Lab of Hepatopharmacology and Ethnopharmacology, School of Pharmaceutical Sciences, South-central Minzu University, No. 182, Minyuan Road, Wuhan, 430074, China.
Medical College of China Three Gorges University, Yichang, 443002, China.
J Ethnopharmacol. 2022 Sep 15;295:115407. doi: 10.1016/j.jep.2022.115407. Epub 2022 May 28.
Our previous studies found that the ethanol extract of Gynura procumbens (EEGS) reduced hepatic steatosis in alcoholic fatty liver disease (AFLD).
To explore the active ingredients from EEGS and their relevant mechanism of action in alleviating alcoholic liver injuries.
To explore the active ingredients from EEGS and their intestinal absorption characteristics as an approach for understanding mechanism of action in alleviating alcoholic liver injuries.
Monitored by high-performance liquid chromatography (HPLC) and thin-layer chromatography (TLC), chemical constituents from the prepared EEGS were isolated by means of solvent extraction, repeated column chromatography, preparative HPLC and other methods, and their structures were identified based on spectroscopic methods. The in vivo intestinal absorption rate of chlorogenic acid (CA), the active component of the EEGS, both in a single form and in the EEGS were monitored by the single-pass intestinal perfusion (SPIP) method in rats. The protective effect of EEGS and its active components on alcoholic liver injuries was evaluated in the alcoholic liver injury model of C57BL/6J male mice induced by Lieber-DeCarli alcohol liquid feed.
Three noncaffeoyl quinic acid components were isolated and identified from the EEGS, namely, 3-trans-p-coumaroyl quinic acid (0.9%), 3-cis-p-coumaroyl quinic acid (2.7%), and trans-p-coumaric acid (0.6%). In vivo intestinal absorption of CA decreased with the increase of pH value of perfusion solution in the range of 5.5-7.8. The maximum absorption percentage of CA alone was 6.7 ± 2.4%, while the maximum absorption percentage of CA in the EEGS was 16.0 ± 2.2%, which was 2.4 times higher than that of CA alone. The results of animal experiments showed that the degree of fatty liver of mice treated with EEGS was significantly lower than that of the CA, trans-p-coumaric acid, and the combination group of CA and trans-p-coumaric acid alone.
The above results indicated that trans-p-coumaric acid isolated from the dried stems of Gynura procumbens assisted CA being absorbed into the body and worked together with CA to improve the function of liver lipid metabolism, reduce hepatic lipid accumulation in a mouse model of AFLD and effectively counteract alcohol-induced fatty liver disease.
我们之前的研究发现,菊三七的乙醇提取物(EEGS)可减轻酒精性脂肪肝疾病(AFLD)中的肝脂肪变性。
探索 EEGS 的活性成分及其在缓解酒精性肝损伤中的作用机制。
探索 EEGS 的活性成分及其肠道吸收特征,作为了解其缓解酒精性肝损伤作用机制的一种方法。
通过高效液相色谱(HPLC)和薄层色谱(TLC)监测,用溶剂提取、反复柱层析、制备高效液相色谱等方法从制备好的 EEGS 中分离出化学成分,并根据光谱方法鉴定其结构。采用大鼠单向肠灌流(SPIP)法监测绿原酸(CA)作为 EEGS 的活性成分,无论是单独形式还是在 EEGS 中,其在体内的肠内吸收率。采用 C57BL/6J 雄性小鼠酒精性肝损伤模型评价 EEGS 及其活性成分对酒精性肝损伤的保护作用,该模型由 Lieber-DeCarli 酒精液体饲料诱导。
从 EEGS 中分离并鉴定出三种非咖啡酰奎宁酸成分,分别为 3-反式对香豆酰奎宁酸(0.9%)、3-顺式对香豆酰奎宁酸(2.7%)和反式对香豆酸(0.6%)。CA 的体内肠内吸收率随灌注液 pH 值在 5.5-7.8 范围内的增加而降低。CA 单独的最大吸收百分比为 6.7±2.4%,而 EEGS 中 CA 的最大吸收百分比为 16.0±2.2%,是 CA 单独的 2.4 倍。动物实验结果表明,EEGS 处理的小鼠脂肪肝程度明显低于 CA、反式对香豆酸和 CA 与反式对香豆酸单独联合组。
上述结果表明,从菊三七干燥茎中分离出的反式对香豆酸辅助 CA 被吸收到体内,并与 CA 一起作用,改善肝脏脂质代谢功能,减少 AFLD 小鼠模型中的肝脂质堆积,有效对抗酒精性脂肪肝疾病。