光甘草定和槲皮素对乳腺癌细胞能量代谢的调控作用

Regulatory effects of glabridin and quercetin on energy metabolism of breast cancer cells

据报道,能量代谢是肿瘤细胞的核心特征。该研究旨在探讨2种中药黄酮成分光甘草定、槲皮素对乳腺癌细胞能量供应、糖酵解的调控作用,为开发具有调控肿瘤能量代谢功能的抗肿瘤中药提供借鉴。该研究以三阴性乳腺癌肿瘤细胞(MDA-MB-231)为研究对象,基于能量代谢各途径的特点,选取葡萄糖摄取、葡萄糖转运子1(GLUT1)的蛋白表达、细胞内三磷酸腺苷(ATP)水平、乳酸脱氢酶(LDH)活力和乳酸(LD)浓度等5个潜在靶点来考察光甘草定和槲皮素对乳腺癌肿瘤细胞能量代谢的调控作用,并初步探讨其相关机制。结果显示,槲皮素和光甘草定均可下调GLUT1的蛋白表达,减少乳腺癌细胞对葡萄糖的摄取。其中槲皮素对LDH活力和LD浓度无明显影响,未影响其糖酵解过程,但可增加乳腺癌细胞内ATP水平;而光甘草定可减弱乳腺癌细胞中LDH活力,降低其LD浓度,从而抑制乳腺癌细胞的糖酵解过程。因此,槲皮素和光甘草定对乳腺癌细胞的能量代谢具有调控作用,可以作为潜在的抗癌剂或抗癌辅助剂。

It is reported that energy metabolism is the core feature of tumor cells. This study is aimed to investigate the regulatory effect of two flavonoids( glabridin and quercetin) on energy supply and glycolysis of breast cancer cells,and provide reference for developing some anticancer herbal drugs with the function of regulating tumor energy metabolism. Based on the characteristics of each pathway during energy metabolism,in the present study,the triple negative breast cancer tumor cells( MDA-MB-231) were selected to investigate the effects of glabridin and quercetin on the energy metabolism of breast cancer cells and discuss the possible mechanisms from the following five potential targets: glucose uptake,protein expression of glucose transporter 1( GLUT1),adenosine triphosphate( ATP) level,lactate dehydrogenase( LDH) activity,and lactic acid( LD) concentration. The results showed that both quercetin and glabridin could decrease the glucose uptake capacity of breast cancer cells by down-regulating the protein expression of GLUT1. Quercetin had no significant effect on LDH activity and LD concentration;it did not affect the glycolysis process,but increased the intracellular ATP level. Glabridin decreased the activity of LDH and reduced LD concentration,thereby inhibiting the glycolysis metabolism of breast cancer cells. Therefore,both quercetin and glabridin can regulate the energy metabolism of breast cancer cells and can be used as potential anticancer agents or anti-cancer adjuvants.