3种抗病毒药对家兔骨髓细胞抑制的比较

目的：评价利巴韦林、更昔洛韦及单磷酸阿糖腺苷3种常用抗病毒药对骨髓细胞的抑制以及停药后恢复情况。方法：将家兔随机分成正常对照（D组）及A、B、C3个实验组，分别给予注射生理盐水、利巴韦林、更昔洛韦及单磷酸阿糖腺苷耳静脉推注，qd，连续注射14d停药。停药1d和8d进行骨髓细胞定量分析，并对照外周血网织红细胞（Ret）计数。结果：A、B、C3组停药1d的骨髓巨核细胞明显低于D组（P〈0.01），骨髓有核细胞总量也均低于D组，其减少程度依次C〉A〉B〉D组，停药8d的骨髓有核细胞均能恢复到D组水平，但巨核细胞恢复缓慢。同期A组停药1d的Ret较D组明显升高（P〈0．01），停药1d和8d的B组Ret变化较小，C组抑制率较高。结论：C组骨髓细胞抑制较明显，B组较轻，A组介于两者之间且伴有较明显的贫血；Ret计数不能完全替代骨髓细胞定量分析。     

3种抗病毒药对家兔外周血血红蛋白和网织红细胞的影响

目的评价利巴韦林、更昔洛韦、单磷酸阿糖腺苷3种常用抗病毒药对家兔外周血血红蛋白含量（Hb)和网织红细胞比率（Ret）的影响。方法取家兔20只，随机分成4组，每组5只。A组按15 mg·kg^-1的剂量给予利巴韦林，B组按10 mg·kg^-1的剂量给予更昔洛韦；C组按10 mg·kg^-1的剂量给予单磷酸阿糖腺苷；D组按每只2 mL的剂量给予0.9%氯化纳注射液。均为每天1次，共14 d。每隔4 d观察家兔外周血Hb和Ret变化。结果 给予抗病毒药后，A组Hb明显下降，而Ret上升，停药1周后，两者均开始逐渐恢复；B组Hb无明显变化，Ret有轻度上升，停药1周后回落；C组 Ret缓慢下降，停药1周后稍有回升，Hb变化不明显；D组无明显变化。结论利巴韦林、更昔洛韦和单磷酸阿糖腺苷3种常用抗病毒药对红细胞的损伤程度不一，选择用药时应引起重视。     

3种抗病毒药对家兔凝血功能影响的初步研究

目的探讨利巴韦林（A组）、更昔洛韦（B组）及单磷酸阿糖腺苷（C组）3组常用抗病毒药对家兔凝血功能影响.方法经家兔耳静脉推注给药两周,测停药第一天和第八天的PT、APTT及TT值,并与注射用生理盐水组（D组）对照分析.结果 4组在停药第一天及第八天的PT、TT值变化均无统计学差异;A、B、C3组停药第一天的APTT值较D组分别缩短9.06、11.91、13.64s,第八天的APTT值较D组分别缩短5.42、14.90、18.56s,其中B、C组与D组比较显示统计学差异.结论 B和C组用药后内源性凝血因子可能被部分活化.     

不同浓度利巴韦林对家兔巨核细胞和血小板的影响

目的研究4种浓度利巴韦林对家兔巨核细胞和血小板的影响。方法设定低浓度（A组）、中浓度（B组）、高浓度（C组）、超高浓度（D组）及生理盐水（E组）5组,经家兔耳缘静脉分别注射两个疗程,定期抽取外周血和骨髓,观察血小板和巨核细胞变化。结果用药两周后（停药第1d）。与E组比较．各组巨核细胞上升率分别为63．3％、47．7％、5．2％、0．8％,且注射浓度越低上升越明显。停药两周（15d）后,巨核细胞与对照比较（P〉0．05）,示明显恢复。血小板用药两周期间,A、B、C组随着用药浓度增加而升高,均呈先升后降趋势．D组持续上升较长．停药两周后血小板均有明显恢复。停药1d的巨核细胞与血小板变化呈负相关性（r=-0．961,P〈0．05）。结论利巴韦林能促进骨髓巨核细胞的增生和外周血小板的增多。对血小板减少的病毒感染患者可首选该药并适当提高用药浓度．且用药后的巨核细胞和血小板变化能在停药后较短时间内恢复。     

两种方案治疗疱疹性口炎的成本-效果分析

目的评价两种方案治疗疱疹性口炎的成本-效果。方法两组均给予维生素C、维生素B6静脉滴注及康复新溶液等综合处理。A组给予更昔洛韦5mg/kg d+0.9%氯化钠注射液50~100mL,静脉滴注,1次/日。B组给予利巴韦林10mg/kg+0.9%氯化钠注射液50~100mL,静脉滴注,1次/日。疗程3~5d。结果更昔洛韦组成本/有效率(C/E)比利巴韦林组小3.36元。结论更昔洛韦、利巴韦林两种方案治疗疱疹性口炎中,更昔洛韦是比较经济的方案,且无明显不良反应,值得推荐。     

更昔洛韦治疗小儿病毒性脑炎42例的疗效观察

目的观察更昔洛韦治疗小儿病毒性脑炎的疗效和安全性.方法将病毒性脑炎患儿随机分为更昔洛韦治疗组(42例)及利巴韦林治疗对照组(44例),治疗组给予更昔洛韦5～10 mg·kg-1·d-1,bid,静脉滴注,疗程7～14 d;对照组给予利巴韦林10mg·kg-1·d-1,bid,疗程7～14 d.两组患儿均接受病毒性脑炎的常规治疗.对两组患儿的临床表现及治疗效果进行观察.结果更昔洛韦治疗组的发热消退时间、头痛、呕吐及抽搐症状和意识障碍恢复的时间较利巴韦林治疗组明显缩短(P＜0.05).结论更昔洛韦对小儿病毒性脑炎有明显疗效.     

更昔洛韦治疗小儿疱疹性咽峡炎的临床观察

目的探讨更昔洛韦对小儿疱疹性咽峡炎的临床效果。方法选用符合诊断标准的疱疹性咽峡炎患儿198例,随机分为2组,更昔洛韦组(治疗组)103例,静脉注射更昔洛韦5 mg/kg。1次/d,疗程5 d。利巴韦林组(对照组)95例,静脉注射利巴韦林10 mg/kg。1次/d,疗程5 d。结果治疗后更昔洛韦组在总有效率、退热时间和疱疹消退时间均较利巴韦林组差异有统计学意义(P<0.05)。结论更昔洛韦治疗小儿疱疹性咽峡炎疗效好、起效快、安全、毒副作用小、值得临床推广。     

西咪替丁、更昔洛韦及利巴韦林治疗小儿水痘的疗效比较

目的:比较西咪替丁、更昔洛韦及利巴韦林治疗小儿水痘的疗效及安全性.方法:90例水痘患儿随机分为三组,利巴韦林组30例用利巴韦林注射液10 mg/(kg·d);更昔洛韦组30例用更昔洛韦注射液5 mg/(kg·d);西咪替丁组30例用西咪替丁注射液15 mg/(kg·d),三组均1次/d静脉滴注,疗程5 d,其他治疗相同.结果:西咪替丁组总有效率86.67%,更昔洛韦组总有效率93.33%,利巴韦林组总有效率63.33%;西咪替丁组和更昔洛韦组症状、体征好转时间比较差异无统计学意义(P＞0.05),与利巴韦林组比较差异有统计学意义(P＜0.05或P＜0.01).结论:西咪替丁和更昔洛韦治疗小儿水痘疗效显著,短期使用安全性好.     

更昔洛韦治疗小儿手足口病疗效观察

目的:观察更昔洛韦治疗小儿手足口病的临床疗效.方法:将158例手足口病患儿随机分成治疗组和对照组,分别静脉给予更昔洛韦5 mg·kg-1·d-1和利巴韦林10～15 mg·kg-1·d-1,对临床症状和体征进行观察和分析.结果:治疗组临床症状和体征均较对照组消失早(P<0.01).结论:更昔洛韦治疗小儿手足口病疗程短,见效快,有明显疗效.     

更昔洛韦联合利巴韦林治疗婴儿巨细胞病毒性肝炎疗效观察

目的观察更昔洛韦联合利巴韦林治疗巨细胞病毒性肝炎的临床效果。方法收集近4年治疗的巨细胞病毒性肝炎43例分为两组,治疗组患儿采用更昔洛韦联合利巴韦林治疗,对照组予以更昔洛韦治疗。结果治疗组总有效率为95.56%,对照组为78.57%,差异有显著性(P<0.05)。结论更昔洛韦联合利巴韦林治疗巨细胞病毒性肝炎效果好,值得临床推广应用。     

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.