Grapefruit Seed Extract 

What are the characteristics of Grapefruit Seed Extract?

Native to Southeast Asia, the grapefruit has been known since ancient times and is said to have been developed in the eastern Mediterranean basin by the Arabs.

It was introduced in the 18th century by the English captain Shaddock in Barbados, hence the name chadèque sometimes given to grapefruit in the Caribbean.

This species will naturally hybridize with an orange tree, probably in Cuba, to provide grapefruit, cultivated in Florida as early as 1880 and widely consumed today.

In the Caribbean islands of Trinidad and Tobago, the grapefruit pericarp is traditionally used in hypertension.

The fruit contains furocoumarins which inhibit enzymes, cytochromes 3A4 capable of decreasing the degradation of drugs in the body and increasing their concentration, inducing an overdose.

Latin name :

• Citrus maxima

Botanical family :

• Rutaceae

Producing organ :

• Seed

Known or suspected mode of action :

• Limonene is expectorant
• Naringenin (flavonoid) is anti-arrhythmic

Precautions for use :

• Beware of the inhibitory effects of cytochromes P450 (modification of the metabolism of drugs with a low therapeutic margin in the sense of an increase in plasma concentrations), due to a synergy of action between flavonoids and coumarins
  • The furocoumarins present in grapefruit are irreversible inhibitors of intestinal cytochromes 3A4 (enzyme) and intestinal PGP (efflux transporter). Thus, any molecule (drug) substrate of these enzymes and / or these transporters will see its blood concentration increase.
  • Details from AFSSAPS: bergamottin and 6,7 dihydroxybergamottin , present in grapefruit, indeed exert a potent inhibitory effect on CYP3A4, which increases the intestinal absorption of drugs which are substrates of CYP3A4. The consequences are an increase in their dose-dependent adverse effects, equivalent to an overdose. Drugs at risk are those with a narrow therapeutic index. It would be:
    • simvastatin , and to a lesser extent, atorvastatin , lovastatin
    • immunosuppressants ( tacroIimus, ciclosporin, etc.), with an increased risk of nephrotoxicity
    • cisapride , with a risk of torsades de pointes
• Risk of numerous drug interactions, ask your pharmacist for advice

Main components of the plant :

• Furanocoumarins
• Flavonoid: naringenin, naringin in the fruit, hesperidin
• Limonoids ( limonine, nomiline ) (modified triterpenes)
• Coumarins ( bergapten, bergamotin, etc.)
• Vitamin C (34.4 mg / 100 g)
• Carotenoids ( lycopene, β − carotene )
• Potassium, Calcium, Magnesium, Copper
• Limonene essential oil: 90%