| 名稱 | Sulforaphane |
| 描述 | Sulforaphane is a natural isothiocyanate that activates Nrf2 and inhibits AMPK-dependent signaling. Sulforaphane has antitumor and anti-inflammatory activities by increasing the transcription of tumor suppressor proteins and inhibiting histone deacetylase activity. |
| 細(xì)胞實驗 | HT29 cells are seeded at low density (5×10^4 cells/mL) in 35- or 120-mm diameter Primaria dishes in standard medium containing 5% FCS. One day after seeding, the medium is changed, and HT29 cells are treated with sulforaphane (0-30 μM). An equivalent amount of the solvent (ethanol) is added to control cells (0.2% final concentration). The drug effect on cellular viability is evaluated using the MTT assay [1]. |
| 動物實驗 | At age 47, 48, 49, 50, and 51 days, each animal receives by gavage either 0.5 mL of Emulphor EL-620 alone or the specified doses (75, 100, or 150 μM daily) of sulforaphane or compound 2, 3, or 4 in 0.5 mL of Emulphor EL-620. On day 50, 3 hr after administration of the vehicle or protector, all rats also receive an intragastric instillation of 8.0 mg of DMBA dissolved in 1.0 mL of sesame oil. This dose of DMBA is selected to produce a substantial tumor incidence, but not one so high as to overwhelm a potential chemoprotective effect. The animals are examined once weekly for the appearance and location of palpable tumors. At age 202 days, i.e., 152 days after carcinogen administration, all animals are euthanized with ether and weighed. The tumors are separated from the fat and connective tissue by dissection weighed and fixed in buffered 10% formalin. All tumors are identified microscopically by examination of stained sections [3]. |
| 體外活性 | 方法: 人結(jié)直腸癌細(xì)胞 HT29 用 Sulforaphane (15 μM) 處理 24-96 h，使用 MTT assay 檢測細(xì)胞活力。
結(jié)果: 15 μM 的 Sulforaphane 能夠抑制細(xì)胞生長并誘導(dǎo)細(xì)胞死亡。24 h 時細(xì)胞死亡率已經(jīng)達(dá)到75%，96 h 時幾乎全部死亡。[1]
方法: 胃癌細(xì)胞 BGC-823 和 MGC-803 用 Sulforaphane (5-10 μM) 處理 48 h，使用 Western Blot 方法檢測靶點蛋白表達(dá)水平。
結(jié)果: 當(dāng)胃癌細(xì)胞用 Sulforaphane 處理時，細(xì)胞周期調(diào)節(jié)蛋白如 p53 和 p21 的表達(dá)水平以劑量依賴性的方式增加，而 S 期相關(guān)蛋白 CDK2 的表達(dá)水平顯著降低。[2] |
| 體內(nèi)活性 | 方法: 為檢測抗炎活性，將 Sulforaphane (50 mg/kg) 單次腹腔注射給 BALB/c 小鼠，三天后注射 LPS 誘導(dǎo)急性肺損傷 (ALI) 。
結(jié)果: Sulforaphane 顯著降低了 LPS 誘導(dǎo)的急性肺損傷小鼠的 LDH 活性、肺的濕干比、血清 IL-6 和 TNF-α 水平以及 NF-κB 蛋白表達(dá)。Sulforaphane 通過 Nrf2/ARE 途徑對 LPS 誘導(dǎo)的 ALI 發(fā)揮保護(hù)作用。[3] |
| 存儲條件 | Keep away from direct sunlight,Keep away from moisture,Store at low temperature,The compound is unstable in solution. Please use soon,
Pure form: -20°C for 3 years
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : 5.5 mg/mL (31.02 mM), Solution.
5% DMSO+95% Saline : 2.89 mg/mL (16.3 mM), Solution.
DMSO : 252.5 mg/mL (1424.22 mM), Sonication is recommended.
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| 關(guān)鍵字 | Sulforaphane | Keap1-Nrf2 | Inhibitor | inhibit | Histone deacetylases | HDAC | Apoptosis |
| 相關(guān)產(chǎn)品 | Allopurinol | Urea | Formamide | Kaolin | Aceglutamide | Alginic acid | Dextran sulfate sodium salt (MW 5000) | Manganese chloride (tetrahydrate) | Stavudine | Ethoxyquin | Tamoxifen | Ethyl linoleate |
| 相關(guān)庫 | 已知活性庫Plus |