Phloretin (Synonyms:根皮素; NSC 407292; RJC 02792)
目录号 : KM17695 CAS No. : 60-82-2 纯度 : 98%

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。

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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.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation.

体外研究

Phloretin induced obvious cytotoxicity against BEL-7402 cells with IC50 of 89.23 μM.
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.

Apoptosis Analysis

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

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

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

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.

Animal Model: Collagen-Induced Arthritis (CIA) Mice
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.
分子式
C15H14O5
分子量
274.27
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。

  • 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。

  • 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。

科研文献
The molarity calculator equation
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