A5012209412- Marine Sponges and Natural Products
- Microbial Natural Products and Biosynthesis
- Traditional and Medicinal Uses of Annonaceae
- Chemical synthesis and alkaloids
- Computational Drug Discovery Methods
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Biological Activity
- Synthetic Organic Chemistry Methods
- Natural product bioactivities and synthesis
- Alkaloids: synthesis and pharmacology
- Adenosine and Purinergic Signaling
- Chemical Synthesis and Analysis
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Biological Evaluation
- Plant biochemistry and biosynthesis
- Bioactive Compounds and Antitumor Agents
- Metabolomics and Mass Spectrometry Studies
- Phytochemical compounds biological activities
- Phytochemistry and Biological Activities
- Synthesis and Catalytic Reactions
- Carbohydrate Chemistry and Synthesis
- Marine Toxins and Detection Methods
- Malaria Research and Control
- Mass Spectrometry Techniques and Applications
Griffith University
2016-2025
Peter Doherty Institute
2021
The University of Melbourne
2021
IP Australia
2020
Brisbane School of Theology
2014-2019
University of the Sunshine Coast
2016
Central Washington University
2014
Shanghai Institute of Materia Medica
2013
Instytut Farmaceutyczny
2011
Queensland Museum
1999-2010
The X-ray crystal structure of the adduct between zinc metalloenzyme carbonic anhydrase II (CA, EC 4.2.1.1) with recently discovered natural product coumarin derivative 6-(1S-hydroxy-3-methylbutyl)-7-methoxy-2H-chromen-2-one showed hydrolysis product, a cis-2-hydroxy-cinnamic acid derivative, and not parent coumarin, bound within enzyme active site. inhibitor exhibits an extended, two-arm conformation that effectively plugs entrance to site no interactions catalytically crucial ion. is...
Maculotoxin, a potent neurotoxin isolated from the posterior salivary glands of blue-ringed octopus. Hapalochlaena maculosa, has now been identified as tetrodotoxin. This is first reported case in which tetrodotoxin found to occur venom.
With the aim of finding new natural product antimalarials, novel indole alkaloids flinderole A−C were found to have selective antimalarial activities with IC50 values between 0.15−1.42 μM. Flinderole A was isolated from Australian plant Flindersia acuminata and flinderoles B C Papua New Guinean F. amboinensis. Flinderoles contain an unprecedented rearranged skeleton compared their related isomers borreverine class compounds.
Addressing drug-like/lead-like properties of biologically active small molecules early in a lead generation program is the current paradigm within drug discovery community. Lipinski's "rule five" has become most commonly used tool to assess relationship between structures and drug-like properties. Sixty percent 126 140 unique compounds The Dictionary Natural Products had no violations five". We have isolated 814 natural products based on their expected generate product library (NPL) which...
While natural products or their derivatives and mimics have contributed around 50% of current drugs, there has been no approach allowing front-loading chemical space compliant with lead- drug-like properties. The importance physicochemical properties molecules in the development orally bioavailable drugs recognized. Classical product drug discovery only able to undertake this analysis retrospectively after compounds are isolated structures elucidated. present addresses both extracts...
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...
The rate at which genome sequencing data is accruing demands enhanced methods for functional annotation and metabolism discovery. Solute binding proteins (SBPs) facilitate the transport of first reactant in a metabolic pathway, thereby constraining regions chemical space chemistries that must be considered pathway reconstruction. We describe high-throughput protein production differential scanning fluorimetry platforms, enabled screening 158 SBPs against 189 component library specifically...
// Martin C. Sadowski 1 , Rebecca H. Pouwer 2 Jennifer Gunter Amy A. Lubik 1,3 Ronald J. Quinn and Colleen Nelson Australian Prostate Cancer Research Centre - Queensland, Institute of Health Biomedical Innovation, Queensland University Technology, Princess Alexandra Hospital, Translational Institute, Brisbane, Australia Eskitis for Drug Discovery, Griffith University, 3 Vancouver Centre, Department Urologic Sciences, British Columbia, Vancouver, Canada Correspondence: Nelson, email: Keywords...
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 genus Corydalis (Papaveraceae), comprising more than 400 species in Eurasia and North America, is a rich source of isoquinoline alkaloids with various biological properties including acetylcholinesterase inhibitory effects, anti-proliferative activities, antiviral activities antiplasmodial activities. Traditionally, some have long been used to treat gastric duodenal ulcers, dysmenorrhoea, rheumatism cardiac arrhythmia disease this traditional background so far has proven pharmacological...
The authors describe first a proof-of-concept experiment to show direct affinity screening using electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry (ESI-FTICR-MS) is rapid and informative approach for natural product extract screening.The study used 10 alkaloid-enriched plant extracts 8 desalted marine spiked with specific inhibitors of bovine carbonic anhydrase II (bCAII; EC4.2.1.1)as model set.The were incubated bCAII then analyzed by ESI-FTICR-MS.The...
The distribution of the P2X7 receptor in inflammatory cells suggests that antagonists have a significant role to play treatment disease. We conducted natural product high-throughput screening campaign discover antagonists. Australian marine sponge Stylissa flabellata yielded two new bisimidazo-pyrano-imidazole bromopyrrole ether alkaloids, stylissadines A (IC50 0.7 microM) and B 1.8 microM), as specific bioactive constituents. compounds inhibit BzATP-mediated pore formation THP-1 cells. Also...