Description |
Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
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Target |
STAT3
NF-κB
ERβ
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In Vitro |
Saikosaponin D (Compound 3) is a triterpene saponin, which inhibits E-selectin, L-selectin and P-selectin binding to THP-1 cells, with IC50s of 1.8 µM, 3.0 µM and 4.3 µM, and such effects are not due to cytotoxic action. Saikosaponin D (1, 5, 10 µM) dose-dependently inhibits the THP-1 adhesion to the HUVECs monolayer activated by TNF-α. Saikosaponin D (30 μM) also inhibits the expression of P-selectin ligand (CD162) in THP-1 cells[1]. Saikosaponin D (5 μM) suppresses the proliferation of HSC-T6 cells induced by H2O2 treatment, reduces the expression levels of α-SMA, TGF-β1, Hyp, COL1 and TIMP-1, and increases MMP-1 expressioon, thus inhibiting H2O2-induced excessive extracellular matrix (ECM) formation, with similar effects to estradiol (E2), and these effects are blocked by ER antagonists. Saikosaponin D also inhibits oxidative stress-induced ROS generation and down reduates MAPK signaling pathway, and the inhibition is also suppressed by ER antagonists[3].
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In Vivo |
Saikosaponin D (2 mg/kg/day, i.p.) shows a protective effect on overdose of acetaminophen (APAP)-induced liver injury of mice. Saikosaponin D affects APAP metabolism, increases GSH levels but does not alter PPARα activation. Saikosaponin D (2 mg/kg/day, i.p.) also suppresses APAP-induced increases in the expression of STAT3 target genes and pro-inflammatory cytokines and inhibits APAP-induced activation of STAT3 and NF-kB[2].
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Cell Assay |
Cell viability is assessed by morphology and by reduction of the tetrazolium salt (MTT). Briefly, the THP-1 cells (2 × 105 cells/well) and various concentrations of compounds 1-4 (including Saikosaponin D) are added to the 96-well plates, incubated for 48 h at 37°C, and 5 µL of MTT solution (5 mg/mL in PBS) is added to each well of the 96-well plates. After incubation for 4 h at 37°C, the absorbance is measured at 540 nm using a microplate reader with the reference absorbance at 650 nm[1].
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Animal Admin |
Mice[2] Male 6- to 7-week-old C57BL6 mice are randomly divided into four groups, vehicle/control, Saikosaponin D (SSd)/control, vehicle/APAP, and SSd/APAP, and killed 4 h or 24 h after single APAP injection. For overdose of acetaminophen (APAP) injection, a typical single dose of 200 mg/kg/day is used. Saikosaponin D, 2 mg/kg once daily is used as the dosing regimen. Saikosaponin D powder is dissolved in a saline solution supplemented with 0.1% Tween 20 and is administered by intraperitoneal injection at a dose of 2 mg/kg/day once daily for five days. Saline solution containing 0.1% Tween 20 without Saikosaponin D is administered as a vehicle. APAP is dissolved in warm saline solution (20 mg/mL) and is injected intraperitoneally 30 minutes after the last Saikosaponin D injection. Saline is injected to mice in the control groups[2].
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Density | 1.4±0.1 g/cm3 |
Boiling Point | 893.7±65.0 °C at 760 mmHg |
Flash Point | 494.3±34.3 °C |
Exact Mass | 780.466003 |
PSA | 207.99000 |
LogP | 3.65 |
Vapour Pressure | 0.0±0.6 mmHg at 25°C |