粉防己碱特异抑制大鼠血小板聚集和ATP释放(英文)

AIM: To examine the effects of tetrandrine (Tet) on the aggregation and ATP-release of rat washed platelets induced by several platelet activators. METHODS: Gel-filtration (Sepharose 2B) was used to isolate washed platelets from adult rats and the platelet aggragation and ATP-release were measured simultaneously. RESULTS: In the presence of Ca2 1 mmol · L-1, Tet 300 μmol·L -1 inhibited the aggregation induced by ADP ( 25 μmol · L -1), collagen (2.5 g·L-1), and thrombin (103 unit·L-1) by 62 %, 60 %, and 34 %, respectively. It also inhibited arachidonic acid (1 mmol · L-1)-induced aggregation. Elevating intracellular Ca2 concentration with the Ca2 ionophore, calcimycin (30 μmol · L-1), or by blocking the intracellular calcium pump with cyclopiazonic acid (5 μmol · L-1) initiated platelet aggregation, which was also inhibited by Tet. In Ca2 -free medium, Tet still elicited an inhibitory effect on aggregation induced by ristocetin (2.5 g·L-1). Lower concentrations of Tet (30 nmol·L-1 to     

粉防己碱对兔血小板聚集和血小板活化因子生成的影响(英文)

目的:探讨粉防己碱(Tet)对兔血小板聚集和PAF生成的影响.方法:卡西霉素(Cal)和PAF诱导血小板聚集的聚集率和Tet对血小板聚集的抑制率被测定;给予或未给予Tet处理之血小板用Cal刺激释放PAF的量也被测定.结果:在4—64 μmol·L~(-1)浓度范围,Tet明显抑制Cal和PAF诱导的血小板聚集.IC_(50)值分别为8.6μmol·L~(-1)和14.0μmol·L~(-1).Tet也浓度依赖性的抑制Cal诱导血小板释放PAF,IC_(50)值为21.0μmol·L~(-1).结论:Tet抑制血小板聚集作用与抑制内源性PAF生成有关.     

粉防己碱与牛磺酸合用对血小板聚集与血栓形成的影响

粉防己碱（Ｔｅｔ）和牛磺酸（Ｔａｕ）均能抑制ＡＤＰ、胶原和凝血酶诱导的大鼠血小板聚集及血栓形成。Ｔｅｔ抑制ＡＤＰ诱导聚集较强，Ｔａｕ则对胶原作用最明显，二药减半量合并应用时，较各药单用强     

兔血小板释放的内源性5—HT对凝血酶诱导的血小板聚集和ATP释放的？…

AIM: To study the effects of arachidonic acid (AA)-induced endogenous serotonin (5-HT) release on platelet aggregation and ATP release by thrombin (Thr). METHODS: Platelet aggregation and release reaction were quantified by light transmission in platelet-rich-plasma (PRP) and the amount of ATP in medium. The effects of endogenous 5-HT were evaluated by the filtration of content in cuvette A (content A) containing endogenous 5-HT into cuvette B in which Thr-induced aggregation was observed in the absence/presence of ?(+/-)-5 (Z)-7-[3-endophenylsulfonylamino [2.2.1] bicyclohept-2-exo-yl]heptanoic acid, sodium salt? (S-145) or/and methysergide (Met). RESULTS: (1) AA 100 and 200 mumol.L-1 induced aggregation and ATP release in cuvette A. When the aggregation reached a peak, the content A directly caused platelet aggregation in cuvette B, and it was inhibited by S-145 100 nmol.L-1, Met 30 mumol.L-1, and inhibited more potently by S-145 + Met. (2) In the presence of S-145 100 nmol.L-1 in cuvette B, aggregations by Thr 0.1 and 0.3 IU.L-1 were enhanced (P < 0.01) by the filtrate, while Thr 0.5 IU.L-1-caused ATP release was suppressed (P < 0.01) without the effect on aggregation. Preincubation with S-145 and Met, the effects of the filtrate on aggregation and ATP release were abolished. (3) By prolongation of the time intervals between filtration and addition of Thr, the aggregation was enhanced and ATP release was reduced. CONCLUSION: Endogenous 5-HT was released from activated platelet and plays, in turn, a role in the regulation of platelet aggregation by the superimposition of cytosolic-free calcium ([Ca2+]i) and the feedback loop to regulate release reaction and calcium.     

粉防己碱对缺血顿抑大鼠心肌功能和ATP酶活力的影响

目的：观察粉防己碱（ｔｅｔｒａｎｄｒｉｎｅ，Ｔｅｔ）对缺血顿抑心肌的保护作用并分析与心肌ＡＴＰ酶活力的关系。方法：离体大鼠工作心脏，全心缺血３０ｍｉｎ再灌４０ｍｉｎ，无机磷显色法分析ＡＴＰ酶活力。结果：顿抑心肌收缩舒张功能均明显降低，再灌期末ＬＶＳＰ×ＨＲ仅恢复５２％±８％，ＬＶＥＤＰ抬高２９８％±６４％，ＣＯ仅恢复４０％±８％，心肌细胞膜和线粒体Ｎａ＋，Ｋ＋－ＡＴＰ酶和Ｃａ２＋，Ｍｇ２＋－ＡＴＰ酶活力均下降，Ｔｅｔ（３０ｍｇ·ｋｇ－１·ｄ－１，ｉｐ，３ｄ，１０μｍｏｌ·Ｌ－１灌流缺血全程）可使ＬＶＳＰ×ＨＲ恢复８５％±１２％，ＬＶＥＤＰ仅抬高１６６％±４４％，ＣＯ恢复７５％±１１％，心肌细胞膜及线粒体Ｎａ＋，Ｋ＋－ＡＴＰ酶和Ｃａ２＋，Ｍｇ２＋－ＡＴＰ酶活力增高。结论：Ｔｅｔ对心肌缺血后顿抑损伤有一定保护作用，这一作用与维护顿抑期心肌细胞ＡＴＰ酶活力有关。     

商陆皂甙甲抑制大鼠腹腔巨噬细胞释放血小板活化因子

卡西霉素(A₂₃₁₈₇)刺激大鼠腹腔巨噬细胞释放血小板活化因子(PAF),用洗涤血小板聚集的方法测定,证明商陆皂甙甲在0.1～100μmol/L浓度范围内及所试的时间范围内,呈剂量及时间依赖性抑制大鼠腹腔巨噬细胞释放PAF:商陆皂甙甲可能就是通过抑制体内PAF生成而起抗炎作用的。     

商陆皂甙甲抑制大鼠腹腔巨噬细胞释放血小板活化因子

卡西霉素(A_(23187))刺激大鼠腹腔巨噬细胞释放血小板活化因子(PAF),用洗涤血小板聚集的方法测定,证明商陆皂甙甲在0.1～100μmol/L浓度范围内及所试的时间范围内,呈剂量及时间依赖性抑制大鼠腹腔巨噬细胞释放PAF:商陆皂甙甲可能就是通过抑制体内PAF生成而起抗炎作用的。     

粉防己碱抑制自发性高血压大鼠心肌纤维化

目的：观察粉防己碱对自发性高血压大鼠心肌胶原和心肌僵硬度的作用。方法：测定羟脯氨酸表示胶原的量，胃酶抽提法和ＳＤＳ－ＰＡＧＥ方法测定胶原Ⅰ／Ⅲ型比例，离体灌注大鼠心脏测定左室心肌舒张僵硬度。结果：粉防己碱显著降低心肌胶原浓度和含量，降低胶原Ⅰ／Ⅲ型比例，改善心肌舒张僵硬度。结论：粉防己碱因其有效的抗纤维化作用，能逆转心肌舒张功能障碍。     

人血小板密度亚群在聚集反应,ATP释放及细胞内游离钙浓度的异质性

研究人血小板密度亚群在聚集和释放反应及细胞内钙浓度的异质性。Ｐｒｅｃｏｌ间断梯度离心法。正常人血小板分为高，中和低密度三个亚群。血小板的大小随密度的降低而减小。ＨＤ对凝血酶，ＡＤＰ和血清素诱导的聚集反应明显强于ＬＤ，ＡＴＰ释放反应，除５－ＨＴ无ＡＴＰ释放外，与聚集反应的结果一致。     

粉防己碱抑制大鼠慢性“炎症”性肺动脉高压

目的：观察粉防己碱（Ｔｅｔ）对ｍｏｎｏｃｒｏｔａｌｉｎｅ（Ｍｏｎ）引起的肺血管收缩和肺血管增生性改变的影响。方法：应用Ｍｏｎ引起的炎性肺动脉高压大鼠模型。结果：每日ｉｇ Ｔｅｔ５０,１００及１５０ｍｇ·ｋｇ＾－１,三周后肺动脉压分别比Ｍｏｎ组低２３．８％（Ｐ〉０．０５）,３４．９％（Ｐ〈０．０５）和４２．０％（Ｐ〈０．０５）;右心指数分别比Ｍｏｎ组低２．０％（Ｐ〉０．０５）,２５．０％（Ｐ〉０．０     

甲基莲心碱对大鼠血压、血小板聚集和血栓形成的影响

采用比浊法研究甲基莲心碱对大鼠血压及血小板聚集、血栓形成的影响，结果显示甲基莲心碱在降低血压的同时，能剂量依赖性地抑制ＡＤＰ和胶原诱导的正常大鼠、肾性高血压大鼠和高脂喂养大鼠血小板聚集；甲基莲心碱亦能明显延长电刺激大鼠颈动脉闭塞性血栓形成时间。此结果表明甲基莲心碱具有降压与抗血小板聚集和血栓形成的双重作用。     

粉防己碱，钩藤碱和维拉帕米对兔主动脉平滑肌细胞内外钙转运的作用

粉防己碱和钩藤碱对由高钾和去甲肾上腺素引起的兔主动脉条收缩的抑制作用没有维拉帕米强。粉防己碱，钩藤碱和维拉帕米在由去甲肾上腺素和５－羟色胺引起的两相收缩中，抑制Ⅰ相收缩的ＩＣ５０小于抑制Ⅱ相收缩的ＩＣ５０．粉防己碱，钩藤碱抑制由去甲肾上腺素引起的Ⅰ相收缩的ＩＣ５０分别是抑制高钾所致收缩的１／１２．８和１／６．但维拉帕米没有表现此种关系，三种药物均不能对抗卡西霉素引起的收缩。粉防己碱和钩藤碱能增强咖啡因所致收缩，但维拉帕米抑制之，这些结果表明粉防己碱和钧藤碱为细胞内钙动员抑制剂，而且它们的作用点不同于维拉帕米。     

粉防己碱,Fura2—AM和BayK8644对脂多糖刺激大鼠腹腔巨噬细胞释…

目的：研究化钙与脂多糖（ＬＰＳ）刺激大鼠腹腔巨噬细胞（ＰＭφ）释放血小板活化因子（ＰＡＦ）的关系，方法：通过ＰＡＦ的生物测定法，观察了粉防己碱（Ｔｅｔ），Ｆｕｒａ２－ＡＭ和Ｂａｙｋ８６４４对ＬＰＳ刺激ＰＭφ释放ＰＡＦ的影响，结果，ＬＰＳ刺激ＰＭφ释放ＰＡＦ，但并不使其细胞内钙增高，Ｔｅｔ在０．１，１．０，１０，１００μｍｏｌ．Ｌ＾－１和Ｆｕｒａ２－ＡＭ在０．０１，０．１，１０，１０μｍｏｌ．Ｌ＾－     

苦豆碱对兔血小板聚集的影响

苦豆碱抑制低浓度花生四烯酸(AA)和胶原诱导的兔血小板聚集,IC_(50)分别为184μg·L~(-1)和38.3mg·L~(-1)提高AA浓度使其抑制作用明显减弱。苦豆碱还抑制兔血小板形成血栓素B_2(TXB_2),此作用可能和其对血小板聚集的抑制有关。