Journal of
Medicinal Plants Research

  • Abbreviation: J. Med. Plants Res.
  • Language: English
  • ISSN: 1996-0875
  • DOI: 10.5897/JMPR
  • Start Year: 2007
  • Published Articles: 3843

Full Length Research Paper

Antiplatelet aggregation and cytotoxic activity of betulinic acid and its acetyl derivative from Melaleuca bracteata

Foluso O. Osunsanmi*
  • Foluso O. Osunsanmi*
  • Department of Biochemistry and Microbiology, University of Zululand, Private Bag X1001,KwaDlangezwa 3886, Republic of South Africa.
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Oluwagbemiga S. Soyingbe
  • Oluwagbemiga S. Soyingbe
  • Department of Biochemistry and Microbiology, University of Zululand, Private Bag X1001,KwaDlangezwa 3886, Republic of South Africa.
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Idiat B. Ogunyinka
  • Idiat B. Ogunyinka
  • Department of Biochemistry and Microbiology, University of Zululand, Private Bag X1001,KwaDlangezwa 3886, Republic of South Africa.
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Rebamang A. Mosa Monisola I. Ikhile
  • Rebamang A. Mosa Monisola I. Ikhile
  • Department of Applied Chemistry, University of Johannesburg, Doornfontein Campus, P.O. Box17011, Doornfontein 2028, Johannesburg, South Africa.
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J. Catherine Ngila
  • J. Catherine Ngila
  • Department of Applied Chemistry, University of Johannesburg, Doornfontein Campus, P.O. Box17011, Doornfontein 2028, Johannesburg, South Africa.
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Francis O. Shode
  • Francis O. Shode
  • Department of Biotechnology and Food Technology, Durban University of Technology, P.O. Box 1334, Durban 4000, South Africa.
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Andy R. Opoku
  • Andy R. Opoku
  • Department of Biochemistry and Microbiology, University of Zululand, Private Bag X1001,KwaDlangezwa 3886, Republic of South Africa.
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  •  Received: 14 May 2015
  •  Accepted: 09 June 2015
  •  Published: 10 June 2015

Abstract

Platelet dysfunctions are implicated in cardiovascular diseases. Management of abnormal platelet aggregations with natural products is a promising approach to the treatment of cardiovascular diseases. In this study, betulinic acid (BA) isolated from Melaleuca bracteata leaf extract, and its acetyl derivative (3-β acetylbetulinic acid) (BAA) were investigated for their antiplatelet aggregation and cytotoxic activity. Structures of the compounds were established and confirmed through spectral (nuclear magnetic resonance [NMR], infrared [IR], mass spectroscopy [MS]) data analysis. The antiplatelet aggregation activity of the compounds was separately evaluated on collagen, adenosine diphosphate [ADP], thrombin and epinephrine induced rat platelet aggregations. The 3-(4,5)-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) cytotoxicity assay was used to determine the cytotoxic effect of the compounds against human embryonic kidney (HEK293) and hepatocellular carcinoma (HEPG2) cell lines. The triterpenoids exhibited significant (p<0.05) dose dependent antiplatelet aggregation activity. The highest inhibitory activity of BA and BAA was observed on epinephrine induced platelet aggregation with IC50 values 0.78 and 0.85 mg/ml, respectively. BA and BAA showed less cytotoxicity effect on both HEK293 cell (IC50 1027 and 1051 µg/ml, respectively) and HEPG2 cells (IC50 448 and 672 mg/ml, respectively). The results suggest that the compounds could serve as potential templates for synthesis of new antiplatelet drugs. 

 

Key words: Antiplatelet aggregation, thrombin, collagen, cytotoxicity, aspirin, triterpenes.