Arbutin easily soluble in water, methanol insoluble in chloroform, ether, petroleum ether, etc. Because it was originally derived from natural green plants, it is a skin whitening active substance. It is an ideal whitening agent for whitening cosmetics. It has two optical isomers, α and ß, and the ß isomer is biologically active.
Source: Derived from bearberry of Rhododendronaceae, named after being found in the leaves of bearberry, found in the leaves of Vaccinium genus Vaccinium in Rhododendronaceae, sand pear tree in Rosaceae Pyrus, etc. After extraction, it can be used as medicine and Cosmetic additives used.
The principle of whitening effect: by inhibiting the activity of the enzyme tyrosinase that produces melanin, reducing the production of melanin, to achieve whitening effect. The arbutin active molecule can penetrate the base layer for deep spot lightening, and has a therapeutic effect on leftover pigmentation such as chloasma. 5% concentration is the safest and most effective concentration for lightening spots, and will not cause irritation to the skin. Arbutin with a concentration of more than 7% may be sensitive to light, absorbed by the skin, decomposed by light, and reduced to hydroquinone, resulting in a whitening effect.
The effect of arbutin：
1.Lighten dark spots
Arbutin inhibits the activity of tyrosinase in the body, prevents the oxidation of tyrosine, affects the synthesis of dopa and dopaquinone, inhibits the production of melanin, reduces the deposition of skin pigment, so as to achieve the effect of lightening spots and whitening skin. Effect.
2.Pain relief and anti-inflammation
Arbutin also has analgesic and anti-inflammatory effects. It has strong anti-inflammatory and analgesic abilities. When applied to burns and scalds, it can effectively reduce inflammation and swelling, and speed up wound healing.
3.Antitussive and expectorant
Arbutin can relieve cough and eliminate phlegm, increase the mucus secretion of organs, prolong the incubation period of cough caused by ammonia water, and reduce the frequency of coughing.
alpha-Arbutin：
The physical state of α-arbutin is white to light gray powder, and it is easily soluble in water and ethanol.
alpha-Arbutin can inhibit the production and deposition of melanin, and remove spots and freckles. Arbutin can inhibit the activity of tyrosinase at a relatively low concentration, and its inhibitory effect on tyrosinase is better than that of arbutin. alpha-Arbutin can be used in cosmetics as a whitening agent.
α-arbutin can inhibit the activity of tyrosinase at a relatively low concentration, and its inhibitory effect on tyrosinase is better than that of arbutin.
The preparation method of arbutin:
The general steps of chemical synthesis of arbutin are to obtain glycosylation after proper protection of glucose and hydroquinone, and then deprotection. The glycosylation reaction is the basis of arbutin synthesis. According to the different glycosyl donors in the reaction, it can be divided into two types: the Koenigs-Knorr synthesis method with bromoglycoside as the donor and the Helferich synthesis with the acyl group as the donor. method.
The preparation methods of arbutin mainly include: natural plant extraction method, plant tissue culture method, chemical synthesis method and enzyme conversion method. The raw materials of the chemical synthesis method are easy to obtain, the process is relatively simple, and the product purity is high. The cost of natural extraction is too high, the purity is not high, and the operation is complicated.
α-Arbutin VS β-Arbutin
1. The price of α-arbutin is about 8 times that of β-arbutin.
2. The whitening effect of α-arbutin is more than 15 times that of β-arbutin.
3. α-arbutin has a strong inhibitory effect on tyrosinase activity.
4. α-Arbutin has good stability, α-Arbutin will not decompose at high temperature of 100°C; β-Arbutin will decompose in a small amount when it exceeds 60°C.
5. α-Arbutin has no photosensitivity and can be used during the day.
6. α-Arbutin does not exist in nature and can only be obtained through fermentation.
7. β-arbutin has been used in the market for a long time, so arbutin is generally called β-arbutin instead of α-arbutin.
Test methods
The determination methods of arbutin are mainly high performance liquid chromatography and capillary electrophoresis. The determination methods of hydroquinone and phenol are mainly high performance liquid chromatography, gas chromatography and gas chromatography-mass spectrometry. The method for the simultaneous determination of arbutin, hydroquinone and/or phenol in cosmetics is mostly HPLC
