Phloretin(Synonyms: 根皮素; NSC 407292; RJC 02792)

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Phloretin (Synonyms: 根皮素; NSC 407292; RJC 02792) 纯度: 99.78%

Phloretin (NSC 407292; RJC 02792) 是一种从夏枯草中提取的黄酮类化合物,具有抗炎活性。Phloridzin 是一种特异性、竞争性和口服活性的钠/葡萄糖协同转运蛋白 (sodium/glucose cotransporters) 抑制剂,在肠道 (SGLT1) 和肾脏 (SGLT2)。Phloretin 抑制 Yeast-made GLUT1 以及人类红细胞 GLUT1 的 IC50 值分别为 49 μM 和 61 μM。Phloretin 具有潜力用于类风湿性关节炎 (RA) 和过敏性气道炎症的相关研究。

Phloretin(Synonyms: 根皮素; NSC 407292;  RJC 02792)

Phloretin Chemical Structure

CAS No. : 60-82-2

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生物活性

Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Prunus mandshurica, has anti-inflammatory activities. Phloridzin 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[1].Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation[4].

IC50 & Target

Human Endogenous Metabolite

 

GLUT1

 

GLUT2

 

体外研究
(In Vitro)

Phloretin induced obvious cytotoxicity against BEL-7402 cells with IC50 of 89.23 μM[2].
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[2].
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[3].
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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: BEL-7402 cell
Concentration: 40-160 μM
Incubation Time: 24 hours
Result: Induced cell apoptosis and activated caspase 3, 6 and 9.

Western Blot Analysis[3]

Cell Line: 3T3-L1 adipocytes
Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 24 hours
Result: Inhibited PPAR-γ, C/EBPα and C/EBPβ expression.

Western Blot Analysis[3]

Cell Line: 3T3-L1 adipocytes
Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 24 hours
Result: Upregulated the expression of p-ACC-1, p-AMPK, p-AMPKα and β .

体内研究
(In Vivo)

Phloretin (oral administration; 50 or 100 mg/kg; 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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Collagen-Induced Arthritis (CIA) Mice[3]
Dosage: 50 or 100 mg/kg
Administration: Oral adminstration
Result: Showed mitigation of clinical symptoms of RA in addition to reduced inflammation of hind-limbs compared to the control group.

分子量

274.27

Formula

C15H14O5

CAS 号

60-82-2

中文名称

根皮素

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
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (182.30 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6460 mL 18.2302 mL 36.4604 mL
5 mM 0.7292 mL 3.6460 mL 7.2921 mL
10 mM 0.3646 mL 1.8230 mL 3.6460 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.12 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 25.0 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Kasahara T, Kasahara M. Expression of the rat GLUT1 glucose transporter in the yeast Saccharomyces cerevisiae. Biochem J. 1996 Apr 1;315 ( Pt 1):177-82.

    [2]. Luo H, et al. Phloretin induces apoptosis of BEL-7402 cells in vitro. Nan Fang Yi Ke Da Xue Xue Bao. 2008 Jul;28(7):1249-51.

    [3]. Huang WC, et al. Phloretin and phlorizin promote lipolysis and inhibit inflammation in mouse 3T3-L1 cells and in macrophage-adipocyte co-cultures.Mol Nutr Food Res. 2013 Oct;57(10):1803-13.

    [4]. Wang SP, et al. Potent Antiarthritic Properties of Phloretin in Murine Collagen-Induced Arthritis.Evid Based Complement Alternat Med. 2016;2016:9831263.

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