Limits...
Pharmacokinetic Interaction of Chrysin with Caffeine in Rats.

Noh K, Oh do G, Nepal MR, Jeong KS, Choi Y, Kang MJ, Kang W, Jeong HG, Jeong TC - Biomol Ther (Seoul) (2016)

Bottom Line: In addition to the oral bioavailability of chrysin, its phase 2 metabolites, chrysin sulfate and chrysin glucuronide, were determined in rat plasma.As results, the pharmacokinetic parameters for caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) were not changed following chrysin treatment in vivo, despite of its inhibitory effect on CYP 1A in vitro.Taken together, it was concluded that the little interaction of chrysin with caffeine might be resulted from the rapid metabolism of chrysin to its phase 2 metabolites which would not have inhibitory effects on CYP enzymes responsible for caffeine metabolism.

View Article: PubMed Central - PubMed

Affiliation: College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea.

ABSTRACT
Pharmacokinetic interaction of chrysin, a flavone present in honey, propolis and herbs, with caffeine was investigated in male Sprague-Dawley rats. Because chrysin inhibited CYP1A-selective ethoxyresorufin O-deethylase and methoxyresorufin O-demethylase activities in enriched rat liver microsomes, the pharmacokinetics of caffeine, a CYP 1A substrate, was studied following an intragastric administration with 100 mg/kg chrysin. In addition to the oral bioavailability of chrysin, its phase 2 metabolites, chrysin sulfate and chrysin glucuronide, were determined in rat plasma. As results, the pharmacokinetic parameters for caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) were not changed following chrysin treatment in vivo, despite of its inhibitory effect on CYP 1A in vitro. The bioavailability of chrysin was found to be almost zero, because chrysin was rapidly metabolized to its sulfate and glucuronide conjugates in rats. Taken together, it was concluded that the little interaction of chrysin with caffeine might be resulted from the rapid metabolism of chrysin to its phase 2 metabolites which would not have inhibitory effects on CYP enzymes responsible for caffeine metabolism.

No MeSH data available.


Related in: MedlinePlus

Structure of chrysin.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
getmorefigures.php?uid=PMC4930290&req=5

f1-bt-24-446: Structure of chrysin.

Mentions: Chrysin (5,7-dihydroxy-2-phenyl-4H-chromen-4-one, Fig. 1) is a naturally present flavone contained in propolis and honey (Siess et al., 1996), and herbs, such as Passiflora coerulea and Passiflora incarnata (Wolfman et al., 1994; Brown et al., 2007). It showed several pharmacological effects, such as hepatoprotective (Pushpavalli et al., 2010), antioxidant (Villar et al., 2002), anti-inflammatory (Cho et al., 2004), and anti-aromatase activity (Kellis and Vickery, 1984). Because chrysin has recently been used as a nutritional supplement to promote anabolic hormones, the possibility of drug interaction has also been increasing. Nevertheless, drug interaction study with chrysin has rarely been reported.


Pharmacokinetic Interaction of Chrysin with Caffeine in Rats.

Noh K, Oh do G, Nepal MR, Jeong KS, Choi Y, Kang MJ, Kang W, Jeong HG, Jeong TC - Biomol Ther (Seoul) (2016)

Structure of chrysin.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4930290&req=5

f1-bt-24-446: Structure of chrysin.
Mentions: Chrysin (5,7-dihydroxy-2-phenyl-4H-chromen-4-one, Fig. 1) is a naturally present flavone contained in propolis and honey (Siess et al., 1996), and herbs, such as Passiflora coerulea and Passiflora incarnata (Wolfman et al., 1994; Brown et al., 2007). It showed several pharmacological effects, such as hepatoprotective (Pushpavalli et al., 2010), antioxidant (Villar et al., 2002), anti-inflammatory (Cho et al., 2004), and anti-aromatase activity (Kellis and Vickery, 1984). Because chrysin has recently been used as a nutritional supplement to promote anabolic hormones, the possibility of drug interaction has also been increasing. Nevertheless, drug interaction study with chrysin has rarely been reported.

Bottom Line: In addition to the oral bioavailability of chrysin, its phase 2 metabolites, chrysin sulfate and chrysin glucuronide, were determined in rat plasma.As results, the pharmacokinetic parameters for caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) were not changed following chrysin treatment in vivo, despite of its inhibitory effect on CYP 1A in vitro.Taken together, it was concluded that the little interaction of chrysin with caffeine might be resulted from the rapid metabolism of chrysin to its phase 2 metabolites which would not have inhibitory effects on CYP enzymes responsible for caffeine metabolism.

View Article: PubMed Central - PubMed

Affiliation: College of Pharmacy, Yeungnam University, Gyeongsan 38541, Republic of Korea.

ABSTRACT
Pharmacokinetic interaction of chrysin, a flavone present in honey, propolis and herbs, with caffeine was investigated in male Sprague-Dawley rats. Because chrysin inhibited CYP1A-selective ethoxyresorufin O-deethylase and methoxyresorufin O-demethylase activities in enriched rat liver microsomes, the pharmacokinetics of caffeine, a CYP 1A substrate, was studied following an intragastric administration with 100 mg/kg chrysin. In addition to the oral bioavailability of chrysin, its phase 2 metabolites, chrysin sulfate and chrysin glucuronide, were determined in rat plasma. As results, the pharmacokinetic parameters for caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) were not changed following chrysin treatment in vivo, despite of its inhibitory effect on CYP 1A in vitro. The bioavailability of chrysin was found to be almost zero, because chrysin was rapidly metabolized to its sulfate and glucuronide conjugates in rats. Taken together, it was concluded that the little interaction of chrysin with caffeine might be resulted from the rapid metabolism of chrysin to its phase 2 metabolites which would not have inhibitory effects on CYP enzymes responsible for caffeine metabolism.

No MeSH data available.


Related in: MedlinePlus