• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.236-236
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• 1994

Acetylsalicylic acid (ASA)와 고려홍삼의 항산화 성분인 maltol을 축합하여 신물질 aspalatone을 합성하고, 흰쥐에서의 지혈시간 연장 효과, 항혈소판 응집 억제 (in Vitro, ex ViVO) 효과 및 생쥐의 혈전 모델을 이용한 항혈전 (in vivo) 효과를 연구하였다. SD계 웅성 흰쥐에 15 mg/kg의 낮은 용량으로 경구투여 할 경우, aspalatone과 ASA는 각각 최소한 8일 연속투여후 지혈시간을 유의적으로 연장시켰으며 같은 용량으로 10일 간 경구투여. 하였을 때, aspalatone 투여군은 대조군에 비하여 지혈시간이 57% (p<0.005) 연장된 반면, ASA 투여군은 44% 연장되었다. 반면, aspalatone의 아세칠 기를 갖지 않는 salicylic acid maltnl ester는 같은 용량에서 지혈시간을 유의적으로 연장시키지 않았다. Aspalatone은 in vitro에서 collagen에 의해 유도된 흰쥐 혈소판 응집을 강력하게 억제하였으나 (IS$_{50}$ = 0.18 mM), ASA와 마찬가지로 ADP에 의한 응집은 억제하지 않았다. Aspalatnne과 다른 대조약물들의 ex vivo에서의 혈소판 응집 억제능은 ASA>dipyridamdle(equation omitted)aspalatone>ticlopidine의 순이었다. 1회 경구투여로 aspalatone은 생쥐의 collagen에 의한 혈전에 기인하는 치사율을 억제하였다 (ED$_{50}$ = 32mg/kg). Aspalatone을 10일 간 투여하면 유효용량이 현저히 감소하여 20 mg/kg에서 치사율을 90% (p<0.001) 억제하였으며, 이러한 항혈전 효과는 투여중단 4일 후에도 지속되었다. 또한, 경구투여시 위궤양을 유발하는 ASA (ulcer index : 29 mm 200 mg/kg p.o.)와는 다르게 aspalatone은 위궤양을 유발하지 않는다는 장점을 갖는다 (0.71 mm, 800 mg/kg p.o.). In vitro에서 malondialdehyde 생성 억제를 지표로 한 aspalatone의 항산화 활성 ($IC_{50}$/ = 0.11 mM)은 maltol ($IC_{50}$/ = 0.084 mM)과 유산하다. 이러한 실험결과를 토대로 하여 aspalatone을 위궤양을 유발하지 않는 항혈전 신약으로 개발하기 위한 연구가 진행 중이다.

• Journal of the Korean Society of Food Science and Nutrition
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• v.34 no.5
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• pp.593-598
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• 2005

Antithrombosis and antioxidant activity of the methanol extracts, which were prepared from 51 different brands of rice, were evaluated to investigate bioactive-substances. Among them, the extract of sample No. 2, 25, 40 and 41 showed strong thrombin inhibition activities ($401\~764\%$ inhibition at 5 mg/mL), and the extract of sample No. 5, 9, 23, 36, 44 and 48 showed strong DPPH scavenging activities ($40.8\~64.1\%$ at 0.4 mg/mL), respectively. The average contents of total flavonoid and polyphenol with 50 brands of rice were 51.89 mg/kg and 195.23 mg/kg, respectively. However, the activities were not linked with the contents of flavonoid and polyphenol. By the treatment at $100^{\circ}C$ for 10 min, the activities of the selected rices were severely decreased. Maximal remaining activities of antithrombosis and antioxidant were $208\%$ of No. 40 and $23.2\%$ of No. 48, respectively. These results support a functional superiority of rice-based livelihood, and suggest that the development of healthy food using functional ingredients of rice is possible.

• Journal of Life Science
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• v.30 no.5
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• pp.443-451
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• 2020

Recently, thrombotic diseases have become rapidly more prevalent due to Westernized lifestyles and high-fat diets. In this study, the anti-thrombosis activities of the aerial parts of Sageretia thea were evaluated using ethanol extracts of the leaf (ST-L), branch (ST-B), and fruit (ST-F), and their anti-coagulation, platelet aggregation inhibition, and hemolytic toxicity were assessed. In comparison to the ST-F extract, the ST-B exhibited 6.7 times more polyphenol content, and the ST-L had 2.7 times more total flavonoid content. The ST-L and ST-B extracts showed stronger inhibitions of thrombin, prothrombin, and blood coagulation factors than aspirin, berry extracts, or commercial oriental herbs. Furthermore, ST-L and ST-B showed superior platelet aggregation-inhibitory activities than aspirin. The ST-F extract demonstrated only minor anti-thrombosis effects, and none of the extracts showed hemolysis against red blood cells up to 1 mg/ml. Phenolic acid and flavonoid analysis of the ST-L and ST-B extracts showed abundant rutin, isoquercitrin, and astragalin as the major active compounds. Further research on the anti-thrombotic activity of isoquercitrin, a rare flavonoid from quercetin, is necessary. This is the first report of isoquercitrin in Sageretia thea, and our results suggest that ST-L and ST-B extracts could therefore developed as anti-thrombosis agents.

• Korean Journal of Food Science and Technology
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• v.41 no.4
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• pp.423-427
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• 2009

This study investigated antithrombotic and hypocholesterolemic activities of defatted soybean grits (DSG) and fermented DSG (FD). The FD was prepared by the solid state fermentation using Bacillus subtilis NUC1 at $40^{\circ}C$ for 24h. The water extracts of fermented DSG (FDW) exhibited higher fibrinolytic activity and inhibition of platelet aggregation induced by ADP than water extracts of DSG (DW). However, the DW and FDW inhibited HMG-CoA reductase activity and significantly decreased the intracellular cholesterol contents in HepG2 cells. In addition, DW treatment did not show any cholesterol adsorption capacity, while FDW demonstrated the highest cholesterol adsorption by 90%. The results suggest that fermented DSG have significant antithrombotic and hypocholesterolemic effects in vitro and these activities were improved during fermentation by B. subtilis NUC1.

• Microbiology and Biotechnology Letters
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• v.37 no.3
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• pp.266-272
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• 2009

The annual productions of yam and its aerial bulbils are estimated to 5,000 and 2,500 ton, respectively. But the majority of bulbils had been discarded without specific use. In this study, methanol extract and its organic solvent fractions were prepared from bulbils of Dioscorea batatas Decne, and their antimicrobial, antithrombin, and antioxidant activities were evaluated, respectively. The methanol extract contained 58.98% of water-soluble materials as like yam's extract. But the bulbils's extract contained 12-folds of total polyphenol and 3.4-folds of total flavonoids compared than yam's extract, respectively. For antimicrobial activity the hexane and ethyl acetate fraction showed strong antibacterial activity at $500{\mu}g/disc$ concentration against gram-negative and gram-positive bacteria. Antifungal activity was not observed in any fractions. Strong antithrombin activity was found in the hexane fractions. At 4.8 mg/mL concentration thrombin time (TT) was over 300 sec, which is 4-folds extended than the TT of yam. In a while, the ethyl acetate fraction showed strong DPPH scavenging activity ($IC_{50}$ of $38.1{\mu}g/mL$), SOD-like activity and reducing power, which are comparable to vitamin C or BHT. Our results suggest that the bulbils of yam as yam tuber have useful bio-activities, such as antibacterial, antithrombosis, and antioxidant activity.

• Microbiology and Biotechnology Letters
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• v.42 no.3
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• pp.285-292
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• 2014

In the course of study for development of functional food ingredients from aged black garlic (ABG), heat-treated ripe bulbs of Allium sativum L., the water extracts from raw-garlic (RG) and ABG, and the subsequent organic solvent fractions of ABG were prepared, and their antioxidant, antimicrobial, and antithrombosis activities were compared. The extraction yield of ABG was 4-folds higher than that of RG, and the contents of total polyphenol, total flavonoid, total sugar and reducing sugar in the ABG extract were 4-folds, 1.56-folds, 3.36-folds and 6.75-folds higher than those of the RG extract, respectively. In antioxidation activity assay, the extract of ABG showed minor scavenging activity against DPPH anion, but revealed strong scavenging activity against ABTS cation and nitrite. Especially, the ethylacetate fraction from the ABG extract demonstrated stronger antioxidation activity than the RG extract and other fractions. Although the antimicrobial and antithrombosis activities of the RG extract did not appear in the ABG extract, the ethylacetate fraction from the ABG extract had antibacterial activity against Staphylococcus aureus and Bacillus subtilis, and strong antithrombosis activity via the inhibition of prothrombin, blood coagulation factors and platelet aggregation. All extracts and fractions did not show any hemolytic activity against human red blood cells up to 5 mg/ml. Our results suggest that the ethylacetate fraction of ABG could be applicable to the development of functional food ingredients for antithrombosis agents.

• Food Engineering Progress
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• v.13 no.4
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• pp.326-334
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• 2009

Blood coagulation and aggregation of platelet are crucial events in the pathogenesis of various ischemic diseases. The substance which can prevent blood coagulation and platelet aggregation was extracted from wood ear mushroom (Auricularia auricular-judae) and its anticoagulation activity was investigated. The dried A. auricular-judae was extracted with 0.1 N NaOH and its supernatant was further extracted with methanol and ethanol followed by $H_{2}O$. The resulting methanol soluble fraction showed significant antithrombotic activity in activated partial thromboplastin time, thrombin time, and prothrombin time assays with values of 100, 124, and 54 sec, respectively. This active substance was purified with DEAE-Sepharose CL6B and Sephacryl 400-HR and was found to be polysaccharide with the average molecular weight of over 150 kDa. This polysaccharide was xyloglucomannan of which the main component was mannose, and its anticoagulant activity was mostly mediated by inhibition of thrombin activity.

• Proceedings of the Korean Nutrition Society Conference
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• 1994.05a
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• pp.50-50
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• 1994

• Herbal Formula Science
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• v.4 no.1
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• pp.75-98
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• 1996

• Food Industry And Nutrition
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• v.5 no.1
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• pp.57-60
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• 2000