• Title/Summary/Keyword: Scopolia

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Inhibitory Effects of Scopoletin in Collagen-induced Human Platelet Aggregation (콜라겐으로 유도한 사람 혈소판 응집에 미치는 Scopoletin의 억제 효과)

  • Kwon, Hyuk-Woo;Shin, Jung-Hae;Park, Chang-Eun;Lee, Dong-Ha
    • Korean Journal of Clinical Laboratory Science
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    • v.51 no.1
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    • pp.34-41
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    • 2019

  • Platelet aggregation is essential for the formation of a hemostatic plug in the case of blood vessel damage. On the other hand, excessive platelet aggregation may cause cardiovascular disorders, such as thrombosis, atherosclerosis, and myocardial infarction. Scopoletin, which found in the root of plants in the genus Scopolia or Artemisia, has anti-coagulation and anti-malaria effects. This study examined the effects of scopoletin on human platelet aggregation induced by collagen. Scopoletin had anti-platelet effects via the down-regulation of thromboxane $A_2$ ($TXA_2$) production and intracellular $Ca^{2+}$ mobilization ($[Ca^{2+}]_i$), which are aggregation-inducing molecules produced in activated platelets. On the other hand, scopoletin increased both the cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) levels, which are known as intracellular $Ca^{2+}$-antagonists and aggregation-inhibiting molecules. In particular, scopoletin increased the potently cAMP level more than cGMP, which led to suppressed fibrinogen binding to ${\alpha}IIb/{\beta}_3$ in collagen-induced human platelet aggregation. In addition, scopoletin inhibited collagen-elevated adenosine triphosphate (ATP) release in a dose-dependent manner. The results suggest that aggregation amplification through granule secretion is inhibited by scopoletin. Therefore, scopoletin has potent anti-platelet effects and may have potential for the prevention of platelet-derived vascular diseases.

  • https://doi.org/10.15324/kjcls.2019.51.1.34 인용 PDF KSCI

Artesunate inhibits collagen-induced human platelets aggregation through regulation of PI3K/Akt and MAPK pathway (PI3K/Akt 및 MAPK 기전 조절을 통한 Artesunate의 콜라겐 유도의 사람 혈소판 응집 억제효과)

  • Lee, Dong-Ha
    • Journal of Applied Biological Chemistry
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    • v.65 no.1
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    • pp.57-62
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    • 2022

  • Excessive activation and aggregation of platelets is a major cause of cardiovascular disease. Therefore, inhibition of platelet activation and aggregation is considered an attractive therapeutic target in preventing and treating cardiovascular diseases. In particular, strong platelet activation and aggregation by collagen secreted from the vascular endothelium are characteristic of vascular diseases. Artesunate is a compound extracted from the plant roots of Artemisia or Scopolia species, and has been reported to be effective in anticancer and Alzheimer's disease fields. However, the effect and mechanism of artesunate on collagen-induced platelet activation and aggregation have not been elucidated. In this study, the effect of artesunate on collagen-induced human platelet aggregation was confirmed and the mechanism of action of artesunate was clarified. Artesunate inhibited the phosphorylation of PI3K/Akt and Mitogen-activated protein kinases, which are phosphoproteins that are known to act in the signal transduction process when platelets are activated. In addition, artesunate decreased TXA2 production and decreased granule secretion in platelets such as ATP and serotonin release. As a result, artesunate strongly inhibited platelet aggregation induced by collagen, a strong aggregation inducer secreted from vascular endothelial cells, with an IC50 of 106.41 µM. These results suggest that artesunate has value as an effective antithrombotic agent for inhibiting the activation and aggregation of human platelets through vascular injury.

  • https://doi.org/10.3839/jabc.2022.008 인용 PDF KSCI

Anti-thrombotic effect of artemisinin through regulation of cAMP production and Ca2+ mobilization in U46619-induced human platelets (U46619 유도의 사람 혈소판에서 cAMP 생성 및 Ca2+동원의 조절을 통한 Artemisinin의 항혈전 효과)

  • Chang-Eun Park;Dong-Ha Lee
    • 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.

  • https://doi.org/10.3839/jabc.2023.054 인용 PDF