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.
Cytotoxicity was expressed as the concentration of bergamottin
inhibiting cell growth by 50% ([IC.
Effect of grapefruit juice, naringin, naringenin, and bergamottin
on the intestinal carrier-mediated transport of talinolol in rats.
like the furanocoumarins bergamottin
and isopimpinellin (Fig.
Metabolism of bergamottin
by cytochromes P450 2B6 and 3A5.