• 동의생리병리학회지
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• 제23권1호
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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.

• Biomolecules & Therapeutics
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• 제21권1호
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• pp.54-59
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• 2013

In this study, we investigated the effect of (-)-epigallocatechin-3-gallate (EGCG), a major component of green tea catechins from green tea leaves, on activities of cyclooxygenase (COX)-1 and thromboxane synthase (TXAS), thromboxane $A_2$ ($TXA_2$) production associated microsomal enzymes. EGCG inhibited COX-1 activity to 96.9%, and TXAS activity to 20% in platelet microsomal fraction having cytochrome c reductase (an endoplasmic reticulum marker enzyme) activity and expressing COX-1 (70 kDa) and TXAS (58 kDa) proteins. The inhibitory ratio of COX-1 to TXAS by EGCG was 4.8. These results mean that EGCG has a stronger selectivity in COX-1 inhibition than TXAS inhibition. In special, a nonsteroid anti-inflammatory drug aspirin, a COX-1 inhibitor, inhibited COX-1 activity by 11.3% at the same concentration ($50{\mu}M$) as EGCG that inhibited COX-1 activity to 96.9% as compared with that of control. This suggests that EGCG has a stronger effect than that of aspirin on inhibition of COX-1 activity. Accordingly, we demonstrate that EGCG might be used as a crucial tool for a strong negative regulator of COX-1/$TXA_2$ signaling pathway to inhibit thrombotic disease-associated platelet aggregation.

• 대한본초학회지
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• 제38권4호
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• pp.31-43
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• 2023

Objectives : The objective of this study was to investigate the phytochemistry and pharmacological activities of Cirsium setidens. Methods : Domestic and international articles about Cirsium setidens were investigated. A review was perfoemed via DB searching engine such as Sci.Direct, Springer, DBpia, KISS, Google scholar, Kipris, and so on. Total 73 listed literature were classified by compound analysis and pharmacological efficacy. Results : C. setidens contains pectolinarin and its glycoside, pectolinarigenin as index compounds, and linarin, apigenin, diosmetin, scopoletin, acacetin, cirsimarin, cirsimaritin, setidenosides A and B, silymarin, hispidulin, 92 volatile compounds, and 15 fatty acids. The Pharmacological activities of C. setidens has been reported to inhibit of platelet aggregation and fat accumulation in the liver, inhibit to hepatitis, anti-cancer, antibacterial, skin improvement, hair growth, liver protection, anti-diabetic, anti-inflammatory, sedative. Also, It has been reported the effect of cholesterol-lowering and anti-obesity, neuroprotective effects, increasing human stem cell viability, inhibiting osteoclast formation and osteogenic differentiation. Conclusion : This reviews showed that C. setidens which has been traditionally used for the treatment of inflammation and hypertension, has anticancer and river protective effect, as well as hair loss and diet. In order to maximize the efficacy of C. setidens, research has also begun on the effect of processing processes such as fermentation or fine powdering and combining natural plant resources.

• Safety and Health at Work
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• 제2권3호
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• pp.282-289
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• 2011

Objectives: We sought to establish a novel method to generate nano-sized carbon black particles (nano-CBPs) with an average size smaller than 100 nm for examining the inhalation exposure risks of experimental rats. We also tested the effect of nano-CBPs on the pulmonary and circulatory systems. Methods: We used chemical vapor deposition (CVD) without the addition of any additives to generate nano-CBPs with a particle size (electrical mobility diameter) of less than 100nm to examine the effects of inhalation exposure. Nano-CBPs were applied to a nose-only inhalation chamber system for studying the inhalation toxicity in rats. The effect on the lungs and circulatory system was determined according to the degree of inflammation as quantified by bronchoalveolar lavage fluid (BALF). The functional alteration of the hemostatic and vasomotor activities was measured by plasma coagulation, platelet activity, contraction and relaxation of blood vessels. Results: Nano-CBPs were generated in the range of 83.3-87.9 nm. Rats were exposed for 4 hour/day, 5 days/week for 4 weeks to $4.2{\times}10^6$, $6.2{\times}10^5$, and $1.3{\times}10^5$ particles/$cm^3$. Exposure of nano-CBPs by inhalation resulted in minimal pulmonary inflammation and did not appear to damage the lung tissue. In addition, there was no significant effect on blood functions, such as plasma coagulation and platelet aggregation, or on vasomotor function. Conclusion: We successfully generated nano-CBPs in the range of 83.3-87.9 nm at a maximum concentration of $4.2{\times}10^6$ particles/$cm^3$ in a nose-only inhalation chamber system. This reliable method can be useful to investigate the biological and toxicological effects of inhalation exposure to nano-CBPs on experimental rats.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1988년도 학술대회지
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• pp.77-80
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• 1988

인삼의 효과는 인삼칠효설로 요약되듯이 각종 장기에 대하여 다양한 약리작용을 나타낸다. 이는 인삼의 약리작용을 중개하는 생체내 생리활성물질의 존재를 생각하게 되며 이같이 생리활성물질을 하나로 prostaglandin을 들 수 있다. 본 연구에서는 인삼성분이 prostaglandin 등 arachidonic acid 대사산물 생성에 미치는 영향을 실험함으로써 인삼의 약리학적 작용과 그 기전을 간접적으로 구명하고자 하였다. 즉 $[^{3}H]$-arachidonic acid를 기질로 넣어주고 토끼 신장 microsome, 소 대동맥 microsome, 사람 혈소판 homogenate 등을 효소원으로 한 in vitro 생합성과정에 변화를 주는 수종 인삼 saponin 및 phenolic acid 성분의 효과를 검정하였다. 실험에 사용한 인삼 saponin 성분은 panaxadiol, panaxatriol 및 protopanaxadio 계 saponin 류인 ginsenoside $Rb_{2}(G-Rb_{2})$, ginsenoside Rc(G-Rc) 및 protopanaxatriol 계 saponin류인 ginsenoside Re(G-Re) 이었고 이들 성분이 arachidonic acid로부터 cyclooxygenase를 통해 최종 대사산물인 prostaglandin 류를 생성하는 과정에 미치는 영향을 관찰하여 다음과 같은 결과를 얻었다. 1. Arachidonic acid 로부터 생성된 총 cyclooxygenase 반응생성물 및 malondialdehyde의 양은 실험에 사용한 인삼 saponin 성분의 전 농도 범위에서 유의적인 변화를 보이지 않았는데 이는 인삼 saponin 성분들은 cyclooxygenase에 직접 작용하지 않는다는 것을 설명해 준다. 2. Panaxadiol (500 ${\mu}g/ml$은 $PGE_{2}$ 생성에는 영향이 없으나 $PGF_{2}{\alpha}$생성에 유의적인 차이를 보이지 않으나 농도의존적으로 $TxB_{2}$의 생성을 감소시켰고 6-keto-$PGF_{1}{\alpha}$의 생성을 증가시켰는데 이는 $TxA_{2}$ synthetase 억제제인 imidazole의 효과와 유사하였다. 4. G-Re는 $1{\times}10^{-5}g/ml$ 이하의 농도에서는 효과가 없으나 $1{\times}10^{-4}g/ml$ 이상의 농도에서 농도의존적으로 유의성 있는 $PGE_{2},\;PGF_{2}{\alpha},\;TXB_{2}$의 생성억제와 함께 6-keto-$PGF_{1}{\alpha}$ 증가를 보였다. 이는 prostacyclin synthetase를 자극하는 serotonin의 효과와 같은 작용으로서 prostacyclin synthetase 억제제인 tranylcypromine에 대하여 길항효과를 보였다. 5. $TxB_{2}$생성억제 작용을 나타내는 ginsenoside들의 효과를 뒷받침하기 위하여 인삼 saponin 성분을 전처치한 patelet rich plasma에서 혈소판 응집시험 결과, ADP로 유도된 혈소판 응집반응에는 모든 인삼 saponin 성분들이 효과가 없었으나 arachidonic acid로 유도된 혈소판 응집반응에는 $G-Rb_{2}$, G-Rc, G-Re의 순으로 농도 의존적인 억제현상을 보였다. 이상의 결과와 같이 인삼 saponin 성분들은 arachidonic acid로부터 cyclooxygenase를 통해 일단 생성된 endoperoxide에서 각각의 prostaglandin을 생성하는 효소, 특히 $G-Rb_{2}$는 $TxA_{2}$ sysnthetase에 강력한 억제제로, G-Re는 prostacyclin 생합성의 촉진제로 심혈관계 균형에 기여하리라 생각된다.

• 대한족부족관절학회지
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• 제18권4호
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• pp.159-164
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• 2014

Purpose: The purpose of this study is to confirm the effect of antiplatelet drugs in diabetic peripheral vasculopathy in diabetic foot patients. Materials and Methods: We designed a retrospective study in diabetic foot patients with diabetic peripheral vasculopathy. From October 2007 to December 2013, 278 cases in 139 patients who took antiplatelet drugs over at least a six-month period were included in this study. We categorized these patients according to the type of drug used. The efficacy of antiplatelet drugs was evaluated using anklebrachial index (ABI) and pulse wave velocity (PWV). Results: Only the aspirin group showed a statistically significant increase of ABI after antiplatelet therapy ($1.10{\pm}0.12$ to $1.12{\pm}0.11$). In addition, only the cilostazol group showed a statistically significant decrease of PWV after antiplatelet therapy ($1,701.20{\pm}396.56$ to $1,627.42{\pm}324.98$). Conclusion: Aspirin and cilostazol may be used in treatment of diabetic peripheral vasculopathy, whereas dual antiplatelet therapy with aspirin and clopidogrel has no specific benefits in diabetic peripheral vasculopathy.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.110.3-111
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• 2003

In the previous studies, we have reported that NQ30l, a synthetic l,4-naphthoquinone derivative, displayed a potent antithrombotic activity, and that this might be due to antiplatelet effect, which was mediated by inhibition of cytosolic $Ca^{2+}$ mobilization in activated platelets. In the present study, the effect of NQ301 on arachidonic acid cascade in activated platlets was examined. NQ301 concentration-dependently inhibited washed rabbit platelet aggregation induced by collagen (10 $\mu$g/ml), arachidonic acid (100 $\mu$M) and U46619 (1 $\mu$M), a thromboxane $A_2$receptor agonist, with $IC_50$ values of 0.60$\pm$0.02, 0.79$\pm$0.04 and 0.58$\pm$0.04 $\mu$M, respectively. (omitted)

• Journal of Ginseng Research
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• 제46권3호
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• pp.387-395
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• 2022

Background: Fermentation may alter the bioavailability of certain compounds, which may affect their efficacy and pharmacological responses. This study investigated the antiplatelet effects of red ginseng extract (RGE) and fermented red ginseng extract (FRG). Methods: A rodent model was used to evaluate the antiplatelet and antithrombotic effects of the extracts. Rats were orally fed with human equivalent doses of the extracts for 1 week and examined for various signaling pathways using standard in vivo and ex vivo techniques. Light transmission aggregometry was performed, and calcium mobilization, dense granule secretion, integrin α_IIbβ₃-mediated signaling molecules, cyclic nucleotide signaling events, and various protein molecules were evaluated ex vivo in collagen-stimulated washed platelets. Furthermore, antithrombotic properties were evaluated using a standard acute pulmonary thromboembolism model, and the effects on hemostasis were investigated using rat and mice models. Results: Both RGE and FRG significantly inhibited platelet aggregation, calcium mobilization, and dense granule secretion along with integrin-mediated fibrinogen binding and fibrinogen adhesion. cAMP levels were found to be elevated in RGE-treated rat platelets. Ginseng extracts did not exert any effect on prothrombin time and activated partial thromboplastin time. RGE-treated mice showed significantly better survival under thrombosis than FRG-treated mice, with no effects on hemostasis, whereas FRG-treated mice exhibited a slight increment in bleeding time. Conclusion: Both extracts, especially RGE, are remarkable supplements to maintain cardiovascular health and are potential candidates for the treatment and prevention of platelet-related cardiovascular disorders.

• 생명과학회지
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• 제19권4호
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• pp.508-513
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• 2009

우리나라에서 자생하고 있는 소나무류 가운데 대표적인 적송(pinus densiflora)을 열수 및 아임계 추출하여 콜레스테롤식이에 의해 혈 중 지질함량이 증가한 상태에서 흰쥐의 지질 및 혈류, 혈소판 응집 억제를 통하여 적송잎이 혈행 및 혈청 중의 지질개선에 미치는 영향을 검토하였다. 본 실험에서는 콜레스테롤식이로 혈행 장애와 혈중의 높은 지질함량을 유도시키기 위해 흰쥐에게 3주간 0.5%콜레스테롤 식이를 투여하였고 적송의 효능을 검토하기 위해 적송잎의 열수 및 아임계추출물을 병합 투여하여 실험하였다. 그 결과 혈청 중 중성지방 및 총콜레스테롤 함량은 적송잎 추출물 투여(열수 및 아임계추출)에 의해 저하되었으며, 특히 중성지방 함량을 유의적으로 감소시키는 결과를 나타내었다. 한편 Hdl-콜레스테롤 농도는 콜레스테롤 식이 투여에 의해 감소하였으나, 적송잎 열수 및 아임계추출물 투여에 의해 증가되었다. Ldl-콜레스테롤과 동맥경화지수(AI)와 심혈관위험지수(CRF) 또한 적송잎 추출물 투여에 의해 저하되었다. 콜레스테롤 식이 투여로 인해 혈장 내 혈액응고인자(coagulation factors)의 지나친 활성화 및 혈소판 응집 촉진으로 혈류의 모세관 통과 시간이 늦어 졌으나, 적송잎 추출물의 투여로 인해 혈류의 속도가 빨라짐을 볼 수 있었고, 이는 적송잎이 혈액의 유동성에 좋은 영향을 줄 것으로 사료되어진다. 적송잎 추출물의 항혈소판 응집에 미치는 영향을 검토한 결과, 0.5%콜레스테롤 식이 투여(0.5%CHOL)군의 경우 대조군(CON)에 비해 혈소판이 응집되는 결과가 나타난 반면 적송잎 추출물을 투여한 군은 0.5%CHOL군에 비해 혈소판 응집이 억제되는 것으로 나타났다 이상의 결과로 미루어 적송잎이 혈행 개선과 혈청 중의 지질개선 효과를 나타내어 동맥경화증, 혈전증 등의 혈관 관련성 질환에 효과가 있을 것으로 기대되며, 기능성 식품 및 식재료로 사용하기 위한 앞으로의 더욱 구체적인 연구가 필요한 것으로 사료된다.

• 한국식품저장유통학회지
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• 제21권5호
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• pp.727-734
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• 2014

식용 및 약용으로 이용되고 있는 우엉 지하부의 혈전 관련 활성과 항산화 활성을 평가하고자, 우엉의 ethanol 추출물 및 이의 순차적 유기용매 분획물을 조제하여 혈액응고 저해 활성, 혈소판 응집저해 활성, 인간 적혈구 용혈활성 및 in-vitro 항산화 활성을 평가하였다. 먼저 우엉 추출 수율은 10.94%로 다른 식용 및 약용식물보다 높았으며, ethanol 추출물의 경우 total polyphenol 함량은 5.01 mg/g으로 낮았으나, 694.53 mg/g의 높은 총당 함량을 나타내었다. 순차적 유기용매 분획의 경우, n-hexane, ethylacetate(EA), n-butanol 분획 수율은 각각 1.62, 0.42 및 5.98%로 나타났으며, 물 잔류물은 85.38%였다. 우엉 시료들의 혈액응고 저해활성을 TT, PT, aPTT를 측정한 결과, ethanol 추출물에서는 유의적인 활성이 나타나지 않았으나, EA 분획에서 강력한 TT, PT, aPTT 연장효과를 확인하였으며, 농도 의존적 혈액응고 저해활성을 확인하였다. 한편 물 잔류물에서는 내인성 혈액응고인자 활성화에 의한 aPTT 감소효과를 확인하여 혈전생성 촉진효과가 있음을 확인하였다. 혈소판 응집저해 활성평가의 경우, 우엉 ethanol 추출물 및 분획물들은 임상에서 사용하는 항혈소판제인 아스피린보다 강력한 저해효과를 나타내었으며, 특히 EA 분획은 정제되지 않은 상태에서도 아스피린의 2배 이상의 강력한 혈소판 응집저해능을 나타내었다. 또한 항산화 활성 평가 결과, EA 분획물은 DPPH 음이온, ABTS 양이온, nitrite에 대해 우수한 소거능 및 환원력을 나타내었다. 또한 우엉 추출물과 분획물들은 0.5 mg/mL 농도까지 인간 적혈구에 대한 특이한 용혈활성을 나타내지 않았다. 상기 결과들은, 우엉 EA 분획물이 천연물 유래의 안전한 항혈전제로 개발 가능함을 제시하고 있다.