Anti-oxidant, anti-inflammatory and antiacetylcholinesterase activity of betulinic acid and 3β- acetoxybetulinic acid from &lt;i&gt;Melaleuca bracteata&lt;/i&gt; ‘Revolution Gold’

Foluso O Osunsanmi,Andy R Opoku,Godfrey E Zharare,Rebamang A Mosa,Francis O Shode,Monisola I Ikhile

doi:10.4314/tjpr.v18i2.12

Abstract

Purpose: To evaluate the anti-oxidant, anti-inflammatory and anti-acetylcholine esterase activities of betulinic acid (BA) and 3β- acetoxybetulinic acid (BAA) from Melaleuca bracteata . ‘Revolution Gold’. Methods: Betulinic acid was isolated from the ethyl acetate extract of M. braceteata while BAA was synthesized by acetylation of BA. Structural elucidation of the compounds was achieved by spectroscopic methods. Antioxidant potential was determined using superoxide dismustase (SOD) and catalase assay kits while iron chelation activity assessed with ferrozin. Anti-inflammatory activity was determined using cotton pellet-induced granuloma rat model. Cyclooxygenase (COX) activity evaluated by COX kits; acetylcholine kit was used for anti-acetylcholinesterase (ACHE) study. Results: The compounds significantly ( p < 0.05) dose-dependently inhibited ACHE and inflammatory activity. They also significantly decreased the inhibition of SOD, catalase activity but increased iron chelation activities in a dose-dependent manner. However, BAA showed higher activity than BA for all the parameters. BAA also had a greater inhibitory effect on COX-2 than on COX-1. BAA (IC 50 , 0.88 mg/mL) showed better iron chelation than citric acid (0.96 ± 0.04) and EDTA (1.04 ± 0.03), the positive control. Conclusion: BA and BAA possess anti-ACHE, anti-inflammatory, antioxidant and anti-COX activities. Structural modification of BAA influences its biological activities. Therefore, BAA can potentially serve as a scaffold in synthesizing potent neurodegeneration drugs. Keywords: Betulinic acid, 3β-Acetoxybetulinic acid, Antioxidant, Anti-inflammatory, Antiacetylcholinesterase, Melaleuca bracteata . ‘Revolution Gold’

Highlights

Oxidative stress, inflammation and acetylcholinesterase activities are hallmarks of neurodegeneration diseases such as; Alzheimer, Amyotrophic lateral sclerosis and Parkinson disease [1]
Acetylcholine attenuates the release of cytokine from parasympathetic anti-inflammatory pathway, modulate inflammatory response against endotoxin in the brain [3]
Betulinic acid was isolated from crude extract of Melaleuca bracteata (Myrtaceae) Muell by following the method of Habila et al [6]

Summary

INTRODUCTION

Inflammation and acetylcholinesterase activities are hallmarks of neurodegeneration diseases such as; Alzheimer, Amyotrophic lateral sclerosis and Parkinson disease [1]. Oxidative stress overwhelms enzymatic and non-enzymatic antioxidant activities, leading to damage of biopolymers including nucleic acid, protein, carbohydrate, and polyunsaturated fatty acids. This study focused on antioxidant, anti-inflammatory and anti-acetylcholine esterase potential of BA and BAA from M. bracteata leaves. Melaleuca bracteata (Myrtaceae) Muell leaves were harvested at University of Zululand, South Africa (28.8524° S, 31.8491° E). Betulinic acid was isolated from crude extract of Melaleuca bracteata (Myrtaceae) Muell by following the method of Habila et al [6]. The SOD activity of the compounds were evaluated using SOD assay kit (Sigma- Aldrich Chemical Company limited). The catalase activity of the compounds were evaluated using the catalase assay kit (SigmaAldrich Chemical Company limited). The reaction was initiated with ferrozin (5 mM; 0.1 mL) after 45 sec of mixture Afterward, it was incubated (25 oC; 10 min), and absorbance read at 562 nm using colorimeter.

RESULTS

DISCUSSION

CONCLUSION

Conflict of interest