Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, 300072, P. R. China.
Faculty of Science and Marine Environment, University Malaysia Terengganu, Kuala Nerus, 21030, Malaysia.
J Food Sci. 2021 Feb;86(2):366-375. doi: 10.1111/1750-3841.15599. Epub 2021 Jan 14.
Liver damage is a common liver disorder, which could induce liver cancer. Oral antioxidant is one of the effective treatments to prevent and alleviate liver damage. In this study, three flavonoids namely myricetin, isoquercitrin, and isorhamnetin were isolated and identified from Laba garlic. The isolated compounds were investigated on the protective effects against H O -induced oxidative damages in hepatic L02 cells and apoptosis inducing mechanism in hepatic cancer cells HepG2 by using MTT assay, flow cytometry and western blotting analysis. Myricetin, isoquercitrin, and isorhamnetin showed proliferation inhibition on HepG2 cells with IC value of 44.32 ± 0.213 µM, 49.68 ± 0.192 µM, and 54.32 ± 0.176 µM, respectively. While they showed low toxicity on normal cell lines L02. They could significantly alleviate the oxidative damage towards L02 cells (P < 0.05), via inhibiting the morphological changes in mitochondria and upholding the integrity of mitochondrial structure and function. The fluorescence intensity of L02 cells pre-treated with myricetin, isoquercitrin, and isorhamnetin (100 µM) was 89.23 ± 1.26%, 89.35 ± 1.43% and 88.97 ± 0.79%, respectively. Moreover, the flavonoids could induce apoptosis in HepG2 cells via Bcl-2/Caspase pathways, where it could up-regulate the expression of Bax and down-regulate the expression of Bcl-2, Bcl-xL, pro-Caspase-3, and pro-Caspase-9 proteins in a dose dependent manner. Overall, the results suggested that the flavonoids from Laba garlic might be a promising candidate for the treatment of various liver disorders. PRACTICAL APPLICATION: Flavonoids from Laba garlic showed selective toxicity towards HepG2 cells in comparison to L02 cells via regulating Bcl-2/caspase pathway. Additionally, the isolated flavonoids expressively barred the oxidative damage induced by H O in L02 cells. These results suggested that the flavonoids from laba garlic could be a promising agent towards the development of functional foods.
肝脏损伤是一种常见的肝脏疾病，可导致肝癌。口服抗氧化剂是预防和减轻肝脏损伤的有效治疗方法之一。本研究从腊八蒜中分离并鉴定了三种类黄酮，分别为杨梅素、异槲皮苷和异鼠李素。采用 MTT 法、流式细胞术和 Western blot 分析，研究了这些化合物对 H2O2 诱导的肝 L02 细胞氧化损伤和肝癌细胞 HepG2 细胞凋亡诱导机制的保护作用。杨梅素、异槲皮苷和异鼠李素对 HepG2 细胞的增殖抑制作用的 IC50 值分别为 44.32 ± 0.213 μM、49.68 ± 0.192 μM 和 54.32 ± 0.176 μM。而它们对正常细胞系 L02 的毒性较低。它们能显著减轻 L02 细胞的氧化损伤（P<0.05），通过抑制线粒体形态变化，维持线粒体结构和功能的完整性。经杨梅素、异槲皮苷和异鼠李素（100 μM）预处理的 L02 细胞荧光强度分别为 89.23 ± 1.26%、89.35 ± 1.43%和 88.97 ± 0.79%。此外，这些类黄酮可以通过 Bcl-2/Caspase 途径诱导 HepG2 细胞凋亡，从而上调 Bax 的表达，下调 Bcl-2、Bcl-xL、pro-Caspase-3 和 pro-Caspase-9 蛋白的表达，呈剂量依赖性。总之，结果表明，腊八蒜中的类黄酮可能是治疗各种肝脏疾病的有前途的候选药物。
与 L02 细胞相比，腊八蒜中的类黄酮通过调节 Bcl-2/caspase 通路对 HepG2 细胞具有选择性毒性。此外，分离出的类黄酮显著阻止了 H2O2 诱导的 L02 细胞氧化损伤。这些结果表明，腊八蒜中的类黄酮可能是开发功能性食品的有前途的候选药物。
