| 名稱 | Piceatannol |
| 描述 | Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1. |
| 細(xì)胞實驗 | Cells are exposed to increasing concentrations of Piceatannol. For the determination of cell proliferation, cells are assayed at 72 hours by trypan blue exclusion using a hemocytometer. After 1 week, colonies are stained with 1.25% crystal violet and quantified by measuring the absorbance at 595 nm. (Only for Reference) |
| 激酶實驗 | In Vitro Protein-tyrosine Kinase Assays: Recombinant Syk is expressed in baculovirus-infected St9 cells. Assays of recombinant Syk activity are carried out using angiotensin I peptide as substrate. The enzyme activities of recombinant Syk are measured by phosphorylation of angiotensin I peptide in the presence of various concentrations of Piceatannol. |
| 體外活性 | 在治療患有葡聚糖硫酸鈉誘導(dǎo)的BALB/c結(jié)腸炎小鼠模型時,口服給藥Piceatannol會明顯改善結(jié)腸結(jié)構(gòu)破壞情況,明顯減少炎癥介質(zhì)產(chǎn)生量（如一氧化氮, 前列腺素E2和前炎癥細(xì)胞因子）,并且會引起結(jié)腸髓MPO活性明顯降低.在2型糖尿病db/db 小鼠模型中,Piceatannol會抑制早期血糖水平的升高,在晚期可以改善糖耐量受損癥狀. |
| 體內(nèi)活性 | 在肥大細(xì)胞中,Piceatannol是一種有效的組胺釋放抑制劑。Piceatannol選擇性抑制肥大細(xì)胞中的Syk從而阻斷受體介導(dǎo)的下游細(xì)胞應(yīng)答,包括對1,4,5-IP3分泌、合成,胞膜邊緣波動以及運(yùn)輸?shù)囊种啤iceatannol對Syk的抑制效果比對Lyn高10倍左右。RBL-2H3 細(xì)胞經(jīng)Piceatannol處理后,抗原刺激的Syk和其它大部分細(xì)胞蛋白的磷酸化會受到強(qiáng)烈抑制,但對不影響受體γ或β亞型的磷酸化, 這種抑制呈劑量依賴性。Piceatannol也可以有效地抑制 CDPK,MLCK,PKC和PKA（IC50 分別為：19 μM,12 μM,8 μM,3 μM）。Piceatannol對IFNα誘導(dǎo)的 STAT3/5酪氨酸磷酸化具有選擇性抑制作用, 但不影響STAT1/2, 同時對 Jak1 和 IFNAR1酪氨酸去磷酸化有選擇性抑制作用,但不影響Tyk2和 IFNAR2。Piceatannol 通過激活半胱天冬酶3和線粒體通透性改變可以有效地誘導(dǎo)BJAB Burkitt樣淋巴瘤細(xì)胞凋亡,ED50 為 25 μM,這一過程實現(xiàn)而不依賴CD95/Fas信號通路。Piceatannol抑制TNF, H2O2, PMA, 脂多糖, 岡田酸和神經(jīng)酰胺誘導(dǎo)的NF-κB 激活。Piceatannol抑制TNF誘導(dǎo)的NF-κB依賴性報告基因（基質(zhì)金屬蛋白酶- 9, 環(huán)氧酶-2和 cyclin D1）表達(dá),該過程通過阻斷TNF誘導(dǎo)的IκBαof、p65磷酸化,p65核轉(zhuǎn)位以及IκBα激酶激活實現(xiàn),而不依賴?yán)野彼峒っ浮?Piceatannol 通過三磷酸腺苷競爭性方式直接結(jié)合胞內(nèi)磷脂酰肌醇激酶進(jìn)而抑制酶活性,其抗硬化效果比resveratrol的抗動脈粥樣更好。Piceatannol抑制雄激素依賴或不依賴的CaP 細(xì)胞增殖,同時能使mTOR和其關(guān)鍵效應(yīng)器 AKT和eIF4EBP-1的表達(dá)明顯下降。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 24.4 mg/mL (100 mM)
DMSO : 160 mg/mL (655.09 mM), Sonication is recommended.
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| 關(guān)鍵字 | Spleen tyrosine kinase | anticancer | Piceatannol | Autophagy | ALI | iNOS | acute | Inhibitor | inhibit | Syk | Apoptosis | injury | lung | anti-inflammatory |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Valproic Acid | L-Glutamic acid | Gefitinib | Hydroxychloroquine | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 植物來源化合物庫 | 苗藥化合物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 中藥單體化合物庫 | 天然產(chǎn)物庫 | 酪氨酸激酶分子庫 | 高通量篩選天然產(chǎn)物庫 |