BERBERINE, A NATURAL TREASURE FOR HUMAN HEALTH

Berberidaceae, the barberry family of the buttercup order (Ranunculales), comprises 14 genera and 701 species of perennial herbs and shrubs. (1)

In the Berberidaceae family, the genus Berberis comprises of around 450–500 species, which represent the main natural source of berberine. Berberine is a plant alkaloid with a long history of medicinal use in both Ayurvedic and Chinese medicine.

Among the various species of Berberis genus, Berberis aristata DC is one of the most important species due to its wide medicinal properties. It has been used in traditional medicine for its antimicrobial, antiprotozoal, antidiarrheal and antitrachoma activity. (2) Berberine is a quaternary ammonium salt derived from isoquinoline alkaloid and it is supported by reliable scientific literature proving its health benefits in multifactorial conditions, including the support in controlling healthy blood levels. (3) The berberine alkaloid can be found in the roots, rhizomes, and stem bark of the plants.

Specifically, berberine’s proven effectiveness in the management of multifactorial conditions is related to its so-called “Cloud Effect”: its pleiotropic effect simultaneously targets both root causes (e.g. low-grade chronic inflammation, oxidative stress, gut microbiota modulation) and marks (e.g. insulin levels) through the modulation of several cellular targets (e.g. AMPK, mitochondria, insulin-receptor, key metabolic and pro-inflammatory enzymes, etc.). This helps optimize peripheral blood metabolic profiles by modulating plasma sugar, insulin and lipids levels, thus resulting as a precious resource for the metabolic wellbeing. (4)

CAROLINA D'INTRONA

Reckitt | Francia

Bio...

Like many natural compounds, berberine has a poor bioavailability. For this reason, high dosages are traditionally recommended for berberine, that means low tolerability and gastrointestinal side effects.

To face such issue, Indena developed since years Phytosome^®, the proprietary biomimetic strategy for the delivery of natural ingredients, allowing human body to absorb them in the best possible way. It is a fundamental asset, and an internationally recognized scientific reference for the delivery systems of natural active ingredients. Phytosome^® combines food-grade sunflower lecithin with botanical and natural substances maintaining the original components’ profile and benefits. Numerous scientific studies have proven that Phytosome^® system delivery offers optimized human pharmacokinetic profiles and effectiveness compared to non- formulated equivalent compounds.

Working on berberine, Indena developed BERBEVIS^®, a new and innovative Phytosome® composition, which includes both pea proteins, as a natural vegetable protein carrier, and a powerful, natural antioxidant such as grape seed extract to optimize BERBEVIS^® tolerability profile (5).

Remarkably, a human pharmacokinetic study has confirmed that BERBEVIS® has optimized berberine bioabsorption, fostering the substance’s bioavailability on molar basis and with observed dose linearity (6).

In vitro studies have also shown that Phytosome^® formulation enhances berberine solubility in gastrointestinal fluids; has a better bioaccessibility than unformulated Berberis extract, improving the amount of berberine released into the gastrointestinal tract and available for absorption; has a higher safety profile than unformulated Berberis extract with the absence of negative impact on intestinal membranes. BERBEVIS^® appears then to be suitable for a long-term administration.

BERBEVIS^®, INDENA’S NEXT GENERATION PHYTOSOME^®, TO FACE THE CHALLENGE OF BERBERINE’S POOR BIOAVAILABILITY

It’s known that berberine has a multiple mechanism of action on multifactorial conditions. With the aim for the first time to measure the whole range of marks modulation, BERBEVIS^® has been used to supplement the diet of subjects enrolled in a human study focused on PCOS (Polycystic Ovary Syndrome), a complex, multifactorial, endocrine-metabolic disorder.

Clinical evidences show that BERBEVIS^® supplementation is the winning multi-target approach to metabolic health maintenance: it optimizes insulin levels effectively and noticeably modulates the blood sugar profile, optimizing both blood glycaemia and insulin. Moreover, a favorable safety profile was reported, with no major adverse events.

As secondary endpoints, BERBEVIS^® effectively supports metabolic health, having a positive effect on blood lipid profile, body composition and fostering the redistribution of adipose tissue even in subjects who are not following a low-calorie diet; it promotes hormonal balance, has a positive effect on low-grade chronic inflammation, and it’s also helpful for healthy skin, being acne a typical condition of PCOS highly affecting quality of life (7).

All in all, BERBEVIS^® is a potent, natural health-food ingredient that might help blood sugar control in a plethora of multifactorial challenges, which represent one of the greatest global health issues of our time.