Reference - Detail
| RRC ID | 44268 |
|---|---|
| Author | Umsumarng S, Pintha K, Pitchakarn P, Sastraruji K, Sastraruji T, Ung AT, Jatisatienr A, Pyne SG, Limtrakul P. |
| Title | Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives. |
| Journal | Chem Pharm Bull (Tokyo) |
| Abstract |
Resistance to chemotherapy in cancer patients has been correlated to the overexpression of the ATP-binding cassette (ABC) drug transporters including P-glycoprotein (P-gp) that actively efflux chemotherapeutic drugs from cancer cells. We examined the multidrug resistance reversing property of stemofoline derivatives in drug-resistance human cervical carcinoma (KB-V1) and human leukemic (K562/Adr) cell lines that overexpress P-gp. Didehydrostemofoline and eleven of its derivatives were synthesized and the cytotoxicity and their effect on doxorubicin, vinblastine and paclitaxel sensitivity in drug resistant (KB-V1 and K562/Adr) and drug sensitive (KB-3-1 and K562) cell lines by a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay were determined. We found that three out of the twelve stemofoline derivatives including OH-A1, NH-B6 and NH-D6 showed commitment efficiency to increase sensitivity to doxorubicin, vinblastine and paclitaxel in KB-V1 cells and increase sensitivity to doxorubicin, and paclitaxel in K562/Adr cells whereas the effects have not been seen in their parental sensitive cancer cell lines (KB-3-1 and K562). These results indicate that stemofoline derivatives reversed P-gp-mediated multidrug resistance in vitro, and thus could be developed as effective chemosensitizers to treat multidrug-resistant cancers. The molecular mechanism of modulation of P-gp would be further determined. |
| Volume | 61(4) |
| Pages | 399-404 |
| Published | 2013-1-1 |
| DOI | 10.1248/cpb.c12-00967 |
| PII | DN/JST.JSTAGE/cpb/c12-00967 |
| PMID | 23358236 |
| MeSH | ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors* ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism Antineoplastic Agents / toxicity Cell Line, Tumor Cell Survival / drug effects Doxorubicin / toxicity Drug Resistance, Neoplasm / drug effects Heterocyclic Compounds, 4 or More Rings / chemical synthesis Heterocyclic Compounds, 4 or More Rings / chemistry* Heterocyclic Compounds, 4 or More Rings / toxicity Humans K562 Cells Paclitaxel / toxicity Vinblastine / toxicity |
| IF | 1.416 |
| Times Cited | 14 |
| WOS Category | PHARMACOLOGY & PHARMACY CHEMISTRY, MULTIDISCIPLINARY CHEMISTRY, MEDICINAL |
| Altmetric score |
オルトメトリクス指標項目
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| The most frequently cited source | X(Twitter) |
| Total number of mentions | 2 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| Human and Animal Cells | K562/Adr(RCB1898) |