Phenolic and flavonoid content and in vitro inhibitory effect of some Amazonian fruit juices on CYP3A4 activity

Many foods interact with drugs and may cause changes in the pharmacological effects of the co-administered therapeutic agent. The enzyme CYP3A4, which belongs to the cytochrome P450 enzyme complex, is responsible for the metabolism of most drugs currently on the market and is involved in many drug interactions. Hence, the interaction of this enzyme with juices of some fruits, such as grapefruit, can affect the pharmacokinetics of various drugs. However, native fruits from the Amazon region have not yet been the target of this type of research. We determined total polyphenols and flavonoids of the Amazonian fruits acai (Euterpe precatoria), buriti (Mauritia flexuosa), camu-camu (Myrciaria dubia), cubiu (Solanum sessiliflorum), cupuacu (Theobroma grandiflorum), jenipapo (Genipa americana), and tapereba (Spondias mombin) and evaluated the effects of each fruit juice on CYP3A4 activity, using the star fruit (Averrhoa carambola) juice as positive control. Acai juice presented the highest content of total polyphenols and flavonoids (102.6 +/- 7.2 mu g gallic acid equivalent (GAE) per mL and 7.2 +/- 0.6 mu g quercetin equivalent (QE) per mL, respectively). All juices were able to inhibit the activity of CYP3A4. There was no residual activity of the drug-metabolizing enzyme for acai, buriti, cubiu, camu-camu, and tapereba juice, while for cupuacu, jenipapo and the positive control, the residual activity was 44.3, 54.3 and 20.2%, respectively. Additional studies should identify the phytocompound(s) responsible for this inhibition activity, to clarify the mechanisms involved in this phenomenon.

Automated summary

This study found that fruits from the Amazon region, including acai, buriti, camu-camu, cubiu, cupuacu, jenipapo, and tapereba, can inhibit the activity of the drug-metabolizing enzyme CYP3A4. Acai juice had the highest content of polyphenols and flavonoids among the fruits tested.