Research Article

Cytotoxic Constituents of the Bark of Hypericum roeperianum towards Multidrug-Resistant Cancer Cells

Table 1

Recorded IC50 values after 72 h incubation of drug-sensitive and MDR cancer cells lines with botanicals from the bark of Hypericum roeperianum.

Cell linesSamples, IC50 values in µg/mL, and degrees of resistance or selectivity index
HRBHRBaHRBa1HRBa2HRBa3HRBa4HRBa5HRBb

CCRF-CEM13.71±0.2615.65±1.1846.42 ± 1.9817.87±1.5316.81±4.0216.27±4.2857.15 ± 3.7648.76 ± 2.83
CEM/ADR500011.43±0.8818.56±1.74>8020.18±1.7623.03 ± 1.2213.55±0.44>8031.55 ± 2.28
Degree of resistance0.841.19>1.721.131.370.83>1.160.65
MDA-MB-231-pcDNA19.87±1.7723.12 ± 1.6572.23 ± 4.5420.42±1.7128.32 ± 1.5718.13±2.0868.91 ± 6.3048.12 ± 1.99
MDA-MB-231-BCRP18.22±0.8126.42 ± 3.0163.16 ± 3.3019.89±0.6224.41 ± 1.7717.66±1.1174.32 ± 3.9237.23 ± 4.51
Degree of resistance0.921.140.870.970.860.971.080.77
HCT116 (p53+/+)26.75 ± 1.2334.52 ± 1.7459.10 ± 3.0633.44 ± 3.6230.76 ± 1.6128.43 ± 3.01>8031.19 ± 1.26
HCT116 (p53/)17.44±2.0141.17 ± 3.14>8024.58 ± 3.4833.63 ± 3.7728.09 ± 1.75>8029.52 ± 0.98
Degree of resistance0.651.190.741.090.990.95
U87MG12.42±0.6618.03±1.7747.84 ± 4.3618.01±1.1916.13±2.0418.44±2.1147.89 ± 2.2446.55 ± 2.43
U87MG.ΔEGFR14.36±1.4820.12±0.8159.60 ± 5.1213.92±2.0718.72±1.4515.52±0.8855.20 ± 4.7928.30 ± 1.11
Degree of resistance1.161.121.250.771.160.841.150.60
HepG217.45±2.0529.17 ± 1.30>8018.75±1.4125.88 ± 1.5614.95±1.34>8069.48 ± 2.93
AML1242.09 ± 1.17>80>8061.34 ± 3.3956.12 ± 2.6765.17 ± 4.31>80>80
Selectivity index2.41>2.743.272.174.561.15

(): the degree of resistance was determined as the ratio of the IC50 value in the resistant divided by the IC50 in the sensitive cell line; CEM/ADR5000, MDA-MB-231-BCRP, HCT116 (p53/), and U87MG.ΔEGFR were used as the corresponding resistant counterpart for CCRF-CEM, MDA-MB-231-pcDNA, HCT116 (p53+/+), and U87MG, respectively; (): the selectivity index was determined as the ratio of the IC50 value in the normal AML12 hepatocytes divided by the IC50 in HepG2 hepatocarcinoma cells; in bold: significant cytotoxic effect [7, 39, 40]; nd: not determined; HRB: crude methanol extract from the bark of Hypericum roeperianum, HRBa: portion obtained by exhaustion of HRB with ethyl acetate; HRBa1-5: fractions from HRBa; HRBb: residual fraction obtained after exhaustion of HRB with ethyl acetate. The data for doxorubicin used as positive control in similar experimental conditions are shown in Table 2.