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1.
Bioorg Med Chem Lett ; 26(15): 3806-9, 2016 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-27293071

RESUMO

Radiographic contrast media facilitate the visibility of internal body structures, but its use to patients with lowered renal function needs to be careful because of severe side effect in kidney. The present study aims to evaluate potential protective effect and mechanism of Alpha mangostin (α-mangostin) against contrast-induced apoptotic damage in LLC-PK1 cells. As a result, α-mangostin in non-toxic concentrations improved the viability of the iodixanol-treated cells up to 90.42% against contrast-induced damage in LLC-PK1 cells. Iodixanol treatment increased the phosphorylation of p38, ERK and cleavage of caspase-3 in LLC-PK1 cells, which were significantly decreased by co-treatment with α-mangostin (2.5 and 5µM). The protective effect of α-mangostin on contrast-induced apoptotic damage was mediated by the inhibition of MAPKs and caspase activation.


Assuntos
Apoptose/efeitos dos fármacos , Ácidos Tri-Iodobenzoicos/antagonistas & inibidores , Xantonas/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Células LLC-PK1 , Estrutura Molecular , Relação Estrutura-Atividade , Suínos , Ácidos Tri-Iodobenzoicos/farmacologia , Xantonas/síntese química , Xantonas/química
2.
Bioorg Med Chem Lett ; 26(5): 1466-70, 2016 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-26838808

RESUMO

This study was performed to investigate the renoprotective effect and mechanism of Momordicae Semen, gac seeds, against the cisplatin-induced damage in LLC-PK1 kidney cells. In order to identify the active components, three major saponins were isolated from extract of the gac seed, gypsogenin 3-O-ß-d-galactopyranosyl(1→2)-[α-L-rhamnopyranosyl(1→3)]-ß-d-glucuronopyranoside (1), quillaic acid 3-O-ß-D-galactopyranosyl(1→2)-[α-L-rhamnopyranosyl(1→3)]-ß-D-glucuronopyranoside (2), and momordica saponin I (3). Compounds 1 and 2 ameliorated cisplatin-induced nephrotoxicity up to 80% of the control value at both 5 and 25µM. Phosphorylation of MAPKs was decreased along cisplatin treatment after treatment with compounds 1 and 2. These results show that blocking the MAPKs signaling cascade plays a critical role in mediating the renoprotective effect of Momordicae Semen extract and compounds 1 and 2.


Assuntos
Apoptose/efeitos dos fármacos , Cisplatino/antagonistas & inibidores , Rim/efeitos dos fármacos , Rim/patologia , Momordica/química , Saponinas/farmacologia , Sementes/química , Animais , Cisplatino/farmacologia , Relação Dose-Resposta a Droga , Células LLC-PK1 , Estrutura Molecular , Saponinas/química , Saponinas/isolamento & purificação , Relação Estrutura-Atividade , Suínos
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