Berbamine dihydrochloride is an inhibitor of NF-κB activity with remarkable anti-myeloma efficacy.

Berbamine, a novel NF-κB inhibitor, inhibits growth and induces apoptosis in human myeloma cells. Berbamine treatment leads to increased expression of A20, down-regulation of IKKα, p-IκBα, and follows by inhibition of p65 nuclear localization. As a result, NF-κB downstream targets such as cyclin D1, Bcl-xL, Bid and survivin are down-regulated. To determine whether Berbamine has growth inhibitory effect on myeloma cells, KM3 cells are treated with Berbamine at various concentrations for 24, 48, and 72 h, respectively, and then cell viability is assessed by MTT assays. Berbamine inhibits the growth of KM3 cells in a dose- and time-dependent manner, and the IC₅₀ values are 8.17 μg/mL, 5.09 μg/mL, and 3.84 μg/mL for treatment of 24, 48, and 72 h, respectively. In contrast, IC₅₀ value of Berbamine for normal hematopoietic cells is 185.20 μg/mL at 48 h^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbal medicine Berberis amurensis and has been used to treat inflammatory and other diseases.The anti-tumor effects of Berbamine are determined on a xenograft animal model. Two liver cancer cell lines, Huh7 (epithelial) and SK-Hep-1 (mesenchymal-like), are inoculated into NOD/SCID mice by subcutaneous injection. The oral Berbamine treatment greatly suppresses the growth of Huh7 xenografted tumors over the time and leads to a tumor reduction by 70% based on the tumor weight. The growth of SK-Hep-1 cells in NOD/SCID mice is less sensitive to Berbamine than that of Huh7. There is a significant suppression of the growth of the SK-Hep-1 xenograft with more than 50% reduction of the tumor weight^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

681.65

C₃₇H₄₂Cl₂N₂O₆

6078-17-7

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

In Vitro: 

DMSO : ≥ 100 mg/mL (146.70 mM)

* “≥” means soluble, but saturation unknown.

*

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 (sealed storage, away from moisture)。-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    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (3.05 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.05 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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

• 2.

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

  Solubility: ≥ 2.08 mg/mL (3.05 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.05 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (3.05 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.05 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Liang Y, et al. Berbamine, a novel nuclear factor kappaB inhibitor, inhibits growth and induces apoptosis in human myeloma cells. Acta Pharmacol Sin. 2009 Dec;30(12):1659-65.

  [2]. Meng Z, et al. Berbamine inhibits the growth of liver cancer cells and cancer-initiating cells by targeting Ca²⁺/calmodulin-dependent protein kinase II. Mol Cancer Ther. 2013 Oct;12(10):2067-77.

The inhibitory effect of Berbamine on growth of KM3 cells is measured by MTT assay. Briefly, KM3 cells (8×10³ per well) are incubated with increasing concentrations of Berbamine (1-32 μg/mL) for 24, 48, or 72 h and then pulsed with 20 μL of 5 mg/mL MTT for the last 4 h, 200 μL DMSO is then added to dissolve the formazan crystals. Dye absorbance in viable cells is measured at 570 nm, and then the inhibitory concentration of 50% (IC₅₀) is calculated^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[2]
5×10⁶ Huh7 cells in 50% Matrigel dissolved in PBS are inoculated in a NOD/SCID mice. 5×10⁶ SK-Hep-1 cells are applied for each xenograft without Matrigel. 100 mg/kg of Berbamine is orally treated to mice with a regimen of twice a day for 5 consecutive days after the tumors reach a size of 2 mm in diameter. After 2 days withdraw, the regimen is repeated once^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Liang Y, et al. Berbamine, a novel nuclear factor kappaB inhibitor, inhibits growth and induces apoptosis in human myeloma cells. Acta Pharmacol Sin. 2009 Dec;30(12):1659-65.

  [2]. Meng Z, et al. Berbamine inhibits the growth of liver cancer cells and cancer-initiating cells by targeting Ca²⁺/calmodulin-dependent protein kinase II. Mol Cancer Ther. 2013 Oct;12(10):2067-77.