Design, synthesis, and preliminary biological evaluation of chrysin amino acid derivatives that induce apoptosis and suppress cell migration

被引：10

作者：

Liu, Yun-Mei ^{[1
,2
]}

Li, Yang ^{[2
]}

Xiao, Jie ^{[2
]}

Zhang, Qi-Zhi ^{[2
]}

Song, Jian-Xin ^{[1
]}

机构：

[1] Hunan Normal Univ, Key Lab Assembly & Applicat Organ Funct Mol Hunan, Minist Educ China, Key Lab Chem Biol & Tradit Chinese Med, Changsha 410081, Hunan, Peoples R China

[2] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China

来源：

JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH | 2020年 / 22卷 / 06期

基金：

湖南省自然科学基金;

关键词：

Chrysin derivatives; amino acid; anticancer; apoptotic; FLAVONOIDS;

D O I：

10.1080/10286020.2019.1597056

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

Amino acid derivatives containing chrysin were synthesized for evaluating their anticancer effects. Among them, compound N-(7-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)heptanoyl)-L-isoleucine (6e) displayed the most potent antiproliferative activity against MGC-803 cells with IC50 value of 20.0M. Preliminary mechanistic studies showed that compound 6e could inhibit the colony formation and migration of MGC-803 cells. Flow cytometry analysis demonstrated that compound 6e mediated cell apoptosis of MGC-803 cells and arrested cell cycle in G2/M-phase. Moreover, 6e treatment in MGC-803 cells downregulated anti-apoptotic protein Bcl-2 and upregulated pro-apoptotic gene Bax in a concentration-dependent manner. Our studies suggest that compound 6e may sever as an effective chemotherapeutic candidate. [GRAPHICS] .

引用

页码：547 / 561

页数：15

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