title: Topoisomerase I and II inhibitory constituents from the bark of Tilia amurensis.
abstract: Two coumarins (1 and 6), one flavan-3-ol (2), one fatty acid (3), and two lignan glycosides (4 and 5) were isolated from the EtOAc and CH(2)Cl(2) extract of the bark of Tilia amurensis. Their chemical structures were identified by comparing their physicochemical and spectral data with those of published in literatures. Compounds 4, 5, and 6 were isolated from Tilia genus for the first time. Compounds 2 and 3 showed potent inhibitory activity against both DNA topoisomerase I (IC(50) values; 49 microM and 4 microM, respectively, with 18 microM of positive control compound, comptothecin) and DNA topoisomerase II (IC(50) values; 13 microM and 3 microM, respectively, with 50 microM of positive control compound, etoposide). However, all compounds did not showed cytotoxicity against the human colon adenocarcinoma cell line (HT-29), the human breast adenocarcinoma cell line (MCF-7), and human liver hepatoblastoma cell line (HepG-2).
authors.affiliation: College of Pharmacy, Yeungnam University, Gyongsan 712-749, Korea.
authors.forename: Jae-Young
authors.initials: JY
authors.lastname: Choi
authors.forename: Chang-Seob
authors.initials: CS
authors.lastname: Seo
authors.forename: Ming-Shan
authors.initials: MS
authors.lastname: Zheng
authors.forename: Chong-Soon
authors.initials: CS
authors.lastname: Lee
authors.forename: Jong-Keun
authors.initials: JK
authors.lastname: Son
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003374:Coumarins / Q000302:isolation & purification / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D017705:Lignans / Q000302:isolation & purification / Q000494:pharmacology; D024301:Plant Bark / Q000737:chemistry; D021241:Spectrometry, Mass, Electrospray Ionization; D032384:Tilia / Q000737:chemistry*; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003374:Coumarins; D004791:Enzyme Inhibitors; D017705:Lignans; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors