TABLE 2

Inhibition of P-gp function and/or expression by TCM

CompoundTest ModelPharmacological ResultsReferences
Flavonoids
 EGCGCEM/ADRDownregulation of P-gpLi et al., 2018
 GQMCF-7/ADRDownregulation of P-gp and MDR1 geneZhang et al., 2019
 Silymarin AA2780/ADRInhibition of P-gp efflux; downregulation of P-gpViktorova et al., 2019
 DihydromyricetinMCF7/ADR; K562/ADRInhibition of P-gp efflux; downregulation of P-gpSun et al., 2018
 CurcuminKB-C2Inhibition of P-gpLopes-Rodrigues et al., 2016
 ApigeninCEM/ADRInhibition of P-gpSaeed et al., 2015
 TaxifolinHeLaS3; KB/VCRInhibition of P-gpChen et al., 2018
Alkaloids
 ChelidonineCaco-2; CEM/ADRInhibition of P-gpHerrmann et al., 2018
 TetrandrineMCF-7/ADRDownregulation of P-gpLiao et al., 2019
 MatrineMCF-7/ADRInhibition of P-gpZhou et al., 2018
Terpenoids
 Ursolic acidMCF-7/ADRInhibition of P-gpZong et al., 2019
 ParthenolideA549/ADRDownregulation of P-gpCarlisi et al., 2017
 CostunolideK562/ADRDownregulation of P-gpCai et al., 2019
 Cryptotanshinone
 Dihydrotanshinone
CEM/ADRDownregulation of P-gp and MDR1 geneHu et al., 2014
Coumarins
 Galbanic acidHL60Inhibition of P-gpMaruszewska and Tarasiuk, 2019
 DecursinolNCI/ADR-RESInhibition of P-gpChoi et al., 2016
 OstholeK562/ADRDownregulation of MDR1 geneWang et al., 2016
Quinonoids
 MiltironeHepG2Inhibition of P-gpZhou et al., 2015
 EmodinK562/ADR; Caco-2 Downregulation of P-gpMin et al., 2017
 ShikoninA2780/PTXInhibition of P-gpWang et al., 2019
TCM extracts
 Asiatic toadCRCInhibition of P-gpYuan et al., 2017
S. miltiorrhizaEverted rat gut sacsInhibition of P-gpDai et al., 2012
S. chinensisK562/A02Downregulation of P-gp; inhibition of P-gpWang et al., 2017
 CRLS180Activation of P-gp transportationYu et al., 2018
 LiquoriceCaco-2 Inhibition of P-gpHe et al., 2020
  • CRC, colorectal cancer cell; EGCG, epigallocatechin-3-gallate; VCR, vincristine.