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(-)-Asarinin is a tetrahydrofurofurano lignan with various biological activities. (-)-Asarinin induces apoptosis in cancer cells. (-)-Asarinin promotes mitochondrial ROS accumulation, inhibits the STAT3 signaling pathway and induces apoptosis in precancerous cells. (-)-Asarinin is a Src family kinase inhibitor that suppresses mast cell activation. (-)-Asarinin is a non-competitive Δ5-desaturase inhibitor with a Ki of 0.28 mM. (-)-Asarinin possesses pain relief, anti-viral, anti-allergic and anti-tuberculous bacilli, and anti-tumor effects.
For research use only. We do not sell to patients.
(-)-Asarinin is a tetrahydrofurofurano lignan with various biological activities. (-)-Asarinin induces apoptosis in cancer cells. (-)-Asarinin promotes mitochondrial ROS accumulation, inhibits the STAT3 signaling pathway and induces apoptosis in precancerous cells. (-)-Asarinin is a Src family kinase inhibitor that suppresses mast cell activation. (-)-Asarinin is a non-competitive Δ5-desaturase inhibitor with a Ki of 0.28 mM. (-)-Asarinin possesses pain relief, anti-viral, anti-allergic and anti-tuberculous bacilli, and anti-tumor effects[1][2][3][4].
In Vitro
(-)-Asarinin (20-140 μM; 24-48 h) significantly inhibits the viability of MC cells, a human gastric precancerous lesion cell line, in a dose-dependent manner with an IC50 value of 140 μM, while having no significant inhibitory effect on the viability of normal gastric epithelial cells GES-1[1].
(-)-Asarinin (80-140 μM; 24-48 h) inhibits the clonogenic ability of MC cells. (-)-Asarinin significantly reduces the migration and invasion abilities of MC cells[1].
(-)-Asarinin (80-140 μM; 24 h) significantly induces apoptosis and induces G0/G1 phase arrest in MC cells. (-)-Asarinin downregulates the expression of cell cycle-related proteins cyclin E1 and cyclin E2 and upregulates the expression of apoptosis - related proteins cleaved caspase 3 and cleaved PARP in MC cells[1].
(-)-Asarinin (80-140 μM; 24 h) causes mitochondrial damage, reduces mitochondrial membrane potential, decreases ATP production, and increases mitochondrial ROS accumulation in MC cells[1].
(-)-Asarinin (80-140 μM;) inhibits the expression of STAT3-pathway-related proteins p-STAT3, Bcl-2, and cyclin D1 in MC cells in the STAT3 pathway-related experiments[1].
(-)-Asarinin (0-90 μM; 48h) induces apoptotic cell death and activates caspase-3, caspase-8, and caspase-9 in human ovarian cancer cells (A2780 and SKOV3)[2].
(-)-Asarinin (25 μM; for 30 min) significantly reduces the calcium flux in sensitized LAD2 cells in the calcium mobilization assay[3].
(-)-Asarinin (50 μM; for 20 min) significantly inhibits the release of β - hexosaminidase in sensitized LAD2 cells in the β-hexosaminidase release assay, with an IC50 value of 35.26 μM[3].
(-)-Asarinin (50 μM; for 20 min) significantly inhibits the release of histamine in sensitized LAD2 cells in the histamine release assay[3].
(-)-Asarinin significantly reduces the concentrations of TNF- α, MCP-1, IL-4, and IL-5 in sensitized LAD2 cells in the cytokine release assay[3].
(-)-Asarinin (100 μM; 6 h) inhibits the phosphorylation of Src family kinases such as Lyn and Fyn and downregulates the phosphorylation levels of downstream signals such as PLC-γ1, p38α, and Akt in LAD2 cells in the phosphorylated kinase analysis experiment[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
At 80 μM, significantly inhibited the migration and invasion of MC cells. At 140 μM, not only significantly inhibited the migration and invasion but also induced apoptosis.
Induced G0/G1 phase arrest, downregulated the expression of cyclin E1 and cyclin E2, and upregulated the expression of cleaved caspase 3 and cleaved PARP.
Increased the fractionation of nuclei accumulated at Sub G1 in A2780 and SKOV3 cells, but did not induce cell cycle arrest.
Induced apoptotic cell death.
Activated caspase-3, caspase-8, and caspase-9.
Inhibited the phosphorylation of Lyn, Fyn and other Src family kinases, and downregulated the phosphorylation levels of PLC-γ1, p38α, Akt, and other downstream signals.
In Vivo
(-)-Asarinin (5-20 mg/kg; gavage; once daily; 16 weeks) improves the morphology of gastric mucosal glands, alleviate intestinal metaplasia, inhibit the STAT3 pathway, promote ROS accumulation, and induce apoptosis of gastric mucosal cells in the N-Nitroso-N-methylurea (MNU) (HY-34758)-induced mouse model of gastric precancerous lesions[1].
(-)-Asarinin (5.0 mg/kg; oral administration; before intranasal OVA challenge) significantly inhibits the allergic reaction, reduces paw swelling and Evans blue exudation in mice, and decreases the degree of mast cell degranulation in the skin in the OVA-induced passive cutaneous anaphylaxis mouse model[3].
(-)-Asarinin (2.50 mg/kg; oral administration) reduces the concentrations of histamine, TNF-α, MCP-1, IL-4, and IL-5 in the serum of mice in the OVA - induced systemic anaphylaxis mouse model<[3].
(-)-Asarinin (5.0 mg/kg; oral administration; once daily; from day 21-28) significantly inhibits the scratching and sneezing responses of mice, reduces the concentrations of histamine, total IgE, and IL-4 in the serum of mice, and alleviates the inflammatory infiltration and thickening of the nasal mucosa in the OVA-induced allergic rhinitis mouse model[3].
(-)-Asarinin (2.5 mg/kg, 5.0 mg/kg, 10 mg/kg; oral administration) inhibits paw swelling and Evans blue exudation in mice and reduces the concentrations of histamine, TNF-α, MCP-1, and IL-8 in the serum in the C48/80-induced allergic reaction mouse model[3].
C57BL/6 mice (male, 18-22 g), OVA-induced passive cutaneous anaphylaxis model3
5.0 mg/kg
Oral administration
Significantly suppressed passive cutaneous anaphylaxis (PCA) in mice, reduced the degree of swelling and Evens blue exudation of mice paw, and decreased the degree of degranulation of MCs in skin.
C57BL/6 mice (male, 18-22 g), OVA-induced passive cutaneous anaphylaxis model3
2.50 mg/kg
Oral administration
Significantly reduced the concentration of histamine, TNF-α, MCP-1, IL-4 and IL-5 in mice serum.
C57BL/6 mice (male, 18-22 g), OVA-induced passive cutaneous anaphylaxis model3
5.0 mg/kg
Oral administration, once daily, from day 21 - 28
Significantly inhibited the scratching and sneezing response of mice, reduced the concentration of histamine, total IgE, and IL - 4 in mice serum, and attenuated the inflammatory infiltrates and nasal mucosa incrassation in the AR mice.
C57BL/6 mice (male, 18-22 g), C48/80-induced allergic reaction model3
2.5 mg/kg, 5.0 mg/kg, 10 mg/kg
Oral administration
Reduced C48/80-induced paw swelling and Evens blue exudation, and decreased the concentration of histamine, TNF-α, MCP-1 and IL-8 in mice serum.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Animal Model: SPF-grade BALB/c mice (male and female, 18-20 g, 4-week-old), established by administration of carcinogenic agent MNU[1]
Dosage:
20 mg/kg, 5 mg/kg
Administration:
Gavage, once daily, 16 weeks
Result:
Reversed the deterioration of the gastric mucosal glands' morphology, reduced the severity of intestinal metaplasia, promoted ROS accumulation, inhibited the STAT3 pathway, and induced apoptosis in the gastric mucosa of GPL mice.
Significantly suppressed passive cutaneous anaphylaxis (PCA) in mice, reduced the degree of swelling and Evens blue exudation of mice paw, and decreased the degree of degranulation of MCs in skin.
Significantly inhibited the scratching and sneezing response of mice, reduced the concentration of histamine, total IgE, and IL - 4 in mice serum, and attenuated the inflammatory infiltrates and nasal mucosa incrassation in the AR mice.
DMSO : 100 mg/mL (282.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.8221 mL
14.1103 mL
28.2207 mL
5 mM
0.5644 mL
2.8221 mL
5.6441 mL
10 mM
0.2822 mL
1.4110 mL
2.8221 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.06 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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