Lappaconitine hydrochloride (LH), as a new synthetic alkaloid, exhibits antitumor activity, whereas its antitumor effect on colorectal cancer (CRC) has not been investigated. In this study, the effect of LH on HCT-116 cell proliferation and apoptosis in vivo and in vitro and underlying molecular mechanism were explored. The Cell Counting Kit-8 (CCK-8) was used to assess cell viability. Morphological change was observed by Hoechst 33342 staining. Cell cycle and apoptosis were performed using a flow cytometer. The western blot method was used to screen for related protein expression. The mitochondrial membrane potential (MMP) was confirmed using the 5, 5, 6, 6′-tetrachloro-1, 1′, 3, 3′-tetraethylbenzimi-dazolyl carbo cyanine iodide (JC-1) staining assay. Reactive oxygen species (ROS) was evaluated by a 20−70-dichlorofluorescein diacetate (DCFH-DA) staining assay. The antitumor effect was evaluated in vivo by the xenograft HCT-116 model. The results showed that LH significantly inhibited cell viability in a time- and concentration-dependent manner. LH induced apoptosis and S phase cell cycle arrest. LH promoted the reduction of MMP and ROS accumulation. Moreover, LH activated the mitochondrial and MAPK pathway. The experiments in vivo showed that LH had significant antitumor effect in tumor-bearing mice, and had virtually no effect on the weight and internal organs of the mice. In conclusion, LH could induce apoptosis in HCT-116 cells through mitochondrial and MAPK signaling pathways. LH may be a promising treatment for CRC.

拉帕乌碱盐酸盐（LH）作为一种新型合成生物碱，具有抗肿瘤活性，而其对结直肠癌（CRC）的抗肿瘤作用尚未研究。本研究探讨了LH在体内外对HCT-116细胞增殖和凋亡的影响及其潜在的分子机制。Cell Counting Kit-8 (CCK-8) 用于评估细胞活力。通过Hoechst 33342染色观察形态变化。使用流式细胞仪进行细胞周期和细胞凋亡。采用蛋白质印迹法筛选相关蛋白表达。使用 5, 5, 6, 6'-四氯-1, 1', 3, 3'-四乙基苯并二唑基碘化羰花青 (JC-1) 染色测定证实线粒体膜电位 (MMP)。通过 20-70-二氯荧光素二乙酸酯 (DCFH-DA) 染色测定评估活性氧 (ROS)。通过异种移植HCT-116模型在体内评估抗肿瘤作用。结果表明，LH以时间和浓度依赖性方式显着抑制细胞活力。LH诱导细胞凋亡和S期细胞周期停滞。LH 促进 MMP 和 ROS 积累的减少。此外，LH 激活了线粒体和 MAPK 通路。体内实验表明，LH对荷瘤小鼠具有显着的抗肿瘤作用，对小鼠的体重和内脏器官几乎没有影响。总之，LH 可通过线粒体和 MAPK 信号通路诱导 HCT-116 细胞凋亡。LH 可能是一种有希望的 CRC 治疗方法。通过异种移植HCT-116模型在体内评估抗肿瘤作用。结果表明，LH以时间和浓度依赖性方式显着抑制细胞活力。LH诱导细胞凋亡和S期细胞周期停滞。LH 促进 MMP 和 ROS 积累的减少。此外，LH 激活了线粒体和 MAPK 通路。体内实验表明，LH对荷瘤小鼠具有显着的抗肿瘤作用，对小鼠的体重和内脏器官几乎没有影响。总之，LH 可通过线粒体和 MAPK 信号通路诱导 HCT-116 细胞凋亡。LH 可能是一种有希望的 CRC 治疗方法。通过异种移植HCT-116模型在体内评估抗肿瘤作用。结果表明，LH以时间和浓度依赖性方式显着抑制细胞活力。LH诱导细胞凋亡和S期细胞周期停滞。LH 促进 MMP 和 ROS 积累的减少。此外，LH 激活了线粒体和 MAPK 通路。体内实验表明，LH对荷瘤小鼠具有显着的抗肿瘤作用，对小鼠的体重和内脏器官几乎没有影响。总之，LH 可通过线粒体和 MAPK 信号通路诱导 HCT-116 细胞凋亡。LH 可能是一种有希望的 CRC 治疗方法。LH 促进 MMP 和 ROS 积累的减少。此外，LH 激活了线粒体和 MAPK 通路。体内实验表明，LH对荷瘤小鼠具有显着的抗肿瘤作用，对小鼠的体重和内脏器官几乎没有影响。总之，LH 可通过线粒体和 MAPK 信号通路诱导 HCT-116 细胞凋亡。LH 可能是一种有希望的 CRC 治疗方法。LH 促进 MMP 和 ROS 积累的减少。此外，LH 激活了线粒体和 MAPK 通路。体内实验表明，LH对荷瘤小鼠具有显着的抗肿瘤作用，对小鼠的体重和内脏器官几乎没有影响。总之，LH 可通过线粒体和 MAPK 信号通路诱导 HCT-116 细胞凋亡。LH 可能是一种有希望的 CRC 治疗方法。