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从. 中提取芦丁和圣草次苷的纯化工艺及体外和体内生物活性评价

Purification Process and In Vitro and In Vivo Bioactivity Evaluation of Pectolinarin and Linarin from .

机构信息

Institute of Chinese Medicine Sciences, Guangdong Pharmaceutical University, Guangzhou 510006, China.

Key Laboratory of Glucolipid Metabolic Disorder, Ministry of Education of China, Guangzhou 510006, China.

出版信息

Molecules. 2022 Dec 8;27(24):8695. doi: 10.3390/molecules27248695.

Abstract

Pectolinarin and linarin are two major flavone O-glycosides of which has been used for thousands of years in traditional Chinese medicine. Pharmacological research on pectolinarin and linarin is meaningful and necessary. Here, a process for the purification of pectolinarin and linarin from was established using macroporous resin enrichment followed by prep-HPLC separation. The results show the purity of pectolinarin and linarin reached 97.39% and 96.65%, respectively. The in vitro bioactivities result shows the ORAC values of pectolinarin and linarin are 4543 and 1441 µmol TE/g, respectively, meanwhile their inhibition rate of BSA-MGO-derived AGEs is 63.58% and 19.31% at 2 mg/mL, which is 56.03% and 30.73% in the BSA-fructose system, respectively. The COX-2 inhibition rate at 50 µg/mL of linarin and pectolinarin reached 55.35% and 40.40%, respectively. Furthermore, the in vivo bioassay combining of histopathologic evaluation and biochemical analysis of liver glutamic oxaloacetic transaminase, serum creatinine and TNF-α show pectolinarin can alleviate lipopolysaccharide (LPS)-induced acute liver and kidney injury in mice. Metabolomics analysis shows that pectolinarin attenuates LPS-challenged liver and kidney stress through regulating the arachidonic acid metabolism and glutathione synthesis pathways. Collectively, our work presents a solid process for pectolinarin and linarin purification and has discovered a promising natural therapeutic agent-pectolinarin.

摘要

柚皮苷和圣草酚是两种主要的黄酮 O-糖苷,已在传统中药中使用了数千年。对柚皮苷和圣草酚的药理学研究具有重要意义和必要性。在这里,建立了一种使用大孔树脂富集再结合制备 HPLC 分离从黄芩中纯化柚皮苷和圣草酚的方法。结果表明,柚皮苷和圣草酚的纯度分别达到 97.39%和 96.65%。体外生物活性结果表明,柚皮苷和圣草酚的 ORAC 值分别为 4543 和 1441 µmol TE/g,在 2 mg/mL 时,它们对 BSA-MGO 衍生 AGEs 的抑制率分别为 63.58%和 19.31%,在 BSA-果糖体系中,分别为 56.03%和 30.73%。在 50 µg/mL 时,圣草酚和柚皮苷对 COX-2 的抑制率分别达到 55.35%和 40.40%。此外,结合肝谷氨酸草酰乙酸转氨酶、血清肌酐和 TNF-α 的组织病理学评价和生化分析的体内生物测定表明,柚皮苷可以减轻脂多糖 (LPS) 诱导的小鼠急性肝和肾损伤。代谢组学分析表明,柚皮苷通过调节花生四烯酸代谢和谷胱甘肽合成途径减轻 LPS 挑战引起的肝和肾应激。总之,我们的工作提供了一种柚皮苷和圣草酚纯化的可靠方法,并发现了一种有前途的天然治疗剂-柚皮苷。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/86fc/9780979/4fd0392f752f/molecules-27-08695-g001.jpg

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