Kobayashi Y, Yamashita Y, Fujii N, Takaboshi K, Kawakami T, Kawamura M, Mizukami T, Nakano H
Tsukuba Research Laboratories, Kyowa Hakko Co., Ltd., Ibaraki, Japan.
Planta Med. 1995 Oct;61(5):414-8. doi: 10.1055/s-2006-958127.
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.
人们发现黄连水提取物具有稳定与哺乳动物DNA拓扑异构酶I形成的可裂解复合物的能力。通过生物活性导向分级分离，确定了两种原小檗碱生物碱，表小檗碱和格陵兰黄连碱，为具有体外拓扑异构酶I介导的DNA切割活性的活性成分。这两种生物碱不会诱导拓扑异构酶II介导的DNA切割。在对结构相关的原小檗碱生物碱进行进一步研究时，黄连根茎作为传统药物加工过程中产生的小檗红碱被确定为体外拓扑异构酶II介导的DNA切割的特异性诱导剂。这些结果表明，原小檗碱生物碱是一类能够与拓扑异构酶I和II诱导形成可裂解复合物的化学家族。
