| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Aloin targets multiple pathways and enzymes. It inhibits key enzymes including Clostridium histolyticum collagenase (ChC), granulocyte matrix metalloproteinases (MMPs), and the human 20S proteasome. It also inhibits interleukin (IL)-1β-stimulated IL-8 production in KB cells and modulates the Nrf2/HO-1 and TGF-β/Smad2/3 signaling pathways. Aloin reduces IL-6 and TNF-α expression as well as nitric oxide (NO) production and COX-2 and inducible NO synthase (iNOS) expression.
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| ln Vitro |
In vitro, Aloin inhibits IL-1β-stimulated IL-8 production in KB cells. It reduces IL-6 and TNF-α expression as well as nitric oxide (NO) production and COX-2 and iNOS expression in LPS-stimulated RAW 264.7 cells when used at concentrations ranging from 100 to 400 mM. Clostridium histolyticum collagenase (ChC) is dose-dependently inhibited by aloe gel, with activity-guided fractionation leading to an active fraction enriched in phenolics and aloins. Aloin also exhibits antibacterial, antifungal, and antioxidant activities.
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| ln Vivo |
In vivo, Aloin effectively inhibits salivary IL-1β-induced IL-8 production by mitigating the p38 and ERK pathway, suggesting it may be a good candidate for modulating oral inflammatory diseases. It has been studied for its anti-inflammatory and immunomodulatory effects in animal models. Detailed dose-response and pharmacokinetic data in vivo are limited in publicly available literature.
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| Enzyme Assay |
No specific cell-free enzyme assay protocol is detailed for Aloin. For anthraquinone compounds, typical cell-free assays include enzyme inhibition studies using purified collagenase, MMPs, or proteasome, with chromogenic or fluorogenic substrates. Activity can be assessed by measuring inhibition of substrate cleavage and calculating IC50 values from dose-response curves.
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| Cell Assay |
Anti-inflammatory activity is assessed in LPS-stimulated RAW 264.7 macrophage cells. Cells are treated with serial dilutions of Aloin (e.g., 100-400 mM). Endpoints include measurement of IL-6 and TNF-α expression (ELISA), nitric oxide (NO) production (Griess assay), and COX-2 and iNOS expression (Western blot or qPCR). IL-8 production inhibition can be assessed in KB cells stimulated with IL-1β.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of oral inflammation or other inflammatory diseases. Aloin is administered via oral gavage or topical application. Endpoints include inflammatory cytokine levels (e.g., IL-8, IL-6, TNF-α), inflammatory cell infiltration, and histopathological examination of affected tissues.
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| ADME/Pharmacokinetics |
Molecular formula: typically C21H22O9 (for aloin A/B); molecular weight: approximately 418.39. CAS No.: 8015-61-0. Appearance: yellow crystalline powder. Solubility: soluble in DMSO, ethanol; sparingly soluble in water. Storage: typical for anthraquinone glycosides (desiccated, protected from light, -20°C).
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural anthraquinone from Aloe vera, it is generally considered to have low toxicity at moderate doses, but high doses may cause gastrointestinal irritation and laxative effects. Standard toxicological studies would be required for drug development.
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| References |
: Evaluation of the Antioxidative, Antibacterial, and Anti-Inflammatory Effects of the Aloe Fermentation Supernatant Containing Lactobacillus plantarum HM218749.1. Mediators Inflamm. 2016;2016:2945650.
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| Additional Infomation |
Aloin A is a C-glycoside compound with the structure β-D-glucopyranose, wherein the terminal hydroxyl group is replaced by the 4,5-dihydroxy-2-(hydroxymethyl)-10-oxo-9,10-dihydroanthracene-9-yl moiety (9S diastereomer). It is a metabolite and a laxative. It is a C-glycoside compound belonging to the anthracene, cyclic ketone, and phenolic classes. Aloin has been reported in Aloe ferox, Aloe africana, and other organisms with relevant data. See also: Aloe leaf (partial); Rhamnus bark (partial); Aloin (note moved to).
Aloin (mixture of A&B) is a research-grade compound, not approved for therapeutic use. It is primarily used for pharmacological research in inflammation, immunology, diabetes, and cancer. No FDA approval has been reported. Its mechanisms involve inhibition of collagenase, MMPs, and proteasome, as well as modulation of Nrf2/HO-1 and TGF-β/Smad2/3 pathways. |
| Molecular Formula |
C21H22O9
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|---|---|
| Molecular Weight |
418.3940
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| Exact Mass |
418.126
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| CAS # |
8015-61-0
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| PubChem CID |
12305761
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
752.6±60.0 °C at 760 mmHg
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| Flash Point |
268.0±26.4 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.741
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| LogP |
1.86
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
630
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C1=CC2=C(C(=C1)O)C(=O)C3=C(C2[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)C=C(C=C3O)CO
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| InChi Key |
AFHJQYHRLPMKHU-CGISPIQUSA-N
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| InChi Code |
InChI=1S/C21H22O9/c22-6-8-4-10-14(21-20(29)19(28)17(26)13(7-23)30-21)9-2-1-3-11(24)15(9)18(27)16(10)12(25)5-8/h1-5,13-14,17,19-26,28-29H,6-7H2/t13-,14?,17-,19+,20-,21+/m1/s1
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| Chemical Name |
1,8-dihydroxy-3-(hydroxymethyl)-10-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]-10H-anthracen-9-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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~239.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.98 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 (5.98 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3901 mL | 11.9506 mL | 23.9011 mL | |
| 5 mM | 0.4780 mL | 2.3901 mL | 4.7802 mL | |
| 10 mM | 0.2390 mL | 1.1951 mL | 2.3901 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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