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APIGENIN
Principal indication: dark circles
PURE ACTIVE A08
Bibliographical summary
 
  • INCI name : APIGENIN
  • Molecule more than 95% pure
    grapefruit extract
    (Citrus paradisi)
 

Apigenin is a flavonoid found naturally in fruits and vegetables like parsley, onion, celery, tea and grapefruit. One of the most common sources of apigenin consumption is chamomile. Apigenin is also found in red wine and beer. Apigenin is recognized as a bioactive flavonoid with anti-inflammatory, antioxidant, antiangiogenic, antiallergenic, antigenotoxic and anticancerous properties.

Epidemiological studies suggest that a diet rich in flavones reduces the risk of certain cancers, particularly breast, digestive tract, skin and prostate cancer. It has been suggested that apigenin plays a protective role in other diseases affected by the oxidative process, like cardiovascular and neurological disorders. Apigenin is also thought to have detoxifying properties, by inducing the UGT-glucuronosyltransferase responsible for the conjugation reaction of glucuronic acid.

This reaction is the main way to eliminate medication, xenobiotics (carcinogens and phytochemical substances) and endogenous substrates such as bilirubin and steroids.

 

  • ACTION MECHANISMS / PROOFS OF EFFECTIVENESS

 

Apigenin has chemopreventive and anti-inflammatory properties. Indeed, after sun exposure, it induces a considerable increase in apoptosis, the cell death mechanism [1]. It inhibits the release of prostaglandin, nitrite and arachidonic acid [2, 3, 4].

Apigenin has numerous vascular properties. It reduces the fragility of the blood capillaries by strengthening the dermal matrix supporting the microvascular network. Indeed, it inhibits a collagenase, matrix 1 metalloproteinase, and reduces its expression by inhibiting activation of the protein, AP-1[5]. Therefore, it reduces collagen degradation in the dermal matrix.

Moreover, it increases the natural ability to eliminate bilirubin. The glucuronide conjugation reaction is catalyzed by UDP-glucuronyltransferase 1A1 (UGT1A1). This enzyme is found in numerous tissues, abundant in the liver and also expressed by both keratinocytes and fibroblasts, although at a lower basal rate. Apigenin induces an increase in chrysin glucuronidation of 346% by UGT1A1 [6]. The induction of UGT1A1 by apigenin is mediated by Nf-B translocation [7].

Apigenin, through its antioxidant properties, considerably inhibits lipoxygenase [8]. Therefore, lipid peroxidation is reduced.

The dark circles caused by vascular coloration are a direct sign of the condition of the blood network. A reduction in the microcirculation of the blood results in darker, more marked and more apparent blood capillaries. The vascular walls are less elastic and less impermeable and will create local dilation and blood stasis. Blood stagnation will lead to capillary permeability and blood will pass from the capillaries to the interstitial environment. Haemoglobin then accumulates in the infraorbital area and degrades by oxidation into biliverdin, bilirubin or iron. Biliverdin is a dark green/purple pigment and bilirubin an orange to red/dark brown pigment. They are the cause of the undereye coloration characteristic of fatigue and accumulate in the epidermis and the dermis.

The release of iron helps to increase the blue coloration of the dark circles, giving that typical purple skin pigmentation. The preoxidant character of iron on lipid peroxidation, which also leads to an aggravating pro-inflammatory situation, as it is vasodilatory, and is an additional cause of activation of blood leakages and pigmentation that veers towards brown over the long term.

Apigenin improves the vascular walls by inhibiting collagenase, increases the capacity for bilirubin elimination by induction of UT1A1 and inhibits lipid peroxidation by inhibiting lipoxygenase, thus preventing the vasodilation causing the pigmentation.
These elements show that apigenin is an excellent active for treating dark circles with vascular coloration.

 

  • OUR EXPERT'S OPINION

 

This flavonoid, which has the activities of its chemical class, offers the originality of having undergone an in vitro assessment of its ability to increase the activity of glucuronyltransferase, the enzyme produced by conjugation to the glucuronide, a key process in increasing the solubility and elimination of hydrophobic molecules in the organism. In this respect, it may promote the elimination of pigments resulting from the degradation of haemoglobin.
This molecule has been proposed to improve the residual coloration of ecchymoses or dark circles…
Possessing an interesting rational factor, convincing clinical proofs should come to light with the use of this active, which is new to cosmetics. It is nonetheless similar to rutin or ruscogenin.
Its optimal active concentration has not yet been fully explored.
To our knowledge, transcutaneous penetration studies are unavailable, but the structure of the molecule should be favourable to its passing into a hydroalcoholic or glycolic environment.
In preventing oxidative damage, the molecule could be used like the other antioxidants. In improving dark circles, use will be continuous and we can assume that the activity will require a few days to express itself.
Other effects: regularization of pigmentation is mentioned in certain documents. The (phenolic) structure and the action mechanisms (electron quencher) make the molecule a credible candidate for evening out the complexion or a back-up treatment for vitiligo.
Interactions with the CPYs (cytochrome P) are reported (interference with the oxidative metabolism).

 

  • EFFECTIVE DOSE

 

The body of publications and scientific studies, customary usages of this active and our expert's opinion concur in using Apigenin pure Active at the dose of 25 mg per bottle.

 

  • BIBLIOGRAPHICAL REFERENCES

[1] Enhancement of UVB-Induced Apoptosis by Apigenin in Human Keratinocytes and Organotypic Keratinocyte Cultures. Abu-Yousif AO et al. Cancer Res, 68(8):3057-3065. 2008.
[2] Apigenin Prevents UVB-Induced Cyclooxygenase 2 Expression: Coupled mRNA Stabilization and Translational Inhibition. Tong X et al. Mol Cell Biol. 27(1):283-96. 2007.
[3] Suppression of inducible cyclooxygenase and inducible nitric oxide synthase by apigenin and related flavonoids in mouse macrophages. Liang YC et al. Carcinogenesis. 20(10):1945-52. 1999.
[4] Inhibition of TPA-induced cyclooxygenase-2 (COX-2) expression by apigenin throught downreglation of Akt signal transduction in human keratinocytes. Van Dross RT et al. Molecular carcinogenesis 44:83-91. 2005.
[5] Inhibition of mammalian collagenase, MMP-1, by naturally occuring flavonoids. Lim H. and Kim H.P. Planta Med. 73(12):1267-1274. 2007.
[6] Induction of human UDP-glucuronosyltransferase UGT1A1 by flavonoids-structural requirements. Walle UK, Walle T. Drug Metab Dispos. 30(5):564-9. 2002.
[7] Interactions between sulforaphane and apigenin in the induction of UGT1A1 and GSTA1 in CaCo-2 cells. Vanda Svehlikova et al. Carcinogenesis. 25(9):1629-37. 2004.
[8] Effect of flavonoids and cynarine from cynara cardunculus L. on lipoxygenase activity. Bezakova L. Acta facultatis pharmaceuticae universitatis comenianae Tomus LIV 2007.

This information is given for informative purposes. In no event does it constitute medical information, nor engage our liability. These documents may be copied and reproduced exclusively for informative purposes for personal and private use. All and any use of copies or reproductions for other purposes is expressly forbidden and shall engage the user's liability under Article L 122-3 of the Intellectual Property Code.