奥硝唑口腔黏贴膜的抗炎和体外抑菌作用

目的：观察奥硝唑口腔黏贴膜的抗炎和体外抑菌作用。方法：通过小鼠耳肿胀试验、小鼠毛细血管通透性试验、小鼠肉芽肿试验，观察奥硝唑口腔黏贴膜对急、慢性炎症的作用；通过体外抑菌试验，观察奥硝唑口腔黏贴膜的抑菌作用。结果：奥硝唑口腔黏贴膜中、高剂量组降低伊文思蓝的吸收，与空白组比较差异有显著性；奥硝唑口腔黏贴膜抑制小鼠毛细血管通透性，降低左右耳片重量差值，其中、高剂量组与空白组比较差异有显著性；奥硝唑口腔黏贴膜对小鼠急性炎症有抑制作用，能降低肉芽干重，其高剂量组与空白组比较差异有极显著性；奥硝唑口腔黏贴膜体外对致病菌有明显的抑菌作用（P〈0．01）。结论：奥硝唑口腔黏贴膜具有抗炎、抑菌的作用。     

冰连清咽喷雾剂的主要药效学研究

目的通过抗炎、镇痛和解热试验,阐明药物的功能主治,为临床应用提供科学依据。方法建立多种动物模型,观察冰连清咽喷雾剂对皮炎,耳肿胀,毛细血管通透性。结果冰连清咽喷雾剂能显著抑制甲醛、巴豆油所致皮肤毛细血管通透性的增高和醋酸所致腹腔毛细血管通透性的增高,有效抑制CMC引起的白细胞游走,对角叉菜胶所致大鼠足跖的肿胀和棉球肉芽肿的生成亦有显著的抑制作用;结论冰连清咽喷雾剂能显著抑制多种炎症模型动物炎症的产生和发展。     

安坤丸的抗炎、镇痛实验

目的：明确安坤丸对小鼠、大鼠抗炎及对小鼠镇痛功能的影响。方法：通过小鼠耳肿胀试验、小鼠毛细血管通透性试验、小鼠琼脂肉芽肿试验观察安坤丸对小鼠抗炎的影响；通过对大鼠子宫内膜炎试验，观察安坤丸对慢性炎症的作用，通过醋酸所致小鼠扭体反应试验，观察安坤丸镇痛作用。结果：安坤丸中、高剂量组均能抑制小鼠毛细血管通透性，能抑制小鼠琼脂肉芽肿的增长，安坤丸中高剂量组抑制大鼠子宫肿胀程度，安坤丸降低醋酸所致小鼠扭体反应次数。结论：安坤丸具有抑制炎症，缓解疼痛的作用     

紫草烧伤露的镇痛、抗炎和体外抑菌作用考察

目的:观察紫草烧伤露的镇痛、抗炎和体外抑菌作用.方法:通过小鼠甩尾试验和小鼠热板试验,观察紫草烧伤露的镇痛作用;通过小鼠耳肿胀试验、小鼠毛细血管通透性试验、小鼠肉芽肿试验,观察紫草烧伤露对急性炎症、慢性炎症的作用;通过体外抑菌试验,反应紫草烧伤露的抑菌作用.结果:紫草烧伤露中、高剂量组延长小鼠甩尾和舔足时间,与空白组比较,差异有显著性(t检验,P＜0.05);紫草烧伤露降低吸收度,其中、高剂量组与空白组比较,差值具有统计学意义(t检验,aP＜0.05,b P＜0.01),紫草烧伤露抑制小鼠毛细血管通透性,紫草烧伤露降低左右耳片重量差值,其中、高剂量组与空白组比较,差值具有统计学意义(t检验,aP＜0.05,bP＜0.01).紫草烧伤露对小鼠急性炎症有抑制作用,紫草烧伤露降低肉芽干重,其高剂量组与空白组比较,差值具有统计学意义(t检验,P＜0.01).紫草烧伤露抑制大鼠肉芽肿增生,具有抗炎的作用;紫草烧伤露体外对致病菌有明显的抑菌作用.结论:紫草烧伤露具有镇痛、抗炎、抑菌的作用.     

清咽糖浆的药理作用研究

目的：观察清咽糖浆抑菌抗病毒，抗炎，对免疫的增强作用和镇痛的药理作用，为临床治疗急慢性咽炎提供实验依据。方法：采用液体试管法，病毒吸附法观察其抑菌，抗病毒作用，用乙酸致小鼠毛细血管通透性增强，蛋清致大鼠足肿胀，羧甲基纤维素钠致小鼠白细胞聚集的方法观察其抗炎作用。采用小鼠尾静脉注射墨汁的方法观察其对小鼠单巨噬细胞蚕噬功能的影响，用乙酸致小鼠扭体次数的改变观察其镇痛作用。结果：清咽糖浆能抑制甲型，乙型溶血型链球菌，金黄色，白色葡萄球菌，肺炎双球菌的体外生长；1：10浓度对腺病毒3型，7型与流感病毒1型，3型有灭活作用。显著降低乙酸所致小鼠的毛细血管通透性，抑制大鼠的足肿胀，抑制大鼠羧甲基纤维素钠诱导的白细胞聚集；有促进小鼠单核巨噬细胞蚕噬功能的作用，显著减少小鼠乙酸扭体次数。结论：本品具抑菌抗病毒作用，有免疫促进和镇痛作用。     

屏风固金颗粒抑菌抗炎作用的实验研究

目的:研究屏风固金颗粒抑菌抗炎作用。方法:采用体内体外相结合的方法观察屏风固金颗粒抑菌作用;通过小鼠腹腔毛细血管通透性实验、二甲苯致小鼠耳廓肿胀实验及大鼠蛋清性足趾肿胀实验测定其抗炎作用。结果:屏风固金颗粒在体外对常见的多种致病菌有不同程度的抑制作用,在体内对感染金黄色葡萄球菌和表皮葡萄球菌的小鼠有明显的保护作用;能明显抑制小鼠腹腔毛细血管通透性亢进、二甲苯致小鼠耳廓肿胀及蛋清性大鼠足肿胀。结论:屏风固金颗粒具有抑菌抗炎作用。     

复方地榆解毒酒的药理作用

复方地榆解毒酒系采用中药按传统方法经白酒浸泡而得的酒剂，用于治疗痤疮。通过体外抑菌试验、鼠耳肿胀试验，小鼠皮肤毛细血管通透性试验，大鼠塑料环肉芽肿试验及小鼠扭体等试验，证明其有抑菌，抗炎和镇痛的作用。     

鱼腥草鼻用喷雾剂拮抗大鼠实验性鼻炎的药效学研究

目的:观察鱼腥草鼻用喷雾剂时克雷伯肺炎杆菌所致实验性大鼠鼻炎的影响及其抗炎活性.方法:以克雷伯肺炎杆菌感染大鼠鼻腔,造成鼻黏膜炎症;采用醋酸致小鼠腹腔毛细血管通透性增加,二甲苯致小鼠耳廓肿胀、大鼠棉球肉芽肿试验,观察其抗炎活性.结果:鱼腥草鼻用喷雾剂能够有效改善鼻炎动物的一般状态及鼻黏膜局部状况;对鼻炎的病理学改变具有抑制修复作用反有效控制致病细菌的局灶性感染.药物能够抑制醋酸所致小鼠腹腔毛细血管通透性增加,明显减轻二甲苯所致小鼠耳廓肿胀的程度,有效控制大鼠棉球肉芽组织的炎性生长.结论:鱼腥草鼻用喷雾剂具有显著的抗炎活性,具备拮抗急、慢性鼻炎的药效学基础.     

止咳祛痰糖浆抗炎抑菌的实验研究

目的研究止咳祛痰糖浆的抗炎抑菌作用。方法采用小鼠耳肿胀试验、小鼠毛细血管通透性试验、小鼠琼脂肉芽肿试验及体外抑菌试验,观察其抗炎作用和抑菌作用。结果止咳祛痰糖浆15mL·kg-1对急、慢性炎症均有抑制作用(P<0.05,P<0.01),止咳祛痰糖浆10mL·kg-1对小鼠耳肿胀有抑制作用(P<0.05),体外抑菌试验表明,对金黄色葡萄球菌、乙型链球菌、甲型链球菌有不同程度的抑菌作用。结论止咳祛痰糖浆对急、慢性炎症均有抑制作用,对金黄色葡萄球菌、乙型链球菌、甲型链球菌有不同程度的抑菌作用。     

槐角颗粒的主要药效学研究

目的观察槐角颗粒的主要药理作用.方法采用断尾凝血法、体外凝血法、扭体法、热板致痛法、耳廓肿胀法、腹腔毛细血管通透性观察法、棉球肉芽肿法、体内外抑菌试验等方法.结果槐角颗粒可明显缩短小鼠断尾后的出血时间及血管内凝血时间;对抗0.6%冰醋酸所致小鼠的扭体次数增加,提高小鼠的痛阈值;抑制致炎液所致小鼠耳廓的肿胀度;抑制冰醋酸所致小鼠腹腔毛细血管通透性的增加;抑制大鼠棉球肉芽肿的增长;并具有明显的抑菌作用.结论槐角颗粒与原丸剂型一样具有明显的止血、凝血及镇痛、抗炎、抗菌等药理作用.     

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.

---

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.