• Biomolecules & Therapeutics
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• v.18 no.2
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• pp.205-210
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• 2010

Several studies have shown that plant-derived polyphenols reduce cardiovascular accidents in high-risk patients and the inhibition of platelet function may be responsible for part of this benefit. Lindera obtusiloba is widely used in traditional herbal medicine for the treatment of cardiovascular and inflammatory diseases. Therefore, the antiplatelet and antithrombotic activities of Lindera obtusiloba Extracts (LOE) on in vitro platelet aggregation, radical scavenging activity and in vivo murine pulmonary thrombosis were examined. LOE was able to directly scavenge the stable DPPH radical in a concentration-dependent manner and its $IC_{50}$ value was 3.9 ${\pm}$ 0.1 ${\mu}g$/ml. LOE significantly inhibited collagen- and ADP-induced platelet aggregation in a concentration-dependent manner and its $IC_{50}$ value is 0.9 ${\pm}$ 0.1 mg/ml and 0.4 ${\pm}$ 0.1 mg/ml respectively. The inhibitory effect of LOE was comparable to aspirin ($IC_{50}$ values were 1.0 ${\pm}$ 0.5 and 1.0 ${\pm}$ 0.7 mg/ml, respectively). Furthermore, oral administration of LOE suppressed the death of mice with pulmonary thrombosis induced by intravenous injection of collagen plus epinephrine. Taken together, our results suggest LOE may be a promising candidate for antithrombotic agent, and the antithrombotic effect of LOE may be due to, at least in part, antiplatelet activity.

• Korean Journal of Food Science and Technology
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• v.46 no.1
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• pp.87-93
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• 2014

We investigated the effects of an ethanol extract from Perilla frutescens sprouts (PFSE) as an antioxidant, and its effects on edema and inflammation in RAW 264.7 cells and HMC-1 cells. The antioxidant activities (DPPH and ABTS radical scavenging) of PFSE were similar to those of butylated hydroxytoluene (BHT) and (${\pm}$)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid (Trolox). We also investigated the anti-inflammatory effects of PFSE on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells and HMC-1 cells stimulated with phorbol 12-myristate 13-acetate (PMA) with the calcium ionophore A23187. TNF-${\alpha}$ and IL-$1{\beta}$ production, which had been increased by treatment with LPS or PMA plus A23187, were significantly inhibited by PFSE in a dose-dependent manner. Furthermore, PFSE significantly reduced the xylene-induced ear edema and the carrageenan-induced paw edema of ICR mice in a dose-dependent manner. The effects of PFSE (200 mg/kg) in reducing ear and paw edema were similar to those of aspirin (50 mg/kg). These results suggest that PFSE can be potentially used as a medicine for treating oxidative stress, an edematous and inflammatory disease.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.70-81
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• 2000

DA-5018 is a synthetic capsaicin derivative under development as a non-narcotic a analgesic ag$\varepsilon$nt. DA-50 18 showed a potent analgesic activity against acute and chronic pain m model(Tablel, 2.), but it had a narrow margin of safety. DA-5018 did not bind to opioid(${\kappa}, {\delta}, {\mu}$), NKl, CGRP receptors in vitro and its analgesic effect was not antagonized by naloxone, a and it did not develop analgesic tolerance. In addition DA-5018 had no inhibitory effects against c cyclooxygenase and 5-lipooxygenase activities. DA-5018 significantly increased the relcase of substance P from the slices of the rat spinal cord. These results suggest that DA-50 18 is not a narcotic nor aspirin-like analgesic and the release of substance P is one of analgesic mechanism of action of DA-5018. We found that DA-5018 was almost ten times more potent and was at l least IOO-times less irritable compared to capsaicin. Accordingly development of topical formula was adopted. Topical formula was desiged and screened by flux test of DA-5018 using hairless mouse skin and several formulas were selected. With these topical formulas we a assessed the analgesic efficacy and carried out the toxicity, skin irritation and pharmacokinetic studies. In streptozotocin-induced hyperalgesic rat and 50 % galactose-fed hyperalgesic rat as diabetic pain models, DA-5018 cream increased the pain thresh이ds up to 77.0% and 24.4% respectively, while Zostrix-HP(capsaicin cream) incr$\varepsilon$as cd by 65.9% and 21.0%. DA-5018 c cream showed a good analgesic effect as welI in FCA-induced arthritic rat. DA-5018 cream did not show any toxicological signs in acute and chronic toxicity test and had little skin irritation in car swclIing and scratching t$\varepsilon$st. Pharmacokinetics of DA-50 18 were studied after topical application of ${14}^C$-Iabelled or unlabelIed DA-5018 cream. Plasma and skin concentrations c except applied skin wcre below the dctection limit and after 7-day cummulative application, plasma concentrations were also below detection limit DA-50 18 may have an advantag$\varepsilon$ ov$\varepsilon$r c capsaicin and is now being developed as a topical agent for the treatment of pains. DA-50 18 cream was approved for Korean IND and is now under a Phase II clinical study for arthritic pain a after finising Phase I study. DA-50 18 was also liscensed out to Stiefel Company in America in

• Korean Journal of Plant Resources
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• v.32 no.4
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• pp.282-289
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• 2019

Gastritis is an inflammatory disease involving the stomach and is caused by several factors, including stress, non-steroidal anti-inflammatory drugs such as aspirin, liquor, and Helicobacter pylori. In Korea, Leonurus japonicus Houttuyn (LJW) has been used as traditional medicine for vaginal bleeding, hematuria, and bruise. Previous studies have reported that LJW exhibited hepatoprotective, cardioprotective, and anti-hyperlipidemic effect. However, the effect of the water extract of LJW on gastritis was not elucidated. Thus, we evaluated the anti-gastric effect and genotoxicity of LJW. LJW effectively prevented the degeneration of surface mucous cells and glandular epithelial cells and vascular congestion induced by HCl/EtOH. Micronucleus assay indicated that the rate of micronucleated polychromatic erythrocytes/polychromatic erythrocytes was not significantly different compared that of the control. Further experiments are required to determine the role of LJW in the gastric injury process such as cyclooxygenase signaling pathway and the secretion of mucus in the stomach.

• Journal of Life Science
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• v.28 no.9
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• pp.1068-1075
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• 2018

Kaempferia parviflora, an herbaceous plant in the family Zingiberaceae, is popular in many tropical regions. It is called as black ginger or krachaidum in Thailand and Laos, and its raw or dried root have been used as spices and teas. The rhizomes also have been traditionally used to treat gastrointestinal disorders, ulcers, gout, dysentery, allergies and to improve physical work capacity. Recently, its anti-obesity, anti-oxidant, anti-inflammatory and blood clot-lysis activities were reported. In this study, the anti-thrombosis activity of black ginger was investigated, since improvement in blood fluidity leads to the prevention of various lifestyle-related diseases. The hot water and ethanol extract and their subsequent solvent fractions (hexane, ethylacetate, butanol fractions and water residue) were prepared, and their anti-coagulation and platelet aggregation inhibitory activities were determined, respectively. Among the black ginger extracts and their fractions, the ethylacetate fraction (EAF) of ethanol extract only showed significant extensions of blood coagulation time determined by thrombin time (TT), prothrombin time (PT), and activated partial thromboplastin time (aPTT). At 5 mg/ml concentration, TT, PT and aPTT were extended to 1.22, 1.49 and >15-folds compared to non-treatment. The EAFs of ethanol and hot water extract showed strong inhibitions against collagen-induced platelet aggregations, which are comparable to inhibitions of aspirin. Also the EAFs from black ginger did not show any hemolysis activity against human RBC up to 0.5 mg/ml. Our results suggest that the EAF of black ginger has a potential as novel anti-coagulation and ant-platelet aggregation agent. This report provides the first evidence of anti-coagulation activity of black ginger.

• The Journal of Dong Guk Oriental Medicine
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• v.8 no.2
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• pp.115-129
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• 2000

The cause that the increase of animality fat intakes, under exercise, fatness, adding the stress, advanced age etc., the occurrence rate of the circulation system disease has been increased. And the thrombosis importantly came to the front as the risk factor of these circulation system's disease. Nowadays, the ischemic disease has especially discussed, for example the angina or myocardial infarction, originated in thrombosis that came from the platelet aggregation. In the western medicine, as the cure and prevention, using the aspirin or ticlopidine for platelet aggregation suppressant. But in the , the curing method must be used properly according to the pectoralgia or heartache's kind, state, grade. The platelet do not attache to the normal hemangioendothelial cell. But when it stimulated by endothelium peronia and so on, it attache to the injury endothelium or rise aggregation between the platelet. On this time, it secrete the platelet aggregation inducer as like ADP, thromboxane A2 from the inside of platelet. So it has first defensive function through the aggregation augment that prevent the celerity consumption of blood. But the activation of abnormal platelet occur the platelet grume and thrombogenesis. So it bring up the occlusive angiosis, so to speak, cardiovascular disease, cerebrovascular disease, arterial sclerosis. In oriental medicine, the thrombosis in the category of blood stasis and this blood stasis present the generalise or local blood circulation disturbance that generated by all kinds of pathological fact or blood stream retention accompanying with a series of syndrome. As the syndrome, stabbing pain fixed at certain region, squamous and dry skin, fullness and pain of the chest and hypochondrium, firmness and fullness of the lower abdomen, black stool, dark purple tongue or with ecchymoses and petechiae etc.. has been created. And it becomes the pathopoiesis cause that the convulsion and palpitation, severe palpitatiion, tympanites, the symtom complex with a mass or swelling in the abdomen, insanity, stricken by wind etc.. Moreover, it used the drugs for invigorating blood circulation and eliminating blood stasis or drugs for removing blood stasis for all kinds of syndrome through the blood stasis. And the drugs for activating the blood circulation, such as Salviae Radix, Angelicae Sinensis Radix, Persicae Semen, Achyranthis Radix, Cnidii Rhizoma, Carthami Flos are used for that. And it is used to the herbs of insects that has strong effect about the disintergrating blood stasis such as Hirudo, Scolopendrae Corpus, Buthus, Lumbricus etc.. On this study, It used Geijibokryunghwan(GBH) and the consisting herbs to investigate the influence of platelet aggregation about drugs that used to improvement various symptoms created by the thrombosis in oriental medicine. GBH formula has as formula recorded in the , action of 'eleminating the evil and not impairment of healthy energy' and 'promoting the flow of QI and cold and heat, so used for the expel blood stasis herbs from the ancient. Therefore we investigated the restraint effect of GBH and the consisting herbs about the platelet agregation induced to the ADP, AA or collagen. The conclusion is following. 1. When it added the aggregation inducer after that it added GBH and individual consisting herbs in the PRP, GBH showed the (+) inhibition effect on the platelet aggregation and it showed the (+) inhibition effect in the individual consisting herbs as like Paeoniae Radix and Moutan Cortex Radicis. 2. It showed the (+), (+,++) inhibition effect on the platelet aggregation in Paeoniae Radix Hoelen, Paeoniae Radix Moutan Cortex Radicis, Hoelen Moutan Cortex Radicis etc. 3. In the aggregation inhibition activating on the difference of density, GBH showed strong inhibition effect to the aggregation state induced to collagen, and it showed the inhibition effect in the individual consisting herbs as like Paeoniae Radix and Moutan Cortex Radicis about the aggregation induced by the collagen. 4. It showed the strong inhibition effect about the aggregation induced by the collagen in Paeoniae Radix Hoelen, Paeoniae Radix Moutan Cortex Radicis, Hoelen Moutan Cortex Radicis etc Like this, as confirm GBH and the individual consisting herb's inhibition effect of platelet aggregation, We considerated that GBH and the individual consisting herbs have practical applicational value of clinical trial in the thrombosis caused by platelet aggregation.

• Clinical and Experimental Pediatrics
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• v.52 no.6
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• pp.680-688
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• 2009

Purpose : Cysteinyl leukotrienes are important proinflammatory mediators in asthma. Recently, it was suggested that a promoter polymorphism in the genes encoding for leukotriene C4 synthase (LTC4S), a key enzyme in the leukotriene synthetic pathway, and cysteinyl leukotriene receptor 1 (CysLTR1) might be associated with aspirin-intolerant asthma. We investigated whether polymorphisms in LTC4S and CysLTR1 genes or their interactions were associated with the asthma phenotype, lung function, or bronchial hyperreactivity (BHR) in Korean children. Methods : A total of 856 asthmatic children and 254 non-asthmatic controls were enrolled; a skin prick test, lung function test and bronchial provocation test were performed. Of those enrolled, 395 children underwent exercise challenge tests. The LTC4S A(-444)C and CysLTR1 T(＋927)C were genotyped by polymerase chain reaction-restriction fragment length polymorphism analysis. Results : Of those enrolled, 699 children were classified as having atopic asthma and 277 children, as having exercise-induced asthma (EIA). LTC4S and CysLTR1 polymorphisms were not associated with atopic asthma, EIA, or asthma per se. Lung function and BHR were not significantly different between the wild type (AA or TT) and the variant (AC＋CC or TC＋CC) genotypes in asthmatics, atopic asthmatics, and EIA (＋) asthmatics, while total eosinophil counts were higher in the variant type of LTC4S than in the wild type in atopic asthmatics. There were no associations between the gene-gene interactions of LTC4S and CysLTR1 genotypes and the asthma phenotypes. Conclusion : LTC4S A(-444)C and CysLTR1 T(＋927)C polymorphisms and their gene-gene interactions are not associated with asthma phenotype, lung function, or BHR in Korean children.