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In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts
Synthetic progesterone and 5α/β-pregnane-3,20-dione derivatives were evaluated as in vitro and in vivo modulators of multidrug-resistance (MDR) using two P-gp-expressing human cell lines, the non-steroidogenic K562/R7 erythroleukaemia cells and the steroidogenic NCI-H295R adrenocortical carcinoma ce...
| Autores principales: | , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Taylor & Francis
2019
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6383615/ https://www.ncbi.nlm.nih.gov/pubmed/30777494 http://dx.doi.org/10.1080/14756366.2019.1575825 |
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| author | Alameh, Ghina Emptoz-Bonneton, Agnès Rolland de Ravel, Marc Matera, Eva L. Mappus, Elisabeth Balaguer, Patrick Rocheblave, Luc Lomberget, Thierry Dumontet, Charles Le Borgne, Marc Pugeat, Michel Grenot, Catherine Cuilleron, Claude Y. |
| author_facet | Alameh, Ghina Emptoz-Bonneton, Agnès Rolland de Ravel, Marc Matera, Eva L. Mappus, Elisabeth Balaguer, Patrick Rocheblave, Luc Lomberget, Thierry Dumontet, Charles Le Borgne, Marc Pugeat, Michel Grenot, Catherine Cuilleron, Claude Y. |
| author_sort | Alameh, Ghina |
| collection | PubMed |
| description | Synthetic progesterone and 5α/β-pregnane-3,20-dione derivatives were evaluated as in vitro and in vivo modulators of multidrug-resistance (MDR) using two P-gp-expressing human cell lines, the non-steroidogenic K562/R7 erythroleukaemia cells and the steroidogenic NCI-H295R adrenocortical carcinoma cells, both resistant to doxorubicin. The maximal effect in both cell lines was observed for 7α-O-benzoyloxy,11α(R)-O-tetrahydropyranyloxy-5β-pregnane-3,20-dione 4. This modulator co-injected with doxorubicin significantly decreased the tumour size and increased the survival time of immunodeficient mice xenografted with NCI-H295R or K562/R7 cells. |
| format | Online Article Text |
| id | pubmed-6383615 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2019 |
| publisher | Taylor & Francis |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-63836152019-02-27 In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts Alameh, Ghina Emptoz-Bonneton, Agnès Rolland de Ravel, Marc Matera, Eva L. Mappus, Elisabeth Balaguer, Patrick Rocheblave, Luc Lomberget, Thierry Dumontet, Charles Le Borgne, Marc Pugeat, Michel Grenot, Catherine Cuilleron, Claude Y. J Enzyme Inhib Med Chem Research Paper Synthetic progesterone and 5α/β-pregnane-3,20-dione derivatives were evaluated as in vitro and in vivo modulators of multidrug-resistance (MDR) using two P-gp-expressing human cell lines, the non-steroidogenic K562/R7 erythroleukaemia cells and the steroidogenic NCI-H295R adrenocortical carcinoma cells, both resistant to doxorubicin. The maximal effect in both cell lines was observed for 7α-O-benzoyloxy,11α(R)-O-tetrahydropyranyloxy-5β-pregnane-3,20-dione 4. This modulator co-injected with doxorubicin significantly decreased the tumour size and increased the survival time of immunodeficient mice xenografted with NCI-H295R or K562/R7 cells. Taylor & Francis 2019-02-19 /pmc/articles/PMC6383615/ /pubmed/30777494 http://dx.doi.org/10.1080/14756366.2019.1575825 Text en © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
| spellingShingle | Research Paper Alameh, Ghina Emptoz-Bonneton, Agnès Rolland de Ravel, Marc Matera, Eva L. Mappus, Elisabeth Balaguer, Patrick Rocheblave, Luc Lomberget, Thierry Dumontet, Charles Le Borgne, Marc Pugeat, Michel Grenot, Catherine Cuilleron, Claude Y. In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts |
| title | In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts |
| title_full | In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts |
| title_fullStr | In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts |
| title_full_unstemmed | In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts |
| title_short | In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts |
| title_sort | in vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-obz-11α(r)-othp-5β-pregnanedione in k562/r7 and h295r cell xenografts |
| topic | Research Paper |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6383615/ https://www.ncbi.nlm.nih.gov/pubmed/30777494 http://dx.doi.org/10.1080/14756366.2019.1575825 |
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