III-10, a newly synthesized flavonoid, induced differentiation of human U937 leukemia cells via PKC未 activation

详细信息	查看全文 | 推荐本文 |

• 作者：Yansu Qin¹ ; ^{qys0518@163.com} ; Zhiyu Li¹ ; ^{zhiyuli@263.net} ; Yan Chen ^{s0710189@sina.com} ; Hui Hui ^{moyehh@163.com} ; Yajing Sun ^{yj7782@126.com} ; Hao Yang ^{yanghao1988717@hotmail.com} ; Na Lu ; ^{luna555@163.com} ; Qinglong Guo ; ^{anticancer_drug@yahoo.com.cn}
• 关键词：PKC未 ; protein kinase C未 ; PLSCR1 ; phospholipids scramblase 1 ; PML ; promyelocytic leukemia protein ; PML-NB ; promyelocytic leukemia-nuclear body ; ERK1/2 ; extracellular signal-regulated kinase 1/2 ; ATRA ; all-trans retinoic acid ; VD3 ; 1 ; 25(OH)2D3 ; PMA ; phorb
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2012
• 期刊代码：15_09280987
• 类别：pha
• 出版时间：11 April, 2012
• 卷：45
• 期：5
• 页码：648-656
• 文件大小：702 K

摘要

Flavonoid is an important group of natural products which exerted anticancer effects against various cancers. III-10 is a newly synthesized flavonoid with a pyrrolidinyl and a benzyl group substitution. It shares a same carbon skeleton with flavonoid which indicates that it may also have potential anticancer activity. To investigate whether III-10 could express anticancer effect on human U937 leukemia cells through differentiation induction, a series of experiments were processed. MTT and trypan-blue excluding assays showed that III-10 possessed growth and viability inhibition effects on U937 cells. Giemsa staining was implemented to observe the morphologic changes of U937 cells after III-10 treatment. Nitroblue tetrazolium (NBT) reduction assay and cell surface antigen flow cytometry were carried out to figure out the way III-10 induced U937 cells to differentiate. These experiments revealed that III-10 could induce U937 cells to differentiate into monocyte-like cells. Western blots and immunofluorescence were performed to inspect the possible underlying mechanism. The results revealed that differentiation-related proteins phospholipids scramblase 1 (PLSCR1) and promyelocytic leukemia protein (PML) were up-regulated after III-10 treatment. And III-10 stimulated PLSCR1 and PML probably through activation of protein kinase C未 (PKC未). All these results suggested that III-10 was a prospective anticancer compound and was requisite to be proceeded further investigation.