4.4 Article

Investigation of U-251 cell death triggered by flavonoid luteolin: towards a better understanding on its anticancer property against glioblastomas

Journal

NATURAL PRODUCT RESEARCH
Volume 35, Issue 22, Pages 4807-4813

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2020.1727470

Keywords

Luteolin; Brazilian plant species; Fridericia platyphylla; anticancer; natural products; glioblastoma

Funding

  1. Capes (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior)
  2. FAPESP (Fundacao de Amparo a Pesquisa do Estado de Sao Paulo) [2016/06137-6, 2016/02345-3]
  3. Maranhao State Research Foundation - FAPEMA [00863/16]
  4. FINEP [MCTI/FINEP/MS/SCTIE/DECIT-01/2013 - FPXII-BIOPLAT]

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This study found that luteolin exhibits antiproliferative activity against various tumor cell lines, with glioblastoma being the most sensitive, inducing apoptosis and DNA damage through multiple mechanisms. These results suggest luteolin's potential as a therapeutic drug.
Recently, many studies have reported the anticancer properties of flavonoid luteolin against a variety of tumors, but there is still a lack in the description of its mechanism of action. In attempt to better contribute to the literature, we evaluated the antiproliferative activity of luteolin extracted by Fridericia platyphylla in a panel of tumor cell lines representative of six different tissues. Luteolin presented antiproliferative activity for all the assessed tumor cell lines, being glioblastoma the most sensitive one. This compound was able to inhibit U-251 cells migration and tumorigenesis. Besides, luteolin leads U-251 tumor cells to apoptosis death by depolarisation of the mitochondrial membrane, ERK proteins phosphorylation, cleavage of PARP and Caspase 9, further inducing DNA damage by H2AX phosphorylation, which had not yet been described for glioblastomas. Altogether, our results reaffirm luteolin as a potential therapeutic drug.

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