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| Targets |
The targets of Engeletin are TLR4 (Toll-like receptor 4) and NF-κB (nuclear factor κB) signaling pathway-related proteins (including NF-κB p65 subunit and its phosphorylated form p-NF-κB p65)[1]
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| ln Vitro |
Hymenaea martiana yields a flavanonol glycoside called elenetin, which suppresses the activation of the NF-κB signaling pathway[1].
1. Inhibitory activity on cellular inflammatory factors: Mouse endometrial epithelial cells (mEECs) were used to establish a lipopolysaccharide (LPS)-induced cellular inflammation model, followed by treatment with Engeletin at concentrations of 20 μM and 40 μM. The results showed that compared with the LPS alone group, Engeletin significantly reduced the mRNA expression levels of inflammatory factors TNF-α (tumor necrosis factor-α), IL-1β (interleukin-1β), and IL-6 (interleukin-6) in cells, and the inhibitory effect at 40 μM was better than that at 20 μM[1] 2. Inhibitory activity on TLR4-NF-κB pathway: In the aforementioned mEECs experiment, Western blot results showed that Engeletin (20 μM, 40 μM) concentration-dependently decreased LPS-induced TLR4 protein expression, and significantly inhibited the phosphorylation level of NF-κB p65 (p-NF-κB p65), indicating that it exerts anti-inflammatory effects by blocking TLR4-mediated NF-κB activation[1] |
| ln Vivo |
By activating the NF-κB pathway, reducing the production of inflammatory mediators (iNOS and COX-2), and suppressing the expression of TLR4-signaling downstream molecules like MyD88, IRAK1, TRAF6, and TAK1 proteins, elenetin (25, 50, and 100 mg/kg, ip) significantly reduces LPS-induced myeloperoxidase activity in mice[1].
1. Pathological improvement of LPS-induced endometritis in mice: ICR mice were used to establish an endometritis model by intrauterine injection of 25 μg LPS, and then treated with Engeletin at doses of 10 mg/kg and 20 mg/kg via intraperitoneal injection. HE staining of pathological sections showed that compared with the model group, the Engeletin treatment groups had significantly reduced inflammatory cell infiltration (e.g., neutrophils) in uterine tissues, alleviated damage to endometrial epithelial cells, and relieved uterine tissue edema; the improvement effect at 20 mg/kg was more significant[1] 2. Inhibitory effect on inflammatory factors in vivo: In the aforementioned animal model, detection of inflammatory factor levels in mouse uterine tissue homogenates showed that Engeletin (10 mg/kg, 20 mg/kg) significantly reduced the protein expression levels of TNF-α, IL-1β, and IL-6 in uterine tissues; meanwhile, Western blot results showed that Engeletin downregulated TLR4 protein expression and the phosphorylation level of NF-κB p65 in uterine tissues, further verifying its anti-inflammatory effect by inhibiting the TLR4-NF-κB pathway in vivo[1] |
| Cell Assay |
1. Culture and treatment protocol for mEECs: mEECs were seeded in medium containing serum and cultured in a 37℃, 5% CO₂ incubator until the logarithmic growth phase; the cells were then divided into 4 groups: normal control group (medium only), LPS model group (1 μg/mL LPS), Engeletin low-dose group (1 μg/mL LPS + 20 μM Engeletin), and Engeletin high-dose group (1 μg/mL LPS + 40 μM Engeletin); after co-culturing for a specified time, the cells were collected for subsequent detection[1]
2. RT-PCR protocol for detecting inflammatory factor mRNA: Total RNA was extracted from the treated mEECs, and RNA purity and integrity were tested; cDNA was synthesized using RNA as a template, and then real-time fluorescent quantitative PCR amplification was performed on the cDNA of TNF-α, IL-1β, and IL-6 with specific primers; a housekeeping gene (e.g., GAPDH) was used as an internal reference, and the relative expression levels of target genes were calculated to analyze the effect of Engeletin on inflammatory factor mRNA levels[1] 3. Western blot protocol for detecting pathway proteins: Total protein was extracted from the treated mEECs by adding protein lysis buffer, and protein concentration was determined; equal amounts of protein were subjected to SDS-PAGE gel electrophoresis, and then the protein was transferred to a PVDF membrane; the membrane was blocked with blocking solution, followed by incubation with primary antibodies against TLR4, p-NF-κB p65, NF-κB p65, and internal reference protein (e.g., β-actin) overnight, and then incubation with corresponding secondary antibodies; finally, chemiluminescence was used for development, and the gray values of protein bands were analyzed to calculate the relative protein expression levels[1] |
| Animal Protocol |
1. Establishment protocol for mouse endometritis model: Female ICR mice (specific week of age) were selected and adaptively fed, and the estrous cycle of mice was determined by vaginal smears; after anesthesia, 25 μg LPS (dissolved in sterile normal saline) was slowly injected into the uterine cavity of mice via the vagina to establish the endometritis model; the normal control group was injected with the same volume of sterile normal saline into the uterine cavity[1]
2. Engeletin administration and animal grouping protocol: The modeled mice were randomly divided into 3 groups: model group (intraperitoneal injection of normal saline), Engeletin low-dose group (intraperitoneal injection of 10 mg/kg Engeletin), and Engeletin high-dose group (intraperitoneal injection of 20 mg/kg Engeletin); the normal control group was injected with the same volume of normal saline intraperitoneally; the administration was performed 1 hour before LPS injection, and then once a day for 3 consecutive days[1] 3. Animal sample collection and detection protocol: After the last administration, the mice were sacrificed and the uterine tissues were quickly removed; part of the uterine tissue was fixed with 4% paraformaldehyde, routinely paraffin-embedded, sectioned, and stained with HE; pathological changes were observed under a light microscope and pathological scores were performed; another part of the uterine tissue was ground into a homogenate, and the supernatant was collected after centrifugation for detecting the protein levels of inflammatory factors; the remaining uterine tissue was used to extract total protein, and the expression of TLR4, p-NF-κB p65 and other proteins was detected by Western blot[1] |
| References | |
| Additional Infomation |
Engeletin has been reported to be found in camellia (Camellia reticulata), white locust (Osyris alba), and other organisms with relevant data. Engeletin is a metabolite found or produced by Saccharomyces cerevisiae. 1. Background of Engeletin's Compounds: Engeletin is a naturally occurring flavonoid (the plant source is not specifically mentioned in the literature). Previous studies have shown that it may have anti-inflammatory and antioxidant biological activities. This study further confirms its therapeutic potential in inflammatory diseases such as endometritis [1]
2. Mechanism of action details: The core mechanism of empagletin in alleviating LPS-induced endometritis is "inhibition of TLR4-mediated NF-κB activation"—LPS can bind to TLR4, initiate downstream signaling pathways, lead to phosphorylation of NF-κB p65 and entry into the cell nucleus, thereby regulating the expression of inflammatory factor genes; however, empagletin can downregulate TLR4 protein expression and reduce the phosphorylation level of NF-κB p65, thereby inhibiting the production and release of inflammatory factors (TNF-α, IL-1β, IL-6), and ultimately alleviating inflammatory damage [1] 3. Association with disease indications: This study clearly confirms that empagletin has a therapeutic effect on LPS-induced endometritis in mice, providing experimental evidence for its potential therapeutic effect on endometritis (especially infection-related inflammation) [1] |
| Molecular Formula |
C₂₁H₂₂O₁₀
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|---|---|
| Molecular Weight |
434.39
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| Exact Mass |
434.121
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| CAS # |
572-31-6
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| PubChem CID |
6453452
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| Appearance |
White to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
820.0±65.0 °C at 760 mmHg
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| Melting Point |
176-177ºC
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| Flash Point |
289.5±27.8 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.746
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| LogP |
0.25
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
638
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)O[C@@H]2[C@H](OC3=CC(=CC(=C3C2=O)O)O)C4=CC=C(C=C4)O)O)O)O
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| InChi Key |
VQUPQWGKORWZII-WDPYGAQVSA-N
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| InChi Code |
InChI=1S/C21H22O10/c1-8-15(25)17(27)18(28)21(29-8)31-20-16(26)14-12(24)6-11(23)7-13(14)30-19(20)9-2-4-10(22)5-3-9/h2-8,15,17-25,27-28H,1H3/t8-,15-,17+,18+,19+,20-,21-/m0/s1
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| Chemical Name |
(2R,3R)-5,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy-2,3-dihydrochromen-4-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 : ≥ 100 mg/mL (~230.21 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.79 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 (4.79 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 (4.79 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 | 2.3021 mL | 11.5104 mL | 23.0208 mL | |
| 5 mM | 0.4604 mL | 2.3021 mL | 4.6042 mL | |
| 10 mM | 0.2302 mL | 1.1510 mL | 2.3021 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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