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Table 2

Distribution of Pemetrexed and pemetrexed polyglutamate derivatives in R5 and HeLa cells grown either in folic acid or 5-formyltetrahydrofolate medium

Cells were exposed to 0.5 μM premetrexed for 2 h at 37°C. The values are expressed in unit of pmol/mg of protein. Numbers in parentheses indicate percentage of total premetrexed accumulation. Data are the average of two independent experiments.

Total PMXa accumulationPMX monoglutamatePMX diglutamatePMX triglutamatePMX tetraglutamatePMX pentaglutamate and higher
R5 in folic acid medium 15.2 3.8 (25.0%) 0.9 (5.9) 1.0 (6.6%) 1.4 (9.2%) 8.1 (53.3%) 
HeLa in folic acid medium 23.1 1.7 (7.4%) 0.6 (2.6%) 0.7 (3.0%) 1.0 (4.3%) 19.1 (82.7%) 
R5 in 5-CHO-THF medium 35.0 2.3 (6.6%) 1.0 (2.9%) 1.4 (4.0%) 1.9 (5.4%) 28.4 (81.1%) 
HeLa in 5-CHO-THF medium 41.1 1.7 (4.1%) 1.0 (2.4%) 0.9 (2.2%) 1.6 (3.9%) 35.9 (87.3%) 
Total PMXa accumulationPMX monoglutamatePMX diglutamatePMX triglutamatePMX tetraglutamatePMX pentaglutamate and higher
R5 in folic acid medium 15.2 3.8 (25.0%) 0.9 (5.9) 1.0 (6.6%) 1.4 (9.2%) 8.1 (53.3%) 
HeLa in folic acid medium 23.1 1.7 (7.4%) 0.6 (2.6%) 0.7 (3.0%) 1.0 (4.3%) 19.1 (82.7%) 
R5 in 5-CHO-THF medium 35.0 2.3 (6.6%) 1.0 (2.9%) 1.4 (4.0%) 1.9 (5.4%) 28.4 (81.1%) 
HeLa in 5-CHO-THF medium 41.1 1.7 (4.1%) 1.0 (2.4%) 0.9 (2.2%) 1.6 (3.9%) 35.9 (87.3%) 
a

PMX, Pemetrexed; 5-CHO-THF, 5-formyltetrahydrofolate.

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