title: Inhibitory effect of triterpenoid saponins from the leaves of Ilex kudingcha on aggregated LDL-induced lipid deposition in macrophages.
abstract: We have investigated the inhibitory effect of triterpenoid saponins from the leaves of Ilex kudingcha C. J. Tseng on aggregated low-density lipoprotein (LDL)-induced lipid deposition in macrophages. A cell-based screening model was initially applied on aggregated LDL (aggLDL)-induced lipid deposition on macrophages to test the inhibitory effects of the 12 triterpenoid saponins from this plant. Eight of these compounds inhibited the formation of foam cells and reduced intracellular total cholesterol and triglyceride contents. Structure-activity relationship analysis showed the essential role of the delta-lactone ring for the biological activity. The promoter action of the OH group at the C-12 position, the number of monosaccharides in the sugar chain and the rhamnose at the terminal of the sugar chain is also discussed.
authors.affiliation: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing, PR China.
authors.forename: Jiao
authors.initials: J
authors.lastname: Zheng
authors.forename: Li
authors.initials: L
authors.lastname: Tang
authors.forename: Xun-De
authors.initials: XD
authors.lastname: Xian
authors.forename: Si-Xiang
authors.initials: SX
authors.lastname: Zhou
authors.forename: Hai-Ming
authors.initials: HM
authors.lastname: Shi
authors.forename: Yong
authors.initials: Y
authors.lastname: Jiang
authors.forename: Yue-Qing
authors.initials: YQ
authors.lastname: Gu
authors.forename: George
authors.initials: G
authors.lastname: Liu
authors.forename: Peng-Fei
authors.initials: PF
authors.lastname: Tu
mesh_terms: D002460:Cell Line; D002784:Cholesterol / Q000378:metabolism; D008078:Cholesterol, LDL / Q000378:metabolism; D005487:Foam Cells / Q000187:drug effects; D006801:Humans; D030017:Ilex / Q000737:chemistry*; D050356:Lipid Metabolism / Q000187:drug effects*; D008077:Lipoproteins, LDL / Q000737:chemistry / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D018515:Plant Leaves; D012503:Saponins / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000378:metabolism; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology
chemical_list: D008078:Cholesterol, LDL; D008077:Lipoproteins, LDL; D012503:Saponins; D014280:Triglycerides; D014315:Triterpenes; C019455:low density lipoprotein inhibitor; D002784:Cholesterol