Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5.
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.
Hegde
Vinod R
VR
Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. vinod.hegde@spcorp.com
Chan
T-M
TM
Pu
Haiyan
H
Gullo
Vincent P
VP
Patel
Mahesh G
MG
Das
Pradip
P
Wagner
Nicole
N
Parameswaran
P S
PS
Naik
C G
CG
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*
D065100:CCR5 Receptor Antagonists; D006027:Glycosides; D007202:Indicators and Reagents; D014020:Tissue Extracts; D014315:Triterpenes