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Phloretin (NSC 407292; RJC 02792) is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively.
Phloretin (40-160 μM; 24 hours) induces BEL-7402 cell apoptosis though the mitochondrial pathway, the cells exposed to phloretin exhibits nuclear chromatin condensation and increased fluorescence intensity. The caspase-9 reaches the peak level at 12 h, and leak levels of caspase-6 and caspase-3 activities occurrs 18 and 24 h after the exposure, respectively. Phloretin (0-100 μM; 24 hours) has effects on transcription factors of adipogenesis in differentiated 3T3-L1 adipocytes, decreases PPAR-γ, C/EBPα and C/EBPβ as a dose-dependent manner. Phloretin (0-100 μM; 24 hours) has effects on the AMPK pathway in differentiated 3T3-L1 adipocytes, increases the phosphorylation of substrate ACC-1, AMPK in PT-treated cells.
Phloretin (50 or 100 mg/kg; oral administration; once daily) decreases oxidative stress and diminished levels of malondialdehyde (MDA) and hydrogen peroxide (H2O2) in paw tissue, reduces productivity of anti-collagen antibodies in serum.
| Cell Experiment | |
|---|---|
| Cell lines | COLO205, HT-29, and FHC cells |
| Preparation method | Flow cytometry (FACS) analysis of DNA was conducted after COLO205, HT-29, and FHC cells were synchronized by 0.04% FCS for 24 h and then switched to culture media supplemented with 10% FBS containing 0.05% DMSO (control) or Ph (100–200 μM in 0.05% DMSO) for an additional 16 h.Flow cytometry chart of all these cells. |
| Concentrations | 100–200 μM |
| Incubation time | 16 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 male mice |
| Formulation | DMSO |
| Dosages | 10 mg/kg |
| Administration | i.p. |
| Molecular Weight | 274.27 |
| Formula | C15H14O5 |
| CAS Number | 60-82-2 |
| Solubility (25°C) | DMSO 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Talita Pizza Anunciato Casarini, et al. Dermatological applications of the flavonoid phloretin
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