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Literature summary for 7.6.2.2 extracted from
- Inhibition of P-glycoprotein activity by limonin and other secondary metabolites from Citrus species in human colon and leukaemia cell lines (2010), Eur. J. Pharmacol., 626, 139-145.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| beta-sitosterol-O-glucoside | inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents | Homo sapiens |  |
| deacetylnomilin | inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents | Homo sapiens | |
| hesperidin | inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents | Homo sapiens | |
| limonin | inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents | Homo sapiens | |
| neohesperidin | inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents | Homo sapiens | |
| stigmasterol | inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents | Homo sapiens | |
| verapamil | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + rhodamine 123/in | Homo sapiens | - |
ADP + phosphate + rhodamine 123/out | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| Caco-2 cell | - |
Homo sapiens | - |
| CEM-ADR5000 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + H2O + rhodamine 123/in | - |
Homo sapiens | ADP + phosphate + rhodamine 123/out | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| MDR1 | - |
Homo sapiens |
| P-glycoprotein | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.134 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 | Homo sapiens | beta-sitosterol-O-glucoside | |
| 0.169 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 | Homo sapiens | neohesperidin | |
| 0.174 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells | Homo sapiens | neohesperidin | |
| 0.195 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells | Homo sapiens | hesperidin | |
| 0.21 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 | Homo sapiens | stigmasterol | |
| 0.22 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 | Homo sapiens | deacetylnomilin | |
| 0.23 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 | Homo sapiens | hesperidin | |
| 0.285 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in leukaemia cell line CEM/ADR5000 | Homo sapiens | limonin | |
| 0.338 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells | Homo sapiens | beta-sitosterol-O-glucoside | |
| 0.387 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells | Homo sapiens | stigmasterol | |
| 0.478 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells | Homo sapiens | deacetylnomilin | |
| 0.52 | - |
37°C, pH is not specified in the publication. Rhodamine 123 efflux assay, in CACO-2 cells | Homo sapiens | limonin | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | mediates drug efflux from cells and plays a major role in causing multidrug resistance | Homo sapiens |
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