Triptolide (TPL) is the most active chemical constituents derived from the traditional Chinese medicine Tripterygium wilfordii so far. It has the effect of anti-inflammation

anti-fertility

anti-rheumatism and immune regulation. In recent years

it has been found that TPL also has high efficiency and broad spectrum anti-tumor activity

and its anti-tumor mechanism has become a hot spot at home and abroad. At present

chemotherapy is the main therapy for tumor. However

the multi-drug resistance (MDR) caused by tumor cells also makes it difficult to achieve good results. In addition

the mechanism of tumor multi-drug resistance is very complex

so it is important to find the MDR reversal agent with high efficiency and low toxicity. In the literature search

it is found that the mechanism of MDR in the tumor mainly includes multi-drug resistance caused by multi-drug resistance protein

multi-drug resistance mediated by regulatory genes (including anti-apoptosis related signaling pathway and apoptosis-related genes and proteins)

and multi-drug resistance mediated by enzymes

as well as the changes of pH in tumor cells

and pharmacokinetic changes.The latest research shows that TPL can not only enhance the anti-tumor effect of a variety of chemotherapy drugs

but also can reverse the multi-drug resistance of tumor. However

its reversal mechanism has not been widely studied at home and abroad. The reversal mechanism of TPL in MDR is mainly related to down-regulating MDR1/P-gp expression

inhibiting Akt/nuclear factor(NF)-κB activity

increasing reactive oxygen specise(ROS) level in cells

inducing apoptosis

inhibiting multidrug resistance-associated protein(MRP) expression

regulating Bax/Bcl-2 expression and inhibiting mutation of Bcr/abl fusion gene T315I. In this paper

an overview would be written from the mechanism of tumor multi-drug resistance and TPL's reversal mechanism of multi-drug resistance

to provide new ideas for the reversal of tumor multi-drug resistance and benefit various patients.