机构：[1]Brain Function and Disease Laboratory, Shantou University Medical College, Shantou 515041, China[2]Guangdong Institute of Microbiology, Guangzhou 510070, China[3]Yueyang Hospital of Traditional Chinese Medicine, Yueyang 414000, China
Astroglioma is the most common primary tumor in the central nervous system without effective treatment strategies. Temozolomide (TMZ) is a chemotherapeutic drug to treat astroglioma but exhibits low potency and has side effects. Therefore, there is an urgent need to develop new compounds to treat astroglioma. Dalbergia sissoo Roxb was the source of Dalbergia odorifera in traditional Chinese medicine (TCM) and has been clinically used as an anti-tumor medicine. 4-Methoxydalbergione (4MOD) is purified from Dalbergia sissoo Roxb., and shows an inhibitory effect on osteosarcoma, but its effects on astroglioma have not been reported. Here, we evaluate its anti-astroglioma effects on both in vitro and in vivo models. In cultured astroglioma U87 cells, 4MOD inhibited cell proliferation and induced cell apoptosis in a time- and concentration-dependent manner. Compared with TMZ, 4MOD exhibited a tenfold greater potency of anti-astroglioma effects. 4MOD effectively stalled the cell cycle in G2 phase. Transcriptome sequencing (RNA-seq) showed that 4MOD upregulated 158 genes and downregulated 204 genes that are mainly enriched in cell membrane, cell division, cell cycle, p53, TNF, and MAPK signaling pathways, which may underlie its anti-tumor mechanisms. In a nude mouse xenograft model transplanted with U87 cells, 10 mg/kg 4MOD slowed down tumor growth rate, while at 30 mg/kg dose, it reduced tumor size. Collectively, this study demonstrates that 4MOD is a potent native compound that remarkably inhibits U87 astroglioma growth in both in vitro and in vivo models.
基金：
This work was supported by the Research Foundation of Hunan Administration of
Traditional Chinese Medicine (No. 2019101); Natural Science Foundation of Hunan
province (No. 2019JJ50631); Research Foundation of Guangdong Administration of
Traditional Chinese Medicine (No. 20202090).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2020]版：
大类|1 区医学
小类|1 区药学2 区化学综合
最新[2025]版：
大类|2 区医学
小类|1 区药学2 区化学：综合
第一作者：
第一作者机构：[1]Brain Function and Disease Laboratory, Shantou University Medical College, Shantou 515041, China
通讯作者：
推荐引用方式(GB/T 7714)：
Li Ran,Xu Chang-Qiong,Shen Jian-Xin,et al.4-Methoxydalbergione is a potent inhibitor of human astroglioma U87 cells in vitro and in vivo.[J].Acta Pharmacologica Sinica.2021,42(9):1507-1515.doi:10.1038/s41401-020-00560-w.
APA：
Li Ran,Xu Chang-Qiong,Shen Jian-Xin,Ren Qiu-Yun,Chen Di-Ling...&Wu Jie.(2021).4-Methoxydalbergione is a potent inhibitor of human astroglioma U87 cells in vitro and in vivo..Acta Pharmacologica Sinica,42,(9)
MLA：
Li Ran,et al."4-Methoxydalbergione is a potent inhibitor of human astroglioma U87 cells in vitro and in vivo.".Acta Pharmacologica Sinica 42..9(2021):1507-1515
医学