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Pharmacol Rep ; 67(3): 581-7, 2015 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-25933972

RESUMEN

Numerous studies have been suggested that derivatives can improve the effects of original substances. Therefore, we made luteolin derivative luteolin 8-C-ß-fucopyranoside (LU8C-FP) for better anti-inflammatory and anti-cancer effects. In a previous study, we demonstrated that LU8C-FP inhibits invasion of human breast cancer cells via suppression of matrix metalloproteinase 9 and IL-8, which play major roles in tumor progression and cancer cell invasion. Various stimuli trigger inflammatory responses by inducing pro-inflammatory cytokines and chemokines in THP-1 cells. IL-6 induces inflammation via inducing various cytokines and appears to be a potential mediator of inflammatory diseases. Here, we investigated the precise mechanism by which LU8C-FP inhibited phorbol 12-myristate 13-acetate-induced IL-6 mRNA and protein expression. We showed LU8C-FP downregulated IL-6 expression by inhibiting mitogen-activated protein kinases and the nuclear factor-kappaB signaling pathway in human monocytic cells. Furthermore, LU8C-FP exerts less cytotoxicity than luteolin and also it has specific inhibitory effect on IL-6 expression. However, luteolin has a variety of inhibitory effects on pro-inflammatory cytokines and chemokines. Our in vitro studies may provide valuable information leading to the use of LU8C-FP to treat inflammatory diseases caused by IL-6.


Asunto(s)
Regulación hacia Abajo/efectos de los fármacos , Interleucina-6/antagonistas & inhibidores , Luteolina/farmacología , Proteínas Quinasas Activadas por Mitógenos/antagonistas & inhibidores , Monocitos/efectos de los fármacos , FN-kappa B/antagonistas & inhibidores , Línea Celular , Regulación hacia Abajo/fisiología , Regulación de la Expresión Génica , Células HEK293 , Humanos , Interleucina-6/biosíntesis , Luteolina/química , Proteínas Quinasas Activadas por Mitógenos/metabolismo , Monocitos/metabolismo , FN-kappa B/metabolismo , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/farmacología , Transducción de Señal/efectos de los fármacos , Transducción de Señal/fisiología
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