Center for Integrated Oncology (CIO), Department of Internal Medicine III, University Hospital Bonn, Sigmund-Freud-Str. 25, 53105 Bonn, Germany.
In Vivo. 2011 Jan-Feb;25(1):99-103.
It was recently confirmed that the antifungal agent ciclopirox olamine inhibits Wnt/beta catenin signaling in myeloma. Piroctone olamine (PO) has very similar chemical features to ciclopirox olamine.
This study investigated the antitumor effect of PO in vitro and in vivo in a murine myeloma model.
PO demonstrated a major apoptotic activity in various human and murine myeloma and lymphoma cell lines, as well as in human primary cells. In vivo, tumor growth, as well as overall survival, was significantly reduced in mice treated with PO as compared to untreated mice. Interestingly, concerning tumor growth and survival of the animals, a significant additive effect was seen by the combination of lenalidomide plus PO as compared to single application.
These results reveal a significant selective induction of apoptosis by PO and suggest a significant in vivo effect against myeloma.
最近证实抗真菌剂环吡酮胺能抑制骨髓瘤中的 Wnt/β 连环蛋白信号通路。吡罗克酮乙醇胺(PO)具有与环吡酮胺非常相似的化学特征。
本研究在鼠骨髓瘤模型中体外和体内研究了 PO 的抗肿瘤作用。
PO 对各种人源和鼠源骨髓瘤和淋巴瘤细胞系以及人原代细胞表现出很强的凋亡活性。在体内,与未治疗的小鼠相比,PO 治疗的小鼠的肿瘤生长和总生存期明显降低。有趣的是,关于动物的肿瘤生长和存活,与单独应用相比,来那度胺加 PO 的联合应用显示出显著的相加效应。
这些结果揭示了 PO 对细胞凋亡的显著选择性诱导,并提示其对骨髓瘤具有显著的体内作用。