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

Autor: Ghina Alameh, Agnès Emptoz-Bonneton, Marc Rolland de Ravel, Eva L. Matera, Elisabeth Mappus, Patrick Balaguer, Luc Rocheblave, Thierry Lomberget, Charles Dumontet, Marc Le Borgne, Michel Pugeat, Catherine Grenot, Claude Y. Cuilleron
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Zdroj: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 684-691 (2019)
Druh dokumentu: article
ISSN: 1475-6366
1475-6374
14756366
DOI: 10.1080/14756366.2019.1575825
Popis: 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.
Databáze: Directory of Open Access Journals
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