Medicinal Chemistry Research

, Volume 27, Issue 2, pp 538–545 | Cite as

In vitro anticholinesterase activity and molecular docking studies of coumarin derivatives isolated from roots of Heptaptera cilicica

  • Hilal Özbek
  • Zühal Güvenalp
  • Gülderen Yılmaz
  • Kadir Ö. Yerdelen
  • Cavit Kazaz
  • Ömür L. Demirezer
Original Research


The chloroform extract of the roots of Heptaptera cilicica (Boiss. & Bal.) Tutin (Apiaceae) was investigated in terms of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory effects by Ellman method. Afterwards, a new furocoumarin: trichoclin angelate with five known coumarin derivatives: umbelliprenin, badrakemone, badrakemin, badrakemin acetate and prunate were isolated from this extract. Their structures were identified by means of spectroscopic methods (1D, 2D-NMR and HRESIMS). The next step of our study was determining AChE and BuChE inhibitory activities of the compounds by molecular docking and in vitro methods. According to the results, prunate was found to be the most potent compound, which exhibited significant inhibitory potency against acetylcholinesterase (IC50 = 1.76 ± 0.003 µM) and butyrylcholinesterase (IC50 = 0.21 ± 0.002 μM) as compared with the reference compound, galantamine hydrobromide.


Heptaptera cilicica Apiaceae Coumarin AChE BuChE 


Compliance with ethical standards

Conflict of interest

The authors declare that they have no competing interests.


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Copyright information

© Springer Science+Business Media, LLC 2017

Authors and Affiliations

  • Hilal Özbek
    • 1
  • Zühal Güvenalp
    • 1
  • Gülderen Yılmaz
    • 2
  • Kadir Ö. Yerdelen
    • 3
  • Cavit Kazaz
    • 4
  • Ömür L. Demirezer
    • 5
  1. 1.Department of Pharmacognosy, Faculty of PharmacyAtatürk UniversityErzurumTurkey
  2. 2.Department of Pharmaceutical Botany, Faculty of PharmacyAnkara UniversityAnkaraTurkey
  3. 3.Department of Pharmaceutical Chemistry, Faculty of PharmacyAtatürk UniversityErzurumTurkey
  4. 4.Department of Chemistry, Faculty of ScienceAtatürk UniversityErzurumTurkey
  5. 5.Department of Pharmacognosy, Faculty of PharmacyHacettepe UniversityAnkaraTurkey

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