常绿钩吻碱抑制人神经胶质瘤U251细胞增殖的体内外作用特征

常绿钩吻碱(sempervirine,SPV)是从钩吻中分离得到的一种育亨宾型生物碱,本研究探讨了常绿钩吻碱抑制人神经胶质瘤细胞体内外增殖的作用特征.以0～16 μmol·L-1不同浓度常绿钩吻碱处理人神经胶质瘤U251细胞24、48和72 h,分别用MTT法和集落形成实验检测细胞增殖,Hoechst细胞核染色和Ann...

Sempervirine inhibits proliferation of human glioma U251 cells in vitro and in vivo

Sempervirine,a yohimbane-type alkaloid isolated from Gelsemium elegans,was found to significantly inhibit the cellular proliferation of U251 cells in vitro and in vivo in a dose-dependent manner.U251 cells were treated with 0-16μmol·L^-1 of sempervirine for 24,48 or 72 h.An MTT assay and clone formation assay were used to investigate cell survival and clone formation.Hoechst staining and Annexin V-FITC/PI staining were used to measure cell apoptosis.The expression of PI3 K,AKT,p-AKT,Bax,Bcl-2,caspase-3 and cleaved caspase-3 was determined by Western blot analysis.The antitumor effect of sempervirine in vivo was investigated by inoculating nude mice with U251 cells.All animal experiments were in strict accordance with the regulations of the Biomedical Ethics Committee of Fujian Medical University(Fujian,China).The results show that sempervirine significantly inhibits the proliferation and induces the apoptosis of U251 cells,promotes cleavage of caspase-3,down-regulates the protein expression of PI3 K and Bcl-2/Bax,and inhibits phosphorylation of AKT in vitro.Intraperitoneal injection of 4 or 8 mg·kg^-1·day^-1 of sempervirine inhibits U251 cells tumor growth in the xenograft nude mice,and tumor weight decreased by 44.76%and 61.26%,respectively.Our study shows that sempervirine significantly inhibits the proliferation of U251 cells in vitro and in vivo,laying a foundation for further research and development of its anti-glioma effect.