Department of Gastrointestinal and Anal Surgery, The First Hospital of Jilin University, Changchun, China.
Department of Digestive Endoscopy, The Second Hospital of Jilin Unersity, Changchun, China.
J Cell Biochem. 2019 Jan;120(1):1011-1017. doi: 10.1002/jcb.27542. Epub 2018 Sep 22.
Curcumin and its chalcone derivatives have well-known, explicit biological antitumor properties, such as instance antiproliferative and apoptotic effects via multiple molecular targets. In this study, we investigated the anticancer activity of curcumin derivative L6H4 (curcumin L6H4) on gastric cancer cells. Inhibitory effects of curcumin L6H4 on gastric cancer cells (BGC-823) were studied by the diphenyltetrazolium (MTT) assay, and cell apoptosis was detected by Annexin-V/propidium iodide (PI) staining and then analyzed by flow cytometry. A mouse xenotransplant gastric tumor model was established to detect the role of curcumin L6H4 in vivo. The apoptosis-related proteins p53, p21, Bax, and Bcl-2 in BGC-823 cells and mouse xenotransplant models treated with curcumin L6H4 were determined by Western blot analysis. Curcumin L6H4 can significantly inhibit the proliferation and induce the apoptosis of BGC-823 cells, thus enhancing the expression levels of p53, p21, Bax, and Bcl-2 noticeably in vivo and in vitro. Meanwhile, curcumin L6H4 can remarkably suppress the growth of tumor cells in animal models. These results suggest that curcumin derivative L6H4 has potent of antitumor properties in vitro or in vivo.
姜黄素及其查尔酮衍生物具有众所周知的明确的抗肿瘤生物特性，例如通过多个分子靶点发挥抗增殖和促凋亡作用。在本研究中，我们研究了姜黄素衍生物 L6H4（姜黄素 L6H4）对胃癌细胞的抗癌活性。通过二苯基四氮唑（MTT）测定法研究姜黄素 L6H4 对胃癌细胞（BGC-823）的抑制作用，并用 Annexin-V/碘化丙啶（PI）染色检测细胞凋亡，然后通过流式细胞术进行分析。建立了小鼠异种移植胃癌肿瘤模型，以检测姜黄素 L6H4 在体内的作用。通过 Western blot 分析确定姜黄素 L6H4 处理的 BGC-823 细胞和小鼠异种移植模型中的凋亡相关蛋白 p53、p21、Bax 和 Bcl-2。姜黄素 L6H4 可显著抑制 BGC-823 细胞的增殖并诱导其凋亡，从而显著提高体内和体外 p53、p21、Bax 和 Bcl-2 的表达水平。同时，姜黄素 L6H4 可显著抑制动物模型中肿瘤细胞的生长。这些结果表明，姜黄素衍生物 L6H4 具有体外或体内的抗肿瘤特性。
