CHED 860 |
| 15 years ago, an observation was made concerning the administering of a high blood-pressure drug, felodipine, with grapefruit juice. Felodipine, when taken with grapefruit juice increased the plasma levels of felodipine in patients, lowering the patients blood pressure more than expected. This suggested that something in the grapefruit juice was inhibiting the metabolic breakdown of the drug. In 2006, researchers were able to show that the cause of the increase in plasma levels was due to the inhibition of an important enzyme, known as cytochrome P450 CYP3A5, found in the small intestine. The cause of the inhibition was from a natural compound known as 8-methoxypsoralen found in the grapefruit juice. The exact nature and mechanism of the inhibition was not investigated. Using a Turner Quantech Digital Filter Flourometer (FM109535) along with a modified assay from BD Biosciences, the inhibitory effects of 8-methoxypsoralen on cytochrome P450 CYP3A5 were examined. At present, 8-methoxyposoraen has been found to inhibit the enzyme in vitro. The possible types of inhibition; competitive, non-competitive, etc are being investigated. |
|
Undergraduate Research Poster Session: Biochemistry
2:00 PM-4:00 PM, Monday, April 7, 2008 Morial Convention Center -- Hall A, Poster
Division of Chemical Education |