In order to search for novel antitumor drugs with high efficiency and low toxicity, the anti-lung cancer activity of phytosphingosine was studied. Phytosphingosine is widely distributed in fungi, plants, animals, and has several biological activities, including anti-inflammation and anti-tumor. However, its anti-lung cancer activity needs to be further investigated. The effects and pharmacological mechanisms of phytosphingosine on lung cancer treatment were investigated both in vitro and in vivo. The results showed that phytosphingosine inhibited the growth of lung cancer cell lines. Phytosphingosine induced apoptosis through a mitochondria-mediated pathway, phytosphingosine arrested the cell cycle at the G2/M phase and induced apoptosis in a dose-dependent manner by increasing Bax/Bcl-2 ratio, which caused the decrease of mitochondrial membrane potential to promote the release of cytochrome C, caspase 9 and 3, and degrade PARP in A549 cells. The results showed that phytosphingosine could damage the mitochondrial functions, increase ROS levels, and arrest the cell cycle at the G2/M stages. Finally, phytosphingosine also inhibited the growth of tumor in mice. Taken together, phytosphingosine suppressed the growth of lung cancer cells both in vitro and in vivo and had potential application in the research and development of antitumor drugs. The aim of the present study was to explain the theoretical basis of phytosphingosine therapy for lung cancer and providing new possibilities for lung cancer treatment.

为了寻找高效低毒的新型抗肿瘤药物，对植物鞘氨醇的抗肺癌活性进行了研究。植物鞘氨醇广泛分布于真菌、植物、动物中，具有抗炎、抗肿瘤等多种生物活性。然而，其抗肺癌活性仍需进一步研究。在体外和体内研究了植物鞘氨醇治疗肺癌的作用和药理机制。结果表明，植物鞘氨醇抑制肺癌细胞系的生长。植物鞘氨醇通过线粒体介导的途径诱导细胞凋亡，植物鞘氨醇将细胞周期阻滞在G2/M期，并通过增加Bax/Bcl-2比值以剂量依赖性方式诱导细胞凋亡，引起线粒体膜电位下降，促进细胞凋亡。释放细胞色素 C、半胱天冬酶 9 和 3，并降解 A549 细胞中的 PARP。结果表明，植物鞘氨醇可以损害线粒体功能，增加ROS水平，并使细胞周期停滞在G2/M阶段。最后，植物鞘氨醇还抑制小鼠肿瘤的生长。综上所述，植物鞘氨醇在体外和体内均能抑制肺癌细胞的生长，在抗肿瘤药物的研发中具有潜在的应用前景。本研究旨在解释植物鞘氨醇治疗肺癌的理论基础，为肺癌治疗提供新的可能性。