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The gallic acid-phospholipid complex improved the antioxidant potential of gallic acid by enhancing its bioavailability.

ABSTRACT: Gallic acid (GA) is well known for its antioxidant and hepatoprotective activity, though its effectiveness is restricted due to rapid metabolism and elimination. To overcome these problems, gallic acid-phospholipid complex was prepared and the effect of phospholipid complexation was investigated on carbon tetrachloride (CCl4)-induced oxidative damage in rat liver. The complex significantly reduced the hepatic marker enzymes in rat serum and restored the antioxidant enzyme levels with respect to CCl4-induced group (P < 0.05 and P < 0.01). Also, the complex improved the pharmacokinetics of GA by increasing the relative bioavailability and elimination half-life. The study therefore suggests that phospholipid complexation has enhanced the therapeutic efficacy of GA which may be due to its improved absorption and increased bioavailability in rat serum.

SUBMITTER: Bhattacharyya S

PROVIDER: S-EPMC3755146 | biostudies-other | 2013 Sep

REPOSITORIES: biostudies-other

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The gallic acid-phospholipid complex improved the antioxidant potential of gallic acid by enhancing its bioavailability.

Bhattacharyya Sauvik S Ahammed Sk Milan SM Saha Bishnu Pada BP Mukherjee Pulok K PK

AAPS PharmSciTech 20130626 3

Gallic acid (GA) is well known for its antioxidant and hepatoprotective activity, though its effectiveness is restricted due to rapid metabolism and elimination. To overcome these problems, gallic acid-phospholipid complex was prepared and the effect of phospholipid complexation was investigated on carbon tetrachloride (CCl4)-induced oxidative damage in rat liver. The complex significantly reduced the hepatic marker enzymes in rat serum and restored the antioxidant enzyme levels with respect to ...[more]

PMID: 23800857

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Project description:To develop a novel emulsifier with an antioxidant capacity, a phosvitin-gallic acid (Pv-GA) complex was prepared via a free-radical method. This emulsifier characterizes some key technologies. Changes in the molecular weight of the Pv-GA complex were analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) and the matrix-assisted laser desorption/ionization time of light mass spectrometry (MALDI-TOF-MS). Fourier transform infrared spectroscopy (FTIR) indicated that C=O, C-N and N-H groups were also likely to be involved in the formation of the complex. A redshift was obtained in the fluorescence spectrogram, thereby proving that the covalent combination of Pv and GA was a free radical-forming complex. The results indicated that Pv and GA were successfully conjugated. Meanwhile, the secondary structure of Pv showed significant changes after conjugation with GA. The antioxidant activity and emulsifying properties of the Pv-GA complex were studied. The antioxidant activity of the Pv-GA complex proved to be much higher than that of the Pv, via assays of the scavenging activities of 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals and because of their ability to reduce power. The emulsification activity of the Pv-GA complex was also slightly higher than that of Pv. To function with the most demanding antioxidant and emulsification activities, the optimum conjugation condition was Pv (5 mg/mL) conjugated 1.5 mg/mL GA. Furthermore, the mechanism of Pv-GA conjugation was studied. This study indicated that GA could quench the inner fluorescence of Pv, and this quenching was static. There was a strong interaction between GA and Pv, which was not obviously affected by the temperature. Furthermore, several binding sites were close to 1, indicating that there was an independent class of binding sites on Pv for GA at different temperatures. The conjugation reaction was a spontaneous reaction, and the interaction forces of GA and Pv were hydrogen bonds and van der Waals force.

Dataset Information

The gallic acid-phospholipid complex improved the antioxidant potential of gallic acid by enhancing its bioavailability.

Publications

The gallic acid-phospholipid complex improved the antioxidant potential of gallic acid by enhancing its bioavailability.

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