白花丹素抗肿瘤活性及其作用机制研究进展

Advances in tumor suppression by plumbagin and it mechanism

研究发现,白花丹素在体内和体外对多种肿瘤细胞均具有明显的生长抑制作用。白花丹素还可通过调节骨内微环境,阻断肿瘤转移的"恶性循环",抑制肿瘤细胞骨转移。本文阐述了白花丹素对多种肿瘤细胞的抑制作用及其机制,并以高骨转移潜能的恶性肿瘤为例,阐述了白花丹素的抗肿瘤作用机制及其作用靶点。目前,大部分动物实验仍采用白花丹素腹腔内给药的方式,但已有学者研发了可明显增强白花丹素抗肿瘤活性的新型高分子缓释给药体系。随着对白花丹素抗肿瘤活性及其作用机制的认识不断深入,今后可通过对白花丹素的化学结构进行优化设计,以进一步提高其抗肿瘤活性。

Recent studies have demonstrated that plumbagin has significant suppressive effect on the proliferation of various tumor cell lines in vivo and in vitro. Plumbagin can also inhibit the metastasis of tumor cells by blocking up the ＂vicious cycle＂ of tumor metastasis through regulating the bone microenvironment. This paper reviews the advances in inhibition effect of plumbagin on many tumor cell lines and the related mechanism, especially illustrating the underlying antitumor mechanism and functional targets of plumbagin in the malignant tumors with high metastatic potential. Currently, the majority of the animal experiments apply systematic drug delivery via intraperitoneal injection of plumbagin; whereas the novel sustained-release drug delivery systems, which are based on high-polymer materials aiming at enhancing the antitumor activity, are under development. With the new insights into the antitumor mechanism of plumbagin, the optimized chemical construction of plumbagin is expected to improve its anti-tumor effect.