机构：[1]Department of Neurosurgery and Institute of Neurosurgery, State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu, 610041, PR China
Glioblastoma multiforme (GBM) is one of the most common and malignant tumor. Luteolin, a polyphenolic compound, has been proposed to have anti-tumor activity against various cancers. However, the greatest obstacle in the administration of luteolin is its hydrophobicity as well as the low oral bioavailability. In this study, we formulated luteolin-loaded MPEG-PCL (Luteolin/MPEG-PCL) micelles aiming to improve its solubility in aqueous solution and investigate the anti-tumor effect on glioma in vitro and in vivo. The spherical Luteolin/MPEG-PCL micelles were completely dispersible in normal saline and could release luteolin in a sustained manner in vitro. We demonstrated that Luteolin/MPEG-PCL micelles had stronger cytotoxicity and induced a higher percentage of apoptosis in C6 and U87 cells than free luteolin in vitro. The immunohistochemical study revealed that Luteolin/MPEG-PCL micelles induced more glioma cell apoptosis than free luteolin and inhibited neovascularization in tumor tissues. The Pro-caspase9 and Bcl-2 down-regulation and cleaved-caspase9 and Bax up-regulation suggested that luteolin induced apoptosis via the mitochondrial pathway in vitro. What is more, we found the drug could cumulated much more in the nano-drug group than free drug group through imaging in vivo. In conclusion, the Luteolin/MPEG-PCL micelles have the potential clinical application in glioma chemotherapy.
基金：
National Natural Science Foundation of ChinaNational Natural Science Foundation of China [NSFC81502165]; Sichuan University Outstanding Young Scholars Research Fund [2016SCU04A04]; Science and Technology Department of Sichuan Province Major Research and Development Projects [2017SZ0006]
语种：
外文
WOS：
PubmedID：
中科院(CAS)分区：
出版当年[2017]版：
大类|2 区医学
小类|2 区肿瘤学3 区细胞生物学
最新[2023]版：
无
第一作者：
第一作者机构：[1]Department of Neurosurgery and Institute of Neurosurgery, State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu, 610041, PR China
共同第一作者：
通讯作者：
通讯机构：[1]Department of Neurosurgery and Institute of Neurosurgery, State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu, 610041, PR China
推荐引用方式(GB/T 7714)：
Songping Zheng,Yongzhong Cheng,Yan Teng,et al.Application of luteolin nanomicelles anti-glioma effect with improvement in vitro and in vivo.[J].Oncotarget.2017,8(37):61146-61162.doi:10.18632/oncotarget.18019.
APA：
Songping Zheng,Yongzhong Cheng,Yan Teng,Xiaoxiao Liu,Ting Yu...&Yuquan Wei.(2017).Application of luteolin nanomicelles anti-glioma effect with improvement in vitro and in vivo..Oncotarget,8,(37)
MLA：
Songping Zheng,et al."Application of luteolin nanomicelles anti-glioma effect with improvement in vitro and in vivo.".Oncotarget 8..37(2017):61146-61162
