產(chǎn)品說明

該產(chǎn)品包含在以下化合物庫中:

• Bioactive Compound Library
• Kinase Inhibitor Library
• Tyrosine Kinase Inhibitor Library
• JAK/STAT Compound Library

質(zhì)量控制

• 純度 = 98.00%

化學(xué)性質(zhì)

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實(shí)驗(yàn)操作

產(chǎn)品描述

Butein是一種具有抗氧化作用的查爾酮，具有多種藥理作用。

活性氧（ROS）在細(xì)胞內(nèi)通過多種機(jī)制產(chǎn)生，依賴于細(xì)胞和組織類型，主要通過細(xì)胞膜、線粒體、過氧化物酶體和內(nèi)質(zhì)網(wǎng)的ROS NADPH氧化酶（NOX）復(fù)合體而產(chǎn)生，可由牙科粘合漂白劑和牙髓病誘導(dǎo)產(chǎn)生，ROS可激活氧化應(yīng)激。[1]ROS是正常氧代謝的天然產(chǎn)物，在細(xì)胞信號(hào)和內(nèi)穩(wěn)態(tài)中具有重要作用。但是，在多次環(huán)境壓力后，ROS水平急劇增加。[2] 在butein 存在時(shí)，H2O2誘發(fā)的細(xì)胞毒性和ROS生成會(huì)被阻斷，這一效果是劑量依賴的。由于ROS的雙重作用，基于促氧化和抗氧化功能的抗癌制劑都被研發(fā)出來。

Butein可誘導(dǎo)B16黑色素瘤細(xì)胞和人早幼粒白血病細(xì)胞凋亡，抑制糖尿病并發(fā)癥，并能抑制諸如蛋白激酶和谷胱甘肽還原酶等酶類。[3，4，5，6]最近，Butein從R. verniciflua中分離出來，通過JNK–Nrf2/ARE依賴的HO-1表達(dá)，抑制HDP細(xì)胞中H2O2引起的氧化性細(xì)胞損傷。[7]另外，體外流式細(xì)胞儀分析和RT-PCR表明，Butein可通過抑制NF-kB活性，減弱VEGF和MMP-9的活性。并且，通過電泳遷移率變動(dòng)分析（EMSA）和酶聯(lián)免疫吸附試驗(yàn)（ELISA）發(fā)現(xiàn)，Butein可抑制腫瘤壞死因子ɑ和佛波醇-12-肉豆蔻酸酯-13-乙酸酯誘導(dǎo)的VEGF和MMP-9表達(dá)，最終導(dǎo)致前列腺癌細(xì)胞生長(zhǎng)、侵襲和血管生成的抑制。[8]因此，Butein有希望成為治療多種牙科疾病的制劑。

參考文獻(xiàn)：
1.?Han D, Williams E, Cadenas E."Mitochondrial respiratory chain-dependent generation of superoxide anion and its release into the intermembrane space". Biochem. J. 2010, 353 (2): 411-6.
2.?Devasagayam, TPA; Tilak JC; Boloor KK; Sane Ketaki S; Ghaskadbi Saroj S; Lele RD. "Free Radicals and Antioxidants in Human Health: Current Status and Future Prospects". Journal of Association of Physicians of India (JAPI), 2004, 52: 796.
3.?S. Sogawa, Y. Nero, H. Ueda, T. Miki. Protective effects of hydroxychalcones on free radical-induced cell damage. Biol. Pharm. Bull., 1994, 251-256.
4.?J.C. Lee, K.T. Lim, Y.S. Jang. Identification of Rhus verniciflua Stokes compounds that exhibit free radical scavenging and anti-apoptotic properties. Biochim. Biophys. Acta, 2002, 181-191.
5.?S.M. Yu, Z.J. Cheng, S.C. Kuo. Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor. Eur. J. Pharmacol., 1995, 69-77.
6.?K. Iwashita, M. Kobori, K. Yamaki, T. Tsushida. Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells. Biosci. Biotechnol. Biochem., 2000, 1813-1820.
7.?Dong-Sung Lee.et al. Butein protects human dental pulp cells from hydrogen peroxide-induced oxidative toxicity via Nrf2 pathway-dependent heme oxygenase-1 expressions.Toxicology in Vitro, 2013, 874-881.
8.?Dong-Oh Moona.et al. Butein suppresses the expression of nuclear factor-kappa B-mediated matrix metalloproteinase-9 and vascular endothelial growth factor in prostate cancer cells. Toxicology in Vitro, 2010,24(7) ,1927-1934.