4.7 Article

Bioassay-guided isolation of anti-tumor polyprenylphloroglucinols from Calophyllum polyanthum and primary mechanism

Journal

BIOMEDICINE & PHARMACOTHERAPY
Volume 151, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.biopha.2022.113129

Keywords

Calophyllum polyanthum; Polyprenylphloroglucinols; Colorectal cancer; AKT; Apoptosis

Funding

  1. Technology Foundation of Health Bureau of Guizhou Province [gzwjkj2019-1-197, gzwkj2022-468]
  2. The First People's Hospital of Zunyi [HZzi-2020-97]

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Apetalic acid isolated from Calophyllum polyanthum leaves exhibits significant anti-tumor activity, particularly against colon cancer cells. It functions by regulating the expression of apoptosis-related genes and proteins. This supports its potential use in the prevention and treatment of colorectal cancer.
Five compounds were isolated from Calophyllum polyanthum leaves (10.09 g) by bioassay-guided fractionation to evaluate their anti-tumor activity. Among these compounds, apetalic acid (1) demonstrated significant inhibitory activity against 8 types of tumor cells (MHCC97H, CNE1, CNE2, B16, LOVO, SW480, A549, 1299), especially against two colon cancer cells (LOVO, SW480). Apetalic acid could inhibit cell proliferation, migration, invasion and induce apoptosis. It could significantly up-regulate the expression levels of apoptosis-related genes (BAX, Caspase-9,) and proteins (BAX, Cleaved-caspase-9, Cleaved-caspase-3) and down-regulated the expression of inhibitor of apoptosis gene (Bcl-2) and proteins (Bcl-2, phosphorylated AKT). Possible mechanism of the antitumor activity of apetalic acid derived from Calophyllum polyanthum supports its use in the prevention and treatment of colorectal cancer.

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