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Phytochemical Quantification and the In Vitro Acetylcholinesterase Inhibitory Activity of Phellodendron chinense and Its Components

by 1,2,†, 1,†, 1, 1,3, 1 and 1,3,*
Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, Korea
College of Pharmacy, Chungnam National University, Daejeon 34134, Korea
Korean Medicine of Life Science, University of Science & Technology, Daejeon 34113, Korea
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2017, 22(6), 925;
Received: 10 April 2017 / Revised: 23 May 2017 / Accepted: 30 May 2017 / Published: 2 June 2017
(This article belongs to the Section Medicinal Chemistry)
The dried bark of Phellodendron chinense has been used as a traditional herbal medicine to remove damp heat, relieve consumptive fever, and cure dysentery and diarrhea. In the present study, we performed quantitative analyses of the two components of P. chinense, phellodendrine and berberine, using high-performance liquid chromatography. A 70% ethanol extract of P. chinense was prepared and the two components were separated on a C-18 analytical column using a gradient solvent system of acetonitrile and 0.1% (v/v) aqueous trifluoroacetic acid. The ultraviolet wavelength used for detection was 200 nm for phellodendrine and 226 nm for berberine. The analytical method established here showed high linearity (correlation coefficient, ≥0.9991). The amount of phellodendrine and berberine used was 22.255 ± 0.123 mg/g and 269.651 ± 1.257 mg/g, respectively. Moreover, we performed an in vitro acetylcholinesterase (AChE) activity assay and an amyloid-β aggregation test to examine the biological properties of phellodendrine and berberine as therapeutic drugs for Alzheimer’s disease. Phellodendrine and berberine inhibited AChE activity in a dose-dependent manner (IC50 = 36.51 and 0.44 μM, respectively). In contrast, neither phellodendrine nor berberine had an effect on amyloid-β aggregation. The P. chinense extract and phellodendrine, but not berberine, exhibited antioxidant activity by increasing radical scavenging activity. Moreover, P. chinense demonstrated a neuroprotective effect in hydrogen peroxide-treated HT22 hippocampal cells. Overall, our findings suggest that P. chinense has potential as an anti-Alzheimer’s agent via the suppression of the enzymatic activity of acetylcholinesterase and the stimulation of antioxidant activity. View Full-Text
Keywords: Phellodendron chinense; phellodendrine; quantitative analysis; neuroprotection Phellodendron chinense; phellodendrine; quantitative analysis; neuroprotection
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Kim, Y.J.; Lim, H.-S.; Kim, Y.; Lee, J.; Kim, B.-Y.; Jeong, S.-J. Phytochemical Quantification and the In Vitro Acetylcholinesterase Inhibitory Activity of Phellodendron chinense and Its Components. Molecules 2017, 22, 925.

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