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Loureirin A, a naturally occurring di-hydrochalcone/flavonoid isolated from Dragon's Blood, can inhibit Akt phosphorylation and has antiplatelet activity. It has been used to promote blood circulation and remove stasis in Chinese traditional medicine.
| Targets |
Akt (protein kinase B) phosphorylation at Ser473, downstream of the PI3K signaling pathway [1]
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| ln Vitro |
In a dose-dependent manner, loureirin A (50 μM, 100 μM) suppresses the release of platelet ATP produced by collagen and the expression of P-selectin activated by thrombin. Additionally, with immobilized fibrinogen, loureirin A dramatically reduces platelet spreading. At a dosage of 100 μM, luminirin A nearly entirely removes collagen-induced Akt phosphorylation at Ser473, and at 50 μM, it exhibits an additive inhibitory effect when combined with the phosphoinositide 3-kinase (PI3K) inhibitor Ly294002 on collage-induced Akt phosphorylation in platelets[1].
Loureirin A dose-dependently inhibited platelet aggregation induced by collagen (50 μM: 77.9±2.3%; 100 μM: 15.2±6.2% of control), collagen-related peptide (CRP), ADP, and thrombin [1] It inhibited collagen-induced ATP secretion from platelet dense granules (50 μM: 29.7±4.0%; 100 μM: 11.6±3.1% of control) [1] Loureirin A inhibited thrombin-stimulated P-selectin expression on the platelet surface, a marker of α-granule release (100 μM: 59.0±3.3%; 300 μM: 15.0±2.3% of control) [1] It significantly impaired human platelet spreading on immobilized fibrinogen, reducing platelet surface area (50 μM: 28.4±6.5 μm²; 100 μM: 20.1±7.3 μm² vs. control) and altering morphology (more filopodia, less lamellipodia) [1] Western blot analysis showed that 100 μM Loureirin A almost completely eliminated collagen-induced Akt phosphorylation at Ser473, but did not affect JNK phosphorylation [1] A submaximal dose (50 μM) of Loureirin A had an additive inhibitory effect with the PI3K inhibitor LY294002 on collagen-induced Akt phosphorylation in platelets [1] |
| Cell Assay |
Platelet Aggregation and Secretion Assay: Washed mouse platelets (3×10⁸/ml) in Tyrode's buffer containing 1 mM CaCl₂ were preincubated with Loureirin A or vehicle (0.33% DMSO) for 5 minutes at room temperature. Agonists (collagen, CRP, ADP, or thrombin) were then added to stimulate aggregation, which was measured using a lumi-aggregometer. For ATP secretion measurement, luciferin-luciferase reagent was added prior to agonist stimulation to record ATP release [1]
P-selectin Expression Assay (Flow Cytometry): Washed mouse platelets were preincubated with Loureirin A or vehicle and then stimulated with thrombin. Fluorescein isothiocyanate (FITC)-labeled anti-mouse CD62P antibody was added, and platelet surface P-selectin expression was analyzed using flow cytometry [1] Platelet Spreading Assay: Washed human platelets (2×10⁷/ml) in Tyrode's buffer containing 1 mM CaCl₂ and 5 mM MnCl₂ were preincubated with Loureirin A or vehicle for 5 minutes. The platelets were then allowed to adhere and spread on cover glasses coated with fibrinogen (25 μg/ml) for 45 minutes at room temperature. Non-adherent platelets were removed by washing. Adherent platelets were fixed with 4% paraformaldehyde, permeabilized with 0.1% Triton X-100, and stained with TRITC-conjugated phalloidin (1 μg/ml) to visualize F-actin. Platelet spreading was observed using a fluorescence microscope, and platelet surface areas were quantified using image analysis software [1] Western Blot Analysis: Washed mouse platelets were preincubated with Loureirin A or vehicle for 5 minutes and then stimulated with collagen for 3 minutes. The reaction was stopped by adding an equal volume of lysis buffer containing protease and phosphatase inhibitors. Proteins were separated by SDS-PAGE, transferred to PVDF membranes, and probed with specific antibodies against phospho-Akt (Ser473), total Akt, phospho-JNK (Thr183/Tyr185), and total JNK. Protein bands were detected using a chemiluminescence imaging system [1] |
| References | |
| Additional Infomation |
It has been reported that loretin A is found in Dracaena cochinchinensis, soybean (Soymida febrifuga), and Garcinia dulcis, and there is relevant data. Loretin A is a flavonoid compound extracted from Dracaena cochinchinensis (a traditional Chinese medicine resin), which has historically been used to promote blood circulation and remove blood stasis[1]. Studies have shown that the antiplatelet mechanism of loretin A involves the inhibition of the PI3K/Akt signaling pathway, which is crucial for platelet activation, aggregation, and extracellular-intracellular signal transduction of integrin αIIbβ3[1]. This study used relatively high concentrations of loretin A (50-300 μM) in in vitro experiments. The authors pointed out that the effective dose may vary depending on the species, and the in vivo efficacy needs further research[1].
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| Molecular Formula |
C17H18O4
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|---|---|
| Molecular Weight |
286.3224
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| Exact Mass |
286.12
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| CAS # |
119425-89-7
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| PubChem CID |
5319081
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
479.1±40.0 °C at 760 mmHg
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| Flash Point |
175.8±20.8 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
323
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RSAIVLRELNGZEY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18O4/c1-20-15-9-5-13(17(11-15)21-2)6-10-16(19)12-3-7-14(18)8-4-12/h3-5,7-9,11,18H,6,10H2,1-2H3
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| Chemical Name |
3-(2,4-dimethoxyphenyl)-1-(4-hydroxyphenyl)propan-1-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 86.6 mg/mL (~302.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4926 mL | 17.4630 mL | 34.9260 mL | |
| 5 mM | 0.6985 mL | 3.4926 mL | 6.9852 mL | |
| 10 mM | 0.3493 mL | 1.7463 mL | 3.4926 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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