二对氯苯甲酰莲心碱对实验性心律失常的影响

目的　研究二对氯苯甲酰莲心碱抗心律失常的药理作用。方法　采用乌头碱、哇巴因、氯化钙 3种抗心律失常模型。结果　二对氯苯甲酰莲心碱 5mg·kg-1iv可明显提高乌头碱致大鼠、哇巴因致豚鼠发生室性早搏、室性心动过速、室颤及心脏停搏用量 ;延长氯化钙诱发大鼠心律失常的出现时间 ,减少早搏、室颤的发生率及死亡率。结论　二对氯苯甲酰莲心碱具有广泛的抗心律失常作用     

二苯甲酰莲心碱抗实验性心律失常的作用

目的：研究二苯甲酰莲心碱抗实验性心律失常的作用。方法：采用乌头碱、哇巴因、氯化钙3种抗心律失常模型。结果：二苯甲酰莲心碱5mg.kg^1可明显提高乌头碱所致大鼠，哇巴因致豚鼠发生室性早搏，室性心动过速，室颤及心脏停搏用量，延长氯化钙诱发大鼠出现心律失常的时间，缩短窦律恢复时间，提高窦律恢复律，延长死亡时间及降低死亡率，结论：二苯甲酰莲心碱具有广泛的抗心律失常作用。     

莲心碱冻干粉针抗室性心律失常的药效学及一般药理学研究

目的:研究莲心碱冻干粉针抗室性心律失常的药理作用及一般药理学.方法:采用哇巴因、氯化钙抗心律失常模型,分别考察不同剂量组的莲心碱冻干粉针的抗室性心律失常作用;并通过实验考察其对血压、心电、呼吸及神经系统的影响.结果:莲心碱冻干粉针按1,2,3 mg· kg -1 给药,均能显著提高哇巴因致豚鼠室性早搏(VE)、室性纤颤(VF)及心脏停搏(CA)时的用量,延长氯化钙(CaCl 2 )诱发大鼠心律失常出现的时间,缩短生存大鼠的窦性心律恢复时间,减少死亡率.3种剂量的莲心碱冻干粉针均能降低大鼠收缩压和舒张压,减慢心律,延长QRS、QT间期,且对呼吸频率和深度及小鼠自主活动次数无明显影响.结论:莲心碱冻干粉针具有抗室性心律失常作用,且能降低血压,对大鼠呼吸、小鼠自主活动次数无明显影响.     

葛根素磺酸钠与葛根素抗心律失常作用的比较

目的:探讨葛根素磺酸钠的抗心律失常作用。方法:用氯仿、乌头碱、哇巴因3种方法建立心律失常模型,比较葛根素磺酸钠与葛根素抗心律失常的作用。结果:葛根素磺酸钠和葛根素均能降低氯仿致KM小鼠心室纤颤的发生率,明显提高乌头碱致SD大鼠室性期前收缩、室性心动过速、室颤、心搏停止的阈剂量,明显提高哇巴因致EWG/B豚鼠室性期前收缩、室性心动过速、室颤、心搏停止的阈剂量,但葛根素磺酸钠的效果更好。结论:葛根素磺酸钠具有较好的抗心律失常的作用,为其临床治疗心律失常奠定基础。     

二乙酰基莲心碱抗实验性心律失常的作用

目的研究二乙酰基莲心碱抗心律失常的药理作用.方法采用乌头碱、哇巴因、氯化钙3种抗心律失常模型.结果二乙酰基莲心碱5mg     

阿魏酸钠抗心律失常机制的初步探讨

目的探讨阿魏酸钠是否具有抗心律失常作用及其可能的抗心律失常机制。方法应用哇巴因及乌头碱建立心律失常的动物模型 ,并观察阿魏酸钠对心律失常的影响。结果阿魏酸钠0 6g/kg静脉推注可对抗哇巴因诱发的室性心律失常 ,使室性早搏、室性心动过速、室颤的发生时间延长 ,并可提高哇巴因致室性早搏、室性心动过速、室颤的剂量 ,两组之间差异有显著意义 (P <0 0 1) ,但阿魏酸钠不能对抗乌头碱诱发的心律失常。结论阿魏酸钠具有对抗哇巴因诱发的心律失常作用 ,机制可能与其对钾离子通道的阻滞作用有关     

毛果芸香碱对实验性心律失常的保护作用

目的：观察毛果芸香碱对实验性心率失常的影响。方法：分别以乌头碱，氯化钡和哇巴因制备实验性动物心律失常模型，观察毛果芸香碱的干预作用。结果：毛果芸香碱可显著延迟乌头碱引起的大鼠室性心律失常的出现（P〈0．05），延长出现心律失常后的存活时间（P〈0．05）；能明显延迟氯化钡引起的大鼠双相室性心律失常的出现（P〈0．01），缩短心律失常的持续时间（P〈0．01）；能显著延长哇巴因引起豚鼠出现心律失常后的存活时间（P〈0．05）。毛果芸香碱的上述作用可被M3受体阻断荆4-DAMP完全逆转。结论：毛果芸香碱具有对抗乌头碱和氯化钡诱发大鼠，哇巴因诱发豚鼠心律失常的作用，提示其具有良好的抗心律失常作用；毛果芸香碱通过激动大鼠和豚鼠心肌M3受体而产生抗心律失常的作用。     

参松养心胶囊联合比索洛尔对心律失常保护作用的实验研究

目的研究参松养心胶囊(SSYX)辅助富马酸比索洛尔(BIS)对乌头碱及哇巴因诱发的实验性心律失常的保护作用。方法制备乌头碱及哇巴因诱导大鼠及豚鼠实验性心律失常模型,实验共分5组,即:对照组、SSYX(25、50、100 mg/kg)辅助BIS(0.5 mg/kg)组及单独应用BIS(0.5 mg/kg)组,预先灌胃给予相应药物3 d,末次给药后,分别给予乌头碱和哇巴因,观察大鼠出现室性早搏(VP)、室性心动过速(VT)、心室颤动(VF)及心脏停搏(CA)的诱发时间以及豚鼠出现上述症状时哇巴因的用量。结果与对照组比较,辅助应用SSYX 50、100 mg/kg组均能使给乌头碱后大鼠VP、VT、VF及CA的诱发时间明显延长(P<0.05或P<0.01),辅助应用SSYX 25 mg/kg仅可使给乌头碱后大鼠VT的诱发时间延长(P<0.05);与对照组比较,辅助应用SSYX 50、100 mg/kg组均能使给哇巴因后豚鼠出现VP、VT、VF及CA时哇巴因的用量明显提高(P<0.05或P<0.01),辅助应用SSYX 25 mg/kg仅可使给哇巴因后豚鼠出现VT、VF时哇巴因的用量提高(P<0.05)。结论 SSYX辅助BIS对乌头碱及哇巴因诱发的实验性心律失常均具有明显的保护作用,且作用优于单独使用BIS,提示SSYX与BIS联合应用具有协同作用。     

4-[对-(1-苯丙三氮唑)甲基]苯丙烯酸钠抗实验性心律失常的作用

目的　研究 4 [对 (1 苯丙三氮唑 )甲基 ]苯丙烯酸钠的抗实验性心律失常作用。方法　采用多种心律失常动物模型观察药物对实验性心律失常的作用。结果　 4 [对 (1 苯丙三氮唑 )甲基 ]苯丙烯酸钠 2 5 ,12 5mg·kg-1iv可明显提高乌头碱诱发大鼠、哇巴因诱发豚鼠室性早博、室性心动过速、室颤及心脏停搏的用量 ;延缓氯化钡诱发大鼠心律失常的出现时间 ,缩短持续时间 ,减少出现双相性心律失常出现的动物数。结论　 4 [对 (1 苯丙三氮唑 )甲基 ]苯丙烯酸钠具有明显的抗心律失常作用。     

莲心总碱抗心律失常的实验研究

目的探讨莲心总碱对实验性心律失常的影响。方法采用乌头碱、毒毛花苷G、氯化钙、氯仿等4种药物诱发的动物心律失常及电刺激诱发家兔心室颤动（室颤）模型，运用在体心电图记录方法，观察莲心总碱的抗实验性心律失常作用。结果莲心总碱对药物及电刺激诱发的动物心律失常有明显对抗作用，可提高药物引起动物出现室性期前收缩、室性动过速、室颤的剂量，降低室颤发生率及死亡率。结论莲心总碱有较好的抗多种实验性心律失常作用，可能与其阻滞Na＋、Ca2＋内流，阻断折返作用有关。     

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.     

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.