Brusatol是一种Nrf2抑制剂，由从鸦嘴茅中分离提取。
Cas No.:14907-98-3
Sample solution is provided at 25 µL, 10mM.
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Brusatol is an Nrf2 inhibitor isolated from Brucea javanica and exhibits significant tumor inhibition in multiple cancers through decreased resistance to cancer oxidative stress injury[1,2,3]. Brusatol is confirmed to inhibit the Nrf2-Notch1 pathway, increse p-P38, LC3, Beclin 1 and p-JNK expression, downregulate BRF2, IGFBP-2, P62 and CD151[3].
In vitro, Brusatol (20, 50, 100, and 200nM; 0, 24, 48, 72, and 96h) treatment at the zygotic stage prevented the early embryo development in Kunming mice embryos[4]. Brusatol (1 and 100nM; 72h) shows an antitumor effect in an acute lymphoblastic leukemia (KOPN-8 cells) model triggered by reactive oxygen species accumulation[5]. Brusatol (0.31 to 10µM; 24 or 48h) results in breast cancer retardation via Nrf2 inhibition in breast cancer cell lines[6].
In vivo, Brusatol (2mg/kg; every 48h; 5 weeks; i.p.) hinders the progression of bladder cancer by Chac1/Nrf2/SLC7A11 pathway[7]. Brusatol (NSC 172924) sensitizes endometrial hyperplasia and cancer to progestin by suppressing NRF2-TET1-AKR1C1-mediated progestin metabolism in a Brusatol (NSC 172924)-treated (10nmol/l; 3 days) endometrial cancer cell (Ishikawa and ECC1) injected nude mice model[8].
References:
[1] Yu, Xiao-Qi et al. “Brusatol: A potential anti-tumor quassinoid from *Brucea javanica*.” *Chinese herbal medicines* vol. 12,4 359-366. 19 Aug. 2020, doi:10.1016/j.chmed.2020.05.007
[2] Sutiningsih, Dwi et al. “Larvicidal Activity of Brusatol Isolated from *Brucea javanica* (L) Merr on *Culex quinquefasciatus*.” *Iranian journal of public health* vol. 48,4 (2019): 688-696.
[3] Li, Kun-Wei et al. “Brucea javanica: A review on anticancer of its pharmacological properties and clinical researches.” *Phytomedicine : international journal of phytotherapy and phytopharmacology* vol. 86 (2021): 153560. doi:10.1016/j.phymed.2021.153560
[4] Lin, Ying et al. “Nrf2 inhibition affects cell cycle progression during early mouse embryo development.” *The Journal of reproduction and development*vol. 64,1 (2018): 49-55. doi:10.1262/jrd.2017-042
[5] Jorge, Joana et al. “Antitumor Effect of Brusatol in Acute Lymphoblastic Leukemia Models Is Triggered by Reactive Oxygen Species Accumulation.” *Biomedicines* vol. 10,9 2207. 6 Sep. 2022, doi:10.3390/biomedicines10092207
[6] Bovilla, Venugopal R et al. “Targeted Inhibition of Anti-Inflammatory Regulator Nrf2 Results in Breast Cancer Retardation In Vitro and In Vivo.” *Biomedicines* vol. 9,9 1119. 30 Aug. 2021, doi:10.3390/biomedicines9091119
[7] Yu, Xi et al. “Brusatol hinders the progression of bladder cancer by Chac1/Nrf2/SLC7A11 pathway.” *Experimental cell research* vol. 438,2 (2024): 114053. doi:10.1016/j.yexcr.2024.114053
[8] Hu, Meiyan et al. “Brusatol sensitizes endometrial hyperplasia and cancer to progestin by suppressing NRF2-TET1-AKR1C1-mediated progestin metabolism.” *Laboratory investigation; a journal of technical methods and pathology* vol. 102,12 (2022): 1335-1345. doi:10.1038/s41374-022-00816-5
Brusatol是一种Nrf2抑制剂，由从鸦嘴茅中分离提取[1]。Brusatol通过降低对癌症氧化应激损伤的抵抗，在多种癌症模型中表现出显著的肿瘤抑制作用[2,3]。Brusatol被证实抑制Nrf2-Notch1通路，增加p-P38、LC3、Beclin 1和p-JNK的表达，下调BRF2、IGFBP-2、P62和CD151的作用[3]。
在体外，Brusatol(20、50、100和200nM；0、24、48、72和96h)可阻止昆明小鼠在合子期胚胎的早期胚胎发育[4]。Brusatol(1, 100nM；72h)在活性氧积累触发的急性淋巴细胞白血病模型（KOPN-8细胞）中显示出抗肿瘤作用[5]。Brusatol(0.31 ~ 10µM；24h或48h)通过Nrf2抑制乳腺癌细胞系导致乳腺癌发育迟缓[6]。
在体内，Brusatol (2mg/kg；每48小时一次，持续5周；腹腔注射)通过Chac1/Nrf2/SLC7A11通路阻碍膀胱癌的进展[7]。Brusatol处理的子宫内膜癌细胞（Ishikawa和ECC1）注射的裸鼠肿瘤模型中中，Brusatol通过抑制NRF2-TET1-AKR1C1介导的黄体酮代谢，使子宫内膜增生和癌症对黄体酮产生敏感[8]。
| Cell experiment [1]: | |
Cell lines | MCF-7, MDA-MB-231, or MDA-MB-468 |
Preparation Method | Various BC cells (MCF-7, MDA-MB-231, or MDA-MB-468) (1.0 × 104cells in 100µL DMEM with 10% FBS) were seeded in 96-well plates and cultured in an incubator at 37 °C with 5% CO2 and 90% relative humidity. Following this, when cell confluence reached about 60 to 70% (36h later), the cells were exposed to gradual concentrations of brusatol (ranging from 0.31 to 10µM) for 24 or 48h. Following this treatment, cell viability was measured using sulforhodamine B (SRB) and MTT(3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) assays. |
Reaction Conditions | 0.31 to 10µM; 24 or 48h |
Applications | The effect of two low/non-toxic concentrations (19.5 and 78nM) of brusatol did not demonstrate any significant effect on cell viability. Brusatol provoked a significant decrease in BC cell viability; however, this effect was not dose- or time-dependent. The highest cytotoxic effects of brusatol were observed at 24 and 48h of treatment. |
| Animal experiment [2]: | |
Animal models | male BALB/c-nude mice |
Preparation Method | T24 cells were injected subcutaneously into mice at a concentration of 1×106 cells per mouse. Three mice were randomly allocated into two groups, consisting of nude mice. The experimental groups were administered intraperitoneal injections of brusatol at a dosage of 2mg/kg every 48h, whereas the control groups were given injections of normal saline. Following a treatment duration of 5 weeks, the mice were administered anesthesia and subsequently euthanized to facilitate additional analysis. Sodium pentobarbital (30mg/kg) was administered as the anesthetic drug. |
Dosage form | 2mg/kg; every 48h; 5 weeks |
Applications | The tumor size of mice treated with brusatol was significantly reduced. |
References: | |
| 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 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9211 mL | 9.6056 mL | 19.2112 mL |
| 5 mM | 384.2 μL | 1.9211 mL | 3.8422 mL |
| 10 mM | 192.1 μL | 960.6 μL | 1.9211 mL |
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