摘要
目的探讨雷公藤内酯醇(triptolide,TPL)在体内外对人结肠癌细胞株SW-480、HT-29的作用。方法体外运用噻唑蓝(MTT)比色法检测TPL对SW-480、HT-29的增殖抑制作用,细胞DNA片段化及Annexin-Ⅴ/FITC流式细胞术检测TPL对SW-480、HT-29细胞诱导凋亡的作用;体内建立荷人结肠癌细胞裸鼠模型,观察不同浓度TPL静脉注射治疗对肿瘤生长的影响。结果在体外,TPL在10μg.L-1时即对2种结肠癌细胞具有明显的抑制生长作用,且呈时间和剂量依赖性,40μg.L-1时具有明显的诱导凋亡作用,凋亡比例分别达22.2%和27.3%;在体内,TPL能显著抑制2种肿瘤的生长,隔日0.4 mg.kg-1静脉给药时其抑瘤率分别达93.7%和94.5%。结论TPL在体内外均具有明显的抗结肠癌作用。
OBJECTIVE To prepare N-trimethyl chitosan（TMC）-coated doxorubicin liposomes and to investigate their uptake by human umbilical vein endothelial cells（HUVECs） in order to evaluate their targeting ability to the vascular endothelial cells in vitro.METHODS Doxorubicin liposomes were prepared by pH gradient method and coated by TMC with different degree of quarternization（DQ）.After nucleic staining with DAPI,laser confocal microscopy was used to investigate the uptake of doxorubicin by HUVECs after incubation with TMC-coated doxorubicin liposomes and the transmission from the cytoplasm to the nucleic.RESULTS TMC-coated doxorubicin liposomes were stable with particle sizes of 100-200 nm and capsulation efficieny above 80%.With the increase of DQ of TMC,the Zeta potential of TMC-coated doxorubicin liposomes was increased（P0.05）.Moreover,their uptake by HUVECs was enhanced and doxorubicin was quickly released in the cytoplasm and transported to the nucleic.CONCLUSION TMC-coated doxorubicin liposomes enhanced the effect on targeting to the vascular endothelial cells with some relationship to the DQ of TMC.Tumor neovasculature target of TMC-coated doxorubicin liposomes will be studied in vivo in the fulure.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2010年第1期28-31,共4页
Chinese Pharmaceutical Journal
基金
福建省重大专项前期研究项目(No.2005YZ1008)
关键词
雷公藤内酯醇
结肠癌
凋亡
裸鼠移植瘤
N-trimethyl chitosan doxorubicin liposomes vascular endothelial cell target
