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Cholinesterase inhibitors from the roots of Harpagophytum procumbens

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Abstract

Inhibition of cholinesterase has been proposed to be a therapeutic target for the treatment of Alzheimer’s diseases. In our preliminary screening study on the acetylcholinesterase (AChE) inhibitory activity, an ethyl acetate soluble fraction of the roots of Harpagophytum procumbens (Pedaliaceae) was found to inhibit AChE activity at the concentration of 100 μg/mL. Ten compounds (1–10) were isolated from the active fraction and evaluated for their inhibitory effect on AChE and butyrylcholinesterase (BChE). Among the isolates, verbascosides (5, 6, and 8) containing a caffeoyl and a 3,4-dihydroxyphenethyl groups in their structures, showed effective AChE inhibitory activity and also possessed BChE inhibitory activity. The findings suggest that verbascoside derivatives may be partially related to the anti-Alzheimer effect of this medicinal plant.

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Acknowledgments

This research was supported by the National Research Foundation of Korea Grant funded by the Korean Government (MEST) (KRF-2012R1A1A2003547) and BK 21 Plus (KRF-22A20130000073). We are grateful to the Korean Basic Science Institute (KBSI) for supplying the NMR spectra.

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Authors and Affiliations

  1. College of Pharmacy, Catholic University of Daegu, Gyeongsan, Gyeongbuk, 712-702, Korea

    Yoon Ho Bae, To Dao Cuong, Tran Manh Hung, Mi Hee Woo & Byung Sun Min

  2. Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Caugiay, Hanoi, Vietnam

    To Dao Cuong

  3. College of Pharmacy, Kyungpook National University, Taegu, 702-701, Korea

    Jeong Ah Kim

  4. Faculty of Food Science and Biotechnology, Pukyung National University, Pusan, 608-737, Korea

    Jeong Su Byeon & Jae Sue Choi

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  1. Yoon Ho Bae
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  2. To Dao Cuong
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  3. Tran Manh Hung
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Correspondence to Byung Sun Min.

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Yoon Ho Bae and To Dao Cuong have contributed equally to this work.

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Bae, Y.H., Cuong, T.D., Hung, T.M. et al. Cholinesterase inhibitors from the roots of Harpagophytum procumbens . Arch. Pharm. Res. 37, 1124–1129 (2014). https://doi.org/10.1007/s12272-013-0316-y

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  • DOI: https://doi.org/10.1007/s12272-013-0316-y

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