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Arch Pharm Res. 2012 Sep;35(9):1583-9. doi: 10.1007/s12272-012-0909-x. Epub 2012 Oct 9.

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

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College of Pharmacy, Yeungnam University, Gyongsan, 712-749, Korea.


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.

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