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| El-demerdash, Amr; Moriou, Celine; Toullec, Jordan; Besson, Marc; Soulet, Stephanie; Schmitt, Nelly; Petek, Sylvain; Lecchini, David; Debitus, Cecile; Al-mourabit, Ali. |
| Herein, we describe the isolation and spectroscopic identification of eight new tetrabrominated tyrosine alkaloids 2–9 from the Polynesian sponge Suberea ianthelliformis, along with known major compound psammaplysene D (1), N,N-dimethyldibromotyramine, 5-hydroxy xanthenuric acid, and xanthenuric acid. Cytotoxicity and acetylcholinesterase inhibition activities were evaluated for some of the isolated metabolites. They exhibited moderate antiproliferative activity against KB cancer cell lines, but psammaplysene D (1) displayed substantial cytotoxicity as well as acetylcholinesterase inhibition with IC50 values of 0.7 μM and 1.3 μM, respectively. |
| Tipo: Text |
Palavras-chave: Brominated tyrosine alkaloids; Suberea ianthelliformis; Cytotoxicity; Acetylcholinesterase inhibition. |
| Ano: 2018 |
URL: https://archimer.ifremer.fr/doc/00439/55076/56506.pdf |
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| Florean, Cristina; Kim, Kyung Rok; Schnekenburger, Michael; Kim, Hyun-jung; Moriou, Celine; Debitus, Cecile; Dicato, Mario; Al-mourabit, Ali; Han, Byung Woo; Diederich, Marc. |
| Treatment of acute myeloid leukemia (AML) patients is still hindered by resistance and relapse, resulting in an overall poor survival rate. Recently, combining specific B-cell lymphoma (Bcl)-2 inhibitors with compounds downregulating myeloid cell leukemia (Mcl)-1 has been proposed as a new effective strategy to eradicate resistant AML cells. We show here that 1(R), 6(S), 1'(R), 6'(S), 11(R), 17(S)-fistularin-3, a bromotyrosine compound of the fistularin family, isolated from the marine sponge Suberea clavata, synergizes with Bcl-2 inhibitor ABT-199 to efficiently kill Mcl-1/Bcl-2-positive AML cell lines, associated with Mcl-1 downregulation and endoplasmic reticulum stress induction. The absolute configuration of carbons 11 and 17 of the fistularin-3... |
| Tipo: Text |
Palavras-chave: Acute myeloid leukemia; ABT-199; Mcl-1; Bromotyrosine; (+)-11(R); 17(S)-fistularin-3; Configuration; Anticancer drug combination. |
| Ano: 2018 |
URL: https://archimer.ifremer.fr/doc/00476/58783/62419.pdf |
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