Agrimol B

Agrimol B, a polyphenol, is an orally active and potent SIRT1 activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ , C/EBPα , FAS , UCP-1 , and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC , SKP2 and p27 In Vitro Agrimol B blocks adipogenesis at the early stage of differentiation in a dose-dependent manner, with an IC 50 of 3.35 ± 0.32 μM. Agrimol B induces SIRT1 (silent information regulator 2 homolog 1) translocation and expression in 3T3-L1 adipocytes. Agrimol B inhibits PC-3 and A549 cells growth, with GI50 (growth inhibition 50%) values of 29 and 19 μM, GI75 values of 49 and 50 μM, and GI90 values of 63 and 76 μM, respectively. Agrimol B (0-76 μM) dose-dependently increases cells at G0 in both cell lines. Agrimol B (0-76 μM, 3 days) reduces the protein expression of c-MYC and SKP2 (S-phase kinase-associated protein 2), increases p27 (cyclin-dependent kinase inhibitor 1B), and down-regulates SPT16 (Suppressor of Ty Homolog-16) and SSRP1 (Structure-Specific Recognition Protein 1). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: PC-3 and A549 cells Concentration: 29 and 63 μM (PC-3), 19 and 76 μM (A549) Incubation Time: 10 min Result: Dose-dependently increased cells at G0 in both cell lines. Reduced percentage of cells positive for Ki-67, and increased p27 positive cell population in PC-3 and A549 cells. Western Blot AnalysisCell Line: PC-3 and A549 cells Concentration: 0, 29, 49, 63 μM (PC-3); 0, 19, 50, and 76 μM (A549) Incubation Time: 3 days Result: Reduced c-MYC, SKP2 and increased p27 in both cell lines, and down-regulated SPT16 and SSRP1 in A549 cells with no effect on CRM1 in both cell lines. ImmunofluorescenceCell Line: 3T3-L1 preadipocyte Concentration: 0, 3, and 10 μM Incubation Time: 6 days Result: Significantly increased nuclear positive rate of SIRT1; Markedly increased SIRT1 expression at 10 μM, the effect vanished at 3 μM. Down-regulated PPARγ and C/EBPα (CCAAT/enhancer-binding protein α) expression; Significantly decreased FAS (fatty acid synthesis), UCP-1 (uncoupling protein-1), and apoE (apolipoprotein E) expression at 10 μM. In Vivo Agrimol B (10 mg/kg, Orally, daily) reduces growth of prostate cancer cell xenograft in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude mice (6-week-old, male, injected with PC-3 cells in 0.2 mL PBS subcutaneously)Dosage: 10 mg/kg Administration: Orally, daily, after 15 days of cancer cell implantation Result: Inhibited tumor growth in a mouse model of human prostate cancer, reduced the tumor volume at day 31 and day 32. Form:Solid IC50& Target:SIRT1 PPARγ

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