RESUMO
OBJECTIVE:To study in vitro anticancer activity of conjugated linoleic acid-gemcitabine conjugate (CLA-GEM). METHODS:IC50 of different tumor cells (breast cancer MCF-7 cell,breast cancer MDA-MB-231 cell,lung cancer A549 cell, small cell lung cancer NCI-H446 cell,glioma C6 cell)were investigated after treated with different concentrations(0.001-100μmol/L)of CLA-GEM and gemcitabine(GEM)for 72 h;survival rates of MCF-7 cell were investigated after treated with above so-lution for 24,48 and 72 h. The dependence of 0.001-100 μmol/L CLA-GEM and GEM to nucleoside transporter was investigated (by IC50)through MCF-7 cells and MDA-MB-231 cells treated with nucleoside transporter inhibitors(NBMPR,100 μmol/L)and di-pyridamole(4 μg/ml). The change of MCF-7 cell cycle was investigated after treated with 1 μmol/L CLA-GEM and GEM for 24 h. RESULTS:Compared with GEM,IC50 of MCF-7,MDA-MB-231 and NCI-H446 cells became lower after treated with CLA- GEM (P0.05). Survival rate of MCF-7 cells de-creased significantly after treated with GEM for 48 h and CLA-GEM for 24 h. Survival rate of MCF-7 cells was the lowest,being 21% after treated with GEM for 72 h,while tumor cells were sacrificed by CLA-GEM completely. Compared with GEM or CLA-GEM,IC50 of MCF-7 and MDA-MB-231 cells increased significantly after treated with NBMPR,dipyridamole combined with GEM (P0.05). Compared with GEM,CLA-GEM could prolong 6% of S stage of MCF-7 cells (P<0.01). CONCLU-SIONS:Compared with GEM,CLA-GEM exhibits significant antitumor activity and rapid action,and it isn’t influenced by nucle-ic acid transportation.