• Title/Summary/Keyword: anti-platelet aggregation

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Potential drug targets in the GPCR-$G{\alpha}_{12}/G{\alpha}_{13}$ signaling pathways

  • Kim, Sang-Geon
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2008.04a
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    • pp.89-99
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    • 2008
  • GPCRs are large families of cell surface receptors that transmit signals through conformational changes upon ligand activation and an interaction with the heterotrimeric G-proteins. GPCRs regulate the cell-signaling pathways and participate in the regulation of physiological processes through the G-proteins defined by their ${\alpha}$ subunits. A family of 20 G protein-coupled receptors (GPCRs) that provide a large class of tractable drug targets for new anti-inflammatory drugs and, in certain instances, for the treatment of the inflammatory indications such as atherosclerosis, rhinitis, asthma, pulmonary disease and arthritis. In view of the important findings showing that $G{\alpha}_{12}/G{\alpha}_{13}$ regulate the various cellular processes such as actin-stress fiber formation, neurite retraction, platelet aggregation, gene induction, and apoptosis, we became interested in whether, after coupling to the activated GPCRs, the G-proteins and their downstream molecules might be involved in the pathologic processes of chronic inflammatory diseases (e.g., liver fibrosis). In this symposium, the possible link of the G-proteins with the pathophysiology will be discussed with the aim of finding potential new drug targets.

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In-vitro Antithrombosis Activity of Different Parts of Sorbus commixta from Ulleung Island (울릉도 마가목의 다양한 부위의 항혈전 활성)

  • Kim, Mi-Sun;Seong, Ha-Jung;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.26 no.3
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    • pp.289-295
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    • 2016
  • Sorbus commixta, a flowering plant in the Rosaceae family, is native to Japan and Ulleung Island, Korea. This plant is also called maga-mok or mai-mok in Korea because the bud of the stem has a similar shape to the teeth of a horse. In this study, hot water extracts from different parts of S. commixta, such as leaf, stem, and immature and mature fruits, were prepared, and their antithrombosis and antioxidant activities were evaluated. The extraction yield and pH of stem extracts were 3.99% and 5.5, respectively. The stem extracts contained 89.2 mg/g of total polyphenols and 28.3 mg/g of total flavonoids. The hot water extracts prepared from the leaf, stem, immature, and mature fruit of S. commixta exhibited no hemolytic activity against human red blood cells, up to a concentration of 0.5 mg/ml. In an anticoagulation assay, the stem extracts showed strong extension in thrombin, prothrombin, and activated partial thromboplastin times, whereas the other extracts had no anticoagulation activity. In a platelet aggregation inhibitory activity assay, all the extracts tested had no inhibitory activity against human platelets. With regard to antioxidation activity, the stem extracts showed stronger radical scavenging activity and reducing power activity than the other extracts. The calculated RC50s, the concentration required for 50% radical scavenging activity, for DPPH anions, ABTS cations, and nitrite of the crude stem extracts were 119.7, 53.3, and 117.5 μg/ml, respectively, whereas they were 13.7, 5.2, and 14.9 μg/ml for DPPH anions, ABTS cations, and nitrite, respectively, for vitamin C. The results suggest that the stem extracts of S. commixta have strong potential for use as a novel resource for antithrombosis agents.

Effect of different drying methods on anti-oxidation and anti-thrombosis activities of Salicornia europaea (함초의 건조방법에 따른 항산화 및 항혈전 활성의 변화)

  • Sung, Hwa-Jung;Kim, Deuk Hoi;Sohn, Ho-Yong
    • Food Science and Preservation
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    • v.24 no.5
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    • pp.658-665
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    • 2017
  • The current study was performed to investigate the changes of bio-activities of Salicornia europaea (SE) depending on the different dry methods. The ethanol extracts were prepared from the freeze-drying SE (FD), hot-air drying SE (HD), and shade drying SE (SD). Their anti-oxidant and anti-thrombosis activities were compared. The yields of ethanol extraction in FD, HD, and SD were 14.4, 13.2 and 11.9%, respectively. The highest contents of total polyphenol (4.6 mg/g) and total sugar (23.4 mg/g) were shown in FD, whereas, the highest content of reducing sugar (14.6 mg/g) was observed in HD. In anti-oxidation activity assay, the FD and HD showed similar radical scavenging activities and reducing power. However, in SD, nitrite scavenging activity and reducing power were severely decreased. In anti-coagulation activity assay, the thrombin time (TT), prothrombin time (PT) and activated partial thromboplastin time (aPTT) of FD, HD and SD did not show significant changes at 5 mg/mL concentration. But the HD at 7 mg/mL had strong inhibitions against thrombin and blood coagulation factors. The platelet aggregation and hemolysis activities were not affected by dry methods. Our results suggest that both FD and HD are effective to maintain the functional ingredient of SE, and HD is economic and efficient dry process for production of functional food.

A New Processed Ginseng with Fortified Activity

  • Park, Jeong-Hill;Kim, Jong-Moon;Han, Sang-Beom;Kim, Na-Young;Surh, Young-Joon;Lee, Seung-Ki;Kim, Nak-Doo;Park, Man-Ki
    • Proceedings of the Ginseng society Conference
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    • 1998.06a
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    • pp.146-159
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    • 1998
  • A new processed ginseng with fortified activity is developed. The process comprise with the heat treatment of fresh or white ginseng at higher temperature and pressure than those used for the preparation of red ginseng. This new processed ginseng showed 7 times higher antioxidant activity and more than 30 times stronger vasodilating activity than those shown in raw ginseng. Other activities found in the new processed ginseng include cancer chemoprevention, antinephrotoxic, and antineurotoxic activities. Less polar ginsenosides isolated from processed ginseng exhibited anti-platelet aggregation activity and anti-cancer activity. Many ginsenosides were isolated from this new processed ginseng, namely 20(S)-$Rg_3$,20(R)-$Rg_3$, $Rg_5$, $Rg_6$, $F_4$, $Rh_4$,20(S)-$Rg_3$,20(R)-$Rg_3$ and $Rg_4$. In addition to these known compounds, seven new ginsenosides, named as gisenoside $Rk_1$, $Rk_2$, $Rk_3$, $Rs_4$, $Rs_5$, $Rs_6$, and $Rs_7$ were isolated. The major constituents of new processed ginseng were 20(S)-$Rg_3$,20(R)-$Rg_3$, $Rk_1$ and $Rg_5$ which are minors in red ginseng. Since the chemical constituents and biological activities of this new processed ginseng are quite different from those of white or red ginseng, we designated it as $'$sun ginseng (仙蔘)$'$.s;$.

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Preventive Effects of Aspirin on Cardiovascular Complications in Prostate Cancer Cases after Endocrinotherapy

  • Li, Xiao-Xia;Zhang, Yong-Gang;Wang, Dong;Chen, Yun-Fang;Shan, Yan-Hua
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.12
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    • pp.4909-4913
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    • 2015
  • Objective: To explore the preventive effect of aspirin on the cardiovascular complications in prostate cancer after endocrinotherapy. Materials and Methods: A total of 92 patients with prostate cancer were divided into observation group (n=44) and control group (n=48). The control group was treated with medical castration plus anti-androgenic drugs. Based on the above treatment, the observation group was added aspirin. The follow-up duration was 2 years. The changes of partial prothrombin time (PT), activated partial thromboplastin time (APTT), platelet aggregation rate (PAG), prostate-specific antigen (PSA) and serum testosterone (T) before and after treatment as well as incidence of cardiovascular disease were observed. Results: The 2-year survival rates of patients without cardiovascular disease in observation group and control group were 95.45% (42/44) and 72.92% (35/48), respectively, and significant difference was presented between two groups by comparison to the survival rates ($x^2=8.5453$, p=0.0035). There was no statistical significance between two groups as well as before and after treatment regarding PT (p>0.05). After treatment, APTT went down and PAG was gradually on the rise in control group, while PAG down and APTT on the rise increasingly in observation group. Significant differences were presented between two groups as well as before and after treatment (p<0.01). Both PSA and T levels were decreased significantly in two groups after treatment (p<0.01), but there was no statistical significant between two groups (p>0.05). Conclusions: Application of endocrinotherapy in prostate cancer can easily lead to occurrence of cardiovascular disease, but cardiovascular complications can be prevented by aspirin, without affecting the effect of endocrinotherapy.

Bibliographic Study on the Moschus used to Acute Stage of Stroke (중풍급성기(中風急性期)에 활용(活用)되는 사향(麝香)에 관(關)한 문헌적(文獻的) 고찰(考察))

  • Huh, Jae-Hyeok;Kim, Sae-Gil;An, Ill-Hoe;Shin, Sun-Ho;Moon, Byung-Soon;Sung, Gang-Kyung
    • The Journal of Korean Medicine
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    • v.16 no.2 s.30
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    • pp.100-114
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    • 1995
  • This bibliographic study was designed to research indications of the Moschus which was representatively used for resuscitation in acute stage of stroke throughout successive books of oriental medicine. Especially, in this study, severe cases with disturbance of consciousness and acute stage of stroke were investigated. The results were summarized as the followings: 1. The Moschus was dried material which secreted from aromatic vescicle of Moschus moschiferus L.. which was pungent in flavor, warm in nature, nontoxic and strongly aromatic. The Moschus removed the obstruction in the channels and used to early stage of stroke. 2. The Moschus was aromatic resuscitatable medicine, which recovered disturbance of consciousness due to stroke. 3. The Moschus had excitatory actions of respirtory center and vascular motor center, heart stimulating action, inhibitatory action of the platelet aggregation and anti thrombin action and recovered cerebral ischemic change. According to these actions, the Moschus could be used cerebral infarction. 4. Prescriptions included the Moschus was used to symptoms of unconsciousness, secretion, stuporous mental state, dysarthria, facial palsy and hemiplegia. That was Angungwoohwangh wan(安宮牛黃丸), Woohwangchungshimwon(牛黃淸心元), Sahyangsohaphangwon(麝香蘇合香元), etc. According to the above mentioned results, the Moschus was aromatic resuscitatable medicine which was used for symptoms of conscius disturbance, convulsion, sudden fainting etc., promoted cerebral blood flow and had good effect on acute stage of stroke and severe cases with conscious disturbance. Therefore, it is considered that the Moschus must be studied for effect of cerebral infarction and hemorrhage in clinic with animal's and pharmacological experimental results.

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Evaluation of in-vitro Antithrombosis Activity of Lees of Korean Traditional Wine (전통주 주박의 항혈전 활성 평가)

  • Kim, Mi-Sun;Lee, Ye-Seul;Kim, Jong Sik;Shin, Woo-Chang;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.24 no.8
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    • pp.865-872
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    • 2014
  • In this study, ethanol and hot water extracts of lees from Korean traditional wine (J-B, J-S, J-Y, J-H, and J-W) were prepared, and their effects on blood coagulation, platelet aggregation, and hemolysis of human red blood cells (hRBCs) were investigated to develop functional food ingredients from lees. The pH and brix of the lees ranged from 3.90 to 4.29 and 5.0 to $27.0^{\circ}$, respectively, and there was a huge difference in the water and ethanol content among the lees. The nuruk and additives used affected the color and physicochemical properties of lees. The J-W takju made from only rice and traditional nuruk, which has $13^{\circ}$ brix and 1.8% of alcohol, has potential as functional food ingredient. With regard to the extraction yields of lees, higher yields were obtained from J-H, which contains different medicinal plants, in ethanol, followed by J-W, J-B, J-S, and J-Y. Higher extraction yields of lees were obtained from J-S in hot water, followed by J-B, J-W, J-H, and J-Y, respectively. The ethanol extract of J-H and the hot water extract of J-Y had the highest contents of total polyphenol and total flavonoids among the lees extracts. The 10 lees extracts did not show hemolysis activity against hRBCs up to 5 mg/ml. In an anticoagulation activity assay, the ethanol extracts of three yakju lees (J-B, J-S, and J-Y) and the hot water extract of J-W inhibited thrombin activity, whereas the hot water extract of J-B, J-S, and J-H inhibited blood coagulation factors. In an antiplatelet aggregation activity assay, only the J-W takju lees showed significant inhibition activity. Our results suggest that lees from traditional wine had high potential as a novel antithrombosis agent.

Evaluation of the Useful Bioactivities of Spent Mushroom Substrate of Shiitake (표고버섯 수확 후 배지의 유용 생리활성 평가)

  • Sung, Hwa-Jung;Pyo, Su-Jin;Park, Jong-Yi;Sohn, Ho-Yong
    • 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.

DENTAL TREATMENT OF THE PATIENT WITH AUTISM AND HEMOPHILIA A UNDER GENERAL ANESTHESIA A CASE REPORT (자폐증상이 있는 혈우병 A 환아의 전신 마취를 통한 치과적 치험례)

  • Park, Kyeong-Sun;Lee, Keung-Ho
    • Journal of the korean academy of Pediatric Dentistry
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    • v.23 no.3
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    • pp.593-600
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    • 1996
  • This case report is a treatment of patient with hemophilia A and autism. The patient's chief complaint was treatment of dental caries on entire dentition and he has an impacted mesiodens located on the apex of the upper right primary central incisor. The patient was consulted with pediatrician and anesthetist about the detailed discussion of the complexities of hemorrhagic disorder. Because he had some problems of behavior management and bleeding, the treatment was done under the gerneral anesthesia. The following results were obtained. 1. Consult with the patient's physician and hematologist about the replacement therapy and bleeding tendency. 2. For the severe hemophiliac child who requires extensive or surgical treatment, general anesthesia may be indicated for the comprehensive care. 3. For the hemophiliac child who has a behavior management problem due to autism and other defects, general anesthesia may be considerable. 4. Care must be taken during dental procedures not to causing a bleeding. 5. Local hemostatic methods must be acquired for the emergency state. 6. Neve prescribe aspirin or non-steroidal anti-inflammatory drugs such as ibuprofen, indomethacin, and phenylbutazone. These drugs affect platelet aggregation and exaggerate the bleeding defect. 7. Do not be afraid of hemophiliac patient, and never compromise quality of dental care.

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Antithrombotic Activity of Hermetia illucens (Black Soldier Fly) (동애등에의 항혈전 활성)

  • Pyo, Su-Jin;Won, Jun;Kang, Deok-Gyeong;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.30 no.4
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    • pp.386-393
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    • 2020
  • Insect industry has been focused as production of food, animal feed, pollinator and for environmental remediation. Hermetia illicens, called as black soldier fly (BSF) is famous as nutritive feed. In this study, to evaluate the antithrombotic activities of BSF, the larvae (instar 2~6), pupae, residue after adult emergence [RAAE] and adult of Hermetia illicens [black soldier fly, BSF] were collected and their ethanol extracts were prepared. Growth of BSF larvae was very rapid and the weight of larvae was increased to 25-folds during 10 days cultivation. The ethanol extraction ratios showed from 1.0% (pupae) to 18.5%(adults). The highest total polyphenol, total flavonoid, and total sugar contents were observed in RAEE (17.2 mg/g), pupae (3.4 mg/g), and instar 6 (37.6 mg/g), suggesting that metabolic changes occur during the life cycle of the BSF. Anti-coagulation assay showed that extracts of RAEE, instar 6 and pupa of BSF significantly inhibited thrombin, prothrombin, and blood coagulation factors. Furthermore, the extracts of RAEE, instar 3 and adult of BSF showed a strong platelet aggregation inhibitory activity. Our results suggest that pupae and RAEE of BSF have potential as antithrombotic agents. This is the first study to provide evidence of the antithrombotic activity of the BSF and bioactivity alterations during its life cycle.