• Title/Summary/Keyword: Thromboplastin

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Effects of the AngiotensinII $AT_1$ Receptor Antagonist SK-1080 on Ischemia/reperfusion in Isolated Rat Hearts and on Platelet Aggregation and Coagulation in Human Blood (Angiotensin II $AT_1$ 수용체 길항제인 SK-1080의 적출심장에 대한 허혈후 재관류시의 작용 및 혈소판응집과 혈액응고에 대한 효과)

  • Woo, Su-Kyoung;Choi, Sang-Su;Lee, Byung-Ho;Kwon, Kwang-Il
    • YAKHAK HOEJI
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    • v.44 no.6
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    • pp.558-565
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    • 2000
  • SK-1080 is one of the newly developed orally active nonpeptide angiotensinII $AT_1-receptor$ antagonist that selectively acts at $AT_1$ receptor with high affinity. The cardiac effect on ischemia/reperfusion injury of SK-1080 was compared with those of losartan, a prototype of this class, in isolated rat hearts. Isolated perfused rat heart was pretreated with drug for 10 min and then subjected to global ischemia for 30 min followed by reperfusion with- or without drug for 30 min. The possible additive effect of SK-1080 on the platelet aggregation and coagulation in human blood was also studied. We investigated whether SK-1080 effects the platelet aggregation induced by ADP, a platelet agonist partially dependent on $thromboxaneA_2$. The clotting times in the prothrombin time (PT) and activated partial thromboplastin time (APTT) were also examined in human plasma in vitro as coagulation screening test. SK-1080 improved reperfusion function (LVDP, left ventricular developed pressure; PRP, rate-pressure product) in a dose-dependent manner. SK-1080 reduced ADP-induced platelet aggregation compared with vehicle but less than losartan, and did not affect clotting times.

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Anticoagulation and Anticancer Constituents from Eugenia caryophyllata Thunb

  • Han, Kyung-Min;Kim, Dong-Hyun;Ahn, Eun-Mi;Lee, Youn-Hyung;Chung, In-Sik;Kim, Dae-Keun;Kwon, Byoung-Mog;Kim, Sung-Hoon;Baek, Nam-In
    • Korean Journal of Medicinal Crop Science
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    • v.15 no.2
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    • pp.82-88
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    • 2007
  • From the EtOAc fraction of Eugenia caryophyllata, four compounds were isolated through activity-guided silica gel column chromatography, From the result of spectroscopic data including NMR, MS and IR, the chemical structures of the compounds were determined as 1-allyl-4-hydroxy-3-methoxybezene acetate (eugenol acetate, 1), 1-allyl-4-hydroxy-3-methoxybezene (eugenol, 2), $3{\beta}-hydroxyolean-12-en-28-oic$ acid (oleanolic acid, 3) and $2{\alpha}$, $3{\beta}-dihydroxyolean-12-en-28-oic$ acid (maslinic acid, 4). Compounds 3 and 4 were isolated for the first time from this plant. Also, compounds 1, 2 and 3 exhibited relatively high platelet aggregation inhibitory activity with the $IC_{50}$ values of 0.24, 0.09 and 0.07 mM, respectively. Compound 2 significantly prolonged activated partial thromboplastin time (aPTT) with the value of $124{\pm}11.2$ seconds as compared to the control with the value of $37.5{\pm}2.2$ seconds at the concentration of 50 ${\mu}g/ml$. Compounds 1 and 3 revealed inhibitory activity on farnesyl protein transferase (FPTase) with the $IC_{50}$ values of 0.49 and 0.24 mM and compounds 1 and 2 highly inhibited the growth of rat-H-ras cells with the $Gl_{50}$ values of 6.63 and 5.70 ${\mu}M$, respectively.

Effects of Sopoongtang on the Cardiovascular System in the Experimental Animals (소풍탕(疎風湯)이 실험동물(實驗動物)의 심혈관계(心血管系)에 미치는 영향(影響))

  • Jeong, Jang-Gyun;Mun, Byeong-Sun
    • The Journal of Internal Korean Medicine
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    • v.16 no.1
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    • pp.197-213
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    • 1995
  • The present experiment was desinged to investigate the effects of Sopungtang water extracts on the Cardiovascular System in the Experimental Animals. Thus, the changes of blood pressure and heart rate were measured after oral administration. Measurments of Mortality rate were observed for measuring the effect of Sopungtang water extract. Sopungtang water extract against pulmonary thromboembolism induced by collagen the mixture(0.1ml/10g, 2mg/kg B.W) plus serotonin(5mg/kg B.W) in mouse. The effects of Sopungtang water extract were examined by observing the change of collagen-induced platelet aggregation, coagulation activity, ex vivo and in vitro fibrinolytic activity of euglobulin fraction in rats. The results were summarized as followings. 1. Sopungtang dropped the blood pressure in spontaneous hypertensive rat. 2. The drug increased the auricular blood flow in rabbit. 3. The drug relaxed the artery contraction by pretreated norepinephrine in rat. 4. The drug inhibited the death rate of mouse which was led to thromboembolism by serotonin and collagen. 5. The drug inhibited the platelet aggregation in rat. 6. The drug prolonged the prothrombin time and activated partial thromboplastin time on the test of plasma coagulation factor activity in rat, but was not valuable. 7. The drug increased the antithrombin activity in rat and the fibrinogen lyses time was reduced and lyses area was increased. 8. Sopungtang reduced fibrinogen lyses time of rat in vitro assay. According to the above mentioned results, Sopungtang increased the blood flow and dropped the blood pressure by the dilation of blood vessel. And the drug presented the antithrombin acivity, inhibited the platelet aggregation.

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Study on the Antiinflammatory, Anticoagulative and Analgesic effects of Sambitang in the experimental animal model (삼비탕(三痺湯)의 항염(抗炎), 항응고(抗凝固) 및 진통효과(鎭痛效果)에 대(對)한 연구(硏究))

  • Rhy, Jun-Kiu;Lee, Young-Goo;Moon, Byung-Soon
    • The Journal of Internal Korean Medicine
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    • v.19 no.2
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    • pp.88-106
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    • 1998
  • This study was designed to elucidate the antiinflammatory, cardiovascular, antithrombotic, and analgesic effect of Sambitang. The antiinflammatory effects was measured by the method of carrageenin induced edema, protein leakage test using CMC-pouch, and the effect of Sambitang on the cardiovascular system was observed by the change of flow rate of Ringer solution in the vascular system in the ear of rabbit, and the contraction and dilatation of rat tail artery. Death rate, platelet aggregation, plasma coagulation activity was observed for the measurement of the anticoagurative effect of Sambitang, and the analgesic effect was measured by the acetic acid method and hot plate method. The result was as follows: 1. Sambitang administration, edema and protein leakage was significantly decreased. 2. The drug increased the auricular blood flow in rabbit. 3. The drug relaxed the artery contraction by pretreated norepinephrine in rat. 4. The drug inhibited the death rate of mouse which was led to thromboembo- lism by serotonin and collagen. 5. The drug inhibited the platelet aggregation in rat. 6. The drug prolonged the prothrombin time and activated partial thromboplastin time on the test of plasma coagulation factor activity in rat, but was not valuable. 7. The slight anagesic effect of Sambitang extract was confirmed by the observation of writhing syndrome, paw licking time, and escape time.

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Differential Effects between Cigarette Total Particulate Matter and Cigarette Smoke Extract on Blood and Blood Vessel

  • Park, Jung-Min;Chang, Kyung-Hwa;Park, Kwang-Hoon;Choi, Seong-Jin;Lee, Kyuhong;Lee, Jin-Yong;Satoh, Masahiko;Song, Seong-Yu;Lee, Moo-Yeol
    • Toxicological Research
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    • v.32 no.4
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    • pp.353-358
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    • 2016
  • The generation and collection of cigarette smoke (CS) is a prerequisite for any toxicology study on smoking, especially an in vitro CS exposure study. In this study, the effects on blood and vascular function were tested with two widely used CS preparations to compare the biological effects of CS with respect to the CS preparation used. CS was prepared in the form of total particulate matter (TPM), which is CS trapped in a Cambridge filter pad, and cigarette smoke extract (CSE), which is CS trapped in phosphate-buffered saline. TPM potentiated platelet reactivity to thrombin and thus increased aggregation at a concentration of $25{\sim}100{\mu}g/mL$, whereas 2.5~10% CSE decreased platelet aggregation by thrombin. Both TPM and CSE inhibited vascular contraction by phenylephrine at $50{\sim}100{\mu}g/mL$ and 10%, respectively. TPM inhibited acetylcholine-induced vasorelaxation at $10{\sim}100{\mu}g/mL$, but CSE exhibited a minimal effect on relaxation at the concentration that affects vasoconstriction. Neither TPM nor CSE induced hemolysis of erythrocytes or influenced plasma coagulation, as assessed by prothrombin time (PT) and activated partial thromboplastin time (aPTT). Taken together, CS affects platelet activity and deteriorates vasomotor functions in vitro. However, the effect on blood and blood vessels may vary depending on the CS preparation. Therefore, the results of experiments conducted with CS preparations should be interpreted with caution.

Effects of Danggi-Jakyak-San on Antiplatelet and Antihemolysis Activity of in Human blood

  • Sa, Eun-Ho;Son, Soo-Gon;Park, Won-Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.20 no.2
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    • pp.460-466
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    • 2006
  • We wondered whether the mechanisms of antiplatelet aggregation of DJS-WE were through multiple pathways. Danggijakyak-san(DJS) consisting of 6 herbes of Paeoniae Radix, Poria Cocos, Angelicae Sinensis Radix, Cnidii Rhizoma, Atractylodis Macrocephalae Rhizoma and Alismatis Rhizoma, is a crude mixture of a commonly used Korean herbal medicine. The water extract (DJS-WE) of DJS has been known to have an anti-platelet aggregation activity. We have reported that DJS-WE inhibited ADP-induced aggregation as well as arachidonic acid-induced aggregation of human platelet. Clinical studies on the cardiovascular effects of DJS-WE have been done in Korea. The DJS has been used as a remedy for gastrointestinal disorders (abdominal pain, dysentery), headache, amenorrhea, and postpartum hemorrhage. It has also been claimed to have a remarkable central stimulant effect, a transient hypertensive effect, and positive inotropic and chronotropic effects. In this paper, we evaluated the possible mechanisms of the antiplatelet activity of DJS-WE using human platelets. On the other hand, the role of DJS-ethanol extract on the inhibition of platelet aggregation and hemolytic effect have not yet been investigated in detail. We also used the method of activated partial thromboplastin times (APTT) for the first time to study the inhibition on platelet aggregation activity of DJS-ethanol extract. The effect of DJS-WE on hemolysis was also investigated. DJS-WE showed a high hemolysis ability on human blood.

Spinach Saponin-Enriched Fraction Inhibits Platelet Aggregation in cAMP- and cGMP-Dependent Manner by Decreasing TXA2 Production and Blood Coagulation

  • Cho, Hyun-Jeong;Choi, Sun-A;Kim, Chun-Gyu;Jung, Tae-Sung;Hong, Jeong-Hwa;Rhee, Man-Hee;Park, Hye-Jin;Park, Hwa-Jin
    • Biomolecules & Therapeutics
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    • v.19 no.2
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    • pp.218-223
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    • 2011
  • In this study, we investigated the effect of spinach saponin-enriched fraction (SSEF) on collagen (10 ${\mu}g/ml$)-stimulated platelet aggregation. SSEF inhibited collagen-induced platelet aggregation, and which was involved in the inhibition of thromboxane $A_2$ ($TXA_2$) production, an intracellular $Ca^{2+}$-agonist as an aggregation-inducing autacoidal molecule. In addition, SSEF significantly increased the formation of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), intracellular $Ca^{2+}$-antagonists as aggregation-inhibiting molecules, in collagen-stimulated platelets. These results suggest that SSEF might inhibit $Ca^{2+}$-elevation and $TXA_2$ formation by increasing the production of $Ca^{2+}$-antagonistic molecules cAMP and cGMP. These mean that SSEF is a potent inhibitor of collagen-stimulated platelet aggregation. On the other hand, prothrombin time (PT) and activated partial thromboplastin time (APTT) were potently prolonged by SSEF. These findings suggest that SSEF prolongs the internal time between the conversion of fibrinogen to fibrin. Accordingly, our data demonstrate that SSEF may be a crucial tool for a negative regulator during platelet activation and blood coagulation on thrombotic diseases.

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.

Physiological Properties of Extracts and the Chemical Composition of Tetraselmis sp. JK-46 Cultured with Deep Seawater (해양심층수로 배양한 해양미세조류 Tetraselmis sp. JK-46의 성분 조성 및 생리활성)

  • Joo, Dong-Sik;Kim, Kwang-Woo;Cho, Soon-Yeong
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.44 no.1
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    • pp.1-7
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    • 2011
  • This study examined Tetraselmis sp. JK-46 isolated from seawater from the East Sea. Deep seawater (DSW) had a greater effect on the growth of Tetraselmis sp. JK-46 than surface seawater (SSW). The crude protein, lipid, carbohydrate and ash contents of Tetraselmis sp. JK-46 cultured with DSW were 27.2, 37.1, 13.2 and 26.3 %, respectively, and these values were similar to the results for samples cultured with SSW. The contents of Mg, Ca, Fe and K in the DSW cultured samples were 7080.3, 1009.6, 251.2, and 2749.7 mg/100 g, respectively. The fatty acid compositions of Tetraselmis sp. JK-46 cultured with DSW and SSW were 53.7 and 49.0 % polyunsaturated fatty acids (PUFA) and 25.7 and 30.7 % saturated fatty acids (SFA), respectively. The total amino acid contents of the samples cultured with DSW and SSW were 7392.6 and 6376.0 mg/100 g respectively. The 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity of Tetraselmis sp. JK-46 extracts increased with the concentration of the chloroform and ethyl acetate fractions. The half maximal inhibitiory concentrations ($IC_{50}$) of the chloroform and ethyl acetate fractions of DSW and SSW cultured samples were 1.2 and 2.6 mg/mL, and 3.1 and 3.3 mg/mL, respectively. The ethyl acetate fractions of DSW and SSW cultured samples has anticoagulant activity and the activated partial thromboplastin times (APTT) were 93.4 and 89.3 sec., respectively. The chloroform and ethyl acetate fractions showed antimicrobial activity against Bacillus subtilis, Escherichia coli and Candida albicans.

Screening of Thrombin Inhibitor from Medicinal and Wild Plants (II) (약용 및 야생식물로부터 트롬빈 저해물질의 탐색 (II))

  • Ryu, Hee-Young;Kwon, Yun-Sook;Kum, Eun-Joo;Kwon, Chong-Suk;Kwon, Gi-Seok;Kim, Kun-Woo;Son, Kun-Ho;Sohn, Ho-Yong
    • Korean Journal of Pharmacognosy
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    • v.36 no.4 s.143
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    • pp.263-272
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    • 2005
  • To develop safe and new anticoagulation agents from natural resources, the inhibitory activities of 291 methanol extracts, which were prepared from different parts of 197 medicinal and wild plants, against human thrombin were evaluated. Based in anti-coagulation activity determined by thrombin time and activated partial thromboplastin time, the extract of leaf of Myrica rubra was finally selected. The extract of M. rubra showed a strong thrombin inhibitory activity (above 1,819%) at 0.5 mg/ml as a final concentration, whereas aspirin showed 337% inhibition at concentration of 1.5 mg/ml. The activity of the extract remained more than 85% and 60% by heat treatment at $100^{\circ}C$ for 30min, and acid treatment at pH 2 for 60 min, respectively. Our results suggested that the extract of Myrica rubra could be the potential source as thrombin inhibitor.