Dipartimento di Scienze Farmaceutiche, Università della Calabria, Edificio Polifunzionale, Arcavacata di Rende (CS) 87036, Italia.
Biomacromolecules. 2010 Dec 13;11(12):3309-15. doi: 10.1021/bm100760x. Epub 2010 Nov 8.
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 IC(50) 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 (IC(50) of 7.1 ± 1.3 mg mL(-1)) implies the conjugate's usefulness in the chemoprevention of Alzheimer's disease, while the inhibition of α-amylase (IC(50) 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.
本研究的目的是对明胶-没食子酸缀合物（Gel-GA）的生物学性质进行表征，以评估其在生物医药和药学中的适用性。通过明胶与没食子酸（GA）之间的自由基接枝反应合成了该高分子缀合物，发现其保留了游离 GA 的抗氧化和酶活性。特别是，过氧亚硝酸盐清除能力与 IC（50）值为 2.17±0.4mgmL（-1）一致。GA 的酶活性被认为对细胞功能有益，部分保留在 Gel-GA 缀合物中。特别是乙酰胆碱酯酶抑制（IC（50）为 7.1±1.3mgmL（-1））表明该缀合物可用于预防阿尔茨海默病，而对α-淀粉酶的抑制（IC（50）为 9.8±1.1mgmL（-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，Gel-GA 的抗癌活性在前列腺癌和肾癌细胞系中得到证实，证实了所提出的蛋白质-多酚缀合物在医学中的潜力。
