Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives
Resistance to chemotherapy in cancer patients has been correlated to the overexpression of the ATPbinding cassette (ABC) drug transporters including P-glycoprotein (P-gp) that actively efflux chemotherapeutic drugs from cancer cells. We examined the mutidrug resistance reversing property of stemofol...
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th-cmuir.6653943832-480372018-04-25T08:46:58Z Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives Sonthaya Umsumarng Komsak Pintha Pornsiri Pitchakarn Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Araya Jatisatienr Stephen G. Pyne Pornngarm Limtrakul Resistance to chemotherapy in cancer patients has been correlated to the overexpression of the ATPbinding cassette (ABC) drug transporters including P-glycoprotein (P-gp) that actively efflux chemotherapeutic drugs from cancer cells. We examined the mutidrug 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. © 2013 The Pharmaceutical Society of Japan. 2018-04-25T08:46:58Z 2018-04-25T08:46:58Z 2013-04-01 Journal 13475223 00092363 2-s2.0-84876493908 10.1248/cpb.c12-00967 https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84876493908&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/48037 |
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Resistance to chemotherapy in cancer patients has been correlated to the overexpression of the ATPbinding cassette (ABC) drug transporters including P-glycoprotein (P-gp) that actively efflux chemotherapeutic drugs from cancer cells. We examined the mutidrug 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. © 2013 The Pharmaceutical Society of Japan. |
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Sonthaya Umsumarng Komsak Pintha Pornsiri Pitchakarn Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Araya Jatisatienr Stephen G. Pyne Pornngarm Limtrakul |
spellingShingle |
Sonthaya Umsumarng Komsak Pintha Pornsiri Pitchakarn Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Araya Jatisatienr Stephen G. Pyne Pornngarm Limtrakul Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives |
author_facet |
Sonthaya Umsumarng Komsak Pintha Pornsiri Pitchakarn Kwankamol Sastraruji Thanapat Sastraruji Alison T. Ung Araya Jatisatienr Stephen G. Pyne Pornngarm Limtrakul |
author_sort |
Sonthaya Umsumarng |
title |
Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives |
title_short |
Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives |
title_full |
Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives |
title_fullStr |
Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives |
title_full_unstemmed |
Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives |
title_sort |
inhibition of p-glycoprotein mediated multidrug resistance by stemofoline derivatives |
publishDate |
2018 |
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https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84876493908&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/48037 |
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