Curcumin and its cyclohexanone analogue inhibited human Equilibrative nucleoside transporter 1 (ENT1) in pancreatic cancer cells
Jezrael L Revalde, Yan Li, Tharaka S Wijeratne, Piyush Bugde, Bill C Hawkins, Rhonda J Rosengren, James W Paxton
EUROPEAN JOURNAL OF PHARMACOLOGY | ELSEVIER SCIENCE BV | Published : 2017
Our group investigated combining the phytochemical curcumin and gemcitabine in a liposome, to improve gemcitabine's activity against pancreatic tumours. While optimising the curcumin: gemcitabine ratio for co-encapsulation, we found that increasing curcumin concentrations relative to gemcitabine resulted in antagonistic interactions. As curcumin is a promiscuous transporter inhibitor; we suspected that increased resistance occurred via inhibition of Equilibrative nucleoside transporter 1 (ENT1)-mediated gemcitabine uptake. To test our hypothesis, we determined whether curcumin and a related analogue, 2,6-bis((3-methoxy-4-hydroxyphenyl)methylene)-cyclohexanone (or A13), inhibited ENT1-mediate..View full abstract
Awarded by Auckland Medical Research Fund (AMRF)
We would like to thank Dr Frederik Pruijn for technical assistance with the scintillation counter and Pamela Murray for help with cell line authentication. This work was funded by the Auckland Medical Research Fund (AMRF) [grant no. 1113026].