title: Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5.
abstract: The aqueous methanolic extract of a sea cucumber was found to contain two triterpene glycosides 1 and 2. The structures of 1 and 2 were established based on high-resolution NMR studies. Compounds 1 and 2 exhibited inhibitory activity (K(i)) of 30 and 5microM, respectively, in a chemokine receptor subtype 5 (CCR5) assay. Both compounds did not show any significant inhibition in a CXCR2 assay at 50microM, suggesting their selectivity for the CCR5 receptor.
authors.affiliation: Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. vinod.hegde@spcorp.com
authors.forename: Vinod R
authors.initials: VR
authors.lastname: Hegde
authors.forename: T-M
authors.initials: TM
authors.lastname: Chan
authors.forename: Haiyan
authors.initials: H
authors.lastname: Pu
authors.forename: Vincent P
authors.initials: VP
authors.lastname: Gullo
authors.forename: Mahesh G
authors.initials: MG
authors.lastname: Patel
authors.forename: Pradip
authors.initials: P
authors.lastname: Das
authors.forename: Nicole
authors.initials: N
authors.lastname: Wagner
authors.forename: P S
authors.initials: PS
authors.lastname: Parameswaran
authors.forename: C G
authors.initials: CG
authors.lastname: Naik
mesh_terms: D000818:Animals; D065100:CCR5 Receptor Antagonists; D006027:Glycosides / Q000302:isolation & purification / Q000494:pharmacology*; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D012616:Sea Cucumbers / Q000737:chemistry*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D014020:Tissue Extracts; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D065100:CCR5 Receptor Antagonists; D006027:Glycosides; D007202:Indicators and Reagents; D014020:Tissue Extracts; D014315:Triterpenes