Cytotoxic constituents from Penicillium concentricum, an endophytic fungus from Trichocolea tomentella
| Autor: | Esperanza J. Carcache de Blanco, Gerardo D. Anaya-Eugenio, Liva Harinantenaina Rakotondraibe, Tehane Ali |
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| Rok vydání: | 2019 |
| Předmět: |
0301 basic medicine
Cancer Research Sulforhodamine B Antineoplastic Agents Apoptosis HeLa 03 medical and health sciences Prostate cancer chemistry.chemical_compound 0302 clinical medicine Neoplasms medicine Tumor Cells Cultured Cytotoxic T cell Humans Pharmacology (medical) IC50 Cell Proliferation Pharmacology Membrane potential Membrane Potential Mitochondrial biology Chemistry Cell Cycle NF-kappa B Penicillium Cell cycle biology.organism_classification medicine.disease Molecular biology 030104 developmental biology Oncology 030220 oncology & carcinogenesis Drug Screening Assays Antitumor Penicillium concentricum Streptophyta |
| Zdroj: | Anti-cancer drugs. 30(4) |
| ISSN: | 1473-5741 |
| Popis: | In our continuing effort to identify bioactive secondary metabolites from natural sources, the antiproliferative activity of 23 compounds, previously isolated from Penicillium concentricum, was assessed using the sulforhodamine B assay. The cytotoxic effect was determined against HeLa cervical, HT-29 colon, MDA-MB-321 breast, PC-3, and DU-145 prostate cancer cell lines. Compounds were also tested in the mitochondrial transmembrane potential (MTP) and nuclear factor kappa B (NF-κB) target-based assays. The results showed that 2-bromogentisyl alcohol (2) and 3-hydroxy-benzenemethanol (8) exhibited the highest cytotoxic activity against different cancer cell lines. Epoxydon (14) showed selectivity against DU-145 prostate cancer cells [inhibitory concentration 50 (IC50)=1.2 μmol/l]. Compounds 2, 8, 14, 18, 21 also induced damage of MTP (IC50=0.1, 0.2, 7.0, 9.6, and 1.8 μmol/l, respectively). In the NF-κB assay, only compound 8 exhibited potent inhibition (IC50=0.3 μmol/l). Compounds 2 and 14 showed cytotoxic activity and induction of damage in mitochondrial membrane potential while compound 8 inhibited NF-κB and MTP damage. Additionally, compound 14 with selectivity against DU-145 prostate cancer cells induced cell cycle arrested in G2/M phase. Thus, compounds 2, 8, and 14 could be useful leads in the development of new anticancer agents from natural sources. |
| Databáze: | OpenAIRE |
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