Abstract
Screening of medicinal plants from Iranian flora against human cancer cell-lines have shown that an hexane extract from roots of Salvia sahendica Boiss. & Buhse, Lamiaceae, is active against human cervical cancer (HeLa) and colorectal adenocarcinoma (Caco-2) cell-lines at the test concentration of 100 μg/ml (100% inhibition). Cytotoxicity of the extract was localized with the aid of HPLC-time-based activity profiling adapted to the tetrazolium colorimetric bioassay. Four abietane-type diterpenoids in active time-windows were identified as cytotoxic compounds namely: sahandone (1), sahandol (2), 12-deoxy-salvipisone (3) and sahandinone (4). Compound 1 showed the highest toxicity against HeLa cells (IC50 = 5.6±0.1 μg/ml), which was comparable with betulinic acid (IC50=4.3± 1.2 μg/ml), the positive control. Compound 2 was active against the HeLa cells (IC50 = 8.9 ±0.7 μg/ml) but not the Caco-2 cell-line. Compounds 1, 3 and 4 exhibited moderate activity (IC50 = 22.9–41.4 μg/ml) against the Caco-2 cells. This study reveals that the HeLa cells are more sensitive to all tested compounds than the Caco-2 cells. In silico molecular docking study showed a rigid binding of the compounds to tyrosine kinase pp60src, and proved their cytotoxic activity.
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FMF, MS, FM and GGB participated in the evaluation of cytotoxicity activity, acquisition and interpretation of data. FMS and SNE carried out phytochemical procedures and analysis. RZ carried out molecular modeling part. All the authors have contributed to critical reading of the final manuscript and approved its submission.
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Moradi-Afrapoli, F., Shokrzadeh, M., Barzegar, F. et al. Cytotoxic activity of abietane diterpenoids from roots of Salvia sahendica by HPLC-based activity profiling. Rev. Bras. Farmacogn. 28, 27–33 (2018). https://doi.org/10.1016/j.bjp.2017.11.007
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DOI: https://doi.org/10.1016/j.bjp.2017.11.007