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| Targets |
Protosappanin A primarily targets the JAK2/STAT3 signaling pathway. By down-regulating the phosphorylation of JAK2 and STAT3, it inhibits the activation of this pathway, which is critical for inflammatory responses and cell survival. The compound also inhibits STAT3 nuclear translocation. Additionally, Protosappanin A targets the NF-kappaB pathway, inducing immunosuppression in heart transplantation by affecting T cells in grafts. It has antimicrobial activity against various pathogens and shows resistance reversal effects against MRSA.
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| ln Vitro |
In LPS-activated BV2 microglia, protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) markedly reduced TNF-α and IL-1β production. PTA decreased the mRNA expression of MCP-1, IL-1β, and IL-6 in the BV2 microglial cell line in a dose-dependent manner [1]. In response to LPS treatment, protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) suppresses the JAK2/STAT3-dependent inflammatory pathway by downregulating JAK2 and STAT3 phosphorylation as well as STAT3 nuclear translocation [1]. Protosappanin A (PTA: 12.5, 25, 50 μM, 24 hours) significantly inhibits the NF-κB-dependent oxidative and nitrative stress-induced increase in LPS by interfering with the interaction between the transmembrane protein CD14 and Toll-like receptor 4. BV2 microglia [2].
In vitro, Protosappanin A (12.5, 25, 50 µM, 24 hours) significantly inhibits the production of TNF-α and IL-1β in LPS-activated BV2 microglia. It suppresses the JAK2/STAT3-dependent inflammation pathway by down-regulating the phosphorylation of JAK2 and STAT3, as well as STAT3 nuclear translocation against LPS treatment. The compound also inhibits the mRNA expressions of IL-6. Protosappanin A shows antimicrobial activity and resistance reversal effects against MRSA. |
| ln Vivo |
In vivo, Protosappanin A induces immunosuppression in heart transplantation by targeting T cells in grafts via the NF-kappaB pathway. It has been studied for its potential as an immunosuppressive agent in organ transplantation. The compound's ability to inhibit the JAK2/STAT3 pathway suggests potential therapeutic applications in inflammatory diseases and autoimmune disorders. Its antimicrobial activity and resistance reversal effects against MRSA indicate potential for the treatment of infectious diseases.
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| Enzyme Assay |
The in vitro activity of Protosappanin A is assessed using various cell-based assays. For anti-inflammatory studies, BV2 microglia or macrophages are stimulated with LPS and treated with various concentrations of Protosappanin A (typically 1-100 µM) for 24 hours. The production of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in the culture medium is measured by ELISA. The phosphorylation of JAK2 and STAT3 is analyzed by Western blotting using phospho-specific antibodies. STAT3 nuclear translocation is assessed by immunofluorescence microscopy or by subcellular fractionation followed by Western blotting. For antimicrobial activity, minimum inhibitory concentrations (MICs) against various bacterial strains are determined using broth microdilution methods.
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| Cell Assay |
Western Blot analysis [1]
Cell Types: mouse BV2 microglial cell line. Tested Concentrations: 12.5, 25, 50 μM. Incubation Duration: 24 hrs (hours). Experimental Results: Inhibited LPS-induced release of NO, TNF-α and IL-1β in BV2 cells. LPS-induced IL-6, IL-1β and MCP-1 gene expression was attenuated in BV2 cells. Inhibits LPS-induced activation of the JAK2/STAT3 pathway in BV2 cells. For cellular assays, BV2 microglia, macrophages, or T cells are cultured in appropriate media. Cells are treated with various concentrations of Protosappanin A (typically 1-100 µM) for defined periods (1-24 hours). Cell viability is assessed using MTT or CellTiter-Glo assays. Cytokine production is measured by ELISA. The expression of inflammatory mediators (iNOS, COX-2) is analyzed by Western blotting or qPCR. The effect on T cell proliferation and activation can be assessed using flow cytometry or by measuring IL-2 production. |
| Animal Protocol |
In vivo, Protosappanin A is typically administered intraperitoneally or orally to animal models. In heart transplantation models, the compound is administered to recipient animals at various doses (typically 5-50 mg/kg) daily for 1-2 weeks. Graft survival is monitored, and the infiltration of immune cells into the graft is assessed by histopathology and immunohistochemistry. The expression of inflammatory markers and JAK2/STAT3 pathway components in graft tissue is analyzed by Western blotting or qPCR. In models of inflammatory disease (e.g., colitis, arthritis), the compound is administered daily, and disease severity is assessed by clinical scoring, histopathology, and measurement of inflammatory markers.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Protosappanin A is not detailed in the provided search results. As a small molecule with a molecular weight of 272.25 g/mol, it is expected to have reasonable oral bioavailability. It is soluble in DMSO. The compound should be stored under appropriate conditions to maintain stability. Its absorption, distribution, metabolism, and excretion would require further investigation.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Protosappanin A is not available in the provided search results. In in vitro studies, the compound did not show significant cytotoxicity at concentrations up to 50 µM. As an immunosuppressive agent, it may increase the risk of infections and malignancies with long-term use. The compound should be used with caution in patients with active infections or a history of cancer. Comprehensive toxicological studies are required to establish its full safety profile.
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| References |
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| Additional Infomation |
Protohematoxylin A is a type of catechin compound and a metabolite. It has been reported that protohematoxylin A exists in Alpinia japonica, Biancaea sappan, and Biancaea decapetala, and relevant data are available for reference.
Protosappanin A is a natural compound isolated from Caesalpinia sappan L., a plant used in traditional medicine for its anti-inflammatory and wound-healing properties. The compound has been studied for its potential as an immunosuppressive agent in organ transplantation and for its anti-inflammatory effects in various disease models. Its mechanism of action involves inhibition of the JAK2/STAT3 and NF-kappaB pathways, which are critical for inflammatory responses and immune cell function. Protosappanin A is not approved for clinical use and is primarily used as a research compound to study immunosuppression and inflammation. It is available from chemical suppliers for research purposes. |
| Molecular Formula |
C15H12O5
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|---|---|
| Molecular Weight |
272.2528
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| Exact Mass |
272.068
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| CAS # |
102036-28-2
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| Related CAS # |
102036-28-2;
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| PubChem CID |
128001
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
613.1±55.0 °C at 760 mmHg
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| Flash Point |
238.8±25.0 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.689
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| LogP |
1.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MUKYVRVYBBYJSI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12O5/c16-9-1-2-11-12-6-14(19)13(18)4-8(12)3-10(17)7-20-15(11)5-9/h1-2,4-6,16,18-19H,3,7H2
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| Chemical Name |
5,14,15-trihydroxy-8-oxatricyclo[10.4.0.02,7]hexadeca-1(16),2(7),3,5,12,14-hexaen-10-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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~125 mg/mL (~459.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.64 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 20.8 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: ≥ 2.08 mg/mL (7.64 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 20.8 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: ≥ 2.08 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6731 mL | 18.3655 mL | 36.7309 mL | |
| 5 mM | 0.7346 mL | 3.6731 mL | 7.3462 mL | |
| 10 mM | 0.3673 mL | 1.8365 mL | 3.6731 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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