白及非多糖组分的止血作用及其机制的初步研究

目的明确白及非多糖部分的止血作用,初步了解其止血机制。方法白及95%乙醇提取物上D101大孔树脂,经水洗脱后,用80%乙醇洗脱得到不含多糖的80%乙醇组分(BS-80EE);以小鼠全身肝素化的出血时间(BT)和凝血时间(CT)为指标考察BS-80EE的止血作用;以二磷酸腺苷(ADP)为诱导剂,采用比浊法观察BS-80EE对大鼠体内血小板聚集率的影响;通过考察BS-80EE对大鼠凝血酶时间(TT)、凝血酶原时间(PT)、活化部分凝血活酶时间(APTT)和纤维蛋白原含量(FIB),以及血小板膜糖蛋白P-选择素(P-S)、凝血酶-抗凝血酶复合物(TAT)、纤溶酶原激活物抑制剂-1(PAI-1)、D-二聚体(D-D)的影响,分别从血小板和凝血纤溶系统角度了解BS-80EE的止血机制。结果BS-80EE可剂量依赖性地缩短全身肝素化小鼠的CT和BT(P<0.01或P<0.05);明显促进ADP诱导的大鼠体内血小板聚集作用(P<0.01);明显缩短大鼠的TT值(P<0.01或P<0.05);高剂量组可明显增加FIB含量(P<0.05);中、高剂量组可明显增加P-S、TAT、PAI-1的含量,减少D-D的生成(P<0.01)。BS-80EE虽有缩短大鼠APTT和PT的趋势,但差异均无显著性。结论白及非多糖组分(BS-80EE)具有良好的止血功效,可通过促进血小板聚集和凝血而发挥止血作用。     

倒卵叶五加根中多聚糖的免疫调节作用

倒卵叶五加Acanthopanax obovatus Hoo为传统的中草药,常用作补药。它与刺五加A.senticasus同属。已证明刺五加中的多聚糖有免疫促进作用,作用通过倒卵叶五加中的多聚糖对巨噬细胞吞噬功能和特异性抗体的产生研究其免疫调节作用。将倒卵叶五加的根粉碎后以沸水提取16h,过滤除去不溶物,滤液经DIA过滤器透析,减压浓缩未透析的部位,加入三倍体积的冷乙醇即得粗品多聚糖。将它溶于蒸馏水中     

金钠多、丹参、血栓通对血液流变学影响的对比研究

通过体外试验,观察金钠多、血栓通、丹参液对病人血液流变学、血小板聚集率、纤溶活性的影响.发现降粘作用以金纳多为最强,其次为血栓通、丹参液;抑制血小板聚集的活性以金钠多作用最强,血栓通与丹参液无明显差异;在纤溶活性方面,金钠多、血栓通作用明显,丹参液未见明显作用.     

中药灯盏花合剂与灯盏花,丹参,脉络宁对血液流变学影响的对比研究

通过体外试验测定血液流变学，血小板聚集，纤溶活性等指标观察到脉络宁降粘作用最强，其次为丹参液，灯盏花合剂，灯盏花液，抑制血小板聚集的活性以灯盏花与灯盏花合剂作用最强，而且丹参液与脉络宁无明显差异，在纤溶活性方面，灯盏花液，灯盏花合剂，脉络宁作用明显，丹参液未见明显作用。     

金钠多、丹参、血栓通过血液流变学影响的对比研究

通过体外试验,观察金钠多、血栓通、丹参液对病人血液流变学、血小板聚集率、纤溶活性的影响。发现降粘作用以金钠多为最强,其次为血栓通、丹参液;抑制血小板聚集的活性以金钠多作用最强,血栓通与丹参液无明显差异;在纤溶活性方面,金钠多、血栓通作用明显,丹参液未见明显作用。     

祖帕穆达派尔糖浆不同提取物的止咳祛痰作用研究

目的评价祖帕穆达派尔糖浆水提取物与体积分数为50%的乙醇提取物的止咳、祛痰作用。方法采用小鼠浓氨水引咳法与气管段酚红排泌量法,评价2种提取物对小鼠镇咳、祛痰作用的影响。结果 2种提取物的不同剂量组与空白对照组咳嗽次数比较差异有统计学意义(P<0.01);与阳性对照组比较,水提物低剂量组止咳作用明显优于阳性对照组(P<0.01);2种提取物同等剂量比较,各组间差异有统计学意义(P<0.05);在延长咳嗽潜伏期方面,与空白对照组比较,2种提取物均能延长咳嗽潜伏期(P<0.05);与阳性对照组比较差异无统计学意义(P>0.05);等剂量组间比较差异无统计学意义。在气管分泌酚红方面,2种提取物的高、中、低剂量组与空白对照组比较差异有统计学意义(P<0.05);与阳性对照组比较,水提物低剂量组酚红排泌量优于阳性对照组(P<0.05);其余组别与阳性对照组间比较差异无统计学意义(P>0.05);2种提取物同等剂量组间比较差异无统计学意义(P>0.05)。结论祖帕穆达派尔糖浆水提取物与体积分数为50%的乙醇提取物均能明显减少咳嗽次数、延长咳嗽潜伏期和促进酚红分泌,具有止咳、祛痰作用,两者比较,体积分数为50%的乙醇提取物的止咳作用更明显。     

倒卵叶五加抗血栓有效活性成分的提取筛选

目的提取倒卵叶五加活性成分并进行药理活性筛选,确定其抗血栓活性成分。方法采用不同的提取分离方法:①水提法;②水提醇沉法;③水提后树脂柱分离法;④正交试验设计醇提法,用药理实验筛选最优的提取方法的有效活性成分。抗血栓实验采用平板法、断头脑缺血症状小鼠喘息时间实验。结果水提醇沉法所得的有效部位对抗血栓效果最好,工艺简单,生产成本较低。结论倒卵叶五加提取物含抗血栓有效活性成分。     

广西瑶药鸡爪风提取物抑制4种人肝癌细胞株体外增殖作用的研究

目的探讨广西瑶药鸡爪风(Desmos chinensis Lour.)体积分数85%乙醇提取物在体外对HCC-LM3、BEL-7404、SMMC-7721、HepG2等4种人肝癌细胞株增殖的影响。方法用体积分数85%乙醇渗漉法提取鸡爪风中组分,采用MTT法评价鸡爪风体积分数85%乙醇提取物对体外培养4种人肝癌细胞株生长的影响情况。结果给予不同质量浓度(0.8,0.4,0.2,0.1和0.05mg·mL-1)体积分数85%乙醇提取物培养HCC-LM3、BEL-7404细胞24和48h,不同质量浓度(0.5,0.25,0.125,0.075和0.037 5mg·mL-1)体积分数85%乙醇提取物培养SMMC-7721、HepG2细胞24和48h,均表现出一定的抑制细胞增殖作用,且作用随药物质量浓度增加而增大、随作用时间的延长而升高,最高抑制率达90%以上。结论鸡爪风体积分数85%乙醇提取物对体外培养的4种不同人肝癌细胞株的增殖均有抑制作用,呈剂量与时间依赖性。     

鹿衔草降血脂作用有效部位的研究

目的观察鹿衔草提取液LSA-5B大孔树脂用体积分数20%乙醇洗脱的水溶性部分和体积分数50%乙醇洗脱的鹿衔草总黄酮对小鼠的降血脂作用。方法以20 mL.kg-1的体积分数为75%蛋黄乳剂进行腹腔注射,建立高脂血症小鼠模型,分为正常组、对照组、菲诺贝特(阳性药)对照组,体积分数20%乙醇洗脱的水溶性部分和鹿衔草总黄酮按剂量等级,灌胃给药,测定胆固醇(TC)、三酰甘油(TG)及高密度脂蛋白(HDL-C)的浓度。结果在体积分数20%乙醇洗脱的水溶性部分,其高、低剂量组对高脂血症小鼠三酰甘油有显著的降低作用。结论鹿衔草提取液LSA-5B大孔树脂体积分数为20%乙醇洗脱的水溶性部分具有降血脂作用。     

三七总皂苷对纤溶与凝血功能的影响

三七总皂苷为五加科人参属植物三七根的主要有效成分,具有活血化瘀的功效。研究表明三七总皂苷具有改善纤溶活性,降低纤维蛋白原,抑制血小板聚集,改善血液流变学,防止血栓形成等作用,从而能够改善微循环,延缓动脉粥样硬化的形成。该文就三七总皂苷对纤溶凝血功能影响的研究进展作一综述。     

吸收性氧化纤维素止血胶囊的止血作用研究

目的研究吸收性氧化纤维素止血胶囊(XYZJ)的止血作用和止血机制。方法通过小鼠凝血、断尾止血模型和大鼠血小板聚集实验,评价本品的止血作用;通过血小板活化实验研究本品的止血机制。结果本品各剂量组小鼠体外凝血和外伤出血时间明显小于对照组(P<0.05,P<0.01);本品高、中剂量组1~5min血小板聚集度明显高于对照组(P<0.05,P<0.01);本品高、中剂量组颗粒膜蛋白(CD62P)血小板阳性表达率明显高于对照组(P<0.05,P<0.01)。结论吸收性氧化纤维素止血胶囊有一定的止血作用,其止血作用可能是缩短凝血时间和增加血小板聚集度,其止血的机制可能是增强血小板活化功能。     

Pharmacological effects of the leaf-nosed viper snake (Eristocophis macmahoni) venom and its HPLC fractions.

Crude venom from Eristocophis macmahoni was demonstrated to exert a potent inhibition of human blood platelet aggregation mediated by adenosine diphosphate (ADP), platelet activating factor (PAF) and arachidonic acid (AA). The venom caused lysis of the platelets, however, the red blood cells were not lysed by the venom. Substantial oedema was produced upon injection of the venom into the rat hind paw. Contrarily, the intraperitoneal injection of the venom to the rats caused an inhibition of the carrageenin-induced rat paw oedema. However, an 100% lethality within 24 h was observed with a dose of 40 mg/kg body weight. The venom was fractionated by reverse phase high pressure liquid chromatography (HPLC) and the fractions were analyzed for their effect on ADP-induced platelet aggregation. The fraction eluted at 15.5 min (20% acetonitrile concentration) exhibited an inhibitory effect of several-fold greater potency than that of the crude venom. Fractions eluted at 18.5 min (25.4% acetonitrile concentration) and onward showed a proaggregatory but insignificant effect. It is suggested that although the venom contains pro aggregatory components, inhibition of platelet aggregation seems to be its predominant activity.     

刺五加茎时对血小板聚集功能的影响

刺五加茎叶的乙醇提取液相当于生药量25～70mg/ml,体外实验能明显地抑制ADP、胶原所诱导的家兔血小板聚集。家兔iv 700mg/kg,10min后明显抑制ADP诱导的家兔血小板聚集,大白鼠iv 1000mg/kg,30min后明显抑制ADP诱导的血小板聚集。体外实验可使家兔血浆复钙时间明显延长。     

The effect of garlic extracts on contractions of rat gastric fundus and human platelet aggregation

Garlic has been extracted and separated chromatographically into various fractions which show different degrees of activity as inhibitors of platelet aggregation and smooth muscle. The most potent smooth muscle inhibitor fraction had little activity on platelet aggregation, but μg ml⁻¹ concentrations greatly reduced the contractions of rat gastric fundus to prostaglandin E₂ and acetylcholine. Material in this fraction may contribute to some of the claimed therapeutic effects of garlic involving smooth muscle. Its identity is not known, but is different from allyl sulphide, dimethyl sulphide and diallyl disulphide. These compounds eluted earlier on liquid chromatography than the most active fraction, and they showed only modest inhibitory activity against prostaglandin E₂ and acetylcholine on rat fundus.     

迷迭香酸抗血栓和抗血小板聚集作用

迷迭香酸是丹参水溶性成分之一。大鼠体内实验(iv)表明,它能抑制静脉血栓形成。阻抑胶原诱导的血小板聚集,促进纤维蛋白溶解活性。当剂量为50及100 mg/kg时,血栓形成的抑制率分别为41.9和54.8%(P<0.vv05)。当剂量为100及150mg/kg时,血小板聚集的抑制率分别为30.4%(P<0.05)和46.4%(P<0.01),血浆优球蛋白溶解时间缩短(P<0.05)。纤维蛋白原含量无明显变化。以上结果说明,迷迭香酸有温和的抗血栓作用。其机理可能与抗血小板聚集和增强纤维蛋白溶解活性有关。     

噻氯匹定对不稳定型心绞痛病人血小板聚集和心肌缺血的影响

Objective　To observe the effects of ticlopidine on platelet aggregation and myocardial ischemia of the patients with unstable angina.     

Mechanisms of aggregation inhibition by aspirin and nitrate-aspirin prodrugs in human platelets

Objectives Aspirin is the mainstay of anti‐platelet therapy in the secondary prevention of cardiovascular disease. However, problems with aspirin safety and resistance demand clinical strategies based on multiple pharmacological approaches. Prodrugs of aspirin may offer beneficial effects in terms of gastro‐intestinal safety and multiple pharmacological approaches. However, the pharmacological profile of aspirin prodrugs in human platelets has not been completed yet. We aimed to compare the effects of aspirin and prodrugs of aspirin ( 1 – 5 ) on human platelet aggregation stimulated by ADP and collagen and associated receptor expression (GPIIb/IIIa and P‐selectin) in platelet‐rich plasma (PRP) and washed platelets (WP). Methods As aspirin is released from prodrugs following esterase hydrolysis we studied the expression and activity of butyrylcholineterase (BuChE) and carboxyesterase (CE) in plasma and platelets. The mechanism of prodrug‐induced platelet aggregation inhibition was explored by studying the effects of plasma and purified human BuChE on aggregation. Finally, the relative contribution of nitric oxide (NO) bioactivity to nitrate‐containing prodrugs of aspirin‐induced inhibition of aggregation was determined using 1H‐[1,2,4]oxadiazolo[4,3‐a]quinoxalin‐1‐one (ODQ,) a selective inhibitor of the soluble guanylyl cyclase. Key findings ST0702, 2 , a nicotinic acid‐aspirin codrug was equipotent with aspirin with respect to inhibition of collagen‐induced platelet aggregation. Compound 4 , a NO releasing aspirin was the most potent inhibitor of ADP‐induced platelet aggregation, an effect partially reversed by ODQ. The platelet inhibitory effects of aspirin prodrugs were time‐dependent as the maximal inhibitory effects against collagen‐induced aggregation were achieved by aspirin at 2 min, 1 at 5 min and ST0702 at 15 min. The aspirin prodrugs were significantly less potent in WP than in PRP and the reverse was true of aspirin. In the presence of complete BuChE inhibition in PRP, there was almost complete loss of aspirin prodrug, but not aspirin anti‐aggregatory activity. Interestingly, CE activity was observed in WP and platelet lysate with pNPA substrate. Accordingly, 1 and ST0702 retained 50% and 100% anti‐aggregatory activity at maximal concentrations in WP, which was attenuated in the presence of esterase inhibitor phenylmethylsulphonyl fluoride. Conclusions The inhibitory effect of aspirin prodrugs in PRP is due to prodrug activation by BuChE. In contrast, the platelet‐inhibitory effects of aspirin prodrugs in WP may be mediated through the activity of platelet CE. Compound 4 , a NO‐containing aspirin prodrug, may exert dual inhibitory effects in platelets. Thus, aspirin prodrugs effectively inhibit human platelet aggregation and as such may be an alternative to conventional aspirin.     

4味中药对酪氨酸酶抑制作用的探讨

目的 :研究14味中药对酪氨酸酶的抑制作用。方法:用50%乙醇提取中药有效成分 ,利用紫外分光光度法测定酶促反应的速度 ,以衡量其对酪氨酸酶的抑制作用。结果 :测得14条酶促反应时间曲线。结论 :13味中药对酪氨酸酶活性呈较好的抑制作用(P<0.01) ,除芦荟以外 ,其余中药不影响酶促反应的平衡。桃仁、僵蚕、芦荟抑制作用最好     

Inhibitory effect of ethanol extract of Piper longum L. on rabbit platelet aggregation through antagonizing thromboxane A2 receptor

Piper longum L. has been used as a crude drug for the treatment of disorders of poor peripheral blood circulation in Asia. However, the detailed mechanism of its action has not been clarified as yet. In the present study, we examined the effects of several extracts of Piper longum L. on rabbit platelet function. Thromboxane A(2) receptor agonist U46619 caused rabbit platelet aggregation, which was potently inhibited by the ethanol or butanol extract of Piper longum L. The ethanol extract inhibited U46619-induced platelet aggregation in a concentration-dependent manner, but only weakly inhibited that induced by thrombin. The maximum response to U46619 was reduced by 100% ethanol extract concentration dependently, suggesting that the inhibitory mode of U46619-induced platelet aggregation by the ethanol extract was non-competitive. The extract also inhibited U46619-induced phosphoinositide hydrolysis with a similar concentration dependency to the platelet aggregation. Furthermore, the extract inhibited binding of [(3)H]SQ29548 to thromboxane A(2) receptor in intact platelets in a concentration-dependent manner. These results suggest that Piper longum L. contains a constituent(s) that inhibits platelet aggregation as a non-competitive thromboxane A(2) receptor antagonist.