Esophageal cancer is one of the malignant cancers with a low 5-year survival rate. Licochalcone (LC) H, a chemically synthesized substance, is a regioisomer of LCC extracted from licorice. The purpose of this study was to determine whether LCH might have anticancer effect on human esophageal squamous cell carcinoma (ESCC) cell lines via apoptosis signaling pathway. After 48 h of treatment, IC₅₀ of LCH in KYSE 30, KYSE 70, KYSE 410, KYSE 450, and KYSE 510 cells were 15, 14, 18, 15, and 16 μM, respectively. This study demonstrated that LCH potently suppressed proliferation of ESCC cells in a concentration- and time-dependent manner. LCH triggered G2/M-phase arrest by modulating expression levels of cdc2, cyclin B1, p21, and p27. LCH also induced apoptosis of ESCC cells through reactive oxygen species-mediated endoplasmic reticulum (ER) stress via JNK/p38 activation pathways. The anticancer effect of LCH was associated with ER stress and mitochondrial dysfunction. It also affected protein levels of Mcl-1, tBid, Bax, Bcl-2, cytochrome c, Apaf-1, PARP, cleaved-PARP, and ER stress-related proteins (GRP78 and CHOP). Our findings provide the first demonstration that LCH has anticancer effect on ESCC. Thus, LCH might have potential for preventing and/or treating human ESCC.

中文翻译：

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通过修饰从甘草中提取的Licochalcone C结构合成的Licochalcone H诱导食管鳞状细胞癌细胞凋亡。

食道癌是5年生存率低的恶性癌之一。化学合成物质Licochalcone（LC）H是从甘草中提取的LCC的区域异构体。这项研究的目的是确定LCH是否可能通过凋亡信号通路对人食道鳞状细胞癌（ESCC）细胞系产生抗癌作用。治疗48小时后，IC ₅₀KYSE 30，KYSE 70，KYSE 410，KYSE 450和KYSE 510细胞中LCH的分别为15、14、18、15和16μM。这项研究表明，LCH以浓度和时间依赖性方式有效抑制ESCC细胞的增殖。LCH通过调节cdc2，cyclin B1，p21和p27的表达水平来触发G2 / M期阻滞。LCH还通过JNK / p38激活途径通过活性氧介导的内质网（ER）应激诱导ESCC细胞凋亡。LCH的抗癌作用与内质网应激和线粒体功能障碍有关。它还影响了Mcl-1，tBid，Bax，Bcl-2，细胞色素c，Apaf-1，PARP，裂解的PARP和ER应激相关蛋白（GRP78和CHOP）的蛋白水平。我们的发现首次证明LCH对ESCC具有抗癌作用。从而，