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.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

780.98

C₄₂H₆₈O₁₃

20874-52-6

柴胡皂苷D；柴胡皂甙D

Room temperature in continental US; may vary elsewhere.

Powder	-20deg;C	3 years
	4deg;C	2 years
In solvent	-80deg;C	6 months
	-20deg;C	1 month

In Vitro:;

DMSO : 50 mg/mL (64.02 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (3.20 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (3.20 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 2.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.5 mg/mL (3.20 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (3.20 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Jang MJ, et al. Saikosaponin D isolated from Bupleurum falcatum inhibits selectin-mediated cell adhesion. Molecules. 2014 Dec 4;19(12):20340-9.

  [2]. Liu A, et al. Saikosaponin d protects against acetaminophen-induced hepatotoxicity by inhibiting NF-κB and STAT3 signaling. Chem Biol Interact. 2014 Nov 5;223:80-6.

  [3]. Que R, et al. Estrogen receptor-β-dependent effects of saikosaponin‑d on the suppression of oxidative stress-induced rat hepatic stellate cell activation. Int J Mol Med. 2018 Mar;41(3):1357-1364.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Jang MJ, et al. Saikosaponin D isolated from Bupleurum falcatum inhibits selectin-mediated cell adhesion. Molecules. 2014 Dec 4;19(12):20340-9.

  [2]. Liu A, et al. Saikosaponin d protects against acetaminophen-induced hepatotoxicity by inhibiting NF-κB and STAT3 signaling. Chem Biol Interact. 2014 Nov 5;223:80-6.

  [3]. Que R, et al. Estrogen receptor-β-dependent effects of saikosaponin‑d on the suppression of oxidative stress-induced rat hepatic stellate cell activation. Int J Mol Med. 2018 Mar;41(3):1357-1364.