Nozaki Akiko, Hori Mami, Kimura Toshikiro, Ito Hideyuki, Hatano Tsutomu
Department of Pharmacognosy, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Tsushima, Japan.
Chem Pharm Bull (Tokyo). 2009 Feb;57(2):224-8. doi: 10.1248/cpb.57.224.
The binding of (-)-epigallocatechin gallate (EGCG), a representative natural polyphenol, to human serum albumin (HSA) and bovine serum albumin (BSA) was investigated using induced circular dichroism (CD). The site of the binding EGCG-HSA was analyzed based on the competition with drugs with known binding sites on HSA, such as phenylbutazone (PB) and diazepam (DP). Double-reciprocal plot analyses showed the competitive relations with the site-I- (PB and tolbutamide, TB) and site-II-binding drugs (DP and ibuprofen, IP) indicating the binding of EGCG to sites I and II on HSA, while digitoxin (DG), a site-III-binding drug, did not affect the binding of EGCG. In an analogous way, the competitive relations were observed between EGCG and the site-I- (PB and TB) and site-II-binding (ethacrynic acid, EA) drugs for the binding of EGCG and BSA. The site-III drug DG also showed competitive binding with EGCG to BSA. The binding of EGCG to the albumins indicated its affinity to sites I and II on HSA, while competitive binding for all three sites was observed on BSA.
使用诱导圆二色光谱法（CD）研究了代表性天然多酚（-）-表没食子儿茶素没食子酸酯（EGCG）与人血清白蛋白（HSA）和牛血清白蛋白（BSA）的结合情况。基于与在HSA上具有已知结合位点的药物（如保泰松（PB）和地西泮（DP））的竞争，分析了EGCG-HSA的结合位点。双倒数图分析显示与位点I结合药物（PB和甲苯磺丁脲，TB）和位点II结合药物（DP和布洛芬，IP）存在竞争关系，表明EGCG与HSA上的位点I和位点II结合，而位点III结合药物洋地黄毒苷（DG）不影响EGCG的结合。以类似的方式，观察到EGCG与位点I结合药物（PB和TB）以及位点II结合药物（依他尼酸，EA）在EGCG与BSA结合方面存在竞争关系。位点III药物DG也显示出与EGCG对BSA的竞争结合。EGCG与白蛋白的结合表明其对HSA上的位点I和位点II具有亲和力，而在BSA上观察到对所有三个位点的竞争结合。
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