Foluso O Osunsanmi1
,
Godfrey E Zaharare1,
Babatunji E Oyinloye2,3,
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