Bakuchiol in the Management of Acne-affected Skin

Jul 1, 2011 | Contact Author | By: Ratan K. Chaudhuri, PhD, Sytheon Ltd. and Francois Marchio, Sytheon SARL
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Title: Bakuchiol in the Management of Acne-affected Skin
acnex bakuchiolx antioxidantx anti-inflammatoryx antibacterialx matrix metalloproteasex
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Keywords: acne | bakuchiol | antioxidant | anti-inflammatory | antibacterial | matrix metalloprotease

Abstract: Bakuchiol, a meroterpene of plant origin, is shown here to act against four major pathophysiologic features that cause acne, suggesting its use to complement and/or enhance the effectiveness of current anti-acne agents. In addition, the material is non-irritating, presents no photo- or hydrolytic- stability issues and is easy to use.

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RK Chaudhuri and F Marchio, Bakuchiol in the Management of Acne-affected Skin, Cosm & Toil 126(7) 502 (2011)

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Acne vulgaris is a common, chronic and recurring disease that involves multiple etiological factors including follicular hyperkeratinization, increased sebum production, Propionibacterium acnes proliferation and inflammation. It affects about 80% of teenagers and young adults and is most prevalent in those aged 12 to 24 years, although it can occur at all ages. As many as 17 million people are thought to be affected in the United States alone and the acne therapeutics market is forecast to show moderate growth in revenues through 2016; market data suggests the global acne market was worth US $2.8 billion in 2009 and is estimated to reach revenues of $3.02 billion by 2016. This moderate increase in revenue is attributed to an overcrowding of the market with generics and increased consumer acceptance of alternative therapies, although the acne therapeutics market is witnessing a shift toward combination products using two or more effective acne treatments.

One of the major causes of acne is the increase in sex hormones, especially androgens such as testosterone, which occurs during puberty. Testerone is converted in the skin to dihydrotestosterone (DHT) by α-reductase, which stimulates the sebaceous glands to enlarge and produce more sebum. The more sebum produced, the worse the acne will become. Further, a study by Lee et al. suggests that DHT may also be involved in the production of proinflammatory cytokines in acne.

Abnormal follicular keratinization is also involved in the development of acne vulgaris. The presence of unsaturated fatty acids in sebum alter the calcium dynamics in epidermal keratinocytes and induce abnormal follicular keratinization,4 and if sebum and keratin block the skin pores, they can cause comedones—small, skin-colored bumps or papules—to develop and hair follicle walls to rupture. Further, bacterial and comedonal debris cause acne pimples or pustules, i.e., inflammatory lesions.

Acne typically appears on the oil-producing areas of the body, namely the face, chest and back, and can have short-term, potentially lasting psychological effects such as decreased self-esteem and self-confidence leading to social withdrawal and even depression. While the three levels of acne severity are generally considered mild, moderate or severe, even mild acne can be troublesome, especially to teenagers who see each pimple as a major cosmetic challenge.

Interestingly, using a genetic-based strategy, Bek-Thomsen et al. recently demonstrated that follicles from healthy skin were exclusively colonized by P. acnes, whereas the follicular microbiota of acne patients included, in addition to P. acnes, Staphylococcus epidermidis and minor proportions of other species.5 However, previous studies excluded Staphylococci as agents that play a role in the pathogenesis of acne due to their rapid development of resistance to therapeutic antibiotics.6 The presence of S. epidermidis exclusively in acne-affected follicles raises the question of the potential role of this species in acne.

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Table 1. Comparative P. acnes inhibitory activity of bakuchiol and salicylic acid*

Table 1. Comparative <em>P. acnes</em> inhibitory activity of bakuchiol and salicylic acid*

Further, while salicylic acid is a poor inhibitor of P. acnes, at certain concentrations, bakuchiol in combination with salicylic acid was found to be synergistic in inhibiting P. acnes (see Table 1).

Table 2. Antioxidant profile of bakuchiol

Table 2. Antioxidant profile of bakuchiol

The described study also showed that bakuchiol has broad-spectrum antioxidant activity and effectively quenches superoxide-, hydroxy-, peroxy-, peroxynitrile radicals and singlet oxygen non-radicals in addition to inhibiting lipid peroxidation (see Table 2).

Table 3. Percent reduction in acne after product treatment

Table 3. Percent reduction in acne after product treatment

The percent reduction in acne using the Global Acne Grading System14 is summarized in Table 3.

Figure 1. Structure of bakuchiol

Figure 1. Structure of bakuchiol

Meroterpene, especially bakuchiol (see Figure 1), has been reported to exhibit strong antibacterial effects.

Figure 2. Down regulation of 5-a-reductase expression

Figure 2. Down regulation of 5-a-reductase expression

At 10 µg/mL, both bakuchiol and retinoic acid showed approximately 40% reductions in 5-α-reductase expression, compared with the placebo (see Figure 2).

Figure 3. Treatment with 1% bakuchiol lotion a) at baseline, and b) after six weeks of treatment

Figure 3. Treatment with 1% bakuchiol lotion a) at baseline, and b) after six weeks of treatment

These results clearly show that bakuchiol is an effective ingredient (see Figures 3 and 4), especially when combined with an exfoliating agent like salicylic acid, for the treatment of acne.

Figure 4. Treatment with 1% bakuchiol lotion a) at baseline, and b) after six weeks of treatment

Figure 4. Treatment with 1% bakuchiol lotion a) at baseline, and b) after six weeks of treatment

These results clearly show that bakuchiol is an effective ingredient (see Figures 3 and 4), especially when combined with an exfoliating agent like salicylic acid, for the treatment of acne.

Footnotes (CT1107 Chaudhuri)

a Sytenol A (INCI: Bakuchiol) is a product of Sytheon Ltd. USA.
b The Cytofluor 2350 Microflurometer is manufactured by Millipore.
c The Enzcheck kit is manufactured by Molecular Probes.
d The Cytofluor 2350 microfluorometer is manufactured by Millipore.
e Retinol 50 C (INCI: Retinol (and) Polysorbate 20) is a product of BASF.
f Neutrophil elastase (cat. # 324681, lot# B74630), is manufactured by Calbiochem.
g Elastase Substrate VIII, Suc-Ala-Ala-Ala-pNA is manufactured by Calbiochem.
h Elastase substrate (cat. # 324745) is manufactured by Calbiochem.
j The BioRad microplate reader is manufactured by BioRad.
k The Oxytherm electrode unit is manufactured by Hansatech.

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