神经酰胺是一种具有生物活性的鞘脂，可诱导细胞凋亡。神经酰胺酶（CD酶）水解脂肪酸链，保持神经酰胺水平在检查中，并已提出作为抗癌治疗的小分子抑制剂的目标。Ceranib-2在SKOV 3细胞中以IC 50 = 28 uM抑制细胞CD酶活性，并且在高达100 uM时未显示出显著的细胞毒性。SKOV 3细胞与Ceranib-2孵育导致所有神经酰胺物质增加，鞘氨醇和S1 P呈剂量依赖性降低。Ceranib-2抑制皮下JC细胞肿瘤小鼠模型中的肿瘤生长。参考文献1）J.M德雷珀等人“人类神经酰胺酶抑制剂的发现和评价”Mol.癌症治疗2011年10月2052-20612）Vethakanraj等人，“Targeting ceramide metabolic pathway induces apoptosis in human breast cancer cell lines”Biophys.生物化学研究通讯2015年464 833-839。
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Ceramides are bioactive sphingolipids which induce apoptosis in cells. Ceramidases (CDase) which hydrolyze the fatty acid chain keep ceramide levels in check and have been proposed as a target for small-molecule inhibitors for anti-cancer therapy. Ceranib-2 inhibits cellular CDase activity with an IC50 = 28 uM in SKOV3 cells and does not show significant cytotoxity up to 100uM. Incubations of SKOV3 cells with Ceranib-2 resulted in an increase in all ceramide species and a dose-dependant decrease in sphingosine and S1P. Ceranib-2 suppressed tumor growth in a mouse model with subcutaneous JC cell tumors.References1) J.M Draper et al. "Discovery and Evaluation of Inhibitors of Human Ceramidase" Mol. Cancer Ther. 2011 10 2052-20612) H.S. Vethakanraj et al. "Targeting ceramide metabolic pathway induces apoptosis in human breast cancer cell lines" Biophys. Biochem. Res. Commun. 2015 464 833-839.
