| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
NO Synthase (indirect inhibition via NF-kappaB pathway).
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|---|---|
| ln Vitro |
Amaroswerin inhibits NO release in LPS-stimulated RAW264.7 macrophages with an IC50 of 5.42 microg/mL. It reduces nitrite accumulation in a concentration-dependent manner without significant cytotoxicity at active concentrations. The compound is a secoiridoid glucoside with a molecular weight of 602.54 Da and shows broad-spectrum bioactivity including anti-inflammatory, antidiabetic, antiviral, anticholinergic, and immunomodulatory activities.
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| ln Vivo |
No in vivo activity data is publicly available for amaroswerin. Based on its ability to inhibit NO production in vitro, it is expected to exhibit anti-inflammatory activity in animal models of inflammation such as LPS-induced endotoxemia, carrageenan-induced paw edema, or collagen-induced arthritis. Further in vivo studies are required to confirm efficacy and pharmacokinetics.
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| Enzyme Assay |
Not available. A generic NOS inhibition assay can be used to determine amaroswerin's effect on NO production. RAW264.7 cells are stimulated with LPS (1 microg/mL) for 24 h to induce iNOS expression. Cytosolic extracts (100 microg protein) are incubated with amaroswerin (0-50 microg/mL) in assay buffer (50 mM Tris-HCl pH 7.4, 10 microM FAD, 10 microM FMN, 10 microM BH4, 1 mM NADPH, 1 mM CaCl2, 2.5 mM L-arginine, 10 microg/mL calmodulin) for 60 min at 37degC. Nitrite accumulation is measured by Griess reaction. Alternatively, iNOS protein expression can be assessed by Western blot to determine if the inhibition is at the expression level rather than direct enzyme inhibition.
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| Cell Assay |
RAW264.7 mouse macrophages are seeded in 96-well plates (5×10⁴/well) in DMEM with 10% FBS. Cells are pre-incubated with amaroswerin (0-50 microg/mL, typically 0.5-50 microg/mL) for 2 h, then stimulated with LPS (1 microg/mL) for 24 h. Culture supernatants are collected for nitrite measurement by Griess assay (1% sulfanilamide, 0.1% N-(1-naphthyl)ethylenediamine in 5% phosphoric acid, OD 540 nm). Cell viability is assessed by MTT or CCK-8 assay to ensure that inhibition of NO production is not due to cytotoxicity. Pro-inflammatory cytokines (TNF-alpha, IL-6, IL-1beta) in supernatants can be measured by ELISA for additional anti-inflammatory characterization. iNOS and COX-2 expression in cell lysates can be analyzed by Western blot.
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| Animal Protocol |
No animal protocol is published. Generic protocol for evaluating anti-inflammatory natural products: female BALB/c mice (6-8 weeks, n=8/group) receive amaroswerin orally or intraperitoneally at 10-100 mg/kg in 0.5% methylcellulose or 10% DMSO/90% corn oil. One hour later, LPS (5-10 mg/kg) is injected i.p. Blood is collected 4-6 h post-LPS, and serum nitrite/nitrate levels are measured by Griess assay. Serum TNF-alpha, IL-6, and IL-1beta levels are measured by ELISA. For topical inflammation models (e.g., croton oil-induced ear edema), amaroswerin is applied topically as a solution or cream, and ear thickness is measured.
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| ADME/Pharmacokinetics |
No PK data reported. Generic PK for secoiridoid glucosides: due to the presence of a glucose moiety, amaroswerin is highly polar and may be rapidly excreted or undergo deglycosylation in the gut. Oral bioavailability is expected to be low (<10-20%). Following IV administration in rats (5-10 mg/kg), t1/2 is typically short (1-2 h). Cmax after oral administration is low, with Tmax of 1-2 h. The aglycone (after deglycosylation) may be responsible for systemic activity. Tissue distribution is likely limited to the gastrointestinal tract and liver.
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| Toxicity/Toxicokinetics |
No toxicity data reported. Generic acute toxicity study: ICR mice (5/sex/group) receive single oral doses of amaroswerin at 100, 300, 1000 mg/kg in 0.5% methylcellulose. Animals are observed for 14 days for mortality, clinical signs, body weight, and food consumption. At termination, gross necropsy and histopathology of major organs (liver, kidney, spleen, heart, lung, GI tract) are performed. For natural secoiridoids, LD50 is typically >1000 mg/kg, indicating low acute toxicity. Subchronic (28-day) toxicity in rats at doses up to 200 mg/kg/day would assess target organs such as liver and kidney.
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| References | |
| Additional Infomation |
Amarosvirine is a member of the biphenyl class of compounds. It has been reported that amarosvirine is found in Swertia japonica, Gentiana scabra, and other organisms for which relevant data exists.
Amaroswerin is a natural product (CAS# 21233-18-1) derived from Swertia species, which are used in traditional medicine for hepatoprotective, anti-inflammatory, and antidiabetic purposes. The compound has a secoiridoid skeleton (C29H30O14, MW 602.54). It is not FDA-approved and has not entered clinical trials. Amaroswerin is a research-grade phytochemical used for studying the anti-inflammatory mechanisms of natural products and for validating traditional medicine claims. The compound may serve as a lead for developing new anti-inflammatory agents, but significant optimization is needed for drug development. |
| Molecular Formula |
C29H30O14
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|---|---|
| Molecular Weight |
602.54
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| Exact Mass |
602.164
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| CAS # |
21233-18-1
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| PubChem CID |
45359883
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| Appearance |
Off-white to light yellow solid powder
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| Source |
Originated from plants: Gentianaceae Swertia mussotii Franch.
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| LogP |
0.171
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
43
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C=C[C@H]1[C@@H](OC=C2[C@]1(CCOC2=O)O)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)OC(=O)C4=C(C=C(C=C4O)O)C5=CC(=CC=C5)O
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| InChi Key |
UZYZCCWBBBCDAD-WCYQFIIKSA-N
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| InChi Code |
InChI=1S/C29H30O14/c1-2-17-27(40-12-18-25(36)39-7-6-29(17,18)38)43-28-24(23(35)22(34)20(11-30)41-28)42-26(37)21-16(9-15(32)10-19(21)33)13-4-3-5-14(31)8-13/h2-5,8-10,12,17,20,22-24,27-28,30-35,38H,1,6-7,11H2/t17-,20+,22+,23-,24+,27-,28-,29+/m0/s1
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| Chemical Name |
[(2S,3R,4S,5S,6R)-2-[[(3S,4R,4aR)-4-ethenyl-4a-hydroxy-8-oxo-3,4,5,6-tetrahydropyrano[3,4-c]pyran-3-yl]oxy]-4,5-dihydroxy-6-(hydroxymethyl)oxan-3-yl] 2,4-dihydroxy-6-(3-hydroxyphenyl)benzoate
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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) |
Ethanol: ≥ 100 mg/mL (~166.0 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.15 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Suspended solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of ethanol stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (4.15 mM) (saturation unknown) in 10% EtOH + 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 ethanol stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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 3: ≥ 2.5 mg/mL (4.15 mM) (saturation unknown) in 10% EtOH + 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 EtOH stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6596 mL | 8.2982 mL | 16.5964 mL | |
| 5 mM | 0.3319 mL | 1.6596 mL | 3.3193 mL | |
| 10 mM | 0.1660 mL | 0.8298 mL | 1.6596 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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