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. Author manuscript; available in PMC: 2009 Nov 10.
Published in final edited form as: Cancer Res. 2006 Sep 1;66(17):8847–8857. doi: 10.1158/0008-5472.CAN-06-0769

Table 2.

Drug sensitivity of platinum compounds

A. Drug sensitivity of structurally diverse platinum complexes in OCT1-transfected cells
Platinum complexes MDCK-MOCK (μmol/L) MDCK-hOCT1 (μmol/L) Resistance factor
Cisplatin 6.3 ± 0.74 3.6 ± 0.30 1.7*
Carboplatin 260 ± 86 230 ± 86 1.1
[Pt(NH3)2(trans-1,2-(OCO)2C6H10)] 21 ± 2.9 11 ± 2.7 2.0†
[Pt(en)Cl2] 33 ± 12 10 ± 4.8 3.3 *
cis-[Pt(NH3)(Cy)Cl2] 1.4 ± 0.15 0.16 ± 0.030 9.0†
Oxaliplatin 11 ± 3.7 0.48 ± 0.19 22†
[Pt(S,S-DACH)oxalato] 30 ± 14 1.4 ± 1.2 21†
[Pt(R,R-DACH)Cl2] 15 ± 3.2 0.65 ± 0.26 23†
[Pt(S,S-DACH)Cl2] 16 ± 3.7 0.57 ± 0.18 28†
B. Drug sensitivity of structurally diverse platinum complexes in OCT2-transfected cells
Platinum complexes HEK-MOCK (μmol/L) HEK-hOCT2 (μmol/L) Resistance factor
Cisplatin 2.6 ± 0.52 1.2 ± 0.54 2.1*
Carboplatin 110 ± 46 62 ± 46 1.8
[Pt(NH3)2(trans-1,2-(OCO)2C6H10)] 19 ± 5.7 9.9 ± 2.8 1.9*
[Pt(en)Cl2] 6.6 ± 1.5 1.1 ± 0.42 6.0†
cis-[Pt(NH3)(Cy)Cl2] 0.22 ± 0.043 0.020 ± 0.0065 11†
Oxaliplatin 4.1 ± 1.69 0.11 ± 0.020 37†
[Pt(S,S-DACH)oxalato] 9.0 ± 1.7 0.27 ± 0.062 33†
[Pt(R,R-DACH)Cl2] 2.1 ± 0.28 0.074 ± 0.026 28†
[Pt(S,S-DACH)Cl2] 4.5 ± 0.71 0.14 ± 0.041 33†
C. The sensitivity of the colon cancer cell lines to oxaliplatin and cisplatin in the presence or absence of cimetidine
Cell lines Oxaliplatin
 Cisplatin
Control Cimetidine treated Resistance
factor		 Control Cimetidine
treated		 Resistance
factor
HCT116‡ 2.4 ± 1.4 19 ± 6.2 7.9† 5.4 ± 1.3 10 ± 3.2 1.9*
HT29‡ 4.6 ± 1.4 52 ± 19 11† 12. ± 3.9 31 ± 11 2.5*
RKO‡ 1.6 ± 0.56 9.7 ± 2.7 5.9† 8.6 ± 2.4 13 ± 4.4 1.5
SW620‡ 2.8 ± 1.0 14 ± 2.8 5.0† 13 ± 2.0 22 ± 4.9 1.8*
LS180‡ 1.3 ± 0.41 8.4 ± 2.8 6.4† 5.7 ± 1.8 8.3 ± 3.4 1.4
DLD 11 ± 6.0 71 ± 13 6.7† 18 ± 7.6 32 ± 10 1.7§

NOTE: The IC50 values (μmol/L) of all the platinum complexes, except for carboplatin, after 7 hours of drug exposure were determined in parallel using a MTT assay as described in Materials and Methods (A and B). The data for carboplatin in (A) and (B) were taken from Table 1A and B, respectively, and were not determined simultaneously with the other compounds. The resistance factor was defined as the ratio of the mean IC50 value in the MOCK cells to that in the OCT-transfected cells. The IC50 values (μmol/L) of oxaliplatin and cisplatin in the colon cancer cell lines (7 hours of drug exposure) were determined in the presence or absence (control) of cimetidine (1.5 mmol/L) in parallel (C). The cell seeding density was 6,000, 8,000, 6,000, 15,000, 12,000, and 4,000 cells per well for HCT116, HT29, RKO, SW620, LS180, and DLD cells, respectively. When cimetidine (1.5 mmol/L) was used, it was added to the wells immediately before the addition of the platinum drugs. The resistance factor was defined as the ratio of the mean IC50 value in the presence to that in the absence of cimetidine. All the data are expressed as mean ± SD of six measurements, and each measurement was done in quadruplicate.

*

P < 0.01.

†

P < 0.001.

‡

The IC50 value of oxaliplatin is significantly lower than that of cisplatin in the absence of cimetidine.

§

P < 0.05.