Chemical constituents from Daphne giraldii and their cytotoxicities and inhibitory activities against acetylcholinesterase.

Fitoterapia

Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Liaoning Province; Engineering Research Center of Natural Medicine Active Molecule Research & Development, Liaoning Province; Key Laboratory of Natural Bioactive Compounds Discovery & Modification, Shenyang; School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China. Electronic address:

Published: November 2022

AI Article Synopsis

  • Seven new compounds were extracted from the stem and root barks of Daphne giraldii, including five that have never been described before.
  • The structures of the new triterpenoids were determined using techniques like NMR and X-ray diffraction.
  • Cytotoxicity testing revealed that two prenylated coumarins had moderate activity, while some triterpenoids showed mild inhibition of an enzyme related to Alzheimer's disease, and further studies were done to explore their mechanisms.

Article Abstract

Seven triterpenoids (1-7), two prenylated coumarins (8 and 9), and one diphenylpropane (10), including five previously undescribed compounds (1-3, 8, and 10), were obtained from the stem and root barks of Daphne giraldii. The structures and absolute configurations of the new triterpenoids were established by NMR, HRESIMS, ECD calculations, and single-crystal X-ray diffraction analysis. All identified compounds were tested for cytotoxicities (human tumour cell line Hep3B) and inhibitory effects on AChE in vitro. Notably, prenylated coumarins (8 and 9) exhibited moderate cytotoxic activities and 3-hydroxy-substituted triterpenoids (2 and 4) showed mild inhibitory effects on AChE. Furthermore, compounds 2 and 4 have also been subjected to molecular docking studies to investigate the inhibitory mechanism.

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Source
http://dx.doi.org/10.1016/j.fitote.2022.105327DOI Listing

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