A5103125714- Microbial Natural Products and Biosynthesis
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthetic Organic Chemistry Methods
- Genomics and Phylogenetic Studies
- Bioactive Compounds and Antitumor Agents
- Crystallography and molecular interactions
- RNA and protein synthesis mechanisms
- Chemical Synthesis and Analysis
- Natural product bioactivities and synthesis
- Marine Sponges and Natural Products
- Plant-Microbe Interactions and Immunity
- Antibiotic Resistance in Bacteria
- Cancer Cells and Metastasis
- Computational Drug Discovery Methods
- Lanthanide and Transition Metal Complexes
- Peptidase Inhibition and Analysis
- Carbohydrate Chemistry and Synthesis
- Plant Disease Resistance and Genetics
- Metal-Catalyzed Oxygenation Mechanisms
- Pesticide and Herbicide Environmental Studies
- Biochemical and Structural Characterization
- Ubiquitin and proteasome pathways
- Tuberculosis Research and Epidemiology
- Bacterial Genetics and Biotechnology
Microbial Chemistry Research Foundation
2014-2024
Kyoto University
2015
Kindai University
2004-2005
Tokyo Metropolitan University
2004
ABSTRACT The WalK (histidine kinase)/WalR (response regulator) two-component signal transduction system is a master regulatory for cell wall metabolism and growth. This conserved in low G+C Gram-positive bacteria, including Bacillus subtilis , Staphylococcus aureus Enterococcus faecalis Streptococcus mutans . In this study, we found the first antibiotic that functions as inhibitor (signermycin B) by screening 10,000 Streptomyces extracts. chemical structure (C 23 H 35 NO 4 ; molecular...
Abstract The abuse of antibacterial drugs imposes a selection pressure on bacteria that has driven the evolution multidrug resistance in many pathogens. Our efforts to discover novel classes antibiotics combat these pathogens resulted discovery amycolamicin (AMM). absolute structure AMM was determined by NMR spectroscopy, X‐ray analysis, chemical degradation, and modification its functional groups. consists trans ‐decalin, tetramic acid, two unusual sugars (amycolose amykitanose),...
The histone acetyltransferase (HAT) activity of p300 is essential for androgen receptor (AR) function. Androgen-independent prostate cancer cells require AR-mediated transcriptional activation their growth. These observations indicate that HAT a promising target to overcome such hormone-resistant cells. We sought inhibitors among microbial metabolites. By culturing production strain belonging Penicillium, we identified two new compounds, NK13650A and NK13650B, which were obtained as specific...
Two novel siderophores, chlorocatechelins A and B, were isolated from a culture broth of Streptomyces sp. Their structures determined by spectroscopic analysis degradation study. They contain chloro-substituted catecholate that has not been reported in natural products, whereas this group was conjugated to guanidine form acylguanidine chlorocatechelin A. This decomposed weakly acidic solutions furnish less potent siderophore B. Chemical biological insights into are also discussed.
New 36-membered polyol macrolides deplelides A and B were isolated from the culture of Streptomyces MM581-NF15 by bioassay-guided fractionation using an ATP depletion assay. The planar structures these novel compounds identified interpretation spectroscopic data (1D/2D NMR, MS, IR). relative stereochemistry was partially established universal NMR database method J-based configuration analysis 1H–1H long-range 1H–13C coupling constants determined 1H or E.COSY J-resolved HMBC another...
The preparation and physical characterization are reported for a novel single-molecule magnet [Mn(12)O(12)(OAc)(12)(dpp)(4)] (dppH = diphenyl phosphate) with no coordinating water molecules. crystal structure analysis reveals that there four five-coordinate Mn(III) ions Mn.H approaches. Addition of in CD(2)Cl(2) solution was monitored by (1)H NMR, which showed H(2)O could coordinate to vacant site ion solution. measurements analyses magnetization hysteresis ac magnetic susceptibility...
Chlorocatechelin A (1) is a structurally unique microbial siderophore containing two units of 4-chloro-2,3-dihydroxybenzoic acid (CDB) and characteristic acylguanidine structure. Purification from the microbe culture not an easy task due to lability its chelating nature. Here we report first convergent total synthesis antimicrobial activity chlorocatechelin (1). The bis-acylated arginine was constructed using Schotten-Baumann reaction whereas CDB component synthesized o-vanillin (8)....
Trehalose has widespread use as a sweetener, humectant and stabilizer, is now attracting attention promising candidate for the treatment of neurodegenerative diseases it an autophagy inducer chemical chaperone. However, bioavailability trehalose low because digested by hydrolyzing enzyme trehalase, expressed in intestine kidney. Enzyme-stable analogs would potentially solve this problem. We have previously reported enzyme-stable analog trehalose, lentztrehalose, herein report two new...
ABSTRACT Tropolone, a phytotoxin produced by Burkholderia plantarii , causes rice seedling blight. To identify genes involved in tropolone synthesis, we systematically constructed mutations the encoding 55 histidine kinases and 72 response regulators. From resulting defective strains, isolated three mutants, KE1, KE2, KE3, which production was repressed. The deleted of these mutants were named troR1 troK troR2 respectively. mutant strains did not cause blight, complementation experiments...
The increasing burden and spread of resistant malaria parasites remains an immense to public health. These factors have driven the demand search for a new therapeutic agent. From our screening, phebestin stood out with nanomolar efficacy against Plasmodium falciparum 3D7. Phebestin was initially identified as aminopeptidase N inhibitor. inhibited in vitro multiplication P. 3D7 (chloroquine-sensitive) K1 (chloroquine-resistant) strains at IC50 values 157.90 ± 6.26 nM 268.17 67.59 nM,...
Tuberculosis (TB) is a serious infectious disease caused by bacterial pathogen. Mortality from tuberculosis was estimated at 1.5 million deaths worldwide in 2013. Development of new TB drugs needed to not only shorten the medication period but also treat multi-drug resistant and extensively drug-resistant TB. Mycobacterium (Mtb) grows slowly multiplies once or twice per day. Therefore, conventional drug screening takes more than 3 weeks. Additionally, biosafety level-3 (BSL-3) facility...
Natural products have contributed to the elucidation of biological mechanisms as well drug discovery research. Even now, expectation for natural is undiminished. We screened prostaglandin release inhibitors that had no effect on in vitro cyclooxygenase activity derived from product sources and discovered pronqodine A. Using spectral analysis total synthesis, structure A was shown be a benzo[d]isothiazole-4,7-dione analogue. Evaluation revealed NAD(P)H dehydrogenase quinone 1 (NQO1) converted...
The first total synthesis of pactalactam was accomplished using substrate-controlled stereoselective aziridination and regioselective aziridine ring-opening to construct three continuous amino groups on an octasubstituted cyclopentane core. framework obtained by ring-closing metathesis aldol coupling a l-threonine-derived oxazoline compound. Cyclic urea formation, m-acetylphenyl group introduction Chan–Lam coupling, primary alcohol-selective acylation yielded the reported structure. presence...
A novel actinomycete, designated MI503-A4T, was isolated from soil. Comparative analysis of 16S rRNA gene sequences indicated that MI503-A4T phylogenetically related to members the family Pseudonocardiaceae. The most closely genus Kibdelosporangium (95.7-96.2 % sequence similarity). Substrate mycelia were branched and pale yellow yellowish-brown. Straight- zigzag-shaped aerial observed, but Sporangium-like structures absent. whole-cell hydrolysate contained meso-diaminopimelic acid. muramic...
Sacchathridine A (1) was isolated from the fermentation broth of strain Saccharothrix sp. MI559-46F5. The structure determined as a new naphthoquinone derivative with an acetylhydrazino moiety by combination NMR, MS spectral analyses, and chemical degradation. Compound 1 showed inhibitory activity prostaglandin E2 release in concentration-dependent manner human synovial sarcoma cells, SW982, IC50 value 1.0 μM, but had no effect on cell growth up to 30 μM.