• 제목/요약/키워드: Platelet aggregation inhibitors

검색결과 16건 처리시간 0.023초

혈소판 응집 억제 작용 생약의 검색(II) (Screening of Potential Inhibitors of Platelet Aggregation from Plant Sources(II))

  • 윤혜숙;김제훈;이종난
    • 생약학회지
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    • 제17권1호
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    • pp.19-22
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    • 1986
  • As a continuation of the previous work, a second group of sixty solvent fractions prepared from twenty plant species were screened for their inhibitory effects on adenosine 5'-diphosphate (ADP)-, arachidonic acid (AA)- or collagen-induced rat platelet aggregation. The results suggested that five plant species including Angelica koreana, Cassia obtusifolia, Gastrodia elata, Paeonia lactiflora and Salvia miltiorrhiza are potential sources of inhibitors of platelet aggregation.

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Thapsigargin Induces Platelet Aggregation, thereby Releases Lactate Dehydrogenase from Rat Platelets

  • Baik, Ji Sue;Seo, You Na;Rhee, Man Hee;Park, Moon-Taek;Kim, Sung Dae
    • 대한의생명과학회지
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    • 제27권3호
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    • pp.170-176
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    • 2021
  • Thapsigargin (TG), a sarco/endoplasmic reticulum (ER) Ca2+-ATPase (SERCA) inhibitor, has been widely used as an agonist for platelet aggregation for decades. In this study, we investigated the effect of TG on the release of lactate dehydrogenase (LDH) for platelets and elucidated its mechanism. Platelet LDH release and platelet aggregation were increased by TG treatment; 1,000 nM of TG induced the complete lysis of platelets. Other agonists such as collagen (2.5 ㎍/mL), thrombin (0.1 U/mL), and ADP (10 mM) did not induce significant platelet LDH release despite platelet aggregation. Finally, we investigated the effects of pharmacological inhibitors on TG-induced platelet aggregation and LDH release. SP600125, a JNK inhibitor, and LY294002, a PI-3K inhibitor, inhibited TG-induced platelet LDH release but not platelet aggregation. Forskolin, an adenylyl cyclase activator, also inhibited LDH release without affecting platelet aggregation by TG. These results suggest that the TG-induced platelet aggregation was accompanied by LDH release but regulated by a different signaling pathway.

버섯류로부터 혈소판 응집억제물질과 혈전용해물질의 탐색 (Detection of Platelet Aggregation Inhibitors and Fibrinolytic Substances from Mushrooms)

  • 박정식;현광욱;서승보;조수묵;유창현;이종수
    • 한국균학회지
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    • 제31권2호
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    • pp.114-116
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    • 2003
  • 농업과학기술원에서 분양 받은 52종의 버섯류의 자실체와 균사체들의 물 추출물과 에탄올 추출물에 대한 혈소판 응집억제 활성과 혈전용해활성을 조사하였다. 차가버섯 ASI 74006 균사체의 에탄올 추출물이 81.2%로 가장 높은 ADP 유도 혈소판 응집 억제활성을 보였고 그 다음은 장수버섯 자실체 에탄올 추출물들이 높았다. 그리고 혈전용해활성은 신령버섯 ASI 1174 균사체의 에탄올 추출물이 9.6 unit로 가장 높았으며 다른 버섯류는 대체로 낮았다.

Inhibitory Effects of PD98059, SB203580, and SP600125 on α-and δ-granule Release and Intracellular Ca2+ Levels in Human Platelets

  • Kwon, Hyuk-Woo
    • 대한의생명과학회지
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    • 제24권3호
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    • pp.253-262
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    • 2018
  • Platelets are activated at sites of vascular injury via several molecules, such as adenosine diphosphate, collagen and thrombin. Full platelet aggregation is absolutely essential for normal hemostasis. Moreover, this physiological event can trigger circulatory disorders, such as thrombosis, atherosclerosis, and cardiovascular disease. Therefore, platelet function inhibition is a promising approach in preventing platelet-mediated circulatory disease. Many studies reported the involvement of mitogen-activated protein kinases (MAPKs) signaling pathways in platelet functions. However, these studies were limited. Thus, we examined MAPK signaling pathways in human platelets using specific MAPK inhibitors, such as PD98059, SB203580, and SP600125. We observed that these inhibitors were involved in calcium mobilization and influx in human platelets. They also suppressed thrombin-induced ${\alpha}$- and ${\delta}$-granule release. These results suggest that PD98059, SB203580, and SP600125 exhibit $Ca^{2+}$ antagonistic effects.

산채류로부터 혈소판응집 억제물질의 검색 (Screening of Inhibitors of Platelet Aggregation from Edible Plants)

  • 윤민호;임치환;오진환;이종철;최우영
    • 농업과학연구
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    • 제24권2호
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    • pp.267-274
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    • 1997
  • 산채류를 비롯한 식물자원으로부터 항혈전 성분을 탐색하기 위하여 전국일원의 농산시장 및 농촌지도소, 평창산채시험장과 한국인삼연초연구원의 실험포장으로부터 약 160점의 시료를 수집하였으며, modified smear method를 적용하여 그 methanol 추출물의 혈소판응집 저해활성을 비교하였다. Platelet rich plasma 즉 혈소판 혈장을 이용하는 modified smear method는 응집유도물질로서 ADP와 collagen을 사용하였을때 electrical impedence method와 높은 상관성을 나타내었고, 재현성도 비교적 우수하여 정제하지 않은 식물체의 조추출물의 항혈전 활성을 효율적으로 검색할 수 있었다. 참취, 개미취, 곤달비, 산마늘, 산도라지, 영양부추, 산뽕, 쇠비름, 생열귀등이 ADP와 collagen 모두 혈소판응집 저해활성을 나타내었으며, 곰취, 사철쑥, 씀바귀, 민들레, 산지치, 갯완두, 참대등은 collagen을 사용한 경우에는 저해활성이 다소 낮게 검출되었다. 반면에 참나물, 옥잠, 냉이, 메밀, 매실, 복분자, 해란초등은 오히려 혈소판응집 촉진효과를 나타내었다. 한편 DPPH법으로 활성산소 억제율을 비교한 결과 산채류중에는 고사리, 참취, 곰취, 구절초, 사철쑥, 고려엉겅퀴, 달개비, 냉이 그리고 생약재중에서는 적작약, 음양곽, 복분자등이 항산화활성이 높았다.

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COX-2 억제제의 구조-활성 (SAR of COX-2 Inhibitors)

  • 권순경
    • Biomolecules & Therapeutics
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    • 제9권2호
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    • pp.69-78
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    • 2001
  • Cyclooxygenase (COX) is an enzyme, which catalyzes the production of prostaglandins from arachi-donic acid and exists in two isoforms (COX-1 and COX-2). COX-1 is involved in the maintenance of physiological functions such as platelet aggregation, cytoprotection in the stomach and maintenance of normal kidney function. COX-2 is induced significantly in vivo under inflammatory conditions. COX-1 and COX-2 serve different physiological and pathological functions. All commercially available nonsteroidal antiinflammatory drugs (NSAIDS) are inhibitors of both COX-1 and COX-2. Therefore, selective inhibitors of COX-2 may be effective antiinflammatory agents without the ulcerogenic effects associated with current NSAms. Since the mid 1990s, a number of reports have been appeared on the preparation and biological activity of selective COX-2 inhibitors. Recently celecoxib, and rofecoxib, the representative COX-2 inhibitors, are introduced in the drug market. In this paper the relationship of structure-activity for selective COX-2 inhibitors is reviewed.

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Variability of Platelet Reactivity on Antiplatelet Therapy in Neurointervention Procedure

  • Yi, Ho Jun;Hwang, Gyojun;Lee, Byoung Hun
    • Journal of Korean Neurosurgical Society
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    • 제62권1호
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    • pp.3-9
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    • 2019
  • As more intracranial aneurysms and other cerebrovascular pathologies are treated with neurointervention procedure, thromboembolic events that frequently lead to serious neurological deficit or fatal outcomes are increasing. In order to prevent the thromboembolic events, antiplatelet therapy is used in most procedures including coil embolization, stenting, and flow diversion. However, because of variable individual pharmacodynamics responses to antiplatelet drugs, especially clopidogrel, it is difficult for clinicians to select the adequate antiplatelet regimen and its optimal dose. This article reviews the neurointervention literature related to antiplatelet therapy and suggests a strategy for tailoring antiplatelet therapy in individual patients undergoing neurointervention based on the results of platelet function testing.

PKC inhibitors RO 31-8220 and Gö 6983 enhance epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation

  • Kim, Sun-Young;Kim, Se-Woon;Kim, Jeong-Mi;Jho, Eek-Hoon;Park, Seon-Yang;Oh, Do-Yeun;Yun-Choi, Hye-Sook
    • BMB Reports
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    • 제44권2호
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    • pp.140-145
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    • 2011
  • Impaired responsiveness of platelets to epinephrine (epi) and other catecholamines (CA) has been reported in approximately 20% of the healthy Korean and Japanese populations. In the present study, platelet aggregation induced by epi was potentiated by RO 31-8220 (RO) or G$\ddot{o}$ 6983 (G$\ddot{o}$). Phosphorylated Akt (p-Akt) was very low in epi-stimulated PRP from CA-hypo- responders (CA-HY), whereas it was detected in those from CA-good responders (CA-GR). RO and G$\ddot{o}$ increased p-Akt, one of the major downstream effectors of phosphoinositol-3 kinase (PI3K), in epi-stimulated PRP from both groups. Wortmannin, a PI3K inhibitor, attenuated the RO or G$\ddot{o}$-induced potentiation of p-Akt in epi-stimulated PRP, suggesting positive effects for RO and G$\ddot{o}$ on PI3K. $TXA_2$ formation was increased by the addition of either RO or G$\ddot{o}$ in epi-stimulated platelets. The present data also suggest that impaired Akt phosphorylation may be responsible for epinephrine hypo-responsiveness of platelets.

Snake Venom Phospholipase A2 and its Natural Inhibitors

  • Singh, Pushpendra;Yasir, Mohammad;Khare, Ruchi;Tripathi, Manish Kumar;Shrivastava, Rahul
    • Natural Product Sciences
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    • 제26권4호
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    • pp.259-267
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    • 2020
  • Snakebite is a severe medical, economic, and social problem across the world, mostly in the tropical and subtropical area. These regions of the globe have typical of the world's venomous snakes present where access to prompt treatment is limited or not available. Snake venom is a complex mixture of toxin proteins like neurotoxin and cardiotoxin, and other enzymes like phospholipase A2 (PLA2), haemorrhaging, transaminase, hyaluronidase, phosphodiesterase, acetylcholinesterase, cytolytic and necrotic toxins. Snake venom shows a wide range of biological effects like anticoagulation or platelet aggregation, hemolysis, hypotension and edema. Phospholipase A2 is the principal constituent of snake venom; it catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid, which is the precursor of eicosanoids including prostaglandins and leukotrienes. The information regarding the structure and function of the phospholipase A2 enzyme may help in treating the snakebite victims. This review article constitutes a brief description of the structure, types, mechanism occurrence, and tests of phospholipase A2 and role of components of medicinal plants used to inhibit phospholipase A2.