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Baicalein Targets MAPK9 to Induce Apoptosis of Hepatocellular Carcinoma Cells.
Wang, Weili; Tang, Yuxiao; Zhuo, Xiaobin; Yang, Jianxin; Gao, Zelong; Li, Chenqi; Wu, Chenghua; Qian, Jianxin; Xie, Feng; Shen, Hui; Wang, Dongyao.
Afiliação
  • Wang W; Jiangxi University of Chinese Medicine, Nanchang, China.
  • Tang Y; Department of Nutrition, Naval Medical University, Shanghai, China.
  • Zhuo X; Eastern Hepatobiliary Surgery Hospital, Naval Medical University, Shanghai, China.
  • Yang J; Department of Nutrition, Naval Medical University, Shanghai, China.
  • Gao Z; School of Pharmacy, Naval Medical University, Shanghai, China.
  • Li C; Department of Nutrition, Naval Medical University, Shanghai, China.
  • Wu C; Department of Nutrition, Naval Medical University, Shanghai, China.
  • Qian J; Eastern Hepatobiliary Surgery Hospital, Naval Medical University, Shanghai, China.
  • Xie F; Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
  • Shen H; Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
  • Wang D; Jiangxi University of Chinese Medicine, Nanchang, China.
Chem Biol Drug Des ; 104(3): e14623, 2024 Sep.
Article em En | MEDLINE | ID: mdl-39279715
ABSTRACT
Hepatocellular carcinoma (HCC) is a significant global health concern. However, there are limited effective treatments available for it. The use of natural products in the management and treatment of HCC is gaining more attention. Baicalein is a flavonoid compound that has been reported to have antitumor activities in HCC. However, the direct binding targets of baicalein are still unknown. Therefore, we used the DNA-programmed affinity labeling method to identify the target of baicalein and validated its function in HCC cells. We set blank and competitive DNA probes as negative controls. The results showed that baicalein had 136 binding targets, of which 13 targets were differently expressed in HCC tissues. The enriched cellular process of these targets was apoptosis, which involved MAPK9. We tested the binding affinity of baicalein with MAPK9 as 89.7 nM (Kd) by surface plasmon resonance and analyzed the binding sites by virtual docking. Notably, the binding of baicalein with MAPK9 increased the protein levels of MAPK9 itself and the related downstream apoptosis signaling, triggering the apoptosis of HCC cells. However, the inhibitor of MAPK9, SP600125, blocked the baicalein-induced apoptosis, and the amounts of MAPK9 and downstream molecules were also decreased, indicating that baicalein acted through MAPK9 to induce apoptosis of HCC cells. In conclusion, we used the DNA-programmed affinity labeling method to identify the direct-binding target MAPK9 of baicalein and validated its function in baicalein-induced apoptosis of HCC cells, which would be helpful to understand and use baicalein in HCC therapy.
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Texto completo: 1 Coleções: 01-internacional Temas: Geral / Tipos_de_cancer / Outros_tipos Base de dados: MEDLINE Assunto principal: Apoptose / Carcinoma Hepatocelular / Flavanonas / Simulação de Acoplamento Molecular / Neoplasias Hepáticas Limite: Humans Idioma: En Revista: Chem Biol Drug Des Assunto da revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China

Texto completo: 1 Coleções: 01-internacional Temas: Geral / Tipos_de_cancer / Outros_tipos Base de dados: MEDLINE Assunto principal: Apoptose / Carcinoma Hepatocelular / Flavanonas / Simulação de Acoplamento Molecular / Neoplasias Hepáticas Limite: Humans Idioma: En Revista: Chem Biol Drug Des Assunto da revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China