繖形科药材的研究 Ⅰ.独活的药材鉴定

本文就目前国內15个省区调查收集所得15种商品独活中的8种作了报导,计资丘独活、牛尾独活、白独活、山独活、光头独活、骚独活、猪独活及毛独活,全部属于繖形科植物。根据初步考证,认为本草所载的独活有多种植物来源,大多是繖形科独活属(Heracleum Linn.)植物,也有为当归属(Angelica Linn.)的。本文对上述8种药材的主产区、植物形态、药材性状以及根部组织等作了叙述。     

独活有效成分大鼠在体单向灌流肠吸收

为了考察独活提取物中二氢欧山芹醇乙酸酯、蛇床子素、二氢欧山芹醇当归酸酯等3种主要有效成分在大鼠的肠吸收性质,了解中药提纯后对大鼠肠吸收的影响，本文运用单向灌流模型并采用HPLC法测定独活提取物I(总香豆素含量＜10%)灌流液中3种成分在体肠灌流的浓度变化，并与独活提取物II(总香豆素含量≥60%)进行比较。结果表明二氢欧山芹醇乙酸酯、蛇床子素及二氢欧山芹醇当归酸酯的质量浓度分别为62～555 μg·mL^-1、101～887 μg·mL^-1和19～186 μg·mL^-1，吸收量与浓度呈线性关系,无高浓度饱和现象，吸收速率常数(K_a)、吸收渗透系数(P_app)值基本保持不变。3种成分在大鼠小肠主要以被动扩散方式吸收；在各肠段均有吸收，其中结肠吸收最好，各肠段的K_a、 P_app是结肠＞十二指肠＞空肠＞回肠，且结肠的K_a、 P_app值显著大于其他肠段；独活提取物II中3种成分的K_a、 P_app值显著小于独活提取物I中相应成分。     

独活药材中欧芹酚甲醚的含量考察

采用ＨＰＬＣ法测定了２１批独活药材中欧芹酚甲醚的含量。方法简便、灵敏、回收率为９８．８％，独活药材中欧芹酚甲醚平均含量为０．９７％。     

RP-HPLC法测定注射用羟喜树碱脂质体含量

目的 建立测定注射用羟喜树碱脂质体含量的方法。方法 采用反相高效液相色谱法。色谱系统为ODS柱,以甲醇-水(60∶40)为流动相,检测波长为266 nm。结果 本品在5.886～10.930μg·ml^-1范围内呈线性关系,回归方程为:A=6.438×10⁴C-2.184×10⁴,r=0.9998。回收率为98.9%,RSD%为0.38(n=9)。结论 本法可测定注射用羟喜树碱脂质体中羟喜树碱的含量,方法快速、简便、准确。     

高效液相色谱法测定中药石韦2种成分的含量高效液相色谱法测定中药石韦2种成分的含量

目的 对中药石韦中的2种成分绿原酸和圣草酚7-O-β-D-吡喃葡糖醛酸苷的分析方法进行研究,并测定了不同种、不同产地石韦中2种成分的含量。方法 用反相C₁₈柱,甲醇-水-磷酸(50∶200∶0.2)为流动相,284 nm作为检测波长。结果 绿原酸和圣草酚7-O-β-D-吡喃葡糖醛酸苷的含量分别在0.01～5 μg和0.004～5 μg有良好的线性关系(R=0.999 7),样品的回收率分别为97.9%(RSD=2.9%)和99.1%(RSD=2.4%)。结论 采用RP-HPLC法对21个不同种、不同产地石韦样品进行了测定,不同产地、不同种石韦中绿原酸及圣草酚7-O-β-D-吡喃葡糖醛酸苷的含量相差悬殊,本方法为控制中药石韦质量及合理采收提供了简便易行的方法。     

RP-HPLC测定抗病毒口服液中连翘苷的含量

目的 以反相高效液相色谱法测定抗病毒口服液中连翘苷的含量。方法 色谱条件为:ODS柱(4.6mm×25cm,5μm);流动相:乙腈-水(25∶75);检测波长277nm;平均回收率为100.22%,RSD为3.61%(n=5)。结果 该方法简便,与样品中其它成分容易分开,稳定性与精密度良好。结论 本法可作为抗病毒口服液中连翘苷含量测定的一种方法。     

长苞凹舌兰化学成分研究

目的研究长苞凹舌兰Coeloglossum viride (L.) Hartm. var. bracteatum (Willd.) Richter的化学成分。方法 采用硅胶、大孔吸附树脂及反相硅胶柱色谱法分离纯化,运用波谱法进行结构鉴定。结果从乙醇提取物中分得8个化合物,分别鉴定为dactylorhin B (I)、loroglossin (II)、dactylorhin A (III)、militarine (IV)、长苞凹舌兰素甲(coelovirin A,V)、天麻苷(gastrodin,VI)、胸腺嘧啶核苷(thymidine,VII)和槲皮素-3,7-二-O-β-D-吡喃葡糖苷(quercetin-3,7-di-O-β-D-glucopyranoside,VIII)。结论8个化合物均为首次从凹舌兰属植物中分得,其中V为新化合物。     

反相高效液相色谱法测定木属植物中黄酮类和香豆精的含量

目的：对木属植物中草本和木本两个自然群进行化学分类学的研究。方法：应用反相高效液相色谱法测定木属植物中4种化学成分［neoliguiritin (I), 5,8-dimethoxycoumarin (II), isoliquritoside (III), 8-［(2″,3″)-prenyl］-4′-methoxy-flavone-7-O-β-D-glucopyranosyl-(2→1)-α-L-rhamnopyranoside (IV)］,对本属11种植物中该4种成分进行了定量分析。色谱柱固定相为Supelco SIL-LC-18;流动相为40%甲醇—甲醇梯度洗脱,根据4种成分紫外吸收波长的不同而改变检测波长;流速1.0 ml.min^-1;4种成分的线性范围分别为(0.5600～0.0175) μg,(0.3760～0.0118) μg,(0.2875～0.0090) μg和(0.3090～0.0097) μg,回收率分别为98.92%,98.27%,94.78%和97.41%。结果：木本自然群中香豆精成分含量较高。结论：香豆精为木本自然群区别于草本自然群的特征成分之一。     

RP-HPLC法测定兰索拉唑口崩片的含量

目的 建立反相高效液相色谱法(RP-HPLC)测定兰索拉唑口崩片中兰索拉唑含量的方法。方法 以十八烷基键合硅胶柱为色谱柱(4.6 mm×250 mm,5μm);流动相为甲醇-水-三乙胺-磷酸(700∶300∶5∶1.5),用磷酸(1→10)调pH至7.3±0.1;检测波长284 nm。结果 在12.24～18.36μg·ml范围内呈良好线性,r=0.9995;平均回收率为101.1%,RSD为1.8%(n=9)。结论 该方法简便快捷,结果可靠。     

盐酸罗哌卡因温敏凝胶注射剂的制备及其含量测定

目的 制备盐酸罗哌卡因温敏凝胶注射剂,并建立其含量测定方法。方法 采用泊洛沙姆作为温敏材料,以冷法制备,利用反相高效液相色谱法测定其中药物的含量。结果 温敏凝胶注射剂中辅料泊洛沙姆P407与P188的质量比为28:1,盐酸罗哌卡因含量为2%,相变温度为37℃。盐酸罗哌卡因在2.03~48.72 μg/ml范围内线性关系良好(r=0.999 8),精密度和重复性良好,低、中、高浓度盐酸罗哌卡因的回收率分别为(99.58±0.20)%、(97.80±0.35)%、(103.60±0.63)%,n=3,3批样品中盐酸罗哌卡因的平均含量分别为标示量的(98.92±0.35)%、(99.18±0.38)%、(98.72±0.62)%,n=3。结论 采用泊洛沙姆为基质制备的盐酸罗哌卡因温敏凝胶注射剂质量可控,是一种很有开发前景的新型止痛剂。     

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.     

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.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

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.