文献类型：期刊文献

英文题名：Fli-1 Activation through Targeted Promoter Activity Regulation Using a Novel 3', 5'-diprenylated Chalcone Inhibits Growth and Metastasis of Prostate Cancer Cells

作者：Ma, Youfen Xu, Bixue Yu, Jia Huang, Lirong Zeng, Xiaoping Shen, Xiangchun Ren, Chunyan Ben-David, Yaacov Luo, Heng

第一作者：Ma, Youfen

通信作者：Ben-David, Y[1];Luo, H[1];Ben-David, Y[2];Luo, H[2];Ben-David, Y[3];Luo, H[3];Luo, H[4]

机构：[1]Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China;[2]Key Lab Chem Nat Prod Guizhou Prov, Guiyang 550014, Peoples R China;[3]Chinese Acad Sci, Guiyang 550014, Peoples R China;[4]Harvard Med Sch, Boston Childrens Hosp, Boston, MA 02115 USA;[5]Guizhou Inst Technol, Coll Food & Pharmaceut Engn, Guiyang 550003, Peoples R China;[6]Guizhou Med Univ, Coll Pharm, Guiyang 550029, Peoples R China

第一机构：Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China

通信机构：corresponding author), Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China;corresponding author), Key Lab Chem Nat Prod Guizhou Prov, Guiyang 550014, Peoples R China;corresponding author), Chinese Acad Sci, Guiyang 550014, Peoples R China;corresponding author), Harvard Med Sch, Boston Childrens Hosp, Boston, MA 02115 USA.

年份：2020

卷号：21

期号：6

外文期刊名：INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

收录：;Scopus(收录号：2-s2.0-85082380710);WOS:【SCI-EXPANDED(收录号:WOS:000529890200312)】；

基金：The work was supported by the National Science Foundation of China (NSFC, Project No. 81702914), the main projects of the Natural Science Foundation of Guizhou province (No. QKHLHZ[2016]7092, QKHJC[2017]1412 and QKHJC[2016]1099), China scholarship fund [2018]3058, the Science and Technology Department of Guizhou Province (QKHPTRC[2016]5678) and Guizhou Provincial Engineering Research Center for Natural Drugs.

语种：英文

外文关键词：prostate cancer; Fli-1 agonist; chalcone; invasion; migration; apoptosis

摘要：The friend leukemia integration 1 (Fli-1) gene is involved in the expression control of key genes in multiple pathogenic/physiological processes, including cell growth, differentiation, and apoptosis; this implies that Fli-1 is a strong candidate for drug development. In our previous study, a 3 ',5 '-diprenylated chalcone, (E)-1-(2-hydroxy-4-methoxy-3,5-diprenyl) phenyl-3-(3-pyridinyl)-propene-1-one (C10), was identified as a novel anti-prostate cancer (PCa) agent. Here, we investigated the molecular mechanisms underlying the anti-cancer effects of C10 on the growth, metastasis, and invasion of PC3 cells in vitro. Our results show that C10 exhibited a strong inhibitory effect on proliferation and metastasis of PC3 cells via several cellular and flow cytometric analyses. Further mechanism studies revealed that C10 likely serves as an Fli-1 agonist for regulating the expression of Fli-1 target genes including phosphatidylinositol 3-kinase (P110), murine double minute2 (MDM2), B-cell lymphoma-2 (Bcl-2), Src homology-2 domain-containing inositol 5-phosphatase 1 (SHIP-1), and globin transcription factor-1 (Gata-1) as well as the phosphorylation of extracellular-regulated protein kinases 1 (ERK1). Further, we confirmed that C10 can regulate the expressions of vascular endothelial growth factor 1 (VEGF-1), transforming growth factor-beta 2 (TGF-beta 2), intercellular cell adhesion molecule-1 (ICAM-1), p53, and matrix metalloproteinase 1 (MMP-1) genes associated with tumor apoptosis, migration, and invasion. Thus, C10 exhibits stronger anticancer activity with novel molecular targets and regulatory molecular mechanisms, indicating its great potency for development as a novel targeted anticancer drug.