用正交试验研究番泻叶中总番泻苷的醇回流浸出方法

本文用正交试验法，建立了由番泻叶中浸出总番泻苷的醇回流提取方法。优选出最佳提取条件：乙醇浓度为55％，药物与醇的比例为1：12．5（g：ml），回流时间为第一次15min，第二次10min，浸泡时间为omin。提取效率考察证明：该法提取总番泻苷为其含量的99．64％。     

乙醇提取番泻叶中总番泻苷的工艺优选

目的：优选乙醇提取番泻叶中总番泻苷的最佳工艺。方法：采用正交设计法，以乙醇为溶媒对番泻叶中总番泻苷的提取工艺进行优选。结果与结论：最佳提取工艺条件为：70%乙醇提取3次，每次提取1h。     

乙醇提取番泻叶中总番泻苷的工艺优选

目的:优选乙醇提取番泻叶中总番泻苷的最佳工艺。方法:采用正交设计法,以乙醇为溶媒对番泻叶中总番泻苷的提取工艺进行优选。结果与结论:最佳提取工艺条件为:70％乙醇提取3次,每次提取1h。     

正交设计-多元回归法优选红景天中红景天苷超声波提取工艺

目的:优选红景天中红景天苷的超声波提取工艺。方法:以红景天苷含量为指标,设计L16(45)正交试验考察乙醇质量分数、料液比、提取时间、超声功率4个因素对红景天提取液中红景天苷含量的影响;采用Matlab 6.5软件,对红景天苷的超声波提取的正交试验数据进行数学模拟,通过多元回归法优选红景天苷的超声波提取工艺,并将优选的工艺与传统的加热回流工艺提取效果进行比较。结果:所得红景天苷最优提取工艺为乙醇质量分数77%、料液比1∶34(g∶ml)、提取时间34 min、超声功率237 W(超声频率40 k Hz)。此条件下提取所得红景天苷含量可达0.982 4%,与预测值0.989 4%相近。与加热回流法相比,两种方法提取所得红景天苷含量相近,但超声波法提取时间缩短了62.2%。结论:超声波提取法提取红景天中红景天苷操作简单、用时较短、提取率较高。     

超声波协同半仿生法提取金银花-连翘药对中4种成分的工艺研究

摘要：目的:优选金银花-连翘（1∶1）药对的超声波协同半仿生法提取工艺。方法:采用正交试验设计法,以金银花-连翘（1∶1）药对中绿原酸、连翘脂苷A、木犀草苷及连翘苷的含量为综合评分指标,考察料液比、提取时间、提取温度3个因素对提取效果的影响,进行验证试验。结果:3种因素对有效成分提取率的影响大小顺序为料液比>提取时间>提取温度,其中料液比具有显著性影响;超声波协同半仿生法提取的最优工艺参数为料液比1∶50、提取温度60℃、超声波时间60 min。结论:优选的超声波协同半仿生法提取工艺操作简单、结果稳定可行,可用于金银花-连翘（1∶1）药对的提取。     

正交实验法优选超声波法提取核桃仁总鞣质的最佳工艺

目的:优选超声波法提取核桃仁总鞣质的最佳工艺.方法:采用正交实验法优选超声波提取核桃仁总鞣质的最佳务件,采用EDTA络合滴定法测定含量.结果:最佳工艺为70%丙酮,lO倍溶剂量.超声提取60min.结论:该工艺提取核桃仁总鞣质是可行的.     

肠必清制剂提取及喷雾干燥工艺

采用L_9（3~4）正交表进行肠必清制剂提取工艺的研究，考察了提取时间、溶剂、溶剂量及pH等4个因素对总番泻甙含量和干粉得率的影响，结果优选出最佳提取工艺为A_1B_2C_3D_4，即提取时间为15min；溶剂量为10倍，8倍；提取液剂为50％乙醇；溶剂pH为4．0±0．2。考察提取液浓缩后总番泻甙的损失率，结果优选出浓缩温度为50℃～60℃，浓缩密度ρ为1．02。考察干粉总番泻甙损失率及含水量，优选出浓缩液喷雾速度为300ml／h～355ml／h，干燥进风温度为150℃～170℃，出风温度为100℃～105℃。     

超声波强化乙醇提取罗汉果甜苷

目的优选超声强化乙醇罗汉果甜苷的提取工艺。方法采用正交试验法考察乙醇溶液提取罗汉果甜苷的主要影响因素,以甜苷提取率为指标,评定优选工艺条件,在此基础上,进行扩展试验。结果在40 kHz、100 W超声波处理下,提取3次,最佳工艺条件为:第1次提取,以体积分数为40%的乙醇溶液,用量为25倍(溶剂体积与罗汉果质量之比),提取温度60℃,提取时间40 min;第2次提取,以体积分数为30%的乙醇溶液,用量为20倍,提取温度65℃,提取时间30 min;第3次提取,以体积分数为20%的乙醇溶液,用量为20倍,提取温度75℃,提取时间20 min。结论采用超声波可以有效地提高罗汉果的提取率。     

响应面法优选浙贝母中总生物碱的超声波提取工艺

目的:优选浙贝母中总生物碱的超声波提取工艺。方法:选取提取时间、超声波功率和液料比为随机因子,在单因素试验的基础上,进行3因素3水平的Box-Behnken试验设计,以总生物碱得率为响应值进行分析。结果:最佳提取条件为提取时间48min、超声波功率420W、液料比6.6(mL:g)。在此条件下,总生物碱得率验证值为0.1685%。结论:响应面法优选浙贝母中总生物碱的超声波提取工艺简便、易行。     

正交试验法优选强肾益精颗粒提取工艺

目的优选强肾益精颗粒提取工艺。方法以出膏率、松果菊苷转移率和总多糖提取量为指标,加水量、提取次数、提取时间为影响因素,采用L9(34)正交试验法,综合加权评分,优选强肾益精颗粒的提取工艺。结果处方最佳提取工艺为8倍量水,煎煮3次,每次为60 min。结论该优选的工艺合理,有效成分提取率高,稳定可行。     

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.