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PI3K/Akt 및 MAPK 기전 조절을 통한 Artesunate의 콜라겐 유도의 사람 혈소판 응집 억제효과
이동하 한국응용생명화학회 2022 Journal of Applied Biological Chemistry (J. Appl. Vol.65 No.1
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 collageninduced 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
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이동하,박화진,권혁우,김현홍,임덕휘,남기석,신정해,김종래,이종진,권호균 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.1
In this study, we investigated the effect ofcordycepin-enriched (CE)-WIB801C from Cordyceps militarison ADP (20 lM)-stimulated platelet aggregation. CE-WIB801C dose-dependently inhibited ADP-inducedplatelet aggregation, and its IC50 value was 18.5 lg/mL. CE-WIB801C decreased TXA2 production, but did notinhibit the activities of COX-1 and thromboxane synthase(TXAS) in ADP-activated platelets, which suggests that theinhibition of TXA2 production by CE-WIB801C is notresulted from the direct inhibition of COX-1 and TXAS. CE-WIB801C inhibited ATP release and [Ca2+]i mobilization,and increased cAMP level and IP3RI (Ser1756)phosphorylation in ADP-activated platelets. cAMP-dependentprotein kinase (A-kinase) inhibitor Rp-8-Br-cAMPSincreased CE-WIB801C-inhibited [Ca2+]i mobilization,and strongly inhibited CE-WIB801C-increased IP3RI(Ser1756) phosphorylation. CE-WIB801C elevated thephosphorylation of VASP (Ser157), an A-kinase substrate,but inhibited fibrinogen binding to aIIb/b3. These resultssuggest that CE-WIB801C-elevated cAMP involved inIP3RI (Ser1756) phosphorylation to inhibit [Ca2+]i mobilizationand, VASP (Ser157) phosphorylation to inhibit aIIb/b3 activation. Therefore, in this study, we demonstrate thatCE-WIB801C may have a preventive or therapeuticpotential for platelet aggregation-mediated diseases, suchas thrombosis, myocardial infarction, atherosclerosis, andischemic cerebrovascular disease.
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콜라겐 유도의 혈소판에서 사이클릭 뉴클레오티드의 조절을 통한 Scoparone의 혈전 형성 억제 효과
이동하 한국식품영양과학회 2020 한국식품영양과학회지 Vol.49 No.1
혈소판 활성화는 혈관 손상에 대한 지혈 과정에 필수적이다. 그러나 과도한 혈소판 활성화는 죽상동맥경화증, 혈전증 및 심근경색을 포함한 여러 심혈관 질환을 유발할 수 있다. Scoparone은 Artemisia 또는 Scopolia 속의 뿌리에서 흔히 발견되며 면역억제 및 혈관 이완을 포함한 약리학적인 특성에 대해 연구되었지만, 항혈소판 효과에 대해서는 아직 보고된 바가 없다. 본 연구는 scoparone이 collagen에 의해 유도한 사람 혈소판 활성화에 미치는 영향을 연구하였다. 그 결과로, scoparone은 농도 의존적으로 cyclic adenosine monophosphate(cAMP)와 cyclic guanosine monophosphate(cGMP) 수준을 유의하게 증가시켰다. 또한 scoparone은 cAMP 의존성 kinase(PKA) 및 cGMP 의존성 kinase(PKG)의 기질로 작용하는 inositol 1,4,5-triphosphate receptor(IP3R) 및 vasodilator-stimulated phosphoprotein(VASP)을 유의하게 인산화시켰다. Scoparone에 의한 IP3R의 인산화는 dense tubular system의 Ca2+ 채널로부터 동원되는 Ca2+ 억제를 유발하였고, VASP의 인산화는 혈소판 막에 있는 αIIb/β3의 불활성화를 일으켜 fibrinogen 결합을 저해함으로써 혈소판 활성을 억제하는 데 관여하였다. Scoparone은 thrombin-유도의 fibrin clot 생성을 억제함으로써 최종적으로 혈전 형성을 감소시켰다. 그러므로 본 연구에서는 scoparone이 강력한 항혈소판 효과를 가지며 혈소판이 유래하는 혈전성 질환의 예방 및 치료제로서 가능성이 있음을 제안한다. Platelet activation is essential for the hemostatic process for vascular damage. Excessive platelet activation, however, can lead to several cardiovascular diseases, including atherosclerosis, thrombosis, and myocardial infarction. Scoparone is found in the roots of the genus Artemisia or Scopolia. The pharmacological properties of this compound, including immunosuppression and vascular relaxation, have been studied, but no antiplatelet effects have been reported. This study examined the activities of scoparone on collagen-induced human platelet activation. Scoparone increased the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in a concentration-dependent manner. In addition, scoparone phosphorylated the inositol 1,4,5-triphosphate receptor (IP3R) and vasodilator-stimulated phosphoprotein (VASP) that act as substrates for cAMP-dependent kinase (PKA) and cGMP-dependent kinase (PKG). The phosphorylation of IP3R by scoparone-inhibited the Ca2+ mobilized from the Ca2+ channel of the dense tubular system. Moreover, the phosphorylation of VASP was involved in the inhibition of fibrinogen binding by inactivating αIIb/β3 in the platelet membrane. Scoparone finally reduced the level of thrombin-induced fibrin clot production and reduced thrombus formation. Therefore, scoparone has strong antiplatelet activity and is a potential prophylactic and therapeutic agent for thrombotic diseases from which platelets are derived.
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