逍遥丸的三维高效液相色谱法鉴定和指标成分的定量

用三维高效液相色谱(three dimensional HPLC)法对中成药逍遥丸进行了分析。结果表明该法用于逍遥丸中单味中药鉴定及其指标成分(marker substances)含量测定均得到满意结果。     

逍遥丸微生物限度检查的方法学验证

目的 考察逍遥丸(小蜜丸)的微生物限度检查方法.方法 按《中国药典》[1]2010年版(二部)附录微生物限度检查法进行方法学验证试验.比较常规法、培养基稀释法(验证法)测定逍遥丸的抑菌率.结果 逍遥丸对金黄色葡萄球菌有一定的抑制作用,常规方法检测样品2010G0260、2010G0192、2010G0287对金黄色葡萄球菌的抑菌率分别为31％、15％、10％,验证方法的抑菌率分别为82％、79％、82％.结论 逍遥丸(小蜜丸)虽为中成药,但是其中药成分仍有抑菌作用,因此,在进行微生物限度检查时,需采用培养基稀释法对其抑菌作用进行去除,以进行细菌计数的检查.     

养血滋阴中药颗粒联合逍遥丸治疗功能性便秘疗效观察

目的 探讨养血滋阴中药颗粒联合逍遥丸治疗功能性便秘的疗效,以及对患者肠神经递质血清P物质(SP)、一氧化氮(NO)及胃肠激素水平的影响.方法 选取医院2018年5月至2020年5月收治的功能性便秘患者105例,按随机数字表法分为研究组(54例)和对照组(51例).两组患者均予逍遥丸治疗,研究组患者加用养血滋阴中药颗粒,...     

逍遥丸高效液相色谱数字化指纹图谱研究

目的建立逍遥丸(Xiaoyao Wan,XYW)HPLC数字化指纹图谱,为逍遥丸整体质量控制提供一个标准。方法采用RP-HPLC法,以色谱指纹图分离信息量指数RI为目标函数优化选择指纹图谱条件,以宏定性相似度Sm和宏定量相似度Pm评价逍遥丸质量。用"中药色谱指纹图谱超信息特征数字化评价系统3.0"软件挖掘体现逍遥丸质量的HPLC指纹图谱的潜信息特征数字化参数并进行评价。结果以芍药苷峰为参照物峰,确定56个共有指纹峰,建立了XYW-HPLC数字化指纹图谱。通过聚类分析确定用其中12批生成对照指纹图谱(RFP),以此RFP为标准用系统指纹定量法鉴别评价13批逍遥丸质量。鉴别出S3和S9的质量很好,S4、S6、S8、S10、S11和S12质量好,S1、S2、S5和S7质量良好,S13质量中。结论所建立的XYW-HPLC数字化指纹图谱可对逍遥丸进行整体定性分析和定量分析,可清晰反映XYW质量变异,是评价逍遥丸质量的有效方法。     

理气逍遥丸对功能性消化不良大鼠的治疗作用研究

目的 研究理气逍遥丸治疗功能性消化不良的治疗效果,为该制剂增加气滞型胃脘痛适应证奠定基础。方法 本研究针对气滞型胃脘痛功能主治开展了功能性消化不良(FD)的药效学研究,将64只健康成年wistar大鼠随机分为4组,每组16只,空白组、模型组均每日给予生理盐水,多潘立酮组每日灌胃给予2.8 mg/kg多潘立酮片,理气逍遥丸组灌胃给予理气逍遥丸1.25 g/kg。除空白组外诱导制备FD动物模型,造模后连续给予各组药物2周,通过分析大鼠一般状态,胃肠运动功能,调节激素分泌水平等指标,研究理气逍遥丸对FD的治疗作用。结果 理气逍遥丸组FD大鼠与模型组相比胃排空率均显著升高(P 0.01),大鼠胃促生长素(Ghrelin)、胃动素(MTL)水平显著升高(P 0.01),血管活性肠肽(VIP)水平显著降低(P 0.01)。理气逍遥丸组FD大鼠胃排空率、血清胃促生长素、MTL及VIP水平等指标与空白组相比均无统计学意义(P 0.05)。结论 理气逍遥丸能有效改善雌雄性FD大鼠胃肠动力,调节胃肠激素分泌。理气逍遥丸对FD大鼠有一定的治疗效果。理气逍遥丸治疗FD药效明确。可为该制剂增加气滞型胃脘痛适应证奠定基础。     

一测多评法同时测定逍遥丸中6种指标性成分的研究

摘 要 目的：建立一测多评(QAMS) 的方法用来测定逍遥丸中6种成分的含量。方法: 以甘草酸为参照物,采用HPLC法,以Kromasil C18色谱柱(250 mm×4.6 mm,5 μm) ;流动相为乙腈（A） 0.1%磷酸水溶液（B）为流动相,梯度洗脱：0～10 min,5% A;10～25 min,5 % A→15 % A;20～70 min,15 % A→60 % A; 流速:1.0 ml·min-1;检测波长: 280 nm;柱温：35℃;进样量：10 μl。应用QAMS法的方法测定6种指标性成分之间的相对校正因子,分别采用外标法和一测多评法测定逍遥丸中的6种指标性成分的含量,并对２种方法计算结果进行对比分析,以验证一测多评法的实用性与稳定性。结果:建立QAMS法用于测定逍遥丸中6种指标性成分的含量,并对6批逍遥丸进行测定,其计算值与测定值的差异无统计学意义(P＞0.05) 。结论:QAMS 法用于测逍遥丸中6种指标性成分的含量,方法简单、有效、结果准确,可用于逍遥丸的质量控制,并为后续的一测多评的研究提供参考价值。     

逍遥丸对抑郁模型大鼠海马突触素mRNA表达的影响

目的研究逍遥丸(舒肝解郁中药方剂)抗抑郁作用的分子机制。方法以原位杂交和RT-PCR方法,研究慢性应激抑郁模型大鼠的海马突触素mRNA表达以及逍遥丸对其影响。结果模型组大鼠海马突触素mRNA表达量明显上升,与正常对照组比较差异有统计学意义(P<0.05);氟西汀组、逍遥丸组大鼠海马突触素mRNA表达量显著下降,与模型组比较差异有统计学意义(P<0.05)。结论模型大鼠海马神经元内突触素表达上调,逍遥丸能下调其表达。     

加味逍遥丸对CYP2C19酶活性的影响

目的:探讨加味逍遥丸对CYP2C19活性的影响,为临床指导联合用药提供依据。方法:将20名受试者按照CYP2C19*2基因型进行分类,野生型纯合子(WW)及突变型纯合子(MM)各10名。以奥美拉唑作为CYP2C19的探针药,研究服用加味逍遥丸对人体内代谢酶CYP2C19活性的影响。采用pyrosequencing测序法对CYP2C19进行基因分型,采用HPLC-MS/MS法测定探针药及其代谢产物的血药浓度。结果:连续服用14 d加味逍遥丸。以AUC0-12为指标,评价CYP2C19代谢酶的活性。受试者用药前CYP2C19代谢酶活性为5.7±1.6,服用加味逍遥丸后CYP2C19代谢酶活性为6.0±1.7。用药后代谢酶的活性升高,用药前后比较采用配对t检验,差异没有统计学意义。结论:服用加味逍遥丸对CYP2C19代谢酶活性没有明显影响。     

逍遥丸微生物限度检查方法学验证

目的建立逍遥丸的微生物限度检查方法。方法按《中国药典》2010版一部方法进行试验。结果逍遥丸对金黄色葡萄球菌有一定的抑制作用,可以通过培养基稀释法予以消除。结论可按平皿法（霉菌及酵母菌）和培养基稀释法（细菌）对逍遥丸的微生物限度进行检查。     

药浴疗法对慢性疲劳综合征的干预研究

目的 观察中医疏肝健脾药浴疗法对肝郁脾虚型慢性疲劳综合征(CFS)的干预效果.方法 228例肝郁脾虚型慢性疲劳综合征患者依据随机表,受试者按2:1:1比例分为3组,研究中缺失16例,最终212例患者符合要求,药浴组(106例)、逍遥丸组(56例)、对照组(50例).药浴组采用疏肝健脾中药配方进行药浴干预,4周为1个疗程;对照组给予安慰剂(食品色素柠檬黄)对照,隔日1次,4周为1个疗程;逍遥丸组口服逍遥丸8粒/次,2次/d.采用中医证候量表、匹兹堡睡眠质量指数、简易症状量表等作为观察指标,综合评价药浴疗法对CFS的干预效果.实验数据以(x)±s表示,组间比较用方差分析,方差不齐时采用K-W 和LSD秩和检验.均数比较用t检验.结果 干预后药浴组患者中医症候主要阳性症状评分明显优于干预前.3组中医证候疗效为药浴组显效6例(5.7％)、有效65例(61.3％)、无效35例(33.0％);对照组分别为0(0)、7例(14.0％)、43例(86.0％);逍遥丸组分别为8例(14.3％)、35例(62.5％)、13例(23.2％).药浴组和逍遥丸组有效率明显高于对照组有效率,差异有统计学意义(x2=38.39、42.54,均P＜0.01),药浴组与逍遥丸组差异无统计学意义.采用减分率的计算方法对简易症状量表干预后疗效进行评定,药浴组显效6例(5.7％)、有效83例(78.3％)、无效17例(16.0％);对照组分别为0(0)、4例(8.0％)、46例(92.0％);逍遥丸组分别为2例(3.6％)、44例(78.6％)、10例(17.8％).药浴组和逍遥丸组总有效率明显高于对照组,差异有统计学意义(x2=43.10、45.98,均P＜0.01),药浴组与逍遥丸组差异无统计学意义.结论 疏肝健脾中医药浴对缓解CFS有良好效果,可作为CFS的有效治疗方法之一.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.