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Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB).
For research use only. We do not sell to patients.
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB)[1][4].
IC50 & Target
5-HT2C Receptor
Cellular Effect
Cell Line
Type
Value
Description
References
A549
IC50
> 50 μM
Compound: 19
Cytotoxicity against human A549 cells assessed as induction of cell death incubated for 2 days by MTT assay
Cytotoxicity against human A549 cells assessed as induction of cell death incubated for 2 days by MTT assay
Saikosaponin B1 (10 nM-10 μM, 36 h) reduces the level of glioma-associated oncogene homolog (GLI)-luciferase activity in transfected Shh Light II cells with an IC50 of 241.8 nM[1].
Saikosaponin B1 (5 μM, 6-24 h) does not target GLI transcription factor and it downstream molecules, as Saikisaponin B1 shows no inhibition activity against PGE2 (HY-P3502B)-induced TCF/LEF and GLI activity in transfected LS174T cells, or TNF-α-induced NF-κB in HEK293T cell[1].
Saikosaponin B1 (3 μM, 36 h) fails to inhibit GLI-luciferase activity increased by limiting negative regulation from SUFU in SUFU-knockout Shh Light II cells, indicating Saikosaponin B1 targets Hh pathway via upstream components of SUFU[1].
Saikosaponin B1 (3 μM, 36 h) significantly prevents the increased of Gli1mRNA expression induced by SAG (HY-12848) (a synthetic Hh pathway agonist binds to SMO) in Shh Light II cells with an IC50 of 3.64 μM[1].
Saikosaponin B1 (10 nM-10 μM, 72 h) significantly inhibits the proliferation of DAOY cell line (derived from nodular MB with GLI transcriptional activity)[1].
Saikisaponin B1 (1-10 μM, 0-24 h) decreases expression of TGF-β1-induced HSC activation biomarkers[2].
Saikisaponin B1 (0-10 μM) with biotin-label retains the inhibition activity of fibrotic protein expression in the activated HSC-T6 cells and shows the most remarkable binding to STAT3[2].
Saikisaponin B1 (50 μM) with biotin-label pulls down the STAT3 protein but no obvious interactions with JAK2 or IL-6 in HSC-T6 cells, LX-2 cells, and mouse liver tissues[2].
Saikisaponin B1 (1-10 μM) inhibits STAT3 phosphorylation in Tyr 705 but does not influence Ser 727 phosphorylation in HSC-t6 and LX-2 cells[2].
Saikisaponin B1 (5-10 μM, 24 h) disrupts STAT3 dimerization even in the presence of IL-6 (20 ng/mL) at 10 μM in HSC-T6 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Shh Light II cells transfected with luciferase reporter plasmids and Renilla-TK construct
Concentration:
10 nM-10 μM
Incubation Time:
36 h
Result:
Significantly reduced the level of Gli1 and Ptch 1 mRNA (two transcriptional targets of GLI), which further confirmed the inhibition of Hh signaling.
Showed little cytotoxicity in response to effective concentrations in Shh Light II cells.
Inhibited the mRNA levels of the HSC activation biomarkers (α-SMA, collagen I, and vimentin) in TGF-β1-stimulated rat HSC-T6 cells.
Decreased expression of TGF-β1-induced α-SMA and Collagen I in human LX-2 cells and suggests that Saikisaponin B1 can reduce TGF-β1-induced HSC activation and matrix protein expression.
In Vivo
Saikosaponin B1 (30 mg/kg, i.p., daily for 18 d) significantly inhibits tumor growth and reduces Gli1mRNA in tumor tissues in MB mice subcutaneously allografted with primary MB tumor tissues[1].
Saikosaponin B1 (200 mg/kg, i.p., three times a week from week 4 to week 7) ameliorates the Thioacetamide (TAA) (HY-Y0698)-induced morphological changes and liver damage with decreased collagen deposition in TAA-induced liver fibrosis model[2].
Saikosaponin B1 (10 mg/kg, s.c., twice a week for 4 weeks) attenuates the fibrosis histopathological characteristics of the liver tissues in CCl4-induced liver fibrotic mice[2].
Saikosaponin B1 (20 mg/kg, i.p., for 4 weeks) fails to further reduce liver fibrosis in response to CCl4 in CCl4mediated liver fibrosis STAT3 knockout mice model, suggesting STAT3 knockdown abrogated the antifibrosis effect of Saikosaponin B1[2].
Saikosaponin B1 (2.5-10 mg/kg, i.p., once per day for 7 consecutive days) inhibits pulmonary edema in LPS (HY-D1056)-induced ALI mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
TAA (100 mg/kg, i.p., three times a week)-induced liver fibrosis male Balb/c mice model[2]
Dosage:
5-20 μM, three times a week from week 4 to week 7
Administration:
Intraperitoneal injection (i.p.)
Result:
Decreased the liver/body weight ratio and the serum levels of ALT, AST, and TBIL compared to untreated model group.
Exerted a considerable effect on fibrosis alleviation with 10 mg/kg.
Animal Model:
CCl4- (5 mg/kg of 40% CCl4 in the first week, 3 mg/kg of 40% CCl4 twice a week for another 6 weeks, s.c. )-induced liver fibrotic mice[2]
Dosage:
10 mg/kg, twice a week for 4 weeks
Administration:
Subcutaneous injection (s.c.)
Result:
Exerted protective effect on liver function using the serum levels of ALT, AST, and TBIL.
Downregulated various proinflammatory cytokines (IL-6 and IL-1β) and fibrotic proteins (FN, collagen I , α-SMA and vimentin) in liver tissues.
Resulted in an obvious decrease in p-STAT3 and Gli1 expression levels.
Decreased STAT3 phosphorylation and Gli1 expression in the aHSCs and blocked interaction between STAT3 and Gli1.
Animal Model:
CCl4- (5 mg/kg of 40% CCl4 in the first week, 3 mg/kg of 40% LPS (5 mg/kg, i.p.)-induced ALI mic
Dosage:
2.5-10 mg/kg, once per day for 7 consecutive days
Administration:
Intraperitoneal injection (i.p.)
Result:
Significantly decreased the lung W/D ratios.
Significantly relieved the histological damage induced by LPS in mouse lungs.
Inhibited the expression of the inflammatory factors IL-6, IL-1β, and TNF-α in a dose-dependent manner.
Lowered TLR4 proteins and NF-κB proteins.
DMSO : 100 mg/mL (128.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% Corn Oil
This protocol yields a clear solution of ≥ 100 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (1000.0 mg/mL) to 900 μLCorn oil, and mix evenly.
Solubility: 10 mg/mL (12.80 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 10 mg/mL.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 10 mg/mL (12.80 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (100.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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