Inhibition of DNA topoisomerases I and II of compounds from Reynoutria japonica

Three Anthraquinones (1, 2 and 4), three Stilbenes (5, 6 and 7) and 3,5-dihydroxybenzyl alcohol (3) were isolated from Reynoutria japonica. Their structures were identified as emodin (1), emodin-8-O-β-D-glucoside (2), 3,5-dihydroxybenzyl alcohol (3), citreorosein (4), cis-resveratrol (5), trans-resveratrol (6) and trans-resveratrol-5-O-β-D-glucopyranoside (7) by comparing their physicochemical and spectral data with published data. Compound 3 was isolated for the first time from the Polygonaceae family. Among the purified compounds, 3 showed more potent inhibitory activity against Topoisomerase I (IC₅₀: 4 μM) than camptothecin, as the positive control (IC₅₀: 18 μM). Compounds 3, 4, 5, 6 and 7 showed stronger inhibitory activities toward DNA Topoisomerase II (IC₅₀: 0.54, 14, 15, 0.77 and 3 μM, respectively) than the positive control, etoposide (IC₅₀: 44 μM). Compounds 1 and 4 displayed weak cytotoxicities against human lung Cancer (A549), ovarian Cancer (SK-OV-3), human liver hepatoblastoma (HepG2) and colon adenocarcinoma (HT-29) cell lines.