Abstract

Agricultural waste from the hulls of water caltrop (Trapa taiwanesis Nakai, TT-hull) was extracted by either steeping them in cold 95% ethanol (C95E), refluxing 95E, refluxing 50E, or refluxing hot water (HW) to obtain C95EE, 95EE, 50EE, and HWE, respectively. These four extracts showed acetylcholinesterase (AChE) inhibitory activities and free radical scavenging activities, as well as anti-non-enzymatic protein glycation in vitro. Eight compounds were isolated from TT-hull-50EE and were used to plot the chromatographic fingerprints of the TT-hull extracts, among which tellimagrandin-I, tellimagrandin-II, and 1,2,3,6-tetra-galloylglucose showed the strongest AChE inhibitory activities, and they also exhibited anti-amyloid β peptide aggregations. The scopolamine-induced amnesiac ICR mice that were fed with TT-hull-50EE or TT-hull-HWE (100 and 200 mg/kg) or tellimagrandin-II (100 and 200 mg/kg) showed improved learning behavior when evaluated using passive avoidance or water maze evaluation, and they showed significant differences (p < 0.05) compared to those in the control group. The enriched hydrolysable tannins of the recycled TT-hull may be developed as functional foods for the treatment of degenerative disorders.

Highlights

  • The global prevalence of dementia is increasing continuously [1], and it has been ranked the 14th (2000), 8th (2010), and 5th (2016) highest cause of death worldwide [2].Among different types of dementia, Alzheimer’s disease (AD) was ranked first for around60–70% of all cases, and the AD populations accounted for 75% and 80%, respectively, of all dementia cases in elderly patients between 80 and years old and older than years [3]

  • The approved therapeutic drugs for clinical AD treatments are only acetylcholinesterase (AChE) inhibitors, which are developed based on the “cholinergic hypothesis”, which suggests that acetylcholine plays a vital role in learning and memory; dysfunctions in the brain neurons associated with acetylcholine may contribute to cognitive decline

  • This study is the first in which the oral administration of TT-hull extracts and the isolated compound of TT-1 showed a significant improvement in the learning and memory functions in amnesiac mice models (Figures 4 and 5), compared to those of the control group

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Summary

Introduction

The global prevalence of dementia is increasing continuously [1], and it has been ranked the 14th (2000), 8th (2010), and 5th (2016) highest cause of death worldwide [2]. The approved therapeutic drugs for clinical AD treatments are only acetylcholinesterase (AChE) inhibitors, which are developed based on the “cholinergic hypothesis”, which suggests that acetylcholine plays a vital role in learning and memory; dysfunctions in the brain neurons associated with acetylcholine may contribute to cognitive decline. The amnesia model induced by scopolamine is generally used to investigate AChE inhibitors and their effects on AD management [9,14,15]. Epidemiological studies showed the relationship between diets rich in fruits and vegetables and decreased risk of cardiovascular diseases [20], several results implied that dietary polyphenol with antioxidant activity in vitro was not correlated with a direct beneficial effect in vivo; further animal experiments and/or clinical trials will be needed to evaluate this in more detail [16,17,18]. The enriched hydrolysable tannins of the recycled TT-hulls were investigated, as well as their potential use as functional foods for degenerative disorders, through in vitro and in vivo animal experiments

Chemical and Reagents
Crude Extract Preparation
Isolation of Purified cCmpounds
AChE Inhibitory Activities In Vitro
2.10. AChE Activities and Reduced GSH Levels in Brain Tissue Extracts
2.11. Statistical Analyses
Results
HPLC Chromatograms of TT-Hull Extracts
Effects of the Oral Administration
Discussion
Full Text
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