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从龙胆花中分离得到的黄酮类成分芹菜素通过 LDLR-LCAT 信号通路抑制氧化应激。

Apigenin, flavonoid component isolated from Gentiana veitchiorum flower suppresses the oxidative stress through LDLR-LCAT signaling pathway.

机构信息

College of Agricultural Science and Technology, Tibet Vocational Technical College, Lhasa 850030, China.

College of Agricultural Science and Technology, Tibet Vocational Technical College, Lhasa 850030, China.

出版信息

Biomed Pharmacother. 2020 Aug;128:110298. doi: 10.1016/j.biopha.2020.110298. Epub 2020 Jun 3.

DOI:10.1016/j.biopha.2020.110298
PMID:32504920
Abstract

Flower of Gentiana veitchiorum has traditionally been used as an herbal medicine in Tibet for treatment of variola, respiratory infection, and pneumonia. However, the effective components contained in flower are not identified yet, and the underlying mechanisms for anti-inflammatory, antibacterial, and antioxidative activities remain to be elucidated. Here, we first extracted the flavonoid mixture from G. veitchiorum flower. The mixture was then further isolated and the within compounds was identified through the high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS). The results showed that apigenin (4',5,7-trihydroxyflavone) was the most abundant flavonoid in G. veitchiorum flower. We next examined the antioxidative activity of the extracted apigenin using the ferric reducing/antioxidant power (FRAP), the 1,1-diphenyl-2-picrylhydrazyl (DPPH), and the 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS) assays and found that a positive correlation between apigenin concentration and reactive oxygen species (ROS) scavenging rate. The biochemical assays further revealed that the levels of total cholesterol (TC), triglyceride (TG), and malondialdehyde (MDA) were reduced, while the activity of superoxide dismutase (SOD) was increased after apigenin treatment in hyperlipidemic rats. Moreover, we performed histopathological investigations and found that the lipidic deposition patterns were recovered and the amount of lipid vacuoles was significantly reduced in apigenin-treated hyperlipidemic rat liver. Western blotting assay showed that the expression of low-density lipoprotein receptor (LDLR) and lecithin-cholesterol acyltransferase (LCAT) were up-regulated in the apigenin-treated samples. Overall, our results demonstrated that the apigenin isolated from G. veitchiorum flower exhibited radical scavenging activities, and reversed the high fat diet-induced oxidative damage in rats. Its antioxidative activities are probably achieved via LDLR-LCAT signaling pathway.

摘要

獐牙菜属植物的花在西藏传统上被用作草药,用于治疗天花、呼吸道感染和肺炎。然而,花中含有的有效成分尚未确定,其抗炎、抗菌和抗氧化活性的潜在机制仍有待阐明。在这里,我们首先从獐牙菜属植物的花中提取了黄酮混合物。然后,通过高效液相色谱串联质谱(HPLC-MS/MS)进一步分离混合物中的化合物,并对其进行鉴定。结果表明,芹菜素(4',5,7-三羟基黄酮)是獐牙菜属植物花中最丰富的黄酮类化合物。接下来,我们使用铁还原/抗氧化能力(FRAP)、1,1-二苯基-2-苦基肼(DPPH)和 2,2'-联氮-双-(3-乙基苯并噻唑啉-6-磺酸)(ABTS)测定法来检测提取的芹菜素的抗氧化活性,发现芹菜素浓度与活性氧(ROS)清除率之间存在正相关关系。生化测定进一步表明,在高脂血症大鼠中,芹菜素处理后总胆固醇(TC)、甘油三酯(TG)和丙二醛(MDA)水平降低,超氧化物歧化酶(SOD)活性增加。此外,我们进行了组织病理学研究,发现脂质沉积模式得到恢复,脂滴数量在芹菜素处理的高脂血症大鼠肝脏中明显减少。Western blot 检测表明,低密度脂蛋白受体(LDLR)和卵磷脂胆固醇酰基转移酶(LCAT)的表达在芹菜素处理的样本中上调。总的来说,我们的研究结果表明,从獐牙菜属植物中分离得到的芹菜素具有清除自由基的活性,并逆转了高脂饮食诱导的大鼠氧化损伤。其抗氧化活性可能是通过 LDLR-LCAT 信号通路实现的。

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