雷公藤红素及其制剂的抗肿瘤研究进展

Process of anti-tumor effects of celastrol and its pharmaceutical preparations

在2006年Huanjie Yang等发现雷公藤红素可以诱导前列腺癌细胞凋亡及肿瘤坏死,是一种有效的天然蛋白酶抑制剂,自此引发了雷公藤红素抗癌作用及其机制的研究热潮。雷公藤红素可以通过多方面发挥其抗癌作用,包括抑制肿瘤细胞生长、阻滞细胞周期和诱导凋亡,抑制癌细胞蛋白酶,抑制信号通路,影响肿瘤相关蛋白、肿瘤坏死因子等,是一种潜在的天然抗肿瘤药物,对前列腺癌、肺癌、肝癌、白血病、胶质瘤、黑色素瘤、结肠癌、卵巢癌、乳腺癌等肿瘤细胞具有一定的抗肿瘤作用。然而由于其性质较为不稳定,而且存在毒性,为了拓宽雷公藤红素的临床应用,充分发挥其药理药效作用,采用药物制剂新技术降低雷公藤红素毒性,提高其溶解度是目前重要的研究方向之一。本文对2006年以来雷公藤红素及其制剂的抗肿瘤作用相关文献资料进行分析和综述,为今后雷公藤红素抗肿瘤新型制剂的研究提供参考。

In 2006,Yang H et al.had found that celastrol is a kind of effective natural protease inhibitor,which can induce cancer cell apoptosis and tumor necrosis.This report has triggered the research upsurge for anti-tumor effects and mechanism of celastrol.Some researchers have found that celastrol can exert anti-tumor effects through a variety of approaches,including inhibiting tumor cell growth,blocking the cell cycle,inducing apoptosis,inhibiting proteases of cancer cells,inhibiting signaling pathways,affecting tumor associated proteins and tumor necrosis factors,etc.Thus,celastrol will become a potential antitumor drug,which has significant effects on prostate cancer,lung cancer,liver cancer,leukemia,glioma,melanoma,ovary cancer,colon cancer and many other tumors.However,celastrol is unstable and toxic.In order to broaden clinical application and fully utilize its pharmacological effects,new technology of pharmaceutical preparations can be used to reduce toxicity and enhance solubility of celastrol,which is one of important research directions currently.Therefore,this article summarized celastrol＇s anti-tumor effects through searching and analyzing literatures since 2006,to provide some ways and means for future researches for new pharmaceutical preparations of celastrol.