bergamottin


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bergamottin

(bĕr-ga-mot'in),
One of a group of chemicals found in grapefruit juice (collectively called furanocoumarins), which inhibit CYP450 3A4.
See also: furanocoumarin.

bergamottin

A natural furanocoumarin found in oil of bergamot, grapefruit juice as well as other citrus fruits. Bergamottin and its related metabolites are of pharmacological interest because they inhibit certain cytochrome P450 enzymes, especially CYP3A4, which metabolises an array of drugs from antihistamines to antihypertensives, explaining why certain drugs have greater bioavailability in people who eat a large amount of grapefruit.
References in periodicals archive ?
It remains to be established if there are any interactions with statins given that bergamot is a source of bergamottin which is believed to be responsible for the grapefruit juice effects on the metabolism of some drugs, including statins (Li et al.
The compounds exerting this action are thought to be either the flavanoids such as naringin and naringinen (17,18,19,20) or the furanocoumarins such as bergamottin and its derivatives (21,22,23,24), but there is no clear consensus.
Drugs associated with moderate (50%-80%) inhibition of 17P were fluconazole (Diflucan), itraconazole (Sporanox), diltiazem, esomeprazole (Nexium), tacrolimus, and bergamottin.
There are several compounds and dimers of bergamottin in grapefruit juice and in vitro they have inhibitory effects on CPY3A4 (17).
This group includes bergamottin, dihydroxybergamottin (DHB), and a variety of related dimers.
Now, researchers at the University of Michigan and Parke-Davis Pharmaceutical Research, both in Ann Arbor, have identified a compound in grapefruit juice called bergamottin that could be responsible for the effect.
The finding builds on previous research, done in collaboration with scientists at Wayne State University in Detroit, that isolated a derivative of bergamottin and found that it inactivates the enzyme.
Bergamottin is "an important lead, but the jury is still out" on whether it causes the grapefruit juice effect, says David G.
Effect of grapefruit juice, naringin, naringenin, and bergamottin on the intestinal carrier-mediated transport of talinolol in rats.