| MDL | MFCD20527284 |
|---|---|
| Molecular Weight | 682.75 |
| Molecular Formula | C37H46O12 |
| SMILES | CC[C@H](C)C(C1=C(O)C(CC2=C(O)C(C(CCC)=O)=C(OC)C(C)=C2O)=C(O)C(CC3=C(O)C(C(CCC)=O)=C(OC)C(C)=C3O)=C1O)=O |
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 [1] [2] [3] .
|
SIRT1 |
PPARγ |
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
[1]
.
Agrimol B induces SIRT1 (silent information regulator 2 homolog 1) translocation and expression in 3T3-L1 adipocytes
[1]
.
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
[2]
.
Agrimol B (0-76 μM) dose-dependently increases cells at G0 in both cell lines
[2]
.
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)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis [2]
| Cell 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 Analysis [2]
| Cell 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. |
Immunofluorescence [1]
| Cell 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. |
Agrimol B (10 mg/kg, Orally, daily) reduces growth of prostate cancer cell xenograft in mice [2] .
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) [2] |
| 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. |
Solid
Room temperature in continental US; may vary elsewhere.
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
DMSO : 8.33 mg/mL ( 12.20 mM ; Need ultrasonic)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4647 mL | 7.3233 mL | 14.6467 mL |
| 5 mM | 0.2929 mL | 1.4647 mL | 2.9293 mL |
| 10 mM | 0.1465 mL | 0.7323 mL | 1.4647 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.43 mg/mL (2.09 mM); Clear solution