Abstract: Bacteria have developed various ways to resist the toxic effects of antibiotics and other drugs, such as produce enzymes that inactivate antibiotics, target alteration by mutation or enzymatic modi?cation, inhibit drug entry into the cell and active ef?ux of drugs. Actively exporting an antibiotic from the bacterial cell by the efflux pump is essential to ensure signi?cant levels of drug resistance. The multidrug efflux pumps that affect such efflux typically export several unrelated substances, including antibiotics and molecules produced by the host organism. There are different kinds of multidrug efflux pumps in gram-negative bacteria and that in gram-positive bacteria as the different structure of cell membrane. In gram-negative bacteria, it has been reported five superfamilies, these include ATP-binding cassette family (ABC), resistance nodulation division(RND) family, major facilitator superfamily (MFS), small multidrug resistanc (SMR) family and multidrug and toxic-compound extrusion family (MATE). In gram-positive bacteria, it has reported four superfamilies, these include ABC, MFS, SMR family and MATE, except RND family. Facing the resistance of bacteria to antibiotics, it is urgent to find new molecules mechanisms against resistant bacteria. Some researchers have been searching for the efflux pumps inhibitors (e.g., MexAB-OprM specific efflux pump inhibitor) for several years, and some possible compounds have been identified from medicinal plant to restore antibiotic activity.