Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Antithrombotic, anticoagulant and antiplatelet activity of betulinic acid and 3β-acetoxybetulinic acid from Melaleuca bracteata Revolution Gold (Myrtaceae) Muell leaf

Foluso O Osunsanmi¹ , Godfrey E Zaharare¹, Babatunji E Oyinloye^2,3, Rebamang A Mosa², Monisola I Ikhile⁴, Francis O Shode⁵, Idiat B Ogunyinka⁶, Andy R Opoku²

¹Department of Agricultural Science, University of Zululand, Private Bag X1001, KwaDlangezwa 3886; ²Department of Biochemistry and Microbiology, University of Zululand, Private Bag X1001, KwaDlangezwa 3886; ³Department of Biochemistry, College of Sciences, Afe Babalola University, PMB 5454, Ado-Ekiti 360001, Nigeria; ⁴Department of Applied Chemistry, University of Johannesburg, Doornfontein Campus, PO Box 17011, Doornfontein 2028, Johannesburg; ⁵Department of Biotechnology and Food Technology, Durban University of Technology, PO Box 1334, Durban 4000; ⁶Department of Consumer Sciences, University of Zululand, Private Bag X1001, KwaDlangezwa 3886, South Africa.

For correspondence:- Foluso Osunsanmi Email: alafin21@yahoo.com Tel:+27791565341

Accepted: 20 September 2018 Published: 31 October 2018

Citation: Osunsanmi FO, Zaharare GE, Oyinloye BE, Mosa RA, Ikhile MI, Shode FO, et al. Antithrombotic, anticoagulant and antiplatelet activity of betulinic acid and 3β-acetoxybetulinic acid from Melaleuca bracteata Revolution Gold (Myrtaceae) Muell leaf. Trop J Pharm Res 2018; 17(10):1983-1989 doi: 10.4314/tjpr.v17i10.13

© 2018 The authors.
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Abstract

Purpose: To investigate the antithrombotic, anticoagulant and antiplatelet activity 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. bracteata leaves by column chromatography, from which BAA was subsequently synthesized by acetylation. Structural elucidation of the compounds was conducted using mass spectrometry (MS), infra-red (IR) spectroscopy and nuclear magnetic resonance (NMR). The antithrombotic potential of the compounds was assessed using chromogenic substrate. Anticoagulation studies were carried using bleeding tail time assay in a rat model. Plasma-rich platelets from rats were employed for platelet aggregation studies using light microscope.

Results: The compounds significantly (p < 0.05) showed antithrombotic activities in a dose-dependent manner. BAA showed significantly (p < 0.05) higher half-maximal concentration (IC₅₀) value of 1.10 ± 0.03 mg/mL than BA (2.36 ± 0.09 mg/mL) and aspirin (2.65 ± 0.01 mg/mL) which served as positive control. The compounds exhibited anticoagulation activity with poor bleeding time, compared to aspirin. Likewise, the compounds attenuated platelets aggregation induced by thrombin.

Conclusion: BAA displays better antithrombotic, antiplatelet, and anticoagulant activities than BA. Therefore, it may be a promising remedy for the management of cardiovascular events.

Keywords: Betulinic acid, Thrombin, Anticoagulation, Antiplatelet, Aspirin, Platelets