• 제목/요약/키워드: anti-platelet aggregation

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A Comparative Study of the Anti-Platelet Effects of cis- and trans-Resveratrol

  • Kim, Hwa;Oh, Seok-Jeong;Liu, Yingqiu;Lee, Moo-Yeol
    • Biomolecules & Therapeutics
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    • 제19권2호
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    • pp.201-205
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    • 2011
  • Although various biological activities of resveratrol have been extensively studied, most reports have focused on trans-resveratrol and little attention has been paid to the cis-isomer. In this study, the effect of cis-resveratrol on platelet activity was examined and compared with that of the trans-isomer. Treatment with cis-resveratrol resulted in inhibition of platelet aggregation induced by thrombin, collagen or ADP, which are representative aggregation-inducing agents, and the trans-isomer elicited the same effects. These effects were concentration-dependent in the range of 1-100 ${\mu}M$. However, the potency of the cis-isomer was much lower than that of the trans-isomer; the $IC_{50}$ values for the cis-isomer versus the trans-isomer were $31{\pm}12$ vs $151{\pm}3$, $161{\pm}3$ vs $91{\pm}4$, and $601{\pm}15$ vs $251{\pm}6\;{\mu}M$ for thrombin-, collagen- and ADP-induced aggregation, respectively. These results indicate that cis-resveratrol has a less potent anti-platelet activity, compared with the trans-isomer, and raise the possibility that the biological activities of the cis-isomer may be different from those of the trans-isomer. It will be necessary to evaluate the activity of cis-resveratrol independently of the trans-isomer.

창포류 추출물이 인간 전혈혈소판 응집억제에 미치는 영향 (Effects of Acori Rhizoma Extract on the in vitro Anti-platelet Activity in Human Whole Blood)

  • 최고야;김슬기;이인선;백지성;전원경
    • 대한본초학회지
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    • 제25권3호
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    • pp.91-95
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    • 2010
  • Objectives : Acori Rhizoma is one of the common widely used herbal medicines with diverse bioactive effects. However, little evidence has been reported about the potential anti-platelet activity of Acori Rhizoma. The present study examined the effects on platelet aggregation by Acori Rhizoma. Methods : In this study, we tested the in vitro effect of 16 kinds of Acori Rhizoma extracts by hot water or 70% ethanol on collagen-induced platelet aggregation in human whole blood using the impedance method of aggregometry. Results : Among them, 2 kinds of 70% ethanol extract and 1 kind of hot water extract showed the significant inhibiting effect on whole blood aggregation. In particular, Acorus gramineus extracts were selected as the most effective candidate. Conclusiions : The results from this experiment provide pharmacological evidence for the traditional medicine, suggesting that Acorus gramineus could be help problems of blood circulation more than Acorus tatarinowii.

블랙커런트의 항산화, 항응고 및 혈소판 응집저해 활성 (Anti-oxidant, Anti-coagulation, and Anti-platelet Aggregation Activities of Black Currant (Ribes nigrum L.))

  • 김미선;손호용
    • 생명과학회지
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    • 제26권12호
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    • pp.1400-1408
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    • 2016
  • 블랙커런트는 장미목 범의귀과의 낙엽관목으로, 즙이 많은 검은 열매와 잎을 주스, 잼, 젤리, 시럽 등으로 가공하여 식용하고 있다. 본 연구에서는 블랙커런트(오스트리아산)의 착즙액과 이의 순차적 유기용매 분획물인 hexane 분획물, ethylacetate (EA) 분획물, butanol 분획물 및 물 잔류물을 조제하여 각각의 성분 분석, 항산화 활성, 혈전 생성과 관련된 항응고 활성 및 혈소판 응집저해 활성을 평가하였다. 그 결과, 착즙액과 폴리페놀 및 플라보노이드 고함유 분획인 EA 분획물에서 강력한 DPPH 음이온, ABTS 양이온, nitrite 소거능과 환원력을 확인하였다. EA 분획의 $RC_{50}$ (활성 radical을 50% 제거하는 데 소요되는 시료의 양)는 각각 136.3, 66.2 및 $115.5{\mu}g/ml$ 값을 나타내어 vitamin C가 나타내는 $RC_{50}$의 각각 1/10, 1/16 및 1/7.7에 해당하는 항산화력을 나타내었다. 또한 착즙액과 이의 EA 분획물, butanol 분획물은 아스피린에 필적하는 강력한 항응고 활성을 나타내었으며, 특히 EA 분획물과 butanol 분획물은 아스피린보다 우수한 혈소판 응집억제활성을 나타내었다. 혈소판 응집을 50% 저해할 수 있는 아스피린 농도는 0.395 mg/ml인 반면, EA 분획 및 butanol 분획은 각각 0.192 및 0.261 mg/ml로 나타났다. 상기의 활성 분획물은 0.5 mg/ml 농도까지 인간 적혈구에 대한 용혈활성을 나타내지 않았다. 이러한 결과는 블랙커런트의 강력한 항산화, 항응고, 혈소판 응집저해 활성을 이용한 신규의 항혈전제 개발 및 이용이 가능함을 제시하고 있다. 본 연구는 블랙커런트의 항혈전 활성에 대한 최초의 보고이다.

Protocatechuic acid 및 Gallic acid 유도체들의 항 혈전작용 (Anti-thrombotic Effects of Analogs of Protocatechuic Acid and Gallic Acid)

  • 윤혜숙;강삼식;김문희;정기화
    • 약학회지
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    • 제37권5호
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    • pp.453-457
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    • 1993
  • Platelet anti-aggregating activities were tested with analogs of protocatechuic acid and gallic acid. Six of them which showed comparable inhibitory effects with aspirin against collagen induced platelet aggregation were selected and their anti-thrombotic effects were evaluated in the mouse thrombosis model and compared with those of aspirin and paeonol. At the dose of 50 mg/kg, p.o., ethyl gailate(13) treated group showed higher % of recovery within 6 min of thrombotic challenge and lower mortality within 5 min than aspirin treated group.

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성숙 마가자의 혈액 응고저해 및 혈소판 응집저해 활성 (Anti-coagulation and Anti-platelet Aggregation Activity of the Mature Fruit of Sorbus commixta)

  • 김미선;손호용
    • 한국미생물·생명공학회지
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    • 제43권4호
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    • pp.373-377
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    • 2015
  • 마가목의 열매인 마가자는 생식하거나 다류, 발효주로 제조되어 음용되며, 한방에서는 고혈압 및 관절염 치료 등에 사용되고 있다. 본 연구에서는 현재까지 보고되지 않은 마가자의 항혈전 활성을 평가하기 위해 울릉도 마가자의 ethanol 추출물 및 이의 순차적 유기용매 분획물을 조제하고 이의 혈액응고 저해 및 혈소판 응집저해 활성을 평가하였다. 그 결과, 마가자의 ethanol 추출물의 ethylacetate 분획에서 강력한 트롬빈, 프로트롬빈, 혈액응고인자 저해와 함께, 혈소판 응집저해 활성을, hexane 분획에서는 아스피린보다 강력한 혈소판 응집저해 활성을 확인하였다. 또한 마가자의 추출물 및 분획물들은 0.5 mg/ml 농도까지 인간 적혈구 용혈활성이 없음을 확인하여, 마가자의 활성분획물이 신규의 항혈전제로 사용 가능함을 제시하였다.

Anti-platelet Effects of Dimethyl Sulfoxide via Down-regulation of COX-1 and $TXA_2$ Synthase Activity in Rat Platelets

  • Ro, Ju-Ye;Lee, Hui-Jin;Ryu, Jin-Hyeob;Park, Hwa-Jin;Cho, Hyun-Jeong
    • 대한의생명과학회지
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    • 제20권2호
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    • pp.70-76
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    • 2014
  • In this study, we investigated the effect of DMSO, a highly dipolar organic liquid, in collagen ($5{\mu}g/ml$)-stimulated platelet aggregation. DMSO inhibited platelet aggregation at 0.5% by inhibiting production of thromboxane $A_2$ ($TXA_2$) which was associated with blocking cyclooxygenase (COX)-1 activity and $TXA_2$ synthase. In addition, DMSO significantly increased the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP) and cyclic guanosine monophosphate (cGMP) from guanosine triphosphate (GTP). On the other hand, DMSO (0.1~0.5% concentration) did not affect the LDH release which indicates the cytotoxicity. Based on these results, DMSO has anti-platelet effect by regulation of several platelet signaling pathways, therefore we suggest that DMSO could be a novel strategy on many thrombotic disorders.

Anticardiovascular Diseases Effects of Fermented Garlic and Fermented Chitosan

  • Kim, Hyun-Kyoung;Lee, Jeong-Hun
    • International Journal of Advanced Culture Technology
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    • 제6권4호
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    • pp.109-115
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    • 2018
  • Garlic is a medicinal plant used throughout the world for its anti-inflammatory, antioxidant, and antiplatelet activities. Chitosan is a natural polysaccharide obtained from chitin, and derivatives of chitosan have been shown to inhibit platelet aggregation and adhesion. We hypothesized that fermented preparations of these products may possess stronger antiplatelet effects than the non-fermented forms owing to the increased bioavailability of the bioactive compounds produced during fermentation. Therefore, we compared these compounds via in vitro and ex vivo platelet aggregation assays by using standard light transmission aggregometry and ex vivo granule secretions from rat platelets. We found that fermented preparations exerted more potent and significant inhibition of platelet aggregation both in vitro and ex vivo. Likewise, ATP release from dense granules of platelets was also significantly inhibited in fermented preparation-treated rat platelets compared to that in non-fermented preparation-treated ones. We concluded that fermented preparations exerted more potent effects on platelet function both in vitro and ex vivo, possibly as a result of the increased bioavailability of active compounds produced during fermentation. We therefore suggest that fermented products may be potent therapeutics against platelet-related CVDs and can be used as antiplatelet and antithrombotic agents.

백단향추출물의 항산화, 항혈소판 응집 및 혈전 용해능에 관한 연구 (Preventive Effects of Santalum album L. Extracts on Oxidation, Platelet Aggregation and Thrombosis)

  • 송영위;이지현;송규주;구병수;김근우
    • 동의신경정신과학회지
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    • 제23권1호
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    • pp.115-128
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    • 2012
  • Objectives : To evaluate the in vitro scavenging activity, inhibitory effect of LDL oxidation of pro-oxidant reactive species, anti-platelet aggregative effects and anti-thrombosis effects in response to treatment with SA using various screening methods including biological and non-biological oxidants. Methods : The antioxidant activity concerning extract from SA was studied with 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 thrombin-induced platelet aggregation and thrombosis. Results : SA extracts were found to have a potent scavenging activity regarding oxidative stress as well as an inhibitory effect towards LDL oxidation, platelet aggregation, and thrombosis. Conclusions : The SA extracts have anti-oxidative and anti-atherosclerotic effects in vitro system, which can be used for developing pharmaceutical drugs against oxidative stress and atherosclerosis.

Ginsenoside Rk1 suppresses platelet mediated thrombus formation by downregulation of granule release and αIIbβ3 activation

  • Shin, Jung-Hae;Kwon, Hyuk-Woo;Irfan, Muhammad;Rhee, Man Hee;Lee, Dong-Ha
    • Journal of Ginseng Research
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    • 제45권4호
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    • pp.490-497
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    • 2021
  • Background and objective: Synthetic ginsenoside compounds G-Rp (1,3, and 4) and natural ginsenosides in Panax ginseng 20(S)-Rg3, Rg6, F4 and Ro have inhibitory actions on human platelets. However, the inhibitory mechanism of ginsenoside Rk1 (G-Rk1) is still unclear thus, we initiated investigation of the anti-platelet mechanism by G-Rk1 from Panax ginseng. Methodology: Our study focused to investigate the action of G-Rk1 on agonist-stimulated human platelet aggregation, inhibition of platelet signaling molecules such as fibrinogen binding with integrin αIIbβ3 using flow cytometry, intracellular calcium mobilization, fibronectin adhesion, dense granule secretion, and thromboxane B2 secretion. Thrombin-induced clot retraction was also observed in human platelets. Key Results: Collagen, thrombin, and U46619-stimulated human platelet aggregation were dose-dependently inhibited by G-Rk1, while it demonstrated a more effective suppression on collagen-stimulated platelet aggregation using human platelets. Moreover, G-Rk1 suppressed collagen-induced elevation of Ca2+ release from endoplasmic reticulum, granule release, and αIIbβ3 activity without any cytotoxicity. Conclusions and implications: These results indicate that G-Rk1 possess strong anti-platelet effect, proposing a new drug candidate for treatment and prevention of platelet-mediated thrombosis in cardiovascular disease.