ArticlePDF AvailableLiterature Review

Fairness via formulations: A review of cosmetic skin-lightening ingredients

Authors:
  • DIC India

Abstract and Figures

Skin-lightening cosmetics are in big demand across Asia, and the quest for fairness has led to identification of many new ingredients. The mechanisms underlying pigmentation have been researched extensively and the knowledge is being updated regularly. This review serves to list the ingredients that are commercially available for that purpose and the modes of action through which the lightening is effected. Skin-lightening ingredients are also classified based on their sources; it is significant that far more botanicals have made the list than have synthesized compounds. Tyrosinase inhibition as a means of skin lightening is still the most reported method, followed by other methods such as Mitf inhibition, down regulation of MC1R activity, interference with melanosomal transfer, and melanocyte loss.
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J. Cosmet. Sci., 63, 43–54 ( January/February 2012)
43
Fairness via formulations: A review of cosmetic
skin-lightening ingredients
R. KAMAKSHI, Cavinkare Research Centre,
Ekkatuthangal, Chennai 600 032, India.
Accepted for publication August 31, 2011.
Synopsis
Skin-lightening cosmetics are in big demand across Asia, and the quest for fairness has led to identifi cation
of many new ingredients. The mechanisms underlying pigmentation have been researched extensively and
the knowledge is being updated regularly. This review serves to list the ingredients that are commercially
available for that purpose and the modes of action through which the lightening is effected. Skin-lightening
ingredients are also classifi ed based on their sources; it is signifi cant that far more botanicals have made the
list than have synthesized compounds. Tyrosinase inhibition as a means of skin lightening is still the most
reported method, followed by other methods such as Mitf inhibition, down regulation of MC1R activity,
interference with melanosomal transfer, and melanocyte loss.
INTRODUCTION
The defi nition of fair skin is given as “not dark and free from spots, specks, dirt or imper-
fection; unblemished; clean; pure.” The booming cosmetics industry in recent decades can
be partly attributed to the elusive search for fair and fl awless skin (1,2). With the vast
information that is accessible in the 21st century, one has an option to choose methods
ranging from that of Cleopatra (soaking in donkey milk that is rich in AHA) to recent
advances in skin-lightening procedures such as dermabrasion, ultrasound, and laser ther-
apies, to name a few (3–9).
Skin-lightening agents are any ingredient or combination of ingredients that interfere
in any step of the melanogenesis pathway, melanin transfer, or desquamation that results in
lowering pigmentation on the surface of the skin (10). Skin-lightening cosmetics are in
big demand across the world, and this review serves to list the ingredients that are com-
mercially available for that purpose and the modes of action through which the lighten-
ing is effected. There are many reports of skin-lightening agents obtained from both
natural and synthetic sources. However, many ingredients in their original form may not
be compatible in cosmetic formulations for application to the skin due to various factors
such as cytotoxicity, insolubility, instability, and their sensitive nature to external condi-
tions. However, consistent efforts are being made by industry to arrive at compatible,
minimally toxic, and highly effi cacious ingredients that serve the purpose.
JOURNAL OF COSMETIC SCIENCE44
PIGMENTATION IN SKIN
The color of our skin is due to the polymeric, amorphous, non-proteinaceous pigment
called melanin. Melanin is produced in the skin through a biochemical process called
melanogenesis. Dermal melanin is produced by melanocytes, which are found in the stra-
tum basale of the epidermis. The pathway of melanogenesis as elucidated by Raper (18)
and Mason (19) is shown below (Figure 1).
The difference in skin color between fair people and dark people is due not to the number
(quantity) of melanocytes in their skin, but to the melanocytes’ level of activity (quantity
and relative amounts of eumelanin and pheomelanin). In skin that exhibits a dark color
the melanosomes are well distributed in the keratinocytes, which absorb radiation (11).
Pigmentation in skin is determined by various physiological processes occurring at
different stages (12):
(a) Development of melanocytes
(b) Density of melanocytes
(c) Expression of the enzymatic and structural constituents of melanosomes
(d) Synthesis of melanin
(e) Transport of melanosomes to dendrites
(f) Transfer of melanosomes to keratinocytes
(g) Distribution of melanin in the supra basal layers of the skin
Figure 1. Raper-Mason pathway of melanogenesis.
SKIN-LIGHTENING COSMETIC INGREDIENTS 45
The fi rst three stages are completely controlled genetically, while the next four stages
are targets for manipulation through skin-lightening agents. The most important
factor other than inheritance affecting skin pigmentation is ultraviolet (UV) radiation
(Figure 2). Exposure to UV triggers the following reactions that cause darkening of the
skin (13–15):
(a) Oxidation and polymerization of melanin
(b) Redistribution of melanosomes
(c) Activation of MITF (microphthalmia-associated transcription factor) leading to
increased melanin content
(d) Increase in expression of α-MSH (melanocyte-stimulating harmone) leading to
enhanced melanocyte responses
(e) Transfer of melanin from the lower to the upper epidermis to prevent damage from
radiation
A very effective method of reducing UV-induced pigmentation would be to incorporate
sunscreens in the vehicle used for skin lightening. Physical sunscreens like zinc oxide and
titanium oxide are available to suit delivery vehicles like creams, lotions, gels, etc. Chem-
ical sunscreens may be chosen from a variety of synthetic compounds such as ethyl hexyl
methoxy cinnamate, butyl methoxydibenzoylmethane, phenyl benzimidazole sulfonic
acid, and other substituted salicylates.
SKIN LIGHTENING
Skin-lightening agents are those that cause depigmenting activity on human skin, and
they have been widely used in dermatology and cosmetics. A huge number of actives
(both from biological sources and synthetic chemical compounds) have been reported in
the literature (16,17). Their mechanism of action is generally through:
(a) Tyrosinase inhibition
(b) Mitf inhibition
(c) Down regulation of MC1R activity
Figure 2. Schematic representation of the effect of UV rays on skin leading to pigmentation.
JOURNAL OF COSMETIC SCIENCE46
(d) Interference with melanosome maturation and transfer
(e) Melanocyte loss, exfoliation
Successful treatments mostly combine two or more modes of action to achieve a synergis-
tic effect.
CLASSIFICATION OF SKIN-LIGHTENING INGREDIENTS
Skin-lightening ingredients can also be classifi ed by their source, such as the classes to
which they belong. The important classes are:
(i) Chemical tyrosinase inhibitors (hydroquinone and similar type of compounds)
(ii) Botanicals (essentially from plants and algae)
(iii) Anti-oxidants
(iv) Vitamins—A, B, C, E
(v) Peptides
(vi) Alpha and beta hydroxyl acids and derivatives
TYROSINASE INHIBITION
The inhibition of tyrosinase is the most widely reported screening method in the litera-
ture for skin-lightening ingredients. Tyrosinase is a copper-containing enzyme present in
melanocytes that catalyzes the production of melanin. The biosynthetic pathway of mela-
nin synthesis was fi rst elucidated by Raper (18). Tyrosinase inhibition may be achieved by
inhibitors from chemical or biological sources.
(i) Chemical tyrosinase inhibitors (Figure 3). There has been tremendous activity in the iden-
tifi cation of tyrosinase inhibitors that are of synthetic origin. Such compounds are gener-
ally highly pure and potent. Synthetic compounds of various classes like hydroquinone
and derivatives, phenolic amines, coumarins, chalcone analogs, hydroxy stilbene deriva-
tives, benzaldehyde analogs, biphenyls, and trihydroxy fl avones have been studied for
their tyrosinase inhibitory properties (21–33).
However, many of these compounds have been screened through in vitro assays and their
effi cacy and adverse effects need to be established through clinical trials. Chemical com-
pounds with depigmenting activity have been used in cosmetics for a long time. Some of
the best known tyrosinase inhibitors are hydroquinone, kojic acid, and similar types of
compounds.
(a) HYDROQUINONE AND DERIVATIVES. Hydroquinone is considered to be the gold standard for
depigmenting agents. Hydroquinone interacts with copper at the active site of the en-
zyme tyrosinase, thus decreasing its activity by nearly 90% (34). It not only limits ty-
rosinase but also oxidizes membrane lipids and proteins through generation of reactive
oxygen species (35). The radicals generated inhibit cellular metabolism by affecting
DNA and RNA synthesis (36). It is generally administered at concentrations ranging from
1.5% to 5% concentration. The use of hydroquinone in cosmetics has diminished because
of adverse side effects due to its cytotoxic nature. Monobenzyl ether of hydroquinone
SKIN-LIGHTENING COSMETIC INGREDIENTS 47
(MBEH) and monomethyl ether of hydoquinone (MMEH) also demonstrate tyrosinase
inhibitory properties (37–39). Further, they also cause melanocyte loss through genera-
tion of free radicals. However, the use of these compounds for depigmentation is limited
by their adverse effects, similar to those of hydroquinone.
(b) ARBUTIN. Arbutin is a naturally occurring β,D-glycopyranoside derivative of hydro-
quinone. Although it shows tyrosinase inhibition, it is not found to affect RNA synthe-
sis as does hydroquinone. The α-derivative shows a stronger inhibitory effect on tyrosinase
and melanosome maturation (40,41). It is also present in many of the botanical extracts.
Arbutin is highly pH-sensitive and can hydrolyze to hydroquinone at both acidic and
alkaline pH. Hence, care should be taken during use in commercial skin-lightening
products.
(c) KOJIC ACID. Kojic acid is a powerful tyrosinase inhibitor. It functions by the chelation of
copper at the active site of the enzyme tyrosinase (42). Further, it acts as an antioxidant
and a free radical scavenger. Although powerful, the use of kojic acid is under scrutiny by
dermatologists because of its adverse side effects such as allergic dermatitis (43). It
is found to be unstable in formulations and may also cause discoloration. Some stable
derivatives, such as kojic acid dipalmitate, are being used to enhance effectiveness by
enhanced skin penetration. Thus there exists a demand for safe and effective alternative
botanicals as preferred skin-lightening ingredients.
Figure 3. Structures of some skin-lightening agents.
JOURNAL OF COSMETIC SCIENCE48
(ii) Botanical extracts. Extracts mostly contain a combination of two or more classes of com-
pounds that work synergistically to achieve skin lightening. Botanicals connote nature and
are hence more acceptable to people. Further, a large number of yet undiscovered plants are
available to provide for exotic products and claims for cosmetics. However, it should also be
observed that natural extracts may be highly unstable and may not be compatible within
formulations. A large number of ingredients (Table I) have been studied for tyrosinase inhi-
bition and have been processed to make them viable for use in cosmetic products. These are
available commercially through suppliers for use as skin-lightening agents.
(iii) Antioxidants as skin-lightening agents. Antioxidants serve to reduce oxidation of tyrosine
to DOPA quinone and therefore are shown to have skin-lightening activity (64).
In addition, they act in the melanogenesis pathway, reducing the synthesis of melanin.
Exposure to UV radiation results in the generation of free radicals. It has been identifi ed
that ROS (reactive oxygen species) are able to oxidize tyrosinase and DOPA to melanin,
and this is one of the major causes for tanning (65). Although antioxidants are present in
tissues, they may not be able to reduce the radicals, depending on the extent of UV expo-
sure. Infl ammation is a source of free radicals. Hence the quenching of free radicals would
also help in reducing the synthesis of melanin, thereby contributing to skin depigmenta-
tion effects (66). The use of phytic acid, glutathione (Figure 4), and ubiquinone as popu-
lar skin-lightening agents is due to their strong antioxidant nature (67–68). Melanin
synthesis in melanocytes is accompanied by the generation of hydrogen peroxide that
can lead to the formation of ROS that further increase the proliferation of melanocytes.
Table I
Botanicals That are Mostly Used in Skin-Lightening Cosmetics
S. No. Extract Type Reference
1Morus alba extract 2-Oxyresveratrol 44
2Aloe barbadensis leaf extract Aloesin 45
3Crocus sativus extract Kaempferol 46
4Uva ursi Arbutin 47
5 Licorice extract Glabridin 48
6Camelia sinesis extract ECG 49
7Phylanthus embelica extract Vitamin C 50
8Citrus limonum extract Hisperidin 51
9Punica granatum extract Ellagitannins 52
10 Vitis vinifera (grape) fruit extract Procyanidins 53
11 Anise extract Anisic acid 54
12 Cumin seed extract Cumic acid 55
13 Cinnamonum cassia extract Trans-cinnamaldehyde 56
14 Artocarpus lakoocha heartwood extract 2-Oxyresveratrol 57
15 Purus comunis (pear) extract Arbutin 58
16 Geranium extract Ellagic acid 59
17 Ramulus mori extract 2-Oxyresveratrol 60
18 Ginseng extract p-Coumaric acid 61
19 Malpighia punicifolia (Acerola) fruit extract Polyphenols 62
20 Mushroom (Agaricus blazei Muril) extract Tri-terpenoids 63
SKIN-LIGHTENING COSMETIC INGREDIENTS 49
Most of the natural extracts contain fl avanoids that provide antioxidant effects and are
thus used as skin-lightening agents (69).
(iv) Vitamins as skin-lightening agents. Vitamins have been known to improve skin tone and
texture, and they have found remarkable acceptance among consumers. Most of the lead-
ing brands of skin-lightening agents that are available commercially utilize vitamins or
their derivatives as ingredients.
VITAMIN A. Vitamin A has been used for some decades for the removal of spots in Kligman’s
treatment (70). It is used along with hydroquinone and topical steroids for the treatment
of melasma. Tretinoin acts as a skin-lightening agent by inducing exfoliation. Further, it
accelerates the loss of epidermal melanin by increasing the turnover rate and by promoting
the proliferation of keratinocytes (71,72). However, users of tretinoin suffer from side
effects such as burning and increased photosensitization. Retinyl palmitate, a derivative
of retinoic acid, is used in skin-lightening cosmetic preparations.
VITAMIN B. Among the classes of vitamins that comprise vitamin B, two have been identi-
ed to have skin-lightening activity:
(a) Vitamin B3 (niacinamide): This is one of the most used hypopigmenting agents.
It is a well known antioxidant and interferes in melanasome transfer leading to skin
lightening. Using co-cultures of human melanocytes and keratinocytes, investiga-
tors have shown that niacinamide inhibits the transfer of melanosomes from mela-
nocytes to keratinocytes (73). The results of clinical studies using topically applied
niacin amide have demonstrated a reversible reduction in hyperpigmented lesions and
increased skin lightness compared with the vehicle alone after four weeks of use (74).
(b) Vitamin B5 (panthenoic acid): A derivative of vitamin B5, calcium pantetheine
sulfonate has been observed to interfere with the glycosylation of tyrosinase,
thereby leading to depigmenting effects (75).
VITAMIN C. Vitamin C is required for the production of collagen and is a photoprotectant as
it deactivates UV-induced free radicals and decreases erythema. Further, Vitamin C also
acts as a tyrosinase inhibitor, thereby lightening the skin (76). Although most effective,
ascorbic acid is a highly unstable compound. Stable derivatives of ascorbic acid in the
Figure 4. Structures of (a) glutathione and (b) phytic acid.
JOURNAL OF COSMETIC SCIENCE50
form of sodium ascorbyl phosphate (SAP), magnesium ascorbyl phosphate (MAP), and
ascorbyl palmitate are widely used in cosmetic products (77).
VITAMIN E. Vitamin E is the most important lipid-soluble antioxidant in the body. It is
abundant in the sebum and acts to absorb the oxidative stress of sunlight and skin expo-
sure. It has been demonstrated that vitamin E provides protection against UV-induced
infl ammation and hyperpigmentation (78). Vitamin E has also been studied in combina-
tion therapies with other vitamins as well as in other classes of skin-lightening com-
pounds (79,80).
Vitamins B, C, and E are used individually or in combination in many skin-lightening
treatment therapies.
(v) Peptides in skin lightening. Peptides are reported to reduce pigmentation through inter-
action with the protease-activated receptor 2 (PAR-2) of keratinocytes. PAR-2 activation
in involved in cell growth, differentiation, and infl ammatory processes and was shown to
affect melanin and melanosome ingestion by human keratinocytes (81). The protease-
activated receptor-2 upregulates keratinocyte phagocytosis. The peptide-based antago-
nist for PAR-2 can be used to regulate melanin ingestion by keratinocytes, thus effecting
skin-lightening.
Short peptides have also been reported in reducing the enzymatic activity of tyrosinase
(82). The use of sericin, a high-molecular-weight soluble glycoprotein from silk, as
a tyrosinase inhibitor has also been documented (83). Peptide residues that act as MSH
inhibitors have been known to lighten the skin. Soy trypsin inhibitors have been identi-
ed as interfering in melanosomal transfer, thereby reducing skin pigmentation (84).
(vi) Alpha and beta hydroxyl acids and derivatives. Alpha and beta hydroxyl acids have been
the most important class of compounds that are most widely used in cosmetic prepara-
tions. These act as superfi cial chemical peels that target the stratum corneum to improve
skin color and tone. They are comparatively pure and inexpensive, and they may be used
in higher amounts without many side effects (85). They are generally used in conjunction
with other skin-lightening agents to improve performance. Also referred to as fruit acids,
they improve skin texture by promoting desquamation or the shedding of the outer layers
of the stratum corneum. Alpha hydroxyl acids (AHA) have also been noted to increase
the enzymatic activity leading to epidermolysis. They are also employed in microderm-
abrasion techniques. In addition, they act as moisturizers and promote the synthesis of
elastin fi bers, leading to improved skin tone. However, care should be taken to neutralize
the skin after AHA treatment, as it might cause burning and erythema. The most com-
monly used AHAs are glycolic, lactic, citric, malic, pyurvic, and salicylic acids and their
derivatives.
THE EFFICACY OF SKIN-LIGHTENING FORMULATIONS
Formulations for skin lightening have been majorly based on o/w emulsions that have a
higher aesthetic appeal. The fact that many of the ingredients get better dispersions is
also an added feature for the choice of such emulsions. Recently gel-based formulations
are being considered for suitability in certain skin types. Effi cacy studies for skin-lightening
formulations are carried out through clinical trails. Some of the techniques used in-
volve the use of the mexameter, chromameter, spectrophotometer, and VISIA, along with
SKIN-LIGHTENING COSMETIC INGREDIENTS 51
dermatologist assessment. Also, other skin parameters such as moisturization, texture,
barrier integrity, pH, etc, are being evaluated to give picture of skin health after the use
of skin-lightening agents. This leads to screening the potentially harmful side effects of
hydroquinone-like substances in addition to the high-value claim proposition for the cos-
metics industry. With advances in technology in measurement techniques, it is becoming
easier to identify the effi cacy of formulations in different skin types.
CONCLUSION
Research in the area of skin-lightening agents in an expanding fi eld, with new ingre-
dients being added to the repertoire with every new discovery. Although tyrosinase
inhibition is still the most sought after mechanism skin lightening, newer pathways
are being identifi ed. It has been noted that ingredients that interfere with the path-
ways affecting melanin synthesis and transfer show promise as depigmenting agents.
Persistent research into skin lightening has also led to new mechanisms being discov-
ered in recent years.
The aspiration for light skin is on an upward curve and can be satisfi ed only when the
cosmetic in the bottle fulfi ls the promise of fair skin. A careful and complete investiga-
tion of the ingredient on the basis of its effi cacy and tolerance to individuals through
clinical trails is essential to ascertain that the product delivers the promise.
ACKNOWLEDGMENTS
We thank Dr. Yash Kamath for reviewing the manuscript. Thanks are also due to
Dr. Usha Ranganathan and Dr. Lakshmi Madhavi for their help in the preparation of the
manuscript.
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... As a result of increasing studies on the toxicity of hydroquinone and its metabolites, the European Union Scientific Committee on Consumer Safety (SCCS) banned the use of hydroquinone in cosmetic products as of January 1, 2001 (Draelos 2007). The ban on hydroquinone has led cosmetic researchers to study different non-cytotoxic and non-mutagenic active ingredients that suppress melanin synthesis by interfering with the melanogenesis process (Baurin et al. 2002;Batubara et al. 2010;Kamakshi 2012;Almeda et al. 2015;Mann et al. 2018). ...
... In addition to these products, natural melanogenesis inhibitors have recently been investigated. It was demonstrated that non-cytotoxic and non-mutagenic plant extracts may be as potent as synthetic whitening agents (Baurin et al. 2002;Batubara et al. 2010;Kamakshi 2012;Almeda et al. 2015). The most important of these is licorice root (Glycyrrhiza glabra), which contains isoflavonoids and chalcone as active ingredients (Nerya et al. 2003;Kao et al. 2014). ...
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This study investigated the effect of some herbal extracts, such as licorice root, white mulberry leaf, green tea leaf, and grape seed, with a combination of bacterial nanocellulose and some bioactive materials, such as ascorbic acid, niacinamide, hexylresorcinol, and alpha-arbutin, on treatment of hyperpigmentation. The effect of the prepared emulsions on hyperpigmentation was revealed by analyzing their tyrosinase inhibition properties, their ability to stop melanin production, or their properties of whitening the brown spot on the skin. In addition to the physicochemical properties of the 5 different emulsions obtained, tyrosinase, collagenase, and elastase enzyme activities, antioxidant properties, cytotoxicity, and microbiological analyzes were performed by cell-culture modelling. Finally, a dermocosmetic facial serum was designed that is compatible with skin pH, is homogeneously mixed, has good spreading properties, does not cause any microbiological growth, does not inhibit elastase activity while stimulating collagenase activity, reduces melanin production by inhibiting the tyrosinase enzyme, and does not have any toxic effects.
... 17 Aside from tyrosinase inhibitors, anti-oxidants and vitamins can directly or indirectly be beneficial as skin lightening ingredients. 18 Antioxidants reduce the oxidation of tyrosine and quench the free radicals 19 , by which the synthesis of melanin will be reduced and skin de-pigmentation effects may occur. 20 Vitamins usually improve the skin texture and tone. ...
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Skin health and complexion improvement have become more prioritized and the need for natural remedies are more in demand than the synthetic options. Research in the area of skin care is growing with regular updation of facts and data. In Ayurveda, skin complexion improvement is comparable to the modern concepts such as tyrosinase inhibition and anti-oxidant activity. In this review, selected Ayurvedic medicinal plants are screened from classical Ayurvedic texts as well as the modern scientific literature to investigate their probable potential for skin health and skin lightening effects. All the plants reviewed are found to act as complexion promoters directly or indirectly by their interference in melanogenesis pathway or through antioxidant potentials. This efficiently confirms the goodness of these plants as potential skin care and whitening agents.
... 12 The chemical-based skin-whitening substances, including hydroquinone and derivatives, phenolic amines, biphenyl, chalcone agents, and mercury compounds, have been used in cosmetic formulations for a long time. 13 But these substances have multiple adverse effects on consumers, 14 and natural melanin inhibitors are attracting masses of people. 15 Although, in recent years, various tyrosinase inhibitor natural compounds (kojic acid, arbutin, azelaic acid, resveratrol, glycolic acid, and epigallocatechin gallate) have been reported that interfere with novel melanin synthesis in melanocytes. ...
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Background: The excessive production and accumulation of melanin in the epidermal skin layer can result in skin hyperpigmentation and darkening. Current technologies for regulating melanin are based on inhibiting melanin biosynthesis. They have low effectiveness and safety issues. Aims: This study aimed to evaluate the potential role of Pediococcus acidilactici PMC48 as a probiotic strain in medicines and cosmetics for skin treatment. Materials and methods: Meanwhile, our research team has reported that P. acidilactici PMC48 strain isolated from sesame leaf kimchi can directly decompose the already synthesized melanin. It can also inhibit melanin biosynthesis. In the present study, we investigated the skin-whitening effect of this strain by arranging an 8-week clinical trial with 22 participants. PMC48 was applied to each participant's artificially UV-induced tanned skin in the clinical trial. Its whitening effect was investigated based on visual evaluation, skin brightness, and melanin index. Results: PMC48 showed a significant effect on the artificially induced pigmented skin. The color intensity of the tanned skin was decreased by 47.647%, and skin brightness was increased by 8.098% after the treatment period. PMC48 also significantly decreased the melanin index by 11.818%, indicating its tyrosinase inhibition capacity. Also, PMC48 improved skin moisture content level by 20.943%. Additionally, 16S rRNA-based amplicon sequencing analysis showed a distinct increase in Lactobacillaceae in the skin by up to 11.2% at the family level without affecting other skin microbiota. Furthermore, it showed no toxicity in in vitro or in vivo analyses. Discussion: These results indicate that P. acidilactici PMC48 is a promising probiotic strain that can be used to develop medicines and cosmetic products to solve skin-related problems. Conclusions: These results demonstrate that P. acidilactici PMC48 can be a potential probiotic for the cosmetic industry against different skin disorders.
... Melanogenesis is suppressed through several mechanisms, including inhibition of reactive oxygen species (ROS) production which triggers melanoma initiation, inhibition of a key transcriptional factor of melanin synthesis, direct suppression of tyrosinase, or induction of pheomelanin synthesis rather than darker eumelanin [2][3][4][5]. Numerous compounds show promising effects through the activation of these mechanisms and are used as skin-lightening agents in the cosmetic industry [6][7][8]. ...
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Glutathione (GSH) is present in almost all human cells and has a beneficial effect on human skin brightness. Cysteinylglycine (Cys-Gly) and γ-glutamylcysteine (γ-Glu-Cys) are GSH synthesis components. In this study, we defined glutathione (GSH), cysteinylglycine (Cys-Gly), and γ-glutamylcysteine (γ-Glu-Cys) as cysteine peptide and performed a randomized, double-blind, placebo-controlled study to investigate the effects of orally administered cysteine peptide on human skin brightness using a CM-26d portable spectrophotometer in healthy males and females aged between 20 and 65 years old. Eligible participants were randomly allocated into three groups (cysteine peptide 45 mg: n = 16, 90 mg: n = 15, and placebo: n = 16). Each subject ingested six tablets every day for 12 weeks, and skin brightness was measured at 0, 4, 8, and 12 weeks. As a result, the 45 mg group exhibited arm brightening in a time-dependent manner, and a significant difference was observed compared to the placebo at week 12 (p = 0.028). Moreover, no serious adverse events and changes related to 270 mg study food were observed in the safety trial. Here, we suggest that cysteine peptide is a promising and safe compound for human skin brightness.
... The skin whitening compound which is widely used for depigmentation is hydroquinone. The compound overcomes hyperpigmentation by inhibiting the tyrosinase enzyme, but it is cytotoxic for melanocyte cells in long-term use [5]. Therefore, it is necessary to explore alternative natural ingredients for skin whitening compounds. ...
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... Dark skin or skin hyperpigmentation is a result of exposure to ultraviolet light or chemical irritants, and also is a manifestation in several skin disorders such as melasma, solar lentigines, or post-inflammatory hyperpigmentation [4]. The use of skin-lightening agents aims to reduce the level of melanin, the main pigment in the skin, resulting in a brighter skin tone [5,6]. ...
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... However, there is a limitation in the clinical efficacy of the currently used tyrosinase inhibitors, as these inhibitors were specifically chosen based on their ability to inhibit mushroom tyrosinase [59]. This is also a widely reported screening method in the literature for skin-lightening ingredients [60]. Tyrosinase is an enzyme responsible for synthesizing melanin through melanogenesis [61]. ...
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... Alpha and beta hydroxyl acids and derivatives Among them botanical extracts mostly contains a combination of two or more classes of compounds that works synergistically to achieve skin lightening. Botanicals connote nature and are hence more acceptable to people (Kmakshi, 2012). ...
Chapter
Denizel kaynaklardan elde edilebilen biyoaktif bileşenlerin, cilt sağlığı için en çok aranan antioksidan, antipigmentasyon, foto-koruyucu, kırışıklık önleyici, nemlendirici gibi etkilere sahip olması kozmetik endüstrisinin denizel kaynaklara olan ilgisini önümüzdeki yıllarda da canlı tutacağını göstermektedir. Bu incelemede, kozmetik/kozmesötik alanında kullanılan belli başlı denizel kaynaklar, elde edilen biyoaktif bileşenlerin keşif ve geliştirilme sürecinde karşılaşılan zorluklar ve bu pazarda başarılı olmuş ürünlerden bahsedilmiştirt.
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Objective To develop and introduce evidence-based guidelines for the treatment of vitiligo in children and in adults. Patients and Setting Patients, residents, and dermatologists from the Department of Dermatology, Academic Medical Center, University of Amsterdam, and the Netherlands Institute for Pigmentary Disorders in Amsterdam. Design Scientific evidence obtained from 3 systematic reviews of the literature was combined with the results of 2 questionnaires and interviews of potential users of the guidelines, 3 internal expert meetings, and 1 local expert meeting, during which preliminary guidelines were presented and commented on. A final version of the guidelines was synthesized and disseminated among potential users. Six months after the introduction of these guidelines, their use was evaluated. Results Before the development of the guidelines, there was no uniformity in treatment selection, and there was a variability in estimates of treatment outcome. The meta-analysis showed class 3 corticosteroids and narrowband UV-B to be the most effective and safest therapies for localized and for generalized vitiligo, respectively. From another systematic review, it could be concluded that patients with segmental, stable, or lip-tip vitiligo could be successfully treated with most autologous transplantation methods. For vitiligo universalis, results of the systematic review showed that depigmentation using monobenzone or a Q-switched ruby laser was equally effective. The final version of the guidelines consisted of a treatment scheme together with detailed treatment protocols. Implementation of the guidelines was evaluated in 5 physicians. After the introduction of these guidelines, they were followed in most adult cases with vitiligo (71% of patients with localized vitiligo, 82% with generalized vitiligo, 100% with stable or segmental vitiligo, and 80% with universal vitiligo). In children with vitiligo, the physicians adhered to the guidelines for 52% of the cases. Conclusions Guidelines for the treatment of vitiligo can be successfully developed and disseminated for daily clinical practice. The results of the implementation of these guidelines should be confirmed in other centers involving more clinicians.
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Complete depigmentation of the normal skin of adult male blacks was procured by the daily application for five to seven weeks of a formula consisting of 0.1% tretinoin, 5.0% hydroquinone, 0.1% dexamethasone, and hydrophilic ointment. Depigmentation was not attainable when any one of the components was omitted.The formula was therapeutically effective in treatment of melasma, ephelides, and postinflammatory hyperpigmentation. Senile lentigines were resistant to this therapy.
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The photoaging index has been developed to determine the level of skin rejuvenation required to reduce the visible signs of aging. Minor photoaging is reversed with free-radical avoidance and peeling with a topical skin care regimen consisting of buffing grains, α-hydroxy acid normalizing tonics and vitamin A conditioning lotions. The reversal of moderate photoaging requires the addition of light-to-moderate peels using α-hydroxy acids combined with microdermabrasion. For the more advanced case the Jessner/trichloroacetic acid (TCA) combination peel (Monheit peel) is used which can be repeated once to twice a year. Laser resurfacing is especially useful to shrink the collagen and produce a ‘face-lift bypass’. The phenol peel remains the standard to reverse heavy lines. A new modified formula (Hetter) is used which contains less phenol and less croton oil. Dermabrasion is helpful for removing multiple actinic keratosis. With this combination of skin care, chemical peels, and dermabrasion it is possible to reverse the photoaging index.
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By bioassay-guided fractionation using mushroom tyrosinase (EC 1.14.18.1), 2-hydroxy-4-methoxybenzaldehyde was characterized as the principal tyrosinase inhibitor from three East African medicinal plants, the root of Mondia whitei (Hook) Skeels (Asclepiaceae), the root of Rhus vulgaris Meikle (Anacardiaceae), and the bark of Sclreocarya caffra Send (Anacardiaceae). It inhibited the oxidation of L-3,4-dihydroxyphenylalanine (L-DOPA) by mushroom tyrosinase with an IDS, of 4.3 mu g/ml (0.03 mM). The inhibition kinetics analyzed by a Lineweaver-Burk plot found this simple benzaldehyde derivative to be a mixed type inhibitor for this oxidation and affects on the enzyme in several ways. Based on finding this potent tyrosinase inhibitor, various related analogues were also tested in order to gain new insights into their inhibitory functions on a molecular basis.