Synthesis, Antiinflammatory and Antibacterial Activity of Novel Indolyl-isoxazoles

Chalcones were synthesized by reacting indole-3-aldehyde, prepared by Vilsemeir Haack reaction with 4-substituted acetophenone in ethanolic KOH solution. These chalcones were immediately reacted with hydroxylamine hydrochloride in presence of glacial acetic acid as reagent to obtain the corresponding isoxazole derivatives. The synthesized heterocycles were characterized on the basis of physical, chemical tests and spectroscopic data. These compounds were tested for the acute antiinflammatory activity and antibacterial activity using carrageenan-induced rat paw edema method and cup-plate method, respectively.     

Potent Antibacterial Activity of Eugenia umbelliflora.

Abstract

The current work describes the antibacterial activity of the crude extract (CE) and some fractions (dichloromethane and ethyl acetate) of fruits and leaves from Eugenia umbelliflora. Berg. (Myrtaceae) against eight pathogenic bacteria. The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) were determined using the agar dilution method. The results showed that almost all the material tested exhibited excellent activity, comparable to the activity of some typical antibiotics, particularly against the Gram-positive bacteria. In summary, the results obtained with this plant extract may be considered very promising, indicating the potential for obtaining new antiinfectious agents against Gram-positive microorganisms.     

Antibacterial Activity of Medicinal Plants Against Pathogens causing Complicated Urinary Tract Infections

Seventeen Indian folklore medicinal plants were investigated to evaluate antibacterial activity of aqueous, ethanol and acetone extracts against 66 multidrug resistant isolates of major urinary tract pathogens (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Enterococcus faecalis) by disc diffusion method. Ethanol extract of Zingiber officinale and Punica granatum showed strong antibacterial activity against Escherichia coli. Ethanol extracts of Terminalia chebula and Ocimum sanctum exhibited antibacterial activity against Klebsiella pneumoniae. Ethanol extract of Cinnamomum cassia showed maximum antibacterial activity against Pseudomonas aeruginosa while ethanol extract of Azadirachta indica and Ocimum sanctum exhibited antibacterial activity against Enterococcus faecalis. The results support the folkloric use of these plants in the treatment of urinary tract infections by the tribals of Mahakoshal region of central India.     

Antibacterial activity in spices and local medicinal plants against clinical isolates of Karachi,Pakistan

Context: Development of resistance in human pathogens against conventional antibiotic necessitates searching indigenous medicinal plants having antibacterial property. Twenty-seven medicinal plants used actively in folklore, ayurvedic and traditional system of medicine were selected for the evaluation of their antimicrobial activity for this study. Eleven plants chosen from these 27 are used as spices in local cuisine.

Objective: Evaluation of the effectiveness of some medicinal plant extracts against clinical isolates.

Material and methods: Nonedible plant parts were extracted with methanol and evaporated in vacuo to obtain residue. Powdered edible parts were boiled three times and cooled in sterile distilled water for 2?min each and filtrate collected. The minimum inhibitory concentration (MIC) of plant extracts and filtrates/antibiotics was evaluated against clinical isolates by microbroth dilution method.

Results: Water extract of Syzygium aromaticum L. (Myrtaceae) buds, methanol extracts of Ficus carica L. (Moraceae) and Olea europaea L. (Oleaceae) leaves and Peganum harmala L. (Nitrariaceae) seeds had MIC ranges of 31.25–250 µg/ml. S. aromaticum inhibited growth of Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Salmonella enterica serovar Typhi and Pseudomonas aeruginosa. F. carica and O. europaea inhibited growth of S. aureus, S. epidermidis, and S. pyogenes whereas P. harmala was effective against S. aureus, Acinetobacter calcoaceticus and Candida albicans. Ampicillin, velosef, sulfamethoxazole, tetracycline and ceftazidime, cefotaxime, cefepime, which are used as control, had MIC ≥50 and 1.5 µg/ml, respectively, for organisms sensitive to extracts.

Discussion and conclusion: Mono/multiextract from identified plants will provide an array of safe antimicrobial agents to control infections by drug-resistant bacteria.     

肤康洗剂的体外抗菌作用

[目的]研究肤康洗剂的体外抗菌活性。[方法]以炉甘石洗剂为对照品，用2倍稀释法比较肤康洗剂对临床分离的6种细菌的体外抗菌活性。[结果]肤康洗剂对表皮葡萄球菌、乙型溶血性链球菌及其他常见的皮肤病菌株的抗菌活力比炉甘石洗剂更强。[结论]作为医院制剂，肤康洗剂有一定的应用前景。     

补骨脂酊联合窄谱中波紫外线治疗白癜风的疗效观察

目的:观察补骨脂酊联合窄谱中波紫外线(NB-UVB)治疗白癜风的疗效和安全性.方法:将92例白癜风患者随机分为3组,分别给予NB-UVB照射、补骨脂酊外用及补骨脂酊联合NB-UVB治疗;按照色素恢复百分比分级评分进行疗效判定.结果:与NB-UVB照射组或补骨脂酊组比较,补骨脂酊联合NB-UVB组的显效率明显升高(P<0.05);而且补骨脂酊联合NB-UVB组中出现第一个色素岛的所需NB-UVB照射次数和最大照射剂量均明显低于NB-UVB照射组(P<0.05).三组患者均未发生严重不良反应,联合治疗组不良反应发生率低于另两组,但差异无统计学意义(P>0.05).结论:补骨脂酊联合NB-UVB治疗白癜风起效快、不良反应小.     

Antibacterial activity of some Indian medicinal plants

Aqueous extracts of ten medicinal plants were examined for their antibacterial potential against some reference strains of human pathogenic bacteria. Anethum graveolens, Elettaria cardamomum, Foeniculum vulgare, Trachyspermum ammi and Viola odorata were found to be better/equally effective compared to standard antibiotics. V. odorata was the most effective antibacterial with minimum inhibitory concentration values ranging from 1 to 2%. The results provide a scientific basis for the centuries-old usage of aqueous extracts of these medicinal plants.     

含硫三环氟喹诺酮类化合物的合成及其抗菌活性研究

目的：寻找具有更好抗菌活性的含硫三环氟喹诺酮类化合物。方法：在芦氟沙星母核的10位引入不同基团，设计并合成8个含硫三环氟喹诺酮类化合物，并测定其体外抗菌活性。结果：合成了目标化合物，其结构经IR、^1HNMR、MS和元素分析确证；它们具有不同强度的抗菌活性，其中几个化合物的抗菌活性优于芦氟沙星。结论：初步的体外抗菌实验证实所合成目标化合物具明显的抗菌活性，甚至优于芦氟沙星。     

消炎止痛栓体外抗菌活性研究

目的:研究消炎止痛栓(主要成分为盐酸小檗碱、冰片、土霉素、盐酸丁卡因)的体外抗菌活性。方法:运用试管稀释法测定并分析消炎止痛栓在体外对标准菌株金黄色葡萄球菌、大肠埃希菌、铜绿假单胞菌的最低抑菌浓度(MIC)和最低杀菌浓度(MBC)。结果:消炎止痛栓对上述3种标准菌株的MIC分别为0.195、0.0488、0.0975mg.mL-1,MBC分别为0.390、0.0975、0.390mg.mL-1。结论:消炎止痛栓在体外对上述3种标准菌株具有良好的抗菌活性。     

Antioxidant Activity of 13 Medicinal Plants

The aqueous extracts of 13 medicinal plants widely used in oriental medicine were examined for their reducing power, scavenging ability toward superoxide and hydroxyl radicals, and their inhibitory effect on lipid peroxidation. The reducing power of Herba Lycopi and Cortex Gleditsiae was more apparent than with other plants. All extracts tested were found to be highly active on scavenging of superoxide radicals. Among them, Fructus Crataegi, Herba Leonuri, Cortex Gleditsiae, and Herba Lycopi composed the highly active group. Although the overall level of hydroxyl radical scavenging activities tended to be lower than those for super-oxide radicals, Fructus Crataegi and Cortex Gleditsiae were found to act most effectively. Inhibitory effects on lipid peroxidation were examined using a rabbit erythrocyte-ghost system, and a high inhibition was obtained by Rhizoma Rhei, Fructus Crataegi, and Cortex Gleditsiae. Reversely, strong pro-oxidant activity was found in five medicinal plants including Semen Thujae Orientalis in this assay system.     

Antibacterial Activity of some Medicinal Mangroves against Antibiotic Resistant Pathogenic Bacteria

The antibacterial activity of the leaves and bark of mangrove plants, Avicennia marina, A. officinalis, Bruguiera sexangula, Exoecaria agallocha, Lumnitzera racemosa, and Rhizophora apiculata was evaluated against antibiotic resistant pathogenic bacteria, Staphylococcus aureus and Proteus sp. Soxhlet extracts of petroleum ether, ethyl acetate, ethanol and water were prepared and evaluated the antibacterial activity using agar diffusion method. Most of the plant extracts showed promising antibacterial activity against both bacterial species. However, higher antibacterial activity was observed for Staphylococcus aureus than Proteus sp. The highest antibacterial activity was shown by ethyl acetate of mature leaf extracts of E. agallocha for Staphylococcus aureus. All ethyl acetate extracts showed higher inhibition against S. aureus while some extracts of chloroform, ethyl acetate and ethanol gave inhibition against Proteus sp. None of the petroleum ether and aqueous extracts showed inhibition against Proteus sp. All fresh plant materials did also show more antibacterial activity against both bacterial strains than did dried plant extracts. Antibacterial activity of fresh and dried plant materials reduced for both bacterial strains with time after extraction. Since L. racemosa and A. marina gave the best inhibition for bacterial species, they were used for further investigations. Charcoal treated plant extracts of L. racemosa and A. marina were able to inhibit both bacterial strains more than those of untreated plant extracts. Phytochemical screening of mature leaf, bark of L. racemosa and leaf extracts of A. marina has been carried out and revealed that leaf and bark contained alkaloids, steroids, triterpenoids and flavonoids. None of the above extracts indicate the presence of saponins and cardiac glycosides. Separated bands of extracts by TLC analysis showed antibacterial activity against S. aureus.     

Screening of Iranian Plants for Antimicrobial Activity

The methanol extracts of 306 plants of 52 families obtained from Northeast of Iran (Khorasan Province), were tested for antimicrobial activity (in vitro) using the cylinder plate assay method. Activity against Escherichia coli, Klebsiella pneumoniae, Salmonella typhi, Pseudomonas aeruginosa, Morganella morganii (Gram negative), Bacillus subtilis and Staphylococcus aureus (Gram positive) and Candida albicans is discussed.     

培氟沙星与锌配合物的制备与抗菌活性测定

目的 制备培氟沙星与锌配合物,并观察其抗菌活性. 方法 氯化锌0.136 3 g和培氟沙星0.666 0 g化学反应制备配合物.对配合物进行元素分析和红外光谱分析,并进行体外抗菌活性测定. 结果 配合物各元素的组成比例为：锌(Zn) 13.16%,碳(C) 41.05%, 氢(H)4.02%, 氮(N)8.43%, 氯(Cl) 7.15%, 水(H2O )12.50%. 由元素分析可推知配合物的分子式为Zn₂(C₁₇H₂0FN₃O₃)₂Cl₂(H₂O)₇.培氟沙星在1 713 cm^-1处出现的羧基上C=O伸缩振动吸收峰,在配合物中消失,而在1 572.1,1 343.7 cm^-1则出现了对应于羧基的不对称和对称伸缩振动吸收峰,培氟沙星在1 634 cm^-1出现的萘啶环上羰基(C=O)伸缩振动吸收峰,在配合物中则红移了13个波数至1 621.2 cm^-1.培氟沙星对流感嗜血杆菌和粪链球菌的最低抑菌浓度分别为1.25和2.5 mg&#8226;mL^-1,配合物对流感嗜血杆菌、粪链球菌最低抑菌浓度分别为0.62和1.25 mg&#8226;mL^-1. 结论 该配合物制备方法简单,体外抗菌活性 结果表明, 培氟沙星与锌配合物对流感嗜血杆菌、粪链球菌的抑制作用略高于培氟沙星.     

注射用盐酸头孢唑兰与3种常用抗菌药物体外抗菌活性比较

目的：本研究旨在评价头孢唑兰对临床分离菌株的体外抗菌作用,为头孢唑兰的临床使用提供参考依据。方法：采用琼脂双倍稀释法测定头孢唑兰对14类127株呼吸系统和泌尿系统感染分离出的病原菌株的体外抗菌活性,并与已经上市的3种常用抗菌药物进行了体外抗菌活性比较,试验平行3次,观察结果。结果：头孢唑兰对7种临床分离G＋菌株包括金黄色葡萄球菌、化脓性链球菌、肺炎链球菌、无乳链球菌、甲氧西林敏感表皮葡萄球菌（MSSE）、甲氧西林敏感金黄色葡萄球菌（MSSA）的MIC50均在0.125-1μg·ml^-1之间,MIC90在0.5-8μg·ml^-1之间;对肺炎克雷伯菌、大肠埃希菌、奇异变形杆菌、流感嗜血杆菌、产气肠杆菌、铜绿假单胞菌、阴沟肠杆菌的MIC均值分别为0.23,0.21,0.42,4.74,6.31,8.75,16.35μg·ml^-1。结论：头孢唑兰对14类127株呼吸系统和泌尿系统感染菌株的体外抗菌活性明显,具有显著的体外抗菌活性。     

Antibacterial activity of some medicinal plant extracts

Antibacterial activity of hot aqueous and methanolic extracts prepared from six plants (Terminallia chebula, Terminallia bellerica, Phyllanthus emblica, Punica granatum, Lawsonia alba and Mikania micrantha) used in traditional folk medicines of India were screened against five pathogenic bacteria (Staphylococcus aureus MTCC 2940, Bacillus subtilis MTCC 441, Escherichia coli MTCC 739, Proteus vulgaris MTCC 426 and Enterobacter aerogenes MTCC 111). The highest antibacterial potentiality was exhibited by the methanolic leaf extract of T. chebula, followed by the aqueous fruit extract of T. bellerica. The leaf extract of T. chebula can be considered to be as equally potent as the most effective antibiotics, such as ciprofloxacin, gentamycin, kanamycin, ofloxacin and cephalexin. A sensitivity test performed with commonly used sensitivity test disks resulted in the appearance of multiple drug resistance phenotypes of the bacteria tested. A comparision of data in the inhibition zones of pathogenic bacteria showed that gentamycin, ofloxacin, kanamycin and tobramycin were effective against all of the bacterial strains tested.     

国产与进口替考拉宁对224株肠球菌的体外抑菌活性比较研究

目的:研究国产替考拉宁对224株肠球菌的体外抑菌活性。方法:采用琼脂稀释法测定国产替考拉宁对169株粪肠球菌和51株屎肠球菌等的最低抑菌浓度(MIC) ,并与进口替考拉宁及其它抗生素进行抑菌效果比较。结果:国产替考拉宁对169株粪肠球菌和51株屎肠球菌的MIC50 分别为0. 125、0 .25μg/ml,MIC90 分别为2、1μg/ml;进口替考拉宁对粪肠球菌和屎肠球菌的MIC50分别为0 .25、0. 25μg/ml,MIC90 分别为1、0 .5μg/ml。结论:两种替考拉宁对224株肠球菌均具有较强的抑菌活性;224株肠球菌对两种替考拉宁的敏感率均为100 %。     

GC法测定痛肿灵酊中樟脑、薄荷脑、异龙脑、龙脑的含量

目的:建立气相色谱法测定痛肿灵酊中樟脑、薄荷脑、异龙脑、龙脑含量的方法.方法:色谱柱:Phenomenex ZB-WAX 石英毛细管柱(30 m×0.32 mm,0.25μm),火焰离子化检测器温度:280℃,进样口温度:250℃,柱温:130℃.结果:樟脑在0.110～5.492 μg范围内线性关系良好(r=0.999 5),平均回收率为99.04％,RSD=0.28％(n=9);薄荷脑在0.120 ～6.024 μg范围内线性关系良好(r =0.9996),平均回收率为99.16％,RSD =0.50％ (n =9);异龙脑在0.028 ～1.402 μg范围内线性关系良好(r =0.9991),平均回收率为99.03％,RSD =0.40％ (n =9),龙脑在0.034 ～ 1.700 μg范围内线性关系良好(r=0.9998),平均回收率为99.27％,RSD =0.41％ (n =9).阴性样品无干扰.结论:该法操作简便,结果准确可靠,可作为痛肿灵酊的质量控制方法.     

重组小鼠β-防御素2的纯化及其对非分型流感嗜血杆菌抗菌活性的测定

目的：运用基因工程方法获得重组小鼠β-防御素2(mouse Beta Defensin 2, mBD2),体外实验观察mBD2对非分型流感嗜血杆菌( Non-typeable Haemophilus influenzae, NTHi)的抑菌活性,初步探讨mBD2的杀菌机制。方法①对工程菌Rosetta-gami(2)-pET32a(+)/mBD2进行诱导培养,采用亲和层析法对目的蛋白进行纯化,SDS-PAGE分析重组mBD2的分子量大小及表达情况。②在不同浓度的重组mBD2和不同浓度的NaCl条件下,不同作用时间内,观察重组mBD2对NTHi的体外抗菌活性;并用二硫苏糖醇处理重组mBD2,观察构象改变对重组mBD2抗菌活性的影响。③体外建立NTHi黏附A549细胞模型,镜下观察细菌黏附情况;菌落稀释培养法观察重组mBD2对NTHi黏附A549细胞的抑制;电子显微镜进一步观察重组mBD2引起的NTHi细胞损伤。结果①SDS-PAGE 分析表明,重组菌Rosetta-gami(2)-pET32a(+)/mBD2在分子量约4 kD处均有一条明显的表达带,与理论重组蛋白的分子量大小相符;经过酶切及纯化,每升工程菌培养物可获得约7.5 mg/L、具有较高纯度的mBD2成熟肽。②体外抗菌实验研究表明,纯化的重组mBD2体外具有明显的抗NTHi活性,培养120 min后,其最小抑菌浓度( MIC)值为40μg/ml,最小杀菌浓度( MBC)值为160μg/ml。外环境NaCl浓度的增高及重组蛋白二硫键的破坏会抑制其抗菌活性。③成功建立了体外NTHi黏附A549细胞模型,镜下观察到NTHi能明显黏附于A549细胞表面;40μg/ml的重组mBD2与NTHi、A549细胞共同孵育2 h,NTHi的细胞黏附率显著降低,下降至2.3%;电镜下观察到,与40μg/mL重组mBD2共同孵育120 min后,NTHi菌细胞的细胞膜变得不完整,出现孔隙,有少量内容物逸出。结论重组mBD2对NTHi具有杀菌作用,其杀菌活性除受本身的浓度和构象(二硫键)影响外,还受杀菌时间、外环境中无机盐浓度的影响,主要抗菌机制是通过损伤细菌细胞膜使细胞内容物外漏而最终杀灭细菌。     

鞣质类化合物的抑菌机制研究进展

摘 要近年来由于抗菌药物滥用,越来越多的微生物基因型产生耐药性。鞣质类化合物因其良好的抗菌活性、不良反应小、来源广泛等优势,已经成为细菌性疾病治疗领域新的研究热点。本文现从鳌合金属离子、抑制酶活力、膜壁损伤、蛋白质和核酸变化、能量代谢以及增强机体免疫力等方面,对鞣质的抑菌机制作出较为完善的总结,旨在为开发鞣质作为有效抗菌药物提供理论参照。