Zhu Minyu, Ying Jinwei, Lin Chaowei, Wang Yu, Huang Kelun, Zhou Yang, Teng Honglin
Department of Spine Surgery, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, China.
Planta Med. 2019 Mar;85(5):360-369. doi: 10.1055/a-0791-1049. Epub 2018 Nov 23.
The aim of the present study was to investigate the cytotoxic and antitumour effects of baicalin in human chondrosarcoma both and . We examined the effects of baicalin on the growth and apoptosis of human chondrosarcoma cells. Baicalin inhibited the growth of SW1353 and CH2879 cells in a dose- and time-dependent manner, but did not inhibit the growth of normal chondrocytes. Baicalin reduced tumour growth and induced apoptotic death in SW1353-transplanted nude mice without reducing their body weight. Further studies showed that baicalin reduced the mitochondrial membrane potential, upregulated the expression of Bax and cytoplasmic cytochrome c, downregulated the expression of Bcl-2 and mitochondrial cytochromes, and activated caspase-3 and caspase-9. Baicalin inhibited the phosphoinositide 3-kinase/protein kinase B/mammalian target of rapamycin pathway by decreasing the expression of phosphorylated phosphoinositide 3-kinase, phosphorylated protein kinase B, and phosphorylated mammalian target of rapamycin both and . Moreover, the mice that received SC79 and baicalin exhibited a greater tumour size compared with the mice that received baicalin. The mice that received LY294002 and baicalin showed a smaller tumour size compared with the mice that received baicalin. In the study, SC79 and LY294002 affected the baicalin-induced cytotoxic effects on chondrosarcoma cells in the same manner. Our data suggest baicalin has therapeutic efficacy in human chondrosarcoma through the induction of apoptosis and inhibition of the phosphoinositide 3-kinase/protein kinase B/mammalian target of rapamycin pathway. Baicalin can be considered a potential therapeutic agent for treating chondrosarcomas.
本研究的目的是调查黄芩苷对人软骨肉瘤的细胞毒性和抗肿瘤作用。我们检测了黄芩苷对人软骨肉瘤细胞生长和凋亡的影响。黄芩苷以剂量和时间依赖性方式抑制SW1353和CH2879细胞的生长，但不抑制正常软骨细胞的生长。黄芩苷可减少SW1353移植裸鼠的肿瘤生长并诱导凋亡性死亡，且不降低其体重。进一步研究表明，黄芩苷降低线粒体膜电位，上调Bax和细胞质细胞色素c的表达，下调Bcl-2和线粒体细胞色素的表达，并激活caspase-3和caspase-9。黄芩苷通过降低磷酸化磷脂酰肌醇3激酶、磷酸化蛋白激酶B和磷酸化雷帕霉素靶蛋白的表达，抑制磷脂酰肌醇3激酶/蛋白激酶B/雷帕霉素哺乳动物靶标通路。此外，与接受黄芩苷的小鼠相比，接受SC79和黄芩苷的小鼠肿瘤体积更大。与接受黄芩苷的小鼠相比，接受LY294002和黄芩苷的小鼠肿瘤体积更小。在 研究中，SC79和LY294002以相同方式影响黄芩苷诱导的对软骨肉瘤细胞的细胞毒性作用。我们的数据表明，黄芩苷通过诱导凋亡和抑制磷脂酰肌醇3激酶/蛋白激酶B/雷帕霉素哺乳动物靶标通路，对人软骨肉瘤具有治疗效果。黄芩苷可被视为治疗软骨肉瘤的潜在治疗剂。
