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Journal of Antibiotics

Jian Ma, Hui Lei, Xiu Chen, Xiaoxu Bi, Yi Jiang, Li Han, Xueshi Huang
Three new metabolites (2-4), together with one known compound, GTRI-02, (1) were isolated from a fermentation broth of Streptomyces violaceoruber derived from Equus burchelli feces. The structures of the new compounds 2-4 were established using comprehensive NMR spectroscopic data analysis as well as UV, IR and MS data. The anti-inflammatory activity of compounds 1-4 was tested by examining their ability to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage cells...
July 12, 2017: Journal of Antibiotics
Hideki Yamamura, Shoya Miyazaki, Kodai Ikoma, Youji Nakagawa, Moriyuki Hamada, Misa Otoguro, Tomohiko Tamura, Katsuhiko Ando, Nyunt Phay, Masayuki Hayakawa
An actinomycete strain, designated MM04-1133(T), was isolated from an anthill soil sample collected in Bagan, Myanmar. To establish the taxonomic status of this strain, the isolate was subjected to a polyphasic approach. Strain MM04-1133(T) was Gram-staining positive, aerobic, motile and formed long and narrow sporangia directly above the surface of the substrate mycelium. Whole-cell hydrolysates of the strain contained 3-OH-diaminopimelic acid, arabinose, glucose, galactose, mannose, rhamnose and xylose. The predominant menaquinones were MK-10(H6) and MK-10(H8)...
July 12, 2017: Journal of Antibiotics
Lili Li, Sofie Kromann, John Elmerdahl Olsen, Søren Wedel Svenningsen, Rikke Heidemann Olsen
Sertraline, an antidepressive drug, has been reported to inhibit general bacterial efflux pumps. In the present study, we report for the first time a synergistic effect of sertraline and tetracycline in a TetA-encoded tetracycline-resistant strain of Escherichia coli. Synergy between sertraline and tetracycline in an E. coli strain with TetA-mediated tetracycline resistance (E. coli APEC_O2) was assessed by the MIC and checkerboard assays. The global transcriptome of E. coli APEC_O2 exposed to ½ MIC concentrations of sertraline and/or tetracycline was analyzed to elucidate the interaction mechanism between sertraline and tetracycline...
July 12, 2017: Journal of Antibiotics
Dhanalakshmi R Nair, Ji Chen, João M Monteiro, Michaele Josten, Mariana G Pinho, Hans-Georg Sahl, Jimmy Wu, Ambrose Cheung
In a loss-of-viability screen of small molecules against methicillin-resistant Staphylococcus aureus (MRSA) USA300, we found a small molecule, designated DNAC-2, which has an MIC of 8 μg ml(-1). DNAC-2 is a quinolinol derivative that is bactericidal at 2X MIC. Macromolecular synthesis assays at 2 × MIC of DNAC-2 revealed inhibition of DNA, cell wall, RNA and protein synthesis within fifteen to thirty minutes of treatment when compared to the untreated control. Transmission electron microscopy of DNAC-2-treated cells revealed a significantly thicker cell wall and impaired daughter cell separation...
July 12, 2017: Journal of Antibiotics
Hiroyasu Ando, Aoi Kimishima, Motoyoshi Ohara, Tomoyasu Hirose, Takanori Matsumaru, Hirokazu Takada, Keisuke Morodome, Takehiro Miyamoto, Akihiro Sugawara, Satoshi Ōmura, Toshiaki Sunazuka
Synthesis of a cis-decalin moiety, containing an oxa-bridged cis-decalin ring system (11-oxatricyclo(5.3.1.(1,7)0(3,8))undecane), as a key intermediate of the total synthesis of luminamicin (1) was accomplished. One of the essential steps in our synthetic route is construction of a cis-decaline framework using a one-pot Michael addition-aldol reaction. Additionally, the bridged ether moiety was obtained by an intramolecular 1,6-oxa-Michael reaction of a conjugated aldehyde.The Journal of Antibiotics advance online publication, 5 July 2017; doi:10...
July 5, 2017: Journal of Antibiotics
Zhengkun Chen, Xiuli Xu, Jinwei Ren, Wenzhao Wang, Xingzhong Liu, Erwei Li
Trichopeptides A (1) and B (2), new linear tetrapeptide and tripeptide, respectively, and three new diketopiperazines trichocyclodipeptides A-C (3-5) were isolated from the fermentation of the ascomycete fungus Stagonospora trichophoricola, a fungus isolated from the soil sample surrounding the fruiting body of Ophiocordyceps sinensis in Maqin Country, Qinghai Province, People's Republic of China. Their structures were primarily elucidated by interpretation of NMR and MS experiments. The absolute configurations of 1-5 were assigned through Marfey's method on their acid hydrolyzates...
July 5, 2017: Journal of Antibiotics
Ko Kumura, Yoshinari Wakiyama, Kazutaka Ueda, Eijiro Umemura, Takashi Watanabe, Mikio Yamamoto, Takuji Yoshida, Keiichi Ajito
Lincomycin derivatives that have a 5-(2-nitrophenyl)-1,3,4-thiadiazol-2-yl thio moiety at the 7-position were synthesized. 5-Substituted 2-nitrophenyl derivatives showed potent antibacterial activities against Streptococcus pneumoniae and Streptococcus pyogenes with erm gene. Antibacterial activities of the 4,5-di-substituted 2-nitrophenyl derivatives were generally comparable to those of telithromycin (TEL) against S. pneumoniae with erm gene and clearly superior to those of TEL against S. pyogenes with erm gene...
July 5, 2017: Journal of Antibiotics
Hue Tu Quach, Riho Tanigaki, Junpei Yokoigawa, Yuriko Yamada, Masamitsu Niwa, Seiya Hirano, Yoshihito Shiono, Ken-Ichi Kimura, Takao Kataoka
Allantopyrone A is a fungal metabolite that uniquely possesses two α,β-unsaturated carbonyl moieties. We recently reported that allantopyrone A inhibited the nuclear factor-κB (NF-κB) signaling pathway induced by tumor necrosis factor (TNF)-α in human lung carcinoma A549 cells. In the present study, the mechanism by which allantopyrone A inhibits the TNF-α-induced signaling pathway was investigated in more detail. Allantopyrone A blocked extensive modifications to receptor-interacting protein 1 (RIP1) in the TNF receptor 1 (TNF-R1) complex...
July 5, 2017: Journal of Antibiotics
Kyriacos C Nicolaou, Stephan Rigol
The advent of modern antibiotics contributed enormously to the dramatic extension of human lifespan since their discovery by virtue of their lethal and selective action against pathogenic microbes. And yet despite our powerful arsenal of weapons against these pathogens, the war against them has not been won. And it may never be. Drug resistance is still menacing the society with many lives being lost due to deadly infections caused by continuously evolving strains spread beyond our means to eradicate them or prevent their spreading...
July 5, 2017: Journal of Antibiotics
Brandon Kulengowski, Jeffrey J Campion, David J Feola, David S Burgess
No abstract text is available yet for this article.
July 5, 2017: Journal of Antibiotics
Henki Rotinsulu, Hiroyuki Yamazaki, Tomohito Miura, Satomi Chiba, Defny S Wewengkang, Deiske A Sumilat, Michio Namikoshi
No abstract text is available yet for this article.
June 28, 2017: Journal of Antibiotics
Yoshiaki Takahashi, Eijiro Umemura, Yoshihiko Kobayashi, Shoichi Murakami, Toru Nawa, Akihiro Morinaka, Toshiaki Miyake, Masakatsu Shibasaki
No abstract text is available yet for this article.
June 28, 2017: Journal of Antibiotics
L Ravithej Singh, Srinivasa Rao Avula, Sneha Raj, Akanksha Srivastava, Gopala Reddy Palnati, C K M Tripathi, Mukesh Pasupuleti, Koneni V Sashidhara
Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris...
June 21, 2017: Journal of Antibiotics
Kosuke Minagawa, Daisuke Urabe, Masayuki Inoue
C19-diterpene alkaloids are a class of alkaloids with pharmacologically important activities having an intricately fused hexacyclic ABCDEF-ring system. Here we report expeditious assembly of the ACE-ring substructure 4a by applying a three-component coupling strategy. A radical-polar crossover reaction between an AE-ring radical precursor, a C-ring radical acceptor and an aldehyde was realized by the actions of Et3B and O2, resulting in the installation of three new stereocenters and extension of the carbon chain corresponding to the B-ring...
June 14, 2017: Journal of Antibiotics
Fabrizio Angius, Enrica Piras, Sabrina Uda, Clelia Madeddu, Roberto Serpe, Rachele Bigi, Wuguo Chen, Dirk P Dittmer, Raffaello Pompei, Angela Ingianni
Kaposi sarcoma herpesvirus (KSHV), also known as human herpesvirus 8, is the causative agent of Kaposi sarcoma; this malignant angiosarcoma is usually treated with conventional antitumor agents that can control disease evolution, but do not clear the latent KSHV episome that binds to cellular DNA. Some commercial antibacterial sulfonamides were tested for the ability to suppress latent KSHV. Quantitative PCR (qPCR) and cytofluorometry assays were used for detecting both viral DNA and the latency factor LANA (latency-associated nuclear antigen) in BC3 cells, respectively...
June 14, 2017: Journal of Antibiotics
Sandra Halecker, Frank Surup, Halvor Solheim, Marc Stadler
No abstract text is available yet for this article.
June 7, 2017: Journal of Antibiotics
Pia Uusitalo, Ulrik Hägglund, Elin Rhöös, Henrik Scherman Norberg, Mikael Elofsson, Charlotta Sundin
Pseudomonas aeruginosa is an opportunistic pathogen that can be very hard to treat because of high resistance to different antibiotics and alternative treatment regimens are greatly needed. An alternative or a complement to traditional antibiotic is to inhibit virulence of the bacteria. The salicylidene acylhydrazide, INP0341, belongs to a class of compounds that has previously been shown to inhibit virulence in a number of Gram-negative bacteria. In this study, the virulence blocking effect of INP0341 on P...
June 7, 2017: Journal of Antibiotics
Fumiaki Tabuchi, Yasuhiko Matsumoto, Masaki Ishii, Keita Tatsuno, Mitsuhiro Okazaki, Tomoaki Sato, Kyoji Moriya, Kazuhisa Sekimizu
Vancomycin is a widely used clinical drug to treat for infection by methicillin-resistant Staphylococcus aureus. Some patients show a weak response to vancomycin treatment. We previously reported that β-lactams increase the susceptibility to vancomycin by vancomycin-highly resistant S. aureus (VRSA) strains obtained following repeated in vitro mutagenesis and vancomycin selection. Here we found that the susceptibility of the VRSA strains to vancomycin was remarkably increased by combined treatment with D-cycloserine...
June 7, 2017: Journal of Antibiotics
Yoshinari Wakiyama, Ko Kumura, Eijiro Umemura, Kazutaka Ueda, Takashi Watanabe, Keiko Yamada, Takafumi Okutomi, Keiichi Ajito
To modify lincomycin (LCM) at the C-6 and the C-7 positions, we firstly prepared various substituted proline intermediates (7, 11-15 and 17). These proline intermediates were coupled with methyl 1-thio-α-lincosamide and tetrakis-O-trimethylsilylation followed by selective deprotection of the TMS group at the 7-position gave a wide variety of key intermediates (23-27, 47 and 50). Then, we synthesized a variety of novel LCM analogs modified at the 7-position in application of the Mitsunobu reaction, an SN2 reaction, and a Pd-catalyzed cross-coupling reaction...
May 31, 2017: Journal of Antibiotics
Konami Takahashi, Kazunari Sakai, Yuriko Nagano, Sakiko Orui Sakaguchi, Andre O Lima, Vivian H Pellizari, Masato Iwatsuki, Kiyotaka Takishita, Kenichi Nonaka, Katsunori Fujikura, Satoshi Ōmura
No abstract text is available yet for this article.
May 31, 2017: Journal of Antibiotics
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