Biological activity of a gallic acid-gelatin conjugate.
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.
Dipartimento di Scienze Farmaceutiche, Università della Calabria, Edificio Polifunzionale, Arcavacata di Rende (CS) 87036, Italia. giuseppe.cirillo@unical.it
Giuseppe
G
Cirillo
Kai
K
Kraemer
Susanne
S
Fuessel
Francesco
F
Puoci
Manuela
M
Curcio
Umile Gianfranco
UG
Spizzirri
Ilaria
I
Altimari
Francesca
F
Iemma
D000110:Acetylcholinesterase / Q000187:drug effects; D000544:Alzheimer Disease / Q000517:prevention & control; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis; D002292:Carcinoma, Renal Cell / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis; D005260:Female; D005707:Gallic Acid / Q000737:chemistry* / Q000627:therapeutic use; D005780:Gelatin / Q000737:chemistry* / Q000627:therapeutic use; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000473:pathology
D000970:Antineoplastic Agents; D000975:Antioxidants; D002800:Cholinesterase Inhibitors; D005707:Gallic Acid; D005780:Gelatin; D000110:Acetylcholinesterase