Hesperidin: Bioavailability Challenges

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Hesperidin is a flavanone glycoside found in citrus fruits of the following kinds:

  • Bitter Orange, Petitgrain
  • Citrus sinensis
  • Zanthoxylum gilletii
  • Lemon
  • Tangerine
  • Lime
  • Leaves of Agathosma serratifolia
  • Peppermint

The challenge with consuming hesperidin is that only 25% of orally consumed hesperidin is absorbed or made bioavailable.

The bioavailability of a natural substance is the measure of how much a substance you take truly gets into your bloodstream and is delivered to its sites of action in your body.

The bioavailability of hesperidin in generally poor. 

The main reason for this is hesperidin in its original form is not very water soluble.  Hesperidin and hesperidin can both exist as (S) and (R) isomers.  Natural hesperidin (e.g., tangerines), contain 100% of the S isomer whereas supplemental hesperidin usually contains S 50% and R 50% isomers.

To solve the challenge of hesperidin’s poor bioavailability, a number of options can be pursued:

Consume dried orange/lemon peels

If orange/tangerine or lemon peels (after being thoroughly washed) are dried for 5 to 7 days, the hesperidin content of the dried peels is roughly 5-10%.  If 5 grams of those dried peels are consumed, then a dose of 500mg of hesperidin can made bioavailable.  The best way to consume these dried peels is to grind the peels down to granules or a fine powder.  These granules or powder can be added to a smoothie.  However, they should never be cooked with heat.  Lemon or orange peel powder can be purchased at health food stores or spice stores.

Supplemental Hesperidin

There are a few forms of hesperidin in supplemental form that are more bioavailable than the original form:

α-Glycosyl hesperidin  (G-Hesperidin)  1

α-Glycosyl hesperidin, a novel hesperidin derivative wherein equimolar or more D-glucose residues are bound to hesperidin via the d-bond, is formed by a saccharide-transferring enzyme in a liquid containing hesperidin and α-glucosyl saccharide. The α-glycosyl hesperidin is easily recovered from the reaction mixture with a synthetic macroporous resin. α-Glycosyl hesperidin is superior in water-solubility, substan­tially tasteless and odorless, free of toxicity, and readily hydrolyzable in vivo into hesperidin and D-glucose to exhibit the physiological activity inherent to hesperidin.

Hesperidin Methyl Chalcone (HMC)

While hesperidin in its original form is not very water soluble, hesperidin methyl chalcone (HMC) is highly water soluble for greater absorption in the gastrointestinal tract. 

CordiartTM  2

Cordiart™ has been specially formulated to contain a very high ratio of the active form of the molecule (the “S” form) compared with the less active form (the “R” form). This mimics natural oranges, which contain 100% “S”—and is distinctly different from conventional hesperidin supplements, which contain nearly equal amounts of “S” and “R” forms.

This increased bioavailability comes as a result of Cordiart™’s unique formulation. BioActor recently conducted a study to determine the bioavailability of Cordiart™ compared to a generic rutinoside extract. In a cross over study, 10 healthy subjects either received 500 mg of Cordiart™, or 500 mg of a generic rutinoside extract on separate days. After ingestion of the product, blood samples were taken at regular intervals during 24 hours and urine was collected. Results showed that Cordiart™ has a 50% higher bioavailability compared to generic rutinoside. Furthermore, Cordiart™ showed a faster and higher absorption into the blood during the first hour after ingestion.


Resources:

Swanson Health Products – EndoPro Endothelial Support Formula

Life Extension – NitroVasc with Cordiart

Doctor’s Best – Best Hesperidin Methyl Chalcone


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