Cappello Anna R, Aiello Francesca, Polerà Nicoletta, Armentano Biagio, Casaburi Ivan, Di Gioia Maria Luisa, Loizzo Monica R, Dolce Vincenza, Pezzi Vincenzo, Tundis Rosa
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Rende, Italy.
Nat Prod Res. 2021 Jun;35(11):1783-1791. doi: 10.1080/14786419.2019.1641805. Epub 2019 Jul 16.
In the present work, the anti-proliferative and anti-bacterial activities of three semi-synthetic benzoate pinocembrin derivatives, isolated from the aerial parts of 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 () were synthesised and assayed in order to ascertain their biological value. Among them, compound 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 IC values in HeLa and SKBR3 cells were 8.5 and 12.7 µM, respectively. Briefly, treatment increased ROS levels, induced mitochondrial membrane damage leading to necrotic death of HeLa cells. Moreover, displayed a promising anti-bacterial activity.
在本研究中，对从L.地上部分分离得到的三种半合成苯甲酸片松素衍生物的抗增殖和抗菌活性进行了研究。与大多数天然化合物一样，片松素的生物利用度非常低，因此应通过旨在延长其保质期并进而提高其活性的化学策略来改善。在此基础上，合成并测定了三种片松素苯甲酸酯衍生物（），以确定它们的生物学价值。其中，化合物对多种癌细胞系表现出最高的抗增殖活性，对非恶性乳腺细胞的毒性作用较低。在HeLa和SKBR3细胞中计算得到的IC值分别为8.5和12.7 μM。简而言之，处理增加了活性氧水平，诱导线粒体膜损伤，导致HeLa细胞坏死死亡。此外，还表现出有前景的抗菌活性。
