Fujian Provincial Key Laboratory of Natural Medicine Pharmacology, School of Pharmacy, Fujian Medical University, Fuzhou, P. R. China.
Department of Pharmacy, Shengli Clinical Medical College of Fujian Medical University, Fujian Provincial Hospital, Fuzhou, P. R. China.
Pharm Biol. 2023 Dec;61(1):918-926. doi: 10.1080/13880209.2023.2220754.
Lucialdehyde B (LB), an effective triterpenoid isolated from (Leyss. ex Fr.) Karst. (Polyproraceae), exerts cytotoxic activity against nasopharyngeal carcinoma CNE2 cells.
To investigate the antiproliferative and pro-apoptotic effects of LB on CNE2 cells and explore its underlying mechanisms.
LB concentrations of 5-40 μg/mL were used. Cell proliferation was determined using MTT, CFSE, and colony formation assays. LB-induced apoptosis and cell cycle arrest were measured by flow cytometry after 48-h LB treatments. Fluorescence microscopy and flow cytometry were performed to measure the alteration of MMP, mPTP opening, ROS level, and Ca content in CNE2 cells. Western blotting was performed to evaluate the expression of mitochondrial apoptosis-related and Ras/ERK signaling proteins.
IC values of LB against CNE2 cells for 24, 48, and 72 h were 25.42 ± 0.87, 14.83 ± 0.93, and 11.60 ± 0.77 μg/mL, respectively. The CFSE assay showed that the cell proliferation index was 12.70 in the LB treatment group and 31.44 in the control group. LB significantly reduced clonogenic capacity, promoted cell apoptosis and induced cell cycle arrest at the G2/M phase. Our observations also revealed that LB induced ROS and calcium aggregation, opening of mPTP, MMP reduction, upregulation of mitochondrial apoptosis-related protein expression and inhibition of Ras/ERK signaling cascades.
LB suppresses proliferation and induces mitochondrial-dependent apoptosis in nasopharyngeal carcinoma CNE2 cells.
LB may have a potential use as a clinical drug candidate for nasopharyngeal carcinoma treatment.
卢西亚醛 B（LB）是从（Leyss. ex Fr.）Karst.（多蕊木科）中分离得到的一种有效的三萜类化合物，对鼻咽癌细胞 CNE2 具有细胞毒性作用。
研究 LB 对 CNE2 细胞的增殖抑制和促凋亡作用及其机制。
采用 5-40μg/ml 的 LB 浓度。MTT、CFSE 和集落形成实验测定细胞增殖。48 小时 LB 处理后，通过流式细胞术测定 LB 诱导的细胞凋亡和细胞周期阻滞。荧光显微镜和流式细胞术测定 LB 处理后 CNE2 细胞中线粒体膜电位（MMP）、mPTP 开放、ROS 水平和 Ca 含量的变化。Western blot 检测线粒体凋亡相关蛋白和 Ras/ERK 信号通路蛋白的表达。
LB 对 CNE2 细胞的 24、48 和 72 h 的 IC 值分别为 25.42±0.87、14.83±0.93 和 11.60±0.77μg/ml。CFSE 实验显示 LB 处理组细胞增殖指数为 12.70，对照组为 31.44。LB 显著降低克隆形成能力，促进细胞凋亡，诱导细胞周期阻滞于 G2/M 期。观察到 LB 诱导 ROS 和钙聚集、mPTP 开放、MMP 降低、线粒体凋亡相关蛋白表达上调和 Ras/ERK 信号通路抑制。
LB 抑制鼻咽癌细胞 CNE2 的增殖并诱导其线粒体依赖性凋亡。
LB 可能作为鼻咽癌治疗的临床候选药物。
