Ito Hiromu, Shoji Yoshimi, Matsumoto Ken-Ichiro, Fukuhara Kiyoshi, Nakanishi Ikuo
Quantum RedOx Chemistry Team, Institute for Quantum Life Science (iQLS), Quantum Life and Medical Science Directorate (QLMS), National Institutes for Quantum Science and Technology (QST), 4-9-1 Anagawa, Inage-ku, Chiba-shi, Chiba 263-8555, Japan.
Quantitative RedOx Sensing Group, Department of Radiation Regulatory Science Research, Institute for Radiological Science (NIRS), Quantum Life and Medical Science Directorate (QLMS), National Institutes for Quantum Science and Technology (QST), 4-9-1 Anagawa, Inage-ku, Chiba-shi, Chiba 263-8555, Japan.
ACS Med Chem Lett. 2023 Oct 3;14(10):1478-1481. doi: 10.1021/acsmedchemlett.3c00328. eCollection 2023 Oct 12.
Catechin is one of the best-known antioxidants and is reported to have some favorable physiological activities, including anti-cancer effects. We previously synthesized a catechin analog, planar catechin, which showed a 10-fold larger radical scavenging activity than (+)-catechin. However, the physiological effects of the planar catechin have remained unclear. In this study, we examined cytotoxicity and mitochondrial membrane potential after planar catechin treatment using a rat normal gastric mucosal cell line, RGM1, and its chemically induced cancer-like cell line, RGK1. Interestingly, the planar catechin showed remarkable cytotoxicity compared to (+)-catechin, with cancer cell specificity. Furthermore, the decrease in the mitochondrial membrane potential of cancer cells was observed at specific concentrations of the planar catechin. These results indicate that the planar catechin, possessing higher antioxidant activity, induces its anti-cancer effect through a decrease in the mitochondrial membrane potential and thus can be a promising agent for cancer treatment.
儿茶素是最著名的抗氧化剂之一,据报道具有一些有益的生理活性,包括抗癌作用。我们之前合成了一种儿茶素类似物,平面儿茶素,其自由基清除活性比(+)-儿茶素大10倍。然而,平面儿茶素的生理作用仍不清楚。在本研究中,我们使用大鼠正常胃黏膜细胞系RGM1及其化学诱导的类癌细胞系RGK1,检测了平面儿茶素处理后的细胞毒性和线粒体膜电位。有趣的是,与(+)-儿茶素相比,平面儿茶素表现出显著的细胞毒性,且具有癌细胞特异性。此外,在平面儿茶素的特定浓度下观察到癌细胞线粒体膜电位的降低。这些结果表明,具有较高抗氧化活性的平面儿茶素通过降低线粒体膜电位诱导其抗癌作用,因此有望成为一种癌症治疗药物。