Synthesis and Evaluation of Analgesic and Anti-inflammatory Activities of Most Active Antioxidant Derivatives of Embelin
S. Mahendran *
Faculty of Pharmacy and Health Sciences, Universiti Kuala Lumpur, Royal College of Medicine Perak, Ipoh – 30450, Peark, Malaysia.
S. Badami
Sree Siddaganga College of Pharmacy, Tumkur – 572 102, KN, India.
S. Ravi
Department of Chemistry, Karpagam University, Coimbatore – 640 021, TN, India.
B. S. Thippeswamy
Sree Siddaganga College of Pharmacy, Tumkur – 572 102, KN, India.
V. P. Veerapur
Sree Siddaganga College of Pharmacy, Tumkur – 572 102, KN, India.
*Author to whom correspondence should be addressed.
Abstract
Objective: To evaluate antioxidant, analgesic and anti-inflammatory properties of embelin and its derivatives.
Methods: In the present study embelin was condensed with various aliphatic substituted primary amines, hydrazines and amino acids to yield seven new and five reported derivatives. All these compounds along with embelin were evaluated for in vitro antioxidant activity using ABTS and DPPH methods. Potent compounds were selected for in vivo analgesic and anti-inflammatory activities.
Results: Hydrazines, amino acids substituted embelin derivatives and phenazines showed potent antioxidant activity. These compounds along with embelin were studied for analgesic and anti-inflammatory activities at 10 and 20 mg/kg doses by standard methods. Potent analgesic activity higher than the standard pentazocine was observed. Embelin and its derivatives almost completely abolished the acetic acid induced writhing. Phenyl alanine and phenazine derivative showed better anti-inflammatory activity than embelin.
Conclusion: Further research would be of interest to explain the exact mechanism of these compounds and chemical modifications, biological screening and toxicity studies can also be explored.
Keywords: Embelin, structure activity relationship, antioxidant, analgesic, anti-inflammatory.