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: 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.
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Zdroj: Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2019, Vol. 34 Issue 1, p684-691, 8p
Abstrakt: 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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