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Bioactive diterpenoids from Croton laevigatus.

Jun-Sheng Zhang1, Ya-Qi Tang1, Jia-Luo Huang1

  • 1School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China.

Phytochemistry
|September 22, 2017
PubMed
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Eight new diterpenoids from Croton laevigatus twigs were identified, including novel halimanes. Two compounds showed significant nitric oxide (NO) inhibition in macrophage cells, outperforming quercetin.

Area of Science:

  • Natural Products Chemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Croton laevigatus is a plant source of bioactive compounds.
  • Diterpenoids are a diverse class of natural products with various biological activities.

Purpose of the Study:

  • To isolate and characterize new diterpenoids from Croton laevigatus.
  • To evaluate the anti-inflammatory potential of isolated compounds by measuring nitric oxide (NO) production.

Main Methods:

  • Isolation of compounds using chromatographic techniques.
  • Structure elucidation via spectroscopic methods (NMR, MS) and X-ray crystallography.
  • Assessment of NO inhibitory activity in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells.
Keywords:
Absolute configurationCroton laevigatus (Euphorbiaceae)DiterpenoidsNO inhibition

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Main Results:

  • Eight new diterpenoids, crolaevinoids A-H (two halimanes, four clerodanes, two laevinanes), were identified.
  • Crolaevinoids A and B are the first halimanes with a C-12/C-17 lactone bridge.
  • Two compounds, Furocrotinsulolide A and 3,4,15,16-diepoxy-cleroda-13(16),14-diene-12,17-olide, potently inhibited NO production (IC50 values 10.4 and 6.0 μM).

Conclusions:

  • The study expands the chemical diversity of diterpenoids from Croton laevigatus.
  • The identified compounds, particularly Furocrotinsulolide A and 3,4,15,16-diepoxy-cleroda-13(16),14-diene-12,17-olide, demonstrate significant potential as anti-inflammatory agents.