Inhibiting and disaggregating effect of gel-filtered Galega officinalis L. herbal extract on platelet aggregation

The in vitro inhibiting and disaggregating effect on platelet aggregation of a gel-fractionated herbal extract from Galega officinalis L. is examined. The obtained Sephadex G-25 filtered fraction was 35-36 times more active than the crude extract. The threshold concentration at which this fraction inhibits platelet aggregation (5-10% inhibition) by 50 microM adenosine 5'-diphosphate (ADP) is 4.5-5 microg per 1 ml platelet-rich plasma (PRP). At a concentration of 35 microg/ml PRP the fraction inhibits 50% of aggregation by ADP and at a concentration of 125 microg/ml PRP fully inhibits the aggregation of PRP by ADP. At a concentration of 40 microg/ml PRP the fraction inhibits initiation of platelet aggregation by 0.18 mg/ml collagen and at 50 microg/ml PRP inhibits the initiation of aggregation by 0.7 units/ml thrombin. The G-25 filtered fraction shows a strong disaggregating effect on aggregated PRP. At a concentration of 65-75 microg/ml PRP, the fraction is able to disaggregate the 50-53% of aggregated platelet-rich plasma by 50 microM ADP, and 25% of aggregated PRP by 0.18 mg/ml collagen.     

银杏叶提取物对兔血小板聚集的影响

目的　探讨银杏叶提取物 (GBE)对兔血小板聚集作用的影响。方法　进行体内、体外实验观察银杏叶提取物 (GBE)对由花生四烯酸 (AA)、二磷酸腺苷 (ADP)及血小板活化因子 (PAF)诱导的兔血小板聚集作用的影响 ,并对其作用的特点进行了初步分析。结果　GBE体外选择性地抑制PAF诱导兔血小板聚集 (比浊法 )及 5 HT的释放 (荧光法 ) ,其抗血小板聚集和 5 HT释放的IC50 分别为 (4 7.5± 9.5 )mg·L-1和 (176 .3± 2 5 .5 )mg·L-1;银杏苦内酯B(BN5 2 0 2 1)体外抗聚集的IC50 为 (5 .5 6×10 -3 ± 1.0 1× 10 -3 )mg·L-1。体内试验GBE也选择性地抑制PAF诱导的兔血小板聚集 :静注GBE 5 0 ,10 0mg·kg-1的作用时间分别可持续 6 0 ,2 40min以上 ;灌胃 10 0 ,2 0 0mg·kg-1的作用持续时间分别可达 180 ,2 40min以上 ;静注和灌胃作用高峰时最大抑制率分别为 (96 .5± 6 .1) %,(83.3± 17.2 ) %。结论　GBE对由PAF ,ADP诱导的体内、体外兔血小板聚集有抑制作用 ,但对由AA诱导的聚集无影响。可见GBE是一种有效的、选择性较高的抗血小板聚集药物。     

Cardamom extract as inhibitor of human platelet aggregation

The inhibitory activity of cardamom extract was studied on human platelets. Platelet aggregation and lipid peroxidation were evaluated with platelet rich plasma (PRP) and platelet membranes, respectively, obtained from blood of healthy volunteers. Human platelets were subjected to stimulation with a variety of agonists including ADP (2.5 mM), epinephrine (2.5 mM), collagen (10 mM), calcium ionophore A 23187 (6 microM) and ristocetin (1.25 microg/mL). The IC50 were 0.49, 0.21, 0.55 and 0.59 mg with ADP, epinephrine, collagen and calcium ionophore A 23187, respectively, and no inhibition with ristocetin. The inhibitory effect was dose dependent with concentrations varying between 0.14 and 0.70 mg and time dependent at IC50. Lipid peroxidation induced by iron--ascorbic acid system in platelet membranes was analysed with malondialdehyde (MDA) as an index. An increase in concentration of cardamom has decreased the MDA formation significantly. Hence, it may be said that aqueous extract of cardamom may have component(s), which protect platelets from aggregation and lipid peroxidation.     

Horse chestnut extract contracts bovine vessels and affects human platelet aggregation through 5‐HT2A receptors: an in vitro study

Extract from seeds and bark of horse chestnut (Aesculus hippocastanum L) is used as an herbal medicine against chronic venous insufficiency. The effect and mechanism of action on veins, arteries, and platelets are not fully understood. The aim of this study was to investigate the effects and mechanisms of action of horse chestnut on the contraction of bovine mesenteric veins and arteries, and human platelet aggregation. Contraction studies showed that horse chestnut extract dose‐dependently contracted both veins and arteries, with the veins being the most sensitive. Contraction of both veins and arteries were significantly inhibited by the 5‐HT_2A receptor antagonist ketanserin. No effect on contraction was seen with the cyclooxygenase inhibitor indomethacin, the α₁ receptor antagonist prazosin or the angiotensin AT₁ receptor antagonist saralasin neither in veins nor arteries. ADP‐induced human platelet aggregation was significantly reduced by horse chestnut. A further reduction was seen with the extract in the presence of ketanserin. In conclusion, horse chestnut contraction of both veins and arteries is, at least partly, mediated through 5‐HT_2A receptors. Human platelet aggregation is reduced by horse chestnut. The clinical importance of these findings concerning clinical use, possible adverse effects, and drug interactions remains to be investigated. Copyright © 2010 John Wiley & Sons, Ltd.     

红花提取物抗血小板聚集及抗血栓作用的观察

我 们的实验观察了红花提取物对体外ADP诱导的血小板聚集和体内血栓 形成的作用。结果发现红花提取物能明显抑制ADP诱导的兔血小板聚集,显抑制大鼠实验性血栓形成并延长其凝血时间和凝血酶时间。     

诺迪康胶囊对大鼠血液流变学及血小板聚集的影响

诺迪康胶囊２ｇ／ｋｇ和１ｇ／ｋｇ可明显降低大鼠全血粘度、红细胞聚集指数、红细胞刚性指数，还能明显抑制血小板聚集。     

15种理气中药体外对人血小板聚集的影响

目的：观察15种理气中药对体外肾上腺素诱导的人血小板聚集的影响,方法：试管内人血小板加中药孵育前后,比浊法测定血小板聚集。结果：11种理气药理有抗血小板聚集作用（P＜0．05－0．001）,其中枳实的抑制作用较阳性对照阿司匹林明显（P＜0．01）,青皮、陈皮与阿司匹林无差异（P＜0．05）,柿蒂、甘松、檀香、沉香对血小板聚集无明显作用（P＞0．05）。结论：多数理气药（11／15）,在体具有抗人血小板聚集作用,枳实、青皮、陈皮3种作用 强于或与阿司匹林相当。     

15种理气中药体外对人血小板聚集的影响

目的观察15种理气中药对体外肾上腺素诱导的人血小板聚集的影响.方法试管内人血小板加中药孵育前后,比浊法测定血小板聚集.结果11种理气药具有抗血小板聚集作用(P＜0.05～0.001),其中枳实的抑制作用较阳性对照阿司匹林明显(P＜0.01),青皮、陈皮与阿司匹林无差异(P＜0.05).柿蒂、甘松、檀香、沉香对血小板聚集无明显作用(P＞0.05).结论多数理气药(11/15)在体外具有抗人血小板聚集作用,枳实、青皮、陈皮3种作用强于或与阿司匹林相当.     

天麻素对家兔体外血小板聚集的影响

目的：研究天麻素对ADP、AA、PAF体外诱导家免血小板聚集的影响。方法：比浊法测定血小板的聚集率。结果：与对照组比天麻素在0.034mmol／L、0.34mmol／L和3．4mmol／L三种浓度下对ADP、AA、PAF三种诱导剂诱导的血小板聚集的聚集率的差异均无显著性意义。结论：天麻素体外无抗血小板聚集作用。     

6种黄酮对大鼠血液流变学指标的影响

目的观察6种黄酮对大鼠血液流变学指标的影响。方法将Wister大鼠60只随机分成6组,即淫羊藿总黄酮组、骨碎补总黄酮组、菟丝子总黄酮组、柚皮甙组、槲皮素组、橙皮甙组,每组10只。6组分别皮下注射去甲肾上腺素大鼠血瘀模型造模。第2d6组分别按200mg／kg的剂量予淫羊藿总黄酮、骨碎补总黄酮、菟丝子总黄酮、柚皮甙、槲皮素、橙皮甙灌胃,每日1次,连续21d。于第22d分离大鼠腹主动脉取血,观察各组血液流变学指标。结果6种黄酮中骨碎补总黄酮与淫羊藿总黄酮对血液流变学全血黏度、红细胞聚集指数的影响作用较明显（P〈0．05）,柚皮甙、菟丝予总黄酮、橙皮甙、擗皮素则无明显影响。结论6种黄酮比较,骨碎补总黄酮与淫羊藿总黄酮可有效降低血液黏度,防止红细胞聚集。     

大豆异黄酮苷元对糖尿病大鼠血小板聚集的抑制作用

目的:研究大豆异黄酮苷元对血小板聚集性的影响。方法:普通饲料中添加20g/kg大豆异黄酮苷元混合物,饲喂糖尿病大鼠20周,测定其血小板聚集率。利用ODS柱层析和高效液相色谱技术分离大豆异黄酮苷元,体外观察大豆异黄酮苷元单体对人血小板聚集率的影响。结果:长期食用大豆异黄酮苷元的糖尿病大鼠血小板聚集率显著降低。在人体外血小板聚集实验中,大豆异黄酮苷元均抑制ADP、胶原蛋白和肾上腺素诱导的血小板聚集,其中金雀异黄素为最强,其半抑制浓度(IC50)值分别为0.38,0.30,0.23mmol/L。结论:大豆异黄酮苷元具有血小板聚集抑制效应,在大豆抗血小板聚集中起着重要作用。     

麻黄体外透皮吸收特性研究

目的:研究麻黄的透皮吸收特性.方法:采用体外透皮实验方法,以Valia-Chien扩散池为实验装置,研究不同因素对麻黄碱和麻黄提取物透皮吸收的影响.结果:麻黄碱和麻黄提取物的渗透性随其浓度增大而增强,pH对麻黄透皮吸收有较大影响.结论:为研究麻黄透皮吸收制剂提供参考.     

黄山药总皂苷和薯蓣皂苷元抗高脂血症及体外抗血小板聚集的比较

 目的：比较黄山药总苷(DX)和薯蓣皂苷元(Dio)抗实验性高脂血症及体外抗血小板聚集作用强度。方法：给小鼠和大鼠喂饲高胆固醇饲料造成高脂血症模型，之后灌胃或腹腔注射给予DX和Dio，测定血清胆固醇含量。结果：给小鼠灌胃DX（400和200 mg·kg^-1）和Dio(160和80 mg·kg^-1)时，Dio对小鼠高胆固醇血症有明显预防和治疗作用，而DX只有大剂量时才有一定预防作用。腹腔注射给药时，Dio(40和20 mg·kg^-1)仍然有效，但DX无效。给大鼠灌胃DX(400和200 mg·kg-1)和Dio(200和100 mg·kg^-1)，均能明显降低血中总胆固醇含量，但在上述剂量，Dio的预防效果明显优于DX。DX(60～240 μg·ml^-1)和Dio(30～120 μg·ml^-1)体外有明显的抗血小板聚集活性，但Dio的抑制率明显高于DX。结论：Dio抗高脂血症及抗血小板聚集作用明显优于DX。     

地锦草对血小板数、血小板聚集性及血脂的影响

目的:探讨地锦草止血作用机理及对血脂的影响。方法:Wistar 大鼠每日1次中药灌胃1.4ml/100g,连续15日,进行如下测定:(1)每2日在尾部采血进行血小板计数;(2)15日后采血测定血小板聚集性;(3)15日后测定血脂。结果:地锦草能快速增加血小板数量(P<0.01),且随给药时间延长,血小板的数量也不断增加;15日后血小板聚集作用显著增强(P<0.01),地锦草还可使甘油三酯和胆固醇显著降低(P<0.01)。结论:地锦草使血小板数不断升高,可能与其兴奋脾脏造血系统有关,地锦草可能通过增强凝血酶的作用,诱导 Ca~(2 )大量释放,加速血小板的聚集反应,这些作用可能与血小板激活因子(PAF)无关。     

桃红四物汤各分离部位对体外ADP诱导血小板聚集、凝血酶活性的影响及效应物质基础研究

评价桃红四物汤各分离部位对体外二磷酸腺苷(ADP)诱导血小板聚集及凝血酶活性的影响,探讨其效应物质基础。采用比浊法测定体外ADP诱导家兔血小板聚集率;采用改进凝血酶时间法测定抑制凝血酶活性;采用UPLC-Q-TOF-MS对各分离部位进行定性分析鉴定。桃红四物汤醇沉沉淀部位、醇沉上清液部位及20%~30%醇洗脱部位对ADP诱导的血小板聚集具有显著的抑制作用;水不溶部位、醇沉上清液部位及40%~70%醇洗脱部位具有显著的抑制凝血酶活性的作用;芳香酸类成分、苷类成分和苯酞类成分是醇沉沉淀部位、醇沉上清液部位及20%~40%醇洗脱部位的主要成分。桃红四物汤抑制ADP诱导家兔血小板聚集及抑制凝血酶活性的主要效应物质基础是芳香酸类成分、苷类成分和苯酞类成分。该实验为进一步探讨活血化瘀方桃红四物汤治疗血瘀证的物质基础及作用机制提供了科学依据。     

Feroniellin B, a new highly potent human platelet aggregation inhibitor from Feroniella lucida

Human platelet aggregation inhibition by coumarins isolated from Feroniella lucida roots extract was investigated. Of 11 coumarins examined, feroniellin B highly inhibited platelet aggregation induced by ADP with an IC(50) value of 0.287 mm while the standard drug ibuprofen displayed this inhibition with an IC(50) value of 11.2 mm. The presence of feroniellin B is possibly linked to the ethnopharmacological use of F. lucida as a remedy for cardiovascular diseases.     

Effects of Panax notoginseng saponins on platelet aggregation in rats with middle cerebral artery occlusion or in vitro and on lipid fluidity of platelet membrane

The effects were examined of Panax notoginseng saponins (PNS) on platelet aggregation in vivo or in vitro and on lipid fluidity of the membrane. PNS (200 mg/kg i.p. ×1 d or ×3 d) significantly inhibited abnormal increases of platelet aggregation and platelet adhesiveness in rats subjected to permanent occlusion of the middle cerebral artery (MCAO). Platelet aggregation induced by ADP in vitro was also inhibited by PNS in a concentration-related manner. PNS could increase the fluidity of platelet membranes. The findings in this study suggest that the anticerebral ischaemic effect of PNS depends, at least partially, for its actions on blood platelets. © 1998 John Wiley & Sons, Ltd.     

肿节风水提物及其市售制剂的HPLC特征图谱研究

目的建立肿节风水提物的HPLC特征图谱并明确其特征色谱峰的化学成分,对肿节风水提物及其市售制剂的质量进行评价。方法以Ultimate XB-C18色谱柱(250 mm×4.6 mm,5μm),乙腈-水(各含0.1%甲酸)为流动相梯度洗脱,体积流量为1.0 mL/min,柱温:30℃,检测波长为330 nm;以共有模式特征图谱为对照,对不同厂家的肿节风水提物及其市售制剂进行相似度评价。结果建立的肿节风水提物的HPLC特征图谱具有良好的稳定性、精密度、重现性。不同厂家生产的12批肿节风水提物及20批市售制剂与共有模式对照特征图谱的相似度分别在0.883~0.987和0.797~0.982。其中8个特征色谱峰经化学指认,分别为新绿原酸、绿原酸、隐绿原酸、-βhydroxypropiovanillone、咖啡酸、异嗪皮啶、迷迭香酸-4-O-葡萄糖苷和迷迭香酸。结论本研究建立了涵盖肿节风中抗炎活性成分与特征成分的HPLC特征图谱,反映了肿节风水提物及相关制剂的多成分的整体面貌,为全面、有效控制肿节风及相关制剂的质量奠定了科学基础。     

淫羊藿提取物对小鼠T淋巴细胞体外活化和增殖的影响

目的研究淫羊藿水溶性提取物对刀豆蛋白A(ConA)刺激的小鼠T淋巴细胞体外早期活化和增殖的影响。方法无菌分离小鼠各部位淋巴结,制备单细胞悬液,加入不同终质量浓度(5、25、50mg/L)的淫羊藿提取物,以MTT法检测药物对T细胞活性的影响;利用流式细胞术(FCM)结合双色荧光抗体染色技术检测早期活化标志CD69分子的表达;运用流式细胞术结合活体染料CFDA-SE染色技术和荧光抗体染色技术检测T细胞增殖。结果MTT法检测淫羊藿提取物在50mg/L时细胞存活率达52.36%。ConA作用6h后,对照组CD69 表达率为(4.61±0.85)%,ConA组CD69 T细胞的比率上升至(38.30±2.54)%,淫羊藿提取物在终质量浓度5、25、50mg/L时均抑制ConA诱导的CD3 T淋巴细胞CD69的表达(P<0.01),其表达率分别下调为(36.16±2.14)%,(30.5±1.72)%,(15.99±0.87)%。培养48、72后,对照组增殖指数(PI)分别为1.01±0.01和1.05±0.01,ConA组PI分别达到1.42±0.01、2.32±0.01,淫羊藿提取物在终质量浓度5、25、50mg/L均抑制T淋巴细胞增殖(P<0.01),48h时PI分别为1.28±0.01、1.26±0.01、1.21±0.01;72h时PI分别为2.30±0.03、2.13±0.02、2.10±0.01。结论淫羊藿提取物能明显抑制ConA刺激的小鼠T淋巴细胞的早期活化和增殖,并呈剂量依赖性。     

银杏二萜内酯A,B,K抗血小板聚集作用机制研究

为研究银杏二萜内酯A,B,K(GA,GB,GK)对家兔血小板聚集功能的影响,比较三者作用机制的异同及强弱,该研究采用体外实验法,观察不同剂量GA,GB,GK对血小板活化因子(PAF)诱导家兔血小板聚集作用的影响。研究结果显示,3种银杏二萜内酯均可抑制PAF诱导的体外家兔血小板聚集,其强弱顺序为GKGBGA;三者还能够拮抗[~3H]PAF与PAF受体的特异性结合,拮抗能力同样为GKGBGA。进一步研究三者对于PAF诱导后血小板中胞内[Ca~(2+)]i动员及胞内c AMP水平的变化,发现三者均能够剂量依赖性的抑制胞内[Ca~(2+)]i动员并提高胞内c AMP水平,且它们的作用强弱与拮抗PAF受体能力的强弱一致。表明银杏二萜内酯GK对于PAF受体具有高度的选择性,并能够通过激活c AMP信号通路、抑制胞内[Ca~(2+)]i动员的方式达到抑制血小板聚集的目的,GB、GA对PAF受体也有较强的拮抗作用,但弱于GK。