七叶莲不同溶剂提取部分的抗炎镇痛作用

目的探讨七叶莲不同溶剂提取部分的抗炎镇痛作用。方法采用醋酸扭体法、小鼠耳二甲苯致炎法、肿胀法等方法评价七叶莲不同提取部分的抗炎镇痛效果,并明确其抗炎镇痛有效部分。结果七叶莲叶挥发油可明显减少小鼠醋酸所致的扭体次数,可明显缓解小鼠二甲苯所致的耳廓肿胀;七叶莲茎水提液氯仿部分、正丁醇部分也可减少小鼠醋酸所致扭体次数,有效缓解小鼠二甲苯所致的耳廓肿胀和角叉菜胶所致的足趾肿胀。结论七叶莲抗炎镇痛药理作用的有效部分主要集中在叶挥发油部分、茎水提液的氯仿部分和正丁醇部分。     

镰形棘豆经皮给药后抗炎镇痛活性有效部位的筛选

目的镰形棘豆经皮给药后,筛选其最佳抗炎镇痛有效组分。方法分离提取镰型棘豆的生物碱、总黄酮、挥发油部位,并进行组合,利用二甲苯诱导的小鼠耳肿胀法、热板法和醋酸扭体法筛选镰形棘豆不同有效部位镇痛抗炎活性的最佳组分。结果镰形棘豆总黄酮与挥发油有效部位组合物有更好的抗炎镇痛活性,其经皮给药后对小鼠耳肿胀的抑制率为90.22%;热板法实验中的镇痛率达87.85%;醋酸扭体法实验中镇痛率达73.23%,与阳性药效果相当。结论镰形棘豆总黄酮与挥发油组合物通过经皮给药方式有良好的抗炎镇痛活性。     

新工艺温通膏主要药效学研究

目的 研究新工艺温通膏镇痛、抗炎消肿、祛瘀作用。方法 采用醋酸扭体法及甲醛致小鼠足痛观察新工艺温通膏低、中、高剂量及原工艺温通膏的镇痛作用;以二甲苯致小鼠耳廓肿胀及角叉菜胶致大鼠足趾肿胀试验,探讨新工艺温通膏低、中、高剂量及原工艺温通膏的抗炎消肿作用;通过建立瘀斑豚鼠模型观察新工艺温通膏低、中、高剂量及原工艺温通膏的祛瘀作用。结果 原工艺温通膏及新工艺温通膏低、中剂量均能显著减少醋酸致小鼠扭体反应次数;新工艺温通膏低、中、高剂量均可明显减轻二甲苯致小鼠耳廓肿胀的肿胀度及肿胀率;新工艺温通膏低剂量可以明显促进豚鼠瘀斑面积消退。结论 新工艺温通膏具有良好的镇痛、抗炎消肿、祛瘀的作用。     

金丝桃苷对急性炎症疼痛模型小鼠的抗炎镇痛作用研究

目的 研究金丝桃苷（Hyp）对急性炎症疼痛模型小鼠的抗炎镇痛作用。方法 昆明种小鼠随机分为对照组,Hyp低、中、高剂量（50、100、200 mg/kg）组及氢化可的松（阳性药,20 mg/kg）组,sc给药,每天给药1次,连续给药5 d后,建立二甲苯所致小鼠耳廓肿胀和醋酸所致小鼠腹腔毛细血管通透性增高的急性炎症模型,观察Hyp对小鼠急性炎症的抗炎作用;阳性药设置为吗啡（1 mg/kg）,其余分组及给药方式同急性炎症实验,连续给药5 d后,建立小鼠醋酸扭体法和热甩尾法模型,观察Hyp对急性疼痛的镇痛作用。结果 100、200 mg/kg的Hyp能够抑制二甲苯所致小鼠耳廓肿胀、降低急性炎症引起的毛细血管通透性增高、减少醋酸扭体次数、提高小鼠热刺激痛阈值,与对照组比较差异显著（P<0.05、0.01）。结论 Hyp对小鼠急性炎症疼痛具有抑制作用。     

黔产毛蒟挥发油抗炎镇痛活性研究

摘 要 目的：探讨黔产毛蒟挥发油的抗炎镇痛活性。方法: 将50只昆明种小鼠随机分为5组,每组10只,分别为模型组（生理盐水）、黔产毛蒟挥发油低（0.125 ml/100 ml）、中（0.25 ml/100 ml）、高浓度组（0.5 ml/100 ml）和阿司匹林组（3 mg·mL^-1）。观察二甲苯致小鼠耳廓肿胀和皮肤毛细血管通透性的影响,以评价黔产毛蒟挥发油的抗炎作用;对醋酸致小鼠疼痛和热刺激致痛的影响,以评价黔产毛蒟挥发油的镇痛作用。结果: 与模型组比较,挥发油中、高浓度组、阿司匹林组的耳肿胀度明显降低,差异具有统计学意义（P＜0.05）;挥发油高浓度组和阿司匹林组能有效降低毛细血管通透性,差异有统计学意义（P＜0.05或P＜0.01）。与模型组比较,挥发油中、高浓度组、阿司匹林组能有效抑制小鼠扭体次数,差异具有统计学意义（P＜0.05或P＜0.01）,同时挥发油高浓度组能有效减缓小鼠痛阈值（P＜0.05或P＜0.01）。结论:黔产毛蒟挥发油具有较好的抗炎镇痛活性。     

右旋布洛芬凝胶的抗炎镇痛作用

目的 考察右旋布洛芬凝胶的抗炎、镇痛作用。方法 以角叉菜胶致大鼠足跖肿胀、二甲苯致小鼠耳廓肿胀、大鼠辐射热刺激及小鼠醋酸扭体法，观察右旋布洛芬凝胶的局部抗炎、镇痛作用。结果 2.5%、4.0%右旋布洛芬凝胶局部涂药能显著抑制角叉菜胶所致大鼠足跖肿胀及二甲苯所致小鼠耳廓肿胀，并能明显提高大鼠对光热刺激的痛阈，减少小鼠醋酸刺激的扭体次数。结论 2.5%右旋布洛芬凝胶局部外用具有显著的抗炎、镇痛活性。     

梅花鹿鹿角托盘提取物的抗炎镇痛作用

目的:探讨梅花鹿鹿角托盘提取物的抗炎镇痛作用。方法:通过小鼠足肿胀、耳郭肿胀的实验研究梅花鹿鹿角托盘提取物的抗炎作用;采用热板法和醋酸扭体法研究梅花鹿鹿角托盘提取物的镇痛作用。结果:梅花鹿鹿角托盘提取物腹腔注射给药能有效地抑制角叉菜胶引起的足肿胀和二甲苯引起的小鼠耳郭肿胀;显著提高热板实验小鼠的痛阈,并能抑制醋酸引起的小鼠扭体反应次数,延长疼痛潜伏期。结论:梅花鹿鹿角托盘提取物腹腔注射给药具有抗炎镇痛作用。     

维药神香草挥发油的抗炎、止咳、祛痰及镇痛药效学研究

摘 要 目的：探讨维药神香草挥发油的抗炎、止咳、祛痰及镇痛作用。方法: 昆明种小鼠 50 只,随机分成神香草挥发油高 (0.8 ml·kg^-1)、中 (0.4ml·kg^-1)、低(0.2 ml·kg^-1)剂量组、空白对照组(0.9% 生理盐水)、阳性对照组(急支糖浆5.0 ml·kg^-1/阿司匹林200 mg·kg^-1),共5 组,每组10 只。采用小鼠二甲苯致炎法观察耳肿胀度和抑制率,氨水致咳法观察2 min内咳嗽次数及咳嗽潜伏期,气管酚红排泌法测定气管酚红排泄量,热刺痛法观察小鼠痛阈值。结果: 神香草挥发油在（0.2～0.8) ml·kg^-1范围内可明显降低二甲苯致小鼠的耳廓肿胀度(P<0.05或P<0.01),其最大肿胀抑制率为80.52%;神香草挥发油高剂量组减少氨水喷雾致小鼠咳嗽次数、延长咳嗽潜伏期(P<0.05),增加小鼠气管段酚红排泌量(P<0.05),明显延长小鼠镇痛潜伏期 (P<0.05)。结论: 维药神香草挥发油具有显著的抗炎、止咳、祛痰和镇痛作用。     

石韦不同提取物的抗炎镇痛作用考察

目的：探讨石韦不同溶剂提取物的抗炎镇痛作用。方法：制备石韦水提取物和75%乙醇提取物,采用二甲苯致小鼠耳廓肿胀法观察其抗炎作用,采用醋酸扭体法和热板法观察其镇痛作用。结果：石韦醇提取物能明显抑制二甲苯所致小鼠耳廓肿胀（P〈0.01）,且具有抑制醋酸致小鼠扭体的作用（P〈0.05）,在给药后1 h、2 h均能提高热板法小鼠的痛阈值（P〈0.05）;石韦水提取物能抑制二甲苯所致小鼠耳廓肿胀和醋酸所致小鼠扭体的作用（P〈0.05）,在给药后1 h能提高热板法小鼠的痛阈值（P〈0.05）。结论：石韦具有一定的抗炎镇痛作用。     

蓖麻子不同炮制品抗炎镇痛作用比较

目的:研究蓖麻子不同炮制品的抗炎镇痛作用。方法:以两种不同方法炮制的蓖麻子,应用醋酸致小鼠扭体法、小鼠热板法、二甲苯致小鼠耳肿胀法和大鼠蛋清足跖肿胀法分别研究其抗炎镇痛作用。结果:两种方法炮制的蓖麻子均可减少醋酸致小鼠扭体次数、延长小鼠舔足时间、减轻二甲苯致小鼠耳郭肿胀程度、减小蛋清致足跖肿胀程度,与正常对照组比较均有显著性差异;炒蓖麻子抗炎镇痛作用强于以鸡蛋为辅料加热炮制的蓖麻子作用效果。结论:中药蓖麻子炮制品均具有明显的抗炎镇痛作用,其中炒蓖麻子抗炎镇痛作用较好。     

Genetic regulation of the ramA locus and its expression in clinical isolates of Klebsiella pneumoniae

Tigecycline resistance has been attributed to ramA overexpression and subsequent acrA upregulation. The ramA locus, originally identified in Klebsiella pneumoniae, has homologues in Enterobacter and Salmonella spp. In this study, we identify in silico that the ramR binding site is also present in Citrobacter spp. and that Enterobacter, Citrobacter and Klebsiella spp. share key regulatory elements in the control of the romA-ramA locus. RACE (rapid amplification of cDNA ends) mapping indicated that there are two promoters from which romA-ramA expression can be regulated in K. pneumoniae. Correspondingly, electrophoretic binding studies clearly showed that purified RamA and RamR proteins bind to both of these promoters. Hence, there appear to be two RamR binding sites within the Klebsiella romA-ramA locus. Like MarA, RamA binds the promoter region, implying that it might be subject to autoregulation. We have identified changes within ramR in geographically distinct clinical isolates of K. pneumoniae. Intriguingly, levels of romA and ramA expression were not uniformly affected by changes within the ramR gene, thereby supporting the dual promoter finding. Furthermore, a subset of strains sustained no changes within the ramR gene but which still overexpressed the romA-ramA genes, strongly suggesting that a secondary regulator may control ramA expression.     

In vitro Studies of Antimicrobial Activity of Crude Extracts of the Indian Grasses Dhaman (Cenchrus ciliaris) and Kala-Dhaman (Cenchrus setigerus)

The aim of present study was to investigate the antimicrobial activity of Cenchrus ciliaris and Cenchrus setigerus extracts in order to use it as a possible source for new antimicrobial substances against important human pathogens. Crude extracts of the stem of Cenchrus ciliaris and Cenchrus setigerus were evaluated against some medically important pathogens viz. Escherichia coli, Raoultella planticola, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis, Enterobacter aerogenes, Candida albicans and Aspergillus flavus. The dried and powdered stems were successively extracted with hexane, toluene, isopropyl alcohol, acetone and ethanol using soxhlet assembly. The antimicrobial activity assay was done by both disc diffusion and serial dilution methods. Isopropyl alcohol extract of Cenchrus setigerus showed highest activity against Escherichia coli. The test pathogens were more sensitive to the isopropyl alcohol, acetone and ethanol extracts than to the hexane and toluene extracts except against Bacillus subtilis. Result reveals that the most bioactive compound was cycloleucolenol-9,19-cycloergost-24 (28)-en-3-ol, 4, 14-dimethyl acetate in both the species of Cenchrus grass, (19.15%) in isopropanol extract of Cenchrus setigerus whereas, (14.03%) in acetone extract of Cenchrus ciliaris.     

Toxicity assessment of crude and partially purified extracts of marine Synechocystis and Synechococcus cyanobacterial strains in marine invertebrates

Among the Cyanoprokaryota, the genera Synechocystis and Synechococcus have rarely been studied with respect to potential toxicity. This is particularly true with marine environments where studies about the toxicity of cyanobacteria are restricted to filamentous forms at the warmer temperate and tropical regions and also to filamentous forms at cold seas such as the Baltic Sea. In this study, we describe the effects of cyanobacterial strains of the Synechocystis and Synechococcus genera isolated from the marine coast of Portugal, on marine invertebrates. Crude and partially purified extracts at a concentration of 100 mg/ml of freeze-dried material of the marine strains were tested for acute toxicity in nauplii of the brine shrimp Artemia salina, in the rotifer Brachionus plicatillis and in embryos of the sea urchin Paracentrotus lividus and the mussel Mytilus galloprovincialis. The cyanobacterial extracts, especially the crude extract, had an impact on A. salina nauplii. No significant toxic effects were registered against the rotifer. A negative impact of all strains was recorded on the embryonic development of the sea urchin, with toxic effects resulting in an inhibition of embryogenesis or development of smaller larvae. To the mussel embryos, the effects of cyanobacterial extracts resulted in a complete inhibition of embryogenesis. The results of all assays indicate that Synechocystis and Synechococcus marine strains contained toxic compounds to marine invertebrates.     

Structure-Based Design of Substituted Piperidines as a New Class of Highly Efficacious Oral Direct Renin Inhibitors

相似文献   

Toxic activities of Brazilian centipede venoms

Centipedes have a venom gland connected to a pair of forceps, which are used to arrest preys. Human victims bitten by centipedes usually manifest burning pain, paresthesia and edema, which may develop into superficial necrosis. The aim of this work was to characterize and compare toxic activities found in venoms of three species of Brazilian centipedes-Otostigmus pradoi, Cryptops iheringi and Scolopendra viridicornis. By SDS-PAGE (4-20%), important differences were noticed among venoms (between 7 and 205kDa). Few bands showed feeble caseinolytic, fibrinogenolytic and gelatinolytic activities by zymography, but strong hyaluronidase activity was observed in S. viridicornis and O. pradoi venoms. In addition, such activities could be inhibited by o-phenanthroline, indicating that these enzymes are metalloproteinases. All venoms induced nociception, edema and myotoxicity in mice, but only S. viridicornis induced mild hemorrhagic activity. No coagulant activity was detected in centipede venoms. Low phospholipase A(2) activity was observed exclusively in S. viridicornis and O. pradoi venoms, but these venoms had intense direct hemolytic activity on human erythrocytes. Cross-reactivity among venoms was observed using species-specific sera raised in rabbits. Differences were noticed among centipede venoms, but S. viridicornis is indeed the most toxic venom and thereby it could induce a more severe envenomation.     

Role of matrikins in melanoma progression

Expression of melanoma invasiveness, ultimately leading to the formation of metastases, requires that cancer cells break through the successive skin barriers (dermo-epidermal junction, dermis) constituted of various extracellular matrix constituents. In order to facilitate their progression, melanoma cells express, in concert with stromal cells, a group of proteolytic systems which degrade this extracellular structures. However, proteolysis of basement membrane, collagen or elastic fibers can uncover cryptic sites or/and liberate matrix fragments whose properties appeared distinct from their intact macromolecule counterparts. Those fragments, called matrikines, are able to empede or to accelerate melanoma progression ex vivo and in vivo. Non-collagenous domains of basement membrane collagens, which behave like potent "matstatins", are seen as potential pharmacological agents in melanoma.     

Effect of Plant Extracts Formulated in Different Ointment Bases on MDR Strains

Extracts of Aloe vera whole plant, Eucalyptus globulus leaves, Ficus infectoria bark, Ficus religiosa bark and Piper betel leaves were studied for antibacterial activity on resistant and sensitive strains, isolated from skin and soft tissue infections. A combination of hot alcoholic extracts of Ficus infectoria, Ficus religiosa and Piper betel were found to be more effective against all the isolates. The combined extract was formulated in different ointment bases such as polyethylene glycol, gelatin, sodium alginate, carbopol, cream base and honey. These were then evaluated to find a suitable base for preparation of an ointment. In vitro study of the release of antimicrobials and kill-time studies of the herbal ointments was carried out against multi-drug resistant isolate of Pseudomonas. The ointment showed bactericidal activity within 2 h against the resistant strain of Pseudomonas spp.     

Hormetic Responses of Lonicera Japonica Thunb. To Cadmium Stress

The hormetic responses of Lonicera japonica Thunb. to cadmium (Cd) stress were investigated in a hydroponic experiment. The present results showed that root length and total biomass dry weight increased in comparison with the control at low concentrations Cd. The height of the plant exposed to 2.5 and 5 mg L^-1 Cd increased significantly by 11.9% and 12.8% relative to the control, and with the increase of Cd concentrations in the medium, plant height began to decrease. The responses of photosynthetic pigments contents and relative water content to Cd stress had a similar trend, which all showed significantly an inverted U-shaped dose–response curve and confirmed that the stimulatory effect of low concentrations Cd occurred in the plant. Furthermore, L. japonica, as a new Cd-hyperaccumulator, could be considered as a new plant model to study the underlying mechanisms of the hormesis.     

Morphological characterization of the venom secretory epidermal cells in the stinger of marine and freshwater stingrays.

Marine and freshwater stingrays are characterized by the presence of one to three mineralized serrated stingers on the tail, which are covered by epidermal cells secreting venom. When these animals are dorsally touched, the stinger can be introduced into the aggressor by a whip reflex mechanism of the tail, causing severe mechanical injuries and inoculating the venom. Accidents in humans are frequent causing intense local pain, oedema and erythema. Bacterial secondary infection is also common. In addition, injuries involving freshwater stingrays frequently cause a persistent cutaneous necrosis. The exact localization of the venom secretory epidermal cells in the stinger is controversial, but it is known that it is preferentially located in the ventrolateral grooves. A comparative morphological analysis of the stinger epidermal tissue of different marine and freshwater Brazilian stingray species was carried out. The results indicate that in freshwater species there is a larger number of protein secretory cells, of two different types, spread over the whole stinger epidermis, while in marine species the protein secretory cells are located only around or inside the stinger ventrolateral grooves. These differences between the stingers of the two groups can justify the more severe envenomation accidents with the freshwater species when compared with the marine species.     

Pharmacognostic and antifungal investigations of Elaeocarpus ganitrus (Rudrakasha)

Rudrakasha is the dried bead obtained from the ripe fruit of Elaeocarpus ganitrus Roxb. (Family: Elaeocarpaceae). Microscopic studies revealed the presence of a hard endocarp with lignified isodiametric sclereids, seeds with membranous seed coat, which enclosed a dense cellular endosperm comprising of calcium oxalate druses. Physicochemical parameters showed that total ash was 1.36 times and 1.56 times more than the acid insoluble ash and water-soluble ash, respectively. Further, ethanol had a maximum extractable value of 2.4% and moisture content was found to be 9.7%. Different extracts, petroleum ether, chloroform, ethanol and water were prepared. Chemically the extracts showed the presence of phytosterols, fats, alkaloids, flavonoids, carbohydrates, proteins and tannins. The extracts were evaluated for antifungal activity on different fungal strains. Chlorofom and ethanol extracts have high antifungal activity against Candida albicans. Whereas, chloroform, ethanol and water extracts showed moderate inhibition against Aspergillus niger.