丹参和丹酚酸B对抗泼尼松致大鼠皮肤衰老作用的观察

目的:探讨丹参(Salvia Miltiorrhiza)和丹酚酸B(Salvianolic acid B,Sal B)对用泼尼松引起的大鼠皮肤衰老作用的影响.方法:32只SD雄性大鼠随机分为4组(n=8):正常对照组,激素模型组(GC)、激素加用丹参组(GC DS),激素加用丹酚酸B组(GC SaL B).正常对照组每天灌胃生理盐水,后3组每天分别灌胃泼尼松3.5 mg·kg-1d-1造模,GC DS组再给予丹参水提液5g·kg-1·d-1;GC Sal B组再给予丹酚酸B原料药125 mg·kg-1·d-1.喂养90 d后处死大鼠取皮肤进行组织病理学检查,并用计算机图像分析系统定量分析表皮厚度、弹力纤维的面积;另外以高效液相色谱法对药品进行丹酚酸B含量测定.结果:GC组可见大鼠皮肤表皮显著变薄,弹力纤维减少(P<0.01),胶原纤维减少,断裂等皮肤衰老样的表现,GC DS、sal B组可使大鼠表皮增厚、弹力纤维总面积增大(P<0.01),皮肤衰老样改变明显减轻;丹参水提液、丹酚酸B原料药分剐检测出相当含量的丹参水溶性成份丹酚酸B.结论:长期灌胃给药泼尼松可使大鼠出现皮肤衰老样改变,丹参和丹酚酸B对其有较好的对抗作用,丹酚酸B可能是丹参对皮肤作用的重要有效成分.     

丹参水提物和丹参素促进成骨细胞活性和防治泼尼松所致大鼠骨质疏松

目的　研究丹参水提物 (DWE)对糖皮质激素造成大鼠骨质疏松的预防作用 ,同时研究DWE和有效成分丹参素对体外培养的大鼠成骨细胞的影响 ,以探讨其作用机制。方法　① 4mon龄SD大鼠分为对照组、模型组 (以泼尼松 2 7mg·kg- 1·d- 1灌胃 ) ,丹参水提物组 (泼尼松 +DWE 5 0g·kg- 1·d- 1)和综合治疗组 (泼尼松 +司坦唑醇 0 5mg·kg- 1·d- 1+VitD3 2 50IU·kg- 1·d- 1+葡萄糖酸钙 0 5g·kg- 1·d- 1) ,共给药 12wk。采用骨组织形态计量学方法定量观察大鼠胫骨松质骨的骨结构 ,同时测定骨无机及有机质含量 ;②采用体外大鼠成骨细胞培养 ,测定DWE和丹参素对细胞碱性磷酸酶 (ALP)的活性及药物量效、时效关系。结果　泼尼松可导致骨小梁面积明显减少 ,骨结构异常 ,破骨细胞增多和骨形成率下降 ,伴随骨无机质钙盐 (Ca)和有机质羟脯胺酸 (HyP)下降 ,血钙上升 (以上指标P <0 0 1)。DWE完全对抗由泼尼松引起的上述异常并增加骨干重 ,对增加骨干重和骨有机质含量优于综合组。DWE和丹参素均可促进大鼠颅骨成骨细胞ALP活性 ,呈量效关系 (DWE最佳作用浓度为 1 0～ 2 0g·L- 1,丹参素为 0 1～ 1 0mg·L- 1)和时效关系 (随时间延长作用明显增强 ) ,DWE的效应按含丹参素量计算 ,与丹参素作用相当。结论　丹参水提?     

脑益康对阿尔茨海默病模型小鼠学习记忆的影响

目的 :观察脑益康对阿尔茨海默病 (Alzhei mer’sdisease ,AD)模型小鼠学习记忆的影响 ,并探讨其改善学习记忆的机制。方法 :采用D 半乳糖 (D Gal)和亚硝酸钠 (NaNO2 )腹腔注射建立小鼠AD模型 ,通过迷宫刺激器和水迷宫实验检测小鼠学习记忆能力 ;生化方法检测小鼠脑组织内超氧化物歧化酶 (SOD)活性和丙二醛 (MDA)含量 ;透射电镜观察小鼠海马神经细胞的超微结构。结果 :模型对照组小鼠学习记忆能力下降 ,SOD活性降低 ,MDA含量升高 ;而与模型对照组比较 ,脑益康小、中、大剂量组(2 .4、7.2、2 4g·kg-1·d-1)均可显著改善模型小鼠的学习记忆能力 ,提高脑内SOD活性 ,降低脑内MDA含量 (P <0 .0 1或P <0 .0 5 ) ,阻抑海马神经细胞的退行性变化。结论 :脑益康可改善D 半乳糖和亚硝酸钠所致AD模型小鼠的学习记忆能力。     

丹参水提液对抗大鼠泼尼松性骨质疏松的作用研究

目的:观察中药丹参水提液对泼尼松所致的大鼠骨质疏松的对抗作用。方法:50只大鼠随机分成正常对照组、泼尼松组和丹参水提液高、中、低剂量组,每组10只。分别灌喂相应药物,每日1次,连续8周后取血清检测生化指标,对骨进行组织切片检查,长度、宽度以及骨质的测量。结果:泼尼松组大鼠股骨重量、骨羟脯氨酸和骨钙含量比正常对照组明显降低,骨髓腔中脂肪组织增多(P<0.01),血浆胆固醇含量上升、碱性磷酸酶和高密度脂蛋白含量下降(P<0.05)。丹参水提液能有效提高骨的重量和骨质的含量(P<0.05),减少骨髓腔中脂肪的含量,升高碱性磷酸酶和高密度脂蛋白含量(P<0.05),但量效关系不明显。结论:泼尼松可抑制大鼠的骨生长及引起骨丢失,丹参水提液对其有较好的对抗作用。     

续断提取物对小鼠D-半乳糖拟痴呆模型的抗氧化作用

目的:观察续断提取物对D-半乳糖(D-galactose,D-gal)模型小鼠脑组织和外周血中SOD活性、MDA含量及学习记忆能力的影响.方法:小鼠皮下注射D-gal 100mg·kg-1·d-1×49 d,用续断的正丁醇、水提取物灌胃给药.于第0 d和49 d进行Y迷宫游泳试验,第50 d处死小鼠,生物化学方法检测脑组织、外周血中超氧化物歧化酶(SOD)活性和脂质过氧化物(MDA)含量.结果:与模型组比较,续断正丁醇提取物按生药剂量7.5 g·kg-1和10 g·kg-1组小鼠学习记忆能力明显改善,其中10 g·kg-1组小鼠脑组织SOD活性明显升高;续断水提取物按生药剂量20 g·kg-1组小鼠游泳时间明显减少,脑组织SOD活性明显升高.两种提取物各剂量组小鼠脑组织、外周血中MDA含量均较模型组显著下降.结论:续断正丁醇和水提取物具有明显的抗氧化作用,并能增强小鼠学习记忆能力.     

醒脑静注射液对乙醇所致记忆功能障碍的影响

目的 :观察醒脑静注射液 (Xnji)对乙醇所致记忆障碍的改善作用。方法 :乙醇一次给大鼠和小鼠灌服和连续灌服造成学习记忆功能障碍 ,学习记忆的测试采用Morris水迷宫法 ,电迷宫法和避暗法。结果 :Xnji 1.4 ,0 .7ml·kg-1可预防一次性灌服乙醇所致的大鼠空间辨别障碍 ;Xnji 1,2ml·kg-1可治疗连续灌服乙醇所致的小鼠空间辨别障碍和记忆获得障碍。结论 :Xnji可防治急、慢性乙醇中毒所致的学习记忆功能减退。     

咪唑酮类化合物ZLJ-6对大鼠脑缺血再灌注损伤的保护作用及其机制研究

目的:考察化合物ZLJ-6对大鼠局灶性脑缺血再灌注损伤的保护作用,并探讨其可能的作用机制.方法:将50只健康雄性大鼠,随机分为假手术组、缺血-再灌注模型组、阿司匹林(10 nag·kg-1)阳性对照组、ZLI-6(20 mg·kg-1)高剂量组和ZLJ-6(10 mg·kg-1)低剂量组.以线栓法制作大鼠大脑中动脉缺血再灌注模型.造模后24小时,进行神经功能评分,并断头取脑制备组织匀浆,测定丙二醛和谷氨酸的含量以及超氧化物歧化酶、髓过氧化物酶、一氧化氮合酶和诱导型一氧化氮合酶的活性.结果:与模型组比较,阳性对照组和ZLJ-6高剂量组大鼠的神经功能评分均明显改善(P<0.05),ZLJ-6高、低剂量组大鼠脑中髓过氧化物酶活性均显著降低(P<0.01),ZLJ-6高剂量组大鼠脑中一氧化氮合酶活性降低(P<0.05),ZLJ-6低剂量组大鼠脑中诱导型一氧化氮合酶活性和丙二醛含量显著降低(P<0.01和JP<0.05);ZLJ-6对大鼠脑中超氧化物歧化酶活性和谷氨酸含量无明显影响.结论:化合物ZLJ-6对大鼠脑缺血再灌注损伤具有一定的保护作用,其作用机制可能与抑制缺血再灌注时中性粒细胞向脑组织浸润和抑制一氧化氮合酶活性有关.     

葡萄籽原花青素对慢性间歇性低氧大鼠空间工作记忆和5-羟色胺的影响

目的 探讨葡萄籽原花青素(GSPE)对慢性间歇性大鼠空间工作记忆和5-羟色胺(5-HT)的影响.方法 健康雄性SD大鼠80只,随机分为正常对照组、模型对照组、GSPE小剂量组(100 mg·kg-1)和GSPE大剂量组(200 rng·kg-1),每组20只.正常对照组暴露于空气中,模型对照组和GSPE小、大剂量组暴露于低氧(50 mL·L-1)条件下,暴露时间每天8h,持续6周;Morris水迷宫检测大鼠的空间记忆能力;应用苏木精-伊红染色观察脑组织形态变化;用高效液相色谱法测定大脑皮质内5-HT的含量.结果 与正常对照组比较,模型对照组水迷宫测试结果显示大鼠潜伏期明显延长,穿台次数明显减少;皮质区存活神经细胞数量减少,5-HT含量明显降低(P＜0.05).与模型对照组比较,GSPE小、大剂量组水迷宫检测大鼠逃避潜伏期时间缩短、穿台次数增多,皮质区存活神经细胞数量增多,5-HT含量明显增多(P＜0.05);上述变化在GSPE大剂量组更为显著(P＜0.05).结论 GSPE可增加5-HT含量,改善间歇性低氧大鼠空间工作记忆能力.     

葛根素对β-淀粉样肽所致痴呆模型小鼠学习记忆的影响

目的 :研究葛根素对 β 淀粉样肽所致痴呆模型小鼠学习记忆障碍的影响。方法 :以 β 淀粉样肽3μl(1mmol·L-1)icv制备小鼠学习记忆障碍模型 ,用Morris水迷宫法检测小鼠学习记忆能力。同时检测脑中及血中超氧化歧化酶 (SOD)、丙二酰醛(MDA)含量。结果 :葛根素 2 5和 5 0mg·kg-1均能改善模型小鼠的学习记忆 (P <0 .0 5或P <0 .0 1)。生化指标测定显示葛根素能使模型小鼠脑及血中的SOD增多、MDA减少 (P <0 .0 5或P <0 .0 1)。结论 :葛根素可对抗 β 淀粉样肽的神经毒性 ,其机制可能与清除脑自由基及提高抗氧化活性作用有关     

大豆异黄酮对高胆固醇血症大鼠血及肝脏MDA含量和SOD活力的影响(英文)

目的 :研究大豆异黄酮对高胆固醇血症大鼠血液及肝脏丙二醛 (MDA )、超氧化物歧化酶(SOD)的影响。方法 :根据血胆固醇水平 ,5 0只雄性Wistar大鼠随机分为 5组 ,正常对照组 (NC)、高胆固醇血症对照组 (HC)和 3个大豆异黄酮治疗组。除正常对照组以外 ,各组均喂以高胆固醇饲料。同时 ,3个治疗组分别灌胃给予 30 ,6 0 ,12 0mg·kg- 1大豆异黄酮 ,对照组给予相应的溶媒 ,持续 9wk。实验结束时 ,分离血清、红细胞 ,取出肝脏 ,制备肝匀浆。采用黄嘌呤氧化酶法测定红细胞和肝匀浆SOD活力 ,以硫代巴比妥酸法测定血清和肝匀浆MDA含量。结果 :与正常对照组比较 ,高胆固醇血症对照组大鼠红细胞及肝匀浆SOD活力明显降低。大豆异黄酮 6 0和 12 0mg·kg- 1组大鼠红细胞及肝脏SOD活力比高胆固醇血症对照组明显升高 (P <0 .0 1和P <0 .0 5 )。高胆固醇血症对照组大鼠血清及肝匀浆MDA含量与正常对照组比较明显升高。与高胆固醇血症对照组比较 ,大豆异黄酮 30和 6 0mg·kg- 1组大鼠血清MDA含量及 30和 12 0mg·kg- 1组大鼠肝脏MDA含量明显降低 (P <0 .0 5 )。结论 :对于高胆固醇血症大鼠红细胞及肝脏SOD活力的降低及血清和肝脏MDA水平的升高 ,能被大豆异黄酮部分逆转     

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.