Inhibitory effect of triterpenoid saponins from the leaves of Ilex kudingcha on aggregated LDL-induced lipid deposition in macrophages.
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.
Zheng
Jiao
J
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing, PR China.
Tang
Li
L
Xian
Xun-De
XD
Zhou
Si-Xiang
SX
Shi
Hai-Ming
HM
Jiang
Yong
Y
Gu
Yue-Qing
YQ
Liu
George
G
Tu
Peng-Fei
PF
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
D008078:Cholesterol, LDL; D008077:Lipoproteins, LDL; D012503:Saponins; D014280:Triglycerides; D014315:Triterpenes; C019455:low density lipoprotein inhibitor; D002784:Cholesterol