滁菊总黄酮对异丙肾上腺素致大鼠急性心肌缺血的影响

目的 观察滁菊总黄酮对异丙肾上腺素（ISO）致急性心肌缺血模型大鼠的保护作用。方法 将大鼠皮下注射ISO复制大急性心肌缺血模型,观察滁菊总黄酮对模型大鼠心电,血清肌酸激酶（CK）、乳酸脱氢酶（LDH）、心肌组织超氧物歧化酶（SOD）、过氧化氢酶（CAT）和丙二醛（MDA）含量的影响。结果 滁菊总黄酮能够抑制急性心肌缺血模型大鼠心电图J点抬高,降低血清CK、LDH活性,升高心肌组织SOD、CAT活性,降低MDA含量。结论 滁菊总黄酮对ISO致心肌缺血模型大鼠有保护作用。     

黑龙江地产山里红叶醇提液对异丙肾上腺素诱导大鼠急性心肌缺血关键酶的影响

摘 要 目的： 观察山里红叶醇提液对异丙肾上腺素诱导的大鼠急性心肌缺血的保护作用并初步探讨其作用机制。方法: 皮下多点注射异丙肾上腺素造成大鼠急性心肌缺血模型,测定血清中谷草转氨酶(AST)、血清肌酸激酶(CK)、乳酸脱氢酶(LDH)、羟丁酸脱氢酶(HBDH)、超氧化物歧化酶(SOD)的活性及血清丙二醛(MDA)水平。结果: 山里红叶醇提液能抑制异丙肾上腺素诱导的大鼠中血清中AST、CK、LDH、HBDH的活性及升高血清SOD活性,降低血清MDA含量。结论: 山里红叶醇提液对大鼠异丙肾上腺素引起心肌缺血的关键酶有一定的保护作用。     

吴茱萸次碱对实验动物急性心肌缺血损伤的保护作用

目的探讨吴茱萸次碱(Rut)对实验动物急性心肌缺血损伤的保护作用。方法采用垂体后叶素及异丙肾上腺素致小鼠急性心肌缺血模型,检测血清中乳酸脱氢酶(LDH)、肌酸激酶(CK)的活性。进一步采用大鼠冠状动脉结扎模型,检测血流动力学指标及血清LDH、CK、超氧化物歧化酶(SOD)的活性及丙二醛(MDA)的含量。结果与模型组相比,Rut组能降低垂体后叶素及异丙肾上腺素所致小鼠血清LDH及CK的升高(P<0.05)。在大鼠冠状动脉结扎实验中,与模型组相比,Rut组能改善结扎大鼠血流动力学指标的变化,血清中LDH、CK的酶活力及MDA的含量下降,SOD活力升高(P<0.05)。结论 Rut对实验动物急性心肌缺血有一定的保护作用。     

参附汤血中移行成分对心肌肥大大鼠血流动力学及能量代谢的影响

摘 要 目的：观察参附汤血中移行成分对异丙肾上腺素所致心肌肥大大鼠血流动力学及能量代谢的影响。方法: 大鼠以剂量递减（20,10,5 mg · kg^-1）的方式皮下注射异丙肾上腺素,连续3 d,再以3 mg · kg^-1剂量连续注射7 d,建立大鼠心肌肥大模型,观察参附汤和参附汤血中移行成分对大鼠血流动力学及能量代谢各项指标的影响;取心肌进行能量代谢相关酶的检测。结果: 与模型组比较,参附汤和参附汤血中移行成分可升高左心室收缩压（P<0.01）,左室内压变化速率（P<0.01）,降低左心室舒张末期压力（P<0.01）;提高心肌肥大大鼠心肌细胞内三磷酸腺苷（ATP）、二磷酸腺苷（ADP）含量（P<0.05）,降低一磷酸腺苷（AMP）含量（P<0.05）;降低丙二醛（MDA）含量（P<0.01）,升高超氧化物歧化酶（SOD）活性（P<0.01）。结论:参附汤及其血中移行成分对异丙肾上腺素所致心肌肥大大鼠具有一定的治疗作用并能调节心脏能量代谢。     

延胡索乙素对大鼠实验性心肌缺血的保护作用

目的 研究延胡乙素（dl-THP)对大鼠实验性心肌缺血的保护作用。方法 观察dl-THP对垂体后叶素（pit)所致大鼠心电图急性缺血性改变的预防作用以及对异丙肾上腺素（Iso)引起心肌损伤大鼠的保护作用。结果 dl-THP对垂体后叶素所致心电图改变有明显预防作用。能对抗Iso所致ECG的ST段升高。显著抑制心肌组织中磷酸肌激酶（CPK）、乳酸脱氢酶（LDH）的释放,降低血清CPK和LDH水平,保护心肌组织超氧化物歧化酶（SOD）活性,减少丙二醛（MDA）生成。结论 dl-THP对实验性心肌缺血有明显的保护作用。     

罗痛定对大鼠心肌缺血的保护作用

目的;研究罗痛定（1－THP）对大鼠心肌缺血的保护作用。方法：观察1－THP对垂体后叶素（Pit)所致大鼠心电图急性缺血性改变的预防作用以及对异丙肾上腺素（Iso)引起心肌损伤大鼠的保护作用,结果：1－THP对垂体后叶素所致心电图（ECG）改变有明显预防作用,能对抗Iso所致CG的ST段升高,显著抑制心肌组织中磷酸肌酸激酶（CK）,乳酸脱氢酶（LDH）的释放,降低血清CK和LDH水平,保护心肌组织超化物歧化酶（SOD）活性,减少丙二醛（MDA）生成。结论：1－THP对心肌缺血有明显的保护作用。     

藏药柳茶挥发油对小鼠急性心肌缺血损伤的干预作用

目的 研究藏药柳茶挥发油对垂体后叶素所致小鼠急性心肌缺血损伤的干预作用。方法 采用垂体后叶素腹腔注射建立小鼠急性心肌缺血损伤模型,给予柳茶挥发油治疗低、中、高剂量组干预后,监测小鼠造模前后心电图Ⅱ导联J点变化,检测血清过氧化氢酶（CAT）、谷胱甘肽转移酶（GSH-Px）、超氧化物歧化酶（SOD）活性以及乳酸（LD）的水平;显微镜下观察心肌缺血损伤的病理学变化及测定心肌梗死面积,并采用RT-PCR法测定组织caspase-3 mRNA的表达差异。结果 与模型组比较,柳茶挥发油中、高剂量组及阳性对照组缺血所致心电图J点的上移均显著降低（P<0.05）;血清CAT、GSH-Px、SOD活力明显增加（P < 0.05或P < 0.01）,LD含量明显降低（P<0.01）,病理学研究发现心肌损害程度减轻,缺血损伤面积明显减少,且高剂量干预组小鼠心肌组织的caspase-3 mRNA表达明显下调（P<0.05）。结论 藏药柳茶挥发油对小鼠急性心肌缺血损伤具有一定的保护作用,且与抑制caspase-3 mRNA的表达有关。     

异丙肾上腺素和精氨酸血管加压素诱导的大鼠心肌损伤模型比较

目的 分别建立异丙肾上腺素（ISO）和精氨酸血管加压素（AVP）诱导的大鼠心肌损伤模型,并将两种模型进行比较。方法 分别建立雄性SD大鼠AVP、ISO心肌损伤模型,ISO模型组大鼠按30 mg/kg的剂量以多点sc方式给药,连续2 d,1次/d;AVP模型组大鼠尾iv精氨酸血管加压素0.05 mg/kg。超声测量心功能,监测大鼠心电图,测量大鼠血清中心钠素（ANP）、脑利钠肽（BNP）、乳酸脱氢酶（LDH）、肌酸激酶（CK）、天冬氨酸转氨酶（AST）、超氧化物歧化酶（SOD）的水平,并对大鼠心脏进行HE染色,观察切片。结果 AVP模型组大鼠心电图ST段较对照组显著上升（P<0.05）,ISO模型组大鼠心电图紊乱且短期内不能恢复。超声结果显示,与对照组比较,ISO和AVP模型组大鼠的左心室舒张末期内径（LVDd）和左心室收缩末期内径（LVDs）显著增加（P<0.05）,射血分数（EF）显著下降（P<0.05）,E/A下降至1以下。AVP和ISO模型组大鼠ANP水平均显著高于对照组（P<0.01）;ISO模型组大鼠BNP水平显著高于对照组（P<0.01）。AVP和ISO模型组大鼠CK、LDH、AST水平均显著高于对照组（P<0.05）,ISO模型组大鼠CK、LDH水平均显著高于AVP模型组（P<0.05）;ISO模型组大鼠SOD含量显著低于对照组（P<0.05）。HE染色结果显示,对照组心肌细胞结构清晰排列紧密,AVP模型组心肌细胞出现细胞核溶解和空泡变性,ISO模型组出现心肌组织纤维化和炎细胞浸润。结论 ISO和AVP诱导的大鼠心肌损伤模型均有明显的心脏病理性改变,且前者对大鼠心肌的损伤的程度较大,初步判断可能是由于缺氧时间更长造成的。     

丹红注射液对多柔吡星所致Lewis肺癌小鼠心肌损伤保护作用的研究

摘 要 目的：研究丹红注射液（DH）对抗肿瘤药物多柔吡星（DOX）所致小鼠心肌损伤的保护作用及其机制。方法: 通过腋下注射Lewis肺癌细胞建立小鼠实体瘤模型,随机分为4组：模型对照组、DOX组、DH组、DH+DOX组。实验结束,颈臼处死小鼠,无菌分离心肌和肿瘤组织,肿瘤称质量,比色法检测心肌组织中乳酸脱氢酶（LDH）、肌酸激酶（CK)、超氧化物歧化酶（SOD）、过氧化物酶（CAT）和谷胱甘肽过氧化物酶（GPx）的活性及丙二醛（MDA）的含量;流式细胞仪检测心肌细胞内的细胞凋亡、活性氧（ROS）和线粒体膜电位（△Ψm）。结果: 与模型对照组相比,DOX和DH+DOX组中肿瘤质量显著下降（P<0.01）,且DH对DOX的抗肿瘤作用无显著影响;小鼠心肌组织中LDH和CK活性、细胞凋亡显著增加（P<0.01）。与DOX组相比,DH+DOX组心肌组织中LDH和CK活性、细胞凋亡显著降低（P<0.01）,且△Ψm、SOD、CAT与GPx的活性显著增加（P<0.05或P＜0.01）,MDA含量和ROS生成减少（P<0.01）。结论:腹腔注射DH不影响DOX的抗肺癌作用,但对于DOX介导的心肌损伤具有保护作用,其机制与DH抑制心肌组织氧化应激和稳定△Ψm有关。     

丹参酮ⅡA静脉乳剂对大鼠急性心肌缺血的保护作用

目的:研究丹参酮ⅡA静脉乳剂对大鼠急性心肌缺血的保护作用。方法:采用垂体后叶素、异丙肾上腺素造成大鼠急性心肌缺血模型,以心电图T波变化,血清CK、LDH,心肌匀浆SOD、MDA、GSH-PX为指标,研究丹参酮ⅡA静脉注射乳剂对大鼠急性心肌缺血的保护作用。结果:丹参酮ⅡA静脉乳剂5.6,2.8,1.4mg·kg-1剂量组均能明显对抗垂体后叶素引起的大鼠急性心肌缺血T波高耸,并且能够显著降低异丙肾上腺素致心肌缺血的大鼠血清中CK和LDH的释放,降低心肌匀浆中MDA的水平(P<0.05),保护心肌SOD和GSH-PX的活性。结论:丹参酮ⅡA静脉乳剂对大鼠急性心肌缺血具有显著的保护作用。其机制与增加冠脉流量,抑制脂质过氧化和改善心肌能量代谢有关。     

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.

---

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.     

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.     

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.     

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.