| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
PKC, cMET, ERK1/2, COX-2 [1]
PPAR-γ [2] Nrf2, HO-1 [10] class III PI3K, Beclin-1, Bcl-2 [9] |
|---|---|
| ln Vitro |
- In HGF-induced human hepatocellular carcinoma (HCC) cells (HepG2, Huh7), Madecassoside (10, 20, 40 μM) dose-dependently inhibited cell proliferation (MTT assay) and invasiveness (Transwell assay). It suppressed the PKC-cMET-ERK1/2-COX-2-PGE2 pathway: downregulated phosphorylated PKC, cMET, ERK1/2, and COX-2 protein expression, and reduced PGE2 secretion (Western blot, ELISA) [1]
- In human umbilical vein endothelial cells (HUVECs) exposed to H2O2 (200 μM), Madecassoside (5, 10, 20 μM) dose-dependently increased cell viability (MTT assay), reduced ROS production (DCFH-DA staining), and decreased apoptosis (Annexin V-FITC/PI staining). It upregulated antioxidant enzymes (SOD, CAT) activity and downregulated caspase-3 activation (Western blot) [5] - In H2O2-induced human melanocytes, Madecassoside (10, 20, 40 μM) alleviated oxidative stress: reduced ROS generation, increased SOD activity, and inhibited excessive autophagy (decreased LC3-II/LC3-I ratio, upregulated p62 expression, Western blot). It also improved cell viability (MTT assay) [7] - In doxorubicin (DOX)-treated HK-2 renal tubular epithelial cells, Madecassoside (5, 10, 20 μM) dose-dependently protected cells from DOX-induced cytotoxicity (MTT assay), reduced ROS production, and inhibited apoptosis (downregulated Bax/Bcl-2 ratio, cleaved caspase-3 expression, Western blot) [3] - In Aβ(25-35)-treated SH-SY5Y neuronal cells, Madecassoside (5, 10, 20 μM) suppressed inflammatory responses (reduced TNF-α, IL-1β mRNA expression, qPCR) and inhibited abnormal autophagy (regulated class III PI3K/Beclin-1/Bcl-2 pathway, Western blot). It improved cell viability (MTT assay) [9] - In LPS-treated BV2 microglial cells, Madecassoside (10, 20, 40 μM) reduced neurotoxicity by activating the Nrf2-HO-1 pathway: upregulated Nrf2 and HO-1 protein expression (Western blot), decreased ROS and pro-inflammatory cytokine (TNF-α, IL-6) production (ELISA) [10] - In INS-1E pancreatic β-cells, Madecassoside (10, 20 μM) improved insulin sensitivity: increased glucose-stimulated insulin secretion (ELISA) and upregulated GLUT2 mRNA expression (qPCR) [8] |
| ln Vivo |
- In bleomycin-induced pulmonary fibrosis mice, oral administration of Madecassoside (20, 40 mg/kg/day) for 21 days ameliorated lung fibrosis: reduced collagen deposition (Masson staining), downregulated fibrosis markers (α-SMA, Col1A1 mRNA expression, qPCR), and promoted colon-derived HGF generation via activating PPAR-γ (upregulated PPAR-γ, HGF mRNA/protein expression in colon, qPCR/Western blot) [2]
- In DOX-induced nephrotoxicity mice, intraperitoneal injection of Madecassoside (10, 20 mg/kg) every other day for 2 weeks protected renal function: reduced serum creatinine (Cr) and blood urea nitrogen (BUN) levels, alleviated renal tissue damage (HE staining). It inhibited oxidative stress (increased SOD activity, decreased MDA level) and apoptosis (TUNEL assay, downregulated Bax/Bcl-2 ratio) [3] - In focal cerebral ischemia-reperfusion (I/R) injury rats, intraperitoneal injection of Madecassoside (10, 20 mg/kg) before reperfusion reduced cerebral infarction volume (TTC staining), improved neurological deficit scores, and protected blood-brain barrier integrity (reduced Evans blue leakage). It inhibited oxidative stress (increased SOD, CAT activity) and inflammation (decreased TNF-α, IL-1β levels, ELISA) [6] - In LPS-induced neurotoxicity rats, oral administration of Madecassoside (20, 40 mg/kg/day) for 7 days ameliorated cognitive impairment (Morris water maze test), reduced hippocampal neuronal damage (HE staining), and activated the Nrf2-HO-1 pathway (upregulated Nrf2, HO-1 protein expression in hippocampus, Western blot) [10] |
| Enzyme Assay |
- COX-2 activity assay: HGF-induced HepG2 cells were treated with Madecassoside (10, 20, 40 μM) for 24 hours. Cells were lysed, and COX-2 activity was measured by detecting the conversion of arachidonic acid to PGE2. The reaction product PGE2 was quantified by ELISA to evaluate COX-2 inhibition [1]
- PPAR-γ binding assay: Recombinant PPAR-γ ligand-binding domain protein was incubated with Madecassoside (0.1-10 μM) and a fluorescent PPAR-γ ligand. Fluorescence polarization was measured to assess the binding affinity of Madecassoside to PPAR-γ [2] |
| Cell Assay |
- HCC cell proliferation and invasion assay: HepG2/Huh7 cells were treated with Madecassoside (10, 20, 40 μM) and HGF (20 ng/mL) for 48 hours. Cell viability was detected by MTT assay; invasiveness was evaluated by Transwell assay (cells stained and counted). Western blot was used to detect pathway-related proteins, and ELISA for PGE2 secretion [1]
- Endothelial cell oxidative stress assay: HUVECs were pretreated with Madecassoside (5, 10, 20 μM) for 1 hour, then exposed to H2O2 (200 μM) for 24 hours. ROS production was detected by DCFH-DA staining; apoptosis by Annexin V-FITC/PI flow cytometry; SOD/CAT activity by colorimetric assay; caspase-3 by Western blot [5] - Melanocyte autophagy assay: Human melanocytes were pretreated with Madecassoside (10, 20, 40 μM) for 2 hours, then treated with H2O2 (100 μM) for 24 hours. Cell viability by MTT assay; SOD activity by colorimetric assay; LC3-II/LC3-I, p62 by Western blot [7] - Renal cell protection assay: HK-2 cells were pretreated with Madecassoside (5, 10, 20 μM) for 1 hour, then treated with DOX (1 μM) for 24 hours. Cell viability by MTT assay; ROS by DCFH-DA staining; Bax, Bcl-2, cleaved caspase-3 by Western blot [3] - Neuronal cell assay: SH-SY5Y cells were pretreated with Madecassoside (5, 10, 20 μM) for 1 hour, then treated with Aβ(25-35) (20 μM) for 24 hours. Cell viability by MTT assay; TNF-α/IL-1β mRNA by qPCR; class III PI3K/Beclin-1/Bcl-2 pathway proteins by Western blot [9] - β-cell insulin sensitivity assay: INS-1E cells were treated with Madecassoside (10, 20 μM) for 24 hours. Glucose-stimulated insulin secretion was detected by ELISA; GLUT2 mRNA by qPCR [8] |
| Animal Protocol |
- Pulmonary fibrosis model: C57BL/6 mice were intratracheally instilled with bleomycin (5 mg/kg) to induce fibrosis. Madecassoside (20, 40 mg/kg/day) was dissolved in 0.5% CMC-Na and administered orally for 21 days. Lung tissues were collected for Masson staining and qPCR; colon tissues for qPCR/Western blot [2]
- Nephrotoxicity model: BALB/c mice were intraperitoneally injected with DOX (15 mg/kg) to induce nephrotoxicity. Madecassoside (10, 20 mg/kg) was intraperitoneally injected every other day for 2 weeks. Serum was collected for Cr/BUN detection; kidney tissues for HE staining, TUNEL assay, and oxidative stress marker detection [3] - Cerebral I/R model: Sprague-Dawley rats were subjected to middle cerebral artery occlusion (MCAO) for 2 hours followed by reperfusion. Madecassoside (10, 20 mg/kg) was intraperitoneally injected 30 minutes before reperfusion. Neurological deficit scores were evaluated; cerebral tissues for TTC staining, Evans blue leakage assay, and oxidative stress/inflammation marker detection [6] - Neurotoxicity model: Sprague-Dawley rats were intraperitoneally injected with LPS (5 mg/kg) to induce neurotoxicity. Madecassoside (20, 40 mg/kg/day) was dissolved in saline and administered orally for 7 days. Morris water maze test was performed; hippocampal tissues for HE staining and Western blot [10] |
| ADME/Pharmacokinetics |
In rats orally administered Centella asiatica extract ECa 233 (containing madecaside), the pharmacokinetic parameters of madecaside were: Cmax = 1.8 ± 0.5 μg/mL, Tmax = 1.5 ± 0.5 h, AUC0-t = 8.2 ± 2.1 μg·h/mL, AUC0-∞ = 9.5 ± 2.4 μg·h/mL, t1/2 = 3.2 ± 0.8 h, and oral bioavailability (F) = 3.1 ± 0.9% [4]
- Madecaside is widely distributed in rat tissues, with higher concentrations in the liver, kidneys, and lungs, and lower concentrations in brain tissue [4] |
| Toxicity/Toxicokinetics |
In all in vivo experiments, the tested doses (10–40 mg/kg/day, oral/intraperitoneal) of asiaticoside did not cause significant changes in animal body weight, food intake, or serum ALT/AST levels, indicating that it had no significant hepatotoxicity [2][3][6][10]. In in vitro experiments, asiaticoside at concentrations up to 40 μM did not show cytotoxicity to normal cells (HUVECs, melanocytes, HK-2 cells) [5][7][3].
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| References |
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| Additional Infomation |
Asiaticin has been reported to exist in Cretaceous frankincense (Actaea dahurica), Centella erecta, and other organisms with relevant data.
See also: Asiaticin (note moved here). - Centella asiatica is a triterpenoid saponin isolated from the traditional Chinese medicine Centella asiatica [3][5][9] - Its core biological activities include anti-tumor (inhibiting the proliferation/invasion of hepatocellular carcinoma cells), anti-fibrosis (improving pulmonary fibrosis), organ protection (kidney, brain, neurons, endothelial cells), anti-oxidative stress, anti-inflammation, and improving insulin sensitivity [1][2][3][5][6][7][8][9][10] - Its potential mechanism involves regulating multiple signaling pathways: PKC-cMET-ERK1/2-COX-2-PGE2, PPAR-γ-HGF, Nrf2-HO-1, class III PI3K/Beclin-1/Bcl-2 pathway, as well as regulating oxidative stress, apoptosis, autophagy, and inflammation [1][2][5][7][9][10] - Centella asiatica glycosides have shown potential therapeutic value in hepatocellular carcinoma, pulmonary fibrosis, drug-induced nephrotoxicity, cerebral ischemia-reperfusion injury, neuroinflammation, and metabolic disorders (insulin resistance) [1][2][3][6][8][10] |
| Molecular Formula |
C48H78O20
|
|---|---|
| Molecular Weight |
975.1209
|
| Exact Mass |
974.508
|
| CAS # |
34540-22-2
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| PubChem CID |
161823
|
| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
1043.6±65.0 °C at 760 mmHg
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| Melting Point |
220 - 223 °C
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| Flash Point |
295.8±27.8 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
1.88
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
68
|
| Complexity |
1860
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(C[C@H]([C@@H]5[C@@]4(C[C@H]([C@@H]([C@@]5(C)CO)O)O)C)O)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
|
| InChi Key |
BNMGUJRJUUDLHW-HCZMHFOYSA-N
|
| InChi Code |
InChI=1S/C48H78O20/c1-19-10-11-48(13-12-46(6)22(28(48)20(19)2)8-9-27-44(4)14-24(52)39(61)45(5,18-50)38(44)23(51)15-47(27,46)7)43(62)68-42-35(59)32(56)30(54)26(66-42)17-63-40-36(60)33(57)37(25(16-49)65-40)67-41-34(58)31(55)29(53)21(3)64-41/h8,19-21,23-42,49-61H,9-18H2,1-7H3/t19-,20+,21+,23-,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
|
| 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,8R,8aR,9R,10R,11R,12aR,14bS)-8,10,11-trihydroxy-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 : ~100 mg/mL (~102.55 mM)
H2O : ~33.33 mg/mL (~34.18 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.56 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 (2.56 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (25.64 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0255 mL | 5.1276 mL | 10.2551 mL | |
| 5 mM | 0.2051 mL | 1.0255 mL | 2.0510 mL | |
| 10 mM | 0.1026 mL | 0.5128 mL | 1.0255 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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