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European journal of medicinal chemistry v.143, 2018년, pp.780 - 791   SCI SCIE
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Aegeline inspired synthesis of novel amino alcohol and thiazolidinedione hybrids with antiadipogenic activity in 3T3-L1 cells

Satish, Sabbu (Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, India ) ; Srivastava, Ankita (Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow 226031, India ) ; Yadav, Pragya (Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, India ) ; Varshney, Salil (Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow 226031, India ) ; Choudhary, Rakhi (Global Institute of Pharmaceutical Education and Research, Jaspur Road, Kashipur, Uttarakhand, India ) ; Balaramnavar, Vishal M. (Global Institute of Pharmaceutical Education and Research, Jaspur Road, Kashipur, Uttarakhand, India ) ; Narender, Tadigoppula (Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, India ) ; Gaikwad, Anil Nilkanth (Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow 226031, India ) ;
  • 초록  

    Abstract Excess adiposity is a hallmark of obesity, which is caused due to an imbalance between energy intake and energy consumed. Obesity is often associated with several metabolic disorders like dyslipidemia, cardiovascular diseases and type 2 diabetes. Earlier, our group had reported natural product Aegeline (amino-alcohol) isolated from the plant Aegle marmelos as an anti-diabetic and anti-dyslipidemic compound. With this background, we synthesized a series of novel amino alcohol and thiazolidinedione hybrid molecules and studied their antiadipogenic activity. As a result, we have identified a potent hybrid compound 12c as an inhibitor of adipocyte differentiation. The compound 12c inhibits lipid accumulation and adipogenesis in 3T3-L1 preadipocyte cell line. Exposure of compound 12c blocks mitotic clonal expansion and arrests cells in S-phase of cell cycle. Detailed analysis showed that compound 12c decreases expression of two major transcription factors that are involved in adipocyte differentiation, PPARγ, C/EBPα, and other adipogenesis associated genes like aP2 and FAS. Thus, we concluded that compound 12c shows potential ability to inhibit adipocyte differentiation which can be used therapeutically for the treatment of obesity and its associated metabolic disorders. Highlights Compound 12c , a hybrid molecule of amino alcohol and thiazolidinedione is a potential anti-adipogenic compound. Compound 12c inhibit adipogenesis in 3T3-L1 adipocyte. Compound 12c inhibit mitotic clonal expansion by arresting cell cycle in S-phase. Compound 12c provide a therapeutic target for the treatment of obesity. Graphical abstract [DISPLAY OMISSION]


  • 주제어

    Obesity .   Adipogenesis .   Thiazolidinedione .   β-amino alcohols .   PPARγ.  

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