Diterpenoids from Acanthopanacis Cortex and their anti-inflammatory activity studies

Area of Science:

• Natural Product Chemistry
• Pharmacology

Background:

• Acanthopanacis Cortex (A.-C) has a documented history of over 1000 years for treating rheumatism.
• Diterpenoids are a significant class of natural products with diverse biological activities.

Purpose of the Study:

• To isolate and characterize diterpenoids from Acanthopanacis Cortex.
• To evaluate the anti-inflammatory potential of isolated compounds, specifically their inhibitory effects on neutrophil elastase, COX-1, and COX-2.

Main Methods:

• Isolation of nineteen diterpenoids from A.-C, including six novel compounds.
• Structural elucidation using NMR spectroscopy and electronic circular dichroism (ECD) analysis.
• Single-crystal X-ray diffraction for definitive structural confirmation of selected compounds.
• In vitro anti-inflammatory assays measuring inhibition of neutrophil elastase, COX-1, and COX-2.

Main Results:

• Six new diterpenoids (1-6) were identified, alongside thirteen known compounds.
• Compounds 7, 9-11, 13, and 17 were reported from A.-C for the first time.
• Compound 15 exhibited potent and selective inhibition of cyclooxygenase-2 (COX-2) with an IC50 of 0.73 μM, while showing minimal COX-1 inhibition.

Conclusions:

• The study successfully isolated and characterized novel diterpenoids from Acanthopanacis Cortex.
• Compound 15 shows significant potential as a selective COX-2 inhibitor, warranting further investigation for anti-inflammatory therapeutic development.