| Literature DB >> 25843566 |
Jamal Kasaian1, Fatemeh Mosaffa1, Javad Behravan1, Milena Masullo2, Sonia Piacente2, Morteza Ghandadi1, Mehrdad Iranshahi3.
Abstract
In the present study, fifteen sesquiterpene coumarins were isolated and purified from different Ferula species, and were tested for their MDR reversal properties. Enhancement of doxorubicin cytotoxicity in MCF-7/Adr cells (doxorubicin resistant derivatives of MCF-7 cells overexpressing P-gp), when combined with very non-toxic concentrations of the sesquiterpene coumarins (50 μM) including umbelliprenin, farnesiferol B, farnesiferol C and lehmferin, proved significant MDR reversal activity of these coumarins. Flow cytometric efflux assay confirmed that the intracellular accumulation of Rho123 was significantly increased in MCF-7/Adr cells when treated with sesquiterpene coumarins. A deeper insight into the structure-activity relationship of sesquiterpene coumarins revealed that ring-opened drimane-type sesquiterpene coumarins including farnesiferol B, farnesiferol C and lehmferin possessed the best inhibitory effects on P-gp pump efflux and they could be considered as lead scaffolds for further structure modifications.Entities:
Keywords: Antiproliferation; Cancer; Multidrug resistance; P-gp; Sesquiterpene coumarins
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Year: 2015 PMID： 25843566 DOI： 10.1016/j.fitote.2015.03.025
Source DB: PubMed Journal: Fitoterapia ISSN： 0367-326X Impact factor: 2.882