Baicalein (5,6,7-Trihydroxyflavone) is a xanthine oxidase inhibitor with an IC₅₀ value of 3.12 μM.

IC50: 3.12 μM (xanthine oxidase)^[1]

Baicalein suppresses mitogen induced T cell proliferation and cytokine secretion in vitro. Pre-treatment with baicalein significantly suppresses Con A or anti-CD3/CD28 mAb induced proliferation as well as cytokine secretion at 25 μM. Baicalein treatment induces DNA binding of NF-κB but inhibits thioredoxin activity in the nuclear compartment^[2]. Baicalein suppresses proliferation, migration, and invasion of MDA-MB-231 cells in a time- and dose-dependent manner. Baicalein significantly decreases the expression of SATB1 in MDA-MB-231 cells. Baicalein also downregulates the expression of Wnt1 and β-catenin proteins and transcription level of Wnt/β-catenin-targeted genes^[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Baicalein suppresses induction of graft versus host disease but does not inhibit homeostatic proliferation of T-cells in mice. This observation clearly shows potent anti-inflammatory activity of baicalein in vivo^[2]. Rats treated with baicalein are protected against an increase in heart to body weight ratio, plasma level of brain natriuretic peptides, intraventricular septum thickness, myocardial collagen volume of left ventricle (all P<0.05, respectively). The antifibrotic effects of baicalein are further illustrated by the suppressed expression of left ventricle pro-collagens I and III accompanied by the decreased expression of 12-lipoxygenase, and by reduced expression and activity of matrix metallopeptidase 9 and extracellular signal-regulated kinases. Baicalein can inhibit cardiac fibrosis in hypertensive rats^[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

270.24

C₁₅H₁₀O₅

491-67-8

黄芩素

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO : 50 mg/mL (185.02 mM; Need ultrasonic)

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 (protect from light)。-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。

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： 0.5% CMC-Na/saline water

  Solubility: 20 mg/mL (74.01 mM); Suspended solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: 2.5 mg/mL (9.25 mM); Clear solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (9.25 mM) 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 3.

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

  Solubility: 2.5 mg/mL (9.25 mM); Clear solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (9.25 mM) 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

• [1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5.

  [2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89.

  [3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41.

  [4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81.

MTT assay is conducted to evaluate the effect of baicalein on proliferation of breast cancer cells. MDA-MB-231 cells are routinely digested, collected, and then seeded in 96-well plates at a density of 8×10³ cells/well. After incubation for 12-24 hours, cells are treated with 0, 20, 40, 60, 80, 100, and 120 μM baicalein according to their experimental grouping and then incubated at 37°C for 24, 48, and 72 hours^[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Rats: Baicalein is suspended in 1% methylcellulose. Rats are treated with baicalein suspension via oral garvage. SHR and WKY rats are divided into 4 groups (n=8 per group): 12-week treatment with high-dose (200 mg/kg/day) or low-dose (50 mg/kg/day) group; and 4-week treatment with high-dose or low-dose group. The 12-week and 4-week negative control groups of SHR and WKY rats (n=8 per group) receive vehicle while positive control groups (Val group, n=8 per group) receive valsartan (20 mg/kg/day) for comparison^[4].

Mice: To study the in vivo anti-inflammatory efficacy of baicalein, graft-versus-host disease (GVHD) model is used. Splenic lymphocytes from C57BL/6 mice are incubated with baicalein in vitro (25 μM, 4h) and adoptively transferred to immune-compromised Balb/c mice^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5.

  [2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89.

  [3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41.

  [4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81.