to inhibit platelet aggregation. These results clearly clarified the effect of esculetin in inhibiting platelet activity and thrombus formation in humans.

• Journal of Life Science
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• v.15 no.6 s.73
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• pp.961-967
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• 2005

Macrophage migration inhibitory fartor (MIF), known as a cytokine, is a multifunctional protein that is ubiquitously expressed in a variety of cells and tissues; however, enzymatic function of MIF still remains elusive in cells. In this study, we assessed details of the tautomerase activity of MIF. We established rapid purification condition for MIF by using pGEX system and compared the L-dopachrome tautomerase activity of GST-MIF, tMIF, and MIF. The results show that GST (glutathione S-transferase)-epitope tag or N-terminal amino acids flanking the essential $P^{2}$ almost completely abrogated L-dopachrome tautomerase activity of MIF. Subsequently, to determine whether the N-terminal tags have effects on oligomerization of MIF, protein cross-linking products were analyzed on $15\%$ SDS-PACE. The result demonstrates that N-terminal tags are dispensable for the formation of MIF's homooligomers. Thus, the results imply that exposure of If containing hydrophobic pocket in the active site is critical for L-dopachrome tautomerase activity of MIF. In addition, our study suggest that the MIF's tautomerase activity might be influenced by interacting with cellular partners.

• Microbiology and Biotechnology Letters
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• v.47 no.1
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• pp.20-24
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• 2019

Moringa oleifera Lam (MOL) has been used as a traditional medicine to treat various cancers and inflammation. Whereas the bioactivities of the MOL leaf and seed are well reported, the study of the root is still rudimentary. In this study, the ethanol extract of MOL (EEMOL) and its subsequent organic solvent fractions were prepared and their anticoagulation activity in vitro and platelet aggregation inhibitory activity were evaluated. The EEMOL had negligible anticoagulation and strong platelet aggregation activities. However, the hexane and ethyl acetate fractions of EEMOL showed significant inhibition against thrombin, prothrombin, coagulation factors, and platelet aggregation, without hemolytic activity up to 1.0 mg/ml. Our results suggest that the active fractions of MOL root have potential as new anti-thrombosis agents.

• Microbiology and Biotechnology Letters
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• v.43 no.4
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• pp.373-377
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• 2015

The mature fruit of Sorbus commixta is known as magaja in Korea and is consumed in the form of tea and wine. In addition, it has been used to treat hypertension and articular neuralgia in folk medicine. In this study, the ethanol extract of magaja and its subsequent organic solvent fractions were prepared, and their in vitro anti-coagulation, and platelet aggregation inhibitory activities were evaluated. Among the fractions, the ethylacetate fraction demonstrated significant inhibition against thrombin, prothrombin, blood coagulation factors and platelet aggregation, without hemolysis activity up to 0.5 mg/ml. Our results suggest that the ethylacetate fraction of magaja has the potential to be used as a new anti-coagulation agent.

• Food Science and Preservation
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• v.21 no.5
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• pp.727-734
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• 2014

To investigate anti-thrombosis and anti-oxidation activities of the root of Arctium lappa L (RALL), which has been used as foodstuff and oriental medicine in Korea, the ethanol extract and its subsequent organic solvent fractions of the RALL were prepared. The yield of ethanol extraction was 10.94%, and the content of total polyphenol and total sugar of ethanol extract were 5.01 and 694.53 mg/g, respectively. The fraction yields of n-hexane, ethylacetate (EA), butanol and water residue were 1.62, 0.42, 5.98 and 85.38%, respectively. In anticoagulation activity assay, the ethanol extract of RALL did not show significant changes in thrombin time (TT), prothrombin time (PT) and activated partial thromboplastin time (aPTT), whereas the EA fractions showed 13 folds extended TT, PT, and aPTT respectively. Interestingly, the water residue showed strong activation effect against blood clotting factors with shortened aPTT, which might provide the evidence of coagulation agent of RALL in folk remedy. In anti-platelet aggregation assay, the activity of the ethanol extract and its fractions were comparable to that of aspirin. Especially the EA fraction showed 2-folds higher inhibitory activity than aspirin. In anti-oxidation activity assay, the EA fraction also showed strong in DPPH, ABTS and nitrite scavenging activity, and reducing power activity. The extract and fractions of RALL have ignorable hemolytic activity against human RBC up to 0.5 mg/mL concentration. Our results suggest that the EA fraction of RALL have potentials as safe and novel anti-thrombosis agent.

• The Korean Journal of Community Living Science
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• v.28 no.1
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• pp.29-43
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• 2017

We studied the antioxidant, the anti-inflammatory, antithrombotic, and antiobesity activities of seven different kinds of edible plants. 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ABTS radical scavenging activities were determined as a measurement of antioxidant activity. NO production inhibition by the macrophage cell line (Raw 264.7) treated with lipopolysaccharide (LPS) was carried out to assess anti-inflammatory activity. Thrombin inhibitory activity was measured for its antithrombotic function and inhibition of 3T3-L1 cell differentiation was evaluated as a measurement of antiobesity activity. Total phenolic components and total flavonoid contents were measured to determine functional materials in medicinal plants. Common sage, Japanese lady bell, and hairy agrimony showed high antioxidant activity ($IC_{50}$) of less than $100{\mu}g/mL$. All samples used in this study showed anti-inflammatory activity. Common sage, hairy agrimony, and hooker chives showed antithrombotic effects. Hairy agrimony showed the highest antithrombotic effect (98.1%). Common sage, Japanese lady belly, hairy agrimony, and hooker chives showed reduced 3T3-L1 cell differentiation and hooker chives strongly inhibited lipid accumulation in the cells compared to other medicinal plants. Common sage and hairy agrimony contained more than 1 mg GAE/g of phenolic compounds and more than 1 mg CE/g of flavonoids. Functional activities were different by plant part and extraction method from each sample. These results suggest that common sage, Japanese lady belly, hairy agrimony, and hooker chives may be used as healthy food sources with antioxidant, anti-inflammatory, antithrombotic, and antiobesity activities, and appropriate extracting methods from each plant need to be developed.

• Herbal Formula Science
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• v.12 no.2
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• pp.175-202
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• 2004

Nitric oxide(NO) play an important role in normal and pathophysiological cells including as a messenger molecule, neurotransmitter, microbiocidal agent, or dilator of blood vessels and artheriosclerosis, hypertension, myocardial infarction, respectively. To investigate that Ondamtang in the potential contribution of the levels of nitric oxide generated by endothelial nitric oxide synthase (eNOS) and the mechanisms of protection against L-NAME, human ECV304 cells, which normally do not express eNOS, were expressed by L-NAME. L-NAME stimulated rat or cells were found to be resistant to injury and delayed death following the Ondam-tang. Inhibition of nitric oxide synthesis abolished the protective effect against L-NAME, thrombin and collagen exposure. Interestingly, such effects have bee observed during stimulation with agents such as KCl on L-NAME mediate rats, were damaged by the NOS inhibitor NG-nitro-L-arginine methyl ester (L-NAME). Cardiovascular diseases is one of the blood vessels and renin-angiotensin system dynfunction. So we studied on herbal medicine that have a relation of vessels endothelium necrosis. In Oriental Medicine, Ondam-tang has been used for disease in relation to cardiovascular system. We studied on the protection and inhibitory effects of cardiovascular diseases in L-NAME induced rat or ECV304 cell lines through the Cell morphological pattern, Tunel assay, LDH activity, heart rate, blood pressure and immunohistochemistric analysis by Ondam-tang. As the result of this study, In group, the anti-apoptosis and necrosis in the cardiovascular system have a potential capacity for prevented, protected and treating the diseases of cardiovascular system, against the necrosis of rat and ECV304 cells with eNOS and calpain expression by L-NAME is promoted.

• The Journal of Internal Korean Medicine
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• v.26 no.1
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• pp.182-198
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• 2005

Object : This study was designed to research whether the protection and inhibitory effects of cardiovascular diseases in L-NAME induced rat or ECV 304 cell lines through the Cell morphological pattern, Tunel assay, LDH activity, heart rate, blood pressure and immunohistochemistric analysis by Boonsimgieum water extract Methods : Nitric oxide(NO) play an important role in normal and pathophysiological cells including as a messenger molecule, neurotransmitter, microbiocidal agent, or dilator of blood vessels and artheriosclerosis, hypertension, myocardial infarction, respectively. Endothelial cell products can modulate the magnitude of a response to a vasoconstrictor, as evinced by the greater constriction after endothelium removal or NO synthesis blockade. To investigate that Boonsimgieum in the potential contribution of the levels of nitric oxide generated by endothelial nitric oxide synthase (eNOS) and the mechanisms of protection against NG-nitro-L-arginine methyl ester (L-NAME), human ECV 304 cells, which normally do not express eNOS, were expressed by L-NAME. L-NAME stimulated rat or cells were found to be resistant to injury and delayed death following the Boonsimgieum. Inhibition of nitric oxide synthesis abolished the protective effect against L-NAME, thrombin and collagen exposure. Interestingly, such effects have been observed during stimulation with agents such as phenylephrine and KCl on L-NAME mediate rats, were damaged by the NOS inhibitor L-NAME. Result : As the result of this study, In group, the anti-apoptosis and necrosis in the cardiovascular system have a potential capacity for prevented, protected and treating the diseases of cardiovascular system, against the necrosis of rat and ECV 304 cells with Caspase 3 and calpain expression by L-NAME is promoted. Conclusion : these results demonstrate neuroprotective and memory enhancing effects of ZIBU, suggesting its beneficial actions for the treatment of AD.

• Journal of Life Science
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• v.29 no.2
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• pp.164-172
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• 2019

In Korea, shiitake mushroom, Lentinula edodes, is cultivated on artificial medium containing oak sawdust and wheat bran. The annual production of spent mushroom substrate (SMS) of shiitake, a byproduct of the mushroom industry, is estimated to reach over 50,000 tons per year. This study aimed to improve the use of SMS as a novel bioresource. Hot water extracts of SMS after the first and third harvest were prepared and their bioactivities evaluated. Hot water extracts of uninoculated medium and shiitake were used as controls. Extracts of SMS showed higher radical scavenging of DPPH anions, ABTS cations, nitrites, and a higher reducing power than those of shiitake or medium extracts. After the first and third harvests at 0.5 mg/disc, SMS extracts showed no antibacterial or antifungal activities against the pathogenic and food-spoilage bacteria and fungi. However, they showed good inhibitory activities against ${\alpha}$-glucosidase at 0.5 mg/ml. In addition, SMS extracts had strong anti-coagulation activities via their inhibition of thrombin, prothrombin, and blood coagulation factors without platelet aggregation activity. Our results suggested SMS should no longer be perceived as a useless byproduct but should be understood as a novel bioresource, the extracts of which could be developed as antioxidant, antidiabetic, and antithrombosis agents.

• Journal of Life Science
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• v.29 no.1
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• pp.52-59
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• 2019

The leave of Polygonum tinctorium (LPT) have been used for centuries as a traditional medicine and as a food ingredient and natural dye. The aim of the current study was to develop high-value added products using LPT. Hot water extract (HWE) and ethanol extract (EE) of LPT were prepared, respectively, and their bioactivity was evaluated. The extraction ratio for the HWE was 27.6%, which was two-fold higher than that of the EE. The contents of total polyphenol in the HWE and total sugar in the EE were 51.2 mg/g and 297.8 mg/g, respectively. The total flavonoid and reducing sugar contents were similar in the extracts, irrespective of the extraction solvent. The HWE did not show antimicrobial activity in a disc-diffusion assay, but the EE showed strong growth inhibition against gram-positive bacteria. The EE exhibited stronger DPPH and ABTS radical scavenging activities and reducing power than those of the HWE. The HWE was particularly effective as a scavenger of nitrite ($RC_{50}$ of $6.0{\mu}g/ml$). In an antithrombosis activity assay, the EE showed significant anticoagulation activity as determined by an extended blood coagulation time (thrombin time, prothrombin time, and activated partial thromboplastin time), in addition to platelet aggregation activity. The HWE also showed platelet aggregation inhibitory activity. This report provides the first evidence of antithrombosis activities of LPT. Our results suggest that LPT has potential as a new antioxidant and antithrombosis agent.