佛波醇-12-十四烷酰-13-乙酸酯 编辑
佛波醇-12-十四烷酰-13-乙酸酯(英語:12-O-Tetradecanoylphorbol-13-acetate,縮寫:TPA)是一種具有潛在促癌作用的佛波酯,在生物醫學研究中常用作蛋白激酶C(PKC)的激活劑。[1][2][3] TPA對PKC的生物學活性源於它的擬甘油二酯樣作用——後者是一種經典蛋白激酶C的天然活化劑。
佛波醇-12-十四烷酰-13-乙酸酯 | |
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IUPAC名 (1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-9a-(乙酰)-4a,7b-二羥基-3-(羥甲基)-1,1,6,8-四甲基-5-氧-1a,1b,4,4a,5,7a,7b,8,9,9a-十氫-H-環丙[3,4]苯並[1,2-e]薁-9-肉豆蔻酸酯 | |
别名 | TPA,PMA,佛波醇肉豆蔻酰乙酸酯, 十四酰佛波乙酯 |
识别 | |
CAS号 | 16561-29-8 |
PubChem | 27924 |
ChemSpider | 25977 |
SMILES |
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InChI |
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InChIKey | PHEDXBVPIONUQT-RGYGYFBIBK |
KEGG | C05151 |
性质 | |
化学式 | C36H56O8 |
摩尔质量 | 616.83 g·mol−1 |
若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。 |
在自由基生物學中,不包含羥基自由基、過氧化氫、過氧亞硝酸鹽在內的超氧化物被認定系TPA而非离子霉素在小鼠巨噬細胞中產生的活性氧衍生物,因此TPA已成為誘生內源性超氧化物的常規用劑。[4][5]
在細胞遺傳學試驗中,TPA被視為B細胞淋巴瘤細胞的有丝分裂原,可刺激B細胞的分裂以便於對特定細胞的染色體進行觀察,從而幫助診斷諸如慢性淋巴细胞白血病的血液癌症。[6]
参考文献
编辑- ^ Castagna; et al. "Direct activation of calcium-activated, phospholipid-dependent protein kinase by tumor-promoting phorbol esters". Journal of Biological Chemistry. 1982, 257 (13): 7847–7851.
- ^ Blumberg. "Protein kinase C as the receptor for the phorbol ester tumor promoters: sixth Rhoads memorial award lecture". Cancer Research. 1988, 48: 1–8.
- ^ Niedel; et al. Phorbol Diester Receptor Copurifies with Protein Kinase C. Proceedings of the National Academy of Sciences. 1983, 80: 36–40. doi:10.1073/pnas.80.1.36.
- ^ Swindle. "A Comparison of Reactive Oxygen Species Generation by Rat Peritoneal Macrophages and Mast Cells Using the Highly Sensitive Real-Time Chemiluminescent Probe Pholasin: Inhibition of Antigen-Induced Mast Cell Degranulation by Macrophage-Derived Hydrogen Peroxide". The journal of Immunology. 2002, 169: 5866–5873..
- ^ Huang. "Megakaryocytic Differentiation of K562 Cells Induced by PMA Reduced the Activity of Respiratory Chain Complex IV". PLOS ONE (journal). 2014, 9: e96246..
- ^ The AGT cytogenetics laboratory manual. 3rd ed. Barch, Margaret J., Knutsen, Turid., Spurbeck, Jack L., eds. 1997. Lippincott-Raven.
- ^ Flow Cytometry Intracellular Staining Guide. eBioscience, Inc. [2011-09-25]. (原始内容存档于2017-01-21).
外部链接
编辑- 醫學主題詞表(MeSH):Tetradecanoylphorbol+Acetate
- NCI Dictionary Entry. [2005-07-02]. (原始内容存档于2015-05-11).
- Phase 1 Clinical Trials. [2005-07-02]. (原始内容存档于2020-11-06).