6533b7d6fe1ef96bd1267269

RESEARCH PRODUCT

Trimeric Hemibastadin Congener from the Marine Sponge Ianthella basta

Peter ProkschWenhan LinWerner E.g. MüllerMichael H.g. KubbutatHendrik NiemannDaowan Lai

subject

StereochemistryPharmaceutical ScienceMarine BiologySesquibastadinAnalytical ChemistryMiceIanthella bastaDrug DiscoveryHalogenated Diphenyl EthersAnimalsNuclear Magnetic Resonance BiomolecularProtein Kinase InhibitorsPharmacologyMolecular StructurebiologyMurine lymphomaOrganic Chemistrybiology.organism_classificationPoriferaSpongeCongenerComplementary and alternative medicineIndonesiaMolecular MedicineDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopy

description

The first naturally occurring trimeric hemibastadin congener, sesquibastadin 1 (1), and the previously reported bastadins 3, 6, 7, 11, and 16 (2-6) were isolated from the marine sponge Ianthella basta, collected in Indonesia. The structure of 1 was elucidated on the basis of 1D and 2D NMR measurements and by HRMS. Among all the isolated compounds, the linear sesquibastadin 1 (1) and bastadin 3 (2) showed the strongest inhibition rates for at least 22 protein kinases (IC(50) = 0.1-6.5 μM), while the macrocyclic bastadins (3-6) demonstrated a strong cytotoxic potential against the murine lymphoma cell line L5178Y (IC(50) = 1.5-5.3 μM).

https://doi.org/10.1021/np300764u