Abstract

Cistanche tubulosa aqueous extract (CTE) is already used as a botanical prescription drug for treating dementia in China. Our previous studies reported that phenylethanoid glycosides of CTE have anti-Alzheimer’s disease (AD) activity by inhibiting amyloid β peptide (Aβ) aggregation and deposition. However, recent studies considered that the phenylethanoid glycosides may be metabolized by intestinal bacteria, because all analysis results showed that the bioavailability of phenylethanoid glycosides is extremely low. In this study we demonstrate how iron chelation plays a crucial role in the Aβ aggregation and deposition inhibition mechanism of phenylethanoid glycosides of CTE. In addition, we further proved phenylethanoid glycosides (1–3) could reach brain. Active CTE component and action mechanism confirmation will be a great help for product quality control and bioavailability studies in the future. At the same time, we provide a new analysis method useful in determining phenylethanoid glycosides (1–3) in plants, foods, blood, and tissues for chemical fingerprint and pharmacokinetic research.

Highlights

  • Dementia is one of the most common chronic aging diseases

  • 75% EtOH extract was subjected to resin and C18 column chromatography to furnish three major compounds, echinacoside (1), acteoside (2) and isoacteoside (3)

  • Their structures were elucidated by analysis of the NMR (Nuclear Magnetic Resonance) spectroscopy and electrospray ionization (ESI)-MS (Electrospray ionization mass) and by comparison with literature data [31,32,33]

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Summary

Introduction

Dementia is one of the most common chronic aging diseases. In 2015 the World Alzheimer Report estimated that about 46.8 million people suffered from dementia, and the number is expected to be74.7 million in 2030 and 131.5 million in 2050 [1]. Dementia is one of the most common chronic aging diseases. Global healthcare expenditures to treat dementia were almost 604 billion US dollars in 2010 and the amount is expected to be 1000 billion in 2030 [2]. Dementia patients have greater risk of accidental death [3] and require more medical care. This is a heavy burden for dementia patient familial caregivers. The impact of dementia on caregivers, family and society can produce great physical, psychological, life and economic stress. AD is the most common dementia and is an irreversible and progressive neurodegenerative disorder [4,5,6]. AD was the sixth leading cause of death in the United States in 2015 [6]

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