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Journal of Antibiotics

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https://www.readbyqxmd.com/read/28096550/the-ups-and-downs-of-drug-discovery-the-early-history-of-fidaxomicin
#1
James B McAlpine
The path from antibiotic compound discovery to the market is marked by many potholes and its negotiation is often dependent on luck and persistence. Perhaps the prime example of this is the case of the development of tiacumicin B to Fidaxomicin, where both parameters were critical and the path was particularly circuitous.The Journal of Antibiotics advance online publication, 18 January 2017; doi:10.1038/ja.2016.157.
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096549/decatamariic-acid-a-new-mitochondrial-respiration-inhibitor-discovered-by-pesticidal-screening-using-drug-sensitive-saccharomyces-cerevisiae
#2
Yoshihiro Watanabe, Takuya Suga, Satomi Narusawa, Masato Iwatsuki, Kenichi Nonaka, Takuji Nakashima, Yasuo Shinohara, Takahiro Shiotsuki, Naoya Ichimaru, Hideto Miyoshi, Yukihiro Asami, Satoshi Ōmura, Kazuro Shiomi
A new decalin, decatamariic acid, was isolated from a cultured broth of the fungus Aspergillus tamarii FKI-6817. Its absolute configuration was elucidated by NMR and electronic circular dichroism. Decatamariic acid (10 μM) elicited ~50% inhibition of the ATP production in mitochondria isolated from wild-type Saccharomyces cerevisiae without affecting the activities of respiratory enzymes. The action manner of this compound may be interesting as a possible seed for new pesticides.The Journal of Antibiotics advance online publication, 18 January 2017; doi:10...
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096548/the-synthesis-and-evaluation-of-the-antiproliferative-activity-of-deacidified-gex1a-analogues
#3
Takamichi Imaizumi, Hiroshi Nakagawa, Ran Hori, Yasuo Watanabe, Shiro Soga, Kyoichiro Iida, Hideyuki Onodera
GEX1A/herboxidiene (1) is a natural product isolated from Streptomyces sp. and has been reported to target the pre-mRNA splicing process. Although 1 was shown to have antitumor activity in vivo, weight loss was observed in mice when 1 was consecutively administered. We assumed that the carboxylic acid moiety was one of the causes of this toxicity. In this study, a series of amide, carbamate and urea analogues of 1 were synthesized and their antiproliferative activity was evaluated in vitro. The synthesis of urea analogues featured Curtius rearrangement following amine treatment with the one-pot procedure from 1...
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096547/trachyspic-acid-19-butyl-ester-a-new-inhibitor-of-plk1-polo-box-domain-dependent-recognition-from-uncharacterized-fungus-rkgs-f2684
#4
Toshihiko Nogawa, Noriko Ogita, Yushi Futamura, Shigenori Negishi, Nobumoto Watanabe, Hiroyuki Osada
No abstract text is available yet for this article.
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096546/ma026-an-anti-hepatitis-c-virus-compound-opens-tight-junctions-of-the-epithelial-cell-membrane
#5
Yusuke Kanda, Youhei Yamasaki, Satomi Shimura, Shinji Kamisuki, Fumio Sugawara, Yoko Nagumo, Takeo Usui
MA026 is an antiviral natural compound against hepatitis C virus (HCV). It was recently reported that MA026 binds claudin-1 (CLDN1) and inhibits HCV infection. Although CLDN1 is an important component of tight junctions (TJ) in the epithelial cell layer, the effects of MA026 on the TJ barrier function remained to be revealed. Here we report that MA026 irreversibly opens the TJ. MA026 irreversibly increased FD4 permeability and decreased transepithelial electrical resistance (TER) for at least 5 h. Although MA026 increased Ca(2+) influx in layered MDCKII cells, the Ca(2+) influx was less than that of capsaicin, a reversible TJ opener...
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096545/thiazomycin-nocathiacin-and-analogs-show-strong-activity-against-clinical-strains-of-drug-resistant-mycobacterium-tuberculosis
#6
Sheo B Singh, Libo Xu, Peter T Meinke, Natalia Kurepina, Barry N Kreiswirth, David B Olsen, Katherine Young
Thiazolyl peptides are a class of natural products with potent Gram-positive antibacterial activities. Lack of aqueous solubility precluded this class of compounds from advancing to clinical evaluations. Nocathiacins and thiazomycins are sub-classes of thiazolyl peptides that are endowed with structural features amenable for chemical modifications. Semi-synthetic modifications of nocathiacin led to a series of analogs with improved water solubility, while retaining potency and antibacterial spectrum. We studied the activities of a selection of two natural products (nocathiacin and thiazomycin) as well as seven polar semi-synthetic analogs against twenty clinical strains of Mycobacterium tuberculosis with MDR phenotypes...
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096544/simamycin-5-o-geranyluridine-a-new-prenylated-nucleoside-from-streptomyces-sp
#7
Yasuhiro Igarashi, Takayuki Kyoso, Youngju Kim, Tsutomu Oikawa
A new nucleoside modified by prenylation, simamycin (1), was isolated from the culture broth of a soil-derived Streptomyces sp. Its structure was determined by spectroscopic analysis and chemical synthesis as 5'-O-geranyluridine. Compound 1 induced differentiation of preadipocytes into matured adipocytes.The Journal of Antibiotics advance online publication, 18 January 2017; doi:10.1038/ja.2016.163.
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074057/development-of-new-polymyxin-derivatives-for-multi-drug-resistant-gram-negative-infections
#8
REVIEW
Pamela Brown, Michael J Dawson
Over the last decade, there has been a resurgence of interest in polymyxins owing to the rapid rise in multi-drug resistant Gram-negative bacteria against which polymyxins offer a last-resort treatment. Although having excellent antibacterial activity, the clinical utility of polymyxins is limited by toxicity, especially renal toxicity. There is much interest therefore in developing polymyxin analogues with an improved therapeutic index. This review describes recent work aimed at improving the activity and/or reducing the toxicity of polymyxins...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074056/biphenyl-ether-derivatives-with-protein-tyrosine-phosphatase-1b-inhibitory-activity-from-the-freshwater-fungus-phoma-sp
#9
Deiske A Sumilat, Hiroyuki Yamazaki, Syu-Ichi Kanno, Ryo Saito, Yuta Watanabe, Michio Namikoshi
No abstract text is available yet for this article.
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074055/effects-of-two-6-quinolinyl-chalcones-on-the-integrity-of-plasma-membrane-of-paracoccidioides-brasiliensis
#10
Nívea P de Sá, Patrícia S Cisalpino, Luciana C Tavares, Leandro Espíndola, Beatriz M Borelli, Paulo Js Barbeira, Gabriele de Matos Cardoso Perdigão, Elaine M Souza-Fagundes, Carlos A Rosa, Moacir G Pizzolatti, Susana Johann
Paracoccidioidomycosis is the most prevalent systemic mycosis in Latin America, yet few therapeutic options exist. Our aim was to search for new compounds with high efficacy, low toxicity, shorter treatment time and affordable cost. We studied two synthetic 6-quinolinyl chalcones, 3b and 3e, to determine their effects on VERO cells, antifungal activity, survival curve, interaction with other drugs and phenotypic effects against several isolates of Paracoccidioides spp. In this study, we verified that the compounds were not toxic, exhibited superior in vitro activity compared with that shown by trimethoprim-sulfamethoxazole, and after 5 days of treatment, decreased the fungal cell viability by approximately 70%...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074054/synergistic-antifungal-indolecarbazoles-from-streptomyces-sp-cns-42-associated-with-traditional-chinese-medicine-alisma-orientale
#11
Mei Liu, Pei Huang, Qian Wang, Biao Ren, Ayokunmi Oyeleye, Miaomiao Liu, Jingyu Zhang, Xiaolin Li, Xiaoping Zhang, Lixin Zhang, Xueting Liu
No abstract text is available yet for this article.
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074053/identification-of-pyripyropene-a-as-a-promising-insecticidal-compound-in-a-microbial-metabolite-screening
#12
Ryo Horikoshi, Kimihiko Goto, Masaaki Mitomi, Kazuhiko Oyama, Toshiaki Sunazuka, Satoshi Omacr Mura
Approximately 300 microbial natural products in our library were screened for insecticidal activities against three species of agricultural pests, including aphids. Among the several compounds that showed insecticidal activities, pyripyropene A had high aphicidal activity in vivo. Furthermore, in advanced tests, pyripyropene A applications with foliar sprays and soil drenching controlled aphids on cabbage. On the basis of its unique and promising activities, we selected pyripyropene A as the active component of potential insecticides...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074052/kribellosides-novel-rna-5-triphosphatase-inhibitors-from-the-rare-actinomycete-kribbella-sp-mi481-42f6
#13
Masayuki Igarashi, Ryuichi Sawa, Manabu Yamasaki, Chigusa Hayashi, Maya Umekita, Masaki Hatano, Toshinobu Fujiwara, Kiyohisa Mizumoto, Akio Nomoto
Yeast capping enzymes differ greatly from those of mammalian, both structurally and mechanistically. Yeast-type capping enzyme repressors are therefore candidate antifungal drugs. The 5'-guanine-N7 cap structure of mRNAs are an essential feature of all eukaryotic organisms examined to date and is the first co-transcriptional modification of cellular pre-messenger RNA. Inhibitors of the RNA 5'-triphosphatase in yeast are likely to show fungicidal effects against pathogenic yeast such as Candida. We discovered a new RNA 5'-triphosphatase inhibitor, designated as the kribellosides, by screening metabolites from actinomycetes...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074051/anti-folates-potentiate-bactericidal-effects-of-other-antimicrobial-agents
#14
Kun Li, Xu-de Wang, Shan-Shan Yang, Jing Gu, Jiao-Yu Deng, Xian-En Zhang
Synergies between sulfonamides and other antimicrobial agents have long been reported, but the reason still remains unclear. Previously, Vilchèze et al. found that, sulfamethoxazole (SMX) could potentiate the bacterialcidal activity of isoniazid (INH) and rifampin (RIF) in Mycobacterium tuberculosis. To test if this was also the case in other bacteria, the ability to potentiate bactericidal effect of RIF by SMX was evaluated in Escherichia coli, Staphylococcus aureus, Salmonella typhimurium and Mycobacterium smegmatis...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074050/enhanced-dereplication-of-fungal-cultures-via-use-of-mass-defect-filtering
#15
Noemi D Paguigan, Tamam El-Elimat, Diana Kao, Huzefa A Raja, Cedric J Pearce, Nicholas H Oberlies
Effective and rapid dereplication is a hallmark of present-day drug discovery from natural sources. This project strove to both decrease the time and expand the structural diversity associated with dereplication methodologies. A 5 min liquid chromatographic run time employing heated electrospray ionization (HESI) was evaluated to determine whether it could be used as a faster alternative over the 10 min ESI method we reported previously. Results revealed that the 5 min method was as sensitive as the 10 min method and, obviously, was twice as fast...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074049/in-vitro-antibacterial-activity-of-%C3%AE-methoxyimino-acylide-derivatives-against-macrolide-resistant-pathogens-and-mutation-analysis-in-23s-rrna
#16
Hiroyuki Sugiyama, Ippei Yoshida, Mayumi Ueki, Katsuhiko Tanabe, Akira Manaka, Keiichi Hiramatsu
We characterized in vitro activities of α-methoxyimino acylides against macrolide-resistant clinical isolates of Streptococcus pneumoniae, Streptococcus pyogenes and Mycoplasma pneumoniae with ribosome modification or substitution and selected acylide-resistant mutants to clarify the binding point of the acylides. The acylides had low MICs against erm(B) gene-containing S. pneumoniae and S. pyogenes (MIC90s, 1-4 μg ml(-1)). For M. pneumoniae, although they had poor potencies against macrolide-resistant strains with the A2058G (Escherichia coli numbering) mutation in 23S rRNA (MICs, >32 μg ml(-1)), one of them showed in vitro activities against macrolide-resistant strains with the A2058U or A2059G mutations (MICs, 0...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074048/elmenols-c-h-new-angucycline-derivatives-isolated-from-a-culture-of-streptomyces-sp-ifm-11490
#17
Yixizhuoma, Naoki Ishikawa, Mohamed S Abdelfattah, Masami Ishibashi
Chemical investigations of the ethyl acetate extract of Streptomyces sp. IFM 11490 have led to the isolation of six new angucycline metabolites, named elmenols C-H (1-6), along with the previously reported elmonin (7) and elmenols A (8) and B (9). The known LS1924A (10), 6-deoxy-8-methylrabelomycin (11), tetrangulol methyl ether (12) and angucyclinone (13) were additionally identified. The structures of the isolated compounds were elucidated by means of spectroscopic methods including UV, IR, HRESIMS, and 1D and 2D NMR...
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28074047/arabilin-overcomes-resistance-to-ar-targeted-therapy
#18
Takahiro Fujimaki, Shun Saito, Masaya Imoto
No abstract text is available yet for this article.
January 11, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/27999446/antimicrobial-activity-and-interactions-of-cationic-peptides-derived-from-galleria-mellonella-cecropin-d-like-peptide-with-model-membranes
#19
José Oñate-Garzón, Marcela Manrique-Moreno, Steven Trier, Chad Leidy, Rodrigo Torres, Edwin Patiño
Antimicrobial peptides are effector molecules of the innate immune system against invading pathogens. The cationic charge in their structures has a strong correlation with antimicrobial activity, being responsible for the initial electrostatic interaction between peptides and the anionic microbial surface. This paper contains evidence that charge modification in the neutral peptide Gm cecropin D-like (WT) improved the antimicrobial activity of the modified peptides. Two cationic peptides derived from WT sequence named as ΔM1 and ΔM2, with net charge of +5 and +9, respectively, showed at least an eightfold increase in their antimicrobial activity in comparison to WT...
December 21, 2016: Journal of Antibiotics
https://www.readbyqxmd.com/read/27999445/identification-of-new-geldanamycin-derivatives-from-unexplored-microbial-culture-extracts-using-a-ms-ms-library
#20
Jae Kyoung Lee, Jae-Hyuk Jang, Dong-Jin Park, Chang-Jin Kim, Jong Seog Ahn, Bang Yeon Hwang, Young-Soo Hong
No abstract text is available yet for this article.
December 21, 2016: Journal of Antibiotics
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