维拉帕米对心肌细胞的毒性作用

维拉帕米（ｖｅｒａｐａｍｉｌ，Ｖｅｒ）可减轻缺血心肌再灌注损伤［１］,也具有直接细胞毒性及增强抗癌药物的作用［２，３］。本实验观察不同浓度维拉帕米对培养心肌细胞的影响。１材料与方法１．１材料Ｗｉｓｔａｒ乳大鼠由第四军医大学动物实验中心提供;小牛血清由第四军医大学附属唐都医院中心实验室提供,用Ｅａｇｌｅ(ＪＲＳＵＳＡ)干粉三蒸水配制培养基;胰蛋白酶１∶２５０（Ｄｉｆｃｏ，ＵＳＡ）;Ｖｅｒ注射剂（芬兰Ｏｒｉｏｎ制药厂生产）;噻唑兰(Ｓｉｇｍａ);ＬＤＨ试剂盒(Ｂｅｃｋｍａｎ，ＵＳＡ)；国产分析纯试剂配制ＰＢＳ液…     

ACTA PHARMACEUTICA SINICA,VOL.34,No.1～12SUBJECT INDEX

ＰｈａｒｍａｃｏｌｏｇｙＩｎｈｉｂｉｔｏｒｙＥｆｆｅｃｔｓｏｆＳｈｉｋｉｍｉｃＡｃｉｄｏｎＰｌａｔｅｌｅｔＡｇｇｒａｇａｔｉｏｎａｎｄＢｌｏｏｄＣｏａｇｕｌａｔｉｏｎＭＡＹ ,ＳＵＮＪＮ ,ＸＵＱＰ ,ＧＵＯＹＪ ( 3 )…………ＥｆｆｅｃｔｓｏｆＳｕｌｆｕｒＣｏｍｐｏｕｎｄｓｆｒｏｍＣａｕｃａｓ (ＡｌｌｉｕｍｖｉｃｔｏｒｉａｌｉｓＬ .)ｏｎｔｈｅＳｐｏｎｔａｎｅｏｕｓＢｅａｔｉｎｇｏｆＭｙｏｃａｒｄｉａｌＣｅｌｌＳｈｅｅｔｓｉｎＶｉｔｒｏＺＨＡＯＨＱ ,ＷＡＮＧＸＹ ,ＮＡＭＢＯＴ ( 6)………………………………     

全身广谱治疗仪对大鼠免疫器官cAMP和CA含量的影响

为探讨全身广谱治疗仪照射对大鼠免疫器官ｃＡＭＰ和ＣＡ的影响。采用全身广谱治疗仪照射７天后,用ＳＲＢＣＶ免疫Ｗｉｓｔａｒ大鼠。在免疫后４天和７天脾脏,胸腺和下丘脑ｃＡＭＰ含量均降低。而在免疫后４天脾脏去甲肾上腺素、肾上腺素均增高,提示：全身广谱治疗仪照射大鼠,使免疫器官儿茶酚胺释放增加,ｃＡＭＰ代谢降低,可能导致淋巴细胞增殖和免疫功能增强。     

品系和年龄对大鼠操作行为的影响

品系和年龄对大鼠操作行为的影响刘苹ＭｉｃｈａｅｌＢＯＲＮＨＡＵＳＥＮ１ＨｅｌｍｕｔＧＲＥＩＭ１（昆明医学院环境卫生学教研室，昆明６５００３１；１德国国家环境与健康研究中心毒理学研究所，慕尼黑Ｄ－８５７５８）在ＳＤ和Ｗｉｓｔａｒ两种近交系大鼠３个年龄段...     

牛磺酸锌抗实验性心律失常的初步研究

牛磺酸 (ｔａｕｒｉｎｅ,Ｔａｕ)和锌 (Ｚｎ)各具有不同程度抗心律失常作用[1,2 ] 。据此合成牛磺酸锌配位化合物 (ｔａｕｒｉｎｅ ｚｉｎｉｅｃｏｏｒｄｉｎａｔｉｏｎｃｏｍｐｏｕｎｄ ,ＴＺＣ) ,研究其对氯化钙所致心律失常的防治作用。1　材料与方法　　体重 (2 0 4± 11)ｇ健康Ｗｉｓｔａｒ大鼠 ,♀♂不拘。随机分为ＴＺＣ(11 8ｍｇ·ｋｇ-1)、Ｔａｕ(7 7ｍｇ·ｋｇ-1)、ＺｎＳＯ4 (10ｍｇ·ｋｇ-1)、Ｔａｕ(7 7ｍｇ·ｋｇ-1) ＺｎＳＯ4 (10ｍｇ·ｋｇ-1)、维拉帕米(Ｖｅｒ 1 5ｍｇ·ｋｇ-1)、生理盐水 (ＮＳ)等实验组。 2 0 %乌拉坦…     

本刊第8届(2002-2004年)编辑委员会(EDITORIAL BOARD)

顾问 (ＣＯＮＳＵＬＴＡＮＴ)　　丁光生 (ＤＩＮＧＧｕａｎｇ ｓｈｅｎｇ)　沈芸荪 (ＳＨＥＮＹｕｎ ｓｕｎ)　吴　珏 (ＷＵＪｕｅ)　　　曹善祥 (ＣＡＯＳｈａｎ ｘｉａｎｇ)主编 (ＥＤＩＴＯＲ -ＩＮ -ＣＨＩＥＦ)　　俞耀松 (ＹＵＹａｏ ｓｏｎｇ)副主编 (ＡＳＳＯＣＩＡＴＥＥＤＩＴＯＲＳ -ＩＮ -ＣＨＩＥＦ)　　徐根福 (ＸＵＧｅｎ ｆｕ)　邓伟吾 (ＤＥＮＧＷｅｉ ｗｕ)　　　李　端 (ＬＩＤｕａｎ)特邀编委 (ＩＮＶＩＴＥＤＭＥＭＢＥＲＳＯＦＴＨＥＥＤＩＴＯＲＩＡＬＢＯＡＲＤ)(按姓名拼音排序 )陈灏珠 (ＣＨＥＮＨａｏ ｚｈｕ)…     

山茱萸对致衰大鼠红细胞的抗氧化作用及钙与衰老的机制研究

本实验以Ｗｉｓｔａｒ大鼠颈背部注射Ｄ－半乳糖人为建立衰老模型,同时以山茱萸作为抗衰老药物观察自由基（ＦＲ）对机体组织的损伤作用,山茱萸的抗氧化能力,了解细胞内Ｃａ＾２＋在致衰前后的变化及在衰老中的作用。实验结果显示,模型组大鼠抗氧化能力下降,表现为ＲＢＣ内ＳＯＤ活力下降（Ｐ〉０．０５）。山茱萸给药组大鼠ＲＢＣ内ＳＯＤ活力、ＲＢＣ膜中ＭＤＡ含量及ＲＢＣ内Ｃａ＾２＋浓度无明显变化,实验结果证明,衰老大     

HBsAg检测中S/CO值的临床意义

乙型肝炎表面抗原 (ＨＢｓＡｇ），检测方法仍以酶联免疫法(ＥＬＩＳＡ法 )为多。在其检验报告单中有Ｓ/ＣＯ值一项 ,对于它的临床意义说法不一。本室用荧光定量ＰＣＲ技术 (ＦＱ -ＰＣＲ )检测ＨＢＶ ＤＮＡ含量作比较 ,说明Ｓ/ＣＯ值在临床实践中可以作为ＨＢｓＡｇ 含量的初步判断指标。１材料乙型肝炎检测试剂盒 (上海实业科华生物技术公司生产 ) ,ＨＢｓＡｇ定值血清 (２μｇ/ｍｌ和５μｇ/ｍｌ,卫生部临检中心提供 )酶标仪 (芬兰ＭｅｓｃａｎＭＫ２），乙型肝炎系统分析软件 (四川省泸洲医学院检验提供 ) ,ＨＢＶ ＤＮＡ试剂盒 (深…     

左氟沙星合成路线图解

左氟沙星合成路线图解苗华，郭惠元（中国医学科学院医药生物技术研究所，北京１０００５０）ＧＲＡＰＨＩＣＡＬＳＹＮＴＨＥＴＩＣＲＯＵＴＥＳＯＦＬＥＶＯＦＬＯＸＡＣＩＮ￥ＭＩＡＯＨｕａ；ＧＵＯＨｕｉ－Ｙｕａｎ（ＩｎｓｔｉｔｕｔｅｏｆＭｅｄｉｃｉｎａｌＢｉｏ...     

羟苯磺酸钙的合成

羟苯磺酸钙的合成姜凤超，周晓（同济医科大学药学院，武汉４３００３０）ＳＹＮＴＨＥＳＩＳＯＦＤＯＢＥＳＩＬＡＴＥＣＡＬＣＩＵＭ￥ＪＩＡＮＧＦｅｎｇ－Ｃｈａｏ；ＺＨＯＵＸｉａｏ（ＳｃｈｏｏｌｏｆＰｈａｒｍａｃｙ，ＴｏｎｇｊｉＭｅｄｉｃａｌＵｎｉｖｅｒｓｉ...     

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.     

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.     

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.