| 名稱 | Rocaglamide |
| 描述 | Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells. |
| 細(xì)胞實(shí)驗(yàn) | HepG2 and Huh-7 cells (1×10^4/well) are seeded in 96-well plates in complete culture medium and incubated for 24 h. The cells are then exposed to 100 nM Rocaglamide and/or 100 ng/mL TRAIL for 24 h. The control cells are treated with DMSO at a concentration equal to that used for the drug-treated cells. The complete culture medium is then removed and MTT (200 μL, 0.5 mg/mL in 10% FBS-containing DMEM) is added to each well and the plate is incubated for 2 h at 37°C in a humidified incubator. The solution is then removed from the wells and 200 μL DMSO is added to each well prior to agitation. The absorbance at 570 nm is read using a microplate reader (Bio-Tek ELx800). The value for the vehicle-treated cells is considered to indicate 100% viability. Furthermore, a crystal violet assay is carried out. Briefly, the cells (1×10^5/mL) are seeded in a 12 well plate for 12 h and treated with TRAIL (0-100 ng/mL) and/or RocA(1-100 nM) for 12 h. The treated cells are washed with phosphate-buffered saline (PBS), fixed with 4% paraformaldehyde for 15 min, and stained using crystal violet for a further 30 min [2]. |
| 動(dòng)物實(shí)驗(yàn) | The Huh-7 cells (3×10^6), suspended in 100 μL mix (equal volumes of DMEM and Matrigel), are implanted subcutaneously into the right flank of 10 female SCID mice (6-week-old) and then randomly divided into two equal groups, one of which received an intraperitoneal injection of Rocaglamide (2.5 mg/kg in 80 μL olive oil; n=5) and the other, used as a vehicle control, received olive oil alone (n=5). These treatments are performed once daily for 32 days and the tumor volumes and body weights of the animals are measured twice a week. The tumor volumes (mm3) are calculated using the following formula: Tumor volume=LS2/2, where L is the longest diameter and S is the shortest. At the end of the experiments, the mice are sacrificed and tumor samples are harvested, fixed in formalin and embedded in paraffin as tissue sections for immunohistochemical analysis [2]. |
| 體外活性 | Rocaglamide是一種有效且選擇性的熱休克因子1（HSF1）激活抑制劑，IC50約為50 nM。它通過(guò)抑制轉(zhuǎn)錄啟動(dòng)因子eIF4A的功能發(fā)揮作用，并且具有針對(duì)白血病[1,2,3]的抗癌特性。單獨(dú)使用Rocaglamide可導(dǎo)致9%的HepG2細(xì)胞和11%的Huh-7細(xì)胞發(fā)生凋亡，而與TRAIL聯(lián)合治療則分別使16%的HepG2細(xì)胞和17%的Huh-7細(xì)胞發(fā)生凋亡。然而，Rocaglamide與TRAIL的組合使用在HepG2和Huh-7細(xì)胞中引發(fā)的凋亡率分別高達(dá)55%和57%，明顯超出了簡(jiǎn)單加成效應(yīng)[2]。 |
| 體內(nèi)活性 | 在Rocaglamide處理組中，腫瘤體積與對(duì)照組相比為45±12%。Rocaglamide顯著抑制腫瘤生長(zhǎng)，與對(duì)照組相比有明顯差異。使用Rocaglamide治療期間，小鼠體重沒(méi)有減少，且未觀察到明顯的毒性跡象[2]。 |
| 存儲(chǔ)條件 | Store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 150 mg/mL (296.7 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.98 mM), Sonication is recommended.
Ethanol : 5 mg/mL (9.89 mM), Sonication is recommended.
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| 關(guān)鍵字 | Rocaglamide | NF-κB | NFκB | NF-kB | NFkB | HSP | HSF1 | Eukaryotic Initiation Factor (eIF) | eIF |
| 相關(guān)產(chǎn)品 | D-Psicose | Sodium propionate | 1,4-Naphthoquinone | Palmitic acid sodium | Daraxonrasib | Palmitic acid | Ethoxyquin | Tamoxifen | Fumaric acid | Kojic acid | Ethyl linoleate | N,N-Dimethylacetamide |
| 相關(guān)庫(kù) | 細(xì)胞焦亡化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌活性化合物庫(kù) | 已知活性化合物庫(kù) | 生物堿類(lèi)天然產(chǎn)物庫(kù) | 激酶抑制劑庫(kù) | 細(xì)胞凋亡化合物庫(kù) | 細(xì)胞骨架化合物庫(kù) | 抗肺癌化合物庫(kù) | 免疫/炎癥分子化合物庫(kù) | NF-κB 通路分子庫(kù) | 高通量篩選天然產(chǎn)物庫(kù) |