期刊
NUTRIENTS
卷 14, 期 17, 页码 -出版社
MDPI
DOI: 10.3390/nu14173633
关键词
chicory; sesquiterpene lactones; acetylcholinesterase; isothermal titration calorimetry; molecular docking simulation; Alzheimer's disease
资金
- Own scholarship fund of the Lodz University of Technology by the Ministry of Science and High Education in Poland
- Plan Propio de Investigacion de la UCAM
- European Regional Development Fund (ERDF)
- Fundacion Seneca del Centro de Coordinacion de la Investigacion de la Region de Murcia [20988/PI/18]
The study found that sesquiterpene lactones in chicory extracts have a strong inhibitory effect on acetylcholinesterase, especially lactucopicrin. Different chicory extracts exhibit complementary patterns in binding the AChE active site.
The aim of the study was to explain the effects of sesquiterpene lactones (SLs) from chicory (Cichorium intybus L.) root extracts as inhibitors of acetylcholinesterase (AChE) at the molecular level and to determine the inhibition of AChE activity by specific SLs (lactucin and lactucopicrin) and different chicory extracts. The obtained SLs-rich extracts were purified by the countercurrent partition chromatography (CPC) technique. AChE inhibitors were analyzed using two models: isothermal titration calorimetry (ITC) and docking simulation. The results of ITC analysis of the enzyme and the ligands' complexation showed strong interactions of SLs as well as extracts from chicory with AChE. In a test of enzyme activity inhibition after introducing acetylcholine into the model system with SL, a stronger ability to inhibit the hydrolysis of the neurotransmitter was observed for lactucopicrin, which is one of the dominant SLs in chicory. The inhibition of enzyme activity was more efficient in the case of extracts, containing different enzyme ligands, exhibiting complementary patterns of binding the AChE active site. The study showed the high potential of using chicory to decrease the symptoms of Alzheimer's disease.
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