| Size | Price | Stock | Qty |
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| Targets |
The target of Saikosaponin B2 involves hepatitis C virus (HCV) entry-related molecules, including HCV E1/E2 glycoproteins and host cell surface receptors (CD81, SR-BI); the EC50 for inhibiting HCV (genotype 2a JFH-1) entry is 0.8 μM [1]
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| ln Vitro |
1. Inhibition of HCV entry (Reference [1]): Saikosaponin B2 (0.1-10 μM) was tested on Huh7.5.1 cells infected with HCV (genotype 2a JFH-1). It selectively inhibited HCV entry without affecting viral replication or assembly. The EC50 for reducing HCV RNA levels was 0.8 μM; at 5 μM, it inhibited HCV entry by >90% (detected by qPCR). It also inhibited entry of other HCV genotypes (1b, 3a) with EC50 values of 1.2 μM and 1.5 μM respectively. Immunofluorescence showed it reduced HCV E2 glycoprotein binding to Huh7.5.1 cells (by 65% at 5 μM) [1]
2. Antiproliferative activity on breast cancer cells (Reference [2]): Saikosaponin B2 (5-40 μM) inhibited proliferation of MCF-7 (estrogen receptor-positive) and MDA-MB-231 (triple-negative) breast cancer cells. The IC50 values were 15 μM (MCF-7) and 12 μM (MDA-MB-231) after 48 hours (CCK-8 assay). BrdU incorporation assay showed it reduced DNA synthesis by 58% (MCF-7) and 62% (MDA-MB-231) at 20 μM [2] 3. Inhibition of breast cancer cell migration and invasion (Reference [2]): Scratch wound healing assay showed Saikosaponin B2 (20 μM) reduced MCF-7 cell migration rate by 45% (24 hours) and MDA-MB-231 by 52%. Transwell invasion assay showed it decreased invasive cell numbers by 60% (MCF-7) and 65% (MDA-MB-231) at 20 μM. Western blot showed it downregulated MMP-9 protein expression by 55% (MCF-7) and 60% (MDA-MB-231) at 20 μM [2] 4. Induction of breast cancer cell apoptosis (Reference [2]): Flow cytometry (Annexin V-FITC/PI) showed Saikosaponin B2 (20 μM) increased apoptotic rates of MCF-7 (from 3.1% to 28.5%) and MDA-MB-231 (from 2.8% to 32.1%) after 24 hours. Western blot showed upregulated Bax (pro-apoptotic) by 2.3-fold and downregulated Bcl-2 (anti-apoptotic) by 50% in both cell lines [2] 5. Regulation of signaling pathways (Reference [2]): Western blot showed Saikosaponin B2 (10, 20 μM) dose-dependently reduced phosphorylation of AKT (p-AKT) and ERK (p-ERK) in MCF-7 and MDA-MB-231 cells. At 20 μM, p-AKT was reduced by 65% (MCF-7) and 70% (MDA-MB-231), and p-ERK by 60% (MCF-7) and 63% (MDA-MB-231) [2] |
| ln Vivo |
1. Inhibition of HCV replication in humanized liver mice (Reference [1]): FRG mice with human hepatocyte engraftment were infected with HCV JFH-1 (1×10⁶ FFU/mouse). Mice were divided into two groups (n=6): control (vehicle) and Saikosaponin B2 (10 mg/kg, intraperitoneal injection, once daily for 14 days). Saikosaponin B2 reduced serum HCV RNA levels by 3.2 log₁₀ IU/mL (from 6.5 log₁₀ IU/mL to 3.3 log₁₀ IU/mL) and liver HCV RNA by 2.8 log₁₀ IU/g. Immunohistochemistry showed reduced HCV Core protein expression in liver tissues (by 70%) [1]
2. Inhibition of breast cancer xenograft growth (Reference [2]): Female BALB/c nude mice (4-6 weeks old) were subcutaneously injected with 5×10⁶ MDA-MB-231 cells. When tumors reached ~100 mm³, mice were divided into three groups (n=6): control (vehicle), Saikosaponin B2 5 mg/kg, and Saikosaponin B2 10 mg/kg (intraperitoneal injection, twice weekly for 3 weeks). The 10 mg/kg group showed: (1) 55% reduction in tumor volume (from 920 ± 85 mm³ to 410 ± 52 mm³); (2) 58% reduction in tumor weight (from 0.85 ± 0.09 g to 0.36 ± 0.04 g); (3) reduced Ki-67 (proliferation marker) expression by 62% and MMP-9 by 65% (immunohistochemistry) [2] |
| Enzyme Assay |
1. MMP-9 activity assay (Reference [2]): MDA-MB-231 cells were treated with Saikosaponin B2 (10, 20 μM) for 24 hours. Culture supernatant was collected and mixed with MMP-9 substrate (fluorogenic peptide) in reaction buffer (50 mM Tris-HCl, pH 7.5, 10 mM CaCl₂). Incubate at 37°C for 1 hour. Fluorescence intensity (excitation 320 nm, emission 405 nm) was measured to calculate MMP-9 activity. Saikosaponin B2 reduced MMP-9 activity by 40% (10 μM) and 65% (20 μM) compared to control [2]
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| Cell Assay |
1. HCV entry assay (Reference [1]): Huh7.5.1 cells were seeded in 24-well plates at 5×10⁴ cells/well. Saikosaponin B2 (0.1-10 μM) was added 1 hour before HCV JFH-1 infection (MOI=0.1). After 4 hours, cells were washed to remove unbound virus and drug, then cultured for 72 hours. Total RNA was extracted, and HCV RNA levels were quantified by qPCR (primers targeting HCV 5' UTR). For E2 binding assay, cells were incubated with HCV E2-Fc fusion protein + Saikosaponin B2 (5 μM) for 1 hour, washed, and stained with Alexa Fluor 488-conjugated secondary antibody. Fluorescence intensity was measured by flow cytometry [1]
2. Breast cancer cell proliferation assay (Reference [2]): MCF-7 and MDA-MB-231 cells were seeded in 96-well plates at 3×10³ cells/well. Saikosaponin B2 (5-40 μM) was added, and cells were cultured for 24, 48, 72 hours. CCK-8 reagent was added, and absorbance at 450 nm was measured to calculate cell viability and IC50. For BrdU assay, cells were incubated with BrdU for 2 hours after drug treatment, fixed, and stained with anti-BrdU antibody; positive cells were counted by microscopy [2] 3. Breast cancer cell migration and invasion assay (Reference [2]): For scratch assay, confluent cells were scratched with a pipette tip, washed, and cultured with Saikosaponin B2 (20 μM). Wound closure was imaged at 0 and 24 hours, and scratch width was measured. For Transwell assay, cells were seeded in the upper chamber (with Matrigel for invasion) with Saikosaponin B2 (20 μM), and medium with 10% FBS was added to the lower chamber. After 24 hours, invasive cells on the lower membrane were fixed, stained with crystal violet, and counted [2] 4. Apoptosis and Western blot assay (Reference [2]): Cells were treated with Saikosaponin B2 (20 μM) for 24 hours. For apoptosis, cells were stained with Annexin V-FITC and PI, then analyzed by flow cytometry. For Western blot, total protein was extracted, quantified by BCA assay, and 30 μg protein per lane was separated by SDS-PAGE. Membranes were probed with antibodies against Bax, Bcl-2, p-AKT, AKT, p-ERK, ERK, MMP-9, and β-actin (internal control); bands were visualized by ECL [2] |
| Animal Protocol |
1. HCV-infected humanized liver mouse model (Reference [1]): FRG mice (6-8 weeks old) were transplanted with human hepatocytes (1×10⁶ cells/mouse) via intrasplenic injection. After 8 weeks (hepatocyte engraftment >70%), mice were infected with HCV JFH-1 (1×10⁶ FFU/mouse) via tail vein injection. After 7 days (viral load >6 log₁₀ IU/mL), mice were divided into groups. Saikosaponin B2 was dissolved in DMSO (10%) + normal saline (90%) to 1 mg/mL, administered intraperitoneally at 10 mg/kg once daily for 14 days. Control mice received DMSO-saline solution. Serum was collected every 3 days to measure HCV RNA, and liver tissues were excised after euthanasia for RNA and immunohistochemical analysis [1]
2. Breast cancer xenograft model (Reference [2]): Female BALB/c nude mice (4-6 weeks old) were housed under SPF conditions. 5×10⁶ MDA-MB-231 cells (resuspended in 100 μL PBS + Matrigel 1:1) were subcutaneously injected into the right flank. When tumors reached ~100 mm³, mice were grouped. Saikosaponin B2 was dissolved in DMSO (5%) + corn oil (95%) to 0.5 mg/mL and 1 mg/mL. Mice were injected intraperitoneally with 5 mg/kg or 10 mg/kg twice weekly for 3 weeks. Tumor volume was measured every 3 days (Volume = length×width²/2), and body weight was recorded weekly. After treatment, tumors were excised, weighed, and fixed in 4% paraformaldehyde for immunohistochemistry [2] |
| Toxicity/Toxicokinetics |
1. Safety in humanized liver mice (Reference [1]): Saikosaponin B2 (10 mg/kg, intraperitoneal injection) did not cause weight loss (control group: 22.5 ± 1.2 g; treatment group: 21.8 ± 0.9 g) or abnormal serum ALT/AST levels (ALT: control group 35 ± 5 U/L, treatment group 38 ± 6 U/L; AST: control group 85 ± 8 U/L, treatment group 82 ± 7 U/L). Histological examination of the liver showed no obvious inflammation or necrosis [1] 2. Safety in nude mice (Reference [2]): Saikosaponin B2 (5, 10 mg/kg, intraperitoneal injection) did not affect the weight of mice for 3 consecutive weeks (control group: 18.2 ± 0.8 g; 10 mg/kg group: 17.5 ± 0.7 g), nor did it cause pathological damage (HE staining) to the liver, kidneys, heart or lungs. No deaths were observed [2]
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| References | |
| Additional Infomation |
Saikosaponin B2 is a saikosaponin. It has been reported that saikosaponin B2 exists in Bupleurum falcatum, and relevant data are available. 1. Source and basic properties (References [1][2]): Saikosaponin B2 is a triterpenoid saponin isolated from the roots of Bupleurum chinense DC. Bupleurum scorzonerifolium Willd. is a traditional Chinese medicine used for anti-inflammatory and hepatoprotective purposes [1][2]
2. Anti-HCV mechanism (reference [1]): Sauceoside B2 inhibits HCV entry by blocking the interaction between HCV E2 glycoprotein and host cell receptors (CD81, SR-BI) without affecting the steps after entry (viral RNA replication, protein translation or viral particle assembly/release) [1] 3. Anti-breast cancer mechanism (reference [2]): Sauceoside B2 exerts its anti-breast cancer effect through the following three pathways: (1) inhibiting the PI3K/AKT and MAPK/ERK signaling pathways to inhibit cell proliferation; (2) downregulating MMP-9 to reduce cell migration/invasion; (3) upregulating the Bax/Bcl-2 ratio to induce apoptosis [2] |
| Molecular Formula |
C42H68O13
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|---|---|
| Molecular Weight |
780.9815
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| Exact Mass |
780.466
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| CAS # |
58316-41-9
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| PubChem CID |
21637642
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
909.9±65.0 °C at 760 mmHg
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| Melting Point |
231-238ºC
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| Flash Point |
504.1±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
3.59
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
55
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| Complexity |
1500
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| Defined Atom Stereocenter Count |
19
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| SMILES |
C[C@@H]1[C@@H]([C@@H]([C@H]([C@@H](O1)O[C@H]2CC[C@]3([C@H]([C@]2(C)CO)CC[C@@]4([C@@H]3C=CC5=C6CC(CC[C@@]6([C@@H](C[C@]54C)O)CO)(C)C)C)C)O)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O)O)O)O
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| InChi Key |
WRYJYFCCMSVEPQ-ORAXXRKOSA-N
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| InChi Code |
InChI=1S/C42H68O13/c1-21-29(47)34(55-35-32(50)31(49)30(48)24(18-43)53-35)33(51)36(52-21)54-28-11-12-38(4)25(39(28,5)19-44)10-13-40(6)26(38)9-8-22-23-16-37(2,3)14-15-42(23,20-45)27(46)17-41(22,40)7/h8-9,21,24-36,43-51H,10-20H2,1-7H3/t21-,24-,25-,26-,27-,28+,29+,30-,31+,32-,33-,34+,35+,36+,38+,39+,40-,41-,42-/m1/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[(2R,3R,4S,5S,6R)-2-[[(3S,4R,4aR,6aR,6bS,8R,8aS,14aR,14bS)-8-hydroxy-4,8a-bis(hydroxymethyl)-4,6a,6b,11,11,14b-hexamethyl-1,2,3,4a,5,6,7,8,9,10,12,14a-dodecahydropicen-3-yl]oxy]-3,5-dihydroxy-6-methyloxan-4-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol
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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 : ~100 mg/mL (~128.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.20 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 (3.20 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 (3.20 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 | 1.2804 mL | 6.4022 mL | 12.8044 mL | |
| 5 mM | 0.2561 mL | 1.2804 mL | 2.5609 mL | |
| 10 mM | 0.1280 mL | 0.6402 mL | 1.2804 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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