title: Oleanane-type triterpene saponins from the bark of Aralia elata and their NF-κB inhibition and PPAR activation signal pathway.
abstract: Two new oleanane-type triterpene saponins, tarasaponin IV (1) and elatoside L (2), and four known; stipuleanoside R(2) (3), kalopanax-saponin F (4), kalopanax-saponin F methylester (5), and elatoside D (6) were isolated from the bark of Aralia elata. Kalopanax-saponin F methyl ester was isolated from nature for the first time. Their chemical structures were elucidated using the chemical and physical methods as well as good agreement with those of reported in the literature. Oleanane-type triterpene saponins are the main component of A. elata. All compounds were investigated the anti-inflammatory activity. We measured their inhibition of NF-κB and activation of PPARs activities in HepG2 cells using luciferase reporter system. As results, compounds 2 and 4 were found to inhibit NF-κB activation stimulated by TNFα in a dose-dependent manner with IC(50) values of 4.1 and 9.5 μM, respectively, when compared with that of positive control, sulfasalazine (0.9 μM). Compounds 2 and 4 also inhibited TNFα-induced expression of iNOS and COX-2 mRNA. Furthermore, compounds 1-6 were evaluated PPAR activity using PPAR subtype transactivation assays. Among of them, compounds 4-6 significantly increased PPARγ transactivation. However, compounds 4-6 did not activate in any other PPAR subtypes.
authors: College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
authors: Nguyen Xuan
authors: NX
authors: Nhiem
authors: Ho Young
authors: HY
authors: Lim
authors: Phan Van
authors: PV
authors: Kiem
authors: Chau Van
authors: CV
authors: Minh
authors: Vu Kim
authors: VK
authors: Thu
authors: Bui Huu
authors: BH
authors: Tai
authors: Tran Hong
authors: TH
authors: Quang
authors: Seok Bean
authors: SB
authors: Song
authors: Young Ho
authors: YH
authors: Kim
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D027983:Aralia / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000276:immunology; D009828:Oleanolic Acid / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D047492:Peroxisome Proliferator-Activated Receptors / Q000276:immunology; D024301:Plant Bark / Q000737:chemistry; D012503:Saponins / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*
chemical_list: D000890:Anti-Infective Agents; D016328:NF-kappa B; D047492:Peroxisome Proliferator-Activated Receptors; D012503:Saponins; D009828:Oleanolic Acid