Potential antitumor agents: flavones and their derivatives from Linaria reflexa Desf.
The antiproliferative activity of several flavonoids isolated from Linaria reflexa Desf. (Scrophulariaceae) was evaluated in vitro by the SRB assay against the large cell lung carcinoma cell line COR-L23, hepatocellular carcinoma cell line HepG-2, renal adenocarcinoma cell line ACHN, amelanotic melanoma cell line C32, colorectal adenocarcinoma cell line Caco-2, and normal human fetal lung MRC5. Chemical modifications, that is acetylation, hydrolysis of rutinose unit, and hydrolysis of the terminal rhamnose unit, were performed on pectolinarin. Pectolinarin exhibited strong cytotoxic activity on COR-L23, Caco-2, and C32 cell lines with an IC50 of 5.03, 6.18, and 7.17 microM. Similar activities were recorded for the three natural monoacetyl pectolinarin derivatives linariin, isolinariin A, and isolinariin B. In contrast, peracetylpectolinarin displayed only marginal activity.
Tundis
Rosa
R
Department of Pharmaceutical Science, University of Calabria, I-87030 Rende (CS), Italy. rosa.tundis@unical.it
Deguin
Brigitte
B
Loizzo
Monica R
MR
Bonesi
Marco
M
Statti
Giancarlo A
GA
Tillequin
François
F
Menichini
Francesco
F
D000107:Acetylation; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002867:Chromones / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D047309:Flavones / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D032221:Linaria / Q000737:chemistry*; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D002867:Chromones; D047309:Flavones; C052786:pectolinarin