Agrimol B 是一种多酚，是一种口服有效的SIRT1激活剂。Agrimol B 具有抗成脂 (anti-adipogenic) 和抗肿瘤 (anticancer) 活性。Agrimol B 对植物病原菌具有抗菌 (antibacterial) 活性。Agrimol B 通过降低PPARγ、C/EBPα、FAS、UCP-1和apoE表达，显著抑制 3T3-L1 脂肪细胞分化。Agrimol B 对癌细胞的作用可能源于其对c-MYC、SKP2和p27的作用。
| 生物活性 | Agrimol B, a polyphenol, is an orally active and potentSIRT1activator. Agrimol B showsanti-adipogenicandanticanceractivity. Agrimol B showsantibacterialactivity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducingPPARγ,C/EBPα,FAS,UCP-1, andapoEexpression. The action of Agrimol B on thecancercells is likely derived from its effect onc-MYC,SKP2andp27[1][2][3]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Agrimol B blocks adipogenesis at the early stage of differentiation in a dose-dependent manner, with an IC50of 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].
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. |
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体内研究
(In Vivo) | Agrimol B (10 mg/kg, Orally, daily) reduces growth of prostate cancer cell xenograft in mice[2].
| 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. |
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| 来源 | - Plants
- Rosaceae
- Agrimonia pilosaLedeb.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 8.33 mg/mL(12.20 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.43 mg/mL (2.09 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (2.09 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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