Biological Activity of a Gallic Acid-Gelatin Conjugate
Biological Activity of a Gallic Acid-Gelatin Conjugate
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DOI：
10.1021/bm100760x
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发表时间：
2010-12-01
影响因子：
6.2
通讯作者：
Iemma, Francesca
中科院分区：
文献类型：
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作者：
Cirillo, Giuseppe;Kraemer, Kai;Iemma, Francesca
本研究的目的是表征明胶-没食子酸缀合物（Gel-GA）的生物学特性，以评价其在生物医学和制药领域的适用性。明胶与没食子酸（GA）通过自由基接枝反应合成了大分子缀合物，共价缀合物保留了游离GA的抗氧化和酶活性。特别是，过氧亚硝酸盐清除能力与IC50值一致，为2.17 +/- 0.4 mg mL（-1）。GA的酶促能力被认为对细胞功能有益，部分保留在Gel-GA偶联物中。特别是，乙酰胆碱酯酶的抑制作用（IC50为7.1 +/- 1.3 mg mL(-1)）表明该缀合物在阿尔茨海默病的化学预防中有用，而α -淀粉酶的抑制作用（IC50为9.8 +/- 1.1 mg mL(-1)）表明该缀合物可以作为抑制碳水化合物分解和控制食品血糖指数的首选替代品。最后，凝胶- ga在前列腺癌和肾癌细胞系中被证实具有抗癌活性，证实了该蛋白-多酚偶联物在医学上的潜力。
Goal of the present study was the characterization of the biological properties of a gelatin-gallic acid conjugate (Gel-GA) to evaluate its applicability in biomedicine and pharmacy. The macromolecular conjugate was synthesized by free radical grafting reaction between gelatin and gallic acid (GA) to form a covalent conjugate that was found to retain the antioxidant and enzymatic activities of free GA. In particular, the peroxynitrite scavenging power was found to be consistent with a IC50 value of 2.17 +/- 0.4 mg mL(-1). The enzymatic capacities of GA, which are regarded beneficial for cell functions, are partly retained in the Gel-GA conjugate. In particular, acetylcholinesterase inhibition (IC50 of 7.1 +/- 1.3 mg mL(-1)) implies the conjugate's usefulness in the chemoprevention of Alzheimer's disease, while the inhibition of alpha-amylase (IC50 of 9.8 +/- 1.1 mg mL(-1)) suggests that the conjugate can be a preferred alternative for inhibition of carbohydrate breakdown and control of glycemic index of food products. Finally, the anticancer activity of Gel-GA was proven in prostate carcinoma and renal cell carcinoma cell lines, confirming the potential of the proposed protein-polyphenol conjugate in medicine.