Society for the Coordination of Therapeutic Research, Algajola, France;
Department of Biotechnology, School of Applied Sciences, REVA University, Bangalore, India;
Anticancer Res. 2021 Dec;41(12):5997-6001. doi: 10.21873/anticanres.15418.
BACKGROUND/AIM: Rhenium(I)-diselenoether (Re-diSe) is a drug under development for the treatment of metastatic cancers, with selective inhibitory effects on MDA-MB231 cancer cells compared to normal HEK-293 cells, and with greater effects than its diselenide (di-Se) ligand. Rhenium (Re) compounds inhibit cathepsins, which are important proteolytic enzymes in cancer. This study investigated the effects of Re-diSe and di-Se on the production of cathepsins B and S in MDA-MB231 malignant and HEK-293 normal cells and their inhibitory effects following treatment with different doses for 72 h.
Elisa tests were used to assay the amount of cathepsins B and S in the medium of cultures.
Re-diSe, but not diSe affected the viability of malignant cells and the expression of cathepsins B and S.
To the best of our knowledge, this is the first demonstration that Re-diSe may decrease the production of cathepsins B and S in cancer cells at doses as low as 10 μM.
背景/目的：铼（I）-二硒醚（Re-diSe）是一种正在开发的用于治疗转移性癌症的药物，与正常 HEK-293 细胞相比，对 MDA-MB231 癌细胞具有选择性抑制作用，其效果大于其二硒化物（di-Se）配体。铼（Re）化合物抑制组织蛋白酶，组织蛋白酶是癌症中重要的蛋白水解酶。本研究探讨了 Re-diSe 和 di-Se 对 MDA-MB231 恶性和 HEK-293 正常细胞中组织蛋白酶 B 和 S 的产生的影响，以及用不同剂量处理 72 小时后对其的抑制作用。
使用 Elisa 试验检测培养物中组织蛋白酶 B 和 S 的量。
Re-diSe 而非 di-Se 影响恶性细胞的活力和组织蛋白酶 B 和 S 的表达。
据我们所知，这是首次证明 Re-diSe 可在低至 10 μM 的剂量下降低癌细胞中组织蛋白酶 B 和 S 的产生。
