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Sparstolonin B (SsnB) is a naturally occurring TLR2 and TLR4 antagonist isolated from the Chinese herb called Scirpus yagara. It blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activity. SsnB inhibited the expression of various inflammatory mediators such as tumor necrosis factor (TNF-α), interleukin (IL)-1β, IL-6, and chemokine (C-C motif) ligand 2 (CCL-2) in lipopolysaccharide (LPS)- or Pam3csk4-stimulated macrophages.
| ln Vitro |
Neuroblastoma cells are inhibited in their growth and viability by sparstolonin B (1–20 µM; 2-4 days) [3]. In mouse macrophages, sparstolonin B suppresses the production of cytokines triggered by TLR ligands. The recruitment of MyD88 to TLR4 and TLR2 is inhibited by sparstolonin B[1]. In neuroblastoma cells, sparstolonin B produces reactive oxygen species (ROS). N-myc expression is decreased in neuroblastoma cells by sparstolonin B [3].
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| ln Vivo |
Sparstolonin B (100 μg/mouse; intraperitoneal injection) can reduce LPS-induced inflammation in mice [1].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: SH-SY5Y, IMR-32, NGP, SKNF-1 and SK-N-BE(2) Cell Tested Concentrations: 1 µM, 5 µM, 10 µM or 20 µM Incubation Duration: 2- 4-day Experimental Results: 2-day (SH-SY5Y and IMR-32), 3-day (NGP cells), or 4-day (SKNF-1 and SK-N-BE(2) cells) treatment. |
| Animal Protocol |
Animal/Disease Models: 5-6 weeks old male C57Bl/6 mice (weight 18-20 g) [1]
Doses: 100 μg/mouse Route of Administration: intraperitoneal (ip) injection Experimental Results: LPS-induced expression levels of TNFα and IL-1β were Dramatically Dramatically reduce sepsis in a mouse model. |
| References |
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| Molecular Formula |
C15H8O5
|
|---|---|
| Molecular Weight |
268.221024513245
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| Exact Mass |
268.037
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| CAS # |
1259330-61-4
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| PubChem CID |
135659042
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
20
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| Complexity |
622
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C2C=CC(=CC=2C2=COC(=C3C(C=CC1=C23)=O)O)O
|
| InChi Key |
KUPDHLFGNQEASI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8O5/c16-7-1-3-11-8(5-7)9-6-19-15(18)14-10(17)2-4-12(20-11)13(9)14/h1-6,16,18H
|
| Chemical Name |
4,14-dihydroxy-8,15-dioxatetracyclo[7.7.1.02,7.013,17]heptadeca-1(16),2(7),3,5,9(17),10,13-heptaen-12-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 : ~10 mg/mL (~37.28 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (18.64 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 3.7283 mL | 18.6414 mL | 37.2828 mL | |
| 5 mM | 0.7457 mL | 3.7283 mL | 7.4566 mL | |
| 10 mM | 0.3728 mL | 1.8641 mL | 3.7283 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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