title: Bio-guided isolation of the cytotoxic terpenoids from the roots of Euphorbia kansui against human normal cell lines L-O2 and GES-1.
abstract: The dried roots of Euphorbia kansui (kansui) have been used for centuries in China as a herbal medicine for edema, ascites, and asthma. The 95% ethanol extract showed a significant inhibition of cell proliferation against human normal cell lines L-O2 and GES-1. Bioassay-guided separation of the 95% ethanol extract from the roots of E. kansui led to the isolation of 12 diverse terpenoids whose structures were identified by (1)H, (13)C NMR spectroscopy and ESI-MS as kansuinine A (1), kansuinine B (2), kansuinine C (3), kansuiphorin C (4), 3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol (5), 3-O-(2'E,4'Edecadienoyl)-20-O-acetylingenol (6), 3-O-(2'E,4'Z-decadienoyl)-20-deoxyingenol (7), 3-O-benzoyl-20-deoxyingenol (8), 5-O-benzoyl-20-deoxyingenol (9), kansenone (10), epi-kansenone (11), euphol (12). All these 12 terpernoids were evaluated in vitro for cytotoxicity on L-O2 and GES-1 cell lines. Most ingenane-type diterpenoids and 8-ene-7-one triterpenoids (5-11) exhibited a relatively lower IC(50) value; therefore, these compounds had stronger cytotoxicity against human normal cell lines L-O2 and GES-1 with dose-dependent relationships. These results will be significantly helpful to reveal the mechanism of toxicity of kansui and to effectively guide safer clinical application of this herb.
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Li
authors.initials: L
authors.lastname: Zhang
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Lan
authors.initials: L
authors.lastname: Gao
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Zhengjun
authors.initials: Z
authors.lastname: Li
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Xiaojing
authors.initials: X
authors.lastname: Yan
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Yanjing
authors.initials: Y
authors.lastname: Yang
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Yuping
authors.initials: Y
authors.lastname: Tang
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Yudan
authors.initials: Y
authors.lastname: Cao
authors.affiliation: Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
authors.forename: Anwei
authors.initials: A
authors.lastname: Ding
mesh_terms: D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D028481:Euphorbia / Q000378:metabolism / Q000633:toxicity*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008516:Medicine, Chinese Traditional / Q000009:adverse effects; D010936:Plant Extracts / Q000494:pharmacology / Q000633:toxicity; D018517:Plant Roots / Q000378:metabolism / Q000633:toxicity*; D010946:Plants, Medicinal / Q000737:chemistry / Q000633:toxicity*; D013729:Terpenes / Q000302:isolation & purification / Q000633:toxicity*
chemical_list: D010936:Plant Extracts; D013729:Terpenes
keywords: Euphorbia kansui; bio-guided separation; cytotoxicity; human normal gastric epithelial cell line GES-1; human normal liver cell lines L-O2; terpenoids