Back to Search
Start Over
Curcumin-3,4-Dichloro Phenyl Pyrazole (CDPP) overcomes curcumin's low bioavailability, inhibits adipogenesis and ameliorates dyslipidemia by activating reverse cholesterol transport
- Source :
- Metabolism. 73:109-124
- Publication Year :
- 2017
- Publisher :
- Elsevier BV, 2017.
-
Abstract
- 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.
- Subjects :
- 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
Subjects
Details
- ISSN :
- 00260495
- Volume :
- 73
- Database :
- OpenAIRE
- Journal :
- Metabolism
- Accession number :
- edsair.doi.dedup.....685a0a7c9aca439ada5fa8c40cffdcad
- Full Text :
- https://doi.org/10.1016/j.metabol.2017.05.005