Preprint / Version 1

Antiproliferative Activity of (-)-Rabdosiin Isolated from Ocimum sanctum L.

Authors

  • Alexandros Flegkas Department of Pharmacognosy and Chemistry of Natural Products, Faculty of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece; [email protected] (A.F.); [email protected] (T.M.I.); [email protected] (C.B.)
  • Tanja Ifantis Department of Pharmacognosy and Chemistry of Natural Products, Faculty of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece; [email protected] (A.F.); [email protected] (T.M.I.); [email protected] (C.B.)
  • Christina Barda Department of Pharmacognosy and Chemistry of Natural Products, Faculty of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece; [email protected] (A.F.); [email protected] (T.M.I.); [email protected] (C.B.)
  • Pinelopi Samara Department of Biology, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15784 Athens, Greece; [email protected] (P.S.); [email protected] (O.T.)
  • Ourania Tsitsilonis Department of Biology, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15784 Athens, Greece; [email protected] (P.S.); [email protected] (O.T.)
  • Helen Skaltsa Department of Pharmacognosy and Chemistry of Natural Products, Faculty of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopolis, Zografou, 15771 Athens, Greece; [email protected] (A.F.); [email protected] (T.M.I.); [email protected] (C.B.)

Keywords:

Ocimum sanctum, Lamiaceae, (-)-rabdosiin, cytotoxic activity, triterpenoids, phenolic derivatives

Abstract

Background:Ocimum sanctum L. (holy basil; Tulsi in Hindi) is an important medicinal plant, traditionally used in India. Methods: The phytochemical study of the nonpolar (dichloromethane 100%) and polar (methanol:water; 7:3) extracts yielded fourteen compounds. Compounds 6, 7, 9, 11, 12, and 13, along with the methanol:water extract were evaluated for their cytotoxicity against the human cancer cell lines MCF-7, SKBR3, and HCT-116, and normal peripheral blood mononuclear cells (PBMCs). Results: Five terpenoids, namely, ursolic acid (1), oleanolic acid (2), betulinic acid (3), stigmasterol (4), and β-caryophyllene oxide (5); two lignans, i.e., (-)-rabdosiin (6) and shimobashiric acid C (7); three flavonoids, luteolin (8), its 7-O-β-D-glucuronide (9), apigenin 7-O-β-D-glucuronide (10); and four phenolics, (E)-p-coumaroyl 4-O-β-D-glucoside (11), 3-(3,4-dihydroxyphenyl) lactic acid (12), protocatechuic acid (13), and vanillic acid (14) were isolated. Compound 6 was the most cytotoxic against the human cancer lines assessed and showed very low cytotoxicity against PBMCs. Conclusions: Based on these results, the structure of compound 6 shows some promise as a selective anticancer drug scaffold. Keywords: Ocimum sanctum, Lamiaceae, (-)-rabdosiin, cytotoxic activity, triterpenoids, phenolic derivatives

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