产品说明书

Phloretin

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Chemical Structure| 60-82-2 同义名 : RJC 02792;NSC 407292;Dihydronaringenin
CAS号 : 60-82-2
货号 : A170374
分子式 : C15H14O5
纯度 : 98%
分子量 : 274.269
MDL号 : MFCD00002288
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(182.3 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • SGLT1
描述 Phloretin is a natural flavonoid with various bioactive properties. It inhibits monocarboxylate transporters MCT1 and MCT2 with IC50 values of 28  8µM and 14  2µM, respectively, thereby suppressing the transport of monocarboxylate across the plasma membrane[3]. Phloretin has also been shown to inhibit human concentrative nucleoside transporter 3 (Ki = 32.28µM) and sodium/D-glucose cotransporter (Ki = 86µM)[4]. Phloretin at 10 and 20µM significantly inhibited toll-like receptor 2/1 (TLR2/1) signaling in Raw264.7 cells by downregulating 37.2% and 66.1% of the Pam3CSK4-induced TNF-α production, respectively. In Pam3CSK4-activated HEK293-hTLR2 cells, one-hour pretreatment with phloretin (1 - 20μM) dose-dependently inhibited TNF-α production by 33.3% – 51.1%. Phloretin at 1 - 20μM also decreased the level of IL-8 by 23.2% – 73.4% in these cells. The treatment of Pam3CSK4-activated Raw 264.7 cells with phloretin (20 μM) suppressed the protein level of TLR2 by 75.1% as compared to the controls[5]. Daily administration of phloretin (50 and 100mg/kg) ameliorated collagen-induced arthritis in the hind-limbs of mice and inhibited the production of proinflammatory cytokines in mouse joints[6].
作用机制 Phloretin inhibits TLR2–TLR1 heterodimerization by directly binding to the interface of TLR2 and TLR1 at a shallower position compared to Pam3CSK4[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
H1299 cells Function assay 30 mins Inhibition of GLUT1 in human H1299 cells assessed as inhibition of 2-deoxy-D-[3H]-glucose uptake incubated for 15 mins prior to 2-deoxy-D-[3H]-glucose addition measured after 30 mins by liquid scintillation counting analysis, IC50=21.4 Μm 24200808
PK15NTD cells Function assay Binding affinity to human recombinant CNT3 expressed in pig PK15NTD cells assessed as [3H]uridine uptake by beta-scintillation, Ki=32.28 μM 19097778
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.65mL

0.73mL

0.36mL

18.23mL

3.65mL

1.82mL

36.46mL

7.29mL

3.65mL
参考文献

[1]Idris I, Donnelly R. Sodium-glucose co-transporter-2 inhibitors: an emerging new class of oral antidiabetic drug. Diabetes Obes Metab. 2009 Feb;11(2):79-88.

[2]Chan SS, Lotspeich WD. Comparative effects of phlorizin and phloretin on glucose transport in the cat kidney. Am J Physiol. 1962 Dec;203:975-9.

[3]Bröer S, Bröer A, Schneider HP, Stegen C, Halestrap AP, Deitmer JW. Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes. Biochem J. 1999 Aug 1;341 ( Pt 3)(Pt 3):529-35.

[4]Wielert-Badt S, Lin JT, Lorenz M, Fritz S, Kinne RK. Probing the conformation of the sugar transport inhibitor phlorizin by 2D-NMR, molecular dynamics studies, and pharmacophore analysis. J Med Chem. 2000 May 4;43(9):1692-8.

[5]Kim J, Durai P, Jeon D, Jung ID, Lee SJ, Park YM, Kim Y. Phloretin as a Potent Natural TLR2/1 Inhibitor Suppresses TLR2-Induced Inflammation. Nutrients. 2018 Jul 5;10(7):868.

[6]Wang SP, Lin SC, Li S, Chao YH, Hwang GY, Lin CC. Potent Antiarthritic Properties of Phloretin in Murine Collagen-Induced Arthritis. Evid Based Complement Alternat Med. 2016;2016:9831263.