| 名稱 | Deferoxamine Mesylate |
| 描述 | Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis. |
| 細(xì)胞實(shí)驗(yàn) | After cells were seeded onto the collagen-GAG discs and allowed to adhere for 3?hours, they were placed into a hypoxic incubator with 1% O2 or incubated under standard cell culture conditions with deferoxamine mesylate (DFO) added to final concentrations of 30, 60, or 120?μM. Scaffolds seeded with AdMSCs cultured under standard conditions were used as a control [3]. |
| 動(dòng)物實(shí)驗(yàn) | The animals were divided into 4 groups: sham, SAH, SAH+vehicle and SAH+DFX (100mg/kg) group. DFX was administered intraperitoneally 2 and 6 hours after hemorrhage followed by every 12 hours for a maximum of 7 days. The same time course and dosage of saline were administered in the SAH+vehicle group. Afterward, rats underwent behavioral testing and were euthanized at day 1, 3, 7 and 28 for brain water content calculation, immunohistochemistry or western blot assays. The study was performed in three parts. Part 1 measured the brain water content, Evan's blue extravasation, and ultrastructural abnormalities at day 1, 3 and 7 after SAH to evaluate the time-dependent changes in brain edema and BBB disruption (n = 4 per time point and group). Part 2 investigated the role of iron in SAH-induced BBB disruption at day 1, 3 and 7 by brain water content (n = 4, per time point and group), Evan's blue extravasation (n = 4, per time point and group), transmission electron microscopy (n = 4, per time point and group), immunohistochemistry (n = 4, per time point and group) and western blot analysis (n = 3, per time point and group). Part 3 compared the acute (n = 61, per group at day 1; n = 42, per group at day 3; n = 23, per group at day 7) and long term (n = 4, per group at day 28) neurological function after SAH in each group to determine the effect of iron chelation on SAH-induced neurologic impairment [4]. |
| 體外活性 | 方法：人宮頸癌細(xì)胞 HeLa 用 Deferoxamine Mesylate (3-100 μM) 處理 72 h，使用 Incucyte HD imaging system 檢測(cè)細(xì)胞數(shù)目。
結(jié)果：Deferoxamine Mesylate 以濃度依賴的方式抑制細(xì)胞生長(zhǎng)，在100 μM 下觀察到顯著的生長(zhǎng)抑制。[1]
方法：人結(jié)直腸癌細(xì)胞 HT29 和 HCT116 用 Deferoxamine Mesylate (50-200 μM) 處理 48 h，使用 Western Blot 方法檢測(cè)靶點(diǎn)蛋白表達(dá)水平。
結(jié)果：Deferoxamine Mesylate 以劑量依賴性方式誘導(dǎo) HIF-1α 的顯著表達(dá)。[2]
方法：人乳腺癌細(xì)胞 MDA-MB-231 和 MCF-7 用 Deferoxamine Mesylate (200 μM) 處理 24 h，使用 Flow Cytometry 方法檢測(cè)細(xì)胞凋亡情況。
結(jié)果：Deferoxamine Mesylate 處理后，與未處理的細(xì)胞相比，MDA-MB-231 細(xì)胞的凋亡率沒(méi)有變化，而 MCF-7 細(xì)胞的凋亡顯著增加。[3] |
| 體內(nèi)活性 | 方法：為研究 Deferoxamine Mesylate 是否能減輕實(shí)驗(yàn)小鼠的炎癥和動(dòng)脈粥樣硬化，將 Deferoxamine Mesylate (100 mg/kg) 腹腔注射給載脂蛋白 E 缺陷 (apoE-/-) 小鼠，每天一次，持續(xù)十周。
結(jié)果：Deferoxamine Mesylate 使主動(dòng)脈動(dòng)脈粥樣硬化病變的發(fā)展減少 26%。Deferoxamine Mesylate 還降低了血清 MCP-1 水平以及主動(dòng)脈和心臟中促炎和巨噬細(xì)胞標(biāo)志物的基因表達(dá)，同時(shí)增加了心臟和肝臟中轉(zhuǎn)鐵蛋白受體的蛋白質(zhì)表達(dá)。相反，Deferoxamine Mesylate 治療對(duì)血清膽固醇和甘油三酯水平?jīng)]有影響。[4]
方法：為研究 Deferoxamine Mesylate 對(duì) ob/ob 小鼠附睪脂肪組織中脂肪細(xì)胞功能障礙的影響，將 Deferoxamine Mesylate (100 mg/kg) 腹腔注射給 ob/ob 小鼠，每天一次，持續(xù)十五天。
結(jié)果：Deferoxamine Mesylate 通過(guò)減少活性氧和炎癥標(biāo)志物的分泌，通過(guò)增加抗氧化酶、HIF-1α 和 HIF-1α 靶向蛋白的水平，以及通過(guò)改變脂肪細(xì)胞鐵、葡萄糖和脂質(zhì)相關(guān)代謝蛋白，顯著改善了脂肪組織生物學(xué)的重要參數(shù)。同時(shí)，Deferoxamine Mesylate 治療后，肥大的脂肪細(xì)胞體積縮小，胰島素信號(hào)通路相關(guān)蛋白也被激活。[5] |
| 存儲(chǔ)條件 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 152.3 mM
H2O : 20.83 mg/mL (31.72 mM)
|
| 關(guān)鍵字 | HIFs | neovascularization | TAMSCs | diabetes mellitus | Akt | Deferoxamine Mesylate | PKB | Protein kinase B | Apoptosis | Autophagy | SH-SY5Y | Hypoxia-inducible factors | Deferoxamine | Desferrioxamine B Mesylate | Inhibitor | MEFs | cancer | Alzheimer’s disease | HIF-PH | Reactive Oxygen Species | BMMSCs | inhibit | HIF/HIF Prolyl-Hydroxylase | COVID-19 |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Hydroxychloroquine |
| 相關(guān)庫(kù) | 抗癌上市藥物庫(kù) | 經(jīng)典已知活性庫(kù) | 抗衰老化合物庫(kù) | FDA 上市藥物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) |