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Design and Synthesis of Novel Indole Ethylamine Derivatives as a Lipid Metabolism Regulator Targeting PPARα/CPT1 in AML12 Cells.
Liu, Yu-Chen; Wei, Gang; Liao, Zhi-Qiang; Wang, Fang-Xin; Zong, Chunxiao; Qiu, Jiannan; Le, Yifei; Yu, Zhi-Ling; Yang, Seo Young; Wang, Heng-Shan; Dou, Xiao-Bing; Wang, Cai-Yi.
Afiliación
  • Liu YC; College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053, China.
  • Wei G; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources/Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences, Collaborative Innovation Center for Guangxi Ethnic Medi
  • Liao ZQ; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources/Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences, Collaborative Innovation Center for Guangxi Ethnic Medi
  • Wang FX; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources/Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences, Collaborative Innovation Center for Guangxi Ethnic Medi
  • Zong C; College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053, China.
  • Qiu J; College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053, China.
  • Le Y; College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053, China.
  • Yu ZL; School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China.
  • Yang SY; Department of Biology Education, Teachers College and Institute for Phylogenomics and Evolution, Kyungpook National University, Daegu 41566, Republic of Korea.
  • Wang HS; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources/Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences, Collaborative Innovation Center for Guangxi Ethnic Medi
  • Dou XB; College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053, China.
  • Wang CY; College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053, China.
Molecules ; 29(1)2023 Dec 19.
Article en En | MEDLINE | ID: mdl-38202597
ABSTRACT
Peroxisome proliferator-activated receptor alpha (PPARα) and carnitine palmitoyltransferase 1 (CPT1) are important targets of lipid metabolism regulation for nonalcoholic fatty liver disease (NAFLD) therapy. In the present study, a set of novel indole ethylamine derivatives (4, 5, 8, 9) were designed and synthesized. The target product (compound 9) can effectively activate PPARα and CPT1a. Consistently, in vitro assays demonstrated its impact on the lipid accumulation of oleic acid (OA)-induced AML12 cells. Compared with AML12 cells treated only with OA, supplementation with 5, 10, and 20 µM of compound 9 reduced the levels of intracellular triglyceride (by 28.07%, 37.55%, and 51.33%) with greater inhibitory activity relative to the commercial PPARα agonist fenofibrate. Moreover, the compound 9 supplementations upregulated the expression of hormone-sensitive triglyceride lipase (HSL) and adipose triglyceride lipase (ATGL) and upregulated the phosphorylation of acetyl-CoA carboxylase (ACC) related to fatty acid oxidation and lipogenesis. This dual-target compound with lipid metabolism regulatory efficacy may represent a promising type of drug lead for NAFLD therapy.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antipsicóticos / Enfermedad del Hígado Graso no Alcohólico Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antipsicóticos / Enfermedad del Hígado Graso no Alcohólico Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Suiza