title: 21-O-angeloyltheasapogenol E3, a novel triterpenoid saponin from the seeds of tea plants, inhibits macrophage-mediated inflammatory responses in a NF-κB-dependent manner.
abstract: 21-O-Angeloyltheasapogenol E3 (ATS-E3) is a triterpenoid saponin recently isolated from the seeds of the tea tree Camellia sinensis (L.) O. Kuntze. ATS-E3 has several beneficial properties including anti-inflammatory, antidiabetic, antiatherosclerotic, and anticancer effects. Unlike other phenolic compounds isolated from tea plants, there are no studies reporting the pharmacological action of ATS-E3. In this study, we therefore aimed to explore the cellular and molecular inhibitory activities of ATS-E3 in macrophage-mediated inflammatory responses. ATS-E3 remarkably diminished cellular responses of macrophages such as FITC-dextran-induced phagocytic uptake, sodium nitroprusside- (SNP-) induced radical generation, and LPS-induced nitric oxide (NO) production. Analysis of its molecular activity showed that this compound significantly suppressed the expression of inducible NO synthase (iNOS), nuclear translocation of nuclear factor- (NF-) κB subunits (p50 and p65), phosphorylation of inhibitor of κB kinase (IKK), and the enzyme activity of AKT1. Taken together, the novel triterpenoid saponin compound ATS-E3 contributes to the beneficial effects of tea plants by exerting anti-inflammatory and antioxidative activities in an AKT/IKK/NF-κB-dependent manner.
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Woo Seok
authors.initials: WS
authors.lastname: Yang
authors.affiliation: Medical Beauty Research Institute, AmorePacific R&D Center, Yongin 446-729, Republic of Korea.
authors.forename: Jaeyoung
authors.initials: J
authors.lastname: Ko
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Eunji
authors.initials: E
authors.lastname: Kim
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Ji Hye
authors.initials: JH
authors.lastname: Kim
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Jae Gwang
authors.initials: JG
authors.lastname: Park
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Nak Yoon
authors.identifier: 0000-0001-8814-8701
authors.initials: NY
authors.lastname: Sung
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Han Gyung
authors.initials: HG
authors.lastname: Kim
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Sungjae
authors.identifier: 0000-0002-5513-5135
authors.initials: S
authors.lastname: Yang
authors.affiliation: Medical Beauty Research Institute, AmorePacific R&D Center, Yongin 446-729, Republic of Korea.
authors.forename: Ho Sik
authors.initials: HS
authors.lastname: Rho
authors.affiliation: Medical Beauty Research Institute, AmorePacific R&D Center, Yongin 446-729, Republic of Korea.
authors.forename: Yong Deog
authors.initials: YD
authors.lastname: Hong
authors.affiliation: Medical Beauty Research Institute, AmorePacific R&D Center, Yongin 446-729, Republic of Korea.
authors.forename: Song Seok
authors.initials: SS
authors.lastname: Shin
authors.affiliation: Department of Genetic Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
authors.forename: Jae Youl
authors.identifier: 0000-0001-8141-9927
authors.initials: JY
authors.lastname: Cho
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000494:pharmacology*; D028241:Camellia sinensis; D002460:Cell Line; D057809:HEK293 Cells; D006801:Humans; D007249:Inflammation / Q000276:immunology / Q000378:metabolism / Q000517:prevention & control; D008264:Macrophages / Q000187:drug effects* / Q000276:immunology / Q000378:metabolism; D051379:Mice; D016328:NF-kappa B / Q000378:metabolism; D009569:Nitric Oxide / Q000096:biosynthesis; D012503:Saponins / Q000302:isolation & purification / Q000494:pharmacology*; D012639:Seeds; D015398:Signal Transduction / Q000187:drug effects; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: C000599761:21-O-angeloyltheasapogenol E3; D000893:Anti-Inflammatory Agents; D016328:NF-kappa B; D012503:Saponins; D014315:Triterpenes; D009569:Nitric Oxide