• Journal of Microbiology and Biotechnology
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• v.17 no.7
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• pp.1134-1138
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• 2007

Cordycepin (3'-deoxyadenosine) is an adenosine analog, isolated from Cordyceps militaris, and it has been used as an anticancer and anti-inflammation ingredient in traditional Chinese medicine. We investigated the effects of cordycepin (3'-deoxyadenosine) on human platelet aggregation, which was induced by thapsigargin, a tumor promoter, and determined the cytosolic free $Ca^{2+}$ levels ($[Ca^{2+}]_i$) (an aggregation-stimulating molecule) and cyclic-guanosine monophosphate (cGMP) (an aggregation-inhibiting molecule). Cordycepin inhibited thapsigargin-induced platelet aggregation in a dose-dependent manner, and it clearly reduced the levels of $[Ca^{2+}]_i$, which was increased by thapsigargin ($1\;{\mu}M$) or U46619 ($3\;{\mu}M$). Cordycepin also increased the thapsigargin-reduced cGMP levels. Accordingly, our data demonstrated that cordycepin may have a beneficial effect on platelet aggregation-mediated thrombotic diseases through the $[Ca^{2+}]_i$-regulating system such as cGMP.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.1
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• pp.181-185
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• 2002

The thrombosis is the category of blood stasis. Blood stasis is a pathologicial state resulting from the reverse or impeded flow of blood in the body or the stagnation of blood flow in local parts as well as abnormal blood outside of the vessles which remains in the body and fails to disperse. Hwao-tang has been reported to have a hypolipidemic effect in patients with hypercholesterolemia, and in highcholesterol-induced experimental models. The present paper reports the effects of HOT on atherosclerosis using a spontaneous experimental model, Kurosawa and Kusanagi-hypercholesterolemic (KHC) rabbits. We have also investigated the pharmacological effect of extracts obtained from HOT on collagen-and ADP-induced blood platelet aggregation, thrombin-induced conversion of fibrinogen and fibrinolysis in in vitro experiments. In conclusion, the protection of extracts of Korean herbs' HOT on the ischemic infarction induced artificially might be involved to their inhibition of thrombotic action.

• Korean Journal of Pharmacognosy
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• v.52 no.1
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• pp.26-33
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• 2021

During blood vessel damage, an essential step in the hemostatic process is platelet activation. However, it is important to properly control platelet activation, as various cardiovascular diseases, such as stroke, atherosclerosis, and myocardial infarction, are also caused by excessive platelet activation. Found primarily in the roots of plants of the genus Artemisia or Scopolia, isoscopoletin has been studied to demonstrate its potential pharmacological effects against Alzheimer's disease and anticancer, but the mechanisms and roles involved in thrombus formation and platelet aggregation are insufficient. This study investigated the effect of isoscopoletin on U46619-induced human platelet activation. As a result, isoscopoletin significantly increased the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) dose-dependently. In addition, isoscopoletin significantly phosphorylated inositol 1, 4, 5-triphosphate receptor (IP3R) and vasodilator-stimulated phosphprotein (VASP), which are known substrates for cAMP-dependent kinases and cGMP-dependent kinases. Phosphorylated IP3R by isoscopoletin inhibited Ca2+ mobilization from the dense tubular system Ca2+ channels to cytosol, and phosphorylated VASP was involved in the inhibition of fibrinogen binding through αIIb/β3 inactivation in the platelet membrane. Isoscopoletin finally reduced thrombin-induced fibrin clotting production. Therefore, this study suggests that isoscopoletin has a potent antiplatelet effect and may be helpful for platelet-related thrombotic diseases.

• Journal of Physiology & Pathology in Korean Medicine
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• v.22 no.6
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• pp.1509-1517
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• 2008

The flowers and buds of Lonicera Flower (LF), are used in Korean herbal medicine for latent-heat-clearing, antipyretic, detoxicant and anti-inflammatory ailments. This plant is used worldwide for the treatment of many types of inflammatory disease including respiratory infections, diabetes mellitus, rheumatoid arthritis and play an important role in immune reaction. These pharmaceutical effects of LF looks like to be related to its antioxidant capacity and phytochemicals containing in LF. In this study, the antioxidant activity of extract from LF was studied in vitro methods by measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) [superoxide anion, hydroxyl radical] and on reactive nitrogen species (RNS) [nitric oxide and peroxynitrite] as well as measuring the inhibitory effect on $Cu^{2+}$ induced human LDL oxidation and the inhibitory effect on collagen induced platelet aggregation. The LF extracts were found to have a potent scavenging activity, as well as an inhibitory effect on LDL oxidation and on platelet aggregation. In conclusion, the LF extracts have anti-oxidative and anti-atherosclerotic effects in vitro system, which can be used for developing pharmaceutical drug against oxidative stress and atherosclerosis.

• Journal of Life Science
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• v.28 no.10
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• pp.1156-1162
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• 2018

To investigate the anti-thrombotic activities of the lotus (Nelumbo nucifera Gaertner), various hot-water extracts were prepared from the leaf, pod of seed (PS), seed, embryo of seed (ES), root, and the node of root (NR) of the lotus. The highest extraction ratio was found in the NR (20.3%), followed by the seed, root, leaf, ES, and PS. These extracts had pH and acidity levels ranging from 5.6~6.5 and 0.06~0.20%, respectively. The seed extract showed 70% brix, whereas the leaf and PS extracts showed less than 0.1% brix. The highest contents of total polyphenol (179.7 mg/g), total flavonoids (161.4 mg/g), and reducing sugar (161.4 mg/g) were observed in the leaf extract, and the highest total sugar content (873.0 mg/g) in the seed extract. Anti-coagulation assay of the extracts of NR, leaf, and PS showed strong activities. In particular, at a concentration of 5 mg/ml, the PS extract had 15-fold extended thrombin, prothrombin, and activated partial thromboplastin times. However, only the ES extract showed activities inhibitory to platelet aggregation, with treatment with 0.25 mg/ml of ES extract decreasing platelet aggregation to 25.1%, a reduction comparable to that effected by aspirin. The extracts other than the seed extract showed no hemolysis activities against human RBC at treatments of up to 1 mg/ml. These results suggest that the NR, PS, seed, and ES, all byproducts of the lotus agriculture industry, have high potential as novel sources of anti-thrombotic agent.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.1
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• pp.135-143
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• 2009

There is currently increased interest in the identification of antioxidant compounds that are pharmacologically potent and have low or no side effects. Plants produce significant amounts of antioxidants to prevent the oxidative stress caused by photons and oxygen, therefore they represent a potential source of new compounds with antioxidant activity. Moutan Root Sark (MRS) has been frequently used as analgesic. antispasmodic, anti-inflammatory and remedies for female diseases. In this study. the antioxidant activity of extract from MRS was studied in vitro methods by measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) [superoxide anion, hydroxyl radical] and on reactive nitrogen species (RNS) [nitric oxide and peroxynitrite] as well as measuring the inhibitory effect on $Cu^{2+}$ induced human LDL oxidation and the inhibitory effect on collagen induced platelet aggregation. The MRS extracts were found to have a potent scavenging activity, as well as an inhibitory effect on LDL oxidation and on platelet aggregation. In conclusion, the MRS extracts have anti-oxidative and anti-atherosclerotic effects in vitro system, which can be used for developing pharmaceutical drug against oxidative stress and atherosclerosis.

• The Journal of Korean Obstetrics and Gynecology
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• v.22 no.1
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• pp.53-78
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• 2009

Purpose: In this study, we investigated the anti-thrombotic and antiinflammatory efficacy of "Gamijoukyungtang(GJKT)". Methods: We studied inhibitory effects of platelet aggregation, FXa activation, $TXB_2$ and $PGE_2$ biosynthesis and suppressive effects of GPIIb/IIIa activity and oxidative damage, pro-inflammatory cytokine reduction effects of 'GJKT(by press extractor)/GJKT-1(by pressless extractor)' in vitro. Also, we studied suppression of pulmonary embolism, AV shunt model in rats and shortening of Rat tail bleeding time in vivo. Results: GJKT/GJKT-1 extract showed inhibitory effects on GPIIb/IIIaactivities and platelet aggregation induced by ADP, epinephrine, collagen and arachidonic acid. They suppressed biosynthesis of $PGE_2$ but GJKT-1 only supressed biosynthesis of $TXB_2$. In FXa assay, they inhibited activation of FXa. they suppressed pulmonary embolism triggered by collagen and epinephrine. In AV shunt model, they decreased the weights of AV shunt thrombus. they inhibited pro-inflammatory cytokines and decreased oxidative damages caused by DPPH. Conclusion: We confirmed the anti-thrombosis, and ant-inflammatory efficacy of 'GJKT(by press extractor)/GJKT-1(by pressless extractor)'.

• Archives of Pharmacal Research
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• v.29 no.10
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• pp.898-903
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• 2006

The antiplatelet and antithrombotic activities of Korean Red Ginseng (KRG) were examined on rat carotid artery thrombosis in vivo, and platelet aggregation in vitro and ex vivo. Administration of KRG to rats not only prevented carotid artery thrombosis in vivo in a dose-dependent manner, but also significantly inhibited ADP- and collagen-induced platelet aggregation ex vivo, while failed to prolong coagulation times such as activated partial thromboplastin time (APTT) and prothrombin time (PT), indicating the antithrombotic effect of KRG might be due to its anti platelet aggregation rather than anticoagulation effect. In line with the above observations, KRG inhibited U46619-, arachidonic acid-, collagen- and thrombin-induced rabbit platelet aggregation in vitro in a concentration-dependent manner, with $IC_{50}$ values of $620{\pm}12$, $823{\pm}22$, $722{\pm}21$ and $650{\pm}14\;{\mu}g/mL$, respectively. Accordingly, KRG also inhibited various agonists-induced platelet serotonin secretions as it suppressed platelet aggregation. These results suggest that KRG has a potent antithrombotic effect in vivo, which may be due to antiplatelet rather than anticoagulation activity, and KRG intake may be beneficial to the individuals with high risks of thrombotic and cardiovascular diseases.

• Journal of Life Science
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• v.21 no.10
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• pp.1355-1363
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• 2011

Many clinical trials have demonstrated the beneficial effects of garlic (Allium sativum) on general cardiovascular health. Aged garlic extract (AGE) is known to display diverse biological activities such as in antioxidant, anti-inflammatory and anticancer activities. However, few studies have been directed on the effect of AGE on cardiovascular function. In this study, we aimed to investigate the effect of AGE and its components on platelet activation, a key contributor in thrombotic diseases. In freshly isolated rat platelets, AGE and its components have shown inhibitory activities on thrombin-induced platelet aggregation. These in vitro results were further confirmed in an in vivo platelet aggregation measurement where tail vein injection of garlic oil and S-Allylmercapto-cysteine (SAMC) significantly reduced thrombin and ADP-induced platelet aggregation. Potential active components for antiplatelet effects of AGE were identified to be SAMC and diallyl sulphide through agonist-induced platelet aggregation assay. These results indicate that aged garlic extract can be a novel dietary supplement for the prevention of cardiovascular risks and the improvement of blood circulation.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.402-407
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• 2023

The regulation of platelet aggregation is crucial for maintaining normal hemostasis, but abnormal or excessive platelet aggregation can contribute to cardiovascular disorders such as stroke, atherosclerosis, and thrombosis. Therefore, identifying substances that can control or suppress platelet aggregation is a promising approach for the prevention and treatment of these conditions. Artemisinin, a compound derived from Artemisia or Scopolia plants, has shown potential in various areas such as anticancer and Alzheimer's disease research. However, the specific role and mechanisms by which artemisinin influences platelet activation and thrombus formation are not yet fully understood. This study investigated the effects of artemisinin on platelet activation and thrombus formation. As a result, cAMP production were increased significantly by artemisinin, as well as phosphorylated VASP and IP₃R which are substrates to cAMP-dependent kinase by artemisinin in a significant manner. The Ca²⁺ normally mobilized from the dense tubular system was inhibited due to IP₃R phosphorylation from artemisinin, and phosphorylated VASP by artemisinin aided in inhibiting platelet activity via αIIb/β3 platelet membrane inactivation and inhibiting fibrinogen binding. Finally, artemisinin inhibited thrombin-induced thrombus formation. Therefore, we suggest that artemisinin has importance with cardiovascular diseases stemming from the abnormal platelets activation and thrombus formation by acting as an effective prophylactic and therapeutic agent.