What is the Effect of Phloretin, a Raw Material of Plant Natural Extracts, on Skin Whitening

1. Introduction of phloretin

Phloretin, alias: trihydroxyphenol acetone, belongs to flavonoids, which is mainly distributed in apple branches and leaves, apple fruit/bark, apple tree rhizome/bark, lychee peel, Tibetan medicine, dry leaves from Malus toringoides and Malus transitoria, and other plants.

Its chemical name is 2,4,6-trihydroxy-3-(4-hydroxyphenyl) propiophenone, the molecular formula is C15H14O5, and the molecular weight is 274.27. It is soluble in alkaline solution, easily soluble in methanol, ethanol and acetone, and almost insoluble in water.

With the increase in the market share of plant-based functional cosmetics, phloretin has successfully attracted the attention of researchers in the beauty industry with its multi-functional beauty effects.

Studies have found that phloretin has various pharmacological effects such as anti-oxidation, anti-tumor, anti-inflammatory, immunosuppressive, and promoting bone formation. In addition, it also has the effects of whitening and removing acne.　

Phloretin can be directly absorbed by the human body, but in plants, there is very little naturally occurring phloretin. Phloretin is mostly in the form of its glycoside derivative - phloridin. Phloredin absorbed by the body is first in the gastric mucosa. After the glycosidic group is removed to produce phloretin, it can enter the circulatory system, thus exerting the phloretin benefits.

2. Biological activity of phloretin

01. Anti-oxidant and anti-free radical effects

Flavonoids have anti-lipid oxidation activity, which has been confirmed as early as the 1960s: Many flavonoids polyhydroxyl structures can be chelated with metal ions to have significant antioxidant properties.

Phloretin, as s kind of antioxidant plant extracts, has strong antioxidant properties, has an antioxidant effect on oils, and can remove free radicals in the skin.

Experiments show that when the final concentration of the system is 13μmol/L, the inhibition rate of phloretin on lipid peroxidation is about 53%; When the final concentration of the system is 32μmol/L, the scavenging rate of phloretin to eliminate DPPH free radicals can reach 74.6%.

Free radicals are harmful substances produced by oxidation reactions and are related to human degenerative diseases. The topical phloretin can prevent carbohydrates from entering the epidermal cells, thereby inhibiting the excessive secretion of the skin glands, and treating exuberant acne.

02. Whitening and spot-fading effect

Numerous research results show that the whitening mechanism of phloretin is mainly to inhibit the body's tyrosinase activity, thereby reducing the body's melanin production.

In terms of tyrosinase, we know that it is an important catalytic enzyme for the synthesis of melanin, and phloretin has a high inhibitory activity on tyrosinase, and the effect is better than that of arbutin and kojic acid.

In addition, the inclusion compound of hydroxypropyl-β-cyclodextrin and phloretin also has a good inhibitory effect on tyrosinase activity. Studies have also found that the combination of 34.9% ferulic acid, 35.1% phloretin and 30% water-soluble VE has a synergistic anti-oxidant whitening effect.

03. Promote transdermal absorption

Phloretin definition is a lipophilic compound that can penetrate into the skin through intercellular lipids. One of the reasons is that it can change the membrane dipole potential of the phospholipid bilayer, affecting the interface structure of the phospholipid bilayer and the water osmotic driven flow dynamics.

Studies have also found that when phloretin is used as a medium to do the transdermal absorption experiment of lidocaine hydrochloride, the absorption amount is 5.4 times that of the original; In the experiment of phloretin and phloridin acidizing intestinal glucuronidation and the absorption of acetylamino acid phenol and 1-naphthol, the results showed that phloretin and phlorizin can inhibit the effect of glucuronidation, promote the absorption of acetaminophen and 1-naphthol in the small intestine, and significantly increase its pharmacological activity.

04. Anti-inflammatory activity

With a plant extracts factory, we know that when the skin barrier is damaged, the permeability of irritants will increase, and different cells will be induced to release pro-inflammatory factors and chemokines to regulate the progress of immunity and inflammation, thereby promoting the production of sensitive skin. Therefore, it is concluded that inhibiting the production of inflammatory factors and chemokines can inhibit or reduce the damage of skin tissue during the inflammatory reaction process.

As a plant extract supplier, we have made many experiments of phloretin to explore its anti-inflammatory activity. In the anti-inflammatory experiment of phloretin, in vitro studies have shown that phloretin can inhibit the production of inflammatory factors, chemokines and differentiation factors; It can inhibit the ability of monocytes to adhere to keratinocytes and hinder signal proteins and hinder the phosphorylation of kinase Akt and MAPK to achieve anti-inflammatory effects.

Not only that, modern medicine shows that the important factors related to the pathogenesis of acne and the factors that cause inflammation are often not isolated.

The topical phloretin can prevent carbohydrates from entering the epidermal cells, inhibit the excessive secretion of the skin glands, and achieve the effect of treating exuberant acne. At the same time, the entry of phloretin into the cell can significantly reduce the activity of the COX-2 promoter, inhibit the production of prostate E2, and alleviate the inflammatory response of acne-type skin.

In summary, phloretin is not only used in whitening and anti-aging products, but also in anti-acne or soothing cosmetics.