Rotenoids from Boerhaavia diffusa as potential anti-inflammatory agents

Area of Science:

• Phytochemistry
• Pharmacology

Background:

• Boerhaavia diffusa is a medicinal plant with a history of traditional use.
• Rotenoids are a class of organic compounds found in plants, known for various biological activities.

Purpose of the Study:

• To isolate and characterize new rotenoids from Boerhaavia diffusa.
• To evaluate the COX-1 and COX-2 inhibitory activities of isolated rotenoids.
• To assess the in vivo anti-inflammatory potential of Boerhaavia diffusa extracts and compounds.

Main Methods:

• Methanol extraction of Boerhaavia diffusa roots.
• Isolation and structural elucidation of rotenoids using spectroscopic data.
• In vitro assays for cyclooxygenase (COX)-1 and COX-2 inhibition.
• In vivo anti-inflammatory testing using a carrageenan-induced rat paw edema model.

Main Results:

• Five new rotenoids (2, 3, 5, 7, 9) and four known rotenoids (1, 4, 6, 8) were identified.
• Compound 7 exhibited the most potent inhibition of both COX-1 (IC₅₀ = 21.7 ± 0.5 μM) and COX-2 (IC₅₀ = 25.5 ± 0.6 μM).
• Boeravinone B (6) displayed significant anti-inflammatory activity (56.6% inhibition at 50 mg/kg).

Conclusions:

• Boerhaavia diffusa roots are a rich source of diverse rotenoids.
• Compound 7 is a potent inhibitor of COX-1 and COX-2 enzymes.
• Boeravinone B possesses notable in vivo anti-inflammatory properties, supporting its traditional medicinal use.