龙眼参多糖对四氯化碳诱导大鼠原代肝细胞损伤的保护作用

目的:研究龙眼参多糖(LYS)对大鼠原代肝细胞损伤的保护作用及其机制。方法:用四氯化碳(CCl4)体外诱导大鼠原代肝细胞损伤,检测培养上清液中天门冬氨酸转移酶(AST)和丙氨酸氨基转移酶(ALT)水平,测定肝细胞中丙二醛(MDA)和谷胱甘肽(GSH)含量,四甲基偶氮唑盐(MTT)法检测细胞活性。结果:与模型组比较,LYS组AST和ALT水平及肝细胞MDA含量明显降低,肝细胞存活率和GSH含量升高。结论:LYS对大鼠原代培养肝细胞损伤有直接保护作用,机制可能与其抗氧化作用有关。     

黄芪总提物对体外肝细胞损伤的保护作用

目的研究黄芪总提物 (TEA)对体外肝细胞损伤的保护作用及其机理。方法采用Ⅳ型胶原酶灌流法分离大鼠肝细胞进行原代培养 ,用CCl4 和H2O2 体外分别诱导肝细胞损伤 ,检测肝细胞丙二醛 (MDA)、谷胱甘肽 (GSH)含量和谷胱甘肽过氧化物酶 (GSHpx)活性以及培养上清液中天门冬氨酸转换酶 (AST)和/或丙氨酸氨基转换酶 (ALT)水平。结果 (1)TEA(5～80mg·L-1)可明显降低或恢复由CCl4 升高的肝细胞MDA含量及肝细胞培养上清液中AST水平 ,还可使CCl4 降低的肝细胞GSH含量和GSHpx活性升高或恢复 ;(2)TEA(5～80mg·L-1)可使H2O2升高的肝细胞培养上清液中ALT水平和肝细胞MDA含量明显降低或恢复 ,还可使H2O2降低的肝细胞GHS含量和GSHpx活性明显升高或恢复。结论提示TEA对体外肝细胞损伤有直接保护作用 ,该作用可能与其抗氧化作用有关     

金丝桃苷对四氯化碳诱导肝细胞损伤的保护作用

目的研究金丝桃苷(hyperfine,HP)对四氯化碳(CCl4)诱导肝细胞损伤的保护作用及其机制。方法用CCl4体外诱导人正常肝细胞L-02损伤,检测培养上清液中天门冬酸氨基转移酶(AST)和丙氨酸氨基转移酶(ALT)水平,测定肝细胞中丙二醛(MDA)和谷胱甘肽(GSH)的含量,四甲基偶氮唑盐微量酶反应比色(MTT)法检测肝细胞存活率。结果金丝桃苷可明显降低由CCl4升高的肝细胞培养上清液中ALT和AST水平及肝细胞MDA含量,还可提高由CCl4降低的肝细胞存活率和GSH含量。结论金丝桃苷对人肝细胞氧化性损伤有直接保护作用,这可能与金丝桃苷抑制抗氧化酶活性和抗自由基活性有关。     

珠蚌多糖对四氯化碳诱导肝细胞损伤的保护作用

目的 研究珠蚌多糖(HCP)对肝细胞损伤的保护作用及其机制.方法 培养L-02型肝细胞,用四氯化碳(CCL)体外诱导肝细胞损伤,检测培养上清液中天门冬氨酸转挟酶(AST)和丙氨酸氨基转换酶(ALT)水平,测定上清液中丙二醛(MDA)的含量扣过氧化物岐化酶(SOD)活力,MTT法检测细胞存活和增殖活性.结果 珠蚌多糖(25,250及1000μg·L-1)剂量组均可明显降低由CCl4升高的肝细胞培养上清波中AST争ALT水平及MDA含量,还可提高CCl4降低的肝细胞存活率和SOD活力.结论 提示珠蚌多糖对肝细胞损伤有直接保护作用,该作用可能与其抗氧化作用有关.     

南沙参多糖对四氯化碳损伤原代培养大鼠肝细胞保护作用的研究

目的:探讨南沙参多糖(RAPS)对四氯化碳(CCl4)损伤原代培养大鼠肝细胞的保护作用及其机制。方法:通过原位灌流法分离大鼠肝细胞,培养36h后加入RAPS,同时造成CCl4损伤,分别于损伤24h和48h时检测培养液中丙二醛(MDA)的含量、丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)、超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-PX)的活性,48h后用MTT法测定肝细胞存活率。结果:RAPS对CCl4引起的ALT、AST活力的升高有抑制作用,同时抑制MDA的产生及肝细胞损伤造成的SOD活性及GSH-PX活性的降低。而且能明显改善肝细胞存活率。结论:RAPS能有效抑制CCl4造成的原代培养大鼠肝细胞损伤,机制可能与其抗氧化作用有关。     

二至丸提取物对体外肝细胞损伤的保护作用

 目的：研究二至丸乙酸乙酯提取物(ethyl acetate extractsof Erzhi pill,EAEP)对体外肝细胞损伤的保护作用及其机理。方法：培养L-O2型肝细胞,采用CCl4和H2O2体外分别诱导肝细胞损伤,检测培养上清液中天门冬氨酸转换酶(AST)和丙氨酸氨基转换酶(ALT)水平,测定上清液中丙二醛(MDA)的含量和过氧化物岐化酶(SOD)活力及谷胱甘肽过氧化物酶(GSH-Px)活性,MTT法检测细胞存活和增殖活性。结果：① EAEP(0.32～40 μg?mL-1)剂量组可明显降低由CCl4所致肝细胞培养上清液中AST和ALT水平及MDA含量的升高,还可提高由H2O2所致肝细胞存活率和SOD活力及GSH-Px活性的降低。② EAEP(0.32～40 μg?mL-1)剂量组可使H2O2升高的肝细胞培养上清液中ALT和ALT水平及MDA含量明显降低或恢复,还可提高CCl4降低的肝细胞存活率和SOD活力及GSH-Px活性。结论：提示AEEP对体外肝细胞损伤有直接保护作用,该作用可能与其抗氧化作用有关。     

二至丸保肝有效部位群对体外肝细胞损伤的保护作用

目的 研究二至丸保肝有效部位群(50％乙醇部位)(EFEP)对体外肝细胞损伤的保护作用及机理.方法 培养L-O2型肝细胞,采用四氯化碳(CCl4)和过氧化氢(H2O2)体外诱导肝细胞损伤,检测培养上清液中AST和ALT水平,测定上清液中丙二醛(MDA)的含量、过氧化物岐化酶(SOD)及谷胱甘肽过氧化物酶(GSH-Px)活性,MTT法检测细胞存活和增殖活性.结果 EFEP0.32-40 μg/ml明显降低由CCl4所致肝细胞培养上清液中AST和ALT水平和MDA含量的升高,也显著提高由CCl4所致肝细胞存活率和SOD活力及GSH-Px活性的降低.EFEP 0.32-40 μg/ml使H2O2升高的肝细胞培养上清液中AST和ALT水平及MDA含量明显降低,还显著提高由H2O2降低的肝细胞存活率和SOD活力及GSH-Px活性.结论 EFEP对体外肝细胞损伤有较强的保护作用.该作用可能与其抗氧化作用有关.     

二至丸水提物对体外肝细胞损伤的保护作用

目的研究二至丸水提物（aqueous extract of Erzhi Pill,AEEP）对体外肝细胞损伤的保护作用及其机制。方法培养L-O2型肝细胞,采用H2O2和CCl4体外分别诱导肝细胞损伤,检测培养上清液中天门冬氨酸转换酶（AST）和丙氨酸氨基转换酶（ALT）水平,测定上清液中丙二醛（MDA）的含量和过氧化物岐化酶（SOD）活力,MTT法检测细胞存活和增殖活性。结果①AEEP（0.32~40μg/ml）剂量组可明显降低由H2O2升高的肝细胞培养上清液中AST和ALT水平及MDA含量,还可提高H2O2降低的肝细胞存活率和SOD活力;②AEEP（0.32~40μg/ml）剂量组可使CCl4升高的肝细胞培养上清液中ALT和ALT水平及MDA含量明显降低或恢复,还可提高CCl4降低的肝细胞存活率和SOD活力。结论提示AEEP对体外肝细胞损伤有直接保护作用,该作用可能与其抗氧化作用有关。     

异甘草素对大鼠急性化学性肝损伤的保护作用

目的研究异甘草素(ISL)对CCl4所致大鼠急性化学性肝损伤的保护作用及其机制.方法①在体实验选用♂Wistar大鼠48只,随机分6组,每组8只.ISL三剂量给药组分别灌服ISL 10,20,40 mg·kg-1·d-1;甘草酸二铵胶囊(DG)组灌服DG 500 mg·kg-1·d-1;正常对照组和模型组每日灌服等容量的溶媒.连续给药7 d,qd.以CCl4诱导大鼠急性肝损伤模型,酶学测定各组大鼠血清谷丙转氨酶(ALT)、谷草转氨酶(AST)和超氧化物歧化酶(SOD)活性,以及肝组织丙二醛(MDA)、谷胱甘肽(GSH)、谷胱甘肽过氧化物酶(GSH-Px)含量.②体外实验采用大鼠离体肝细胞原代培养,并建立CCl4诱导肝细胞损伤模型,检测ISL对其作用的影响.结果①lSL剂量依赖性降低大鼠血清中升高的ALT和AST活性,升高肝组织中降低的GSH含量、SOD和GSH-Px活性,同时降低过氧化物终产物含量.②ISL浓度(5.0～20.0 μmol·L-1)依赖性抑制CCl4引起的ALT和AST升高,ISL 20.0 μmol·L-1可阻断CCl4产生的肝细胞ALT和AST漏出.结论ISL对大鼠化学性肝损伤具有显著的保护作用.其机制与清除肝组织中的自由基和抗脂质过氧化等作用有关.     

红丝线多糖对大鼠急性肝损伤的保护作用

目的 研究红丝线多糖对大鼠急性肝损伤的保护作用.方法 采用CCl4诱导大鼠急性肝损伤模型,观察红丝线多糖对大鼠血清中丙氨酸氨基转换酶(ALT)、天门冬氨酸氨基转换酶(AST)、丙二醛(MDA)、超氧化物歧化酶(SOD)水平的影响.结果 红丝线多糖各剂量组可抑制急性肝损伤大鼠血清中ALT、AST的活性,降低MDA的水平,升高SOD的活性.结论 红丝线多糖对CCl4致大鼠急性肝损伤具有较好的保护作用.     

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.     

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.