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| ln Vitro |
Treatment with Isosilybin B (10-90 μM) for 24 and 48 hours inhibited the growth of human prostate cancer LNCaP cells in a dose- and time-dependent manner, causing an 11-46% decrease in cell number. It also induced a slight but significant increase in cell death at 60 and 90 μM concentrations. [1]
In human prostate cancer 22Rv1 cells, Isosilybin B (10-90 μM) treatment for 24 and 48 hours caused a 7-66% decrease in cell number and a more pronounced increase in cell death (7-16% dead cells at 30-90 μM). [1] Isosilybin B induced a significant G1 phase cell cycle arrest in both LNCaP and 22Rv1 cells, accompanied by a decrease in S phase population. [1] Western blot analysis showed that Isosilybin B treatment decreased protein levels of cyclins (D1, D3, E, A), cyclin-dependent kinases (Cdk4, Cdk2), and Cdc25A in both cell lines. It increased the levels of p27 and p53 in both cell lines, but increased p21 only in LNCaP cells while decreasing it in 22Rv1 cells. [1] Isosilybin B induced apoptotic cell death, as evidenced by a 2-fold increase in apoptotic population in LNCaP cells and a 3- to 4-fold increase in 22Rv1 cells at 60-90 μM after 48 hours (Hoechst staining). [1] Consistent with apoptosis induction, Isosilybin B treatment increased cleavage of PARP, caspase-9, and caspase-3, and decreased the level of survivin in both LNCaP and 22Rv1 cells. [1] In non-neoplastic human prostate epithelial PWR-1E cells, Isosilybin B showed minimal effects on cell growth and viability at 24 hours, but caused a 25% decrease in cell number at 90 μM after 48 hours, suggesting a selective cytotoxicity against cancer cells. [1] An earlier study cited within this review reported an IC50 of 20.5 μM for Isosilybin B in human prostate carcinoma DU145 cells. [1] |
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| Cell Assay |
For cell growth and death assays, LNCaP, 22Rv1, and PWR-1E cells were plated at 40-50% confluency and treated with Isosilybin B (10-90 μM, dissolved in DMSO, final DMSO ≤0.1%) in complete medium for 24 or 48 hours. After treatment, both adherent and non-adherent cells were collected by trypsinization, washed, and counted using a hemocytometer. Cell viability was determined by trypan blue exclusion. [1]
For cell cycle analysis, cells treated with Isosilybin B were collected, suspended in a saponin/PI solution containing propidium iodide and RNase A, incubated overnight at 4°C, and analyzed by flow cytometry to determine DNA content and cell cycle distribution. [1] For apoptosis analysis (Hoechst assay), cells treated with Isosilybin B were collected, stained with DNA-binding dyes Hoechst 33342 and propidium iodide, and apoptotic cells (characteristic nuclear morphology) were quantified by counting under a fluorescence microscope. [1] For western blot analysis, cells treated with Isosilybin B were lysed in a non-denaturing lysis buffer. Equal amounts of protein (50-70 μg) were separated by SDS-PAGE, transferred to nitrocellulose membranes, blocked, and probed with specific primary antibodies against target proteins (cyclins, CDKs, CDKIs, p53, cleaved caspases, PARP, survivin). Proteins were detected using peroxidase-conjugated secondary antibodies and an ECL system. Blots were stripped and reprobed with β-actin or tubulin antibodies for loading normalization. [1] |
| References |
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| Additional Infomation |
Isosilybin B has been reported in Anastatica hierochuntica and Silybum marianum, and relevant data are available. See also: Milk thistle (partial). Isosilybin B is a diastereomer of a flavonoid lignan isolated from silybin (silybin is an extract of milk thistle (Silybum marianum)). It accounts for approximately 2-4.5% (w/w) of silybin. [1] Its anti-prostate cancer activity mechanism involves inducing G1 phase cell cycle arrest and apoptosis. This arrest is associated with downregulation of G1/S phase promoting proteins (cyclins D1, D3, E, A; Cdk4, Cdk2; Cdc25A) and upregulation of CDK inhibitors (p27 and p21 in LNCaP cells). Apoptosis is associated with increased p53 levels, caspase (-9 and -3) activation, PARP cleavage, and downregulation of the anti-apoptotic protein survivin. [1] This study suggests that isosilymarin B and its isoform isosilymarin A may have different cellular targets and potencies due to stereochemical differences. [1]
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| Molecular Formula |
C25H22O10
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|---|---|
| Molecular Weight |
482.43618
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| Exact Mass |
482.121
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| CAS # |
142796-22-3
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| PubChem CID |
10885340
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| Appearance |
White to off-white solid powder
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| Density |
1.527±0.06 g/cm3(Predicted)
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| Boiling Point |
793.0±60.0 °C(Predicted)
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| LogP |
2.362
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| Hydrogen Bond Donor Count |
5
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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 |
750
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| Defined Atom Stereocenter Count |
4
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| SMILES |
COC1=C(C=CC(=C1)[C@H]2[C@@H](OC3=C(O2)C=CC(=C3)[C@@H]4[C@H](C(=O)C5=C(C=C(C=C5O4)O)O)O)CO)O
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| InChi Key |
FDQAOULAVFHKBX-WAABAYLZSA-N
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| InChi Code |
InChI=1S/C25H22O10/c1-32-17-6-11(2-4-14(17)28)24-20(10-26)33-18-7-12(3-5-16(18)34-24)25-23(31)22(30)21-15(29)8-13(27)9-19(21)35-25/h2-9,20,23-29,31H,10H2,1H3/t20-,23-,24-,25+/m0/s1
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| Chemical Name |
(2R,3R)-3,5,7-trihydroxy-2-[(2S,3S)-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-6-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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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