96(P35) 植物由来のトポイソメラーゼII阻害活性を有するポリフェノール類(ポスター発表の部)

概要

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DNA topoisomerase II can relax supercoiled DNA and resolve knotted or catenated DNA rings. Therefore, functional significance of the enzyme seems to be involved in proliferative processes such as DNA replication, chromosome condensation, and chromosome segregation. By above mentioned reason, topoisomerase II inhibitors are noted as cellular targets of anticancer and antimicrobial agents. In the course of our screening program of topoisomerase II inhibitors, we isolated many inhibitory polyphenols (sixty-two compounds) together with five new compounds from the plants belonging to the Guttiterae, the Leguminosae, the Cyperaceae, the Cupressaceae, and the Berberidaceae, respectively. These structures were characterized by a combination of various NMR technique including COSY, HMBC and NOESY, and chemical evidences. From kobresia neparensis, a stilbene tetramer (2) and two stilbene trimers (1 and 3) were isolated as new resveratrol oligomer, in addition two new lignans, 4 from thujopsis dolabrata and 5 from mahonia japonica. After inhibitory screening of isolated polyphenols against topoisomerase II, sixteen compounds were found to show significant inhibitory activity. Particularly, a xanthone 6 and five stilbene oligomers 1, 2, 3, 8, 9, 10, 11, and 13 exhibited potent inhibitory activity at less than 1μg/ml concentration (MIC).
天然有機化合物討論会の論文
1997-07-20