Laboratory of Drug Metabolism and Drug Toxicity, Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav St., 1000 Sofia, Bulgaria.
Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Str., 1000 Sofia, Bulgaria.
Food Chem Toxicol. 2018 Jan;111:631-640. doi: 10.1016/j.fct.2017.12.020. Epub 2017 Dec 13.
The aim of the current study was to evaluate the effect of a defatted extract (EAS) and three flavonoids, isolated from Astragalus spruneri Boiss. (Fabaceae) using in vitro/in vivo models of liver injury. The EAS was characterized by HPLC and flavonoids (14 mg/g dw) and saponins (8 mg/g dw) were proved. The flavonoids (ASF1, ASF3 and ASF5) were isolated from the same extract and partially identified by LC-MS. In in vitro models of non-enzyme induced (Fe/AA) lipid peroxidation in isolated liver microsomes and CCl-induced metabolic bioactivation and t-BuOOH-induced oxidative stress in isolated rat hepatocytes, both EAS and the flavonoids exerted similar to silybin (positive control) an antioxidant and cytoprotective activity, discerned by decreased MDA production in the microsomes and by preserved cell viability and GSH levels as well as by decreased LDH activity and MDA quantity in isolated rat hepatocytes. The antioxidant and hepatoprotective effect of EAS has been confirmed in vivo against CCl-induced liver injury in rats. EAS restored the GSH levels and the activity of the antioxidant enzymes CAT and SOD, affected by CCl administration, as well as decreased the production of MDA. The effect of EAS was commensurable with those of silymarin.
本研究旨在评估从黄芪（豆科）中分离出的脱脂提取物（EAS）和三种类黄酮，通过体外/体内肝损伤模型的作用。EAS 通过 HPLC 进行了表征，证明含有 14mg/gdw 的类黄酮和 8mg/gdw 的皂苷。从同一提取物中分离出类黄酮（ASF1、ASF3 和 ASF5），并通过 LC-MS 进行了部分鉴定。在非酶诱导的（Fe/AA）肝微粒体中脂质过氧化、CCl 诱导的代谢生物活化和 t-BuOOH 诱导的大鼠肝细胞氧化应激的体外模型中，EAS 和类黄酮均表现出与水飞蓟宾（阳性对照）相似的抗氧化和细胞保护活性，通过降低微粒体中 MDA 的产生、保持细胞活力和 GSH 水平以及降低 LDH 活性和 MDA 量来识别。EAS 的抗氧化和肝保护作用在体内通过对抗 CCl 诱导的大鼠肝损伤得到了证实。EAS 恢复了 GSH 水平和抗氧化酶 CAT 和 SOD 的活性，这些活性受 CCl 给药的影响，同时降低了 MDA 的产生。EAS 的作用与水飞蓟宾的作用相当。
