| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
- Crocin II targets inflammatory-related enzymes and mediators, including inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). It inhibits nitric oxide (NO) production with an IC50 of 18.2 μM and prostaglandin E2 (PGE2) production with an IC50 of 22.5 μM in LPS-stimulated RAW264.7 macrophages [1]
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| ln Vitro |
- In LPS-stimulated RAW264.7 murine macrophages, Crocin II inhibited NO production in a concentration-dependent manner. At 10 μM, 20 μM, and 40 μM, it reduced NO levels by 28%, 52%, and 76%, respectively, compared to the LPS-only group [1]
- Crocin II suppressed PGE2 production in LPS-activated RAW264.7 cells. At 10 μM, 20 μM, and 40 μM, PGE2 levels were decreased by 22%, 48%, and 70%, respectively, relative to the LPS-treated control [1] - Western blot analysis showed Crocin II downregulated iNOS and COX-2 protein expression in LPS-stimulated RAW264.7 cells. At 40 μM, iNOS protein levels were reduced by 68% and COX-2 protein levels by 62% [1] - RT-PCR results indicated Crocin II decreased iNOS and COX-2 mRNA expression in LPS-induced RAW264.7 macrophages. At 40 μM, iNOS mRNA was reduced by 72% and COX-2 mRNA by 65% [1] - Crocin II inhibited the NF-κB signaling pathway in LPS-stimulated RAW264.7 cells, as evidenced by reduced phosphorylation and nuclear translocation of the NF-κB p65 subunit [1] |
| ln Vivo |
- In the carrageenan-induced mouse paw edema model, oral administration of Crocin II (20 mg/kg, 40 mg/kg, 80 mg/kg) significantly inhibited paw edema. At 4 hours post-carrageenan injection, edema inhibition rates were 25%, 42%, and 60%, respectively, compared to the vehicle control [1]
- Crocin II (40 mg/kg, 80 mg/kg, oral) reduced tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) levels in paw tissues of carrageenan-treated mice. TNF-α levels were decreased by 38% and 55%, while IL-1β levels were reduced by 35% and 52%, respectively [1] - Histopathological examination revealed Crocin II (80 mg/kg, oral) attenuated carrageenan-induced inflammatory cell infiltration and tissue edema in mouse paw tissues [1] |
| Cell Assay |
- RAW264.7 cell culture and treatment: RAW264.7 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin at 37°C in a 5% CO₂ incubator. Cells were seeded into 96-well plates (5×10⁴ cells/well) for NO/PGE2 detection or 6-well plates (2×10⁶ cells/well) for western blot/RT-PCR. After 24-hour culture, cells were pretreated with Crocin II (0 μM, 10 μM, 20 μM, 40 μM) for 1 hour, then stimulated with LPS (1 μg/mL) for 24 hours [1]
- NO detection: 100 μL of cell supernatant was mixed with 100 μL of Griess reagent in a 96-well plate, incubated at room temperature for 15 minutes, and absorbance was measured at 540 nm. NO concentration was calculated using a sodium nitrite standard curve [1] - PGE2 detection: PGE2 levels in supernatants were measured via ELISA. Supernatant was added to antibody-coated wells, followed by detection antibody and enzyme conjugate. After incubation and washing, substrate solution was added, and absorbance was read at 450 nm. PGE2 concentration was determined using a standard curve [1] - Western blot for iNOS/COX-2/NF-κB p65: Total protein was extracted from cells using RIPA lysis buffer with protease inhibitors. Protein concentration was measured via BCA assay. 30 μg of protein was separated by SDS-PAGE, transferred to PVDF membranes, blocked with 5% non-fat milk for 1 hour, and incubated with primary antibodies (iNOS, COX-2, phospho-NF-κB p65, NF-κB p65, GAPDH) at 4°C overnight. Membranes were then incubated with secondary antibodies for 1 hour at room temperature, and bands were visualized via enhanced chemiluminescence and quantified [1] - RT-PCR for iNOS/COX-2: Total RNA was extracted using Trizol reagent. 1 μg of RNA was reverse-transcribed to cDNA. PCR amplification was performed with specific primers for iNOS, COX-2, and GAPDH. Products were separated by agarose gel electrophoresis, stained with ethidium bromide, and bands were quantified [1] |
| Animal Protocol |
- Animal model: Male ICR mice (20-25 g) were used. Paw edema was induced by subcutaneous injection of 0.1 mL of 1% carrageenan into the right hind paw [1]
- Drug preparation and administration: Crocin II was dissolved in 0.5% carboxymethyl cellulose sodium (CMC-Na) solution. Mice were randomly divided into 4 groups (n=6/group): vehicle control (0.5% CMC-Na, oral), Crocin II 20 mg/kg (oral), Crocin II 40 mg/kg (oral), Crocin II 80 mg/kg (oral). Drugs were administered 1 hour before carrageenan injection [1] - Paw volume measurement: Paw volume was measured using a plethysmometer at 0, 1, 2, 3, and 4 hours post-carrageenan injection. Edema volume was calculated as the difference between the right (edematous) and left (normal) paw volumes [1] - Sample collection and analysis: At 4 hours post-carrageenan injection, mice were euthanized. Paw tissues were homogenized in physiological saline and centrifuged to obtain supernatants. TNF-α and IL-1β levels in supernatants were measured via ELISA. For histopathology, paw tissues were fixed in 10% formalin, embedded in paraffin, sectioned, stained with hematoxylin and eosin (H&E), and observed under a light microscope [1] |
| Toxicity/Toxicokinetics |
In in vivo studies, no significant acute toxicity was observed in mice after oral administration of Crocin II at doses up to 80 mg/kg. Mice did not exhibit abnormal behavior, weight loss, or organ damage (observed visually) [1]
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| References | |
| Additional Infomation |
β-D-Gentiobiose-β-D-glucosylcrocin is a diester formed by the condensation of the carboxylic acid group of β-D-gentiobiose-crocin with the terminal hydroxyl group of β-D-glucopyranose. It is a β-D-glucoside and diester.
It has been reported that gardenia (Gardenia jasminoides) and saffron (Crocus sativus) contain crocin gentiobiose-glucose ester, and there is relevant data. - Crataegrin II is a crocin derivative isolated from processed gardenia (Gardenia jasminoides), a traditional Chinese medicine that is widely used for its anti-inflammatory properties[1]. - Crataegrin II's anti-inflammatory mechanism involves inhibiting the NF-κB signaling pathway, thereby further reducing the expression of pro-inflammatory enzymes (iNOS, COX-2) and cytokines (TNF-α, IL-1β)[1]. |
| Molecular Formula |
C38H54O19
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|---|---|
| Molecular Weight |
814.8240
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| Exact Mass |
814.325
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| CAS # |
55750-84-0
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| PubChem CID |
9940690
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
1032.1±65.0 °C at 760 mmHg
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| Flash Point |
309.8±27.8 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.636
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| LogP |
1.64
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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 |
17
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| Heavy Atom Count |
57
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| Complexity |
1550
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| Defined Atom Stereocenter Count |
15
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| SMILES |
C/C(=C\C=C\C=C(/C)\C=C\C=C(/C)\C(=O)O[C@H]1[C@@H]([C@H]([C@@H]([C@H](O1)CO[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)O)O)O)/C=C/C=C(\C)/C(=O)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O
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| InChi Key |
CZSBHMFVVLYIQQ-DRVLGOCHSA-N
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| InChi Code |
InChI=1S/C38H54O19/c1-18(11-7-13-20(3)34(50)56-37-32(48)29(45)26(42)23(16-40)54-37)9-5-6-10-19(2)12-8-14-21(4)35(51)57-38-33(49)30(46)27(43)24(55-38)17-52-36-31(47)28(44)25(41)22(15-39)53-36/h5-14,22-33,36-49H,15-17H2,1-4H3/b6-5+,11-7+,12-8+,18-9+,19-10+,20-13+,21-14+/t22-,23-,24-,25-,26-,27-,28+,29+,30+,31-,32-,33-,36-,37+,38+/m1/s1
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| Chemical Name |
1-O-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] 16-O-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl] (2E,4E,6E,8E,10E,12E,14E)-2,6,11,15-tetramethylhexadeca-2,4,6,8,10,12,14-heptaenedioate
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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) |
DMSO : ~25 mg/mL (~30.68 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.07 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 25.0 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: ≥ 2.5 mg/mL (3.07 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2273 mL | 6.1363 mL | 12.2726 mL | |
| 5 mM | 0.2455 mL | 1.2273 mL | 2.4545 mL | |
| 10 mM | 0.1227 mL | 0.6136 mL | 1.2273 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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