九节龙皂苷抗肿瘤作用研究进展

九节龙皂苷是金牛科紫金牛属植物川产九节龙Ardisia pusilla中分离出的1种三萜皂苷单体。皂苷大多具有抑瘤、抗菌等重要的生物活性,而其抗肿瘤作用具有重要的研究价值和诱人的开发前景。文章调研了有关九节龙皂苷的国内外文献报道,并分析了其相关抗肿瘤机制。研究表明,九节龙皂苷对肿瘤细胞有一定的抑制作用,对胶质瘤细胞较为突出。其诱导肿瘤细胞凋亡与促进Fas/Fas L表达及Caspase-3/Caspase-8活化,促进Bax表达,抑制Bcl-2表达,及BAD去磷酸化途径以及核内Ca2+浓度等有关;诱导肿瘤细胞自噬与促进Beclin-1及LC-3等表达有关;诱导肿瘤细胞侵袭与转移与下调MMP-2/MMP-9表达及E-钙黏素活性等有关。同时,体内药效学及药代动力学研究也证实了九节龙皂苷具有一定的抑制肿瘤作用。通过对九节龙皂苷体外抗肿瘤机制及体内抗肿瘤活性研究进展概述,以期为后期肿瘤治疗的临床前研究提供参考。

Advances in Studies of Anti-tumor Activity of Ardipusilloside

Ardipusilloside is a triterpenoid saponin isolated from Ardisia pusilla. Most saponins have anti-tumor, anti-bacterial and other biological activities, and their anti-tumor effects have important research value and attractive developing prospects. This article investigates the literatures on ardipusilloside, and analyzes its anti-tumor mechanism. Researches show that ardipusilloside has anti-tumor activity, especially in glioma cells. it induced tumor cells apoptosis via promoting Fas/FasL expression and Caspase-3/Caspase-8 activation, promoting Bax expression, inhibiting Bcl-2 expression, and BAD dephosphorylation pathways and nuclear Ca²⁺ concentration. It induced tumor cells autophagy via promoting Beclin-1 and LC-3 expression;it induced tumor cells invasion and metastasis via inhibiting MMP-2/MMP-9 expression and activity of E-cadherin. At the same time, in vivo pharmacodynamic and pharmacokinetic study also confirmed its anti-tumor activity. This review summarized the in vitro anti-tumor mechanism and in vivo anti-tumor research progress on ardipusilloside, in order to provide a reference for tumor treatment of pre-clinical studies.