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| Targets |
The primary mechanism of Forsythoside B involves the inhibition of the nuclear factor-kappa B (NF-κB) signaling pathway. It achieves this by down-regulating the levels of key pro-inflammatory cytokines, including tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6), and by inhibiting the IκB kinase (IKK) pathway, which prevents the degradation of IκB and subsequent NF-κB activation. Additionally, Forsythoside B has been identified as a channel blocker of the Transient Receptor Potential Vanilloid 3 (TRPV3) ion channel. It also binds directly to lipopolysaccharide (LPS), thereby reducing the biological activity of serum LPS and contributing to its antisepsis mechanism. These combined actions on inflammatory signaling and direct pathogen-associated molecular pattern neutralization underline its multi-targeted therapeutic potential.
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| ln Vitro |
The quantity of forsythoside B suppresses the effects of lipopolysaccharide (LPS) on TNF-α, IL-6, and high mobility group protein 1 (HMGB1) levels. It also inhibits the pigmentation of IκB (IKK) and regulates nuclear factor (NF) in RAW264.7 cells by κB.
In vitro studies have demonstrated that Forsythoside B exhibits a concentration-dependent down-regulation of TNF-α, IL-6, and high-mobility group box 1 protein (HMGB1) in LPS-stimulated RAW264.7 macrophage cells. This anti-inflammatory effect is mediated through the inhibition of the IKK/NF-κB pathway. Furthermore, its antioxidant properties are evident in its ability to reduce oxidative stress in various cellular models. Forsythoside B has also shown potent neuroprotective effects in vitro, with studies indicating it can reduce the degree of cerebral ischemia and reperfusion injury. Its ability to attenuate blood-brain barrier (BBB) breakdown in these models further supports its potential in treating neurological conditions where inflammation plays a critical role. |
| ln Vivo |
Intravenous injection of forsythin B, either alone or in combination with imipenem, can raise blood IL-10 levels while lowering serum levels of endotoxin, TNF-α, IL-6, HMGB1, and myeloid cell expressed receptor (TREM-1). and decreased MPO (myeloperoxidase) in the liver, small intestine, and lungs [1]. At dosages of about 8 mg/kg, forsythin B demonstrated considerable neuroprotective potential in the brain and following reperfusion. Significant neuroprotective efficacy was demonstrated by forsythin B (20 mg/kg) even after intracerebral reperfusion delays of 1, 3, and 5 hours. In addition to reducing brain Evans blue extravasation and myeloperoxidase activity and weakening tissue pathological damage, forsythin B (20 mg/kg) can also decrease the expression of NF-κB and cephalin-IκB-α[2]. While inhibiting the reduction of SOD and GPx activities, forsythin B significantly restored myocardial function and improved LVSP myocardial infarction volume, serum Tn-T, TNF-α, and IL-6 levels, myocardial tissue MDA content, and MPO activity. It also reduced HMGB1, phosphorus-I kappaB-α, and phospho-NF-kappaB protein expression and transcription.
In vivo, Forsythoside B has demonstrated significant neuroprotective effects, with studies showing it can reduce cerebral ischemia and reperfusion injury and attenuate BBB breakdown. These protective effects are thought to be primarily due to the inhibition of the inflammatory response. The compound's antisepsis effect has also been validated in animal models, where its ability to bind LPS and reduce systemic levels of inflammatory mediators contributes to improved outcomes. These in vivo findings corroborate its in vitro anti-inflammatory and neuroprotective mechanisms, highlighting its therapeutic potential for conditions like stroke and sepsis. While specific pharmacokinetic data is limited, its oral bioavailability and efficacy in these models make it a compound of interest for further preclinical development. |
| Enzyme Assay |
In cell-free systems, the primary assay for studying Forsythoside B involves evaluating its binding to lipopolysaccharide (LPS). This can be performed using methods such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to directly measure the binding affinity between Forsythoside B and LPS. Additionally, its inhibition of the IKK/NF-κB pathway can be studied in cell-free kinase assays using purified IKK enzyme and a specific substrate, measuring the phosphorylation of IκB in the presence of the compound. For its role as a TRPV3 channel blocker， cell-free electrophysiology or fluorescence-based ion flux assays using TRPV3-expressing membrane preparations can be employed to determine its inhibitory potency (IC50).
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| Cell Assay |
For in vitro cellular assays, LPS-stimulated RAW264.7 macrophage cells are a standard model to evaluate the anti-inflammatory activity of Forsythoside B. Cells are typically seeded in multi-well plates and pre-incubated with Forsythoside B at various concentrations before stimulation with LPS. After a defined incubation period (e.g., 24 hours), cell culture supernatants are collected to measure the levels of pro-inflammatory cytokines like TNF-α and IL-6 using ELISA. Cellular lysates can be prepared for Western blot analysis to assess the expression of proteins involved in the NF-κB pathway, such as IκB and phosphorylated NF-κB, or for qPCR to measure the mRNA expression of inflammatory genes. Cell viability is concurrently assessed using MTT or similar assays to ensure any observed effects are not due to cytotoxicity.
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| Animal Protocol |
For in vivo efficacy studies, rodent models of cerebral ischemia-reperfusion injury are commonly employed to evaluate the neuroprotective effects of Forsythoside B. In such models, the compound can be administered via intraperitoneal or intravenous injection at specific time points before or after the induction of ischemia. Endpoints typically include the measurement of infarct size, assessment of neurological deficit scores, and evaluation of BBB integrity using tracers like Evans blue. In models of sepsis, Forsythoside B's antisepsis effect is evaluated by administering the compound to animals challenged with a lethal dose of LPS or in a cecal ligation and puncture (CLP) model. The primary endpoints are survival rate, reduction in serum levels of inflammatory cytokines (TNF-α, IL-6), and bacterial load.
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| ADME/Pharmacokinetics |
Forsythoside B (C29H36O15) has a molecular weight of 624.59 g/mol. It is soluble in water (90 mg/mL) and DMSO (100 mg/mL), making it suitable for both in vitro and in vivo applications. Recommended storage conditions for the compound are -20°C, protected from light. For in vivo administration, it can be formulated in saline or other suitable vehicles, and its stability in solution should be confirmed prior to use. As a natural product, its purity is typically determined by HPLC, with research-grade material often exceeding 98%.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available from comprehensive safety pharmacology or toxicology studies. However, as a natural phenylethanoid glycoside from a plant with a history of medicinal use, it is generally considered to have low toxicity at the doses used in research. In vitro cytotoxicity assays, such as the MTT test in various cell lines, are typically performed alongside efficacy studies to confirm that the observed effects are not due to a general reduction in cell viability. For any potential therapeutic development, standard in vivo toxicological profiling, including acute and repeated-dose toxicity studies in rodents, would be required to establish a complete safety profile.
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| References |
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| Additional Infomation |
According to reports, forsythoside B has been found in jasmine, white verbena, and other organisms with available data.
Forsythoside B is a research-grade compound and is not approved for any therapeutic use. It serves primarily as a valuable pharmacological tool and a reference standard for studying inflammatory and neuroprotective pathways. Its mechanism of action centers on the inhibition of the NF-κB pathway and the modulation of cytokine production, contributing to its anti-inflammatory and antisepsis effects. While no clinical trials have been reported for Forsythoside B itself, its parent plant, Forsythia suspensa, is a well-known component in various traditional Chinese medicine formulations. The compound's potent neuroprotective and anti-inflammatory activities make it a promising lead for further drug discovery efforts targeting conditions like stroke, neurodegenerative diseases, and severe inflammatory disorders. |
| Molecular Formula |
C34H44O19
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|---|---|
| Molecular Weight |
756.70176
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| Exact Mass |
756.247
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| CAS # |
81525-13-5
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| PubChem CID |
23928102
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| Appearance |
White to light yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
1040.3±65.0 °C at 760 mmHg
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| Flash Point |
323.9±27.8 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.696
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| LogP |
1.87
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
53
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| Complexity |
1190
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| Defined Atom Stereocenter Count |
13
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| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)O[C@@H]2[C@H]([C@@H](O[C@@H]([C@H]2OC(=O)/C=C/C3=CC(=C(C=C3)O)O)CO[C@H]4[C@@H]([C@](CO4)(CO)O)O)OCCC5=CC(=C(C=C5)O)O)O)O)O)O
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| InChi Key |
JMBINOWGIHWPJI-UNSOMVRXSA-N
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| InChi Code |
InChI=1S/C34H44O19/c1-15-24(41)25(42)26(43)32(50-15)53-29-27(44)31(47-9-8-17-3-6-19(37)21(39)11-17)51-22(12-48-33-30(45)34(46,13-35)14-49-33)28(29)52-23(40)7-4-16-2-5-18(36)20(38)10-16/h2-7,10-11,15,22,24-33,35-39,41-46H,8-9,12-14H2,1H3/b7-4+/t15-,22+,24-,25+,26+,27+,28+,29+,30-,31+,32-,33+,34+/m0/s1
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| Chemical Name |
[(2R,3R,4R,5R,6R)-2-[[(2R,3R,4R)-3,4-dihydroxy-4-(hydroxymethyl)oxolan-2-yl]oxymethyl]-6-[2-(3,4-dihydroxyphenyl)ethoxy]-5-hydroxy-4-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-3-yl] (E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
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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 : ~125 mg/mL (~165.19 mM)
H2O : ~110 mg/mL (~145.37 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.75 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 (2.75 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 (2.75 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: 100 mg/mL (132.15 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 | 1.3215 mL | 6.6076 mL | 13.2153 mL | |
| 5 mM | 0.2643 mL | 1.3215 mL | 2.6431 mL | |
| 10 mM | 0.1322 mL | 0.6608 mL | 1.3215 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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