Key Laboratory of Xin'an Medicine, Ministry of Education, Anhui University of Chinese Medicine, Hefei, 230038, Anhui, China.
School of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230038, Anhui, China.
Appl Microbiol Biotechnol. 2021 Mar;105(5):2033-2042. doi: 10.1007/s00253-020-11045-5. Epub 2021 Feb 13.
Liver cancer, one of the most common types of cancer in the world, is the second leading cause of death for cancer patients. For liver cancer, there is an urgent need for an effective treatment with no or less toxic side effects. Lactonic sophorolipids (LSL), as a potential anticancer drug, has attracted wide attention of pharmaceutical researchers with its good biological activities. The effects of LSL and cell death inhibitors were measured by MTT test on HepG2 cells. Meanwhile, the morphology of the cells was observed under a microscope. The apoptosis rate was detected by flow cytometry, and the expression levels of enzyme activity of Caspase-3 and Caspase-9 were measured by detection kits. Meanwhile, mRNA levels of Apaf-1, Caspase-3, Bax, and Bcl-2 were measured by quantitative real-time RT-PCR; protein levels of Caspase-3, Cleaved Caspase-3, Bax, and Bcl-2 were measured by western blot. LSL can inhibit the proliferation of cells, and it is possible to induce apoptosis in cells. The HepG2 cells with LSL co-culture exhibited typical apoptotic morphology, and the expression levels of enzyme activity of Caspase-3 and Caspase-9 increased (P< 0.05). We also found that LSL increases cell apoptosis rate and regulates the expression of genes and proteins associated with apoptosis through the Caspase-3 pathway. These results indicate that LSL may be one of the potential drug candidates to inhibit the proliferation and induce apoptosis in HepG2 cells.Key points• LSL, which is of good biological activities such as anti-bacterium, virus elimination, and inflammatory response elimination, has been firstly used to intervene in vitro to investigate its effect on HepG2 cell proliferation.• LSL can inhibit the proliferation of cells, and it is possible to induce apoptosis in HepG2 cells through the Caspase-3 pathway.• The mechanism of LSL action on HepG2 cell proliferation was firstly also discussed, which provides a certain experimental reference for the clinical treatment of liver cancer.
肝癌是世界上最常见的癌症类型之一，也是癌症患者死亡的第二大主要原因。对于肝癌，迫切需要一种有效且毒性副作用小或无的治疗方法。乳酰基槐糖脂（LSL）作为一种有潜力的抗癌药物，因其良好的生物活性而引起了药物研究人员的广泛关注。通过 MTT 试验在 HepG2 细胞上测量 LSL 和细胞死亡抑制剂的作用。同时，在显微镜下观察细胞形态。通过流式细胞术检测细胞凋亡率，并通过检测试剂盒测量 Caspase-3 和 Caspase-9 酶活性的表达水平。同时，通过定量实时 RT-PCR 测量 Apaf-1、Caspase-3、Bax 和 Bcl-2 的 mRNA 水平；通过 Western blot 测量 Caspase-3、Cleaved Caspase-3、Bax 和 Bcl-2 的蛋白水平。LSL 可抑制细胞增殖，并可能诱导细胞凋亡。与 LSL 共培养的 HepG2 细胞呈现出典型的凋亡形态，并且 Caspase-3 和 Caspase-9 的酶活性表达水平增加（P<0.05）。我们还发现，LSL 通过 Caspase-3 通路增加细胞凋亡率并调节与凋亡相关的基因和蛋白的表达。这些结果表明，LSL 可能是抑制 HepG2 细胞增殖并诱导其凋亡的潜在药物候选物之一。
关键点
• 首先使用具有抗菌、抗病毒和消除炎症反应等良好生物活性的乳酰基槐糖脂（LSL）在体外干预，研究其对 HepG2 细胞增殖的影响。
• LSL 可抑制细胞增殖，并可能通过 Caspase-3 通路诱导 HepG2 细胞凋亡。
• 还首次讨论了 LSL 对 HepG2 细胞增殖作用的机制，为肝癌的临床治疗提供了一定的实验参考。
