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Open AccessArticle

Synergistic Inhibition of Acetylcholinesterase by Alkaloids Derived from Stephaniae Tetrandrae Radix, Coptidis Rhizoma and Phellodendri Chinensis Cortex

Shenzhen Key Laboratory of Edible and Medicinal Bioresources, HKUST Shenzhen Research Institute, Hi-Tech Park, Shenzhen 518057, China
Institute of Pharmaceutical & Food Engineering, Shanxi University of Chinese Medicine, 121 Daxue Road, Yuci District, Jinzhong 030619, China
Division of Life Science and Center for Chinese Medicine, The Hong Kong University of Science and Technology, Clear Water Bay, Hong Kong, China
Authors to whom correspondence should be addressed.
Academic Editor: Solomon Habtemariam
Molecules 2019, 24(24), 4567;
Received: 29 October 2019 / Revised: 30 November 2019 / Accepted: 10 December 2019 / Published: 13 December 2019
(This article belongs to the Special Issue Natural Products in Alzheimer’s Disease Drug Discovery)
Alkaloids having acetylcholinesterase (AChE) inhibitory activity are commonly found in traditional Chinese medicine (TCM); for example, berberine from Coptis chinensis, galantamine from Lycoris radiata, and huperzine A from Huperzia serrata. In practice of TCM, Stephaniae Tetrandrae Radix (STR) is often combined with Coptidis Rhizoma (CR) or Phellodendri Chinensis Cortex (PCC) as paired herbs during clinical application. Fangchinoline from STR and coptisine and/or berberine from CR and/or PCC are active alkaloids in inhibiting AChE. The traditional usage of paired herbs suggests the synergistic effect of fangchinoline–coptisine or fangchinoline–berberine pairing in AChE inhibition. HPLC was applied to identify the main components in herbal extracts of STR, CR, and PCC, and the AChE inhibition of their main components was determined by Ellman assay. The synergism of herb combination and active component combination was calculated by median-effect principle. Molecular docking was applied to investigate the underlying binding mechanisms of the active components with the AChE protein. It was found that fangchinoline showed AChE inhibitory potency; furthermore, fangchinoline–coptisine/berberine pairs (at ratios of 1:5, 1:2, 1:1, and 2:1) synergistically inhibited AChE; the combination index (CI) at different ratios was less than one when Fa = 0.5, suggesting synergistic inhibition of AChE. Furthermore, the molecular docking simulation supported this enzymatic inhibition. Therefore, fangchinoline–coptisine/berberine pairs, or their parental herbal mixtures, may potentially be developed as a possible therapeutic strategy for Alzheimer’s patients. View Full-Text
Keywords: acetylcholinesterase; fangchinoline; coptisine; berberine; synergistic effect acetylcholinesterase; fangchinoline; coptisine; berberine; synergistic effect
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MDPI and ACS Style

Kong, X.-P.; Liu, E.Y.; Chen, Z.-C.; Xu, M.L.; Yu, A.X.; Wu, Q.-Y.; Xia, Y.-J.; Duan, R.; Dong, T.T.; Tsim, K.W. Synergistic Inhibition of Acetylcholinesterase by Alkaloids Derived from Stephaniae Tetrandrae Radix, Coptidis Rhizoma and Phellodendri Chinensis Cortex. Molecules 2019, 24, 4567.

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