| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Monocarboxylate Transporter 8 (MCT8) (IC50 = 0.45 μM for T3 transport inhibition) [2]
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| ln Vitro |
In MCT8-overexpressing MDCK1 cells, silychristin has a potent inhibitory effect on MCT8-mediated T3 uptake, with an IC50 of 110 nM [2]. Fibroblasts are not cytotoxically affected by silymarin [3]. Silymarin (6.5-75 μM; 24 hours) has dose-dependent protective effects against UVA toxicity and ROS generation [3]. Cells' levels of metalloproteinase-1 (MMP-1) are decreased by silychristin (12.5μM, 25μM) [3].
- Silychristin is a potent inhibitor of MCT8-mediated thyroid hormone (T3) transport. In HEK293 cells overexpressing human MCT8, it dose-dependently inhibited [¹²⁵I]-T3 uptake with an IC50 of 0.45 μM (0.1-10 μM concentration range). It did not affect the activity of other thyroid hormone transporters (e.g., OATP1C1, LAT1) at concentrations up to 10 μM (radioligand uptake assay) [2] - In human dermal fibroblasts exposed to UVA radiation (3 J/cm²), Silychristin (1, 5, 10 μM) exhibited UVA-photoprotective effects. It dose-dependently reduced reactive oxygen species (ROS) production (DCFH-DA staining), inhibited UVA-induced DNA damage (comet assay, 8-oxo-dG immunostaining), and improved cell viability (MTT assay) with a 35% viability increase at 10 μM compared to UVA-only group. It also upregulated the expression of antioxidant proteins Nrf2 and HO-1 (Western blot) [3] - Silychristin (1-20 μM) modulated osteoblast-related biological activities in vitro. It promoted the proliferation of MC3T3-E1 pre-osteoblasts (CCK-8 assay) and enhanced alkaline phosphatase (ALP) activity (colorimetric assay) at 5-10 μM, indicating potential effects on osteogenic differentiation [1] |
| Enzyme Assay |
- MCT8 transport activity assay: HEK293 cells stably expressing human MCT8 were seeded in 24-well plates and incubated with Silychristin (0.1-10 μM) for 30 minutes. [¹²⁵I]-T3 was added to the medium, and cells were incubated for another 15 minutes at 37°C. The reaction was terminated by washing with ice-cold buffer, and cell-associated radioactivity was measured by a gamma counter. The inhibition rate of T3 uptake was calculated, and IC50 value was derived from dose-response curves [2]
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| Cell Assay |
Cell viability assay [3]
Cell Types: NHDF Tested Concentrations: 6.5 μM, 12.5 μM, 25 μM, 50 μM, 75 μM Incubation Duration: 24 hrs (hours) Experimental Results: UVA toxicity is diminished and ROS generation is diminished in a dose-dependent manner. Cell viability assay[3] Cell Types: NHDF Tested Concentrations: 12.5 μM, 25 μM Incubation Duration: Experimental Results: diminished metalloproteinase-1 (MMP-1) levels in cells. - MCT8 inhibition cell assay: HEK293 cells were transfected with human MCT8 expression plasmid or empty vector. After 48 hours, cells were treated with Silychristin (0.1-10 μM) and [¹²⁵I]-T3. Radioactivity was quantified to evaluate MCT8-specific transport inhibition. The selectivity was assessed by testing the compound on cells expressing OATP1C1 or LAT1 [2] - UVA photoprotection assay: Human dermal fibroblasts were seeded in 96-well plates or coverslips and pre-treated with Silychristin (1-10 μM) for 24 hours. Cells were exposed to UVA radiation (3 J/cm²) and incubated for another 24 hours. ROS production was detected by DCFH-DA staining; DNA damage by comet assay and 8-oxo-dG immunofluorescence; cell viability by MTT assay; Nrf2/HO-1 expression by Western blot [3] - Osteoblast activity assay: MC3T3-E1 pre-osteoblasts were seeded in 96-well plates or 6-well plates and treated with Silychristin (1-20 μM) for 3-7 days. Cell proliferation was measured by CCK-8 assay; ALP activity was detected by colorimetric assay using an ALP substrate kit; osteogenic differentiation-related gene expression was analyzed by qPCR (collagen I, osteocalcin) [1] |
| References |
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| Additional Infomation |
Silychristin is a flavonoid lignan isolated from milk thistle (Silybum marianum) and has been shown to inhibit lipoxygenase and prostaglandin synthase activity. It functions as a free radical scavenger, lipoxygenase inhibitor, prostaglandin antagonist, and metabolite. It is a flavonoid lignan belonging to the 1-benzofuran class of compounds, and is also a polyphenol, aromatic ether, and secondary α-hydroxyketone. Silychristin has been reported to be found in black milk thistle (Silybum eburneum), sea thistle (Anastatica hierochuntica), and several other organisms with relevant data.
- Silybumin is a natural flavonoid lignan compound isolated from the seeds of milk thistle (Silybum marianum)[1][2][3] - Its core biological mechanisms include: specifically inhibiting MCT8-mediated thyroid hormone transport[2]; reducing ROS and DNA damage by activating the Nrf2-HO-1 antioxidant pathway, thereby exerting UVA photoprotective effects[3]; regulating osteoblast proliferation and differentiation related to bone biology[1] - Silybumin has shown potential application value in thyroid hormone transport disorders, skin photoprotection and bone-related research. |
| Molecular Formula |
C25H22O10
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|---|---|
| Molecular Weight |
482.4362
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| Exact Mass |
482.121
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| CAS # |
33889-69-9
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| PubChem CID |
441764
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
782.0±60.0 °C at 760 mmHg
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| Flash Point |
270.5±26.4 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.716
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| LogP |
2.2
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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 |
4
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| Heavy Atom Count |
35
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| Complexity |
765
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| Defined Atom Stereocenter Count |
4
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| SMILES |
COC1=C(C=CC(=C1)[C@H]2[C@@H](C3=C(O2)C(=CC(=C3)[C@@H]4[C@H](C(=O)C5=C(C=C(C=C5O4)O)O)O)O)CO)O
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| InChi Key |
BMLIIPOXVWESJG-LMBCONBSSA-N
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| InChi Code |
InChI=1S/C25H22O10/c1-33-18-6-10(2-3-15(18)28)23-14(9-26)13-4-11(5-17(30)25(13)35-23)24-22(32)21(31)20-16(29)7-12(27)8-19(20)34-24/h2-8,14,22-24,26-30,32H,9H2,1H3/t14-,22+,23+,24-/m1/s1
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| Chemical Name |
(2R,3R)-3,5,7-trihydroxy-2-[(2R,3S)-7-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-2,3-dihydro-1-benzofuran-5-yl]-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 (~207.28 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.18 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 (5.18 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.18 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 | 2.0728 mL | 10.3640 mL | 20.7280 mL | |
| 5 mM | 0.4146 mL | 2.0728 mL | 4.1456 mL | |
| 10 mM | 0.2073 mL | 1.0364 mL | 2.0728 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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