title: Complement-inhibiting cucurbitacin glycosides from Picria fel-terrae.
abstract: Four cucurbitacin glycosides were isolated from Picriafel-terrae and identified by MS and NMR spectroscopy as picfeltarraenin IA (1), picfeltarraenin IB (2), picfeltarraenin IV (4), and a new compound picfeltarraenin VI (3) (picfeltarraegenin I 3-O-beta-D-xylopyranoside). All four compounds acted as inhibitors on both the classical and alternative pathways of the complement system, with compound 3 exhibiting the highest inhibitory activity (IC50 29 +/- 2 microM and 21 +/- 1 microM, respectively). Compounds 1-4 showed no antiviral, antibacterial, or antifungal activities. Picfeltarraenin IA and IB were tested in an in vitro human tumor cell line panel, but displayed no cytotoxic activity.
authors.affiliation: Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
authors.forename: Y
authors.initials: Y
authors.lastname: Huang
authors.forename: T
authors.initials: T
authors.lastname: De Bruyne
authors.forename: S
authors.initials: S
authors.lastname: Apers
authors.forename: Y
authors.initials: Y
authors.lastname: Ma
authors.forename: M
authors.initials: M
authors.lastname: Claeys
authors.forename: D
authors.initials: D
authors.lastname: Vanden Berghe
authors.forename: L
authors.initials: L
authors.lastname: Pieters
authors.forename: A
authors.initials: A
authors.lastname: Vlietinck
mesh_terms: D000890:Anti-Infective Agents / Q000302:isolation & purification / Q000494:pharmacology; D002681:China; D003169:Complement Inactivator Proteins / Q000302:isolation & purification* / Q000494:pharmacology*; D003170:Complement Pathway, Alternative / Q000187:drug effects; D003171:Complement Pathway, Classical / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D010946:Plants, Medicinal / Q000737:chemistry*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D014407:Tumor Cells, Cultured
chemical_list: D000890:Anti-Infective Agents; D003169:Complement Inactivator Proteins; D006027:Glycosides