日光灯光响应混晶纳米TiO2乳液的制备及抗菌性能

以四氯化钛、氨水、表面活性剂为主要原料,采用常压液相两步水解法制备了晶型比例可控的混晶纳米TiO2粉末及高分散乳液。对样品形貌、组成及结构进行了表征。结果表明,混晶乳液分散性好,粒径约15 nm;在普通日光灯照射下,乳液对一些细菌和真菌有很好的抗菌性能:对革兰氏阳性菌(金黄葡萄球菌和枯草芽孢杆菌)的杀灭率达到100%,对革兰氏阴性菌(大肠杆菌)也有很好的杀灭性能,对黑曲霉、黄曲霉和白色念珠菌等真菌产生清晰的抑菌圈,抑菌直径约20 mm。     

噻唑类不对称双缩二氨基硫脲的合成及其抗菌活性研究（英文）

噻唑-5-甲醛与氨基硫脲缩合反应,高产率的合成了14个未见文献报道的新型双缩二氨基硫脲类化合物,其结构经光谱和元素分析所表征。分别进行其对金黄色葡萄球菌、大肠杆菌、枯草芽孢杆菌、绿脓杆菌的抗菌活性测试。初步结果表明化合物3d,3f,3h对绿脓杆菌和金黄色葡萄球菌有很好的抑菌效果。     

新型脱氧胆酸1,2,4-三唑席夫碱类化合物的微波合成及其抗菌活性研究（英文）

利用微波辐射技术合成了16个未见文献报道的新型含1,2,4-三唑希夫碱结构的脱氧胆酸化合物,该方法具有反应时间短、产率高等优点;其结构经光谱和元素分析所确证。分别进行其对金黄色葡萄球菌、枯草芽孢杆菌、绿脓杆菌和大肠杆菌的抗菌活性测试。初步结果表明部分化合物对绿脓杆菌和金黄色葡萄球菌有很好的抑菌效果。其中化合物8d具有潜在的药物应用前景。     

5′位羟基异戊烯基查尔酮类天然产物的合成及其抗菌活性研究

首次合成了Bartericin A (1), 2’,6’-二羟基-5’-(2’’-羟基-3’’-甲基-3’’-丁烯基)-4’-甲氧基查尔酮(2), Xanthohumol D (3)和Angusticornin B (4) 4个羟基异戊烯基查尔酮类天然产物.为了探讨天然产物中不同官能团对其核心骨架结构抗菌活性的影响,设计合成了衍生物6.所合成的目标产物和未知中间体化合物经过1H NMR、13C NMR、IR、HRMS进行了确证.选取大肠杆菌[CMCC(B)44102]、绿脓杆菌[CMCC(B)10104]、金黄色葡萄球菌[CMCC(B)260003]和枯草芽孢杆菌[CMCC(B)63 501],采用稀释点样法对所合成的4个天然产物及1个新型衍生物进行了抗菌活性评估.结果显示,天然产物1、4和衍生物6对革兰氏阳性菌金黄色葡萄球菌和枯草芽孢杆菌表现出了一定的抑制活性.天然产物3对枯草芽孢杆菌表现出了较为明显的抑制活性,但对其他3种菌株无抑制活性(最小抑菌浓度>200μg/mL).     

新型鹅去氧胆酸衍生物的合成及其抗菌活性

以提取胆红素后的猪胆膏余料中分离提纯的鹅去氧胆酸为原料，经酯化反应合成了6种新型的鹅去氧胆酸衍生物（3a～3f)，其结构经¹H NMR, ¹³C NMR, IR, MS(ESI)和元素分析表征。采用滤纸片法测试了3a~3f对铜绿假单胞杆菌、大肠杆菌、枯草芽孢杆菌和金黄色葡萄球菌的抑菌活性。结果表明：用药量为2 mg·mL^-1时，3a对铜绿假单胞杆菌（d=15.3 mm），大肠杆菌（d=18.6 mm），枯草芽孢杆菌（d=11.2 mm），金黄色葡萄球菌（d=12.2 mm）有抑制作用，3b对铜绿假单胞杆菌（d=8.0 mm），金黄色葡萄球菌（d=10.6 mm）有抑制作用，3c对铜绿假单胞杆菌（d=10.4 mm），大肠杆菌（d=12.6 mm），枯草芽孢杆菌（d=9.7 mm），金黄色葡萄球菌（d=15.3 mm）有抑制作用，3d对大肠杆菌（d=9.5 mm），枯草芽孢杆菌（d=8.5 mm）有抑制作用，3e对枯草芽孢杆菌（d=9.3 mm）有抑制作用。     

Cu0.05Zn0.95O/聚吡咯纳米复合物的制备和抗菌性能

在CTAB/正己烷/正丁醇/水（W/O）四元反相微乳液体系中原位聚合制备了铜掺杂氧化锌/聚吡咯（CZ/PPy）纳米复合物.用X射线衍射仪、扫描电子显微镜、透射电子显微镜、红外光谱仪和紫外-可见光谱仪分别表征了样品的结构、形貌和光谱学性能;以大肠杆菌（Escherichia coli）、金黄色葡萄球菌（Staphylococcus aureus）和白色念珠菌（Candida albicans）为测试菌株研究了样品的抗菌活性.结果表明PPy包覆在CZ粒子表面形成了核-壳结构的CZ/PPy复合物,PPy链与CZ纳米粒子之间存在一定的相互作用;复合物的抗菌性能优于CZ,且抗菌活性随着CZ含量的增加而增大.     

具有高效阳性菌抗菌活性的合成多肽聚合物研究

合成了具有抗菌活性的β-氨基酸聚合物,采用核磁共振和凝胶渗透色谱表征聚合物的数均分子量,通过最低抑菌浓度实验测试了β-氨基酸聚合物对多种革兰氏阳性菌(包括多株耐药菌)的抗菌活性,并开展了可能的耐药性研究。通过细胞膜去极化实验和扫描电子显微镜探究了抗菌聚合物对革兰氏阳性菌,尤其是对耐甲氧西林金黄色葡萄球菌的抗菌机理。结果表明,β-氨基酸聚合物通过作用于细菌的细胞膜杀死革兰氏阳性菌从而获得高效的抗菌活性,其对枯草芽孢杆菌的抗菌活性最好,最低抑菌浓度为3.13μg/mL。金黄色葡萄球菌对β-氨基酸聚合物不产生耐药性,但在相同条件下测试的对照抗生素诺氟沙星的最低抑菌浓度增加了124倍,表明细菌对抗生素很快产生了耐药性。     

静电纺丝法制备抑菌性聚酰亚胺纳米纤维

采用静电纺丝技术,以联苯四甲酸二酐(BPDA)和4,4'-二氨基二苯醚(ODA)为单体,硝酸银为银源,通过两步法制备含银聚酰亚胺(PI/Ag)纳米纤维.通过X射线衍射(XRD)、透射电子显微镜(TEM)及扫描电子显微镜(SEM)表征了PI/Ag纳米纤维的结构和微观形貌;通过浸渍培养法研究了聚酰亚胺(PI)及PI/Ag纳米纤维的抑菌性能.结果表明,聚酰亚胺基体中存在单质银的立方晶体结构,银粒子在聚酰亚胺基体表面均匀分散,平均粒径为10 nm;PI/Ag纳米纤维对大肠杆菌(E.coli)、金黄色葡萄球菌(S.aureus)和枯草芽孢杆菌(B.subtilis)表现出良好的抑菌效果,最大抑菌率可达99.1%,为聚酰亚胺在耐高温抑菌生物医用材料等领域的应用提供了新的方向.     

新型胆酸不对称双缩二氨基硫脲类衍生物的合成及其抗菌活性

在微波辐射条件下,甾酮与取代单缩二氨基硫脲经缩合反应合成了12个新型的胆酸不对称双缩二氨基硫脲衍生物(3a~3l),其结构经1H NMR,IR,ESI-MS和元素分析表征。初步抗菌活性测定结果表明:部分化合物对枯草芽孢杆菌、金黄色葡萄球菌、大肠杆菌及绿脓杆菌有一定的抗菌活性,其中,1-(2-羟基苯苄叉基)-5-[3-(3,7-二氧代-24-胆烷酸甲酯)亚甲基]二氨基硫脲(3f)对大肠杆菌的抑菌活性(IC507.40)与阿莫西林(IC507.30)相当。     

钕与乌洛托品配合物的合成、表征及抗菌活性研究

报道了配合物NdI3·C6 H1 2 N4 ·HI·13H2 O的新的合成方法 ,通过元素分析、X射线粉末衍射、红外光谱、核磁共振谱、质谱、差热 热重分析 ,确定了配合物的组成和结构 ,9个水分子与Nd3+ 形成配合阳离子 [Nd(H2 O) 9] 3+ ,C6 H1 2 N4 分子以N原子与Nd3+ 直接作用 ,而 3个I- ,HI以及剩余 4个水分子与配合阳离子 [Nd(H2 O) 9] 3+ 以静电引力或氢键的形式作用。首次测定了配体碘化钕、氢碘酸乌洛托品和配合物对枯草芽孢杆菌、大肠杆菌和葡萄球菌的抗菌活性。所有试样对枯草芽孢杆菌的杀死作用较对葡萄球菌、大肠杆菌的杀死作用显著 ,且高浓度溶液(0 .0 5mol·L - 1 )比低浓度溶液 (0 .0 1mol·L - 1 )的抗菌效果好。浓度为 0 .0 5mol·L - 1时 ,由于协同性 ,配合物NdI3·C6 H1 2 N4 ·HI·13H2 O对枯草芽孢杆菌的杀死作用大于相应的配体     

微米级花状结构铜/聚乙烯吡咯烷酮的制备及其抗菌性能

采用液相还原的方法,以聚乙烯吡咯烷酮(PVP)为修饰剂,氯化铜为前驱体,水合肼为还原剂,成功制备了微米级Cu/PVP花状结构.采用扫描电子显微镜和X射线粉末衍射仪分析了所得样品的形貌与结构;利用差热分析测定了样品的热稳定性,并采用肉汤稀释法测试了其抗菌性能.结果表明,所制备的样品具有由多个Cu/PVP圆片组装而成的直径为6μm的花状结构,其形貌依赖于反应条件.与此同时,花状结构的Cu/PVP对金黄色葡萄球菌和大肠杆菌具有明显的抗菌作用,相应的最小抑菌浓度(MIC)和最小杀菌浓度(MBC)分别为:41.25mg/L、82.5mg/L,以及20.63mg/L、82.5mg/L.与单一Cu纳米微粒相比,花状结构的Cu/PVP复合物的抗菌持久性明显较好.     

含有1H-1,2,4-三唑咪唑[2,1-b]-1,3,4-噻二唑、S-三唑[3,4-b]-1,3,4-噻二唑衍生物的合成及生物活性

合成了18个含有1H-1,2,4-三唑的咪唑[2,1-b]-1,3,4-噻二唑以及S-三唑[3,4-b]-1,3,4-噻二唑的稠杂环衍生物,经元素分析及谱学表征,探讨2,5,6-三取代咪唑[2,1-b]-1,3,4-噻二唑的可能生成机制.对大肠杆菌、绿脓杆菌、枯草杆菌等初步抑菌试验证明,多数化合物表现了较好的抑菌活性.     

Novel dihydropyrazole derivatives linked with multi（hetero）aromatic ring： Synthesis and antibacterial activity

Eight novel heterocycle-substituted dihydropyrazole derivatives were synthesized and characterized by ESI-MS,~1H NMR and ~(13)C NMR.All of the compounds have been screened for their antibacterial potential in vitro against Bacillus subtilis, Staphylococcus aureus,Escherichia coli and Pseudomonas aeruginosa.The results show that compounds 9b,9g and 9h displayed significant activity with MIC values in the range of 0.39-1.562μg/mL against B.subtilis.     

Synthesis and Crystal Structure of the Copper（Ⅱ） Complex [Cu2Cl2（HEMDP）2]·THF

One dinuclear complex [Cu2Cl2(HEMDP) 2]·THF 1(H2EMDP = 2-[(2-hydroxyethylimino)-methyl]-4,6-diiodo-phenol,THF = tetrahydrofuran) has been designed and synthesized by H2EMDP with CuCl2·2H2O in THF solvent. Complex 1 was characterized by UV,IR,ESI-MS,and elemental analyses. 1 was characterized by X-ray crystallography. The crystal belongs to the monoclinic system,space group C2/c with a = 27.886(3) ,b = 8.6890(12) ,c = 26.698(2) ,β = 105.521(2) o,V = 6233.1(12) 3,Z = 8,Mr = 1102.01,μ = 5.533 mm-1,Dc = 2.349 Mg/m3,F(000) = 4112,the final R = 0.0486 and wR = 0.1175(I > 2σ(I)) . In addition,further investigation revealed that the central copper(Ⅱ) atom in the complex is five-coordinated by one nitrogen atom and two oxygen atoms from H2EMDP and two chlorine atoms from chlorid. The 3,5-diiodosalicylaldehyde Schiff base acts as a tridentate ligand. H2EMDP and 1 were assayed for antibacterial(B. subtilis,S. aureus,S. faecalis,P. aeruginosa,E. coli and E. cloacae) activities by MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl trtrazolium bromide) method. 1 showed the most favorable antimicrobial activity with MICs of 3.125,6.25,6.25,12.5,3.125 and 6.25 μg/mL against B. subtilis,S. aureus,S. faecalis,P. aeruginosa,E. coli and E.cloacae,respectively.     

新型吡唑Schiff碱及金属配合物的合成和抑菌活性

以3-氨基-4-氰基吡唑和芳醛为原料合成了10个新型吡唑Schiff碱及铜(II)、镍(II)、锌(II)、钴(II) 4个金属配合物. 用元素分析, IR, 1H NMR及单晶解析表征了Schiff碱及金属配合物的结构. 测定了Schiff碱及金属配合物对金黄色葡萄球菌、大肠杆菌、枯草杆菌和绿脓杆菌的抑菌活性. 生物活性研究表明, Schiff碱及金属配合物对金黄色葡萄球菌、大肠杆菌和绿脓杆菌都有较好的抑菌效果, 其中铜(II)和锌(II)配合物对金黄色葡萄球菌和大肠杆菌的抑菌活性最好.     

5-氯水杨醛缩乙醇胺合铜(Ⅱ)的微波直接合成、晶体结构及抑菌活性

以5-氯水杨醛、乙醇胺和氯化铜为原料,在微波作用下合成了5-氯水杨醛缩乙醇胺合铜(Ⅱ)配合物。 利用红外光谱、元素分析和单晶X射线衍射方法对目标化合物进行了表征,标题配合物为单斜晶系,P21/n空间群。晶胞参数：a=0.49793(6) nm,b=1.7037(2) nm,c=1.07120(12) nm,β=94.579(3)°,F(000)=470,Z=2,V=0.905(8) nm3,Dc=1.689 mg/m3,R[I＞2σ(I)],R1=0.0624,ωR2=0.1555。 配合物分子中,2种Schiff碱配体中的2个O原子和2个N原子参与配位,Cu(Ⅱ)处于四边形配位中心。 用MTT法测得标题配合物对6种革兰氏细菌（B.subtilis、S.aureus、S.faecalis、P.aeruginosa、E.coli和E.cloacae）的最小抑制浓度分别为12.25、25、12.5、12.5、6.25和6.25 mg/L。     

An antifungal cadinanolide from Pseudoelephantopus spicatus

A new sesquiterpene lactone was obtained from the chloroform extract of Pseudoelephantopus spicatus. Its structure was elucidated by extensive one dimentional (1D) and 2D NMR spectroscopy and mass spectrometry. It was found to exhibit moderate antifungal activity against C albicans and A. niger, and low activity against T. mentagrophytes, S. aureus, E. coli and P. aeruginosa. It was inactive against B. subtilis.     

Formulation,characterization and biological evaluation of injectable nanocrystals from stem exudate gel of Caralluma retrospiciens (Ehrenb) – Part C

The purpose of this study was to develop injectable nanocrystals (NC) from stem exudate gel (EG) from Caralluma retrospiciens (Ehrenb) using the technique of nanoprecipitation. The NC had a zeta potential of ?5.58 ± 4.27 mV. Size distribution analysis showed that it ranged in size from 100 to 300 nm. The polydispersity index (PDI) was 0.467, while its percentage PDI was 68.4. Scanning electron microscopic analysis and transmission electron microscopy studies revealed the morphological features of NC as discrete crystals with rough surfaces. The mobility of NC was 5.5 µm.cm/Vs, while its conductivity was 0.16 mS/cm. Antibacterial studies showed broad activity against both Gram-positive and Gram-negative bacteria. The minimum inhibitory concentrations (MICs) of NC against Bacillus subtilis (B. subtilis), Staphylococcus aureus (S. aureus), Streptococcus pyogenes (S. pyogenes), Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa) and Klebsiella pneumoniae (K. pneumoniae) were 6, 8, 8, 4, 8, and 6 % (w/v), respectively. The antibacterial effect was highest against K. pneumoniae (25.6 ± 1.5 mm), followed by E. coli (25.5 ± 1.8 mm), P. aeruginosa (24.1 ± 1.2 mm), S. pyogenes (22.2 ± 1.2 mm), S. aureus (21.83 ± 1.2 mm) and B. subtilis (20.33 ± 1.8 mm). In this study, the cytotoxicity properties of NC were determined against MCF-7 breast cancer cells ATCC. The NC failed to inhibit the proliferation of MCF-7 cells against the even at 300 µg/mL concentration. These results indicated that the NC is a promising antibacterial injectable dosage form.     

Synthesis, characterization and biological evaluation of mononuclear Co(II), Ni(II), Cu(II) and Pd(II) complexes with new N2O2 Schiff base ligands

New tetradentate N(2)O(2) donor Schiff bases and their mononuclear Co(II), Ni(II), Cu(II), and Pd(II) complexes were synthesized and characterized extensively by IR, (1)H-, (13)C-NMR, mass, ESR, conductivity measurements, elemental and thermal analysis. Specifically the magnetic and electronic spectral measurements demonstrate the octahedral structures of cobalt(II), nickel(II) complexes and square planar geometries of copper(II), palladium(II) complexes. All the ligands and complexes were screened for their in vitro antibacterial activity against two gram-positive bacteria (Bacillus subtilis, Staphylococcus aureus) and two gram-negative bacteria (Escherichia coli, Klebsiella pneumonia). In this study, Pd(II) complexes exhibited potent antibacterial activity against B. subtilis, S. aureus whereas other metal complexes also exerted good activity towards all tested strains even than standard drugs streptomycin and ampicillin.     

Antimicrobial activity and pollen composition of honey samples collected from different provinces in Turkey

The antibacterial activity of honey samples from different sources were collected and investigated against Bacillus cereus, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae ATCC 27736, Morganella morganii, Micrococcus luteus NRRL B-4375, Escherichia coli ATCC 35218, and Candida albicans. Pathogens exhibited different sensitivities towards the honey samples. The results showed that majority of the honey samples (75%) generally inhibitied the bacteria tested. The honey samples which were obtained from Izmir (samples 1 and 2) proved more effective as inhibitors against P. aeruginosa, E. coli, and S. aureus. The honey which was obtained from Mu?la (sample 5) exhibited high anticandidal activity on C. albicans. A comparison of the honey samples on the basis of pollen content revealed that they were heterofloral, and samples which had highest antibacterial activity against P. aeruginosa, E. coli, and S. aureus were dominated by pollen from Chenopodiaceae/Amaranthaceae (sample 1), and Trifolium, Trigonella, Cyperaceae, Zea mays and Anthemis taxa (sample 2). The honey proved more effective on bacteria than antibiotics.