In vitro anti-proliferative and anti-bacterial properties of new C7 benzoate derivatives of pinocembrin

被引:8
作者
Cappello, Anna R. [1 ]
Aiello, Francesca [1 ]
Polera, Nicoletta [1 ]
Armentano, Biagio [1 ]
Casaburi, Ivan [1 ]
Di Gioia, Maria Luisa [1 ]
Loizzo, Monica R. [1 ]
Dolce, Vincenza [1 ]
Pezzi, Vincenzo [1 ]
Tundis, Rosa [1 ]
机构
[1] Univ Calabria, Dept Pharm Hlth & Nutr Sci, Arcavacata Di Rende, Italy
关键词
Glycyrrhiza glabra L. leaves; pinocembrin; anti-proliferative activity; anti-bacterial activity; cell cycle arrest; CANCER STEM-CELLS; ANTIOXIDANT PROPERTIES; APOPTOSIS;
D O I
10.1080/14786419.2019.1641805
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
In the present work, the in vitro anti-proliferative and anti-bacterial activities of three semi-synthetic benzoate pinocembrin derivatives, isolated from the aerial parts of Glycyrrhiza glabra L., were investigated. As occurs in most natural compounds, the bioavailability of pinocembrin is very poor, therefore it should be improved by chemical strategies aimed to prolong its shelf life and, consequently, its activity. On this basis, three benzoate derivatives of pinocembrin (a1-a3) were synthesised and assayed in order to ascertain their biological value. Among them, compound a1 showed the highest anti-proliferative activity on a wide panel of cancer cell lines, as well as low toxic effects on non-malignant breast cells. The calculated IC50 values in HeLa and SKBR3 cells were 8.5 and 12.7 mu M, respectively. Briefly, a1 treatment increased ROS levels, induced mitochondrial membrane damage leading to necrotic death of HeLa cells. Moreover, a1 displayed a promising anti-bacterial activity. [GRAPHICS] .
引用
收藏
页码:1783 / 1791
页数:9
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