title: LAT Transport Inhibitors from Pittosporum venulosum Identified by NMR Fingerprint Analysis.
abstract: (1)H NMR fingerprints were used as the guiding principle for the isolation of minor compounds related to the l-type amino acid transporter inhibitors venulosides A (1) and B (2). Two new monoterpene glycosides, namely, venulosides C (3) and D (4), were isolated from a Queensland collection of the plant Pittosporum venulosum. Compounds 3 and 4 were found to inhibit l-leucine transport in LNCaP cells with IC50 values of 11.47 and 39.73 μM, respectively. The venulosides are the first reported natural product inhibitors of leucine transport in prostate cancer cells, and the isolation of the minor compounds provides some early SAR information.
authors.affiliation: †Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Tanja
authors.initials: T
authors.lastname: Grkovic
authors.affiliation: †Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Rebecca H
authors.initials: RH
authors.lastname: Pouwer
authors.affiliation: ⊥Sydney Medical School, University of Sydney, Sydney, NSW 2006, Australia.
authors.forename: Qian
authors.initials: Q
authors.lastname: Wang
authors.affiliation: ∥Queensland Herbarium, Department of Science, Information Technology and the Arts, Brisbane Botanic Gardens, Brisbane, QLD 4066, Australia.
authors.forename: Gordon P
authors.initials: GP
authors.lastname: Guymer
authors.affiliation: ⊥Sydney Medical School, University of Sydney, Sydney, NSW 2006, Australia.
authors.forename: Jeff
authors.initials: J
authors.lastname: Holst
authors.affiliation: †Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia.
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Quinn
mesh_terms: D026905:Amino Acid Transport Systems / Q000737:chemistry*; D000596:Amino Acids / Q000378:metabolism*; D001692:Biological Transport; D006027:Glycosides / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D027283:Large Neutral Amino Acid-Transporter 1; D007930:Leucine / Q000378:metabolism*; D008297:Male; D015394:Molecular Structure; D039821:Monoterpenes / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology*; D019906:Nuclear Magnetic Resonance, Biomolecular; D019685:Rosales / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D026905:Amino Acid Transport Systems; D000596:Amino Acids; C000600629:ESK242; C000600628:ESK246; D006027:Glycosides; D027283:Large Neutral Amino Acid-Transporter 1; D039821:Monoterpenes; C000601016:venuloside C; D007930:Leucine