title: Phytochemical and cytotoxic studies on the roots of Euphorbia fischeriana.
abstract: With the aim of supporting the folk applications of Euphorbia fischeriana, a phytochemical study was performed, which led to the discovery of 9 compounds, including three new ones (1-3) and six known ones (4-9). Their structures were determined by 1D, 2D NMR, and HRESIMS analysis. In the cytotoxic assays on Hep-3B cell line, 2 showed stronger inhibitory effects (IC508.1μmol/L) than that of positive control, and 1, 8 and 9 also gave inhibitory effects in a certain degree with IC50values of 12.5, 12.0 and 18.7μmol/L, respectively. While on A549, the cytotoxic activities of 1 (IC5011.9μmol/L) and 8 (IC509.4μmol/L) were superior to that of 5-Fu, and those of 4 and 9 were moderate with IC50values of 28.2 and 29.8μmol/L, respectively. In addition, both petroleum ether and dichloromethane extracts showed cytotoxic activities with different degree, while n-butanol extracts had no effect. The results clarified that the low-polarity fractions of E. fischeriana, including triterpenoids, abietane and tigliane-type diterpenoids might be the potential bioactive ingredients which will exert strong antitumor effects.
authors.affiliation: School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Wenhua Road 103, Shenyang 110016, PR China.
authors.forename: Qun
authors.initials: Q
authors.lastname: Shi
authors.affiliation: School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Wenhua Road 103, Shenyang 110016, PR China.
authors.forename: Yi-Wei
authors.initials: YW
authors.lastname: Sun
authors.affiliation: School of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, Wenhua Road 103, Shenyang 110016, PR China. Electronic address: mengdl@163.com.
authors.forename: Dali
authors.initials: D
authors.lastname: Meng
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D028481:Euphorbia / Q000737:chemistry*; D006801:Humans; D015394:Molecular Structure; D064209:Phytochemicals / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D064209:Phytochemicals
keywords: Cytotoxic activities; Diterpenoids; Euphorbia fischeriana; Pyrazine; Triterpenoids