Table 1.
Natural products with their mechanisms of inhibition.
| Substance | Mechanism of Inhibition | References |
|---|---|---|
| Dauriporphine | ↓ P-g expression | [125] |
| Glaucine | ↓ P-g expression ↓ MDR1 ↓ MRP1 |
[125] |
| Hernandezine | ↓ P-g expression | [125] |
| Antofine | ↓ P-g expression ↓ MDR1 mRNA |
[125] |
| Harmine | ↓ BCRP | [132,133,138] |
| Tryptanthrin | ↓ P-g expression ↓ MRP2 |
[125] |
| Lobeline (from Lobelia inflate) |
↓ P-g expression | [120,125] |
| Tetramethylpyrazine | ↓ P-g expression ↓ MDR1 mRNA ↓ MRP1, MRP2, MRP3 |
[105,138,144,238] |
| Danshensu and tetramethylpyrazine (from the Chinese herbs) | ↓ P-g expression | [239] |
| Acrimarine E | ↓ P-g expression | [125] |
| Gravacridonetriol | ↓ MDR1 mRNA | [125] |
| 2-Methoxycitpressine I | ↓ P-g expression | [125] |
| Capsaicin (extracted from Capsicum annuum) |
↓ P-g expression | [100,125] |
| Acacetin | ↓ BCRP ↓ MRP1 |
[119,125] |
| Amorphigenin | ↓ P-g expression | [125] |
| Apigenin | ↓ BCRP ↓ MRP1 ↓ P-g expression ↓ HIF-1α |
[7,138,143,144,240] |
| Ampelopsin | ↓ P-g expression | [125] |
| Biochanin A | ↓ BCRP ↓ MRP1 ↓ P-g expression |
[132,133,138,143] |
| Catechin | ↓ ATPase activity ↓ P-g expression |
[125] |
| Chalcone | ↓ MRP1 ↓ P-g expression |
[125] [141] |
| Chrysin | ↓ BCRP ↓ P-g expression |
[125] [119,141] |
| Diosmetin | ↓ BCRP | [125] |
| Green tea catechins (EGCG, ECG, CG) | ↓ P-g expression ↓ MDR1 ↓ ATPase activity |
[100,141] |
| Epicatechin gallate | ↓ P-g expression | [118,125] |
| Epigallocatechin gallate | ↓ P-g expression ↓ MDR1 ↓ ABCG2 ↓ HIF-1α |
[113,114,132,138,143,144,241] |
| Formononetin | ↓ P-g expression | [125] |
| Genistein | ↓ BCRP ↓ MRP1 |
[132,133,138,143] |
| Glabridin | ↓ P-g expression | [7,114,138] |
| 3,3’,4’,5,6,7,8- Heptamethoxyflavone | ↓ P-g expression | [125] |
| Kaempferol | ↓ BCRP ↓ MRP1 ↓ P-g expression |
[7,134,138,143] |
| Luteolin | ↓ BCRP ↓ MRP1 |
[125,141] |
| Morin | ↓ P-g expression ↓ MRP1 |
[132,133,138,143] |
| Myricetin | ↓ MRP1 and MRP2 activity ↓ Calcein efflux |
[7,105,133,138,143] |
| Naringenin | ↓ P-g expression | [134,138,143] |
| Naringenin-7-glucosid | ↓ BCRP | [125] |
| Nobiletin (found in citrus fruit) | ↓ P-g expression ↓ MRP1 |
[114,138,143,146] |
| Phloretin | ↓ P-g expression ↓ MRP1 |
[132,133,138,143] |
| Procyanidine | ↓ P-g expression | [125] |
| Quercetin | ↓ MRP1-mediated drug transport ↓ BCRP ↓ MRP1, 4 and 5. ↓ P-g expression ↓ PKC ↓ HIF-1α ↓ MDR1 |
[7,118,119,120,124,125,141,146,169,232,242,243,244,245,246,247] |
| Robinetin | ↓ MRP1 and MRP2 activity (inhibited calcein efflux) | [125] |
| Rotenone | ↓ P-g expression | [125] |
| Silymarin | ↓ P-gp ATPase activity ↓ P-gp-mediated cellular efflux ↓ [3 H]azidopine photoaffinity labeling of P-gp suggesting a direct interaction with the P-gp substrate binding ↓ MRP1-mediated drug transport ↓ BCRP |
[7,132,133,138,143] |
| Tangeretin | ↓ P-g expression ↓ BCRP |
[132,138,143,146] |
| Curcumin | ↓ P-g expression ↓ BCRP ↓ MRP1 ↓ MDR1 mRNA ↓ ABCG2 and ABCC1 ↓ PKC-α and –ζ ↓ GSTπ ↓ Topo IIα ↓ HIF-1α |
[7,94,100,118,119,120,124,125,145,186,236,237,242,246,248,249,250,251] |
| Matairesinol (found in soybean (Glycine max)) |
↓ P-g expression ↓ MRP1 |
[100,125] |
| Sesamin | ↓ P-g expression | [100,125] |
| Gomisin A | ↓ P-g expression | [125] |
| Schisandrol A | ↓ P-g expression | [125] [119] |
| Chlorogenic acid | ↓ P-gp ATPase activity | [125] |
| Ginkgolic acid | ↑ DNR accumulation ↓ P-g expression |
[125] |
| Agnuside | ↓ P-gp ATPase activity | [125] |
| Picroside-II | ↓ P-gp ATPase activity | [125] |
| Santonin | ↓ P-gp ATPase activity | [125] |
| beta-Amyrin | ↓ P-g expression | [125] |
| Glycyrrhetinic acid (Enoxolone) (Licorice) |
↓ P-g expression ↓ MRP1 |
[100,125] |
| Obacunone | ↓ P-g expression | [125] |
| Oleanolic acid | ↓ P-g expression | [125,247] |
| Uvaol | ↓ P-g expression | [125,247] |
| Alisol B 23-acetate | ↓ P-g expression | [113,133,138] |
| Ginsenoside Rg3 | ↓ Binding of [3 H] azidopine to P-gp ↓ P-g expression |
[119,125] |
| Protopanaxatriol ginsenosides 20S-ginsenoside Ginsenoside Rb1 Ginsenoside Rg3 |
↓ P-g expression ↓ BCRP ↓ MRP1 ↓ MDR1 ↓ LRP |
[113,133,138,144,146] |
| Tenacigenin B: P8, P26 and P27 | ↓ P-g expression ↓ MRP1 ↓ ABCG2-mediated efflux |
[125] |
| Tenacigenin B: P2, P3 and P6 | ↓ P-g expression ↓ MRP1 |
[125] |
| Tenacigenin B: P1, P4, P5, P9 and P28 | ↓ P-g expression | [125] |
| Aurochrome | ↓ P-g expression | [125] |
| Diepoxycarotene | ↓ P-g expression | [125] |
| Mutatochrome | ↓ P-g expression | [125] |
| Clausarin | ↓ P-gp-mediated drug efflux | [125] |
| Phyllodulcin | ↑ DNR accumulation (inhibition of P-gp-mediated efflux of DNR) | [125] |
| Acteoside (Verbascosine) | ↓ P-gp ATPase activity | [125] |
| Berbamine | ↓ MDR1 gene expression | [125,242] |
| Glaucine | ↓ P-g expression ↓ MRP1 ↓ MDR1 and MRP1 genes |
[125] |
| Fangchinoline | ↓ P-g expression | [125] |
| O-(4-ethoxyl-butyl)- berbamine | ↓ MDR1 gene expression | [125] |
| Tetrandrine (dried root of Stephania tetrandra) |
↓ P-g expression ↓ LRP |
[103,113,135,138,144] |
| Matrine | ↓ P-g expression | [125] |
| Antofine | ↓ MDR1 mRNA ↓ P-g expression |
[125] |
| Ephedrine | ↓ MDR1 mRNA ↓ P-g expression |
[125,242] |
| Indole-3-carbinol | ↓ P-g expression | [125] |
| Staurosporine | ↓ P-g expression ↓ MDR1 gene expression |
[125] |
| Vauqueline | ↓ MDR1 mRNA ↓ P-g expression |
[125] |
| Gravacridonetriol | ↓ MDR1 mRNA | [125] |
| Clitocine | ↓ MDR1 mRNA ↓ P-g expression) |
[125] |
| Sulfinosine | ↓ MDR1 mRNA ↓ P-g expression |
[125] |
| Bisdemethoxycurcumin | ↓ P-gp expression ↓ MDR1 |
[118,125] |
| Honokiol and magnolol (isolated from Magnolia officinali) | ↓ MDR1 ↓ P-gp expression |
[7,125] |
| Schisandrin A (Deoxyschizandrin) | ↓ P-gp expression ↓ MDR1 ↓ PKC |
[104,113,125,133,137,146] |
| Schisandrin B (Sch B) | ↓ P-gp expression and P-gp mediated efflux of Dox. ↓ MRP1 |
[93] |
| Triptolide | ↓ MDR1 ↓ MRP1 protein expression |
[125] |
| Pyranocoumarins | ↓ P-gp expression ↓ MDR1 mRNA expression |
[119,125] |
| Ginger phytochemicals (6-Gingerol,10- Gingerol) |
↓ P-gp expression ↓ MRP1 |
[100,125] |
| Ginger phytochemicals (6-gingerol, 10-gingerol, 4-shogaol, 6-shogaol, 10-shogaol, and 6-dehydrogingerdione) |
↓ GSTπ ↓ MRP1 |
[194] |
| Alisma orientalis | ↓ P-gp expression | [250] |
| Piper methysticum | ↓ P-gp expression | [250] |
| Guggulsterone | ↓ P-gp expression ↓ MRPs |
[113,114,134,252] |
| Phenolic diterpenes | ↓ P-gp expression | [250] |
| Vincristine | ↓ P-gp expression | [250] |
| 5-Bromotetrandrine | ↓ P-gp expression | [119] |
| Abietane diterpene | ↓ P-gp expression | [119] |
| Amooranin | ↓ P-gp expression | [119] |
| Baicalein and derivatives | ↓ P-gp expression ↓ MRPs |
[118,119,120,124,141,247] |
| Bitter melon extract | ↓ P-gp expression | [119] |
| Bufalin | ↓ P-gp expression | [119] |
| Cannabinoids | ↓ P-gp expression ↓ BCRP ↓ MRPs |
[119] |
| β-Carotene | ↓ P-gp expression | [101,119] |
| Fucoxanthin | ↓ GST | [166] |
| Catechins | ↓ P-gp expression | [111,133,143] |
| Cepharanthine | ↓ P-gp expression ↓ MRP1 |
[119] |
| Coumarins | ↓ P-gp expression | [119] |
| Cycloartanes | ↓ P-gp expression | [119] |
| Didehydrostemofolines | ↓ P-gp expression | [119] |
| Eudesmin | ↓ P-gp expression | [119] |
| Euphocharacins A-L | ↓ P-gp expression | [119] |
| Ginkgo biloba extract | ↓ P-gp expression ↓ MRP1 |
[119] |
| Grapefruit juice extracts | ↓ P-gp expression | [119] |
| Hapalosin | ↓ P-gp expression | [119] |
| Hypericin and hyperforin | ↓ P-gp expression ↓ BCRP |
[119,246] |
| Isoquinoline alkaloid, isotetrandrine | ↓ P-gp expression | [119] |
| Isostemofoline | ↓ P-gp expression | [119] |
| Jatrophanes | ↓ P-gp expression | [119] |
| Kaempferia parviflora extracts | ↓ P-gp expression ↓ MRP1 |
[119] |
| Kavalactones | ↓ P-gp expression | [119] |
| Ningalin B and derivatives | ↓ P-gp expression | [119] |
| Opiates | ↓ P-gp expression | [119] |
| Piperine | ↓ P-gp expression ↓ BCRP ↓ MRPs ↓ ABC transporter genes (ABCB1, ABCG2, and ABCC1) |
[119,120,121,122] |
| Polyoxypregnanes | ↓ P-gp expression | [119] |
| Sesquiterpenes | ↓ P-gp expression | [119,247] |
| Tenulin | ↓ P-gp expression | [104] |
| Sinensetin | ↓ P-gp expression | [119,247] |
| Taxane derivatives | ↓ P-gp expression | [119] |
| Terpenoids | ↓ P-gp expression ↓ BCRP |
[119] [246] |
| Tetrandine | ↓ P-gp expression | [119] |
| Vitamin E TPGS | ↓ P-gp expression | [119] |
| 3′-4′-7-Trimethoxyflavone | ↓ BCRP | [119,141] |
| 6-Prenylchrysin | ↓ BCRP | [119,141] |
| Eupatin | ↓ BCRP | [119] |
| Daizein | ↓ BCRP | [119] |
| Hesperetin | ↓ BCRP | [119,141,244] |
| Plumbagin | ↓ BCRP | [119] |
| Resveratrol | ↓ BCRP ↓ P-gp expression ↓ HIF-1α ↓ GST mRNA expression |
[114,133,140,253] |
| Rotenoids | ↓ BCRP | [119] |
| Stilbenoids | ↓ BCRP | [119] |
| Tectochrysin | ↓ BCRP | [119,141] |
| Tetrahydrocurcumin | ↓ BCRP | [119] |
| Ligustrazine | ↓ Expression of P-gp | [7] |
| Sophocarpidine | ↓ Expression of P-gp | [7] |
| Strychnine | ↓ Gene and protein expression of MRP | [7] |
| Three hydroxyl soy isoflavone | ↓ MRP, MDR1, MRP2 | [7] |
| Ecteinascidin | ↓ P-gp expression | [7] |
| Ecteinascidin 743 | ↓ P-gp expression ↑ Cellular accumulation of DOX/VCR in P-gp-overexpressed cervix cells |
[118] |
| 7,3′,4′-trihydroxyisoflavone | ↓ mRNA expression of MRP, MDR1, and MRP2 | [7] |
| Paeonol (extracted from the dry velamen of peony or any part of Cynanchum paniculatum) |
↓ P-g expression ↓ MDR1 ↓ MRP ↓ LRP |
[7] |
| Oroxylin A-7-glucuronide | ↓ MDR1 ↓ P-g expression |
[7] |
| 3′,4′,5′,5,7-pentamethoxyflavone (PMF) and derivatives of epimedium | ↓ MDR1 ↓ P-g expression |
[7] |
| Osthole (isolated from Fructus Cnidii) |
↓ P-g expression | [7] |
| Praeruptorin A (extracted from Radix Peucedani) |
↓MDR1 and P-gp mRNA | [7,247] |
| Diphyllin | ↓ P-gp expression | [7] |
| Emodin | ↓ P-gp expression ↓ MRP1 ↓ GSTπ ↓ Topo IIβ ↓ HIF-1α |
[113,144,215,216,254,255,256] |
| Psoralen | ↓ P-g expression | [7,242] |
| Gypenoside | ↓ BCRP ↓ P-gp expression ↓ MRP1 |
[7] |
| Allicin | ↓ MDR1 ↓ P-g expression |
[7] |
| Taccalonolide A and B (extracted from Tacca chantrieri) |
↓ P-g expression |
[7] |
| Oridonin | ↓ P-gp expression ↓ GSTπ ↓ LRP1 |
[113,144,222] |
| Ursolic acid (found in Rosmarinus officinalis) |
↓ P-gp expression | [7,100] |
| Sipholenol A (found in sponge Callyspongia siphonella) |
↓ P-g expression | [113,132,146] |
| Cantharidin (extracted from Mylabris phalerata Pallas or Mylabris cichorii L.) |
↓ P-g expression |
[7] |
| Beta-Elemene (isolated from Aeruginous Turmeric rhizome) |
↓ P-g expression ↓ MRP |
[7] [242] |
| As2O3, or white arsenic Arsenic Trioxide |
↓ P-gp expression ↓ MRP |
[7,242] |
| Artemisinin | ↓ P-gp expression | [242] |
| Artesunate | ↓ P-gp expression | [242] |
| Baicalin | ↓ P-gp expression ↓ MRP1 |
[242] |
| Berberine (isolated from ancient Chinese herb Coptis chinensis French) |
↓ P-gp expression ↓ABCG2 |
[242] [246] |
| Carnosic acid (Rosemary) |
↓ P-gp expression | [114,134,144] |
| Chelerythrine | ↓ P-gp expression | [242] |
| Gambogic acid | ↓ P-gp expression | [242] |
| Neferine | ↓ P-gp expression | [242] |
| Oxymatrine | ↓ P-gp expression | [242] |
| Peimine | ↓ LRP | [242] |
| Sodium norcantharidate | ↓ P-gp expression ↓ MRP |
[242] |
| Brucea Javanica | ↓ P-gp expression ↓ MRP |
[242] |
| Cinobufacini | ↓ P-gp expression ↓ MRP1 |
[242] |
| Grape seed polyphenols | ↓ P-gp expression | [124,242] |
| Hyaluronate Oligomers | ↓ P-gp expression ↓ MRP |
[242] |
| Jew ear | ↓ P-gp expression ↓ MRP |
[242] |
| Radix notoginseng | ↓ P-gp expression | [242] |
| Rhizoma pinelliae | ↓ P-gp expression | [242] |
| Realgar | ↓ P-gp expression | [242] |
| Thallus laminariae | ↓ P-gp expression | [242] |
| Algerian propolis | ↓ transport function of P-gp-pump | [257] |
| Dihydroptychantol A (isolated from A. angusta) |
↓ P-g expression |
[250] [258] |
| Riccardin F (isolated from P. intermedium) |
↓ P-gp expression |
[258] |
| Riccardin D | ↓ Topo II ↓ P-gp expression |
[214] |
| Andrographolid | ↓ P-gp expression | [94] |
| Parthenolide | ↓ Pgp expression | [94] |
| Rhei Rhizoma, Scutellariae Radix, Poria, Zizyphi Fructus, Zingiberis Rhizoma, Asiasari Radix, Sophorae Radix (herbal extract) |
↓ P-gp expression |
[94] |
| Tripterygium wilfordii | ↓ P-gp expression ↓ EGFR |
[94] |
| Shenghe Powder (consisting of Radix codonopsis pilosulae, Radix pseudostellariae, Radix scrophulariae, Rhizoma atractylodis macrocephalae, and 6 additional herbs) |
↓ P-gp expression |
[94] |
| Shen-qi-jian-wei Tang | ↓ MDR1 ↓ LRP |
[94] |
| Yu Ping Feng San (YPFS) (Astragali Radix, Atractylodis Macrocephalea Rhizoma, and Saposhnikoviae Radix) |
↓ ATP-binding cassette transporters ↓ GST |
[178] |
| Chinese supplement energy and nourish lung (SENL) herbs (ginsenoside Rg1, ginsenoside Rb1, ginsenoside Rg3, astragaloside IV, ophiopogonin D, and tetrandrine) |
↓ GSTπ |
[193] |
| Icaritin | ↓ P-gp expression | [118,120] |
| Icariin | ↓ P-gp expression | [118] |
| Sesquiterpene ester 1 | ↓ P-gp expression | [118] |
| Celafolin A-1 | ↓ P-gp expression | [118] |
| Celorbicol ester | ↓ P-gp expression | [118] |
| Demethoxycurcumin | ↓ P-gp expression | [118] |
| Euphomelliferine | ↓ P-gp expression | [118] |
| Euphodendroidin D | ↓ P-gp expression | [118,247] |
| Pepluanin A | ↓ P-gp expression | [118,247] |
| Sipholenone E | ↓ P-gp expression | [118,247] |
| Siphonellinol D | ↓ P-gp expression | [118] |
| GUT-70 (From C. Brasiliense) |
↓ P-gp expression | [118] |
| Lamellarin I | ↓ P-gp expression | [118] |
| Wogonin | ↓ P-gp expression ↓ MRP1 |
[118] |
| Aposterol A | ↓ P-gp expression ↓ MRP1 |
[118] |
| Fumitremorgin C | ↓ BCRP ↓ P-gp expression ↓ MRP1 |
[109,132,162] |
| Tryprostatin A | ↓ BCRP | [118] |
| Terrein | ↓ BCRP | [118] |
| Lamellarin O | ↓ BCRP ↓ P-gp expression |
[118] |
| Secalonic acid D | ↓ BCRP ↓ P-gp expression ↓ MRP1 |
[118] |
| Quinine and its isomer quinidine | ↓ P-gp expression |
[120] |
| Reserpine and yohimbine (isolated from Rauwolfia serpentine) |
↓ BCRP ↓ P-gp expression |
[120] |
| Bromocriptine ergot alkaloid |
↓ P-gp expression |
[120] |
| β-Sitosterol-O-glucoside | ↓ P-gp expression | [120] |
| cardiotonic steroid 3 | ↓ P-gp expression | [120] |
| Menthol | ↓ P-gp expression | [120] |
| Aromadendrene | ↓ P-gp expression | [120] |
| Citronellal | ↓ P-gp expression | [120] |
| Citronellol | ↓ P-gp expression | [120] |
| Carnosol | ↓ P-gp expression | [100,120] |
| Limonin | ↓ P-gp expression | [120] |
| Kaempferide | ↓ BCRP ↓ P-gp expression |
[141,244] |
| Diosmin | ↓ P-gp expression | [244] |
| Daidzein | ↓ BCRP | [141,244] |
| Tanshinone microemulsion | ↓ P-gp expression | [124] |
| Tea polyphenol | ↓ P-gp expression | [124] |
| Stemocurtisine | ↓ P-gp expression | [120] |
| Stemofoline | ↓ P-gp expression | [120] |
| Oxystemokerrine | ↓ P-gp expression | [120] |
| Amurensin G (from Vitis amurensis) | ↓ P-gp expression | [241] |
| Sakuranetin | ↓ P-gp expression | [141] |
| Floretin | ↓ P-gp expression | [141] |
| Fisetin | ↓ P-gp expression ↓ GST |
[141,192] |
| Xanthohumol (derived from Humulus lupulus) |
↓ mRNA expression of P-gp, MRP1, MRP2 and MRP3 | [141] |
| Silybin (isolated from Silybum marianum) |
↓ MRP1 ↓ P-gp expression |
[141] |
| Sophoraisoflavone A | ↓ MRP1 | [141] |
| LANGDU (a traditional herbal medicine) |
↓ P-g expression | [246] |
| Tanshinone IIA (isolated from Salvia miltiorrhiza) | ↓ MRP1 ↓ BCRP ↓ P-g expression |
[246] |
| Auraptene (grapefruit) | ↓ P-g expression | [100] |
| Nimbolide | ↓ P-gp gene | [140] |
| Marsdenia tenacissima | ↓ P-g expression ↓ ABCG2 ↓ MRP1 |
[97] |
| Taxifolin | ↓ ABCB1 ↓ P-gp expression |
[243] |
| Heterotheca inuloides Cass. | ↓ MDR1 ↓ MRP1 ↓ BCRP |
[98] |
| Saikosaponin D | ↓ MDR1 gene ↓ P-gp expression |
[259] |
| Kanglaite (isolated from Coix lacryma-jobi) |
↓ MDR1 ↓ MRP2 ↓ BCRP |
[240] |
|
Astragalus membranaceus polysaccharides Astragaloside II, another component from A. membranaceus |
↓ P-gp expression ↓ MDR1 |
[254] |
| Wilforine | ↓ P-gp expression | [112] |
|
Boswellia serrata extracts 3- O-acetyl-11-keto-β-boswellic acid (AKBA), the major active ingredient of the gum resin from Boswellia serrata and Boswellia carteri Birdw |
↓ P-gp expression | [255] |
| Pervilleine F | ↓ P-gp expression | [247] |
| Ellipticine | ↓ P-gp expression | [247] |
| Cnidiadin | ↓ P-gp expression | [247] |
| Conferone | ↓ P-gp expression | [247] |
| Rivulobirin A | ↓ P-gp expression | [247] |
| Dicamphanoyl khellactone (DCK) | ↓ P-gp expression | [247] |
| Cannabidiol | ↓ P-gp expression | [247] |
| Taccalonolides A | ↓ P-gp expression | [247] |
| Jolkinol B | ↓ P-gp expression | [247] |
| Portlanquinol | ↓ P-gp expression | [247] |
| Dihydro-β-agarofuran | ↓ P-gp expression | [247] |
| Pentadeca-(8,13)-dien-11-yn-2-one | ↓ P-gp expression | [247] |
| Silibinin | ↓ P-gp expression | [247] |
| Nirtetralin | ↓ P-gp expression | [247] |
| Cordycepin | ↓ P-gp expression | [104] |
| Nuciferine | ↓ HIF-1α | [235] |
| Dauriporphine | ↓ P-g expression | [138] |
| Glaucine | ↓ P-g expression ↓ MDR1 ↓ MRP1 |
[138] |
| Hernandezine | ↓ P-g expression | [138] |
| Antofine | ↓ P-g expression ↓ MDR1 mRNA |
[138] |
| Harmine | ↓ BCRP | [132,133,138] |
| Tryptanthrin | ↓ P-g expression ↓ MRP2 |
[138] |
| Lobeline (from Lobelia inflate) |
↓ P-g expression | [134,138] |
| Tetramethylpyrazine | ↓ P-g expression ↓ MDR1 mRNA ↓ MRP1, MRP2, MRP3 |
[105,138,144,238] |
| Danshensu and tetramethylpyrazine (from the Chinese herbs) | ↓ P-g expression | [238] |
| Acrimarine E | ↓ P-g expression | [138] |
| Gravacridonetriol | ↓ MDR1 mRNA | [138] |
| 2-Methoxycitpressine I | ↓ P-g expression | [138] |
| Capsaicin (extracted from Capsicum annuum) |
↓ P-g expression | [114,138] |
| Acacetin | ↓ BCRP ↓ MRP1 |
[133,138] |
| Amorphigenin | ↓ P-g expression | [138] |
| Apigenin | ↓ BCRP ↓ MRP1 ↓ P-g expression ↓ HIF-1α |
[138,143,144,145,240] |
| Ampelopsin | ↓ P-g expression | [138] |
| Biochanin A | ↓ BCRP ↓ MRP1 ↓ P-g expression |
[132,133,138,143] |
| Catechin | ↓ ATPase activity ↓ P-g expression |
[138] |
| Chalcone | ↓ MRP1 ↓ P-g expression |
[138] [143] |
| Chrysin | ↓ BCRP ↓ P-g expression |
[138] [133,143] |
| Diosmetin | ↓ BCRP | [138] |
| Green tea catechins (EGCG, ECG, CG) | ↓ P-g expression ↓ MDR1 ↓ ATPase activity |
[114,143] |
| Epicatechin gallate | ↓ P-g expression | [132,138] |
| Epigallocatechin gallate | ↓ P-g expression ↓ MDR1 ↓ ABCG2 ↓ HIF-1α |
[113,114,132,138,143,144,241] |
| Formononetin | ↓ P-g expression | [138] |
| Genistein | ↓ BCRP ↓ MRP1 |
[132,133,138,143] |
| Glabridin | ↓ P-g expression | [114,138,145] |
| 3,3′,4′,5,6,7,8- Heptamethoxyflavone | ↓ P-g expression | [138] |
| Kaempferol | ↓ BCRP ↓ MRP1 ↓ P-g expression |
[134,138,143,145] |
| Luteolin | ↓ BCRP ↓ MRP1 |
[138,143] |
| Morin | ↓ P-g expression ↓ MRP1 |
[132,133,138,143] |
| Myricetin | ↓ MRP1 and MRP2 activity ↓ Calcein efflux |
[105,133,138,143,145] |
| Naringenin | ↓ P-g expression | [134,138,143] |
| Naringenin-7-glucosid | ↓ BCRP | [138] |
| Nobiletin (found in citrus fruit) | ↓ P-g expression ↓ MRP1 |
[114,138,143,146] |
| Phloretin | ↓ P-g expression ↓ MRP1 |
[132,133,138,143] |
| Procyanidine | ↓ P-g expression | [138] |
| Quercetin | ↓ MRP1-mediated drug transport ↓ BCRP ↓ MRP1, 4 and 5. ↓ P-g expression ↓ PKC ↓ HIF-1α ↓ MDR1 |
[103,111,113,132,133,134,138,143,144,145,146,181,182,260,261,262] |
| Robinetin | ↓ MRP1 and MRP2 activity (inhibited calcein efflux) | [138] |
| Rotenone | ↓ P-g expression | [138] |
| Silymarin | ↓ P-gp ATPase activity ↓ P-gp-mediated cellular efflux ↓ [3 H]azidopine photoaffinity labeling of P-gp suggesting a direct interaction with the P-gp substrate binding ↓ MRP1-mediated drug transport ↓ BCRP |
[132,133,138,143,145] |
| Tangeretin | ↓ P-g expression ↓ BCRP |
[132,138,143,146] |
| Curcumin | ↓ P-g expression ↓ BCRP ↓ MRP1 ↓ MDR1 mRNA ↓ ABCG2 and ABCC1 ↓ PKC-α and –ζ ↓ GSTπ ↓ Topo IIα ↓ HIF-1α |
[103,105,113,114,132,133,134,138,144,180,212,252,262,263,264,265,266,267] |
| Matairesinol (found in soybean (Glycine max)) |
↓ P-g expression ↓ MRP1 |
[114,138] |
| Sesamin | ↓ P-g expression | [114,138] |
| Gomisin A | ↓ P-g expression | [138] |
| Schisandrol A | ↓ P-g expression | [138] [133] |
| Chlorogenic acid | ↓ P-gp ATPase activity | [138] |
| Ginkgolic acid | ↑ DNR accumulation ↓ P-g expression |
[138] |
| Agnuside | ↓ P-gp ATPase activity | [138] |
| Picroside-II | ↓ P-gp ATPase activity | [138] |
| Santonin | ↓ P-gp ATPase activity | [138] |
| beta-Amyrin | ↓ P-g expression | [138] |
| Glycyrrhetinic acid (Enoxolone) (Licorice) |
↓ P-g expression ↓ MRP1 |
[114,138] |
| Obacunone | ↓ P-g expression | [138] |
| Oleanolic acid | ↓ P-g expression | [138,146] |
| Uvaol | ↓ P-g expression | [138,146] |
| Alisol B 23-acetate | ↓ P-g expression | [113,133,138] |
| Ginsenoside Rg3 | ↓ Binding of [3 H] azidopine to P-gp ↓ P-g expression |
[133,138] |
| Protopanaxatriol ginsenosides 20S-ginsenoside Ginsenoside Rb1 Ginsenoside Rg3 |
↓ P-g expression ↓ BCRP ↓ MRP1 ↓ MDR1 ↓ LRP |
[113,133,138,144,146] |
| Tenacigenin B: P8, P26 and P27 | ↓ P-g expression ↓ MRP1 ↓ ABCG2-mediated efflux |
[138] |
| Tenacigenin B: P2, P3 and P6 | ↓ P-g expression ↓ MRP1 |
[138] |
| Tenacigenin B: P1, P4, P5, P9 and P28 | ↓ P-g expression | [138] |
| Aurochrome | ↓ P-g expression | [138] |
| Diepoxycarotene | ↓ P-g expression | [138] |
| Mutatochrome | ↓ P-g expression | [138] |
| Clausarin | ↓ P-gp-mediated drug efflux | [138] |
| Phyllodulcin | ↑ DNR accumulation (inhibition of P-gp-mediated efflux of DNR) | [138] |
| Acteoside (Verbascosine) | ↓ P-gp ATPase activity | [138] |
| Berbamine | ↓ MDR1 gene expression | [138,144] |
| Glaucine | ↓ P-g expression ↓ MRP1 ↓ MDR1 and MRP1 genes |
[138] |
| Fangchinoline | ↓ P-g expression | [138] |
| O-(4-ethoxyl-butyl)- berbamine | ↓ MDR1 gene expression | [138] |
| Tetrandrine (dried root of Stephania tetrandra) |
↓ P-g expression ↓ LRP |
[103,113,135,138,144] |
| Matrine | ↓ P-g expression | [138] |
| Antofine | ↓ MDR1 mRNA ↓ P-g expression |
[138] |
| Ephedrine | ↓ MDR1 mRNA ↓ P-g expression |
[138,144] |
| Indole-3-carbinol | ↓ P-g expression | [138] |
| Staurosporine | ↓ P-g expression ↓ MDR1 gene expression |
[138] |
| Vauqueline | ↓ MDR1 mRNA ↓ P-g expression |
[138] |
| Gravacridonetriol | ↓ MDR1 mRNA | [138] |
| Clitocine | ↓ MDR1 mRNA ↓ P-g expression) |
[138] |
| Sulfinosine | ↓ MDR1 mRNA ↓ P-g expression |
[138] |
| Bisdemethoxycurcumin | ↓ P-gp expression ↓ MDR1 |
[132,138] |
| Honokiol and magnolol (isolated from Magnolia officinali) | ↓ MDR1 ↓ P-gp expression |
[113,138] |
| Schisandrin A (Deoxyschizandrin) | ↓ P-gp expression ↓ MDR1 ↓ PKC |
[104,105,113,133,137,138,146] |
| Schisandrin B (Sch B) | ↓ P-gp expression and P-gp mediated efflux of Dox. ↓ MRP1 |
[104] |
| Triptolide | ↓ MDR1 ↓ MRP1 protein expression |
[138] |
| Pyranocoumarins | ↓ P-gp expression ↓ MDR1 mRNA expression |
[133,138] |
| Ginger phytochemicals (6-Gingerol,10- Gingerol) |
↓ P-gp expression ↓ MRP1 |
[114,138] |
| Ginger phytochemicals (6-gingerol, 10-gingerol, 4-shogaol, 6-shogaol, 10-shogaol, and 6-dehydrogingerdione) |
↓ GSTπ ↓ MRP1 |
[221] |
| Alisma orientalis | ↓ P-gp expression | [252] |
| Piper methysticum | ↓ P-gp expression | [252] |
| Guggulsterone | ↓ P-gp expression ↓ MRPs |
[113,114,134,252] |
| Phenolic diterpenes | ↓ P-gp expression | [252] |
| Vincristine | ↓ P-gp expression | [252] |
| 5-Bromotetrandrine | ↓ P-gp expression | [133] |
| Abietane diterpene | ↓ P-gp expression | [133] |
| Amooranin | ↓ P-gp expression | [133] |
| Baicalein and derivatives | ↓ P-gp expression ↓ MRPs |
[103,132,133,134,143,146] |
| Bitter melon extract | ↓ P-gp expression | [133] |
| Bufalin | ↓ P-gp expression | [133] |
| Cannabinoids | ↓ P-gp expression ↓ BCRP ↓ MRPs |
[133] |
| β-Carotene | ↓ P-gp expression | [116,133] |
| Fucoxanthin | ↓ GST | [201] |
| Catechins | ↓ P-gp expression | [111,133,143] |
| Cepharanthine | ↓ P-gp expression ↓ MRP1 |
[133] |
| Coumarins | ↓ P-gp expression | [133] |
| Cycloartanes | ↓ P-gp expression | [133] |
| Didehydrostemofolines | ↓ P-gp expression | [133] |
| Eudesmin | ↓ P-gp expression | [133] |
| Euphocharacins A-L | ↓ P-gp expression | [133] |
| Ginkgo biloba extract | ↓ P-gp expression ↓ MRP1 |
[133] |
| Grapefruit juice extracts | ↓ P-gp expression | [133] |
| Hapalosin | ↓ P-gp expression | [133] |
| Hypericin and hyperforin | ↓ P-gp expression ↓ BCRP |
[133,262] |
| Isoquinoline alkaloid, isotetrandrine | ↓ P-gp expression | [133] |
| Isostemofoline | ↓ P-gp expression | [133] |
| Jatrophanes | ↓ P-gp expression | [133] |
| Kaempferia parviflora extracts | ↓ P-gp expression ↓ MRP1 |
[133] |
| Kavalactones | ↓ P-gp expression | [133] |
| Ningalin B and derivatives | ↓ P-gp expression | [133] |
| Opiates | ↓ P-gp expression | [133] |
| Piperine | ↓ P-gp expression ↓ BCRP ↓ MRPs ↓ ABC transporter genes (ABCB1, ABCG2, and ABCC1) |
[133,134,135,136] |
| Polyoxypregnanes | ↓ P-gp expression | [133] |
| Sesquiterpenes | ↓ P-gp expression | [133,146] |
| Tenulin | ↓ P-gp expression | [107] |
| Sinensetin | ↓ P-gp expression | [133,146] |
| Taxane derivatives | ↓ P-gp expression | [133] |
| Terpenoids | ↓ P-gp expression ↓ BCRP |
[133] [262] |
| Tetrandine | ↓ P-gp expression | [133] |
| Vitamin E TPGS | ↓ P-gp expression | [133] |
| 3′-4′-7-Trimethoxyflavone | ↓ BCRP | [133,143] |
| 6-Prenylchrysin | ↓ BCRP | [133,143] |
| Eupatin | ↓ BCRP | [133] |
| Daizein | ↓ BCRP | [133] |
| Hesperetin | ↓ BCRP | [133,143,145] |
| Plumbagin | ↓ BCRP | [133] |
| Resveratrol | ↓ BCRP ↓ P-gp expression ↓ HIF-1α ↓ GST mRNA expression |
[114,133,140,253] |
| Rotenoids | ↓ BCRP | [133] |
| Stilbenoids | ↓ BCRP | [133] |
| Tectochrysin | ↓ BCRP | [133,143] |
| Tetrahydrocurcumin | ↓ BCRP | [133] |
| Ligustrazine | ↓ Expression of P-gp | [113] |
| Sophocarpidine | ↓ Expression of P-gp | [113] |
| Strychnine | ↓ Gene and protein expression of MRP | [113] |
| Three hydroxyl soy isoflavone | ↓ MRP, MDR1, MRP2 | [113] |
| Ecteinascidin | ↓ P-gp expression | [113] |
| Ecteinascidin 743 | ↓ P-gp expression ↑ Cellular accumulation of DOX/VCR in P-gp-overexpressed cervix cells |
[132] |
| 7,3′,4′-trihydroxyisoflavone | ↓ mRNA expression of MRP, MDR1, and MRP2 | [113] |
| Paeonol (extracted from the dry velamen of peony or any part of Cynanchum paniculatum) |
↓ P-g expression ↓ MDR1 ↓ MRP ↓ LRP |
[113] |
| Oroxylin A-7-glucuronide | ↓ MDR1 ↓ P-g expression |
[113] |
| 3′,4′,5′,5,7-pentamethoxyflavone (PMF) and derivatives of epimedium | ↓ MDR1 ↓ P-g expression |
[113] |
| Osthole (isolated from Fructus Cnidii) |
↓ P-g expression | [113] |
| Praeruptorin A (extracted from Radix Peucedani) |
↓MDR1 and P-gp mRNA | [113,146] |
| Diphyllin | ↓ P-gp expression | [113] |
| Emodin | ↓ P-gp expression ↓ MRP1 ↓ GSTπ ↓ Topo IIβ ↓ HIF-1α |
[113,144,215,216,254,255,256] |
| Psoralen | ↓ P-g expression | [113,144] |
| Gypenoside | ↓ BCRP ↓ P-gp expression ↓ MRP1 |
[113] |
| Allicin | ↓ MDR1 ↓ P-g expression |
[113] |
| Taccalonolide A and B (extracted from Tacca chantrieri) |
↓ P-g expression |
[113] |
| Oridonin | ↓ P-gp expression ↓ GSTπ ↓ LRP1 |
[113,144,222] |
| Ursolic acid (found in Rosmarinus officinalis) |
↓ P-gp expression | [113,114] |
| Sipholenol A (found in sponge Callyspongia siphonella) |
↓ P-g expression | [113,132,146] |
| Cantharidin (extracted from Mylabris phalerata Pallas or Mylabris cichorii L.) |
↓ P-g expression |
[113] |
| Beta-Elemene (isolated from Aeruginous Turmeric rhizome) |
↓ P-g expression ↓ MRP |
[113] [144] |
| As2O3, or white arsenic Arsenic Trioxide |
↓ P-gp expression ↓ MRP |
[113,144] |
| Artemisinin | ↓ P-gp expression | [144] |
| Artesunate | ↓ P-gp expression | [144] |
| Baicalin | ↓ P-gp expression ↓ MRP1 |
[144] |
| Berberine (isolated from ancient Chinese herb Coptis chinensis French) |
↓ P-gp expression ↓ABCG2 |
[144] [262] |
| Carnosic acid (Rosemary) |
↓ P-gp expression | [114,134,144] |
| Chelerythrine | ↓ P-gp expression | [144] |
| Gambogic acid | ↓ P-gp expression | [144] |
| Neferine | ↓ P-gp expression | [144] |
| Oxymatrine | ↓ P-gp expression | [144] |
| Peimine | ↓ LRP | [144] |
| Sodium norcantharidate | ↓ P-gp expression ↓ MRP |
[144] |
| Brucea Javanica | ↓ P-gp expression ↓ MRP |
[144] |
| Cinobufacini | ↓ P-gp expression ↓ MRP1 |
[144] |
| Grape seed polyphenols | ↓ P-gp expression | [103,144] |
| Hyaluronate Oligomers | ↓ P-gp expression ↓ MRP |
[144] |
| Jew ear | ↓ P-gp expression ↓ MRP |
[144] |
| Radix notoginseng | ↓ P-gp expression | [144] |
| Rhizoma pinelliae | ↓ P-gp expression | [144] |
| Realgar | ↓ P-gp expression | [144] |
| Thallus laminariae | ↓ P-gp expression | [144] |
| Algerian propolis | ↓ transport function of P-gp-pump | [268] |
| Dihydroptychantol A (isolated from A. angusta) |
↓ P-g expression |
[252] [269] |
| Riccardin F (isolated from P. intermedium) |
↓ P-gp expression |
[269] |
| Riccardin D | ↓ Topo II ↓ P-gp expression |
[237] |
| Andrographolid | ↓ P-gp expression | [105] |
| Parthenolide | ↓ Pgp expression | [105] |
| Rhei Rhizoma, Scutellariae Radix, Poria, Zizyphi Fructus, Zingiberis Rhizoma, Asiasari Radix, Sophorae Radix (herbal extract) |
↓ P-gp expression |
[105] |
| Tripterygium wilfordii | ↓ P-gp expression ↓ EGFR |
[105] |
| Shenghe Powder (consisting of Radix codonopsis pilosulae, Radix pseudostellariae, Radix scrophulariae, Rhizoma atractylodis macrocephalae, and 6 additional herbs) |
↓ P-gp expression |
[105] |
| Shen-qi-jian-wei Tang | ↓ MDR1 ↓ LRP |
[105] |
| Yu Ping Feng San (YPFS) (Astragali Radix, Atractylodis Macrocephalea Rhizoma, and Saposhnikoviae Radix) |
↓ ATP-binding cassette transporters ↓ GST |
[219] |
| Chinese supplement energy and nourish lung (SENL) herbs (ginsenoside Rg1, ginsenoside Rb1, ginsenoside Rg3, astragaloside IV, ophiopogonin D, and tetrandrine) |
↓ GSTπ |
[220] |
| Icaritin | ↓ P-gp expression | [132,134] |
| Icariin | ↓ P-gp expression | [132] |
| Sesquiterpene ester 1 | ↓ P-gp expression | [132] |
| Celafolin A-1 | ↓ P-gp expression | [132] |
| Celorbicol ester | ↓ P-gp expression | [132] |
| Demethoxycurcumin | ↓ P-gp expression | [132] |
| Euphomelliferine | ↓ P-gp expression | [132] |
| Euphodendroidin D | ↓ P-gp expression | [132,146] |
| Pepluanin A | ↓ P-gp expression | [132,146] |
| Sipholenone E | ↓ P-gp expression | [132,146] |
| Siphonellinol D | ↓ P-gp expression | [132] |
| GUT-70 (From C. Brasiliense) |
↓ P-gp expression | [132] |
| Lamellarin I | ↓ P-gp expression | [132] |
| Wogonin | ↓ P-gp expression ↓ MRP1 |
[132] |
| Aposterol A | ↓ P-gp expression ↓ MRP1 |
[132] |
| Fumitremorgin C | ↓ BCRP ↓ P-gp expression ↓ MRP1 |
[109,132,162] |
| Tryprostatin A | ↓ BCRP | [132] |
| Terrein | ↓ BCRP | [132] |
| Lamellarin O | ↓ BCRP ↓ P-gp expression |
[132] |
| Secalonic acid D | ↓ BCRP ↓ P-gp expression ↓ MRP1 |
[132] |
| Quinine and its isomer quinidine | ↓ P-gp expression |
[134] |
| Reserpine and yohimbine (isolated from Rauwolfia serpentine) |
↓ BCRP ↓ P-gp expression |
[134] |
| Bromocriptine ergot alkaloid |
↓ P-gp expression |
[134] |
| β-Sitosterol-O-glucoside | ↓ P-gp expression | [134] |
| cardiotonic steroid 3 | ↓ P-gp expression | [134] |
| Menthol | ↓ P-gp expression | [134] |
| Aromadendrene | ↓ P-gp expression | [134] |
| Citronellal | ↓ P-gp expression | [134] |
| Citronellol | ↓ P-gp expression | [134] |
| Carnosol | ↓ P-gp expression | [114,134] |
| Limonin | ↓ P-gp expression | [134] |
| Kaempferide | ↓ BCRP ↓ P-gp expression |
[143,145] |
| Diosmin | ↓ P-gp expression | [145] |
| Daidzein | ↓ BCRP | [143,145] |
| Tanshinone microemulsion | ↓ P-gp expression | [103] |
| Tea polyphenol | ↓ P-gp expression | [103] |
| Stemocurtisine | ↓ P-gp expression | [134] |
| Stemofoline | ↓ P-gp expression | [134] |
| Oxystemokerrine | ↓ P-gp expression | [134] |
| Amurensin G (from Vitis amurensis) | ↓ P-gp expression | [270] |
| Sakuranetin | ↓ P-gp expression | [143] |
| Floretin | ↓ P-gp expression | [143] |
| Fisetin | ↓ P-gp expression ↓ GST |
[143,218] |
| Xanthohumol (derived from Humulus lupulus) |
↓ mRNA expression of P-gp, MRP1, MRP2 and MRP3 | [143] |
| Silybin (isolated from Silybum marianum) |
↓ MRP1 ↓ P-gp expression |
[143] |
| Sophoraisoflavone A | ↓ MRP1 | [143] |
| LANGDU (a traditional herbal medicine) |
↓ P-g expression | [262] |
| Tanshinone IIA (isolated from Salvia miltiorrhiza) | ↓ MRP1 ↓ BCRP ↓ P-g expression |
[262] |
| Auraptene (grapefruit) | ↓ P-g expression | [114] |
| Nimbolide | ↓ P-gp gene | [164] |
| Marsdenia tenacissima | ↓ P-g expression ↓ ABCG2 ↓ MRP1 |
[106] |
| Taxifolin | ↓ ABCB1 ↓ P-gp expression |
[111] |
| Heterotheca inuloides Cass. | ↓ MDR1 ↓ MRP1 ↓ BCRP |
[112] |
| Saikosaponin D | ↓ MDR1 gene ↓ P-gp expression |
[271] |
| Kanglaite (isolated from Coix lacryma-jobi) |
↓ MDR1 ↓ MRP2 ↓ BCRP |
[272] |
|
Astragalus membranaceus polysaccharides Astragaloside II, another component from A. membranaceus |
↓ P-gp expression ↓ MDR1 |
[273] |
| Wilforine | ↓ P-gp expression | [110] |
|
Boswellia serrata extracts 3- O-acetyl-11-keto-β-boswellic acid (AKBA), the major active ingredient of the gum resin from Boswellia serrata and Boswellia carteri Birdw |
↓ P-gp expression | [274] |
| Pervilleine F | ↓ P-gp expression | [146] |
| Ellipticine | ↓ P-gp expression | [146] |
| Cnidiadin | ↓ P-gp expression | [146] |
| Conferone | ↓ P-gp expression | [146] |
| Rivulobirin A | ↓ P-gp expression | [146] |
| Dicamphanoyl khellactone (DCK) | ↓ P-gp expression | [146] |
| Cannabidiol | ↓ P-gp expression | [146] |
| Taccalonolides A | ↓ P-gp expression | [146] |
| Jolkinol B | ↓ P-gp expression | [146] |
| Portlanquinol | ↓ P-gp expression | [146] |
| Dihydro-β-agarofuran | ↓ P-gp expression | [146] |
| Pentadeca-(8,13)-dien-11-yn-2-one | ↓ P-gp expression | [146] |
| Silibinin | ↓ P-gp expression | [146] |
| Nirtetralin | ↓ P-gp expression | [146] |
| Cordycepin | ↓ P-gp expression | [107] |
| Nuciferine | ↓ HIF-1α | [275] |