Wang Cong, Yang Dongxiao, Jiang Liping, Wang Saiqi, Wang Junwei, Zhou Kairui, Shi Xiaoli, Chang Liming, Liu Ying, Ke Yu, Liu Hongmin
Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Collaborative Innovative Center of New Drug Research and Safety Evaluation, Key Laboratory of Henan Province for Drug Quality and Evaluation, Zhengzhou University School of Pharmaceutical Sciences, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.
Department of Pharmacy, The Third Affiliated Hospital Of Xinxiang Medical University, 83 Hualan Avenue, Xinxiang, Henan 453003, China.
Bioorg Med Chem Lett. 2017 May 1;27(9):2058-2062. doi: 10.1016/j.bmcl.2017.02.008. Epub 2017 Feb 7.
The novel compound jesridonin, has extensive anti-tumor activity. In this study, we aim to investigate the cytotoxic effects of jesridonin in combination with paclitaxel. Our results showed that jesridonin in combination with paclitaxel had synergistic cytotoxic effects on human esophageal carcinoma both in vitro and in vivo. Hoechst 33258 staining and the Annexin-V FITC assay demonstrated that paclitaxel synergized with jesridonin in a stronger induction of apoptosis than treatment with paclitaxel or jesridonin alone. Western blotting results revealed that the synergistic apoptosis-induction effects of paclitaxel and jesridonin were mediated by the mitochondrial pathway. This may provide a novel strategy to overcome drug resistance for esophageal cancer therapy.
新型化合物杰斯里多宁具有广泛的抗肿瘤活性。在本研究中，我们旨在研究杰斯里多宁与紫杉醇联合使用的细胞毒性作用。我们的结果表明，杰斯里多宁与紫杉醇联合使用在体外和体内对人食管癌均具有协同细胞毒性作用。Hoechst 33258染色和膜联蛋白V-FITC检测表明，与单独使用紫杉醇或杰斯里多宁相比，紫杉醇与杰斯里多宁联合使用能更强地诱导细胞凋亡。蛋白质印迹结果显示，紫杉醇和杰斯里多宁的协同凋亡诱导作用是由线粒体途径介导的。这可能为克服食管癌治疗中的耐药性提供一种新策略。
