GLPBio

Hydroxy-α-sanshool

Catalog No.: GC36277Purity:>98.00%
COASDSData Sheet
Hydroxy-α-sanshool is a transient receptor potential base 1 (TRPA1) and TRP vanilloid 1 (TRPV1) agonist with EC50 values of 69 and 1.1µM, respectively, commonly used in hyperlipidemia studies.

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Hydroxy-α-sanshool
Cas No.: 83883-10-7
10mM (in 1mL DMSO)In Stock
$248.00
1
5mgIn Stock
$225.00
1
10mgIn Stock
$360.00
1
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Description

Hydroxy-α-sanshool is a transient receptor potential base 1 (TRPA1) and TRP vanilloid 1 (TRPV1) agonist with EC50 values of 69 and 1.1µM, respectively, commonly used in hyperlipidemia studies[1].

In HaCaT cells, Hydroxy-α-sanshool (10-40μM; 24h) effectively inhibited intracellular ROS production induced by C. acnes.10μM of Hydroxy-α-sanshool significantly reduced ROS levels in THP-1 cells[2]. Hydroxy-α-sanshool showed a significant protective effect on H2O2-stimulated PC12 cells without significant cytotoxicity against normal PC12 cells. Hydroxy-α-sanshool also reduced H2O2-induced apoptosis of PC12 cells by decreasing intracellular ROS and increasing mitochondrial membrane potential (MMP)[3].

Hydroxy-α-sanshool (0.5, 1.25, 2.5, 5mg/kg; po) reduces blood glucose in the T2DM mouse model by regulating glycogen metabolism through a mechanism involving the regulation of the PI3K/Akt/GSK3β/GS signaling pathway[4]. In the insulin resistance model, the Hydroxy-α-sanshool (8mg/kg) intervention lowered serum total cholesterol and LDL cholesterol and significantly reduced triacylglycerol[5].

References:
[1]. Riera C E, Menozzi‐Smarrito C, Affolter M, et al. Compounds from Sichuan and Melegueta peppers activate, covalently and non‐covalently, TRPA1 and TRPV1 channels[J]. British journal of pharmacology, 2009, 157(8): 1398-1409.
[2]. Zhou X, Su Y, Wang H, et al. Hydroxy-α-sanshool has anti-inflammatory and antioxidant effects and affects the NF-κB/STAT3 pathway via TRPV1 in acne[J]. Journal of Functional Foods, 2023, 110: 105823.
[3]. Li R L, Zhang Q, Liu J, et al. Hydroxy‐α‐sanshool Possesses Protective Potentials on H2O2‐Stimulated PC12 Cells by Suppression of Oxidative Stress‐Induced Apoptosis through Regulation of PI3K/Akt Signal Pathway[J]. Oxidative Medicine and Cellular Longevity, 2020, 2020(1): 3481758.
[4]. Zhang Q, Li R L, Wang L Y, et al. Hydroxy-α-sanshool isolated from Zanthoxylum bungeanum Maxim. has antidiabetic effects on high-fat-fed and streptozotocin-treated mice via increasing glycogen synthesis by regulation of PI3K/Akt/GSK-3β/GS signaling[J]. Frontiers in Pharmacology, 2022, 13: 1089558.
[5]. Xu F, Zhu Y, Lu M, et al. Effects of hydroxy-alpha-sanshool on intestinal metabolism in insulin-resistant mice[J]. Foods, 2022, 11(14): 2040.

Protocol

Cell experiment [1]:

Cell lines

PC12 cells

Preparation Method

PC12 cells were pretreated with different concentrations of Hydroxy-α-sanshool (15, 30, and 60μM) for 2 hours and then incubated with 90μM H2O2 for another 4 hours. The control group was administered with the same amount of 1640 medium and then stimulated with H2O2. Hydroxy-α-sanshool was solubilized with DMSO and subsequently diluted in culture medium with the final concentration of DMSO less than 0.1% (v/v).

Reaction Conditions

15, 30, 60μM; 2h

Applications

Hydroxy-α-sanshool showed a significant protective effect on H2O2-stimulated PC12 cells without significant cytotoxicity against normal PC12 cells. Hydroxy-α-sanshool also reduced H2O2-induced apoptosis of PC12 cells by decreasing intracellular ROS and increasing mitochondrial membrane potential (MMP).
Animal experiment [2]:

Animal models

Type 2 diabetic mouse model (T2DM)

Preparation Method

Male C57BL/6J mice were prepared as a model of T2DM. The mice were randomly divided into five groups, including HFD/STZ (HFD feeding plus STZ treatment), HFD/STZ+Metformin (Met 150mg/kg), HFD/STZ+Hydroxy-α-sanshool -L (HAS 1.25mg/kg), HFD/STZ+HAS-M (Hydroxy-α-sanshool 2.5mg/kg), and HFD/STZ+Hydroxy-α-sanshool-H (Hydroxy-α-sanshool 5mg/kg). Subsequently, Hydroxy-α-sanshool was dissolved in 0.5% CMC-Na, and mice in the NC+Hydroxy-α-sanshool (5mg/kg) and HFD/STZ+Hydroxy-α-sanshool (1.25, 2.5, 5mg/kg) groups were administered Hydroxy-α-sanshool orally at doses of 5mg/kg, 1.25mg/kg, 2.5mg/kg, or 5mg/kg for 4 weeks, respectively. The positive control treatment used in this study was Met, which was administered daily by gavage at 150mg/kg. The mice in the NC and HFD/STZ groups received vehicle solvent. During the experiment, changes in blood glucose, body weight, feed intake, and water intake were recorded.

Dosage form

0.5, 1.25, 2.5, 5mg/kg; po; 4 weeks

Applications

Hydroxy-α-sanshool reduces blood glucose in the T2DM mouse model by regulating glycogen metabolism through a mechanism involving the regulation of the PI3K/Akt/GSK3β/GS signaling pathway.

References:
[1]. Li R L, Zhang Q, Liu J, et al. Hydroxy‐α‐sanshool Possesses Protective Potentials on H2O2‐Stimulated PC12 Cells by Suppression of Oxidative Stress‐Induced Apoptosis through Regulation of PI3K/Akt Signal Pathway[J]. Oxidative Medicine and Cellular Longevity, 2020, 2020(1): 3481758.
[2].Zhang Q, Li R L, Wang L Y, et al. Hydroxy-α-sanshool isolated from Zanthoxylum bungeanum Maxim. has antidiabetic effects on high-fat-fed and streptozotocin-treated mice via increasing glycogen synthesis by regulation of PI3K/Akt/GSK-3β/GS signaling[J]. Frontiers in Pharmacology, 2022, 13: 1089558.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
83883-10-7
SMILES
C/C=C/C=C/C=C\CC/C=C/C(NCC(C)(O)C)=O
Molecular Formula
C16H25NO2
Molecular Weight
263.38
Solubility
DMSO : 100 mg/mL (379.68 mM; Need ultrasonic)
Storage
Store at -20°C,protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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