雷公藤甲素及其纳米制剂抗肿瘤作用研究进展

Research progress on the anti-tumor effect of triptolide and its nano preparations

雷公藤甲素是从卫茅科雷公藤根部提取的一种环氧二萜内酯化合物,已经证实具有抗炎、抗病毒、免疫调节、抗生育等多种药理活性,近年来,尤其在抗肿瘤方面显示出巨大潜力。雷公藤甲素对多种肿瘤细胞具有显著抑制作用,其作用机制包括抑制肿瘤细胞增殖与迁移、诱导肿瘤细胞凋亡、诱导肿瘤细胞自噬、诱导肿瘤细胞周期阻滞等。但其水溶性差、生物利用度低及不良反应严重等缺陷限制其临床应用,目前通过纳米制剂手段如脂质纳米粒、聚乳酸纳米粒、聚合物胶束、外泌体等,可将药物精准递送到肿瘤部位,提高药物疗效,降低毒性等,其展现出良好的应用前景。本文通过对近年来国内外雷公藤甲素的抗肿瘤活性、作用机制及其纳米制剂抗肿瘤应用的研究进行归纳总结,以期为雷公藤甲素及其纳米制剂在抗肿瘤方面的进一步开发应用提供指导。

Triptolide is an epoxy diterpene lactone extracted from the root of Tripterygium wifordi Hook f.It has been proved to have a variety of pharmacological activities such as anti-inflammatory,anti-virus,immune regulation,and anti-fertility.In recent years,triptolide was reported great potential in anti-tumor effect.Triptolide has significant inhibitory effects on wide range of tumor cell lines.The mechanism of actionincludes inhibiting tumor cell proliferation and migration,inducing tumor cell apoptosis,inducing tumor cell autophagy,and inducing tumor cell cycle arrest.However,its disadvantages limit its clinical application,such as poor water solubility,low bioavailability,strong toxicity and side effects.At present,nano preparations,such as lipid nanoparticles,polylactic acid nanoparticles,polymer micelles and exosomes,could deliver drugs to tumor sites,thus could improve drug efficacy and reduce toxicity,exhibiting good prospects of application.This paper summarizes the research on the antitumor effect,the mechanism,and the antitumor application of triptolide in recent years,in order to guide the further development and application of triptolide and its preparations in antitumor effect.