The cytotoxic activity of Linum grandiflorum leaves

Abstract

The CHCl₃ and MeOH fractions of the leaves of Linum grandiflorum, showed cytotoxic activity against EL₄ (Murine Leukemia) cell line with IC₅₀ = 60 and 250 mg/mL respectively. Bioassay guided fractionation and isolation (BGFI) of the MeOH fraction resulted in the isolation of two new cytotoxic compounds 1 [luteolin 7-O-α-D-(6```-E-feruloyl)glucopyranosyl (1→2)-β-D-glucopyranoside] and 6 [2-[(3`-isopropoxy-O-β-D-glucopyranosyl)oxy]-2-methylbutane nitrile] against EL₄ with IC₅₀ = 0.2 and 0.3 mM/mL respectively, together with 2 [luteolin 7-O-β-D-glucopyranoside], 3 [vicenin-1], 4 [vicenin-2], 5 [vicenin-3], 7 [linamarin], 8 [lotaustralin], 9 [neolinustatin], and  10 [butan-2-O-β-D-glucopyranoside] which showed cytotoxicity against EL₄ with IC₅₀ = 0.2, 0.9, 0.8, 0.9, 0.4, 0.4, 0.2, 0.4 mM/mL respectively. BGFI of the CHCl₃ fraction revealed the isolation of three cytotoxic aryltetrahydronaphthalene-type lignans identified as 11 [podophyllotoxin], 12 [deoxypodophylotoxin] and 13 [5-methoxypodophyllotoxin] against EL₄ with IC₅₀ = 0.2, 0.09 and 0.2 mM/mL respectively. The isolated compounds were structurally elucidated using 1D, 2D NMR, HR-ESI-MS, and HR-MALDI-MS techniques.