Curcumin-3,4-Dichloro Phenyl Pyrazole (CDPP) overcomes curcumin's low bioavailability,inhibits adipogenesis and ameliorates dyslipidemia by activating reverse cholesterol transport |
| |
| Institution: | 1. Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow 226031, India;2. Academy of Scientific and Innovative Research, New Delhi 110025, India;3. Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, India;4. Division of Pharmacokinetics, CSIR-Central Drug Research Institute, Lucknow 226031, India;5. Global Institute of Pharmaceutical Education and Research, Jaspur Road, Kashipur 244713, India;1. Department of Endocrinology, 424 General Military Hospital, Thessaloniki, Greece;2. Department of Cardiology, 424 General Military Hospital, Thessaloniki, Greece;3. Department of Cardiology, Skaraborg Hospital, Skovde, Sweden;4. Department of Medicine, Aristotle University of Thessaloniki, Thessaloniki, Greece;5. Division of Endocrinology, Diabetes and Metabolism, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA, USA;6. Department of Hygiene and Epidemiology, School of Medicine, Aristotle University of Thessaloniki, Thessaloniki, Greece;7. Department of Pharmacology, 424 General Military Hospital, Thessaloniki, Greece;1. Department of Endocrinology and Metabolism, The Second Affiliated Hospital of Guilin Medical University, Guilin, Guangxi, PR China;2. Department of Human Anatomy, Southwest Medical University, Luzhou, Sichuan, PR China;3. Center of Diabetic Systems Medicine, Guilin Medical University, Guilin, Guangxi, PR China;4. Department of Laboratory Medicine, The Second Affiliated Hospital of Guilin Medical University, Guilin, Guangxi, PR China;5. Department of Epidemiology and Health Statistics, Guilin Medical University, Guilin, Guangxi, China;1. Nutritional Epidemiology Institute and School of Public Health, Tianjin Medical University, Tianjin, China;2. Tianjin University of Traditional Chinese Medicine, Tianjin, China;3. Health Management Centre, Tianjin Medical University General Hospital, Tianjin, China;1. Center for Biomedical Science, Korea National Institute of Health, Cheongju, Chungcheongbuk-do, Republic of Korea;2. Department of Family Medicine, Obesity Research Institute, Seoul-Paik Hospital, Inje University, Seoul 100-032, Republic of Korea;3. Department of Family Medicine, Hallym University Sacred Heart Hospital, Hallym University, Anyang, Gyeonggi-do 431-796, Republic of Korea |
| |
| Abstract: | BackgroundAdipocyte 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.MethodsTo 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.ResultCDPP 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.ConclusionCDPP could be used as a potential drug candidate against adipogenesis and dyslipidemia with enhanced gastrointestinal stability and bioavailability. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
