Institute of Resource Biology and Biotechnology, Department of Biotechnology, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China.
Food Funct. 2019 Apr 17;10(4):2209-2220. doi: 10.1039/c8fo02506a.
Ginkgo biloba has long been used in ancient China for the treatment of cough, asthma, and other lung diseases. However, the active constituents in G. biloba for pulmonary disease treatment remain unclear. The objective of this study was to evaluate the anti-inflammatory active constituents in G. biloba and clarify their associated molecular mechanisms. The biological effects of different G. biloba extracts were evaluated in an ovalbumin-induced allergic mouse model. Anti-inflammatory compounds were present in the ethyl acetate phase of the extract, which were analysed by HPLC-MS. Biflavones were identified as the main compounds, which were further evaluated by docking calculations. Leukocyte elastase showed a high fit score with ginkgetin, one of the identified biflavones. The lowest binding free energy was -6.69 kcal mol-1. The effects of biflavones were investigated in vivo and in vitro. Ginkgetin markedly suppressed the abnormal expression of the Akt and p38 pathways in human neutrophil elastase (HNE)-stimulated A549 cells. Biflavones also decreased MUC5AC mRNA expression in HNE-stimulated A549 cells and the allergic mouse model. Inflammatory cells (neutrophils) and cytokines (IL-8) also decreased in mice treated with biflavones. The results suggest that G. biloba biflavones could inhibit the activity of leukocyte elastase. This in turn implicates G. biloba as a functional food for the treatment of airway inflammation.
银杏在古代中国一直被用于治疗咳嗽、哮喘和其他肺部疾病。然而，用于肺部疾病治疗的银杏的活性成分仍不清楚。本研究的目的是评估银杏中的抗炎活性成分，并阐明其相关的分子机制。在卵清蛋白诱导的过敏性小鼠模型中评估了不同银杏提取物的生物效应。提取物的乙酸乙酯相具有抗炎作用，通过 HPLC-MS 进行分析。鉴定出双黄酮类化合物是主要化合物，并通过对接计算进一步进行评估。白细胞弹性蛋白酶与银杏素（鉴定出的一种双黄酮）具有很高的拟合分数。双黄酮的作用在体内和体外进行了研究。银杏素显著抑制了人中性粒细胞弹性蛋白酶（HNE）刺激的 A549 细胞中 Akt 和 p38 通路的异常表达。双黄酮还降低了 HNE 刺激的 A549 细胞和过敏性小鼠模型中 MUC5AC mRNA 的表达。用双黄酮治疗的小鼠中炎症细胞（中性粒细胞）和细胞因子（IL-8）也减少了。结果表明，银杏双黄酮可以抑制白细胞弹性蛋白酶的活性。这反过来表明银杏作为一种功能性食品可用于治疗气道炎症。
