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

• Published in: Mediators of inflammation 2014-01, Vol.2014 (2014), p.1-9
• Main Authors: Hong, Yong Deog, Shin, Song Seok, Cho, Jae Youl, Yang, Sungjae, Kim, Han Gyung, Sung, Nak Yoon, Park, Jae Gwang, Kim, Ji Hye, Kim, Eunji, Ko, Jaeyoung, Yang, Woo Seok, Rho, Ho Sik
• Format: Article
• Language: English
• Subjects: Animals; Anti-Inflammatory Agents - isolation & purification; Anti-Inflammatory Agents - pharmacology; Camellia sinensis; Cell Line; Health aspects; HEK293 Cells; Humans; Inflammation; Inflammation - immunology; Inflammation - metabolism; Inflammation - prevention & control; Macrophages; Macrophages - drug effects; Macrophages - immunology; Macrophages - metabolism; Mice; NF-kappa B - metabolism; Nitric Oxide - biosynthesis; Saponins; Saponins - isolation & purification; Saponins - pharmacology; Seeds; Signal Transduction - drug effects; Tea (Plant); Terpenoids; Triterpenes - isolation & purification; Triterpenes - pharmacology
• ISSN: 0962-9351; 1466-1861
• DOI: 10.1155/2014/658351

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.