连翘酯苷的研究进展

连翘酯苷作为连翘属植物中的主要有效成分之一,目前被广泛研究.连翘酯苷是一种还原剂,具有多种药理作用,包括有很强的抗菌活性,其抗菌谱广,并有较强的抗病毒和抗氧化活性,还有解热镇痛和免疫调节作用,为此,是一种多功效的中药活性成分,具有较大的研究价值.     

连翘叶中7种成分的抗氧化活性研究

试验旨在筛选出连翘叶抗氧化的主要药效物质，探讨其抗氧化的作用效果。采用化学法、过氧化氢诱导巨噬细胞RAW264.7损伤模型，以清除DPPH自由基、ABTS自由基、·O2-自由基和细胞抗氧化酶活力为指标，综合评价连翘叶中7种成分的抗氧化活性。结果显示，连翘叶中连翘酯苷A (FSA)、连翘酯苷B (FSB)、连翘酯苷H (FSH)和连翘酯苷I (FSI)成分对DPPH自由基、ABTS自由基、·O2-自由基均具有较好的清除能力。FSA、FSB、FSH和FSI可提高过氧化氢诱导的巨噬细胞RAW264.7中超氧化物歧化酶（SOD）、过氧化氢酶（CAT）活性，提高还原性谷胱甘肽（GSH）含量，降低丙二醛（MDA）含量，改善过氧化氢诱导的细胞氧化损伤。经热图分析及主成分分析，发现FSA、FSB、FSH、FSI 4种苯乙醇苷类成分与抗氧化能力呈正相关。研究表明，连翘叶中的FSA、FSB、FSH、FSI 4种苯乙醇苷类成分具有较好的抗氧化活性，是连翘叶发挥抗氧化活性的主要药效物质。     

连翘的作用机理及其在猪和鸡生产中的应用

现代化畜牧养殖面临全面禁抗的挑战,而植物提取物具有分布广、无残留和微量高效的特点,是极佳的抗生素替代品。连翘提取物具有抗氧化、抗炎、抗菌、抗过敏、抗应激和增强免疫力等功能,在猪和鸡生产中有广泛应用。连翘酯苷是连翘提取物的主要活性组分,但其作用机理有待进一步研究。本文集中探讨连翘酯苷的深层作用机理以及连翘在猪和鸡生产中的应用前景,为科学研究和畜牧生产提供可借鉴的思路。     

连翘酯苷对体外培养细胞的毒性研究

探讨了连翘酯苷对体外培养细胞的毒性,以期为人们更好地研究利用连翘酯苷提供实验依据。实验采用细胞病变法观察连翘酯苷对猪肾细胞（PK-15）、猴肾细胞（Mare-145）、鸡胚肾细胞（CEK）、鸡外周血淋巴细胞（PBL）等4种细胞的形态损伤;用MTT法检测连翘酯苷作用这4种细胞后的细胞活性和细胞数量的变化。根据这两种方法的结果计算出连翘酯苷对这4种细胞的半数致死量。实验结果显示高剂量的连翘酯苷可致细胞发生病变,而低剂量组的细胞形态优于对照组。经SPSS16．0统计,连翘酯苷对PK-15、Mare-145、CEK3种细胞的半数致死量分别为137．8、87．1、384．4μg／mL,对PBL应用到中华人民共和国兽药典（2000年版）规定药量的10倍剂量,结果未发现致死性。因此,适当合理的连翘酯苷用量对体外培养的细胞没有毒性,反而有一定的维持细胞形态的营养作用和刺激细胞增殖的作用。     

连翘酯苷A对感染H9N2-AIV小鼠的炎症基因水平表达的影响

本研究旨在探究连翘酯苷A对感染H9N2禽流感病毒后小鼠的炎症基因水平表达的影响,探讨连翘酯苷A抗病毒的免疫作用机制。对不同分组处理的小鼠于3、5、7、14d采血(n=3),检测白介素1β(IL-1β)含量;取第7d小鼠肺组织(n=3),通过荧光定量PCR检测髓样分化因子(My D88)与核因子-κB(NF-κB)变化,分析连翘酯苷A对其表达的影响。结果表明连翘酯苷A可减少IL-1β分泌;与模型组相比,连翘酯苷A治疗后My D88与NF-κB基因表达水平降低。研究提示,连翘酯苷A的免疫调节作用可能是通过调控炎症基因表达,降低炎症因子的分泌来实现的。     

连翘酯苷对LPS诱导的肉鸡法氏囊中NO及抗氧化酶活性的影响

本试验研究了连翘酯苷对内毒素(LPS)诱导的肉鸡法氏囊中一氧化氮(NO)、总抗氧化能力(T-AOC)、总超氧化物歧化酶(T-SOD)、还原型谷胱甘肽(GSH)和丙二醛(MDA)含量的影响.结果表明:连翘酯苷组中T-AOC、T-SOD和GSH活性明显升高,与正常组比较差异显著(P＜0.05)；LPS组中NO和MDA含量明显升高,T-AOC、T-SOD和GSH活性明显降低,与正常组比较差异显著(P＜0.05)；连翘酯苷治疗组中NO和MDA含量明显降低,T-AOC、T-SOD和GSH活性明显升高,与LPS组比较差异显著(P＜0.05).研究结果表明:连翘酯苷可提高肉仔鸡抗氧化功能,并且可以抑制由LPS引起的氧化反应.     

连翘酯苷A抗大鼠类风湿性关节炎机制研究

[目的]探讨连翘酯苷A对类风湿性关节炎大鼠的抗炎作用及作用原理。[方法]将30只SD大鼠[体重(120±2)g],随机分成3组,每组10只,分别为对照组(A组)、类风湿性关节炎组(B组)和连翘酯苷A治疗组(C组)。首先构建大鼠类风湿性关节炎模型,再观察各组大鼠临床症状、血清中TNF-α蛋白表达量、抗氧化酶和自由基含量。[结果]类风湿性关节炎模型组大鼠血清中TNF-α蛋白表达量增加,SOD含量下降,NO含量上升;而连翘酯苷A治疗组上述指标的趋势正好与之相反。[结论]连翘酯苷A可通过抑制炎症因子TNF-α的含量,并干扰TNF-α蛋白的翻译,影响抗氧化酶及自由基含量,最终发挥抗炎功效。     

连翘酯苷A对内毒素致鸡脾淋巴细胞白介素-1β的影响

试验旨在研究内毒素和连翘酯苷A对鸡脾淋巴细胞中白介素-1β(IL-1β)水平的影响,将1日龄雏鸡常规饲养至50日龄时,心脏采血处死后,无菌剖检取脾,并用鸡脾淋巴细胞分离液将鸡脾淋巴细胞分为20个组,具体为5个时间点×4个剂量组=20个组。作用时间分别为0、6、12、24和48 h,作用剂量组分别为对照组、内毒素(LPS)组(5μg/m L)、连翘酯苷A预防低剂量组(5μg/m L LPS+200μg/m L连翘酯苷A)和连翘酯苷A预防高剂量组(5μg/m L LPS+400μg/m L连翘酯苷A)。按上述方法培养后,收集鸡脾淋巴细胞,采用酶联免疫吸附试验(ELISA)和实时荧光定量PCR(qRT-PCR)方法检测鸡脾淋巴细胞中IL-1β水平。ELISA结果显示:与对照组相比,LPS组鸡脾淋巴细胞中IL-1β蛋白含量升高;与LPS组相比,连翘酯苷A预防组鸡脾淋巴细胞中IL-1β蛋白含量下降,并与连翘酯苷A添加剂量呈正相关。qRT-PCR结果显示:与对照组相比,LPS组鸡脾淋巴细胞中IL-1βmRNA表达量升高;与LPS组相比,连翘酯苷A预防组鸡脾淋巴细胞中IL-1βmRNA表达量下降,并呈剂量时间效应。试验表明LPS可以诱导鸡脾淋巴细胞中IL-1β蛋白含量和mRNA表达量升高,而连翘酯苷A预防组鸡脾淋巴细胞中IL-1β蛋白含量和mRNA表达量下降,表明连翘酯苷A可以通过转录和翻译途径抑制LPS诱导的鸡脾淋巴细胞中IL-1β蛋白含量和mRNA表达量的升高,减轻炎症反应,发挥抗炎功能。     

两种提取方法对连翘中连翘苷含量的影响

连翘[Forsythia suspen（Thunb．）Vahl]为木犀科连翘属植物连翘的干燥果实，为常用的清热解毒中药，气微香味苦。具有清热解毒、消肿散结的功效。其主要成分为连翘苷、连翘苷元、连翘酯苷、连翘酚、芦丁等。现代药理研究表明。连翘有抗菌、抗炎、解热、抗肝损伤、镇吐、利尿、解压等作用。《中国药典》以连翘苷作为指标成分控制连翘的质量。     

TLC法检测银翘天甘复方制剂中的连翘苷

银翘天甘复方制剂是由金银花、连翘、天花粉和甘草四味中药组成,具有良好的抗菌、抗病毒、抗炎解热等功效.其中,连翘的主要成分为连翘苷、连翘酯苷、连翘酯素.目前,测定中药复方制剂中连翘苷的含量多采用高效液相色谱法(HPLc).本试验旨在应用薄层色谱(TLC)法对银翘天甘复方制剂中的连翘苷进行测定.     

连翘酯苷在体外与体内的抑菌效果研究

本文提取制备了连翘酯苷,并对其进行了体内和体外的抑菌试验。试验结果表明,连翘酯苷在体外和体内对引发奶牛乳房炎的主要致病菌金黄色葡萄球菌、停乳链球菌、无乳链球菌均有较好的抑制作用。     

牡丹籽油的化学成分及药理作用研究进展

牡丹籽油是以牡丹籽为原料,经过不同提取工艺制成金黄色的油。目前研究发现,牡丹籽油主要成分为脂肪酸、不皂化物以及微量元素。此外,牡丹籽油还具有抗氧化、保肝、降血脂、降血糖等多种功效。通过系统查阅牡丹籽油的相关文献,对牡丹籽油的化学成分及药理作用的研究进展进行了系统阐述,以期为牡丹籽油的进一步研究提供理论参考依据。     

动物源多糖的药理活性研究进展

随着动物源多糖所具有的多种生物活性逐渐被研究证实,人们对动物源多糖关注度日渐提高。大多数的动物类药材既具有重要的药理作用,又具有丰富的营养价值。动物源多糖具有提高机体免疫力、抗氧化、抗疲劳、降血脂、抗肿瘤和保肝等药理作用。文中就动物源多糖的药理作用研究进行综述,以期为动物源多糖的医药和保健作用开发提供科学参考。     

Influence of Different Protocols of Urethral Catheterization after Pharmacological Induction (Ur.Ca.P.I.) on Semen Quality in the Domestic Cat

The aim of this study was to evaluate the influence that different protocols of urethral catheterization after pharmacological induction (Ur.Ca.P.I.) may have on the semen quality of the domestic cat. The study has been divided into two experiments: one in which different dosages of medetomidine administrated are evaluated and the second one in which the timing of the catheterization after pharmacological induction is tested. In the first experiment, 18 cats were sedated with the recommended dosage of medetomidine (130 μg/kg i.m.) while the other 18 were sedated with a lower dose of the same drug (50 μg/kg i.m.). In the second experiment, three groups were implemented, each containing 25 subjects. In group 1, the semen collection was performed immediately once the pharmacological effect of the drug was reached; in group 2, the semen collection was performed three times every 5 min after the pharmacological effect was reached; finally, in group 3, Ur.Ca.P.I. was performed 20 min after the pharmacological effect was reached. All the different protocols permitted sperm collection, nevertheless the first experiment showed a better quality in terms of volume, concentration, total number of spermatozoa (p < 0.01) and quality of the movement (motility p < 0.05 and forward progressive motility p < 0.01), using a high medetomidine dosage rather than 50 μg/kg i.m. In the second experiment, forward motility was statistically higher (p < 0.01) in the first group and total volume was higher (p < 0.01) in the second and third group, while other parameters were statistically not different. Results suggest that a single catheterization immediately after the onset of the pharmacological effect leads to a good‐quality semen with the lowest possibility of damaging the urethra and that a sedation with 130 μg/kg of medetomidine leads to a better quality sperm collection than 50 μg/kg does.     

Insulin glargine has a long duration of effect following administration either once daily or twice daily in divided doses in healthy cats

The pharmacological effects of glargine administered once or twice daily were compared in six healthy cats. A two-way crossover study was performed with insulin and glucose concentrations measured following subcutaneous administration of glargine once daily (0.5U/kg) or twice daily (0.25U/kg, repeated after 12h). Nadir glucose concentration and mean daily glucose concentration did not differ significantly following insulin administration once daily or twice daily in divided doses. Time to reach last glucose nadir differed, with longer intervals occurring following twice daily dosing. Blood glucose failed to return to baseline concentration by 24h in three of six cats in each treatment group. Insulin variables were not significantly different following once or twice daily dosing. This study in healthy cats demonstrates that glargine has a long duration of action with carry-over effects to the next day likely, regardless of dosing regimen. A study in diabetic cats is required to determine the best dosing regimen.     

中草药牛蒡子化学成分及药理研究进展

牛蒡子是一种常用中药,性寒,味辛、苦,归胃、肺经,具有疏散风热、宣肺透疹的功效,临床上用于治疗外感风热、咳嗽气喘、咽喉肿痛等症。综述了牛蒡子的主要化学成分木脂素类、挥发油类、脂肪油类及帖类及其抑菌、抗病毒、抗肿瘤、治疗肾病、降血糖等众多药理作用现状,旨在为牛蒡子的化学成分及其药理作用的研究与开发提供参考,指导传统中草药牛蒡子在畜牧业养殖生产中的临床应用。     

Chirality: a major issue in veterinary pharmacology

The sole purpose of this comment is to draw attention to the significance of enantiomorphism in the interpretation of pharmacokinetic/pharmacodynamic studies of drugs that are present in dosage forms as racemates. The proportion of the enantiomers formed from a racemate can vary in different animal species, and both the pharmacokinetic behaviour and pharmacodynamic activity can differ between the enantiomers. As a consequence, the pharmacological effects produced by a racemic drug represent the combined effects of the enantiomers formed in the particular species of animal. Enantiomorphism has a major influence on the prediction of dosage regimens for different animal species.     

Cloning and pharmacological characterization of the equine adenosine A2A receptor: a potential therapeutic target for the treatment of equine endotoxemia

The aim of the current study was to clone the equine adenosine A(2A) receptor gene and to establish a heterologous expression system to ascertain its pharmacologic profile via radioligand binding and functional assays. An eA(2A)-R expression construct was generated by ligation of the eA(2A) cDNA into the pcDNA3.1 expression vector, and stably transfected into human embryonic kidney cells (HEK). Binding assays identified those clones expressing the eA(2A)-R, and equilibrium saturation isotherm experiments were utilized to determine dissociation constants (K(D)), and receptor densities (B(max)) of selected clones. Equilibrium competition binding revealed a rank order of agonist potency of ATL > CV-1808 > NECA > 2-CADO > CGS21680, and a rank order of antagonist potency as ZM241385 > 8-phenyltheophylline > p-sulfophenyltheophylline > caffeine. Furthermore, adenylate cyclase assays using selective A(2A)-R agonists revealed that the eA(2A)-R functionally coupled to Galpha(s) as indicated by an increase in intracellular [(3)H]cAMP upon receptor activation. Finally, NF-kappaB reporter gene assays revealed a CGS21680 concentration-dependent inhibition of NF-kappaB activity. These results indicate that the heterologously expressed eA(2A)-R has a pharmacological profile similar to that of other mammalian A(2A) receptors and thus can be utilized for further characterization of the eA(2A)-R to ascertain whether it can serve as a suitable pharmacological target for equine inflammatory disease.     

桑椹的药用价值与开发利用

桑椹化学成分复杂，营养丰富。桑椹可以入药，其药理作用广泛。本文概括了桑椹的营养成分、药理作用及药用等开发利用。