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Journal of Antibiotics

Binglin Zhang, Shukun Tang, Ximing Chen, Gaoseng Zhang, Wei Zhang, Tuo Chen, Guangxiu Liu, Shiweng Li, Luciana Terra Dos Santos, Helena Carla Castro, Paul Facey, Matthew Hitchings, Paul Dyson
A novel actinobacterial strain, designated S10T , was isolated from a sand sample collected from the Qaidam Basin in Qinghai province, China. The strain S10T exhibited antibacterial activity against MRSA. The taxonomic position of the strain S10T was determined by a polyphasic approach. There were six copies of 16S rDNA in S10T which were not same exactly (MH257693-MH257698). Phylogenetic analysis of 16S rRNA gene sequences indicated the strain belonging to the genus Streptomyces and it showed high sequence similarities with Streptomyces chartreusis NBRC 12753T (99...
July 19, 2018: Journal of Antibiotics
Yoichi Hayakawa, Risako Sone, Haruna Aoki, Shoko Kimata
Two new cytotoxic antibiotics designated quinomycins H1 (2) and H2 (3) were isolated from the culture broth of Streptomyces sp. RAL404. The molecular formula of both compounds was established as C52 H65 N11 O13 S2 by electrospray ionization mass spectrometry (ESI-MS). Their structures were determined as echinomycin (1) derivatives containing a 3-hydoxyquinaldic acid molecule in place of one of the two quinoxaline-2-carboxylic acid chromophores. Quinomycins H1 (2) and H2 (3) showed selective cytotoxicity against RG-E1-4 cells bearing the adenovirus oncogenes with IC50 s of 11 nM and 12 nM, respectively...
July 17, 2018: Journal of Antibiotics
Daniela Rebollar-Ramos, Martha L Macías-Ruvalcaba, Mario Figueroa, Huzefa A Raja, Martín González-Andrade, Rachel Mata
From the rice-based culture of Malbranchea flavorosea, three new compounds namely flavoroseoside B (5-desoxy-5-chloro-flavoroseoside) (2), 4-hydroxy-2-O-α-ribofuranosyl-5-methylacetophenone (3), and (S)-3,4-dihydro-3-(1H-indol-3-ylmethyl)-4-methyl-1H-1,4-benzodiazepine-2,5-dione (4), along with three known compounds, rosigenin (5), massarilactone B (6), and riboxylarinol B (7) were obtained. The structures were determined by spectroscopic methods. Compound 4 and its synthetic analog 3,4-dihydro-3-(1H-indol-3-ylmethyl)-1-methyl-1H-1,4-benzodiazepine-2,5-dione (9) inhibited the activity of Ruminococus obeum α-glucosidase enzyme...
July 17, 2018: Journal of Antibiotics
Xiao-Dong Liu, Kang-Bo Gu, Sha-Sha Xia, Dao-Jing Zhang, Yuan-Guang Li
Two novel cyclopeptides with special skeleton, namely, dolyemycins A (1) and B (2) were isolated from Streptomyces griseus subsp. griseus HYS31 by bio-guided isolation. Their structures were elucidated by detailed analysis of spectroscopic data. These two compounds were cyclopeptides containing eleven amino acids including five unusual amino acids (hydroxyglycine, 3-hydroxyleucine, 3-phenylserine, β-hydroxy-O-methyltyrosine, 2,3-diaminobutyric acid) in both of them and an extra nonprotein amino acids (3-methylaspartic acid) in Dolyemycin B only...
July 6, 2018: Journal of Antibiotics
Wataru Kitagawa, Shinya Mitsuhashi, Miyako Hata, Tomohiro Tamura
A novel bacteriocin-like protein and its structural gene (rap) were identified from Rhodococcus erythropolis JCM 2895. The rapA and B genes are located on a 5.4-kb circular plasmid, and were obtained using a modified suppression-subtractive hybridization method. The rapA and B genes were heterologously expressed in Rhodococcus sp. or Escherichia coli, and then characterized. The results indicated that RapA is a small, water-soluble, heat-stable antimicrobial protein, and that RapB is an immunity protein against RapA, estimated to be located on the cell membrane...
July 6, 2018: Journal of Antibiotics
Dewu Zhang, Jianyuan Zhao, Xinwei Wang, Lili Zhao, Hongyu Liu, Yuzhen Wei, Xuefu You, Shan Cen, Liyan Yu
A new azaphilone derivative, named peniazaphilin A (1) and one known isocoumarin, (R)-3-methyl-6-hydroxy-8-methoxy-3,4-dihydroisocoumarin (2) were isolated from the fungus Penicillium sp. CPCC 400786. Their structures were elucidated by means of extensive spectroscopic analysis. The absolute configuration of 2 was established by circular dichroism for the first time. Compounds 1 and 2 exhibited weak anti-HIV activities with the IC50 values of 60.4 and 69.3 μM, respectively.
July 5, 2018: Journal of Antibiotics
Lijian Ding, Te Li, Xiaojian Liao, Shan He, Shihai Xu
Three new itaconic acid derivatives, asperitaconic acids A-C (1-3), were isolated from the ethyl acetate extracts of the rice fermentation of a marine-derived fungus Aspergillus niger, and asperitaconic acids A-C were characterized by an itaconic acid unit and an alkyl chain moiety. Their structures were established by interpretation of their spectroscopic data including NMR and HRESIMS. Asperitaconic acids A-C exhibited antibacterial effect against Staphylococcus aureus with MIC values of 16-32 μg/mL, whereas these compounds showed no cytotoxicity against HepG2 and HeLa cancer cell lines...
July 4, 2018: Journal of Antibiotics
Shohei Ueda, Shigeru Kitani, Takushi Namba, Masayoshi Arai, Haruo Ikeda, Takuya Nihira
β-Carboline alkaloids and related compounds show a broad spectrum of biological activities. We previously identified new members of the β-carboline alkaloid family by using an engineered Kitasatospora setae strain and a heterologous Streptomyces host expressing the plausible biosynthetic genes, including the hypothetical gene kse_70640 (kslB). Here, we elucidated the chemical structure of a new tetrahydro-β-carboline compound (named kitasetalic acid) that appeared in a heterologous Streptomyces host expressing the kslB gene alone...
July 4, 2018: Journal of Antibiotics
Yuanzheng Zhou, Yuan Ju, Yang Yang, Zitai Sang, Zhenling Wang, Gu He, Tao Yang, Youfu Luo
With antibiotics resistance developing rapidly, new antibacterial agents are needed to be discovered. We readily synthesized 11 indolin-2-one compounds and found a hybrid of indolin-2-one and nitroimidazole 3-((1-methyl-5-nitro-1H-imidazol-2-yl)methylene)indolin-2-one to be effective on Staphylococcus aureus strains. Six derivatives of this compound were further designed and synthesized in order to enhance its efficacy. After a second turn of structural refinement, a novel hybrid of indolin-2-one and nitroimidazole 3-((1-methyl-5-nitro-1H-imidazol-2-yl)methylene)-5-nitroindolin-2-one with a nitro group on C-5 position of indolin-2-one was shown to exhibit remarkable antibacterial activities with a low MIC value against MRSA ATCC 33591...
July 3, 2018: Journal of Antibiotics
Tran Hong Quang, Dong Cheol Kim, Phan Van Kiem, Chau Van Minh, Nguyen Xuan Nhiem, Bui Huu Tai, Pham Hai Yen, Nguyen Thi Thanh Ngan, Hye Jin Kim, Hyuncheol Oh
Five new secondary metabolites, modiolides D-G (1-4) and 1-(2,5-dihydroxyphenyl)-3-methoxy-butan-1-one (8), one new natural product, 1-(2,5-dihydroxyphenyl)-3-hydroxybutan-1-one (7), along with three known compounds, modiolides A (5) and B (6), and 1-(2,5-dihydroxyphenyl)-2-buten-1-one (9) were isolated from a fermentation culture of the marine endophytic fungus Paraconiothyrium sp. VK-13. Their chemical structures were elucidated by the NMR and MS spectroscopic analysis as well as the modified Mosher's method...
June 26, 2018: Journal of Antibiotics
Satoshi Ōmura, Yukihiro Asami, Andy Crump
Staurosporine, together with such examples as penicillin, aspirin, ivermectin and sildenafil, exemplifies the role that serendipity has in drug discovery and why 'finding things without actually searching for them' retains a prominent role in drug discovery. Hitherto not clinically useful, due to its potency and promiscuity, new delivery technology is opening up new horizons for what was previously just the parent compound of innovative, highly-successful anti-cancer agents.
June 22, 2018: Journal of Antibiotics
Ikuro Abe
Teleocidin B, with its unique indolactam-terpenoid scaffold, is a potent activator of protein kinase C. This short review summarizes our recent research progress on the biosynthesis of teleocidins in Streptomyces blastmyceticus NBRC 12747. We first identified the biosynthetic genes for teleocidin B, which include genes encoding a non-ribosomal peptide synthetase (tleA), a cytochrome P450 monooxygenase (tleB), an indol prenyltransferase (tleC), and a C-methyltransferase (tleD). Notably, the tleD gene is located outside the tleABC cluster...
June 14, 2018: Journal of Antibiotics
Shamil Sh Afiyatullov, Olesya I Zhuravleva, Alexandr S Antonov, Dmitrii V Berdyshev, Mikhail V Pivkin, Vladimir A Denisenko, Roman S Popov, Andrey V Gerasimenko, Gunhild von Amsberg, Sergey A Dyshlovoy, Elena V Leshchenko, Anton N Yurchenko
Five new prenylated indole alkaloids, 17-hydroxynotoamide D (1), 17-O-ethylnotoamide M (2), 10-O-acetylsclerotiamide (3), 10-O-ethylsclerotiamide (4), and 10-O-ethylnotoamide R (5) were isolated from a co-culture of marine-derived fungi Aspergillus sulphureus KMM 4640 and Isaria felina KMM 4639. The structures of 1-5 were determined by detailed analysis of spectroscopic data and by comparison with related known compounds. The absolute configurations of 1-5 were determined by time-dependent density functional theory (TD-DFT) calculations of ECD spectra...
June 8, 2018: Journal of Antibiotics
Yoshimasa Ishizaki, Yuko Shibuya, Chigusa Hayashi, Kunio Inoue, Teruo Kirikae, Tatsuya Tada, Tohru Miyoshi-Akiyama, Masayuki Igarashi
The NpmA bacterial 16S rRNA methyltransferase, which is identified from Escherichia coli strains, confers high resistance to many types of aminoglycoside upon its host cells. But despite its resistance-conferring ability, only two cases of its isolation from E. coli (14 years apart) have been reported to date. Here, we investigated the effect of the npmA gene on aminoglycoside resistance in Pseudomonas aeruginosa and Klebsiella pneumoniae and its stability in E. coli cells by comparing it with armA, another 16S rRNA methyltransferase gene currently spreading globally...
June 8, 2018: Journal of Antibiotics
Martin A Makary, Katerina Kaczmarski, Keeve Nachman
No abstract text is available yet for this article.
May 31, 2018: Journal of Antibiotics
Angelo Iacobino, Federico Giannoni, Lanfranco Fattorini, Federico Brucoli
Mycobacterium tuberculosis (Mtb) is the aetiological agent of tuberculosis, the leading cause of death worldwide from a single infectious agent. Mtb is a highly adaptable human pathogen that might enter a dormant non-replicating (NR), drug-tolerant stage. Reactivation of dormant Mtb can lead to active disease. Antibiotic treatments of active and latent tuberculosis are long, complex and may fail to fully eradicate the infection. Therefore, it is imperative to identify novel compounds with new mechanisms of action active against NR bacilli...
May 24, 2018: Journal of Antibiotics
Kimihiko Goto, Ryo Horikoshi, Masaaki Mitomi, Kazuhiko Oyama, Tomoyasu Hirose, Toshiaki Sunazuka, Satoshi Ōmura
The C-1, C-7, and C-11 positions of pyripyropene A were chemically modified to improve the insecticidal activity. Some derivatives showed higher insecticidal activities against aphids than pyripyropene A. In particular, the derivative 5c, which possesses three cyclopropyl carbonyl groups at the C-1, C-7, and C-11 positions, had excellent insecticidal activity levels in field and laboratory trials.
May 23, 2018: Journal of Antibiotics
Yuting Zhang, Li Liu, Li Bao, Yanlong Yang, Ke Ma, Hongwei Liu
Three new cyathane diterpenes erinacines T-V (1-3), and two known cyathane diterpenes erinacine A (4) and erinacine P (5) were isolated from the liquid cultures of Hericium erinaceus. The structures of 1-3 were determined by extensive spectroscopic analysis. All isolated compounds were evaluated for the cytotoxicity, and neurite-promoting activities using PC12 cell line. Compounds 1-3, and 5 exhibited pronounced neurite outgrowth-promoting effects on PC12 cells in the range of 2.5-10 μM. Compound 4 showed weak cytotoxicity against PC12 cells with IC50 of 73...
May 21, 2018: Journal of Antibiotics
Ji-Yul Kim, E-Eum Woo, In-Kyoung Lee, Bong-Sik Yun
In our effort to find antioxidants from the higher fungi, we isolated three new compounds (1-3) with a known compound, spirobenzofuran (4), from the culture broth of Hericium coralloides. Bioassay-guided fractionation led to the isolation of these compounds, and we determined the chemical structures through spectroscopic methods. These compounds exhibited antioxidant activity in the range of IC50 values of 29-66 μM in the 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical-scavenging assay...
May 17, 2018: Journal of Antibiotics
Jia Meng, Zheng Zhong, Pei-Yuan Qian
Four peptide antibiotics, named paenialvin A-D, were isolated from Paenibacillus alvei DSM 29. Mass spectrum analysis determined the molecular masses of paenialvin A-D to be 1891, 1875, 1877, and 1923 Da, respectively. Tandem mass spectra and nuclear magnetic resonance (NMR) were used to elucidate their chemical structures. Paenialvin A-D showed antimicrobial activity against most strains that were tested, including methicillin-resistant Staphalococcus aureus, Staphylococcus aureus, Bacillus subtilis, Loktanella hongkongensis, Escherichia coli, and Pseudomonas aeruginosa...
May 14, 2018: Journal of Antibiotics
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