title: Cytotoxic activity of withanolides isolated from Tunisian Datura metel L.
abstract: Withanolide-type steroids, withametelin Q (1) and 12α-hydroxydaturametelin B (2) along with three known withanolides, were isolated from leaves of Datura metel L. (Solanaceae). The respective structures, characterized mainly by NMR spectroscopy, were identified as (20R,22R,24R)-21,24-epoxy-1α,3β-dihydroxywitha-5,25(27)-dienolide-3-O-β-D-glucopyranoside (1) and (20R,22R,24R)-12α,21,27-trihydroxy-1-oxowitha-2,5,24-trienolide-27-O-β-D-glucopyranoside (2). The cytotoxicity of isolated compounds was evaluated against human lung carcinoma cells (A549) and human colorectal adenocarcinoma cells (DLD-1), respectively. Compound 2 exhibited cytotoxicity against A549 and DLD-1 cell lines, with IC50 values of 7 and 2.0 μM, respectively. However, for compounds 6 and 7, cytotoxicities were higher against DLD-1 cells with IC(50) values of 0.6 and 0.7 μM. Both compounds blocked the cell cycle in the S-phase and induced apoptosis.
authors.affiliation: Aromatic and Medicinal Plants Unit, Biotechnological Center in Borj-Cedria Techno-park, 901 Hammam-Lif, Tunisia.
authors.forename: Amor
authors.initials: A
authors.lastname: Bellila
authors.forename: Cindy
authors.initials: C
authors.lastname: Tremblay
authors.forename: André
authors.initials: A
authors.lastname: Pichette
authors.forename: Brahim
authors.initials: B
authors.lastname: Marzouk
authors.forename: Vakhtang
authors.initials: V
authors.lastname: Mshvildadze
authors.forename: Serge
authors.initials: S
authors.lastname: Lavoie
authors.forename: Jean
authors.initials: J
authors.lastname: Legault
mesh_terms: D045744:Cell Line, Tumor; D005591:Chemical Fractionation; D054697:Cytostatic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D058530:Datura metel / Q000737:chemistry*; D006801:Humans; D019906:Nuclear Magnetic Resonance, Biomolecular; D010936:Plant Extracts / Q000737:chemistry; D054358:Withanolides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D054697:Cytostatic Agents; D010936:Plant Extracts; D054358:Withanolides