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Planta Med 1995; 61(5): 414-418
DOI: 10.1055/s-2006-958127
Paper

© Georg Thieme Verlag Stuttgart · New York

Inhibitors of DNA Topoisomerase I and II Isolated from the Coptis Rhizomes

Yoshinori Kobayashi1 , Yoshinori Yamashita2 , Noboru Fujii2 , Kouji Takaboshi1 , Toshiyuki Kawakami1 , Michio Kawamura1 , Tamio Mizukami2 , Hirofumi Nakano2
  • 1Tsukuba Research Laboratories, Kyowa Hakko Co., Ltd., 2-Miyukigaoka, Tsukuba-City, Ibaraki, 305 Japan
  • 2Tokyo Research Laboratories, Kyowa Hakko Co., Ltd., 3-6-6 Asahimachi, Machida, Tokyo, 194 Japan
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Publication History

1994

1995

Publication Date:
04 January 2007 (online)

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Abstract

A water extract of Coptis chinensis was found to have the ability to stabilize the cleavable complex with mammalian DNA topoisomerase I. As the result of bioassay-guided fractionation, two protoberberine alkaloids, epiberberine and groenlandicine, were identified as active principles with topoisomerase I-mediated DNA cleavage activity in vitro. These two alkaloids did not induce topoisomerase II-mediated DNA cleavage. During further examination of the structurally related protoberberine alkaloids, berberrubine which is produced during the processing of Coptis rhizome as traditional medicine, was identified as a specific inducer of topoisomerase II-mediated DNA cleavage in vitro. These results indicated that protoberberine alkaloids are a chemical family which can induce cleavable complexes with topoisomerases I and II.

Key words

Coptis chinensis Franch - Ranunculaceae - topoisomerase I - topoisomerase II - protoberberine - epiberberine - groenlandicine - berberrubine