TABLE 1.
The antitumor experiment of auraptene in vitro and in vivo.
| Type of cancer | Experimental model | Dose | IC50 | Mechanism | References |
|---|---|---|---|---|---|
| Breast cancer | SW-620, MDA-MB-231, MCF-7 | 0.1–100 µM | 4.18 μg/ml | Modulation of ERs and suppression of acyl-CoA | De Medina et al. (2010) |
| Breast cancer | MDA-MB-231, MCF-7 and rat | 1–50 µM 200, 500 ppm | 85% inhibition | Inhibition of cyclin D1 | Krishnan et al. (2009) |
| Breast cancer | MCF-7 | 250 μg/ml | 61.3 μg/ml | Up-regulation of caspase-3 and caspase-8 and down-regulation of MMP9, MMP2, VEGFR-1, and VEGFR-2 | Charmforoshan et al. (2019) |
| Breast cancer | MCF-7 | 10, 20, 40 μg/ml | 17.26–29.66 μg/ml | Down-regulation of Mcl-1 mRNA | Motlagh and Gholami (2017) |
| Breast cancer | MCF-7 cells | 500 ppm | Reduction of cyclin D1 protein expression and inhibition of IGF-1 | Krishnan and Kleiner-Hancock (2012) | |
| Gastric cancer | MGC-803 cells | 0–4 µM | 0.78–10.78 µM | Expression of apoptosis- related protein | Li et al. (2018) |
| Gastric cancer | C57BL/6 mice | 100, 500 ppm | Inhibition of CD74 production | Sekiguchi et al. (2012) | |
| Gastric cancer | NCI-N87 cells | 20 µM | Reduction of ERK 1/2 activation and IL-8 production | Sekiguchi et al. (2010) | |
| Gastric cancer | SNU-1 cells | 25–200 μg/ml | ≤25 µM | Inhibition of mTOR, activation of p53 and increase in the phosphorylation of Akt | Moon et al. (2015) |
| Colon cancer | HT-29 and HT-116 cells | 10 µM | ≥50% | Suppression of CD166 and CD44 and inhibition of colonospheres | Epifano et al. (2013) |
| Colon cancer | F344 rats | 100, 500 ppm | Activation of the phase II enzymes QR and GST | Tanaka et al. (1998a); Tanaka et al. (1997) | |
| Colon cancer | C57BL/KsJ-db/db mice | 10 mg/kg | Inhibition of COX-2 and iNOS, reduction of cell proliferation and lipid profiles | Hayashi et al. (2007) | |
| Colon cancer | C57BL/KsJ-db/db mice | 10 mg/kg | 67–80% inhibition | Reduction of triglycerides and anti-inflammatory activity of auraptene | Tanaka et al. (2008) |
| Colon cancer | CD-1 (ICR) mice | 100, 500 ppm | 63–83% inhibition | Suppression of colonic inflammation and modulation of proinflammatory cytokines | Tanaka et al. (2010) |
| Colon cancer | HT-29 cell line | 1–50 µM | 2.8 and 3 µM | Suppression of proMMP-7 and inhibition of ERK1/2 | Kawabata et al. (2006b) |
| Colon cancer | ICR mice | 100, 500 ppm | Reduction of COX-2, PCNA, iNOS | Kohno et al. (2006) | |
| Colon cancer | Colonic mucosa mouse | 0.1% w/w | 82% inhibition | Inhibition of MMP-2, MMp-9 and suppression DSS | Kawabata et al. (2006a) |
| Colon cancer | HT29 cells | 10, 20 μg/ml | 39 μg/ml | Reduction of hyperthermia and down-regulation of HSP27 | Moussavi et al. (2018) |
| Colon cancer | HT29 cells | 10, 20, 40, and 80 μg/ml | 31.8–42.1% | Down regulation of CD44, ALDH1 and inhibited expression of GATA6 | Moussavi et al. (2017) |
| Hepatic cancer | F344 rats | 100, 500 ppm | 83% inhibition | Reduction of GST, TGF-α | Sakata et al. (2004) |
| Hepatic cancer | F344 rats | 100, 500 ppm | β-catenin mutation | Hara et al. (2005) | |
| Hepatic cancer | C57BL/6 mice | 30 mg/kg | Reduction of toxic bile acids, inhibition of inflammation and HSCs activation | Gao et al. (2018) | |
| Hepatic cancer | Rat | 500 ppm | Nob induction of cell cycle inhibition and apoptosis | Ohnishi et al. (2004) | |
| Hepatic cancer | RCC4 cell line | 0–100 μM | Inhibition the mitochondrial respiration and blockade HIF-1α | Jang et al. (2015) | |
| Prostate cancer | PC3 and DU145 | 30, 60 μM | 30–45% | Activation of caspase-9/3, Bax, inhibition of Bcl-2 and Mcl-1, increase the TUNEL-positive cells | Lee et al. (2017) |
| Prostate cancer | PC3 and DU145 | 500 ppm | Induction of apoptosis and cell cycle arrest | Tang et al. (2007) | |
| Skin cancer | ICR mouse skin | 18 μM | 450 μM | Inhibition of TPA and suppression of O2 − | Murakami et al. (1997) |
| Skin cancer | C57BL/6 mice | 500, 1,000 mg/kg | Induction of apoptosis, inhibition of metastasis of B16BL6 melanoma cells | Tanaka et al. (2000) | |
| Skin cancer | Xenograft mouse | 200 mg/kg | 84% inhibition | Suppression of LPS-induced NF-κB activation | Kleiner-Hancock et al. (2010) |
| Skin cancer | M4Beu melanoma | 10 μg/ml | 17.1 µM | Induction of caspase-dependent apoptosis and cell-cycle arrest | Barthomeuf et al. (2008) |
| Ovarian cancer | Hela cell line | 10, 20, 40 μg/ml | 13.33–13.87 μg/ml | Down-regulation of MCl-1 gene expression | Motlagh and Gholami (2017) |
| Ovarian cancer | Hela and A2780 cell line | 12.5–100 μM | 31.49 and 47.93 μM | Reduction of MMP-2 and MMP-9 enzymatic activity | Jamialahmadi et al. (2018) |
| Esophageal cancer | KYSE30 cells | 20 μg/ml | 76–80 μg/ml | Reduction expression of CD44, BMI-1 | Saboor-Maleki et al. (2017) |
| Esophageal cancer | KYSE30 cells | 10, 20, 40 μg/ml | 11.75–15.25 μg/ml | Down-regulation of Mcl-1 gene expression | Motlagh and Gholami (2017) |
| Leukaemia | Jurkat cells | 20 μg/ml | 16.5 μg/ml | Activation of caspase cascade, caspase-8 and caspase-3, degradation of PARP and suppression of Bcl-xL | Jun et al. (2007) |
| Leukaemia | Jurkat cells | 10, 20, 40 μg/ml | 11.3–11.49 μg/ml | Down-regulated Mcl-1 mRNA expression | Motlagh and Gholami (2017) |
| Oral carcinogenesis | F344 rats | 100, 500 ppm | 63–91% reduction | Suppression of 4-NQO activity, decreased dysplastic lesions, inhibited the expression of cell proliferation | Tanaka et al. (1998b) |