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Background: Ponciri Fructus, a crude drug consisting of the dried immature fruits of (L.) Raf., is a popular folk medicine used for the treatment of allergy and gastrointestinal disorders in Korea and China. In this study, the anti-adipogenic activity of extracts and isolated compounds were evaluated using 3T3-L1 preadipocytes.
Methods: Dried immature fruits were extracted and fractionated into -hexane, ethyl acetate (EtOAc), -butanol and water-soluble fractions. The ethanol extract and fractions were tested for anti-adipogenic activity in the 3T3-L1 cell line. The active fractions (-hexane and EtOAc fractions) were further subjected to chromatographic techniques to isolate and identify active compounds. Furthermore, the isolated compounds were evaluated for their anti-adipogenic activity.
Results: Altogether, seven compounds, including two flavonoids, one phytosteroid and four coumarin derivatives, were isolated. Ethanol extract, -hexane fraction, EtOAc fraction and three isolated compounds (phellopterin, oxypeucedanin and poncirin) showed significant anti-adipogenic activity as observed by reduced lipid deposition in differentiated 3T3-L1 cells. Further, oxypeucedanin downregulated the key adipogenic markers, such as peroxisome proliferator-activated receptors proteins (PPAR-), sterol response element binding proteins-1 (SREBP-1), CCAAT/enhancer binding proteins- (C/EBP-), adipocyte-specific lipid binding proteins (FABP-4), adipocyte fatty acid binding proteins (aP2), lipoprotein lipase (LPL) and leptin.
Conclusion: This study indicated that the ethanol extract, hexane fraction and ethyl acetate fraction of fruits possess strong anti-adipogenic activity, containing the active compounds such as phellopterin, oxypeucedanin and poncirin. Further research is recommended to explore their efficacy and safety in animal and clinical models.
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http://dx.doi.org/10.3390/molecules27030676 | DOI Listing |
Front Pharmacol
August 2025
Hunan Provincial Key Laboratory of the Research and Development of Novel Pharmaceutical Preparations, "The 14th Five-Year Plan" Application Characteristic Discipline of Hunan Province (Pharmaceutical Science), College of Pharmacy, Changsha Medical University, Changsha, Hunan, China.
Introduction: Obesity is characterized by excessive fat accumulation resulting from adipocyte hypertrophy and hyperplasia, with adipocyte differentiation being a central process driving these changes.
Methods: The anti-adipogenic effects of CRT0066101 (CRT), a pan-protein kinase D (PKD) inhibitor, were evaluated in 3T3-L1 adipocytes. Potential drug targets of CRT were predicted using network pharmacology analysis.
Tissue Cell
August 2025
Major of Human Bio-convergence, Division of Smart Healthcare, Pukyong National University, Busan 48513, Republic of Korea. Electronic address:
Curcumin, a hydrophobic polyphenol derived from turmeric, exhibits diverse biological activities as a natural supplement. However, its low gastrointestinal absorption significantly limits its oral bioavailability. In this study, we investigated the effects of curcumin-loaded nanospheres (CN) on adipocyte differentiation in 3T3-L1 cells and obesity development in high-fat diet-induced obese mice.
View Article and Find Full Text PDFBioorg Chem
August 2025
Department of Biopharmaceutical Convergence, School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea; School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea. Electronic address:
Type 2 diabetes mellitus (T2DM) remains a major metabolic disorder requiring the development of novel therapeutics. GPR120, a G-protein-coupled receptor involved in metabolic regulation, has emerged as a promising target; however, potent agonists are still scarce, underscoring the need for new candidates. In this study, we designed and synthesized a series of flavone and isoflavone derivatives to identify potent GPR120 agonists.
View Article and Find Full Text PDFRegen Ther
December 2025
Department of Orthopedics, XianJu People's Hospital, Zhejiang Southeast Campus of Zhejiang Provincial People's Hospital, Affiliated Xianju's Hospital, Hangzhou Medical College, Xianju, Zhejiang, 317399, China.
Background: Fibro-adipogenic progenitors (FAPs) contribute to excessive muscular fatty infiltration after rotator cuff tears (RCT), impairing shoulder function. Tanshinone IIA (Tan IIA), a major active compound from Salvia miltiorrhiza Bunge, has known anti-adipogenic effects, yet its impact on FAP adipogenesis remains unclear.
Methods: Human FAPs from rotator cuff muscles were isolated via FACS, cultured, and treated with Tan IIA.
Front Pharmacol
July 2025
Therapeutics and Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
Background: Dual-specificity tyrosine phosphorylation-regulated kinase 1B (DYRK1B) is implicated in metabolic diseases, with high expression linked to adipocyte differentiation and metabolic disorders. This study investigated the anti-adipogenic and anti-diabetic effects of a novel selective DYRK1B inhibitor, N-(4-(3-(4-methoxyphenyl)-1H-pyrazolo [3,4-b]pyridin-5-yl) phenyl)acetamide (KS-40070).
Methods: The efficacy of KS-40070 was evaluated using 3T3-L1 cells, adipose-derived mesenchymal stem cells (ADMSC), and diet-induced obesity (DIO) mice.