title: Anticomplement triterpenoids from the roots of Ilex asprella.
abstract: Five new (1-5) and twenty-eight known (6-33) triterpenoids were isolated from the roots of Ilex asprella. The structures of the new compounds were elucidated by the detailed spectral analysis. The ursane and oleanane triterpenoids were found to show anticomplement activity with some structure-activity relationships. Several triterpenoids (1-3, 6-7) exhibited potent anticomplement activity with the CH50and AP50values of 0.058-0.131mg/mL and 0.080-0.444mg/mL, respectively. It was found that caffeoyl group could enhance activity remarkably, followed by coumaroyl and feruloyl group. The 28-carboxyl group was also important to anticomplement activity for the triterpenoids. However, the triterpenoids with lactone ring (4, 9-14) exhibited weak activity and triterpenoid glycosides (5, 23-33) showed no inhibition. The targets of several bioactive triterpenoids in complement activation cascade were identified as well.
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, PR China.
authors.forename: Quan
authors.initials: Q
authors.lastname: Wen
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Lu
authors.affiliation: School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, PR China.
authors.forename: Zhi
authors.initials: Z
authors.lastname: Chao
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, PR China. Electronic address: dfchen@shmu.edu.cn.
authors.forename: Dao-Feng
authors.initials: DF
authors.lastname: Chen
mesh_terms: D000818:Animals; D003169:Complement Inactivator Proteins / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D004912:Erythrocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D006461:Hemolysis / Q000187:drug effects; D030017:Ilex / Q000737:chemistry* / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000737:chemistry; D018517:Plant Roots / Q000737:chemistry / Q000378:metabolism; D012756:Sheep; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D053978:Pentacyclic Triterpenes
chemical_list: D003169:Complement Inactivator Proteins; D009828:Oleanolic Acid; D014315:Triterpenes; C012749:anticomplement; C413246:oleanane; C000606873:ursane; D053978:Pentacyclic Triterpenes
keywords: Anticomplement; Ilex asprella; Oleanane-type; Triterpenoids; Ursane-type