A series of seleno-biotin analogs were synthesized and their anticancer activity and mode of action were assessed using ovarian cancer cells. Compound 2, out of the other analogs, in direct comparison to biotin alone, more effectively reduced the cell viability and induced apoptosis in ovarian cancer cell lines in a dose dependent manner as demonstrated by the cell viability assay, trypan blue dye exclusion assay, Annexin V/7-AAD, and Caspase 3/7 apoptosis assays. Furthermore, compound 2 showed efficacy better than 5-fluorouracil (5-FU) and similar to cisplatin, in vitro; notably it was more cytotoxic to drug-resistant Hey A8 cells than cisplatin. The cytotoxicity of compound 2 was primarily mediated by reactive oxygen species (ROS) as demonstrated by DCFDA based ROS estimation. Biotin receptors (BR) saturation and the use of a BR negative cell line showed a significant decline in the cytotoxic ativity of the compound 2, confirming that its activity is BR-mediated. These experiments demonstrated that selenium modified biotin which contains an ester linked redox cycling selenocyanate group has the potential for human therapeutic applications against ovarian and other cancers over-expressing BR.

合成了一系列硒生物素类似物，并使用卵巢癌细胞评估了它们的抗癌活性和作用方式。在其他类似物中，与单独的生物素直接比较，化合物2以剂量依赖性方式更有效地降低卵巢癌细胞系的细胞活力并诱导细胞凋亡，如细胞活力测定、台盼蓝染料排除测定、膜联蛋白所示V/7-AAD 和 Caspase 3/7细胞凋亡测定。此外，化合物2在体外显示出比 5-氟尿嘧啶 (5-FU) 更好的功效，并且与顺铂相似；值得注意的是，它对耐药 Hey A8 细胞的细胞毒性高于顺铂。化合物2的细胞毒性如基于 DCFDA 的 ROS 估计所示，主要由活性氧 (ROS) 介导。生物素受体 (BR) 饱和和使用 BR 阴性细胞系显示化合物2的细胞毒性活性显着下降，证实其活性是 BR 介导的。这些实验表明，含有酯连接的氧化还原循环硒氰酸酯基团的硒改性生物素具有用于人类治疗卵巢癌和其他过度表达 BR 的癌症的潜力。