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色胺酮是一种天然吲哚喹唑啉生物碱,具有抗微生物、抗肿瘤和抗炎活性。以色胺酮(Try)为配体,溶剂热法合成色胺酮Zn(Ⅱ)配合物,通过X-射线单晶衍射分析,确定了金属配合物的晶体结构。光谱法研究及琼脂糖凝胶电泳实验表明,色胺酮及其Zn(Ⅱ)配合物均表现出较强的稳定G-四链体H21T-DNA作用,结合常数Kb>107,而且对p BR322质粒DNA也表现出较强的切割作用,色胺酮锌(Ⅱ)配合物的切割作用强于配体色胺酮。研究结果为进一步筛选色胺酮及其配合物的抗肿瘤活性以及探讨生物碱与G4-DNA的稳定作用构效关系及设计生物碱抗肿瘤药物提供了参考。
Tryptamine is a natural indole quinazoline alkaloid with anti-microbial, anti-tumor and anti-inflammatory activity. The tryptamine (Try) was used as ligand and solvothermal method to synthesize Zn (Ⅱ) complexes of tryptamine. The crystal structure of metal complexes was confirmed by X-ray single crystal diffraction analysis. Spectroscopic studies and agarose gel electrophoresis showed that both the tryptamine and its Zn (II) complexes showed a strong and stable G-quadruplex H21T-DNA binding constant Kb> 107, and pBR322 Plasmid DNA also showed a stronger cleavage effect, and the cleavage of the zinc (II) -selenate complex was stronger than that of the tryptophan ligand. The results provide a reference for further screening antitumor activity of tryptanthrin and its complexes and exploring the structure-activity relationship between alkaloids and G4-DNA and designing anticancer drugs of alkaloids.