阿司匹林与DNA相互作用的光谱研究

[目的]研究阿司匹林（ASP）与DNA相互作用的机理。[方法]在pH值为4．5的Tnis—HCl缓冲溶液体系中,应用荧光光谱法和紫外光谱技术研究ASP和DNA分子间的相互作用;利用Stem-Volmer方程探讨DNA对阿司匹林的荧光猝灭机制。[结果]DNA与ASP之间存在较强的相互作用,25qc时结合常数为2．17×10^6L／mol,结合位点数为1．7735,结合方式是ASP通过嵌入结合的方式与DNA结合。[结论]该研究可为进一步研究ASP的药理活性提供重要信息。     

Platelet thromboxane synthetase inhibitors with low doses of aspirin: possible resolution of the "aspirin dilemma"

Selective pharmacological inhibition of thromboxane A2 synthesis did not prevent arachidonate-induced aggregation of human platelets in vitro. Prevention was instead achieved by a combination of thromboxane A2 inhibitors with low concentrations of aspirin. The latter partially reduced the proaggregatory cyclooxygenase products that accumulated when thromboxane A2 synthesis was blocked. The aspirin concentrations did not affect per se either platelet aggregation or prostacyclin synthesis in cultured human endothelial cells. The combination of thromboxane synthetase inhibitors with low doses of aspirin may offer greater antithrombotic potential than either drug alone.     

Aspirin: its effect on platelet glycolysis and release of adenosine diphosphate

Incubation of human platelets with aspirin inhibited glycolysis and produced a fall in the concentration of adenosine triphosphate. When platelets were exposed to collagen there was an increase in glycolysis and release of adenosine diphosphate. Prior incubation of the platelets with aspirin for 5 minutes did not totally suppress the increase in glycolysis after exposure to collagen but completely inhibited the collagen-induced reaction of the release of adenosine diphosphate. It is suggested that aspirin acts on human platelets by inhibiting both release of adenosine diphosphate and the transport of glucose across the platelet membrane.     

淀粉支载阿司匹林前药的合成及其体外释放

以淀粉和乙酰水杨酰氯为原料,合成了淀粉支载的阿司匹林高分子前药,用核磁共振谱对其进行结构表征,用紫外分光光度计测定阿司匹林的接入率,并在人工胃液和人工肠液中进行体外释放研究．结果表明,阿司匹林成功接入到淀粉分子上,该复合物在不同介质的体外释放中均呈现零级缓慢释药且释药的开始阶段无爆释现象出现,与阿司匹林相比较,其作用时间明显增长,有望显著减轻药物对胃粘膜和肠的刺激作用．     

浸种对油松种子发芽的影响

测定了阿司匹林、GA和稀土不同浓度、不同浸泡时间交互作用对油松种子发芽的影响,同时测定了水中不同浸种时间对油松种子发芽的影响。结果表明:浸种时间36 h、阿司匹林浓度0.05%、GA浓度50 mg/kg时种子发芽势较高,稀土作用不大;水中浸泡时,浸泡时间以36 h较好,种子发芽势较高。     

The ancient drug salicylate directly activates AMP-activated protein kinase

Salicylate, a plant product, has been in medicinal use since ancient times. More recently, it has been replaced by synthetic derivatives such as aspirin and salsalate, both of which are rapidly broken down to salicylate in vivo. At concentrations reached in plasma after administration of salsalate or of aspirin at high doses, salicylate activates adenosine monophosphate-activated protein kinase (AMPK), a central regulator of cell growth and metabolism. Salicylate binds at the same site as the synthetic activator A-769662 to cause allosteric activation and inhibition of dephosphorylation of the activating phosphorylation site, threonine-172. In AMPK knockout mice, effects of salicylate to increase fat utilization and to lower plasma fatty acids in vivo were lost. Our results suggest that AMPK activation could explain some beneficial effects of salsalate and aspirin in humans.     

采前氯化钙和阿司匹林处理对芍药切花保鲜的影响

采前处理即在鲜花栽培的适宜时期如花蕾期进行处理.如果采前处理能改善切花品质,延长切花寿命,无疑与采后保鲜相比更方便、实用、环保.为了探讨采前保鲜剂的处理效果,试验以芍药品种锦红为试验材料,用不同浓度的Ca2+和阿司匹林(Aspirin)的复配液进行采前处理,分别测定切花花朵直径、花瓣花青素含量、花瓣细胞膜相对透性、花瓣蛋白质含量、花枝叶片叶绿素的含量,分析其对瓶插锦红切花寿命的影响.结果表明,切花花朵直径、花瓣花青素含量、花瓣细胞膜相对透性、花瓣蛋白质含量、花枝叶片叶绿素含量所有处理间均存在一定的差异.虽然各个处理间差异显著性变化规律不明显.但综合分析结果仍可以看出,15 mg·L-1阿司匹林+3 000 mg·L-1 CaCl2(处理4)的复配液处理效果最好.     

2味中药复方对大鼠胃黏膜损伤保护作用及血液指标的影响

[目的]观察2味中药复方(LWZY)抗大鼠胃黏膜损伤作用及对血液指标的影响。[方法]采用无水乙醇致大鼠胃黏膜损伤模型、阿司匹林致大鼠胃黏膜损伤模型、盐酸致大鼠胃黏膜损伤模型,预防性灌胃给药,以胃黏膜的损伤指数、凝血酶原时间(PT)、纤维蛋白原(FIB)、活化部分凝血活酶时间(APTT)、凝血酶时间(TT)为指标,评价2味中药复方药剂对各动物模型的抗胃黏膜损伤作用及对血液指标的影响。[结果]西米替丁及LWZY各给药组对阿司匹林大鼠胃黏膜损伤模型、盐酸大鼠胃黏膜损伤模型、无水乙醇大鼠胃黏膜损伤模型均有明显的保护作用,各给药组胃黏膜损伤指数均较模型组明显降低(P0.05;P0.01);无水乙醇模型中的血液值;LWZY组较模型组比较PT、FIB、APTT、TT值有明显降低(P0.05;P0.01),有统计学意义;盐酸模型中的血液值,模型组PT、FIB、APTT、TT值较正常组比较略有升高,LWZY组较模型组比较PT、FIB值有明显降低,但无统计学意义,而APTT、TT值有明显降低(P0.05;P0.01),有统计学意义;阿司匹林模型中的血液指标中模型组PT、FIB、APTT、TT值较正常组比较明显升高,LWZY组较模型组比较PT、FIB、APTT、TT值有明显降低(P0.05;P0.01),有统计学意义。[结论]LWZY对无水乙醇、阿司匹林、盐酸致大鼠胃黏膜损伤有明显的保护作用,并且有一定的体内促凝血作用,作用机制可能和凝血因子以及调节激素水平有关。     

Aspirin: action on receptor in the tooth

Impulse frequency recorded from dentinal receptors in the cat's tooth provided an indication of sensory excitation. Topical application of aspirin to the dentin promptly inhibited both steady-state discharge and response to a brief heat stimulus. When the drug was washed out, the initial excitability was restored in 15 minutes.     

热应激状态下阿司匹林对蛋鸡产蛋性能和蛋品质的影响

在热应激条件下,研究了不同水平阿司匹林对蛋鸡产蛋性能和蛋品质的影响,并探讨了其作用机制.结果表明:蛋鸡日粮中添加500和1 000 mg/kg阿司匹林分别能显著提高产蛋率6.60%(P<0.05)和7.46%(P<0.05),降低料蛋比6.22%(P<0.05)和7.05%(P<0.05);500、1 000和1 500 mg/kg阿司匹林均能提高蛋壳厚度(P<0.05)和蛋壳相对重(P<0.05),并降低破蛋率和异常蛋的百分率(P<0.01).研究发现,适量阿司匹林可以提高血清中总蛋白(P<0.05)和白蛋白含量(P<0.05),降低尿酸含量(P<0.05);并提高碱性磷酸酶活性(P<0.05)、血清钙(P<0.05)和磷(P<0.05)的水平.阿司匹林还具有提高促卵泡生成素(FSH)(P<0.01),降低三碘甲腺原氨酸(T3)、甲状腺素(T4)(P<0.05),提高甲状旁腺素和前列腺素(P<0.05)的作用.上述结果提示:在热应激条件下,阿司匹林通过影响神经内分泌活动,可以促进蛋白质和钙、磷的代谢,提高蛋鸡产蛋率和改进蛋壳品质.     

Pulmonary alveolar hypoxia: release of prostaglandins and other humoral mediators

Hypoxic ventilation of isolated perfused cat lungs caused the frequent appearance in pulmonary perfusates of biologically active substances, which included prostaglandins or prostaglandin-like compounds. In anesthetized cats, inhibition of prostaglandin biosynthesis with infusions of aspirin (more than 50 milligrams per kilogram) reduced the pulmonary vasoconstrictor and bronchoconstrictor responses to hypoxic breathing.     

Arachidonic acid causes sudden death in rabbits

Injection of sodium arachidonate (1.4 milligrams per kilogram) into the marginal ear veins of rabbits caused death within 3 minutes. Histological examination showed platelet thrombi in the microvasculature of the lungs. Rabbits were protected from the lethal effects of arachidonic acid by pretreatment with aspirin. Fatty acids closely related to arachidonic acid did not cause death.     

大黄提取液对大鼠颈总动脉内膜增生防治作用的研究

[目的]研究大黄提取液对大鼠颈总动脉挤压后内膜增生的防治作用。[方法]正常SD大鼠40只,随机分为动物模型组、阿司匹林组和大黄组(大黄Ⅰ组0.45 g/kg、大黄Ⅱ组1.35 g/kg、大黄Ⅲ组4.05 g/kg)。术后30天取颈总动脉,进行形态学观察。[结果]1.大黄Ⅰ组、阿司匹林组和动物模型组血管壁组织结构基本相似,(内膜+中膜)占有率、管腔横切面积占有率均差异不显著(P>0.05)。2.与动物模型组相比,大黄Ⅱ、Ⅲ组大鼠左侧颈总动脉内膜增生均明显减轻。大黄Ⅲ组(内膜+中膜)占有率差异极显著(P<0.01),大黄Ⅱ、Ⅲ组管腔横切面积占有率均差异极显著(P<0.01)。[结论]大黄提取液对大鼠颈总动脉挤压后内膜增生具有一定的防治作用。     

Aspirin: intestinal damage in rats

Lesions induced by aspirin in the small intestine of the rat were visualized after 4 hours by the intravenous administration of a 5 percent solution of pontamine sky blue, 6 BX dye. Dose-response curves in fasted and fed rats indicated that the fed rat was about eight times more susceptible to aspirin-induced intestinal damage than was the fasted rat, while the fasted rat was about 13 times more susceptible to aspirin-induced gastric damage than was the fed rat.     

交联辛烯基琥珀酸淀粉酯微球对阿司匹林的吸附性能研究

采用反相微乳法制备交联辛烯基琥珀酸淀粉酯微球,利用红外光谱、粒度分析仪、扫描电镜和X射线衍射仪对微球进行表征,研究微球对阿司匹林的吸附性能,采用单因素固定变量法探讨投药量、交联剂用量、反应时间对吸附量的影响。结果表明:原淀粉已成功酯化交联合成变性淀粉微球,微球平均粒径为42.61μm,粒径在80μm以下占93.7%;微球表面粗糙多孔,外观圆整,由原淀粉颗粒的晶体形态变为无定性态;在交联剂用量1.5 g,反应时间3.5 h,投药量22 mg的最佳制备条件下,微球的载药量达到21.48%,包封率达到97.63%,可以作为一种优良的阿司匹林吸附载体。     

阿斯匹林在黄牛体内的药代动力学研究

本文报道用高压液相色谱法研究了黄牛一次口服阿斯匹林片剂（100mg/kg）后药代动力学规律。测定条件：Nucleosil-C18,7μm,4×250mm不锈钢柱;流动相：乙腈—0．05％磷酸（30：70,V：V）;紫外检测波长：237nm。主要动力学参数：t1／2Ke,4．295±1．043hr;Tmax,4．375±0．773hr;Cnax29．18±5．121μg／ml;AUC,366．532±86．554μg／ml．hr。     

水杨酸乙酯体外抗菌活性的测定

[目的]测定水杨酸乙酯体外抗菌活性。[方法]采用琼脂稀释法进行水杨酸乙酯溶液体外抗菌活性的试验测定其最低抑菌浓度MIC值。[结果]测得水杨酸乙酯溶液体外对肠道常见细菌的MIC值为0．15～0．40mg／ml。其对各种菌都有较好的抑菌作用,对志贺氏菌属的抑制效果尤为明显。与复方乙酰水杨酸片相比,水杨酸乙酯抗菌作用强、抗菌谱广。[结论]水杨酸乙酯溶液对肠道常见细菌具有显著的抗菌作用。     

先兆子痫及子痫并发HELLP综合征的诊断与治疗（附4例报告）

先兆子痫及子痫并发ＨＥＬＬＰ综合征的典型症状为上腹部疼痛、恶心、呕吐及出血倾向等，以溶血性贫血、红细胞压积降低、外周血涂片见到异形红细胞、肝酶及胆红素升高，血小板减少等为主要诊断依据。小剂量阿斯匹林和潘生丁联合应用以抗血小板凝聚和及时终止妊娠是最为有效的治疗手段。     

东北红豆杉抗炎作用研究

[目的]研究东北红豆杉的抗炎作用。[方法]采用二甲苯致小鼠耳廓肿胀、甲醛致小鼠足肿胀的方法,以阿司匹林为阳性药对照,将东北红豆杉水煎液分为低、中、高剂量组（0．5、1．0、2．0g／ml）,观察东北红豆杉水煎液对小鼠的抗炎作用及其与剂量的关系。[结果]东北红豆杉水煎液低剂量组对二甲苯致小鼠耳廓肿胀及甲醛致小鼠足肿胀没有显著抑制作用（P〉0．05）;中、高剂量组对二甲苯致小鼠耳廓肿胀及甲醛致小鼠足肿胀均有显著抑制作用（P〈0．05）。[结论]东北红豆杉水煎液具有一定的抗炎作用。     

Study of aldose reductase inhibition in intact lenses by 13C nuclear magnetic resonance spectroscopy

Carbon-13 nuclear magnetic resonance spectroscopy has been used in the study of glucose metabolism, specifically aldose reductase inhibition, in intact rabbit lenses maintained in organ culture. This technique provides an effective method of screening potential inhibitors of aldose reductase under conditions that more closely approximate in vivo conditions than do earlier methods. The aspirin substitutes acetaminophen and ibuprofen were studied as aldose reductase inhibitors and were found to be effective in reducing sorbitol accumulation in lenses exposed to high glucose stress. Results of this work with various inhibitors of aldose reductase are discussed in terms of lens metabolism and implications regarding diabetic complications such as cataract formation.