What is 4-Butylresorcinol

The official chemical name is 4-n-butyl resorcinol, but generally, everyone likes to simplify writing butyl resorcinol. The first one to add to the whitening product is the Japanese POLA, um~ the one that relies on the whitening pill in the domestic fire.

It is characterized by poor solubility in water and soluble in ethanol.

Mechanism action of 4-Butylresorcinol

• Tyrosinase plays a crucial role in melanin production because it controls the rate of melanin deposition.
• 4-n-butylresorcinol has an inhibitory effect on melanin production by directly inhibiting the activity of tyrosinase and B16 black-speed tumor cells inhibiting the synthesis of tyrosinase without causing any cytotoxicity.
• In some in vitro studies, 4-n-butylresorcinol was shown to inhibit melanin production, as well as tyrosinase activity and TRP-1.

Benefits of 4-Butylresorcinol

• Strong inhibitor of tyrosinase and peroxidase
• Effective skin whitening agent and normal skin toner
• An effective whitening agent for pigmentation of the skin
• Effective against chloasma (exposed hyperpigmented skin in the sun)
• It has a strong protective effect on DNA damage induced by H2O2.
• Proven to have an anti-glycation effect

Why you should choose 4-Butylresorcinol

First, we need to know why there is resorcinol.

Lipofuscin is one of the more difficult to deal with in melanin. In general, hydroquinone is used in medical beauty.

Hydroquinone is a very effective whitening agent. The whitening mechanism completely inhibits the activity of tyrosinase and prevents the formation of melanin, and the effect is very remarkable.

However, its side effects are equally obvious, and the benefits are much more harmful than the benefits of whitening.

• It is highly oxidizable in the air, and it must be used when adding it to cosmetics.
• can cause redness of the skin;
• If the concentration exceeds 5%, it will cause sensitization, and there are clinical examples of leukoplakia. Currently, the US Food and Drug Administration stipulates that hydroquinone products with a concentration greater than 4% are medical grade and are not allowed to be marketed.

Chemists and pharmacists have modified the potent drug hydroquinone to get 4-hydroxyphenyl-beta-D-glucopyranoside, which is what we often hear about as “arbutin”. The difference between hydroquinone is that arbutin has a small tail – glycoside than hydroquinone. It is a pity that the whitening effect is greatly reduced.

In recent years, the most popular ingredients of major brands are various derivatives of benzenediol.

But light stability of arbutin is very poor and only effective at night.

The safety of 4-n-butyl resorcinol has become a prominent highlight. Without the side effects of hydroquinone, it has a better curative effect than other resorcinol derivatives.

In the tyrosinase activity inhibition experiment, its data is even better than the big brother phenethyl resorcinol, which is 100~6000 times of the traditional whitening agent such as kojic acid arbutin!

Then in the subsequent advanced experimental melanin B16V, also showed a common advantage of resorcinol derivatives – inhibition of melanin production at concentrations that did not produce cytotoxicity.

In addition, there are many human experiments on 4-n-butyl resorcinol. In some 32 patients with chloasma, 0.3% 4-n-butylresorcinol and placebo were used on both cheeks. Twice a day for 3 months, the result was a significantly lower pigment reduction in the 4-n-butylresorcinol group than in the placebo group. There are people who do artificial pigmentation inhibition experiments after artificial sunburn, hmm~ the result is of course quite good~

Inhibition of human tyrosinase by 4-butylresorcinol

4-butylresorcinol, kojic acid, arbutin, and hydroquinone show in L-DOPA oxidase activity of tyrosinase. Determined by various concentrations of the inhibitors to allow for the calculation of IC50 values. This data is the average of three independent experiments.

Inhibition of melanin producing in MelanoDerm skin models by 4-butylresorcinol

Compare with 4-butylresorcinol, kojic acid, arbutin, and hydroquinone. Treat the spots twice a day for 12 weeks with the respective inhibitors. Assess efficacy after 4, 8, and 12 weeks. Data represent the mean of 14 subjects. *P < 0.05: statistically significant vs. the untreated control age spots.

Dosage and usage of 4-Butylresorcinol

The recommended dosage is 0.5%-5%. Although there are studies in Korea that have a certain effect on 0.1% cream, India has researched 0.3% cream but the market is mainly 0.5%-5%. It is more common, and the Japanese formula is still unclear, but POLA has been used. And the results and sales are quite impressive.

As mentioned above, 4-Butylresorcinol can be used in creams, but it is insoluble in water. Others such as lotions, creams, and gels are also available. Both POLA and Eucerin have 4-Butylresorcinol products.