雷公藤甲素抗肿瘤机制及其新型给药系统

Anti-Tumor Mechanism of Triptolide and Its New Drug Delivery System

雷公藤甲素具有广谱、高效的抗肿瘤性能,可多靶点、多途径发挥功用,其抗肿瘤机制与诱导肿瘤细胞凋亡和自噬、降低转录、影响蛋白表达等密切相关,并涉及主要通路上的许多关键基因,可改变肿瘤微环境,从而抑制肿瘤的发生发展。但雷公藤甲素毒具有不良反应强、水溶性差、体内消除快等缺点,临床应用受到了极大的限制,故药物的减毒增效仍是目前研究的重要方向之一。目前,雷公藤甲素抗肿瘤新型给药系统的研究主要包括脂质体、聚合物胶束、纳米粒、微球等,各种类型的药物递送系统降低了药物毒性,但在缓释、体内消除、制备工艺、成本、生物利用度、稳定性等方面仍需进一步改良与研发。

Triptolide has a wide spectrum and high-efficiency anti-tumor performance,and can play its function in multiple targets and multiple ways.Its anti-tumor mechanism is closely related to inducing apoptosis and autophagy,reducing transcription and affecting protein expression,and involves many key genes in the main pathway,which can change the tumor microenvironment and inhibit the development of tumor.However,the toxicity of triptolide has many disadvantages,such as strong side effects,poor water solubility,rapid elimination in vivo and so on.The clinical application of triptolide has been greatly limited,so the attenuation and efficiency of the drug is still one of the important directions of current research.At present,the research of new anti-tumor drug delivery system of triptolide mainly includes liposomes,polymer micelles,nanoparticles,microspheres and so on.Various types of drug delivery systems reduce the drug toxicity,but it still needs further improvement and development in the aspects of sustained release,elimination in vivo,preparation process,cost,bioavailability,stability and so on.