Application of topoisomerase assays in the evaluation of natural products as antitumor agents.
Application of topoisomerase assays in the evaluation of natural products as antitumor agents.
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DOI：
10.1089/jmf.1999.2.167
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发表时间：
1999
影响因子：
2.4
通讯作者：
A. Constantinou;G. Salti
中科院分区：
文献类型：
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作者：
A. Constantinou;G. Salti
最初，DNA拓扑异构酶（topo）抑制剂作为抗生素和癌症化疗剂发现了临床应用。最近，我们证明了抑制哺乳动物topo I或topo II的植物类黄酮可用作癌症化学预防剂（Constantinou等人，1995年b）。植物化学物质可以以不同的方式抑制DNA拓扑异构酶;根据酶的模式和类型，这些可以被分类为topo I毒药，topo II毒药，topo I拮抗剂或topo II拮抗剂。正确分类拓扑异构酶抑制剂是至关重要的，因为它提供了一个重要的线索，植物剂是否可以在化学预防或化疗。我们在下面概述了一种旨在鉴定和分类拓扑异构酶I和II抑制剂的策略。
Initially, DNA topoisomerase (topo) inhibitors found clinical applications as antibiotics and cancer chemotherapeutic agents. Recently, we demonstrated that plant flavonoids that inhibit mammalian topo I or topo II might be useful as cancer chemopreventive agents (Constantinou et al., 1995b). Phytochemicals can inhibit DNA topoisomerases in different ways; depending on the mode and the type of enzyme, these can be classified as topo I poisons, topo II poisons, topo I antagonists, or topo II antagonists. Correctly classifying topo inhibitors is critical because it provides an important lead as to whether the plant agent can be useful in chemoprevention or in chemotherapy. We outline below a strategy that was designed to identify and classify topo I and II inhibitors.