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    Cytotoxicity, Phagocytic Activity, and Leishmanicidal Potential of Extract Standardized in Geranylgeraniol Obtained from the Fruit of Pterodon emarginatus Vogel

    Suzana Ferreira Alves2,3★, Clayson Moura Gomes3,4, Matheus Gabriel de Oliveira2, Wanessa Machado de Andrade3,5, Larissa Cleres Moreira5, Leonardo Luiz Borges3,6, Cláudio Carlos da Silva7, Graciella Ottoni de Souza7, Vinicius Barreto da Silva3, Marize Campos Valadares5, Maria Teresa Freitas Bara2★ Corresponding author

    1. 1Faculty of Pharmacy, Natural Products Research Laboratory, Federal University of Goiás, Brazil.
    2. 2Pharmacy Course, School of Medical Sciences, Pharmaceuticals and Biomedical Sciences, Pontifical Catholic University of Goiás, Brazil.
    3. 3Institute of Tropical Pathology and Public Health, Brazil.
    4. 4Faculty of Pharmacy Laboratory of Pharmacology and Cell Toxicology – Farmatec, Federal University of Goiás, Brazil.
    5. 5Pharmacy Course, University Unit of Exact and Technological Sciences, State University of Goiás, Anápolis, Go, Brazil.
    6. 6Replicon Research Center, Department of Biology, Pontifical Catholic University of Goiás, Goiânia, Brazil.

    CORRESPONDENCE

    Suzana Ferreira Alves

    Pharmacy Course, School of Medical Sciences, Pharmaceuticals and Biomedical Sciences, Pontifical Catholic University of Goiás, Brazil.

    suzanafal@gmail.com

    Received: 29-05-2019; Revised: 27-06-2019.

    Volume 16, Issue 67 · pp. 140–147 · PUBLISHED 11 February 2020 · DOI: 10.4103/pm.pm_231_19

    View on Pharmacogn. Mag. original site ↗

    ABSTRACT

    Background: P. emarginatus is a Brazilian medicinal plant with several constituents shown to have anti‑inflammatory, antinociceptive, antimicrobial, and antiproliferative activities. Materials and Methods: The standardized extract in geranylgeraniol obtained from the fruit of P. emarginatus was investigated for clastogenic and cytotoxic effects, as well as phagocytic activity against Leishmania guyanensis. Results: A 24‑h exposure of Allium cepa roots to standardized geranylgeraniol extract (9.77 mg/mL) promoted clastogenic effects, with a mitotic index (MI) of 10.33 ± 0.61. Extending the exposure time to 48 or 72 h significantly reduced the MI (P < 0.05). The IC50 for geranylgeraniol in 3T3 and RAW 264.7 cells was found to be 15.5 mg/mL and 12.2 mg/mL, respectively. The standardized extract in geranylgeraniol exhibited high phagocytic and microbicidal activities in Leishmania, promoting a >60% increase in macrophage infection, with greater internalization and destruction of the parasite. In silico study results suggest that geranylgeraniol acts in Leishmania by interfering with the biosynthesis of sterols through steric hindrance of the active site of the enzyme CYP51. Conclusion: The standardized extract in geranylgeraniol may be useful as an antiproliferative agent, macrophage immunomodulator, and as a cytotoxic treatment against infectious agents.

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      Alves, S. F., Gomes, C. M., Oliveira, M. G. D., Andrade, W. M. D., Moreira, L. C., Borges, L. L., Silva, C. C. D., Souza, G. O. D., Silva, V. B. D., Valadares, M. C., & Bara, M. T. F. (2020). Cytotoxicity, Phagocytic Activity, and Leishmanicidal Potential of Extract Standardized in Geranylgeraniol Obtained from the Fruit of Pterodon emarginatus Vogel. Pharmacognosy Magazine, 16(67), 140–147. https://doi.org/10.4103/pm.pm_231_19