Fedorov Sergey N, Dyshlovoy Sergey A, Kuzmich Alexandra S, Shubina Larisa, Avilov Sergey A, Silchenko Alexandra S, Bode Ann M, Dong Zigang, Stonik Valentin A
Nat Prod Commun. 2016 Sep;11(9):1239-1242.
Triterpene glycosides isolated from holothurians are natural products known to possess cytotoxic properties against cancer cells. However, their anticancer prophylactic activity has not been studied sufficiently. The anticancer prophylactic; cytotoxic, and pro-apoptotic properties of 18 triterpene glycosides, as well as their effects on the transcriptional activities of activator protein-I (AP-1) and nuclear factor-KB (NF-KB), were examined using methods that included EGF-induced JB6 C141 P' cell transformation in soft agar, flow cytometry, MTS assessment of cell viability, and a luciferase activity assay. The compounds inhibited EGF-induced neoplastic JB6 C141 P' cell transformation in soft agar and caused apoptosis and necrosis of human HL-60 and THP-I leukemia cells. AP- and NF-KB were involved in the cellular response to the treatment by the compounds. Conclusion: glycosides isolated from holothurians of Cucumariidae, Stichopodidae, Psolidae, Holothuriidae and Synaptidae families have potential for development as new antitumor agents and as instruments to study AP-I and NF-kB.
从海参中分离出的三萜糖苷是已知具有抗癌细胞细胞毒性的天然产物。然而,它们的抗癌预防活性尚未得到充分研究。使用包括软琼脂中表皮生长因子诱导的JB6 C141 P'细胞转化、流式细胞术、MTS细胞活力评估和荧光素酶活性测定等方法,研究了18种三萜糖苷的抗癌预防、细胞毒性和促凋亡特性,以及它们对激活蛋白-I(AP-1)和核因子-κB(NF-κB)转录活性的影响。这些化合物抑制了软琼脂中表皮生长因子诱导的肿瘤性JB6 C141 P'细胞转化,并导致人HL-60和THP-1白血病细胞凋亡和坏死。AP-1和NF-κB参与了细胞对这些化合物治疗的反应。结论:从瓜参科、刺参科、芋参科、海参科和锚参科海参中分离出的糖苷有潜力开发成为新型抗肿瘤药物以及研究AP-1和NF-κB的工具。