Peltophorum Africanum, a Traditional South African Medicinal Plant, Contains an Anti HIV-1 Constituent, Betulinic Acid

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  • Theo Andros
    Laboratory of Emerging Infectious Diseases, Internal Medicine, Graduate School of Medicine, Tohoku University
  • Masebe Tracy
    Department of Microbiology, University of Venda, Thohoyandou, Limpopo Province
  • Suzuki Yasuhiro
    Laboratory of Emerging Infectious Diseases, Internal Medicine, Graduate School of Medicine, Tohoku University
  • Kikuchi Haruhisa
    Graduate School of Pharmaceutical Sciences, Tohoku University
  • Wada Shoko
    Graduate School of Pharmaceutical Sciences, Tohoku University
  • Obi Chikwelu Larry
    Academic and Research Directorate, Walter Sisulu University
  • Bessong Pascal Obong
    Department of Microbiology, University of Venda, Thohoyandou, Limpopo Province
  • Usuzawa Motoki
    Laboratory of Emerging Infectious Diseases, Internal Medicine, Graduate School of Medicine, Tohoku University Japan Foundation for AIDS Prevention
  • Oshima Yoshiteru
    Graduate School of Pharmaceutical Sciences, Tohoku University
  • Hattori Toshio
    Laboratory of Emerging Infectious Diseases, Internal Medicine, Graduate School of Medicine, Tohoku University

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説明

The biodiversity of medicinal plants in South Africa makes them rich sources of leading compounds for the development of novel drugs. Peltophorum africanum (Fabaceae) is a deciduous tree widespread in South Africa. The stem bark has been traditionally employed to treat diarrhoea, dysentery, sore throat, wounds, human immunodeficiency virus/ acquired immune deficiency syndrome (HIV/AIDS), venereal diseases and infertility. To evaluate these ethnobotanical clues and isolate lead compounds, butanol and ethyl acetate extracts of the stem bark were screened for their inhibitory activities against HIV-1 using MAGI CCR5+ cells, which are derived from HeLa cervical cancer cells and express HIV receptor CD4, a chemokine receptor CCR5 and HIV-LTR-β- galactosidase. Bioassay-guided fractionation using silica gel chromatography was also conducted. The ethyl acetate and butanol extracts of the stem bark of Peltophorum africanum showed inhibitory activity against HIV-1, CXCR4 (X4) and CCR5 (R5) tropic viruses. The ethyl acetate and butanol extracts yielded previously reported anti-HIV compounds, (+)-catechin, a flavonoid, and bergenin, a C-galloylglycoside, respectively. Furthermore, we identified betulinic acid from the ethyl acetate fraction for the first time. </i>The fractions, which contained betulinic acid, showed the highest selective index. We therefore describe the presence of betulinic acid, a not well-known anti-HIV compound, in an African medicinal herb, which has been used for therapy, and claim that betulinic acid is the predominant anti-HIV-1 constituent of Peltophorum africanum. These data suggest that betulinic acid and its analogues could be used as potential therapeutics for HIV-1 infection.

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