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由色胺酮合成卤代Phaitanthrin A及其对DNA的切割作用
Synthesis and DNA-Cleavage Activities of Halogenated-Phaitanthrin A Based on Tryptanthrin
【摘要】 色胺酮(Tryptanthrin)和Phaitanthrin A是药用植物马蓝(Strobilanthes cusia)、蓼蓝(Polygonum tinetoriumL.)、菘蓝(Isatis tinctoria L.)的生物碱有效成分。本文以卤代色胺酮:8-溴色胺酮(1)和8-碘色胺酮(2)为底物,在溶剂热条件下,一步合成8-Br-Phaitanthrin A(3)和8-I-Phaitanthrin A(4),通过1H NMR、13C NMR及X-射线单晶衍射方法确定化合物3、4的结构和手性构型。光谱法和凝胶电泳法研究表明,两个卤代Phaitanthrin A均对DNA具有较强的切割作用。
【Abstract】 Tryptanthrin and phaitanthrin A are active alkaloids derived from Strobilanthes cusia,Polygonum tinetoriumL.,and Isatis tinctoria L.In this study,halogenated tryptanthrin of 8-bromo-tryptanthrin(1) and 8-iodine tryptanthrin(2) were used as substrate to synthesize 8-Br-Phaitanthrin A(3) and 8-I-Phaitanthrin A(4) under solvothermal conditions.The structures and chiral configuration of the synthesized compounds were determined by 1HNMR,13CNMR and Xray diffraction.Spectroscopy and gel electrophoresis had shown that compounds 3 and 4 had a strong cleavage action towards DNA.
- 【文献出处】 天然产物研究与开发 ,Natural Product Research and Development , 编辑部邮箱 ,2017年03期
- 【分类号】TQ460.1;Q523
- 【被引频次】1
- 【下载频次】75