Brusatol (NSC 172924)
(Synonyms: 鸦胆子苦醇; NSC 172924) 目录号 : GC34070
A quassinoid with diverse biological activities
Cas No.:14907-98-3
Sample solution is provided at 25 µL, 10mM.
Brusatol is a quassinoid that has been found in B. javanica and has diverse biological activities, including antimalarial, lipolytic, antioxidative, anticancer, and anti-inflammatory properties.1,2,3,4 It is active against chloroquine-resistant isolates of P. falciparum (EC50 = 7.58 ng/ml) and induces lipolysis in 3T3-L1 adipocytes when used at a concentration of 160 nM.1,2 Brusatol (40 nM) reduces nuclear erythroid 2-related factor 2 (Nrf2) ubiquitination and degradation and Nrf2 target gene expression in A549 lung cancer cells.3 It enhances cytotoxicity induced by cisplatin in A549 cells when used at a concentration of 40 nM in vitro and in an A549 mouse xenograft model when administered at a dose of 2 mg/kg. Brusatol also inhibits LPS-induced production of TNF-α, pro-IL-1β, prostaglandin E2 , and nitric oxide (NO) in RAW 264.7 macrophages. It reduces diarrhea and the severity of histopathological injury, as well as increases colonic levels of catalase (CAT), glutathione (GSH), and superoxide dismutase (SOD), in a mouse model of ulcerative colitis when administered at doses of 0.5 and 1 mg/kg.4
1.Lee, K.-H., Tani, S., and Imakura, Y.Antimalarial agents, 4. Synthesis of a brusatol analog and biological activity of brusatol-related compoundsJ. Nat. Prod.50(5)847-851(1987) 2.Lahrita, L., Moriai, K., Iwata, R., et al.Quassinoids in Brucea javanica are potent stimulators of lipolysis in adipocytesFitoterapia137104250(2019) 3.Ren, D., Villeneuve, N.F., Jiang, T., et al.Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanismProc. Natl. Acad. Sci. USA108(4)1433-1438(2011) 4.Zhou, J., Wang, T., Dou, Y., et al.Brusatol ameliorates 2, 4, 6-trinitrobenzenesulfonic acid-induced experimental colitis in rats: Involvement of NF-κB pathway and NLRP3 inflammasomeInt. Immunopharmacol.64264-274(2018)
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Cell experiment: |
CT-26 cells in logarithmic growth are seeded onto a 96-well plate at a density of 4×103 cells/well. After 24 h of incubation at 37°C, fresh medium containing a series of concentrations of Brusatol (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) and CDDP (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) is added at 100 μL/well; each concentration is used to treat six replicate wells. After 48 h of incubation at 37°C, the cells are further incubated with MTT (10 mg/mL) at 37°C for 4 h. The supernatant is then removed and the precipitate is dissolved with 100 μL DMSO. Absorbance is measured using a microplate reader at a wavelength of 490 nm. Cytotoxicity is expressed as the concentration of Brusatol and CDDP that inhibit cell growth by 50% (IC50 value). The inhibitory rate is calculated. The possible synergistic effect of Brusatol combined with CDDP is investigated by exposing CT-26 cells to various concentrations of each agent alone or in combination for 48 h. The synergistic effect is assessed using CalcuSyn software 2.0[2]. |
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Animal experiment: |
Mice[3]Athymic nude mice are used. Mice 4-6 wk old are injected with A549 cells. Once the tumors reach 80 mm3 (for the two times five-time Cisplatin treatment regimen) or 280 mm3 (for the single five-time Cisplatin treatment regime), mice are randomly allocated into four groups and treated i.p. with DMSO, Cisplatin (2 mg/kg), Brusatol (2 mg/kg), or in combination every other day for a total of five times. After the initial five-time Cisplatin treatment regimen, treatment stops for 1 wk to allow mice to recover before the second five-time Cisplatin treatment regimen is repeated[3]. |
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References: [1]. Olayanju A, et al. Brusatol provokes a rapid and transient inhibition of Nrf2 signaling and sensitizes mammaliancells to chemical toxicity-implications for therapeutic targeting of Nrf2. Free Radic Biol Med. 2015 Jan;78:202-12. |
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| Cas No. | 14907-98-3 | SDF | |
| 别名 | 鸦胆子苦醇; NSC 172924 | ||
| Canonical SMILES | CC([C@](C[C@@](O1)2[H])3[H])=C(O)C(C[C@]3(C)[C@]4([H])[C@]2(CO[C@@]5([C@@H](O)[C@@H]4O)C(OC)=O)[C@@]5([H])[C@@H](OC(/C=C(C)/C)=O)C1=O)=O | ||
| 分子式 | C26H32O11 | 分子量 | 520.53 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | 储存条件 | 4°C, protect from light, stored under nitrogen |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9211 mL | 9.6056 mL | 19.2112 mL |
| 5 mM | 0.3842 mL | 1.9211 mL | 3.8422 mL |
| 10 mM | 0.1921 mL | 0.9606 mL | 1.9211 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet