花生四烯酸在紫杉醇生物合成途径上作用位点的研究

利用短期诱导实验,分析了花生四烯酸对红豆杉细胞培养中紫杉烷合成的影响,在适宜浓度的花生四烯酸诱导下,紫杉醇的产量提高了近３倍,同时１０－去乙酰基巴卡亭Ⅲ（ＤＡＢ）巴卡亭Ⅲ相应上升。结合花生四烯酸短期诱导实验结果,提出了花生四烯酸的加入提高了１０－ＤＡＢ合成通量的观点,诱导子作用位点的多诱导子配伍方案奠定了基础。     

分蘖葱头化学成分的研究

分蘖葱头AlliumcepaL.var.agrogatumDon(缩写为ACAD)为百合科葱属植物。我们曾对ACAD干扰花生四烯酸代谢系列及有效成分进行了研究[1～7]。从ACAD中分离得到了具有抑制血小板聚集作用的甲基烯丙基三硫化物(MATS)等8种含硫化合物[2]和具有降压作用的前列腺素A1[3],又测定了该植物的微量元素及氨基酸含量[4～6],且在体外实验中证明其醇提取物具有抑制血小板聚集和干扰血小板的花生四烯酸代谢,抑制其环氧化酶途径,抑制血栓素A2及12(S)-羟基-十七碳三烯酸合成的作用[1,7]。为了寻找新的生理活性成分,我们对该植物的非挥发性成分进行了…     

复方昆明山海棠颗粒对花生四烯酸致大鼠炎症模型的初步研究

目的:观察复方昆明山海棠颗粒对花生四烯酸致大鼠足趾炎症的影响。方法:采用大鼠左后足跖皮下注射花生四烯酸诱发足跖水肿,检测足跖容积的变化。结果:复方昆明山海棠颗粒高、中、低3个剂量组均能显著减小大鼠足跖水肿体积。结论:复方昆明山海棠颗粒可显著抑制花生四烯酸诱导的局部炎症反应。     

复方昆明山海棠颗粒对花生四烯酸致大鼠炎症模型的初步研究

目的：观察复方昆明山海棠颗粒对花生四烯酸致大鼠足趾炎症的影响。方法：采用大鼠左后足跖皮下注射花生四烯酸诱发足跖水肿,检测足跖容积的变化。结果：复方昆明山海棠颗粒高、中、低3个剂量组均能显著减小大鼠足跖水肿体积。结论：复方昆明山海棠颗粒可显著抑制花生四烯酸诱导的局部炎症反应。     

药物对花生四烯酸代谢的影响

 花生四烯酸(arachidonic acid,AA)的主要代谢产物前列腺素(prostaglandin,PG)和白三烯(leukotriene,LT)是两类具有高度生物活性的物质，它们参与了炎症、血检、速发性过敏反应等多种病理生理过程，因而是研究防治这些疾病的药物的重要目标。本文仅就PG和LT的生物合成、生物活性及药物对其影响作一简要介绍。     

芒果苷对血小板聚集和释放CD62P的影响

目的:观察芒果苷对人血小板聚集和活化后释放抗血小板P-选择素(CD620P)的影响。方法:采集24份健康成人外周血并分成6组,采用电阻法测定血小板聚集率;用流式细胞仪检测血小板表达CD62P的阳性率。结果:芒果苷呈剂量依赖性抑制体外胶原和花生四烯酸诱导的血小板聚集;相同浓度芒果苷对胶原及花生四烯酸诱导的聚集率,其IC50分别为140.77μg/mL和98.61μg/mL。血小板活化后表达CD62P的阳性率,在胶原诱导及花生四烯酸诱导中,与生理盐水组比较无显著性差异(P>0.05)。结论:芒果苷对血小板的聚集有抑制作用,对花生四烯酸诱导的血小板聚集抑制活性强于胶原,但对于两者诱导血小板活化后释放CD62P没有影响。     

和汉药成分与花生四烯酸代谢

介绍了各种和汉药成分对花生四烯酸代谢和（或）白细胞脱颗粒及血小板的影响。     

广西眼镜蛇毒L-氨基酸氧化酶对血小板聚集、释放及超微结构的影响

目的研究广西眼镜蛇毒L-氨基酸氧化酶(L-amino acid oxidase,LAAO)对人体外血小板聚集、释放及超微结构的影响。方法比浊法测定广西眼镜蛇毒LAAO对二磷酸腺苷(ADP)、胶原、凝血酶、花生四烯酸(AA)引起的血小板聚集率的影响,双抗夹心放免法测定GMP-140含量,并观察血小板超微结构。结果广西眼镜蛇毒LAAO剂量能明显抑制二磷酸腺苷(ADP)、胶原、凝血酶、花生四烯酸(AA)引起的血小板聚集,并呈明显的正相关;明显降低凝血酶诱导的血浆GMP-140水平,减轻血小板超微结构的损伤程度。结论广西眼镜蛇毒LAAO能明显抑制二磷酸腺苷(ADP)、胶原、凝血酶、花生四烯酸(AA)引起血小板聚集、降低凝血酶引起的血小板释放功能,减轻血小板损伤。     

麝香对离体家兔肾髓质环氧酶活性的影响

本文采用麝香醇溶成分甲醇再提取物与离体家兔肾髓质环酶、花生四烯酸液共同温育,用RIA方法分析前列腺素产物(PGE、PGF),间接观察了该药对环氧酶活性的抑制作用。结果表明,当每毫升反应液中药物的剂量为400～1600微克时,可显著地抑制花生四烯酸代谢成PGE、PGE(均P<0.01)。     

牛黄降压醇对血栓素A2,羟基花生四烯酸生物合成的影响

本文报道采用放射薄层扫描、放射自显影等现代同位素技术,研究了牛黄降压醇对兔血小板中花生四烯酸代谢的影响。结果表明:牛黄降压醇抑制血栓素A_2(TXA_2)、羟基花生四烯酸(HETE)的生物合成。提示牛黄降压醇治疗高血压病的机理可能与抑制TxA_2的生物合成有关;牛黄降压醇对心脑血管疾病的预防有一定作用。     

Effect of Desmodium adscendens fraction 3 on contractions of respiratory smooth muscle

The third flash chromatography fraction prepared from an aqueous extract of Desmodium adscendens leaves (DAF3) was evaluated for pharmacological activity using contractions of tracheal spirals and lung parenchymal strips caused by ovalbumin, arachidonic acid, histamine and carbachol. DAF3 inhibited both the early and late phases of antigen-induced contractions of both tissues dose-dependently, but had no effect on arachidonic-induced contractions. With tracheal spirals, the inhibition occurred whether the tissue was pretreated with indomethacin or not. On tracheal spirals, the maximum contraction (Emax) caused by histamine and carbachol were enhanced, but the pD2 value for histamine was not affected while that for carbachol was decreased. DAF3 had no effect on Emax or pD2 values for these agonists on lung parenchymal strips. The results suggest that DAF3 may inhibit the release of free arachidonic acid.     

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??OBJECTIVE To analyze the endogenous metabolite changes in the sera of kidney-yang deficiency syndrome mice infected with influenza virus A after intervention by ribavirin. And to explore the mechanism of pharmacological or toxicity effect of ribavirin. METHODS KM mice were randomly divided into three groups as normal group, model group and ribavirin group. Mice were infected with virus A after fifteen days Kidney-Yang deficiency syndrome was established. Ribavirin group were orally administrated with ribavirin for 6 consecutive days after inoculation, and the other two groups were given with equal volume of saline solution in the same way. Body weight, rectal temperature were recorded daily. Serum samples were collected from mouse 24 h after the last administration for HPLC-TOF/MS analysis. RESULTS The results show that ribavirin has good therapeutic effects on the lung index and high mortality rate of mice model. Compared with normal and model groups, the body weight and rectal temperature of them performed falling continuously. The LC-MS data were analyzed with multivariate statistical analysis and 14 potential metabolic markers were obtained which contained D-glucose, sphinganine, linoleic acid and so on. In ribavirin group, metabolism of linoleic acid, arachidonic acid and sphinganine appeared the trend of normal. And sugar and glycerophospholipid became disorders. CONCLUSION The metabolomics study and pharmacological experiment show that ribavirin might play a role of efficacy in a way that has close correlation with the linoleic acid, arachidonic acid and sphingolipid metabolic pathways. And the toxicity effect may be related to sugar and glycerophospholipid metabolic pathways.     

单宁酸及其纳米颗粒的药理作用研究进展

单宁酸（tannic acid）存在于五倍子等中药中，是一种简单的水解鞣质类化合物，是许多传统鞣质类药物的关键成分，具有抗氧化、抗炎、抗肿瘤等药理作用，已获得美国食品药品监督管理局的安全认证，并被广泛应用于食品添加剂领域。经纳米化处理后，单宁酸的生物利用度和药效得以显著提高，从而赋予其更大的治疗潜力。在神经保护、抗氧化、抗炎、抗肿瘤等领域，单宁酸及其纳米颗粒表现出广泛的应用前景。通过综述单宁酸及其纳米颗粒在药理研究方面的最新进展，为进一步探讨其在促进人体健康方面的应用提供新思路。     

Pharmacology of oleanolic acid and ursolic acid

Oleanolic acid and ursolic acid are triterpenoid compounds that exist widely in food, medicinal herbs and other plants. This review summarizes the pharmacological studies on these two triterpenoids. Both oleanolic acid and ursolic acid are effective in protecting against chemically induced liver injury in laboratory animals. Oleanolic acid has been marketed in China as an oral drug for human liver disorders. The mechanism of hepatoprotection by these two compounds may involve the inhibition of toxicant activation and the enhancement of the body defense systems. Oleanolic acid and ursolic acid have also been long-recognized to have antiinflammatory and antihyperlipidemic properties in laboratory animals, and more research is warranted to develop a therapy for patients. Recently, both compounds have been noted for their antitumor-promotion effects, which are stimulating additional research in this field. Oleanolic acid and ursolic acid are relatively non-toxic, and have been used in cosmetics and health products. The possible mechanisms for the pharmacological effects and the prospects for these two compounds are discussed.     

Modification of arachidonic metabolism by flavonoids

The pharmacological effects of many plants depend on their flavonoid constituents. This review is concerned with the influence of flavonoids on arachidonic metabolism as the possible mechanism of action of such natural products. Especial attention has been paid to structure-activity relationships since this knowledge may allow the synthesis of more potent and selective analogs with therapeutic applications.     

通俗环毛蚓的化学成分研究

从通俗环毛蚓[Pheretimavulgaris（chen）]（沪地龙），中提取分离得到一白色结晶，经红外光谱鉴定为玻珀酸（Amberacid）；用气相色谱一质谱联用方法，分析鉴定了其中18种脂肪酸，且油酸，花生烯酸和花生四烯酸的含量较高；用氨基酸分析仪鉴定了其中的20种游离氨基酸，总游离氨基酸含量为8．629％。     

复方丹参制剂药理作用的比较研究

目的:以复方丹参片与滴丸为代表,考察二者药理作用的异同,为临床优选药物提供科学根据。方法:采用犬急性心肌缺血模型、家兔血小板聚集试验、FeCl3致家兔颈总动脉栓塞试验,比较复方丹参片与滴丸药理作用的异同。结果:片剂与滴丸均具有减轻冠脉结扎所导致的犬急性心肌缺血损伤,抑制胶原、ADP和花生四烯酸诱导的家兔血小板聚集,减轻FeCl3致家兔颈总动脉栓塞及血管内皮损伤等作用。按临床等效剂量的18倍和10倍剂量给药,片剂的作用在部分指标上强于滴丸。结论:复方丹参片与滴丸治疗冠心病有效,且片剂优于滴丸。     

石榴抗肿瘤有效成分的研究进展

石榴为药食同源的药材,具有抗肿瘤、抗炎、抗氧化、降血糖、降血压及预防心脑血管疾病等多种药理和生理作用。因此,近年来对石榴的研究与探索越来越受到世界各国相关领域的重视。在我国石榴栽培历史悠久,资源丰富,但目前国内学者对石榴的研究大多都集中在石榴多酚类或黄酮类的提取工艺报道、化学成分分离和体外药理作用等方面,对石榴中单体化合物抗肿瘤的研究方面报道较少。石榴中存在多种药效活性成分,包括鞣花酸、安石榴苷、没食子酸、石榴皮鞣素、石榴酸等。本文对其抗肿瘤作用药效成分单体化合物的研究进展进行了综述,以期为石榴抗肿瘤作用的后续研究提供参考。     

Discovery and identification of quality markers of Sparganii Rhizoma based on zebrafish thrombosis model

Objective: The aim of the present study was to determine the Q-markers of Sparganii Rhizoma against thrombus through an integration of investigations on its antithrombotic effect, content determination and spectrum-effect correlation analysis. Methods: Based on the concept of Q-Marker, Sparganii Rhizoma was investigated for the identification of chemical component. The pharmacological effects on arachidonic acid-induced thrombosis in zebrafish were also investigated. The material basis in ethanol extract was determined by HPLC-UV. Furthermore, the potential Q-markers were analyzed and predicted according to the effect-chemical correlation analysis. Finally, the anti-thrombotic Q-markers were verified through the anti-thrombotic test of monomer components. Results: The model of thrombosis zebrafish was established with larvae exposed to 100 μmol/L arachidonic acid for 1 h. Nine ingredients in Sparganii Rhizoma were identified as 5-hydroxymethylfurfural, vanillic acid, ferulic acid, p-hydroxybenzaldehyde, p-hydroxybenzoic acid, vanillin, protocatechuic acid, p-coumaric acid and isoferulic acid. According to the determination effect of zebrafish thrombosis model and HPLC content analysis results, all the other contents present positive correlation except 5-hydroxymethylfurfural, and the P values of three representative potential Q-markers (ferulic acid, protocatechuic acid and p-coumaric acid) were 0.002, 0.001 and 0.026, respectively. Conclusion: Sparganii Rhizoma showed a dose-dependent effect on the recovery of reducing cardiac red blood cell on zebrafish model. Three phenolic acids (ferulic acid, protocatechuic acid and p-coumaric acid) were proved to possess the anti-thrombotic effects which could be regarded as the potential Q-markers for quality assessment of Sparganii Rhizoma.     

脉君安片的降压抵抗机制研究

目的：研究脉君安片对自发性高血压大鼠（SHR）细胞色素P450羟化酶和肾素-血管紧张素-醛固酮系统（RAAS）的影响,探讨其降压抵抗机制。方法：12只成年SHR随机分为给药组和对照组,给药组灌胃模拟脉君安片（氢氯噻嗪10mg.kg-1.d-1,葛根素36mg.kg-1.d-1,钩藤总碱122mg.kg-1.d-1）,对照组灌胃等量去离子水。每周测血压1次,4wk后处死动物。用放射免疫法检测血浆中血管紧张素Ⅱ和醛固酮含量,实时荧光定量PCR测定组织中细胞色素P450 4A1（CYP4A1）和血管紧张素Ⅱ1型受体（AT1）mRNA的表达,western blot法测定组织中细胞色素P450 4A1（CYP4A1）蛋白的表达量。结果：与对照组相比,用药4wk时给药组不仅降压效果显著,而且显著上调CYP4A1 mRNA和蛋白水平、血管紧张素Ⅱ1型受体（AT1）mRNA水平、血浆中血管紧张素Ⅱ和醛固酮的含量。结论：脉君安片在降低血压的同时,激活了肾素-血管紧张素-醛固酮系统和花生四烯酸羟化代谢途径,对降压产生了抵抗作用。