title: Cytotoxic and Pro-apoptotic Activities of Sesquiterpene Lactones from Inula britannica.
abstract: In this study, five known sesquiterpene lactones (STL) with an α-methylene-γ-lactone motif, including two eudesmanolides, 1β-hydroxyalantolactone (1) and ivangustin (2), and three 1,10-seco-eudesmanolides, 1-O-acetylbritannilactone (3), 1,6-O,O-diacetylbritannilactone (4), and 6α-O-(2- methylbutyryl)britannilactone (5) were isolated from the flower heads of the medicinal plant Inula britannica. Their structures were characterized by spectroscopic methods. X-ray data of 2 is reported for the first time. Among them, eudesmanolides 1 and 2 exhibited remarkable cytotoxicity against HEp2, SGC-7901 and HCT116 human cancer cell lines, comparable with etoposide (Vp-16) used as reference drug. Furthermore, treatment of HEp2 cells with 1 induced apoptosis associated with cleaved procaspase-3 and PARP. The biological assays carried out with normal cells (CHO) revealed that all sesquiterpenes were weakly selective against the cancer cell lines tested.
authors.forename: Ping
authors.initials: P
authors.lastname: Xiang
authors.forename: Xin
authors.initials: X
authors.lastname: Guo
authors.forename: Yang-Yang
authors.initials: YY
authors.lastname: Han
authors.forename: Jin-Ming
authors.initials: JM
authors.lastname: Gao
authors.forename: Jiang-Jiang
authors.initials: JJ
authors.lastname: Tang
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D035264:Flowers / Q000737:chemistry; D006801:Humans; D038143:Inula / Q000737:chemistry*; D007783:Lactones / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D007783:Lactones; D012717:Sesquiterpenes