Colletofragarone A2 and Colletoins A-C from a Fungus Colletotrichum sp. Decrease Mutant p53 Levels in Cells.
J Nat Prod
; 84(12): 3131-3137, 2021 12 24.
Article
en En
| MEDLINE
| ID: mdl-34854682
ABSTRACT
p53 is frequently mutated in tumor cells. Mutant p53 (mut p53) accumulates in cells to promote cancer progression, invasion, and metastasis, and it is attracting attention as a target for cancer therapies. In this study, we used immunofluorescence staining of Saos-2 cells harboring doxycycline-inducible p53R175H [Saos-2 (p53R175H) cells] to search for compounds from natural sources that can target mut p53 and found an extract of Colletotrichum sp. (13S020) that was active. Bioassay-guided fractionation of the extract afforded a known polyketide, colletofragarone A2 (1), and three new analogues, colletoins A-C (2-4). The relative and absolute configurations of 1 were determined by the spectroscopic method and DFT calculation. Compounds 1 and 2 inhibited the growth of Saos-2 (p53R175H) cells and decreased mut p53 in the cells.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Proteína p53 Supresora de Tumor
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Colletotrichum
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Policétidos
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Mutación
Límite:
Humans
Idioma:
En
Revista:
J Nat Prod
Año:
2021
Tipo del documento:
Article
País de afiliación:
Japón