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Nrf2 activators from Glycyrrhiza inflata and their hepatoprotective activities against CCl4-induced liver injury in mice
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2017-08-15 , DOI: 10.1016/j.bmc.2017.08.018
Yan Lin , Yi Kuang , Kai Li , Shuang Wang , Shuai Ji , Kuan Chen , Wei Song , Xue Qiao , Min Ye

Glycyrrhiza inflata (licorice) has been used to treat liver diseases for a long history. However, the bioactive compounds are still not clear. In this work, 77 compounds, including 9 new ones, were isolated from the EtOAc extract of the roots and rhizomes of G. inflata. The Nrf2 activation activities of all compounds were screened using ARE-luciferase reporter assay on HepG2C8 cells. The results indicated a number of chalcones were potent Nrf2 activators, including 11 (licochalcone A, 4.07-fold), 12 (licochalcone B, 5.17-fold), and 19 (echinatin, 4.09-fold). Further studies indicated that 11, 12 and 19 remarkably attenuated CCl4-induced acute liver injury in mice (10 or 50 mg/kg, 7 days, ig.). These compounds could be promising hepatoprotective natural agents.



中文翻译:

甘草的Nrf2激活剂及其对小鼠CCl 4肝损伤的肝保护活性

甘草(甘草)用于治疗肝脏疾病已有很长的历史。然而,生物活性化合物仍不清楚。在这项工作中,从膨胀大豆根和根茎的EtOAc提取物中分离出77种化合物,包括9种新化合物。使用ARE-萤光素酶报告基因分析法在HepG2C8细胞上筛选了所有化合物的Nrf2活化活性。结果表明,许多查耳酮是有效的Nrf2激活剂,包括11种(利古耳康A,4.07倍),12种(利古耳康B,5.17倍)和19种(紫锥花,4.09倍)。进一步的研究表明,111219显着地衰减的CCl 4引起的小鼠急性肝损伤(10或50 mg / kg,7天,如图)。这些化合物可能是有希望的保肝天然药物。

更新日期:2017-08-15
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