Abstract
Lichens have exhibited numerous biological activities, including growth inhibition of tumor cells. This study evaluated the antiproliferative activity of hypostictic and salazinic acids against tumor cell lines (B16-F10, PC-03, MCF7, HT-29, HEP-G2, K562 and 786-0) by the SRB assay in vitro and antitumor activity in experimental murine melanoma in vivo. Activation of caspase-3 was quantified by flow cytometry. The murine experimental melanoma model B16-F10 was used in BALB/c mice for evaluation of antitumor activity. Hypostictic acid showed significant antiproliferative activity in K562 cells (GI50 2.20 μM), B16-F10 (GI50 13.78 μM) and 786-0 (GI50 14.24 μM), whereas salazinic acid was more active against K562 cells (GI50 64.36 μM), HT-29 (GI50 67.91 μM) and B16-F10 (GI5078.64 μM). Quantification of capase-3 revealed that the test compounds did not increase the expression of that enzyme. In the in vivo antitumor evaluation in B16-F10 melanoma, the isolated compounds inhibited tumor growth in relation to weight and volume. Hypostictic acid (16.7 mg/kg) inhibited 72% and salazinic acid 88% of tumor volume (p < 0.05). The results indicated that, both in the in vitro and in vivo models, the compounds evaluated showed antiproliferative and antitumor activities.
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DB, NKH and MFCM designed and supervised the study; CAFA, MCBLS and PRBS performed the experiments and analyzed the data; LC contributed to the histological analyzes; MCTK and RCA Gaided in vivo study and contributed to the interpretation of the results; RTP participated in the analysis of caspase; CAFA wrote the manuscript with support from MCBLS, NKH and DB. All authors reviewed the final manuscript.
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Alexandrino, C.A.F., Honda, N.K., de Matos, M.F.C. et al. Antitumor effect of depsidones from lichens on tumor cell lines and experimental murine melanoma. Rev. Bras. Farmacogn. 29, 449–456 (2019). https://doi.org/10.1016/j.bjp.2019.04.005
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DOI: https://doi.org/10.1016/j.bjp.2019.04.005