Production,Purification and Characterization of ‘Iturin A-2’ a Lipopeptide with Antitumor Activity from Chinese Sauerkraut Bacterium Bacillus velezensis T701

International Journal of Peptide Research and Therapeutics - This study was done to purify and characterize antitumor lipopeptide from Bacillus strains. Bacillus velezensis strain T701, which was...     

Propargylglycine-based antimicrobial compounds are targets of TolC-dependent efflux systems in Escherichia coli

A library of novel l-propargylglycine-based compounds were designed and synthesized with the goal of inhibiting the growth of Gram-negative bacteria by targeting LpxC, a highly conserved Gram-negative enzyme which performs an essential step in the lipid A biosynthetic pathway. These compounds were designed with and without a nucleoside and had varying tail structures, which modulate their lipophilicity. The synthetic scheme was improved compared to previous methods: a methyl ester intermediate was converted to a hydroxamic acid, which obviated the need for a THP protecting group and improved the yields and purity of the final compounds. Antimicrobial activity was observed for non-nucleoside compounds containing a phenyl propargyl ether tail (5) or a biphenyl tail (6). An MIC of 16 µg/mL was achieved for 6 in Escherichia coli, but inhibition was only possible in the absence of TolC-mediated efflux. Compound 5 had an initial MIC >160 µg/mL in E. coli. Enhancing outer membrane permeability or eliminating efflux reduced the MIC modestly to 100 µg/mL and 80 µg/mL, respectively. These results highlight the importance of hydrophobicity of this class of compounds in developing LpxC inhibitors, as well as the design challenge of avoiding multidrug efflux activity.     

中国台湾小车蝗属三新种及中国已知种检索表(直翅目,蝗总科,斑翅蝗科,斑翅蝗亚科)（英文）

记述了中国台湾小车蝗属Oedaleus Fieber,1853的3新种。新种夏氏小车蝗Oedaleus xiai sp.nov.前翅短,刚到达后足股节顶端,可同本属所有已知种相区别。新种高雄小车蝗Oedaleus kaohsiungensis sp.nov.与台湾小车蝗Oe.formosana(Shiraki,1910)近似,不同之处为后足股节内侧具黑色斑纹和后足胫节黄褐色,非红色。新种南投小车蝗Oedaleus nantouensis sp.nov.与台湾小车蝗Oe.formosana(Shiraki,1910)近似,不同之处为复眼较大,纵径等于眼下沟的长度;中胸腹板中隔很宽,最小宽度为长的1.8倍。新种南投小车蝗Oedaleus nantouensis sp.nov.与高雄小车蝗Oedaleus kaohsiungensis sp.nov.也近似,不同之处为后足股节下缘红色,后足胫节红色。列出了产于中国的小车蝗属13个种的检索表。模式标本存于自然科学博物馆,台中,台湾,中国。     

Probing immune infiltration dynamics in cancer by in vivo imaging

Cancer immunotherapies typically aim to stimulate the accumulation and activity of cytotoxic T-cells or pro-inflammatory antigen-presenting cells, reduce immunosuppressive myeloid cells or regulatory T-cells, or elicit some combination of effects thereof. Notwithstanding the encouraging results, immunotherapies such as PD-1/PD-L1-targeted immune checkpoint blockade act heterogeneously across individual patients. It remains challenging to predict and monitor individual responses, especially across multiple sites of metastasis or sites of potential toxicity. To address this need, in vivo imaging of both adaptive and innate immune cell populations has emerged as a tool to quantify spatial leukocyte accumulation in tumors non-invasively. Here we review recent progress in the translational development of probes for in vivo leukocyte imaging, focusing on complementary perspectives provided by imaging of T-cells, phagocytic macrophages, and their responses to therapy.     

Fluorogenic 7-azidocoumarin and 3/4-azidophthalimide derivatives as indicators of reductase activity in microorganisms

A series of fluorogenic heterocyclic azides were prepared and assessed as reductase substrates across a selection of Gram-negative and Gram-positive microorganisms. The majority of these azides showed similar activity profiles to nitroreductase substrates. Microorganisms that do not produce hydrogen sulfide reduced the azides, indicating reductase activity was not linked to hydrogen sulfide production.