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Cytotoxic Activity of Abietane Diterpenoids From Roots of Salvia Sahendica by Hplc-Based Activity Profiling Publisher



Moradiafrapoli F1, 2 ; Shokrzadeh M3 ; Barzegar F4 ; Gorjibahri G5 ; Zadali R6 ; Ebrahimi SN7
Authors
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Authors Affiliations
  1. 1. Department of Pharmacognosy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
  2. 2. Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland
  3. 3. Department of Toxicology, Faculty of Pharmacy, Mazandaran Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari, Iran
  4. 4. Department of Clinical Pharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
  5. 5. Department of Pharmaceutical Biotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  6. 6. Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  7. 7. Department of Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid Beheshti University, Evin, Tehran, Iran

Source: Revista Brasileira de Farmacognosia Published:2018


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. © 2018 Sociedade Brasileira de Farmacognosia. Published by Elsevier Editora Ltda.