不同品种水蛭抗凝抗血栓作用的比较

目的:比较研究宽体金线蛭和菲牛蛭的体内外的抗凝、抗血栓作用。方法:采用凝血酶直接滴定法测定不同处理方法的2种水蛭体外抗凝血活性;采用胶原蛋白-肾上腺素诱导小鼠脑血栓,角叉菜胶诱导小鼠尾静脉血栓以及大鼠动-静脉旁路血栓形成的方法,观察不同处理方法的两种水蛭的抗血栓作用。采用毛细管法和剪尾法,观察不同处理方法的两种水蛭的抗凝血作用。结果:菲牛蛭鲜体和干品的体外抗凝活性远优于鲜体及干燥宽体金线蛭;鲜品菲牛蛭、干燥菲牛蛭以及经不同方法处理的宽体金线蛭均具有明显的体内抗凝抗血栓活性,其中以菲牛蛭鲜品的作用最强烈;煎煮后的菲牛蛭几乎无体内外生物活性。结论:菲牛蛭与宽体金线蛭的活性成分有很大区别,且菲牛蛭比目前广泛应用的宽体金线蛭具有更优的药效活性。     

宽体金线蛭与菲牛蛭抗凝血酶活性及抗凝机制比较研究

摘 要 目的：比较宽体金线蛭和菲牛蛭抗凝血酶活性及对凝血途径的影响,为进一步揭示水蛭抗凝作用机制提供参考。方法: 采用凝血酶滴定法、发色底物法 萃取 HPLC联合法测定水蛭对凝血酶的作用;同时采用凝固法测定其活化部分凝血活酶时间（APTT）、凝血酶原时间（PT）和凝血酶时间（TT）,比较宽体金线蛭与菲牛蛭对不同凝血途径的影响。结果: 凝血酶滴定法的结果表明,不同水蛭的抗凝活性顺序依次为：菲牛蛭活体冻干品>菲牛蛭清水吊干品>>宽体金线蛭清水吊干品;发色底物法 萃取 HPLC法测定不同水蛭对凝血酶抑制作用的结果表明：不同水蛭水提取物对凝血酶的作用均表现出低浓度促进,高浓度抑制,且菲牛蛭具有强烈凝血酶抑制活性,而宽体金线蛭在加入更高剂量时才表现出抑制作用,且抑制作用较弱,菲牛蛭的抗凝血酶活性远远高于宽体金线蛭;不同水蛭样品均使APTT、PT、TT延长,但是菲牛蛭活体冻干品主要延长TT,清水吊干品主要延长APTT,而宽体金线蛭使APTT、TT延长更加显著。结论:宽体金线蛭和菲牛蛭对凝血酶及凝血途径的作用很大区别。     

中药水蛭原动物的本草学考证

本文就中药材水蛭的原动物来源分别从原动物、加工炮制及主治功能进行本草学考证。认为药用水蛭的原动物成该为医蛭科日本医蛭Hirudo nipponica Whitman及丽医蛭H.pulchra Song。与中国药典(一九八五年版一部)水蛭项下规定的原动物来源不完全一致;并就目前中药水蛭中最常见的宽体金线蛭Whitmania pigra(Whitman)的正确鉴定作了探讨。     

水蛭冻干粉的急性毒性及对急性血淤证大鼠的治疗作用

目的 评价水蛭冻干粉的急性毒性,比较水蛭冻干粉及水蛭饮片对急性血淤证大鼠的作用.方法 采用最大给药量实验评价水蛭冻干粉的急性毒性;将SD大鼠随机分为空白组、模型组、阿司匹林组(31.25 mg·kg-1)、宽体金线蛭冻干粉和日本医蛭冻干粉高、中、低剂量组(0.3125、0.2083、0.1042 g·kg-1)、宽体金...     

水蛭治疗脑梗塞相关研究近况

水蛭俗称蚂蝗，属于环节动物水蛭科，药用以日本水蛭(Hirudonipponica unit man)、宽体金线蛭(Whitmania pigra Whitman)、尖细金线蛭(Tarantula)的全体。世界各地均有分布，生长于我国大部分地区，栖息于沟渠、水田、湖沼中。     

凝血酶滴定法测定宽体金线蛭抗凝血活性的影响因素

对测定宽体金线蛭抗凝血活性的凝血酶滴定方法的影响因素进行分析。方法：用白瓷点滴板代替试管进行滴定反应（简称白瓷板法）,考察白瓷板法和常规的试管法、不同凝血酶滴定间隔时间和凝血酶浓度对抗凝血活性测定的影响。结果：在同样条件下,白瓷板法测定抗凝血活性的精确度和稳定性较试管法高。用白瓷板法测定,宽体金线蛭样品浓度在一定范围内（0．125～0．333g·ml^-1）、凝血酶浓度为20u·ml^-1或10U·ml^-1时,每隔1min滴加1次,每次5μ1,样品浓度与消耗的凝血酶体积呈线性相关,r值分别为0．961和0．992;所测得样品的抗凝血活性分别为（33．08±2．64）和（31．24±1．32）U·g^-1．RSD分别为8．0％和4．2％;对于0．333g·ml^-1的样品,其测量产生的理论误差不大于10％和5％。结论：白瓷板法可用于测定宽体金线蛭样品的抗凝血活性,用10U·ml^-1的凝血酶溶液,每分钟滴加一次,每次5山进行测定,其线性和精确度均较好。     

宽体金线蛭提取工艺研究

目的:筛选宽体金线蛭的最佳提取工艺。方法:以水蛭提取液中蛋白质含量及活化部分凝血活酶时间为指标,考察宽体金线蛭在不同溶媒、温度、提取时间、溶媒倍量及提取次数条件下的提取效果。结果:以10倍药材量的4 %NaCl溶液为提取溶媒,在60℃条件下分3次提取药材6h(3h +2h +1h) ,所得结果较为满意。结论:该提取工艺方法简单、科学,有推广应用价值。     

基于斑马鱼模型比较宽体金线蛭和菲牛蛭对血管新生的影响

摘 要 目的：探讨及比较宽体金线蛭和菲牛蛭对Tg（kdrl:mCherry）斑马鱼的血管新生影响。方法: 将受精后 6 ~ 8 h（6 ~ 8hpf）的胚胎暴露在含不同浓度宽体金线蛭和菲牛蛭水提取物的胚胎培养液中,每24 h更换一次含药培养液。72 hpf时,在显微镜下观察发育形态和节间血管,测定48,72 hpf孵化率,72 hpf节间血管数目、心率。结果: 在抑制血管新生方面,宽体金线蛭组浓度≥30 μg· ml^-1时,菲牛蛭组浓度≥20 μg· ml^-1时,斑马鱼节间血管数目均较空白组明显减少（P<0.01）。毒性方面,在48 hpf,给药组浓度≥40 μg· ml^-1时,宽体金线蛭和菲牛蛭组斑马鱼的孵化率均较空白组明显降低（P<0.01）;在72 hpf,宽体金线蛭组斑马鱼的孵化率在100 μg·ml^-1时较空白组明显降低（P<0.01）,而菲牛蛭组斑马鱼的孵化率在80 μg· ml^-1就明显降低（P<0.01）。宽体金线蛭和菲牛蛭组斑马鱼的卵黄囊、心囊无明显水肿,脊柱未弯曲;两组心率显著降低（P<0.01）,但在正常心率范围内。结论: 宽体金线蛭和菲牛蛭都具有抗血管生成活性,且菲牛蛭的抗血管生成活性强于宽体金线蛭。两者对斑马鱼发育有一定程度的影响,但毒性不大。     

宽体金线蛭抗凝血活性物质的提取方法

目的:比较不同提取方法对宽体金线蛭提取物抗凝活性的影响,确定抗凝活性物质的较佳提取方法。方法:应用凝血酶滴定法、APTT试剂盒法、PT试剂盒法等3种检测方法比较干品冷提、干品热提、干品脱脂后热提及鲜品冷提等提取物中抗凝活性的差异。结果:与空白对照组比较,各种提取方法所得提取物均具有明显的抗凝活性,各种检测方法所得结果一致。其中,水蛭鲜品和干品脱脂后提取物中抗凝活性较强。结论:水蛭提取物的抗凝活性强弱与原料的处理和提取方法有关。水蛭干品脱脂有利于提高提取物的抗凝活性。凝血酶滴定法可作为提取物抗凝活性的初步检测方法,其结果稳定,易于操作。APTT、PT试剂盒法可作为抗凝活性进一步检测的方法。     

应用聚合酶链式反应技术快速鉴别中药水蛭

目的 建立聚合酶链式反应法(polymerase chain reaction,PCR)对中药水蛭进行快速种间鉴别。方法 根据中国药典项下3种水蛭(宽体金线蛭、日本医蛭及尖细金线蛭)CO1序列的差异设计并合成3对种属特异性引物,对其进行PCR反应条件优化;对不同批次的水蛭进行稳定性试验,并对同批次的水蛭进行灵敏度试验;利用优化的PCR条件对水蛭混合样品进行分析。结果 3对引物分别能在60,61,59℃的退火温度下扩增出1 000~2 000,1 000~2 000,3 000 bp左右的明亮条带,检测限分别为0.1,1,10 ng,并能够准确鉴别以不同比例混合的水蛭样品。结论 所设计的3对引物可以快速鉴别中药水蛭、常见伪品及混掺水蛭,并具有较高的种间特异性及良好的种内稳定性和灵敏度,可作为中药水蛭传统基原鉴别方法的补充,为其质量控制提供更多参考。     

水蛭活性溶液脱腥脱色工艺研究

目的：采用不同方法对3种水蛭活性溶液进行脱腥脱色处理,评选出最优工艺方法。方法：采用羟丙基-β-环糊精、β-环糊精、粉末（颗粒）活性炭、高岭土、酵母粉为脱腥脱色材料研究了3种水蛭活性溶液的脱腥脱色工艺方法,并以感官评分、有效肽含量、物质活力单位为指标,得出最优脱腥脱色方法。结果：粉末活性炭-高岭土方法、酵母粉发酵方法的脱腥脱色效果良好,有效肽含量可以达到80%左右,活力基本不变,达到了脱腥脱色的目的。结论：粉末活性炭-高岭土方法、酵母粉发酵方法的脱腥脱色效果良好,为水蛭的后期开发利用奠定基础。     

Immunomodulatory and therapeutic properties of the Nigella sativa L. seed

A larger number of medicinal plants and their purified constituents have been shown beneficial therapeutic potentials. Seeds of Nigella sativa, a dicotyledon of the Ranunculaceae family, have been employed for thousands of years as a spice and food preservative. The oil and seed constituents, in particular thymoquinine (TQ), have shown potential medicinal properties in traditional medicine. In view of the recent literature, this article lists and discusses different immunomodulatory and immunotherapeutic potentials for the crude oil of N. sativa seeds and its active ingredients. The published findings provide clear evidence that both the oil and its active ingredients, in particular TQ, possess reproducible anti-oxidant effects through enhancing the oxidant scavenger system, which as a consequence lead to antitoxic effects induced by several insults. The oil and TQ have shown also potent anti-inflammatory effects on several inflammation-based models including experimental encephalomyelitis, colitis, peritonitis, oedama, and arthritis through suppression of the inflammatory mediators prostaglandins and leukotriens. The oil and certain active ingredients showed beneficial immunomodulatory properties, augmenting the T cell- and natural killer cell-mediated immune responses. Most importantly, both the oil and its active ingredients expressed anti-microbial and anti-tumor properties toward different microbes and cancers. Coupling these beneficial effects with its use in folk medicine, N. sativa seed is a promising source for active ingredients that would be with potential therapeutic modalities in different clinical settings. The efficacy of the active ingredients, however, should be measured by the nature of the disease. Given their potent immunomodulatory effects, further studies are urgently required to explore bystander effects of TQ on the professional antigen presenting cells, including macrophages and dendritic cells, as well as its modulatory effects upon Th1- and Th2-mediated inflammatory immune diseases. Ultimately, results emerging from such studies will substantially improve the immunotherapeutic application of TQ in clinical settings.     

北沙参活性成分与药材质量的动态监测

目的研究不同年份山东道地药材北沙参活性成分与质量的动态变化情况,监测北沙参药材的稳定性。方法追踪研究不同年份山东道地药材北沙参活性成分欧前胡素、异欧前胡素及多糖的动态含量变化,同时测定水分、总灰分、酸不溶性灰分、浸出物的含量,综合评价北沙参药材质量的稳定性。结果不同批次北沙参样品中欧前胡素、异欧前胡素、多糖、浸出物、灰分及水分的含量均呈现出良好的稳定性。结论山东道地药材北沙参内在质量具有良好的稳定性。     

Herb-drug interactions with Danshen (Salvia miltiorrhiza): a review on the role of cytochrome P450 enzymes

Danshen, the dried root and rhizome of Salvia miltiorrhiza Bunge, is a widely used medicinal plant for the treatment of cardiovascular diseases in China and a complementary medicine in the West. Danshen is indexed in the 2010 Chinese Pharmacopoeia, with more than 35 formulations and concoctions containing Danshen water-extracts, ethanolic extracts or their combination, which are rich in phenolic acids and different levels of tanshinones. There are rare reports on the adverse effects of Danshen preparations. It is, however, well-known that Danshen leads the anticoagulation failure of warfarin. The Danshen-warfarin interaction may be mediated via both pharmacodynamic and pharmacokinetic mechanisms. This review does not summarize recent progress, but the effects of Danshen and its active ingredients on the interactions of cytochrome P450 (CYP450) and drug transporters, as well as the analysis of ingredients, and the metabolism and pharmacokinetics that are related to these interactions. Tanshinones play significant roles in the inhibition and induction of several CYP450 isozymes. It can be concluded that precautions should be taken when using Danshen preparations rich in tanshinones for CYP-related herb-drug interactions.     

酒火炙水蛭的生物活性考察

目的:评价酒火炙水蛭的生物活性及安全性。方法:采用SNK法统计生水蛭、酒炙水蛭、酒火炙水蛭3组的抗凝血酶活性,并进行小鼠最大给药量实验:给予小鼠156mg酒火炙水蛭1d的最大给药量(相当于《中国药典》规定成人每日最大服用量的130倍)。结果:传统酒炙水蛭组与生水蛭组、酒火炙水蛭组比较,均有显著性差异P<0.05;酒火炙水蛭组与生水蛭组比较无显著性差异(P>0.05)。安全性实验小鼠未见异常,无死亡。结论:酒火炙水蛭具有较好抗凝活性,且用药安全。     

Network pharmacology and metabolomics-based detection of the potential pharmacological effects of the active components in Chrysanthemum morifolium 'Chuju'

Chrysanthemum morifolium 'Chuju' is a famous medicinal species in traditional Chinese medicine. 'Chuju' contains various active ingredients that can be used to treat multiple diseases without toxic side effects. In the present study, we combined metabolomics and network pharmacology to further explore the active ingredients in 'Chuju', as well as the target and pharmacological mechanisms of the active ingredients. A visualized network analysis model based on chemistry, pharmacokinetics, and pharmacology was constructed to predict the potential pharmacological mechanism of 'Chuju'. A total of 424 metabolites of 'Chuju' were identified, of which 21 ingredients had positive pharmacological effects after ADME screening. The network pharmacology revealed that acacetin and beta-sitosterol in 'Chuju' could act on GSK3B, MAPK14, ADRA1R, and NOS2 to regulate diabetes mellitus, Alzheimer's disease, breast cancer, and inflammatory diseases. These results indicated the potential pharmacological effects of the active components in 'Chuju'.     

中药材质量的本质与评价方法探讨

目的：为传统中药材质量评价及标准制订提供概念上的依据。方法：从中医药学的发展过程及影响中药材药性和质量的诸多因素,对中药材的质量本质以及与天然药物的关系、“地道药材”产生的人文及生态原因作一些探讨。结果：中药材和民间药虽然都是天然药物,作为药物,其性质有时是完全不同的,中药材是在传统中医理论指导下使用的药物,其质量评价方法也应根据传统质量评价情况与天然药物或民间药物区别对待。结论：中药材具有明确的药性（药效谱）、较好的性状质量、较高的有效成分含量,以及稳定的各成分比例关系,“道地药材”就是其中的典型代表。天然药物和民间药是属于辨病用药的药物,而不是中医的辨证用药。本文根据中药材质量的内涵,提出指纹图谱结合成分权重的质量评价模式用于评价中药材的质量。     

关于中药饮片处方药味、剂量的调查分析

目的：调查比较古、现、今中药饮片处方的药味数、剂量数,了解它们的变化趋势,为指导临床用药提供依据。方法：采用随机抽样法抽取《伤寒论》和《金匮要略》中的500首方剂、《现代实用方剂》（1989年版）[1]中500首方剂及本院2008年前半年处方中的5 000张处方,将处方数据输入微机,进行统计分析。结果：处方药味数、剂量数均渐增加,然后根据药理学进行分析。结论：药味、剂量的变化应与现代药理研究相结合。     

水蛭活性肽的纯化工艺

目的：对水蛭活性肽进行纯化,并对水蛭活性肽进行树脂纯化条件考察。方法：采用DA201-C大孔吸附树脂进行极性分离,后经D201阴离子交换树脂进行电荷分离,最终得到纯化的水蛭活性肽组分。结果：DA201-C大孔树脂,上样肽浓度20 mg·mL^-1,流速1.0 BV·h^-1,依次用25%乙醇、50%乙醇和75%乙醇溶液洗脱,各洗脱部位得率及活力较高,但总体活性成分被分散,以上各洗脱部位经D201离子交换树脂,pH 4.0,上样肽浓度30 mg·mL^-1,流速3.0 BV·h^-1,分别用2.5%氯化钠的25%乙醇、2.5%氯化钠的50%乙醇、2.5%氯化钠的75%乙醇溶液洗脱,2.5%氯化钠的25%乙醇和2.5%氯化钠的50%乙醇洗脱部位有明显的抗凝活性,经过分析性RP-HPLC验证后,基线平稳,各组分分离度良好。结论：经DA201-C大孔树脂和D201离子交换树脂纯化后的水蛭活性肽,2.5%氯化钠的25%乙醇和2.5%氯化钠的50%乙醇洗脱部位活力较高,分离度好。     

Safety evaluation and biochemical efficacy of celery seed extract (Apium Graveolens) capsules in hypertensive patients: a randomized,triple-blind,placebo-controlled,cross-over,clinical trial

Inflammopharmacology - The present study was conducted to evaluate the safety of celery seed extract (Apium graveolens), as a medicinal herb with active ingredients such as 3-n-butylphthalide...