Curcumin-3,4-Dichloro Phenyl Pyrazole (CDPP) overcomes curcumin's low bioavailability, inhibits adipogenesis and ameliorates dyslipidemia by activating reverse cholesterol transport
| Autor: | Kripa Shankar, Abhishek Gupta, Durgesh Kumar, Narender Tadigoppula, Sujith Rajan, Anil N. Gaikwad, R. J. Choudhary, Pragya Yadav, Vishal M. Balaramnavar, Rabi Sankar Bhatta, Salil Varshney, Ankita Srivastava, Vinay Kumar Singh, Muheeb Beg, Santosh Kumar |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
medicine.medical_specialty Curcumin Cell cycle checkpoint Endocrinology Diabetes and Metabolism Biological Availability Biological Transport Active Mice 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Endocrinology Pharmacokinetics Cricetinae Adipocyte Internal medicine medicine Animals Dyslipidemias Adipogenesis Mesocricetus Reverse cholesterol transport 3T3 Cells Cell Cycle Checkpoints medicine.disease Bioavailability Cholesterol 030104 developmental biology chemistry 030220 oncology & carcinogenesis Pyrazoles Dyslipidemia |
| Zdroj: | Metabolism. 73:109-124 |
| ISSN: | 0026-0495 |
| Popis: | Background Adipocyte dysfunction, obesity and associated metabolic disorders are of prime healthcare concern worldwide. Among available medications, natural products and inspired molecules hold 40% space in clinically prescribed medicines. In queue, this study overcomes the drawback of curcumin's low bioavailability with potent anti-adipogenic and anti-dyslipidemic activity. Methods To evaluate the role of CDPP on adipocyte differentiation, 3T3-L1 adipocytes were used as an in-vitro model. Flow cytometry was performed for cell cycle analysis. Syrian golden hamsters were used to study pharmacokinetic profile and dyslipidemic activity exhibited by CDPP. Result CDPP was found to be a potent inhibitor of adipogenesis in-vitro. It blocked mitotic clonal expansion by causing cell cycle arrest. CDPP showed marked improvement in gastrointestinal stability and bioavailability in-vivo as compared to curcumin. Administration of CDPP (100 mg/kg) significantly improved HFD induced dyslipidemic profile in hamsters and activated reverse cholesterol transport machinery. Conclusion CDPP could be used as a potential drug candidate against adipogenesis and dyslipidemia with enhanced gastrointestinal stability and bioavailability. |
| Databáze: | OpenAIRE |
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