Evidence-Based Complementary and Alternative Medicine / 2020 / Article / Tab 2

Research Article

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

Table 2

Recorded IC50 values following RRA for phytochemicals isolated from the bark of Hypericum roeperianum and reference drug, doxorubicin, towards drug-sensitive, MDR cancer cells lines and hepatocytes after 72 h incubation.

Cell linesSamples, IC50 values in µM, and degrees of resistance or selectivity index
134578Doxorubicin

CCRF-CEM14.44 ± 0.5316.80 ± 0.9619.94 ± 2.1238.58 ± 2.1123.28 ± 1.4616.31 ± 2.120.02±0.00
CEM/ADR500018.27 ± 1.5652.95 ± 3.0823.21 ± 1.6638.46 ± 4.0754.04 ± 4.3843.47 ± 2.97122.96 ± 10.94
Degree of resistance1.263.151.161.002.322.666,683.00
MDA-MB-231-pcDNA16.47 ± 0.7443.80 ± 3.47>153.8575.15 ± 4.8820.73 ± 1.3236.89 ± 2.730.13±0.01
MDA-MB-231-BCRP14.95 ± 1.1733.60 ± 1.9920.38 ± 1.1762.94 ± 5.3222.16 ± 2.8830.50 ± 1.880.79±0.08
Degree of resistance0.910.77<0.130.841.070.836.14
HCT116 (p53+/+)17.36 ± 1.8446.67 ± 3.3840.17 ± 3.0975.48 ± 6.10>91.7437.79 ± 2.920.48±0.06
HCT116 (p53/)44.20 ± 3.21>165.29>153.85112.27 ± 8.49>91.74>85.471.78±0.08
Degree of resistance2.55>3.54>6.151.49nd>2.263.73
U87MG16.16 ± 1.0974.44 ± 4.75106.00 ± 6.7461.42 ± 3.3929.70 ± 1.7735.50 ± 3.280.26±0.03
U87MG.ΔEGFR14.69 ± 1.5544.98 ± 5.2230.37 ± 2.9159.04 ± 6.0112.72 ± 0.7530.61 ± 3.140.98±0.07
Degree of resistance0.910.600.290.960.430.863.79
HepG221.68 ± 3.1844.21 ± 2.6532.40 ± 3.7264.73 ± 5.7725.19 ± 1.6931.29 ± 1.194.56±0.48
AML1247.34 ± 0.81>165.2945.35 ± 3.52150.02 ± 7.0320.89 ± 1.17>85.4752.90 ± 4.09
Selectivity index2.18>3.741.402.320.83>2.7311.59

(): 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 counterparts 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], the cytotoxicity of compound 6 (betulenic acid) on these cell lines was previous reported [41], and this compound was no more tested in this study, no IC50 value was recorded at up to 100 µM with compound 2; nd: not determined; 1: trichadonic acid; 3: 2-hydroxy-5-methoxyxanthone; 4: 1,3,6,7-tetrahydroxyxanthone or norathyriol; 5: 1,3,5,6-tetrahydroxyxanthone; 7: 3′-hydroxymethyl-2′-(4″-hydroxy-3″,5″-dimethoxyphenyl)-5′,6′:5,6-(6,8-dihydroxyxanthone)-1′,4′-dioxane; and 8: 3′-hydroxymethyl-2′-(4″-hydroxy-3″,5″-dimethoxyphenyl)-5′,6′:5,6-(xanthone)-1′,4′-dioxane.

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