Abstract

β-acetoxyisovalerylalkannin (β-AIVA) is one of shikonin/alkannin derivative, which were mainly extracted from Boraginaceae family. The effects of β-AIVA on human melanoma A375 cells and U918 cells were investigated in vitro. The CCK-8 assay showed that β-AIVA inhibited proliferation of cells. Results from flow cytometry, ROS assay and JC-1 assay showed that β-AIVA increased late apoptosis rate, induced the production of ROS and promoted mitochondrial depolarization in cells. β-AIVA regulated expressions of BAX and Bcl-2 proteins, and increased the expression of cleaved caspase-9 and cleaved caspase-3. These findings suggest that β-AIVA may be a potential therapeutic drug for treating melanoma.

摘要

β-乙酰氧基异戊酰基烷宁（β-AIVA）是紫草素/紫草素衍生物之一，主要从紫草科植物中提取。体外研究了β-AIVA对人黑色素瘤A375细胞和U918细胞的影响。CCK-8检测显示β-AIVA抑制细胞增殖。流式细胞术、ROS测定和JC-1测定结果表明，β-AIVA增加细胞晚期凋亡率，诱导ROS产生并促进细胞线粒体去极化。β-AIVA 调节 BAX 和 Bcl-2 蛋白的表达，并增加 cleaved caspase-9 和 cleaved caspase-3 的表达。这些发现表明β-AIVA可能是治疗黑色素瘤的潜在治疗药物。