College of Korean Medicine, Kyung Hee University, Seoul 02447, Republic of Korea.
Institute of Sports Science, Kyung Hee University, Yongin 17104, Republic of Korea.
Int J Mol Sci. 2024 Aug 30;25(17):9418. doi: 10.3390/ijms25179418.
Though Ginsenoside F2 (GF2), a protopanaxadiol saponin from Panax ginseng, is known to have an anticancer effect, its underlying mechanism still remains unclear. In our model, the anti-glycolytic mechanism of GF2 was investigated in human cervical cancer cells in association with miR193a-5p and the β-catenin/c-Myc/Hexokinase 2 (HK2) signaling axis. Here, GF2 exerted significant cytotoxicity and antiproliferation activity, increased sub-G1, and attenuated the expression of pro-Poly (ADPribose) polymerase (pro-PARP) and pro-cysteine aspartyl-specific protease (procaspase3) in HeLa and SiHa cells. Consistently, GF2 attenuated the expression of Wnt, β-catenin, and c-Myc and their downstream target genes such as HK2, pyruvate kinase isozymes M2 (PKM2), and lactate dehydrogenase A (LDHA), along with a decreased production of glucose and lactate in HeLa and SiHa cells. Moreover, GF2 suppressed β-catenin and c-Myc stability in the presence and absence of cycloheximide in HeLa cells, respectively. Additionally, the depletion of β-catenin reduced the expression of c-Myc and HK2 in HeLa cells, while pyruvate treatment reversed the ability of GF2 to inhibit β-catenin, c-Myc, and PKM2 in GF2-treated HeLa cells. Notably, GF2 upregulated the expression of microRNA139a-5p (miR139a-5p) in HeLa cells. Consistently, the miR139a-5p mimic enhanced the suppression of β-catenin, c-Myc, and HK2, while the miR193a-5p inhibitor reversed the ability of GF2 to attenuate the expression of β-catenin, c-Myc, and HK2 in HeLa cells. Overall, these findings suggest that GF2 induces apoptosis via the activation of miR193a-5p and the inhibition of β-catenin/c-Myc/HK signaling in cervical cancer cells.
虽然人参皂苷 F2(GF2)是一种源自人参的原二醇皂苷,已知具有抗癌作用,但它的作用机制仍不清楚。在我们的模型中,研究了 GF2 在人宫颈癌细胞中通过 miR193a-5p 和 β-连环蛋白/ c-Myc/己糖激酶 2(HK2)信号轴的抗糖酵解机制。在这里,GF2 对 HeLa 和 SiHa 细胞表现出显著的细胞毒性和抗增殖活性,增加了 sub-G1,并减弱了 pro-Poly(ADPribose)聚合酶(pro-PARP)和 pro-半胱氨酸天冬氨酸特异性蛋白酶(procaspase3)的表达。一致地,GF2 减弱了 Wnt、β-连环蛋白和 c-Myc 及其下游靶基因如 HK2、丙酮酸激酶同工酶 M2(PKM2)和乳酸脱氢酶 A(LDHA)的表达,同时减少了葡萄糖和乳酸的产生在 HeLa 和 SiHa 细胞中。此外,GF2 分别在 HeLa 细胞中存在和不存在环己酰亚胺的情况下抑制了 β-连环蛋白和 c-Myc 的稳定性。此外,β-连环蛋白的耗竭降低了 HeLa 细胞中 c-Myc 和 HK2 的表达,而丙酮酸处理逆转了 GF2 在 GF2 处理的 HeLa 细胞中抑制 β-连环蛋白、c-Myc 和 PKM2 的能力。值得注意的是,GF2 上调了 HeLa 细胞中 microRNA139a-5p(miR139a-5p)的表达。一致地,miR139a-5p 模拟物增强了对 β-连环蛋白、c-Myc 和 HK2 的抑制作用,而 miR193a-5p 抑制剂逆转了 GF2 减弱 HeLa 细胞中 β-连环蛋白、c-Myc 和 HK2 表达的能力。总之,这些发现表明 GF2 通过激活 miR193a-5p 和抑制宫颈癌细胞中的 β-连环蛋白/c-Myc/HK 信号诱导细胞凋亡。