| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| ln Vitro |
Keloid fibroblast proliferation was dose-dependently reduced by isoxazolinone (0, 100, 250, and 500 mg/L). Asiaticoside (100, 250, and 500 mg/L) enhances the expression of Smad7, but has no effect on Smad2, Smad3, or the deep depression phosphorylation of Smad4, Smad2, and Smad3 in fibroblasts. It also decreases the expression of collagen and mRNA, TGF-bRI, TGF-bRII protein, and mRNA [1]. In endothelial cells, hypoxia-induced decrease of cell viability and NO generation is prevented by Asiaticoside (12.5 and 50, and 25 and 50 μg/mL). In hypoxia-induced HPAECs, asticoside (50 μg/mL) upregulates and phosphorylates AKT/eNOS while shielding the endothelial cell base from hypoxia-induced cell closure [2].
In vitro, Asiaticoside (50 μg/ml) protected human pulmonary artery endothelial cells (HPAECs) from hypoxia-induced damage. Asiaticoside treatment under hypoxia (5% O2) for 24 h significantly increased cell viability in a dose-dependent manner (12.5-50 μg/ml), restored NO production, and prevented hypoxia-induced apoptosis as assessed by TUNEL assay. Asiaticoside (50 μg/ml) reduced caspase-3 activity compared to hypoxia control. Western blot analysis showed that Asiaticoside (50 μg/ml) upregulated the phosphorylation of Akt (p-Akt/Akt ratio) and eNOS (p-eNOS/eNOS ratio) in HPAECs under hypoxia. The protective effects of Asiaticoside were significantly inhibited by co-treatment with the PI3K inhibitor LY294002 (20 μmol/l), which reduced cell viability, decreased NO production, increased apoptosis, and suppressed the phosphorylation of Akt and eNOS [2]. |
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| ln Vivo |
Makingcassoside (5, 15, or 45 mg/kg, sidewall) improves learning and memory deficits, protects hippocampal neck lesions, reduces Aβ deposition in the hippocampus, and improves subcellular damage treated with Aβ oligomers structure[3]. Asiaticoside (50 mg/kg/d) inhibits the development of hypoxic pulmonary hypertension (PH), cardiovascular and endothelial cell damage [2].
In vivo, Asiaticoside (50 mg/kg/day, intragastric administration) prevented and reversed hypoxia-induced pulmonary hypertension in male Sprague-Dawley rats. In prevention group (HP, treated from day 1 of hypoxia for 4 weeks) and treatment group (HT, treated from week 2 of hypoxia for 2 weeks plus 2 weeks after hypoxia? as described), Asiaticoside significantly reduced mean pulmonary artery pressure (mPAP) compared to hypoxia control (Hx), without causing systemic hypotension (no significant effect on carotid arterial pressure). Asiaticoside attenuated right ventricular hypertrophy (RV/LV+S ratio) and reduced medial wall thickness of pulmonary arterioles. Transmission electron microscopy revealed that Asiaticoside ameliorated hypoxia-induced ultrastructural abnormalities of endothelial cells, including swelling, mitochondrial edema, vacuoles, and basement membrane exfoliation. Asiaticoside reduced serum endothelin-1 (ET-1) levels, increased serum NO levels (HP group), and increased lung tissue cGMP concentrations (HP group). Prostacyclin (PGI2) levels showed no significant change. Western blot analysis of lung tissue showed that Asiaticoside increased the phosphorylation of Akt (p-Akt/Akt ratio) and eNOS (p-eNOS/eNOS ratio) compared to hypoxia control [2]. |
| Cell Assay |
Cell viability was quantified using CCK-8 assay. HPAECs were cultured under normoxia (21% O2, 5% CO2) or hypoxia (5% O2, 5% CO2) for 24 h with or without Asiaticoside (12.5, 25, 50 μg/ml) and/or LY294002 (20 μmol/l). NO production in HPAECs was measured using a colorimetric assay kit for total nitrate/nitrite. Apoptosis was detected by TUNEL assay: air-dried cell samples were fixed, incubated with blocking solution and permeabilization solution, then TUNEL reaction mixture was added and incubated for 60 min at 37°C, and positive cells were counted under fluorescence microscope at 550 nm. Caspase-3 activity was quantified using a colorimetric assay: cytosolic extracts were incubated with DEVD-pNA substrate (200 μM final concentration) at 37°C for 1-2 h, and absorbance was measured at 400 nm. For Western blot, HPAECs were lysed, proteins (25 μg) were resolved by SDS-PAGE (12% gel), transferred to PVDF membranes, blocked with 5% skimmed milk, incubated with primary antibodies against Akt, p-Akt (Ser473), eNOS, p-eNOS (Ser177) and GAPDH overnight at 4°C, then with peroxidase-conjugated secondary antibody for 1 h, and visualized by enhanced chemiluminescence [2].
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| Animal Protocol |
Adult male Sprague-Dawley rats (body weight 180-200 g) were randomly divided into four groups (n=10 each): Nox (normoxia for 4 weeks, vehicle control), Hx (hypoxia for 4 weeks, vehicle), HP (hypoxia for 4 weeks with Asiaticoside from day 1), HT (hypoxia for 2 weeks then received Asiaticoside for 4 weeks, i.e., continued another 2 weeks after finishing 4-week hypoxia exposure). Hypoxia was induced in a sealed ventilated chamber with 9% O2. Asiaticoside (50 mg/kg) diluted in normal saline was administered daily by intragastric gavage. Vehicle groups received normal saline (1.5-2 ml). After treatment, rats were anesthetized with sodium pentobarbital (35 mg/kg i.p.). Mean pulmonary artery pressure (mPAP) and mean carotid arterial pressure (mCAP) were measured invasively. Right ventricular hypertrophy index (RV/LV+S) was calculated. Lung tissue was collected for H&E staining and transmission electron microscopy. Blood samples were collected for serum ET-1, NO, PGI2 by ELISA, and lung tissue cGMP by immunoassay [2].
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| References |
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| Additional Infomation |
Asiaticoside is a triterpenoid saponin. It has been reported that asiaticoside is found in Centella asiatica, Akebia trifoliata, and other organisms with relevant data. See also: Centella asiatica inflorescence (partial).
Asiaticoside is a saponin monomer from Centella asiatica with documented antioxidant, anti-inflammatory, anti-hepatofibrotic, and neuroprotective effects. Previous study showed it blocks TGF-β1/SMAD2/3 signaling to prevent hypoxic PH. This study is the first to demonstrate that Asiaticoside activates the PI3K/Akt/eNOS pathway, promotes NO production, and inhibits endothelial cell apoptosis, thereby preventing and reversing hypoxia-induced pulmonary hypertension in rats. It may be a potential therapeutic option for hypoxic PH patients [2]. |
| Molecular Formula |
C48H78O19
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|---|---|
| Molecular Weight |
959.1215
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| Exact Mass |
958.513
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| CAS # |
16830-15-2
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| PubChem CID |
11954171
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
949.4±65.0 °C at 760 mmHg
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| Melting Point |
235-238ºC
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| Flash Point |
268.4±27.8 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
8.34
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
67
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| Complexity |
1820
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| Defined Atom Stereocenter Count |
27
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| SMILES |
C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(C[C@H]([C@@H]([C@@]5(C)CO)O)O)C)C)[C@@H]2[C@H]1C)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O[C@H]8[C@@H]([C@@H]([C@H]([C@@H](O8)C)O)O)O)O)O)O)O)O
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| InChi Key |
WYQVAPGDARQUBT-FGWHUCSPSA-N
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| InChi Code |
InChI=1S/C48H78O19/c1-20-10-13-48(15-14-46(6)23(29(48)21(20)2)8-9-28-44(4)16-24(51)39(60)45(5,19-50)27(44)11-12-47(28,46)7)43(61)67-42-36(58)33(55)31(53)26(65-42)18-62-40-37(59)34(56)38(25(17-49)64-40)66-41-35(57)32(54)30(52)22(3)63-41/h8,20-22,24-42,49-60H,9-19H2,1-7H3/t20-,21+,22+,24-,25-,26-,27-,28-,29+,30+,31-,32-,33+,34-,35-,36-,37-,38-,39+,40-,41+,42+,44+,45+,46-,47-,48+/m1/s1
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| Chemical Name |
[(2S,3R,4S,5S,6R)-6-[[(2R,3R,4R,5S,6R)-3,4-dihydroxy-6-(hydroxymethyl)-5-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-2-yl]oxymethyl]-3,4,5-trihydroxyoxan-2-yl] (1S,2R,4aS,6aR,6aS,6bR,8aR,9R,10R,11R,12aR,14bS)-10,11-dihydroxy-9-(hydroxymethyl)-1,2,6a,6b,9,12a-hexamethyl-2,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydro-1H-picene-4a-carboxylate
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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 : ~50 mg/mL (~52.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.61 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 25.0 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: ≥ 2.5 mg/mL (2.61 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.61 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. Solubility in Formulation 4: ≥ 2.5 mg/mL (2.61 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 25.0 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. Solubility in Formulation 5: ≥ 2.5 mg/mL (2.61 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 25.0 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. Solubility in Formulation 6: ≥ 2.5 mg/mL (2.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: ≥ 2.5 mg/mL (2.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 8: ≥ 2.5 mg/mL (2.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 9: ≥ 2.5 mg/mL (2.61 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0426 mL | 5.2131 mL | 10.4262 mL | |
| 5 mM | 0.2085 mL | 1.0426 mL | 2.0852 mL | |
| 10 mM | 0.1043 mL | 0.5213 mL | 1.0426 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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