三七及单体对P糖蛋白抑制作用的研究进展

The Inhibiting Effects of Panax notoginseng and Its Monomer Compositions on P-glycoprotein

P-糖蛋白属于ABC跨膜转运蛋白超家族中的一员,是一种ATP依赖性的外向型转运泵,参与生物的各种生理功能以及多类药物的体内转运过程,同时也是产生临床多药耐药作用的主要原因.三七作为云南的特色中草药,在很多疾病的治疗与预防方面有着显著疗效,其副作用小、多靶点及多途径的综合调节作用,在逆转Mdr1和P-gp表达的研究中,具有一定的前景.综述近年来从蛋白质水平和基因水平上通过多种途径下调P-gp及Mdr1基因的表达,以及三七及其单体成分对P-gp及Mdr1基因下调机制的进展研究及展望.

P-glycoprotein （P-gp） belongs to the member of the super-family of ATP-binding cassette （ABC） transporters. It is the 170KD glycoprotein which is the product of the MDR1 gene, located in chromosome 7q21. It is an ATP-dependent exported and oriented transporter and involved in various physiological functions as well as the transport process of many types of drugs in the body. The physiological function of P-gp is to pump the toxic metabolites out of the cell in order to reduce the accumulation of toxic products so as to protect the cells from the poison. However, in pathological condition, the drug which used to treat the disease may be pumped out of the cells by the P-gp. Therefore,the P-gp is the main cause of the multidrug resistance in clinical disease such as tumor and some neurologic diseases. The cross-resistance phenomenon is leading to poor efficacy for these diseases treatment.Panax notoginseng as the characteristic Chinese herbal medicine in Yunnan province, it has many significant effects in the treatment and prevention of many diseases such as cerebrovascular diseases. It can improve the blood hemorrheology,prevent the produce of the peroxy radical, alleviate intracellular calcium overload,treat inflammation,as well as improve the immune system function. Meanwhile, some research recently reported that it also has a considerable prospect with its multi-target and multi-channel regulation in the reversal of the MDR1 and the P-gp genes expression. This paper reviews the progress of the down-regulated expression of P-gp and MDR1 genes through different pathways, and the mechanism of Panax notoginseng and its monomer compositions on down-regulated the expression of the P-gp and MDR1 genes.