替莫唑胺
胶质瘤
榄香烯
药理学
血脑屏障
药代动力学
体内
医学
脑瘤
分布(数学)
内科学
癌症研究
化学
生物
病理
细胞凋亡
中枢神经系统
生物化学
生物技术
数学分析
数学
作者
Xiaomin Zhang,Yidan Chen,Yao Ju,Yingxin Zhang,Mengying Li,Bo Yu,Kaifeng Wang
标识
DOI:10.1016/j.bbrep.2021.101144
摘要
Temozolomide (TMZ) is a widely used chemotherapeutic agent for malignant glioma. β-Elemene has been reported to have the ability of passing through the blood-brain barrier and reverse multidrug resistance. In the present study, transport of drugs through the in vitro blood-brain barrier (BBB) model also suggested that β-elemene can assist in TMZ transport to the brain. Plasma and brain pharmacokinetics demonstrated that when β-elemene is used in combination with TMZ, the metabolic rate of TMZ in plasma is slowed, and mean residence time (MRT) in brain is prolonged. The brain tissue distribution at 1 h indicated that the combination of TMZ and β-elemene promotes the distribution of β-elemene in the brain but slightly reduces the distribution of TMZ in the brain. Furthermore the antitumor effect and toxicity in vivo were also investigated. The combination of β-elemene and TMZ was well tolerated and significantly inhibited tumor growth in glioma xenografts. In summary, the present study indicates a synergistic antitumor effect of β-elemene and TMZ in glioma.
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