No abstract

No abstract

Naringenin is a naturally occurring flavanone, possessing a variety of biological activity. Due to its rapid elimination, naringenin needs frequent administration to maintain an effective plasma concentration. We have evaluated the therapeutic potential of naringenin-phospholipid complex under oxidative stress conditions compared with free naringenin. Naringenin-phospholipid complex was prepared and assessed for antioxidant activity in carbon tetrachloride intoxicated rats at a dose level of 100 mg kg-1 (p.o.). Liver function tests were studied by assessing serum glutamate oxaloacetate transaminase, serum glutamate pyruvate transaminase, serum alkaline phosphatase and total bilirubin. Marker enzymes of liver, namely glutathione peroxidase, superoxide dismutase, catalase and thiobarbituric acid reactive substances, were measured to evaluate the antioxidant potential at the same dose level. The plasma concentration of naringenin was also measured. It was observed that the naringenin-phospholipid complex enhanced the antioxidant activity of the biomolecule and protected the liver significantly for a longer time as compared with free naringenin at the same dose level. Phospholipid complex of naringenin produced better antioxidant activity than the free compound with a prolonged duration of action, which may be helpful in reducing the fast elimination of the molecule from body.

Ellagic acid (EA) has been reported as a potent antioxidant from natural resources with several nutritional benefits. The major disadvantage of this phytoconstituent is its rapid elimination from the body after administration. To overcome this limitation, a novel dietary formulation of EA with phospholipid was developed to investigate the effect of this complex on carbon tetrachloride induced liver damage in rats. The antioxidant activity of the complex (equivalent of EA = 25 and 50 mg/kg of body weight) and free EA (25 and 50 mg/kg of body weight) was evaluated by measuring various enzymes in oxidative stress condition. The complex significantly protected the liver by restoring the activity of superoxide dismutase, catalase and liver glutathione, and thiobarbituric acid reactive substances with respect to the carbon tetrachloride treated group (P < 0.05 and < 0.01). The complex provided better protection to rat liver than free EA at the same dose. The serum concentration of EA obtained from the complex (equivalent to 80 mg/kg of EA) was higher (C(max) = 0.54 microg/mL) than that of pure EA (80 mg/kg) (C(max) = 0.21 microg/mL), and the complex maintained effective concentration for a longer period of time in serum. The experimental outcome highlighted better hepatoprotective activity of the EA complex due to its potential antioxidant property compared with the free EA tested at the same dose level.

The results proved that the andrographolide complex produced by this method has better bioavailability and hence improved hepatoprotective activity compared with andrographolide at the same dose. Andrographolide complexation is therefore helpful in solving the problem of rapid clearance and low elimination half-life associated with andrographolide from A. paniculata.