Characterization and Biological Evaluation of Diterpenoids from Casearia graveolens

J Nat Prod. 2015 Nov 25;78(11):2648-56. doi: 10.1021/acs.jnatprod.5b00583. Epub 2015 Oct 16.

Abstract

Biologically active substances that promote the neurite outgrowth of nerve cells against neuron degeneration may be useful for the treatment of Alzheimer's disease. In a continuing search for bioactive compounds from plants, an ethyl acetate-soluble extract of the twigs of Casearia graveolens showed moderate stimulatory activity of neurite outgrowth from PC12 cells. Further investigation to obtain bioactive compounds led to the isolation of 10 new clerodane diterpenoids, graveopenes A-J (1-10). Their structures including absolute configurations were elucidated based on analysis of their NMR spectroscopic data and experimental and calculated ECD spectra. Compounds 3-6 and 8 were shown to stimulate NGF-mediated neurite outgrowth from PC12 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / drug therapy
  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / isolation & purification*
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Casearia / chemistry*
  • Diterpenes, Clerodane / chemistry
  • Diterpenes, Clerodane / isolation & purification*
  • Diterpenes, Clerodane / pharmacology*
  • Drug Screening Assays, Antitumor
  • Drugs, Chinese Herbal / chemistry
  • Drugs, Chinese Herbal / isolation & purification*
  • Drugs, Chinese Herbal / pharmacology*
  • Molecular Structure
  • Nerve Growth Factor / drug effects
  • Neurites / drug effects
  • Nuclear Magnetic Resonance, Biomolecular
  • PC12 Cells
  • Plants, Medicinal / chemistry*
  • Rats

Substances

  • Antineoplastic Agents, Phytogenic
  • Diterpenes, Clerodane
  • Drugs, Chinese Herbal
  • Nerve Growth Factor