Abstract
BackgroundShikonin derivatives have cytotoxic and antitumor effects. This study aims to investigate the antitumor effects of acetylshikonin isolated from a Chinese medicinal herb Arnebia euchroma (Royle) Johnst.MethodsThe 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to determine the in vitro antitumor effects of acetylshikonin on human lung adenocarcinoma cell line A549, human hepatocellular carcinoma cell line Bel-7402, human breast adenocarcinoma cell line MCF-7 and mouse Lewis lung carcinoma (LLC) cell line. C57BL/6 mice with LLC model were used to study the in vivo antitumor effects of acetylshikonin. The expression of bax, bcl-2 and caspase-3 proteins in LLC tissue was determined with immunohistochemical staining.ResultsIn A549, Bel-7402, MCF-7 and LLC cell lines, acetylshikonin inhibited cell growth in a dose-dependent manner. IC50 (means ± SD) were 5.6 ± 0.86 μg/ml, 6.82 ± 1.5 μg/ml, 3.04 ± 0.44 μg/ml and 2.72 ± 0.38 μg/ml respectively. Acetylshikonin suppressed tumor growth in C57BL/6 mice with LLC. The inhibition rate of acetylshikonin (2 mg/kg) was 42.85%. Immunohistochemical staining revealed that in the acetylshikonin groups the expression of bax and caspase-3 increased, whereas the expression of bcl-2 decreased, suggesting that acetylshikonin induced tumor cell apoptosis through activating the pro-apoptotic bcl-2 family and caspase-3.ConclusionAcetylshikonin isolated from Arnebia euchroma (Royle) Johnst cell suspension cultures exhibits specific in vivo and in vitro antitumor effects.
Highlights
Shikonin derivatives have cytotoxic and antitumor effects
This study aims to evaluate the in vivo and in vitro antitumor effects of acetylshikonin extracted from the cell suspension cultures of Arnebia euchroma (Royle) Johnst
Cells treated with 25.6 μg/ml acetylshikonin became round in shape and condensed nuclei were seen, many of which lost intact membranes, leading to necrosis (Figure 2)
Summary
Shikonin derivatives have cytotoxic and antitumor effects. This study aims to investigate the antitumor effects of acetylshikonin isolated from a Chinese medicinal herb Arnebia euchroma (Royle) Johnst. Arnebia euchroma (Royle) Johnst (Ruanzicao), a Chinese medicinal herb that induces apoptosis and exerts antitumor effects, is used to treat inflammatory diseases and cancer [1]. E.g. shikonin, acetylshikonin (Figure 1), β, β-dimethyl-acrylshikonin, are active components in Arnebia euchroma (Royle) Johnst. Natural shikonin-like compounds have in vitro inhibitory effects on malignant carcinoma cells. Zhen et al [2] showed that shikonin induced apoptosis of human malignant melanoma A375-S2 cells via activated p53 and caspase-9 pathways. Yoon et al [3] found that shikonin induced HL60 cells apoptosis via caspase-3 dependent pathways. Gao et al [4] reported that shikonin reacted with cellular thiols such as glutathione, and that the depletion of cellular thiols induced apoptosis in HL60
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