A5058286128- Marine Sponges and Natural Products
- Microbial Natural Products and Biosynthesis
- Chemical synthesis and alkaloids
- Synthetic Organic Chemistry Methods
- Traditional and Medicinal Uses of Annonaceae
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Biological Activity
- Computational Drug Discovery Methods
- Genetics, Bioinformatics, and Biomedical Research
- Microbial Metabolism and Applications
- Genomics and Phylogenetic Studies
- Synthesis of heterocyclic compounds
- Cancer, Hypoxia, and Metabolism
- Insect and Pesticide Research
- Metabolomics and Mass Spectrometry Studies
- Plant biochemistry and biosynthesis
- Carbohydrate Chemistry and Synthesis
- Phytochemistry and Bioactive Compounds
- Enzyme function and inhibition
- Asymmetric Synthesis and Catalysis
- Cancer therapeutics and mechanisms
- Plant-Derived Bioactive Compounds
- Electron Spin Resonance Studies
- Bee Products Chemical Analysis
National Cancer Institute
2011-2025
Center for Cancer Research
2011-2025
Target (United States)
2011-2024
Frederick National Laboratory for Cancer Research
2012-2020
Leidos (United States)
2015-2020
Leidos Biomedical Research Inc. (United States)
2020
Frederick Community College
2020
Griffith University
2011-2017
University of Auckland
2006-2016
University of Canterbury
2010
A comprehensive review of 1411 new MNPs and their structural diversity analysis including the cyanobacterial metabolite lezoside.
High resolution Fourier transform mass spectrometry (HRFTMS) and nuclear magnetic resonance (NMR) spectroscopy were employed as complementary metabolomic tools to dereplicate the chemical profile of new antitrypanosomally active sponge-associated bacterium Actinokineospora sp. EG49 extract. Principal Component (PCA), hierarchical clustering (HCA), orthogonal partial least square-discriminant analysis (OPLS-DA) used evaluate HRFTMS NMR data crude extracts from four different fermentation...
Two sponge-derived actinomycetes, Actinokineospora sp. EG49 and Nocardiopsis RV163, were grown in co-culture the presence of induced metabolites monitored by 1H NMR. Ten known compounds, including angucycline, diketopiperazine β-carboline derivatives 1–10, isolated from EtOAc extracts RV163. Co-cultivation RV163 biosynthesis three natural products that not detected single culture either microorganism, namely N-(2-hydroxyphenyl)-acetamide (11), 1,6-dihydroxyphenazine (12)...
The US National Cancer Institute's (NCI) Natural Product Repository is one of the world's largest, most diverse collections natural products containing over 230,000 unique extracts derived from plant, marine, and microbial organisms that have been collected biodiverse regions throughout world. Importantly, this national resource available to research community for screening isolation bioactive products. However, despite success in drug discovery, compatibility issues make challenging liquid...
An automated, high-capacity, and high-throughput procedure for the rapid isolation identification of biologically active natural products from a prefractionated library is presented. The semipreparative HPLC method uses 1 mg primary hit fraction produces 22 subfractions in an assay-ready format. Following screening, all fractions are analyzed by NMR, LCMS, FTIR, principle structural classes elucidated. In proof-of-concept study, we show processes involved generating subfractions, throughput...
Abstract The NMR spectrum of a mixture small molecules is fingerprint all its components. Herein, we present an method that takes advantage the fact fractions contain simplified profiles, with minimal signal overlap, to allow identification unique spectral patterns. approach exemplified in novel natural product, iotrochotazine A ( 1 ), sourced from Australian marine sponge Iotrochota sp. Compound was used as chemical probe phenotypic assay panel based on human olfactory neurosphere‐derived...
Inhibition of the hypoxia-inducible factor 1α (HIF-1α) pathway by disrupting its association with transcriptional coactivator p300 inhibits angiogenesis and tumor development. Development HIF-1α/p300 inhibitors has been hampered preclinical toxicity; therefore, we aimed to identify novel inhibitors. Using a cell-free assay designed test compounds that block binding, 170 298 crude natural product extracts prefractionated samples were screened, identifying 25 active extracts. One these...
The continuing emergence of antibiotic-resistant microbes highlights the need for identification new chemotypes with antimicrobial activity. One most prolific sources molecules has been systematic screening natural product samples. National Institute Allergy and Infectious Diseases Cancer here report a large screen 326,656 partially purified fractions against panel four microbial pathogens, resulting in >3000 antifungal and/or antibacterial A small sample these active was further chemical...
A high-throughput cell-based reporter assay designed to identify small-molecule stabilizers of the tumor suppressor Pdcd4 was used screen extracts in NCI Natural Products Repository. Bioassay-guided fractionation an extract from a Papua New Guinea collection tropical tree Cryptocarya sp. provided series new 5,6-dihydro-α-pyrone-containing 1,3-polyols (1–8), named cryptocaryols A–H. Their structures were assigned combination NMR, MS, and CD studies conjunction with NMR database comparisons....
The metabolite profiles of three sponge-derived actinomycetes, namely, Micromonospora sp. RV43, Rhodococcus RV157, and Actinokineospora EG49 were investigated after elicitation with N-acetyl-d-glucosamine. 1H NMR fingerprint methodology was utilized to study the differences in metabolic bacterial extracts before elicitation. Our found that addition N-acetyl-d-glucosamine modified secondary actinomycete isolates. N-Acetyl-d-glucosamine induced production 3-formylindole (11) guaymasol (12)...
Pyrrole-containing natural products form a large group of structurally diverse compounds that occur in both terrestrial and marine organisms. In the present study formation trideuteromethylated artifacts pyrrole-containing was investigated, focusing on discorhabdins. Three deuterated discorhabdins, 1, 3, 5, were identified to be isolation procedure caused by presence DMSO-d6 during NMR sample preparation handling. additional semisynthetic derivatives, 7–9, made investigation mechanism...
Enantiomeric pairs of the cytotoxic pyrroloiminoquinone marine alkaloids discorhabdins B (2), G*/I (3), L (4), and W (5) have been isolated from Latrunculia species sponges collected at different locations around coast New Zealand. The absolute configuration all compounds was secured by comparison observed data with results time-dependent density functional theory (TDDFT) calculations electronic circular dichroism (ECD) spectra. exhibit equipotent antiproliferative biological activity.
Investigations of four different sponge populations Latrunculia species collected in New Zealand waters has led to the characterization a new diastereomer discorhabdin H, named H2, confirmation structure K ((+)-7), and presentation diastereomer, K2 ((−)-8). In each case structures were established by extensive NMR MS studies absolute configurations interrogated electronic circular dichroism (ECD). Absolute assigned known metabolites discorhabdins D, 2-hydroxy-D, N, Q comparison ECD spectra...
The l-type amino acid transporter (LAT) family consists of four members (LAT1–4) that mediate uptake neutral acids including leucine. Leucine is not only important as a building block for proteins, but plays critical role in mTORC1 signaling leading to protein translation. As such, LAT are commonly upregulated cancer order fuel increased translation and cell growth. To identify potential LAT-specific inhibitors, we established function-based high-throughput screen using prefractionated...
The growing number of sequenced microbial genomes has revealed a remarkably large secondary metabolite biosynthetic clusters for which the compounds are still unknown. aim present work was to apply strategy detect newly induced natural products by cultivating microorganisms in different fermentation conditions. metabolomic analysis 4160 fractions generated from 13 actinomycetes under 32 culture conditions carried out 1H NMR spectroscopy and multivariate analysis. principal component (PCA)...