Novel organobismuth(III) complex of 5H-dibenzo[c,f][1,5]oxabismocin-12(7H)-yl nitrate (C2) was synthesized and characterized by spectral and elemental analysis. It was compared with other five C,E,C-chelating (E = N, O, S) organobismuth(III) complexes against human adenocarcinoma alveolar basal epithelial cells (A549), human liver cancer cell line (SMCC7721), human gastric cancer cell line (SGC-7901), human colon adenocarcinoma cell line (SW480) and healthy human bronchial cell line (16HBE14o-) in vitro. It was found that C2 exhibited the best anticancer activity. Further mechanistic investigation indicated that toxicological activity of C2 was ascribable to apoptosis rather than anti-proliferative activity. Apoptosis was induced through up-regulating the level of Bcl-2/Bax as well as the activation of caspase-3. The results demonstrate that heterocyclic organobismuth(III) complexes of this type have great potential in the treatment of cancer.

合成了新型的5H-二苯并[ c，f ] [ 1,5 ]氧杂烟酰胺-12（7H）-硝酸硝酸根（C2）有机铋（III）配合物，并通过光谱和元素分析对其进行了表征。将其与其他五种针对人腺癌，肺泡基底膜上皮细胞（A549），人肝癌细胞系（SMCC7721），人胃癌的C，E，C-螯合（E = N，O，S）有机铋（III）配合物进行了比较细胞系（SGC-7901），人结肠腺癌细胞系（SW480）和健康人支气管细胞系（16HBE140-）。发现C2表现出最佳的抗癌活性。进一步的机理研究表明C2的毒理活性归因于细胞凋亡而不是抗增殖活性。通过上调Bcl-2 / Bax的水平以及激活caspase-3来诱导细胞凋亡。结果表明，这种类型的杂环有机铋（III）配合物在治疗癌症方面具有巨大潜力。