Reference - Detail
| RRC ID | 45319 |
|---|---|
| Author | Umsumarng S, Pitchakarn P, Sastraruji K, Yodkeeree S, Ung AT, Pyne SG, Limtrakul P. |
| Title | Reversal of human multi-drug resistance leukaemic cells by stemofoline derivatives via inhibition of P-glycoprotein function. |
| Journal | Basic Clin Pharmacol Toxicol |
| Abstract |
Our previous study reported multi-drug resistance (MDR) reversing properties of synthetic stemofoline derivatives (STFD), OH-A1, NH-B6 and NH-D6 on P-glycoprotein (P-gp) overexpressing leukaemic cells (K562/Adr); however, the mechanism was unclear. In this study, we further investigated whether the STFD reverse MDR through either the inhibition of P-gp function or expression in K562/Adr cells, or both. The P-gp functional studies showed that the STFD increased the accumulation of calcein-AM, rhodamine 123 and [(14) C]-doxorubicin in K562/Adr cells, while the effects have not been seen in their parental sensitive cancer cell line (K562). Further, the STFD did not alter the P-gp expression as determined by Western blotting. This study concludes that the STFD reverse MDR via the inhibition of P-gp function. The efficacy of the STFD to inhibit P-gp function followed the order: NH-B6 > OH-A1 > NH-D6. These compounds could be introduced as candidate molecules for treating cancers exhibiting P-gp-mediated MDR. |
| Volume | 116(5) |
| Pages | 390-7 |
| Published | 2015-5-1 |
| DOI | 10.1111/bcpt.12331 |
| PMID | 25265513 |
| MeSH | ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors* ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism Antineoplastic Agents / pharmacology* Cell Cycle Checkpoints / drug effects Cell Survival / drug effects Dose-Response Relationship, Drug Drug Resistance, Multiple / drug effects* Drug Resistance, Neoplasm / drug effects* Heterocyclic Compounds, 4 or More Rings / pharmacology* Heterocyclic Compounds, 4 or More Rings / toxicity Humans K562 Cells Leukemia, Erythroblastic, Acute / drug therapy* Leukemia, Erythroblastic, Acute / genetics Leukemia, Erythroblastic, Acute / metabolism Leukemia, Erythroblastic, Acute / pathology |
| IF | 2.651 |
| Times Cited | 6 |
| WOS Category | PHARMACOLOGY & PHARMACY TOXICOLOGY |
| Altmetric score |
オルトメトリクス指標項目
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| Total number of mentions | 0 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| Human and Animal Cells | K562(RCB1897) K562/Adr(RCB1898) |