Synthesis and cytotoxicity evaluation of 3-amino-2-hydroxypropoxygenistein derivatives / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 871-880, 2017.
Artículo
en Inglés
| WPRIM
| ID: wpr-812046
ABSTRACT
Soy isoflavones exhibit various biological activities, such as antioxidant, anti-tumor, anti-inflammatory, and cardiovascular protective effects. The present study was designed to investigate the effects of sixteen synthesized 3-amino-2-hydroxypropoxy genistein derivatives on cell proliferation and activation of Nrf2 (Nuclear factor erythroid 2-related factor 2)/ARE (antioxidant response elements) pathway in human cancer cell lines. Most of the tested compounds exerted greater cytotoxic activity than genistein, as measured by MTT assay. Moreover, compound 8c showed the highest ARE-luciferase reporter activity among the test compounds. It strongly promoted Nrf2 nuclear translocation and up-regulated the expression of total Nrf2 and downstream targets NQO-1 and HO-1 at protein level. The present study may provide a basis for the application of isoflavone derivatives as Nrf2/ARE pathway inducers for cancer therapy and cancer prevention.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Glycine max
/
Transducción de Señal
/
Regulación hacia Arriba
/
Química
/
Genisteína
/
Línea Celular Tumoral
/
Usos Terapéuticos
/
Proliferación Celular
/
Quimioterapia
Límite:
Humanos
Idioma:
Inglés
Revista:
Chinese Journal of Natural Medicines (English Ed.)
Año:
2017
Tipo del documento:
Artículo
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