Relationship between the antibacterial activity towards Escherichia coli NCTC 5933 and the physico-chemical properties of some esters of 3,4,5-trihydroxybenzoic acid (Gallic acid).

Aqueous solubilities, oleyl alcohol: water and octanol: water partition coefficients, RM values, reduction in surface tension of water, relative antioxidant activities and pKa values, were determined for gallic acid and a series of its alkyl esters. Correlations were sought between these physico-chemical measurements and MIC, MBC and killing-rate determinations against Escherichia coli. Variations in antibacterial activity generally correlated well with partition parameters, but these correlations did not accurately predict the cut-off point in antibacterial activity.     

Synthesis and antibacterial activity of eremomycin esters through the carboxyl group]

Methyl, benzyl and diphenylmethyl esters of the glycopeptide antibiotic eremomycin were obtained by its treatment with corresponding diazoalkanes. The esters have high antibacterial activity but are less active than the parent antibiotic.     

Antiproliferative and antibacterial activity of some glutarimide derivatives

Antiproliferative and antibacterial activities of nine glutarimide derivatives (1–9) were reported. Cytotoxicity of compounds was tested toward three human cancer cell lines, HeLa, K562 and MDA-MB-453 by MTT assay. Compound 7 (2-benzyl-2-azaspiro[5.11]heptadecane-1,3,7-trione), containing 12-membered ketone ring, was found to be the most potent toward all tested cell lines (IC₅₀?=?9–27?μM). Preliminary screening of antibacterial activity by a disk diffusion method showed that Gram-positive bacteria were more susceptible to the tested compounds than Gram-negative bacteria. Minimum inhibitory concentration (MIC) determined by a broth microdilution method confirmed that compounds 1, 2, 4, 6–8 and 9 inhibited the growth of all tested Gram-positive and some of the Gram-negative bacteria. The best antibacterial potential was achieved with compound 9 (ethyl 4-(1-benzyl-2,6-dioxopiperidin-3-yl)butanoate) against Bacillus cereus (MIC 0.625?mg/mL; 1.97?×?10^?3?mol/L). Distinction between more and less active/inactive compounds was assessed from the pharmacophoric patterns obtained by molecular interaction fields.     

Isolation and characterization of novel glycoproteins from fish epidermal mucus: correlation between their pore-forming properties and their antibacterial activities

In fish, a layer of mucus covers the external body surface contributing therefore, among other important biological functions, to the defense system of fish. The prevention of colonization by aquatic parasites, bacteria and fungi is mediated both by immune system compounds (IgM, lysozyme, etc.) and by antibacterial peptides and polypeptides. We have recently shown that only the hydrophobic components of crude epidermal mucus of fresh water and sea water fish exhibit strong pore-forming properties, which were well correlated with antibacterial activity [N. Ebran, S. Julien, N. Orange, P. Saglio, C. Lemaitre, G. Molle, Comp. Biochem. Physiol. 122 (1999)]. Here, we have isolated novel glycosylated proteins from the hydrophobic supernatant of tench (Tinca tinca), eel (Anguilla anguilla) and rainbow trout (Oncorhynchus mykiss) mucus. The study of their secondary structure was performed by circular dichroism and revealed structures in random coil and alpha-helix in the same proportions. When reconstituted in planar lipid bilayer, they induced the formation of ion channels. This pore-forming activity was well correlated with a strong antibacterial activity (minimal inhibitory concentration < 1 microM for the three proteins) against both gram-negative and gram-positive bacteria. Our results suggest that fish secrete antibacterial glycoproteins able to kill bacteria by forming large pores (several hundreds to thousands of pS) in the target membrane.     

Biological activity of some synthetic gibberellin glucosyl esters

Four gibberellin (GA₁, GA₃, GA₄ and GA₃₇) glucosyl esters were synthesized and found to be as active as their respective free acids in the rice seedling bioassay. The rapid hydrolysis of the glucosyl esters in rice seedlings was demonstrated by feeding experiments with glucosyl esters of [³H]GA₁ and [³H]GA₄.     

Synthesis and antibacterial activity of some new derivatives of pyrazole

In this study, we report the synthesis and antibacterial activity of a new series of 5-amido-1-(2,4-dinitrophenyl)-1H-4-pyrazolecarbonitriles. Our results show that all compounds exhibit antimicrobial activities against methicillin susceptible Staphylococcus aureus and methicillin resistant S. aureus with MIC values of 25.1 and 91.0 μM.     

Synthesis and antibacterial activity of some novel imidazole-based dicationic quinolinophanes

Synthesis of novel quinoline based dicationic benzimidazolophanes and imidazolophanes incorporating various spacer units is described. Some of the quinolinophanes 1b, 3a, 3b and 4a exhibit good antibacterial activity against most of the human pathogenic bacteria in the tested concentrations as compared to the other cyclophanes as well as the test control, streptomycin.     

黄粉甲幼虫抗菌物质的诱导及其抗菌活性

采用饥饿法、紫外线照射法和针刺法处理黄粉甲Tenebriomolitor 6龄幼虫后均能诱导其 产生抗菌物质,收集的血淋巴上清液对真菌有抑制作用,对细菌无抑制作用;经热处理后的血 淋巴上清液则对细菌有抑制作用,而对真菌无抑制作用。SDS-PAGE检测结果发现,与未诱导的 对照相比经诱导的黄粉甲幼虫血淋巴中,原有的一类大分子蛋白质如分子量分别为97kD、44 kD和37 kD左右的蛋白质缺失;而ESI-MS分析结果显示诱导后比诱导前黄粉甲幼虫血淋巴中有 小分子物质产生,推测可能是此类缺失蛋白质分解为小分子量的抗菌肽,从而表现出抗菌活性 。     

Inverse correlation of maturity and antibacterial activity in human dendritic cells

Dendritic cells (DCs) are a key part of host defense against microbial pathogens, being part of the innate immune system, but also instructing the adaptive T cell response. This study was designed to evaluate whether human DCs directly contribute to innate immunity by killing intracellular bacteria, using tuberculosis as a model. DCs were detected in bronchoalveolar lavage samples indicating that DCs are available for immediate interaction with Mycobacterium tuberculosis (M. Tb) after inhalation of the pathogen. The phenotype of DC in bronchoalveolar lavage closely resembles monocyte-derived immature DC (iDC) according to the expression of CD1a, CD83, and CCR7. The antimicrobial activity of iDC against intracellular M. Tb inversely correlated with TNF-alpha-release and was enhanced by treatment with anti-TNF-alpha Abs. Differentiation of iDC into mature DC by addition of TNF-alpha or activation via Toll-like receptors further reduced killing of M. Tb. The antibacterial activity against intracellular M. Tb of all DCs was significantly lower than alveolar macrophages. Therefore, the maintenance of a pool of DCs at the site of disease activity in tuberculosis, and the maturation of these DC by TNF-alpha provides a mechanism by which M. Tb escapes the innate immune system.     

油松毛虫幼虫抗菌物质及其抗菌活性研究

采用体内注射法,对油松毛虫Dendrolimus tabulaeformis Tsai et Liu 3龄幼虫注射浓度为1．0&#215;10^8孢子／mL的大肠杆菌Escherichia coli菌悬液,诱导其产生抗菌物质,12h后收集制备血淋巴粗提液。分别测定对4种细菌和4种真菌的抗菌活性,并检测温度、pH值变化和反复冻融对抗菌活性的影响。采用Tricine—SDS—PAGE电泳法确定抗菌物质的分子量大小。结果发现,诱导后的油松毛虫3龄幼虫血淋巴粗提液对试验的细菌和真菌均有不同程度的抑制作用,其中对革兰氏阴性细菌大肠杆菌E．coli和变形杆菌Proteus species的抑制作用强于革兰氏阳性细菌金黄色葡萄球菌Staphylococcus aureus和枯草芽孢杆菌Bacillus subtilis。血淋巴粗提液的的抗菌活性在50℃水浴处理和4～9的pH值条件下保持稳定,反复冻融1～5次抗菌物质的活性降低4．3％～14．9％。电泳结果显示,诱导组血淋巴粗提液在23．2kD和15．0kD处分别出现一条特异性条带,在60．4kD处蛋自带变浅。由此推测从油松毛虫幼虫体内诱导产生的抗菌物质分子量可能是23．2kD和15．0kD。     

Synthesis and antibacterial activity of alkyl derivatives of the glycopeptide antibiotic A40926 and their amides

New derivatives of the glycopeptide antibiotic A40926 were synthesized and evaluated for antimicrobial activity against VRE. Deacylated A40926 was obtained by microbial transformation of the parent antibiotic with the use of Actinoplanes teichomyceticus ATCC 31121. Regioselective synthesis of alkylated derivatives of Deacyl A40926 was carried out using lipophilic aliphatic and aromatic halides or aldehydes. Further modification of the two carboxylic acids was performed to increase antibiotic activity. Poor antimicrobial activity was observed for the derivatives obtained by lipophilic mono- or dialkylation of the amino groups present on the molecule, while simultaneous condensation of both carboxylic groups, in hydrophobic derivatives, with dibasic amines led to a strong increase in antibiotic activity.     

Magnetic force microscopy of iron oxide nanoparticles and their cellular uptake

Magnetic force microscopy has the capability to detect magnetic domains from a close distance, which can provide the magnetic force gradient image of the scanned samples and also simultaneously obtain atomic force microscope (AFM) topography image as well as AFM phase image. In this work, we demonstrate the use of magnetic force microscopy together with AFM topography and phase imaging for the characterization of magnetic iron oxide nanoparticles and their cellular uptake behavior with the MCF7 carcinoma breast epithelial cells. This method can provide useful information such as the magnetic responses of nanoparticles, nanoparticle spatial localization, cell morphology, and cell surface domains at the same time for better understanding magnetic nanoparticle‐cell interaction. It would help to design magnetic‐related new imaging, diagnostic and therapeutic methods. © 2009 American Institute of Chemical Engineers Biotechnol. Prog., 2009