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Cytotoxic and Antimigratory Activity of Retrochalcones from Glycyrrhiza echinata L. on Human Cancer Cells
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2022-11-30 , DOI: 10.1002/cbdv.202200589 Dicle Çevik 1 , Suat Erdogan 2 , Riza Serttas 2 , Yüksel Kan 3 , Hasan Kırmızıbekmez 4
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2022-11-30 , DOI: 10.1002/cbdv.202200589 Dicle Çevik 1 , Suat Erdogan 2 , Riza Serttas 2 , Yüksel Kan 3 , Hasan Kırmızıbekmez 4
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Cytotoxic activity-guided fractionation studies on Glycyrrhiza echinata roots led to the isolation of eight compounds (1–8). Chemical structures of the isolates were identified by NMR and MS analysis. Among the tested molecules, retrochalcones namely echinatin (3) (IC50=23.45–41.83 μM), licochalcone B (4) (IC50=36.04–39.53 μM) and tetrahydroxylmethoxychalcone (5) (IC50=7.09–80.81 μM) were the most active ones against PC3, MCF7 and HepG2 cells. Moreover, 5 exhibited selectivity on prostate cancer cells (SI: 5.19). Hoechst staining and Annexin V/PI binding assays as well as cell cycle analysis on the compounds 3 (23 μM) and 5 (5 and 7 μM) demonstrated that these retrochalcones induced apoptosis and significantly suppressed cell cycle in G1 and G2/M phases. Furthermore, 3 and 5 showed antimigratory effects on PC3 cells by wound healing assay. The results indicated that tested retrochalcones most particularly 5 could be potential anticancer drug candidates that prevent proliferation and migration of cancer cells.
中文翻译：
紫果甘草后查尔酮对人类癌细胞的细胞毒性和抗迁移活性
对紫果甘草根进行的细胞毒性活性引导的分级分离研究导致八种化合物的分离 ( 1 – 8 )。分离物的化学结构通过 NMR 和 MS 分析确定。在测试的分子中，retrochalones 即 echinatin ( 3 ) (IC 50 =23.45–41.83 μM)、licochalcone B ( 4 ) (IC 50 =36.04–39.53 μM) 和四羟基甲氧基查尔酮 ( 5 ) (IC 50 =7.09–80.81 μM)对 PC3、MCF7 和 HepG2 细胞的活性最强。此外，5对前列腺癌细胞表现出选择性 (SI: 5.19)。Hoechst 染色和膜联蛋白 V/PI 结合测定以及化合物3 (23 μM) 和5 (5 和 7 μM) 的细胞周期分析表明，这些逆查尔酮诱导细胞凋亡并显着抑制 G 1和 G 2 /M细胞周期阶段。此外，通过伤口愈合试验， 3和5显示出对 PC3 细胞的抗迁移作用。结果表明，测试的逆查尔酮，尤其是5可能是潜在的抗癌候选药物，可防止癌细胞增殖和迁移。
更新日期：2022-11-30
中文翻译：
紫果甘草后查尔酮对人类癌细胞的细胞毒性和抗迁移活性
对紫果甘草根进行的细胞毒性活性引导的分级分离研究导致八种化合物的分离 ( 1 – 8 )。分离物的化学结构通过 NMR 和 MS 分析确定。在测试的分子中，retrochalones 即 echinatin ( 3 ) (IC 50 =23.45–41.83 μM)、licochalcone B ( 4 ) (IC 50 =36.04–39.53 μM) 和四羟基甲氧基查尔酮 ( 5 ) (IC 50 =7.09–80.81 μM)对 PC3、MCF7 和 HepG2 细胞的活性最强。此外，5对前列腺癌细胞表现出选择性 (SI: 5.19)。Hoechst 染色和膜联蛋白 V/PI 结合测定以及化合物3 (23 μM) 和5 (5 和 7 μM) 的细胞周期分析表明，这些逆查尔酮诱导细胞凋亡并显着抑制 G 1和 G 2 /M细胞周期阶段。此外，通过伤口愈合试验， 3和5显示出对 PC3 细胞的抗迁移作用。结果表明，测试的逆查尔酮，尤其是5可能是潜在的抗癌候选药物，可防止癌细胞增殖和迁移。
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