Please use this identifier to cite or link to this item:
https://hdl.handle.net/10216/130465
Author(s): | Brandão, P. Moreira, J. Almeida, J. Nazareth, N. Sampaio-Dias, I.E. Vasconcelos, V. Martins, R. Leão, P. Pinto, M. Saraíva, L. Cidade, H. |
Title: | Norhierridin B, a new hierridin B-based hydroquinone with improved antiproliferative activity |
Publisher: | MDPI |
Issue Date: | 2020 |
Abstract: | Hierridin B (6), a methylated hydroquinone isolated from the marine picocyanobacterium Cyanobium sp. LEGE 06113, moderately inhibited the growth of colon adenocarcinoma HT-29 cells. Aiming to improve the potential antitumor activity of this natural product, the demethylated analogue, norhierridin B (10), as well as its structurally-related quinone (9), were synthesized and evaluated for their growth inhibitory effect on a panel of human tumor cell lines, including the triple-negative breast cancer (TNBC) cells MDA-MB-231, SKBR3, and MDA-MB-468. Norhierridin B (10) showed a potent growth inhibitory effect on all cancer cell lines. Moreover, the growth inhibitory effect of compound 10 on MDA-MB-231 cells was associated with cell cycle arrest and apoptosis. Norhierridin B (10) interfered with several p53 transcriptional targets, increasing p21, Bax, and MDM2, while decreasing Bcl-2 protein levels, which suggested the potential activation of a p53 pathway. Altogether, these results evidenced a great improvement of the antitumor activity of hydroquinone 10 when compared to 6 and its structurally-related quinone (9). Notably, hydroquinone 10 displayed a prominent growth inhibitory activity against TNBC cells, which are characterized by high therapeutic resistance. |
Subject: | Antitumor activity Hierridin B Hydroquinones Quinones |
URI: | https://hdl.handle.net/10216/130465 |
Source: | Molecules 2020, 25(7), 1578 |
Document Type: | Artigo em Revista Científica Internacional |
Rights: | openAccess |
Appears in Collections: | CIIMAR - Artigo em Revista Científica Internacional |
Files in This Item:
File | Description | Size | Format | |
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Brandao_P_2020.pdf | 1.02 MB | Adobe PDF | View/Open |
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