Article

Aloesin inhibits hyperpigmentation induced by UV radiation

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Abstract

Skin hyperpigmentation is caused by the overproduction of melanin pigment, which is synthesized by the action of tyrosinase. We recently reported that aloesin inhibits tyrosinase activity. The present study was undertaken to test the inhibitory effect of aloesin on pigmentation in human skin after UV radiation. Experimental subjects were UV-irradiated (210 mJ) on the inner forearm. UV-irradiated regions were assigned to four groups: vehicle control, aloesin treated, arbutin treated, and aloesin and arbutin treated. Aloesin and/or arbutin were administered four times a day for 15 days. Aloesin treatment suppressed pigmentation by 34%, arbutin by 43.5%, and the cotreatment by 63.3% compared with the control (n = 15; P < 0.05). Moreover, aloesin treatment showed pigmentation suppression in a dose-dependent manner (n = 7; P < 0.05). These results raise the possibility that aloesin may be used as an agent that inhibits melanin formation induced by UV radiation.

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... Aloe vera (Table 1) contains aloesin [183], which produces a skin-lightening effect, inhibits melanogenesis, and decreases tyrosinase and DOPA polymerase actions [156,[183][184][185]. Mucopolysaccharides and the amino acid profile of Aloe vera (e.g., arginine, histidine, threonine, glycine, serine, and alanine) improve water retention in the stratum corneum [186]. Aloe gel has antioxidant properties. ...
... Aloe vera (Table 1) contains aloesin [183], which produces a skin-lightening effect, inhibits melanogenesis, and decreases tyrosinase and DOPA polymerase actions [156,[183][184][185]. Mucopolysaccharides and the amino acid profile of Aloe vera (e.g., arginine, histidine, threonine, glycine, serine, and alanine) improve water retention in the stratum corneum [186]. ...
... Hesperidin (flavanone) and ascorbic acid in lemon (Table 1) can decrease tyrosinase activity and prevent melanin biosynthesis [157,183]. Additionally, citral, D-limonene, and β-pinene have a depigmenting effect. They decrease tyrosinase activity and L-dihydroxyphenylalanine (L-DOPA) oxidation [190]. ...
Article
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Nowadays, much attention is paid to issues such as ecology and sustainability. Many consumers choose "green cosmetics", which are environmentally friendly creams, makeup, and beauty products, hoping that they are not harmful to health and reduce pollution. Moreover, the repeated mini-lock downs during the COVID-19 pandemic have fueled the awareness that body beauty is linked to well-being, both external and internal. As a result, consumer preferences for makeup have declined, while those for skincare products have increased. Nutricosmetics, which combines the benefits derived from food supplementation with the advantages of cosmetic treatments to improve the beauty of our body, respond to the new market demands. Food chemistry and cosmetic chemistry come together to promote both inside and outside well-being. A nutricosmetic optimizes the intake of nutritional microelements to meet the needs of the skin and skin appendages, improving their conditions and delaying aging, thus helping to protect the skin from the aging action of environmental factors. Numerous studies in the literature show a significant correlation between the adequate intake of these supplements, improved skin quality (both aesthetic and histological), and the acceleration of wound-healing. This review revised the main foods and bioactive molecules used in nutricosmetic formulations, their cosmetic effects, and the analytical techniques that allow the dosage of the active ingredients in the food.
... Alternatively, the use of the combination would allow for higher doses of benzoyl peroxide to be used, thereby increasing the efficacy of the treatment. Another study reported that topical application of aloesin (a major component of A. ferox leaves) significantly inhibits hyperpigmentation of human skin following UV radiation damage (Choi et al., 2002). Furthermore, the same study also demonstrated that combinations of either aloesin or Aloe extract (containing >40% aloesin) with arbutin had additive effects, with arbutin potentiating the protective effects of aloesin. ...
... Wistar rats Aqueous A. ferox leaf extract (400 mg/kg) 57À88% pain reduction (Mwale and Masika, 2015) Inflammatory sports injuries (e.g., sprains and inflamed joints) (Gruber, 1986) Hyperpigmentation and skin damage Human Topical application of aloesin isolated from A. ferox leaves Inhibits hyperpigmentation of human skin following UV radiation damage (Choi et al., 2002) ARTICLE [m5G;December 12, 2021;8:29] HAD safety levels be established and enforced, and that decolourised aloe products not be subject to the EFSA's bans. The European Commission, however, based on EFSA's opinion, moved forward with proposing a ban of HAD as food-and hence food-supplement ingredients, which is set to come into force in 2021 (European Commission, 2020). ...
Article
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Aloe and Aloe products have at a long history of use dating back to antiquity. Use and trade were originally dominated by Barbados or Cura¸cao (A. vera), and Socotra aloe (A. perryi). Commercialization of Cape Aloe was initiated by the Dutch East India Company (VOC), likely to add to their existing aloe trade, and Cape Aloe was brought back to Europe as early as 1761. Albeit aloes’ early official history was marred by taxonomic confusion, Cape Aloe made its way into the world’s pharmacopoeias as early as the late 18th century and its popularity has held steady into the 20th century. While it is still an ingredient in established phytomedicines with standard monographs and multiple of products in the marketplace, it has lately become the subject of a safety concern, along with other anthraquinone-yielding plant species, and its ban for use in food products by the European Commission is imminent. In the following study we review the history of Cape Aloe products establishing themselves in world markets, alongside the milestones of pre-clinical and clinical research into the safety and efficacy of these products.
... [15,16] While retinoids and azelaic acid work effectively both on active acne and PIH, hydroquinone, kojic acid, niacinamide, Vitamin C, and liquorice extract are promising agents on PIH. Other newer agents such as rucinol, pycnogenol, ellagic acid, [17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33] and silymarin are usually used in combination with other depigmenting agents [ Figure 4]. [34] ...
... Erythema, burning, pruritus, dryness Aloesin [33] Competitively inhibits tyrosine hydroxylase and DOPA-oxidase ...
Article
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Post-inflammatory hyperpigmentation (PIH) is a reactive hypermelanosis, profoundly common in the Asian skin. The post-acne sequelae may have profound effects on the patients’ mental status, sometimes even more than the acne itself, as they are long lasting and sometimes treatment refractory. PIH occurs secondary to release of inflammatory mediators such as prostaglandins and interleukins in acne which stimulate melanogenesis. There are a multitude of therapeutic modalities available for the treatment of PIH associated with acne. Treating acne and PIH simultaneously would be a logical approach. Epidermal PIH usually responds to topical skin lightening agents which are the first line in these cases. Patients refractory to topical and oral treatment modalities usually have dermal PIH and may be offered interventional therapies. These therapies can be utilized simultaneously along with conventional therapies to hasten up the results, as combination treatment works synergistically by multipronged action at different pathways of etiopathogenesis. The patients with dermal PIH refractory to standard treatment may require other adjunctive therapies such as chemical peels, PRP, and lasers. This review provides an insight into rational and holistic approach to the management of the underlying acne, early customized treatment along with correction of underlying nutritional deficiencies, and lifestyle modifications in effective treatment of PIH.
... Choi et al. evaluated the depigmenting efficacy of aloesin and arbutin in a human study [117]. After irradiating the skin area of the forearm with UVR, a 10% solution of each substance was treated alone or together 4 times daily for 15 days. ...
... Substances and therapies that can synergize with arbutin are attracting attention [117,120,122]. Rather than using arbutin alone, a strategy for maximizing the skin lightening efficacy by combining it with other active ingredients with different mechanisms of action is preferred [124][125][126]. ...
Article
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Arbutin is a compound of hydroquinone and D-glucose, and it has been over 30 years since there have been serious studies on the skin lightening action of this substance. In the meantime, there have been debates and validation studies about the mechanism of action of this substance as well as its skin lightening efficacy and safety. Several analogs or derivatives of arbutin have been developed and studied for their melanin synthesis inhibitory action. Formulations have been developed to improve the stability, transdermal delivery, and release of arbutin, and device usage to promote skin absorption has been developed. Substances that inhibit melanin synthesis synergistically with arbutin have been explored. The skin lightening efficacy of arbutin alone or in combination with other active ingredients has been clinically evaluated. Combined therapy with arbutin and laser could give enhanced depigmenting efficacy. The use of arbutin causes dermatitis rarely, and caution is recommended for the use of arbutin-containing products, especially from the viewpoint that hydroquinone may be generated during product use. Studies on the antioxidant properties of arbutin are emerging, and these antioxidant properties are proposed to contribute to the skin depigmenting action of arbutin. It is hoped that this review will help to understand the pros and cons of arbutin as a cosmetic ingredient, and will lead to future research directions for developing advanced skin lightening and protecting cosmetic products.
... A number of these drugs have been studied in human trials on melasma, solar lentigines or UV induced hyperpigmentation with encouraging results as elucidated in Table 9. [39,[49][50][51][52][53][54][55][56][57][58][59][60][61][62][63][64][65] Others such as cinnamic acid, green tea extracts, flavonoids, gentistic acid, pyronic acrylic acid inhibitors, zinc dihydrolipoylhistidinate and resveratrol are in the process of development and preclinical studies. The knowledge of the properties of these agents enables the dermatologist to choose a product that gives the best benefit to their patients while minimizing the side effects Although experimental evidence suggests their possible benefits, rigorous controlled trials are mostly lacking for these agents. ...
Article
Melasma is one of the most common hyperpigmentary disorders found mainly in women and dark-skinned patients. Sunlight, hormones, pregnancy, and genetics remain the most implicated in the causation of melasma. Although rather recalcitrant to treatment, topical agents such as hydroquinone, modified Kligman's Regime, azelaic acid, kojic acid, Vitamin C, and arbutin still remain the mainstay of therapy with sun protection being a cornerstone of therapy. There are several new botanical and non botanical agents and upcoming oral therapies for the future. There is a lack of therapeutic guidelines, more so in the Indian setup. The article discusses available evidence and brings forward a suggested treatment algorithm by experts from Pigmentary Disorders Society (PDS) in a collaborative discussion called South Asian Pigmentary Forum (SPF).
... 10 The application of aloesin four times a day for 15 days on the volar aspect of UV-irradiated human forearm showed dose-dependent inhibition of pigmentation. 12 A combination of aloesin and arbutin synergistically inhibit melanin synthesis by the combined action of non-competitive and competitive tyrosinase inhibition. 13 TRP1, tyrosinase-related protein 1; MITF, micropthalmia associated transcription factor ...
Chapter
Melasma is a common, acquired, symmetrical hypermelanosis, which is often difficult to treat and has a significant negative impact on patients’ quality of life. The most commonly implicated etiological factors include genetic predisposition, ultraviolet radiation (UVR) and hormonal influence. Melasma has been classically described as a linear model and classified on the basis of the presence of localization of melanosomes in the skin as epidermal, dermal, and mixed. However, with the use of newer modalities such as in vivo reflectance confocal microscopy, it has been discovered that the distribution of melanophages is heterogeneous and perhaps, suggests that all melasma is in fact ‘mixed’. Further, changes such as increased solar elastosis and vascular proliferation suggest a significant involvement of the dermis in melasma. Melasma is now being learned as a complex interplay amongst the epidermal melanocytes, keratinocytes, dermal fibroblasts, mast cells, and vascular endothelial cells. The elaboration of this new concept has unlocked several other potential targets for research and treatment in the field of melasma.
... As shown in Figure 3, tyrosinase plays a crucial role in catalyzing the hydroxylation of Ltyrosine to L-3,4-dihydroxyphenylalanine (L-DOPA) and followed by the oxidization L-DOPA to L-DOPAquinone. The inhibitory activity of aloesin was proven by a study conducted Choi et al. [24] who reported that the topical treatment of aloesin on the UV-irradiated on the inner forearm resulted in the suppression of skin pigmentation in a dosedependent manner. ...
... Various important enzymes, such as elastase and hyaluronidase that play a key role in the aging process, were also inhibited by 5,7-dihydroxy-methylchromone (Carola et al. 2010). Similarly, aloesin, a glycoprotein found in Aloe ferox, was clinically proven to have an inhibitory effect on pigmentation in human skin following UV radiation (Choi et al. 2002). It was found to suppress skin pigmentation by 34% compared to the normal control. ...
Article
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Chromones are naturally occurring phenolic compounds that are universally present in a healthy human diet. To date, thousands of chromone derivatives, including chromone glycosides have been discovered, both from natural and synthetic origin. Many plant genera, including Aloe, Aquilaria, Cassia, Hypericum and Polygonum, are rich sources of chromones. Several genera of fungi, such as Aspergillus, Mycoleptodiscus, Orbiocrella, and Penicillium produce bioactive chromones. This class of compounds is mainly associated with anti-oxidant, antimicrobial, anticancer and anti-inflammatory activities. Various in vitro, in vivo and clinical studies have established the role of chromones in alleviating allergies, reducing oxidative damage, inhibiting cancer, infections and inflammation, and for treating neurological and psychiatric disorders. This review focuses mainly on natural chromones, and elaborates on their nutritional benefits, pharmacological activities, and mechanisms of action. Various scientific databases, including PubMed, Scopus and Google Scholar, were used to find relevant literature on chromones covering all available literature up to, and including the year 2019. This critical analysis of completed research regarding the nutraceutical properties of various chromone derivatives may provide new insight to scientists working in related fields.
... Further histology showed that areas of skin treated with green tea extract had a reduced num-study showed that the topical application of aloesin following ultraviolet (UV)-irradiation (210 mJ) on the inner forearm provided pigmentation suppression in a dose-dependent manner. 6 Another in vitro study showed that aloesin induced melanin aggregation in isolated tail melanophores of tadpoles, B. melanostictus, which lead to lightening of the skin. 7 More recently, aloe vera was tested in a double-blinded randomized clinical trial aimed at determining the clinical efficacy of a topical liposome-encapsulated aloe vera in the treatment of melasma in pregnant women. ...
Article
Recent years have seen a growth in the Asian cosmeceutical industry and an expanding worldwide marketplace with increasing consumer use of plant-based skin care products. The rising prevalence of Asian cosmeceuticals has led to research studies assessing the safety and efficacy of these products. We seek to review current evidence on safety and efficacy of key ingredients used in Asian cosmeceuticals to treat disorders of hyperpigmentation. A comprehensive search on PubMed was conducted to identify hyperpigmentation-related research studies on eight popular ingredients used in Asian cosmeceuticals: green tea, soy, orchid, licorice, rice water, ginseng, bamboo, and aloe. Both in vitro studies and clinical trials involving human subjects were included. Of the ingredients reviewed, soy and licorice had the most clinical evidence supporting their efficacy, while all other ingredients were supported by in vitro studies. More research is needed to further evaluate the safety and efficacy of Asian cosmeceutical ingredients in treatment of hyperpigmentation.
... Furthermore, a separate experiment was performed by Choi and colleagues on UV radiated human skin. This work revealed that aloesin and arbutin can also be useful as combination therapy for UV mediated hyper-pigmentation (Choi et al., 2002). Later in 2002, aloesin was identified as a competitive inhibitor with respect to human tyrosinase (ex-vivo). ...
Article
Tyrosinase is a key regulatory multifunctional enzyme containing copper that is responsible for the biosynthesis of melanin that determines the color of the skin. Accumulation of excessive melanin causes various dermatological disorders including melasma and age spots. Also, tyrosinase is responsible for enzymatic browning reactions in damaged fruits and vegetables. It deteriorates the color clarity of plant-derived food product which results in loss of nutritional quality. The study of Tyrosinase inhibition is an active field of research in dermatological, biomedical, food and agricultural science and also has potential impact in the domain of insect physiology. Despite several developments on tyrosinase inhibitors, their safety concern still requires investigations due to their undesirable side-effects. Research in this context is being carried out to find potent and safe leads as tyrosinase inhibitors from medicinal plants. This review provides comprehensive overviews of various tyrosinase inhibitors obtained from medicinal plants with their mechanism of action. Several medicinal plants as tyrosinase inhibitors have been extensively studied and successfully marketed. The polyphenol and stilbenes group of phyto-molecules have been established as effective tyrosinase inhibitors. Few of these molecules however have been clinically investigated in the context of potential anti-melanogenic medicinal plants. Tyrosinase inhibitors are commercially available for cosmetic purposes to lighten the complexion. Clinically, they are also used in the treatment of hyper-pigmentary disorders. They are equally applicable for the anti-browning agents in the food-processing industry. This review will be useful for the development and evaluation of tyrosinase inhibitors from medicinal plants.
... In an in vitro study conducted by Jones et al. (77), aloesin proved to have the ability of inhibiting melanin production from mushroom and murine sources. Choi et al. (78) investigated aloesin pigmentary inhibition effects on UV-induced pigmentation on human skin. The study involved topical application of aloesin on the human forearm that has been exposed to UV radiation four times daily for 15 days. ...
Article
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A blemish free, even-toned skin is universally associated with healthy skin. This reasoning makes people desire to have a flawless skin. Melanin is a naturally occurring pigment in humans. This pigment is responsible for skin, hair, and eye color, therefore determines our race and phenotypic appearance. On darker skin types, it is common that melanin production processes malfunctions. These malfunctions often lead to overproduction and secretion of melanin. As a result, unwanted pigmentary problems such melasma occur. Due to unknown etiology and its recurrence in nature, melasma is challenging to treat. The current available melasma treatment options often produce undesired side effects and suboptimum results. First-line topical treatments usually involve hydroquinone or topical steroids. Apart from the irritant reactions, this treatment mode is not suitable for all skin types. Skin care specialists are in search of an effective long-term cosmetics and cosmeceuticals to address hypermelanosis problems. Understanding of naturally occurring depigmenting agents provides an opportunity for more effective ways to manage melasma in all skin types. This review considers the benefits of naturally occurring ingredients which could help address skin pigmentation problems and broaden the choice for skin-lightening treatments.
... It is mainly used as skin whitening agents. Kaempferol, its 3-o glycoside derivative and flavonols (quercetin 3-o-glycoside) are isolated from the fresh flowers of crocus sativus and tyrosinase inhibitory activity is investigated in mushroom 18 . Inhibition of Diphenolase is due to crocin obtained from stigmas of Crocus sativus, but studies showed that the affinity specifically to mushroom tyrosinase was less 19 . ...
Article
Full-text available
Tyrosinase (polyphenolic oxidase) is a multifunctional and copper containing enzyme. Tyrosinase is an enzyme which is responsible for melanin biosynthesis which is responsible for color of the skin. Melanin is synthesised in melanocyte cells by melanogenesis process. Melanogenesis protects skin surface from harmful ultraviolet radiations. Melanin is mainly synthesized in plants, micro organisms and mammalian cells. Melanin pigment is responsible for hyperpigmentation and hypopigmentation. When melanin is present in very less amount it causes local vitiligo and posttraumatic hypopigmentation. When melanin is present in very less amount it causes local vitiligo and posttraumatic hypopigmentation. Abnormal amount of melanin deposit in the specific sites of skin causes abnormal skin colored patches like solar lentigos, chloasma, freckles, post inflammatory hyperpigmentation etc. Tyrosinase is also responsible for color changes in fruits due to enzymatic reactions. Tyrosinase inhibitor compounds are used in cosmetics, food, agriculture science and also used in remedy for imbalance in pigmentations. Some Indian herbal plants and agents like Aloe barbedensis, Crocus sativus, Curcuma longa, Camellia sinensis, Glycyrrhiza glabra, Glycine max, Nelumbo nucifera, Hemidesmus indicus, Vitis Vinifera, Broussonetia papyrifera, resorcinol, arbutin, kojic acid, hydroquinone and ascorbic acid have antityrosinase enzymatic activity. So these plants and inhibitory agents are used in cosmetic industries due to their tyrosinase inhibitory effects or antityrosinase activity or antihyperpigmentation effects. Keywords: Anti-hyperpimentation, Tyrosinase Inhibitor, Melanin, Herbal drugs.
... This study also supported the synergism between arbutin and aloesin as cotreatment resulted in greater pigmentation suppression than either ingredient alone. 7 These promising results should pave the way for further clinical studies. ...
Article
BACKGROUND: Hyperpigmentation disorders are commonly encountered in dermatology clinics. Botanical and natural ingredients have gained popularity as alternative depigmenting products.OBJECTIVE:We sought to review clinical studies evaluating the use of different natural products in treating hyperpigmentation so clinicians are better equipped to educate their patients. Specific ingredients reviewed include azelaic acid, aloesin, mulberry, licorice extracts, lignin peroxidase, kojic acid, niacinamide, ellagic acid, arbutin, green tea, turmeric, soy, and ascorbic acid.METHODS:Systematic searches of PubMed and SCOPUS databases were performed in March 2016 using the various ingredient names, "melasma"and "hyperpigmentation." Two reviewers independently screened titles, leading to the selection of 30 clinical studies.RESULTS:Review of the literature revealed few clinical trials that evaluated the treatment of hyperpigmentation with natural ingredients. Despite the limited evidence-based research, several natural ingredients did show efficacy as depigmenting agents, including azelaic acid, soy, lignin peroxidase, ascorbic acid iontophoresis, arbutin, ellagic acid, licorice extracts, niacinamide, and mulberry.CONCLUSION:The aforementioned ingredients show promise as natural treatments for patients with hyperpigmentation disorders. These agents might also provide clinicians and researchers with a way to further characterize the pathogenesis of dyschromia. However, the paucity of clinical studies is certainly a limitation. Additionally, many of thein-vivostudies are limited by the short length of the trials, and questions remain about the long-term efficacy and safety of the ingredients used in these studies. Lastly, we suggest a standardized objective scoring system be implemented in any further comparative studies.
... The types and content of phenolic compounds in four aloe species are different, the concentration of the chromone and hyperpigmentation (Choi et al. 2002). Aloesin is more abundant in A. barbadensis and A. ferox than A. chinensis and A. arborescens. ...
Article
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Aloe barbadensis, A. vera var. chinensis, A. ferox and A. arborescens are the most widely cultivated and used aloe species due to their potential and potent bioactivity. In this study, clot lysis and fibrin plate model were used to assess the in vitro thrombolytic and fibrinolysis activity of protein and phenolic extracts, as well as three pure compounds (aloin A, Aloin B and aloe emodin) from aloe. Meanwhile, the phenolic compounds in aloe were analyzed by high-performance liquid chromatography (HPLC) and LC–mass spectrometry (LC–MS). The in vitro thrombolytic and fibrinolytic activity assay results indicated that the protein and phenolic extracts of four aloe species had good clot lysis, fibrinolytic activity and enzyme activity, and aloin A and aloin B may be the main active ingredients. In addition, the chromatographic analysis shows obviously differences in components, such as aloenin A, isoaloeresin D and aloesin.
... The study included 15 male Korean volunteers (23-27 years old), treated four times a day, for 15 days. The pigmentation was decreased in a dose-dependent manner [76]. ...
Article
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The skin is the largest organ and functions as a barrier to protect the underlying tissues against the elements and pathogens, while also fulfilling many physiological roles and biochemical functions such as preventing excessive water loss. Skin disorders vary greatly in terms of origin, severity, symptoms and affect persons of all ages. Many plants have been used for medicinal purposes since ancient times including the treatment of skin disorders and diseases. Aloe represents one of the earliest medicinal plant species mentioned in antique scriptures and even in rock art dating back thousands of years. Different Aloe species and materials have been used in the prevention and treatment of skin related disorders. Aloe vera is the most commonly used Aloe species for medicinal purposes. Some of the most prominent skin related applications and disorders that Aloe materials have been investigated for are discussed in this paper, which include cosmetic, radiation, cancer, wound and antimicrobial applications. Both in vitro and in vivo studies are included in the discussions of this paper and comprehensive summaries of all these studies are given in tables in each section. Although some contradictory results were obtained betweenamong studies, certain Aloe materials have shown excellent efficacy and exhibited potential for the treatment of skin related disorders and cosmetic applications.
... It works by inhibiting L-DOPA oxidation and has shown better affinity than kojic acid, arbutin etc. However, it has poor stratum corneum penetration due to its hydrophilicity and high molecular weight, suggesting the need for novel delivery systems to be more effective (Choi et al., 2002). ...
Article
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Hyperpigmentation of the skin refers to a dermatological condition which alters the color of the skin, making it discoloured or darkened. The treatments for hyperpigmentation disorders often take very long to show results and have poor patient compliance. The first‐line treatment for hyperpigmentation involves topical formulations of conventional agents such as hydroquinone, kojic acid, glycolic acid followed by oral formulations of therapeutic agents like tranexamic acid, melatonin, cysteamine hydrochloride. The second‐line approaches include chemical peels and laser therapy given under the observation of expert professionals. However, these therapies pose certain limitations and adverse effects like erythema, skin peeling and drying and require long treatment duration to show visible effects. These shortcomings of the conventional treatments provided scope for further research on newer alternatives for managing hyperpigmentation. Some of these therapies include novel formulations like solid lipid nanocarriers, liposomes, phytochemicals, platelet‐rich plasma, microneedling. This review focuses on elaborating on several hyperpigmentation disorders and their mechanisms, the current, novel and emerging treatment options for management of hyperpigmentation.
... In the skin, they are transferred from melanocytes to neighboring keratinocytes in order to form perinuclear melanin caps [6]. The processing of melanin is catalyzed by the action of tyrosinase [7,8]. Sunscreens represent a practical approach to photoprotection for skin [9]. ...
... Aloesin in combination with arbutin inhibited UV-induced melanogenesis (Choi S et al, 2002). ...
Article
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It is a review article on vitiligo
... In an in vivo study on UV-induced pigmentation in human skin, Choi et al. have investigated anti-tyrosinase activity of aloesin (an anti-inflammatory) alone and combined with arbutin. They showed that combined therapy could be considerably effective (63.3% suppression of pigmentation) in treating hyperpigmentation disorders by synergistic inhibition mechanism of tyrosinase compared to therapy of aloesin (34%) and arbutin (43.5%) alone (Choi, Park, Lee, Kim, & Chung, 2002). Also, in another study, it is revealed that co-therapy with arbutin can suppress UV-induced nuclear factor-kappa B activation in human keratinocytes (Ahn, Moon, Lee, & Kim, 2003). ...
Article
Cosmetic dermatology preparations such as bleaching agents are ingredients with skin‐related biological activities for increasing and improving skin beauty. The possibility of controlling skin hyperpigmentation disorders is one of the most important research goals in cosmetic preparations. Recently, cosmetics containing herbal and botanical ingredients have attracted many interests for consumers of cosmetic products because these preparations are found safer than other preparations with synthetic components. However, high‐quality trial studies in larger samples are needed to confirm safety and clinical efficacy of phytotherapeutic agents with high therapeutic index. Arbutin (p‐hydroxyphenyl‐β‐d‐glucopyranoside) is a bioactive hydrophilic polyphenol with two isomers including alpha‐arbutin (4‐hydroxyphenyl‐α‐glucopyranoside) and β‐arbutin (4‐hydroxyphenyl‐β‐glucopyranoside). It is used as a medicinal plant in phytopharmacy. Studies have shown that alpha‐arbutin is 10 times more effective than natural arbutin. A comparison of IC50 values showed that α‐arbutin (with concentration 2.0 mM) has a more potent inhibitory activity on human tyrosinase against natural arbutin (with higher concentration than 30 mM). A review of recent studies showed that arbutin could be beneficial in treatment of various diseases such as hyperpigmentation disorders, types of cancers, central nervous system disorders, osteoporosis, diabetes, etc. This study was designed to describe the therapeutic efficiencies of arbutin.
... Laxative effect (Celestino et al., 2013;Izzo et al., 1999), antidiarrhoea effect with no toxic effects in loperamide-induced constipated rats (Wintola and Afolayan, 2011), skin and wound healing properties; the leaf exudate accelerated wound closure in animal model and selectively inhibited microbial growth with no dermal toxicity (Jia et al., 2008), inhibited hyperpigmentation of human skin after exposure to UV radiation in a dose dependent manner (Choi et al., 2002), antioxidant activity (Frum and Viljoen, 2006); antiinflammatory activity (Lindsey et al., 2002;Speranza et al., 2005), antimicrobial activity (Afolayan et al., 2002;Kambizi et al., 2005), anticancer activity of emodin against the activation of Epstein-Barr (Koyama et al., 2001), permeation enhancing activity of emodin (Kai et al., 2002), antihelmintic activity against eggs and larvae of Haemonchus contortus at 20 mg/ml and 2.5 mg/ml respectively (Maphosa et al., 2010), antimalarial activity against Plasmodium falciparum at concentrations of 32-77 µg/ml and potential anti-plasmodial activity (IC 50 = 8 µg/ml) (Clarkson et al., 2004), analgesic activity (Mwale and Masika, 2010). The ethanol root extract showed significant toxicity on brine shrimp (LD 50 < 1.0 mg/ml) (Abosede et al., 2015). ...
Article
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Introduction There is widespread use of Aloe species in traditional healing practices in East Africa for a variety of diseases. Unfortunately, there is a tendency of mistakenly referring to all species of the genus Aloe as Aloe vera, despite the diversity of aloes in the region. The names for the different Aloe species in local languages are usually the same for the different species. Aim The aim of this review was to assess the medicinal uses of the indigenous little-known and other popular Aloe species in East Africa. Methods Relevant articles, books, theses, dissertations, patents, and other English-only reports on the ethnobotany, traditional medicinal uses, pharmacological or biological activity, toxicity, phytochemistry, trade, conservation, etymology, and distribution of aloe species in East Africa (Uganda, Tanzania, Kenya, Rwanda, and Burundi) were reviewed. Databases such as PubMed, Web of Science, Scopus, Science Direct, and search engines such as Google Scholar, were searched between May and September 2020. Scientific names and synonyms of the aloe species were verified and resolved using Plants of the World Online (POWO, http://powo.science.kew.org/). Results Forty-nine of the over 180 Aloe species known in East Africa, are traditionally used for treating various ailments. Most of the Aloe species (85.7%) had direct references to their use in traditional medicine. Thirty-six species (73.5%) had some form of phytochemical analysis performed on them. Most of the Aloe species (67.3%) have never been investigated for any biological activity. The distinctive constituents in aloe leaves are phenolic compounds including chromone, anthraquinone or anthrone derivatives. Aloe aageodonta, A. ballyi, and A. christianii are known to be poisonous to humans when used in high doses, despite being used in traditional medicine. Aloe elgonica, A. ferox, and A. lateritia are all highly toxic to brine shrimp, whereas A. macrosiphon, A. vera, and A. volkensii cause a wide range of toxic side effects, such as bloody diarrhoea, dehydration, kidney damage, miscarriage, nausea and vomiting, hepatotoxicity, and acute renal failure, when used for long periods and in high doses. Conclusion Several Aloe species are used in East Africa for treating various ailments. However, most of the local Aloe species have not been scientifically investigated for their biological activity, as well as their toxicity.
... It has been shown to be a potent and selective tyrosinase's inhibitor which has direct inhibitory effects on melanogenesis (Jin and Lee, 1999). After UV radiation aloesin may be able to inhibit the hyperpigmentation in a dosedependent manner (Choi et al., 2002). ...
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Tyrosinase is a copper-containing monooxygenase involved in the catalysis of the hydroxylation and oxidation reaction of monophenols and diphenols, respectively, into O-quinones intermediates. Tyrosinase is mainly involved in melanogenesis via two reactions. Firstly, 3,4-dihydroxyphenylalanine is produced through tyrosine hydroxylation then it oxidized into dopaquinone, and finally gives melanin. However, dopaquinones can results in neuronal damage and cell death through the excessive production, suggesting that tyrosinase may be implanted in the formation human brain's neuromelanin and association with Parkinson's diseases. Thus, down regulating the melanin pigments and its intermediates by inhibiting tyrosinase activity is the major pharmaceutical challenge to prevent hyperpigmentation, in addition to therapy of neuromelanin disorders. Thus, this review has been focused on exploring the biochemical and molecular properties of tyrosinase from different sources and its potential inhibition with different natural and synthetic compounds.
... Various bioactive compounds isolated from aloe such as barbaloin, aloesin, aglycone of aloenin, 2 "-O-feruloylaloesin, isoaloeresin D and aloeresin E have shown effective inhibition of tyrosinase[20][21]. However, aloesin appeared to be more effective towards crude murine tyrosinase than mushroom tyrosinase and has been used in topically applied cosmetics due to its multifunctional skin care activity[22][23]. The biological activity of aloe gel was found to vary with the genotypes of aloe[18][19]. ...
... Several biological activities have been reported for various chromone glycosides. For example, aloesin and its analogues, from Aloe, are used in cosmetic preparations to treat hyperpigmentation induced by UV radiation, owing to their role in inhibition of tyrosinase enzyme [2,3]. Additionally, 8-[C-β-D-[2-O-(E)cinnamoyl]glucopyranosyl]-2-[(R)-2-hydroxypropyl]-7-methoxy-5-methylchromone), isolated from certain Aloe species, was reported to have potent topical anti-inflammatory activity comparable to the effect of hydrocortisone without affecting thymus weight [3]. ...
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Chromone glycosides comprise an important group of secondary metabolites. They are widely distributed in plants and, to a lesser extent, in fungi and bacteria. Significant biological activities, including antiviral, anti-inflammatory, antitumor, antimicrobial, etc., have been discovered for chromone glycosides, suggesting their potential as drug leads. This review compiles 192 naturally occurring chromone glycosides along with their sources, classification, biological activities, and spectroscopic features. Detailed biosynthetic pathways and chemotaxonomic studies are also described. Extensive spectroscopic features for this class of compounds have been thoroughly discussed, and detailed 13C-NMR data of compounds 1–192, have been added, except for those that have no reported 13C-NMR data.
... Recently, aloesin was reported to promote wound healing via several processes, including cell migration, tissue development, angiogenesis and cytokine release (Wahedi et al., 2017). Moreover, aloesin treatment showed pigmentation suppression via its inhibitory effect on tyrosinase activity after UV radiation (Choi et al., 2002). The depigmenting effects of this compound tend to be dose-dependent (Wang et al., 2008). ...
Article
Ethnopharmacological relevance Skin diseases are among the most common human health affections. A healthy skin promotes a healthy body that can be achieved through modern, allopathic and natural medicines. Therefore, medicinal plants can be a reliable therapy in treating skin diseases in humans through a diverse range of bioactive molecules they contain. Aim of the study This review aims to provide for the first-time scientific evidence related to the dermatological properties of Morocco's medicinal plants and it aims to provide a baseline for the discovery of new drugs having activities against skin issues. Methods This review involved an investigation with different search engines for Moroccan ethnobotanical surveys published between 1991 and 2021. The plants used to treat skin diseases have been determined. Information regarding pharmacological effects, phytochemical, and clinical trials related to the plants listed in this review was collected from different scientific databases like PubMed, Science Direct, Google Scholar, Web of Science and Scopus. The data were analyzed and summarized in the review. Results A total of 401 plants belonging to 86 families mainly represented by Asteraceae, Lamiaceae, Fabaceae, and Apiaceae which have been documented to be in common use by Moroccans for managing skin diseases. Among those plants recorded, the most commonly used are Allium cepa L, Chamaeleon gummifer (L.) Cass and Salvia rosmarinus Schleid. Mill. Leaves were the most commonly used plant part, while powder and decoction were the most common method of traditional drug preparation. 107 of the 401 plants (27%) have undergone pharmacological validation. A total of 44 compounds isolated from 27 plants were investigated to treat different types of skin diseases, and 25 plants have been clinically studied for their activities against skin diseases. Conclusion The beneficial effects of using Moroccan medicinal plants to treat skin diseases, according to traditional practices, have been proven in numerous scientific studies. Therefore, other studies should focus on isolating and identifying specific bioactive compounds from plant extracts, revealing more valuable therapeutic properties. Furthermore, additional reliable clinical trials are needed to confirm their beneficial effect on patients with skin diseases.
... Particularly, aloesin is an aromatic C-glucosylated 5-methylchromone found in Aloe vera that is known to possess anti-oxidant activity ( Loots du et al., 2007 ). In addition, it has been reported to mediate skin whitening through a reduction in melanin synthesis by inhibiting tynosinase activity, especially in UVB-irradiated skin ( Choi et al., 2002 ). It has been shown to lower blood glucose in a diabetic mouse model ( Yimam et al., 2014 ). ...
Article
Background: Cutaneous wound healing is a complex process involving various regulatory factors at the molecular level. Aloe vera is widely used for cell rejuvenation, wound healing, and skin moisturizing. Hypothesis/purpose: This study aimed to investigate the effects of aloesin from Aloe vera on cutaneous wound healing and mechanisms involved therein. Study design: This study consisted of both in vitro and in vivo experiments involving skin cell lines and mouse model to demonstrate the wound healing effects of aloesin by taking into account several parameters ranging from cultured cell migration to wound healing in mice. Methods: The activities of Smad signaling molecules (Smad2 and Smad3), MAPKs (ERK and JNK), and migration-related proteins (Cdc42, Rac1, and α-Pak) were assessed after aloesin treatment in cultured cells (1, 5 and 10µM) and mouse skin (0.1% and 0.5%). We also monitored macrophage recruitment, secretion of cytokines and growth factors, tissue development, and angiogenesis after aloesin treatment using IHC analysis and ELISAs. Results: Aloesin increased cell migration via phosphorylation of Cdc42 and Rac1. Aloesin positively regulated the release of cytokines and growth factors (IL-1β, IL-6, TGF-β1 and TNF-α) from macrophages (RAW264.7) and enhanced angiogenesis in endothelial cells (HUVECs). Aloesin treatment accelerated wound closure rates in hairless mice by inducing angiogenesis, collagen deposition and granulation tissue formation. More importantly, aloesin treatment resulted in the activation of Smad and MAPK signaling proteins that are key players in cell migration, angiogenesis and tissue development. Conclusion: Aloesin ameliorates each phase of the wound healing process including inflammation, proliferation and remodeling through MAPK/Rho and Smad signaling pathways. These findings indicate that aloesin has the therapeutic potential for treating cutaneous wounds.
... Aleosin as skin-lightening agent is isolated from Aloe vera plant. Choi et al., (2002) revealed that aloesin shows tyrosinase inhibitory activity in human skin after UV radiation. ...
Article
Melanin is the pigment in the human and animal skin that is synthesized by tyrosinase from L-tyrosine to L-DOPA, following the oxidation of L-DOPA to L-DOPA quinone. Skin whitening agents have been desired as treatment of skin diseases caused by the excess accumulation of melanin on the human skin, because skin darkening is one of the serious aesthetic problems in human beings. Inhibiting the tyrosinase activity and the protein expression are the target to develop the skin whitening agent. A large number of active compounds have been isolated and identified from natural product to develop whitening agents so far. This review reports the potential of traditional medicinal plant extractives and the effective novel ingredients as anti-melanogenesis.
Chapter
A cosmetic is a formulation containing substances of natural or artificial origin intended to boost the appearance of any part of the body for which it is designed to gain the esthetic appeal to the members of the audience. Such products are meant for use on the face to supplement one’s appearance and are often designated as makeup. Several undesirable effects are concomitant to synthetically based cosmetics owing to their content of harmful synthetic ingredients. Attention has then been shifted toward herbal bioactive-based cosmetics containing phytoconstituents possessing antioxidant and free-radical scavenging actions exploited to control skin disorders like dry skin, eczema, ageing, inflammations, etc., and in aromatherapy. Cosmetics appear as solids, semisolids, or liquids and in a broad sense, could be formulated as solutions, creams/emulsions, lotions, suspensions, ointments, pastes, powders, gels, sticks, pencils, tablets, capsules, or aerosols. They can be itemized according to the part of the body they are meant to be used at, such as products for the skin, hair, nails, teeth, and eye or on the basis of their function as emollients, cleansing, decorative, deodorant/antiperspirants, and protective preparations. Herbal bioactive ingredients suitable for preparing cosmetics could be extracted from various parts of organic materials, especially plants that are in abundance. With innovations in research and development and technology, these phytoconstituents are standardized and their novel products are patentable. The future and market for herbal bioactive-based cosmetics are high.
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Background Pigment melanin has primarily a photo defensive role in human skin, its unnecessary production and irregular distribution can cause uneven skin tone ultimately results in hyper pigmentation. Melanin biosynthesis is initiated by tyrosine oxidation through tyrosinase, the key enzyme for melanogenesis. Not only in humans, tyrosinase is also widely distributed in plants and liable for browning of vegetables and fruits. Search for the inhibitors of tyrosinase have been an important target to facilitate development of therapies for the prevention of hyperpigmentary disorders and an undesired browning of vegetables and fruits. Methods Different natural and synthetic chemical compounds have been tested as potential tyrosinase inhibitors, but the mechanism of inhibition is not known, and the quest for information regarding interaction between tyrosinase and its inhibitors is one of the recent areas of research. Computer based methods hence are useful to overcome such issues. Successful utilization of in silico tools like molecular docking simulations make it possible to interpret the tyrosinase and its inhibitor’s intermolecular interactions and helps in identification and development of new and potent tyrosinase inhibitors. Results The present review has pointed out the prominent role of computer aided approaches for the explication of promising tyrosinase inhibitors with a focus on molecular docking approach. Highlighting certain examples of natural compounds whose antityrosinase effects has been evaluated using computational simulations. Conclusion The investigation of new and potent inhibitors of tyrosinase using computational chemistry and bioinformatics will ultimately help millions of peoples to get rid of hyperpigmentary disorders as well as browning of fruits and vegetables.
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Post-inflammatory hyperpigmentation (PIH) is a common dermatosis most often seen in those with skin of color. PIH results when cutaneous inflammation or injury promotes activation of cytokines that induce melanin production and dispersion in the epidermis. Damage to the basement membrane results in pigment incontinence and eventual phagocytosis by melanophages in the upper dermis. The most common causes of PIH include acne, lichen planus, contact dermatitis, mechanical trauma, and skin-directed physical therapy such as dermabrasion, chemical peels, and laser surgery. PIH is a clinical diagnosis with light–dark brown macules or patches at the site of inflammation or trauma. Prevention is critical given the well-documented adverse effects on quality of life as well as the management challenge that it presents. PIH can take months to years to fade away. Diverse treatment modalities have been documented with variable success and include topical preparations, chemical peels, and laser therapy. Currently, the gold-standard treatment for PIH is 4% hydroquinone in combination with photoprotection.
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Magnolia officinalis var. biloba is used as a traditional medicine in China and as a food additive in the United Kingdom and the European Union. In this study, total phenylethanoid glycosides (TPG) and magnoloside Ia (MIa) from M. officinalis var. biloba fruits showed excellent radical scavenging activities and potent inhibition activities against ultraviolet B (UVB)-induced oxidative damage in vitro. In vivo, TPG and MIa inhibited UVB-induced skin phototoxicity in mice upon continuous irradiation for 10 days. Changes in the levels of malondialdehyde, catalase, glutathione peroxidase, superoxide dismutase, and hydroxyproline caused by UVB irradiation were remarkably reversed in a dose-dependent manner after treatment with TPG or MIa. Protein-level analysis further showed that compared with the UVB group, the TPG high-dose group or MIa group significantly down-regulated MAPK/NF-κB signaling pathways. Therefore, TPG and MIa possessed a powerful photoprotective property that can be applied in food and antiphototoxicity formulations.
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Aloesone was synthesized in four steps from 4-acetyl-5-methylresorcinol in overall 59% yield. The key strategy includes the concomitant formation of the chromone ring and deprotection of two protecting groups in one batch to lead aloesone shortly.
Chapter
Disorders of hyperpigmentation commonly afflict the ethnic population. Given current immigration trends, dyschromias are poised to become a condition increasingly encountered by clinicians. Developing a strong understanding of treatment options and associated side effects is essential. This chapter will focus on the treatment hierarchy of the most common acquired disorders of hyperpigmentation (i.e., melasma, post-inflammatory hyperpigmentation): (i) topical hypopigmenting agents, (ii) chemical peels, and (iii) oral agents, microdermabrasion, microneedling, and laser therapy. In addition to discussing the advantages and disadvantages of these therapies, it will provide a brief overview of emerging treatment options.
Chapter
Cosmeceuticals have biologically active ingredients and show beneficial results. However, they may not be US FDA approved. Most cosmeceuticals are made of extracts from marine algae, fruits, herbs, and other botanicals, and these ingredients may be existing already. There are a number of topical antiaging cos‐meceuticals that patients can use depending on their needs. Also known as fruit acids, alpha‐hydroxy acids (AHAs) are a group of chemical compounds that consist of a carboxylic acid substituted with a hydroxyl group on the adjacent carbon. The cosmetic and the pharmaceutical market is flooded with lightening products each claiming to be the best, but with limited clinical evidence to support their claim. Botanicals are active compounds that are isolated from plants. The potential concerns could be the lack of proper testing for efficacy. There are many false claims made, and products are highly priced.
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Background: Cosmeceuticals are commonly used in skincare regimens to maintain healthy skin and improve visible signs of aging. In recent years, South Korean skincare has gained prominence in the global beauty industry by introducing innovative cosmeceutical products and aesthetic trends. Objectives: To describe the global impact of Korean skincare and to review the current research evidence for bioactive ingredients commonly found in Korean cosmeceuticals. Methods: A review of the biomedical literature was conducted using PubMed to identify laboratory, animal, and clinical studies that evaluated the biological properties and potential dermatologic uses of ingredients found in Korean cosmeceuticals. Results: Bioactive ingredients in Korean cosmeceutical products are increasingly undergoing scientific validation and are derived from various sources including animals (eg, bee venom and snail mucin), plants (eg, dragon's blood and tiger grass extract), and biotechnology (eg, synthetic snake venom). Their bioactive components and pharmacologic activities have been shown to provide dermatologic benefits with potential applications for skin rejuvenation, photoprotection, wound healing, and more. Conclusion: Further research studies are warranted to elucidate any biological or therapeutic mechanisms of action of these ingredients, which may translate into clinical practice. With the rising public awareness and interest in Korean cosmeceuticals, patients may seek advice from dermatologists about how to incorporate these bioactive ingredients into their skincare regimens to improve skin health and aesthetics.
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UV radiation (UV) is considered as a complete carcinogen as it is both a mutagen and a non-specific damaging agent. It is the most important risk factor for skin cancer and many other skin disorders like Hyperpigmentation. There is a need of long-term topical skin care treatments (both cosmetic and cosmeceutical) to address problems associated with hyperpigmentation. Synthetic depigmenting agents, such as hydroquinone, mequinol, although highly effective, can raise several safety concerns (for example, ochronosis, cataract, impaired wound healing, desquamation, and other local or systemic side effects) with long-term exposure. The benefits of phytochemicals and natural extracts offer opportunities to develop new formulations to treat pigmentation problems. Cosmeceuticals are topical cosmetic-pharmaceutical preparations containing active ingredients which improve the appearance of skin. Among cosmeceuticals, the phytochemicals have been known to have a multitude of cellular actions for various dermatological diseases. Plant-derived compounds and their effectiveness in the treatment of hyperpigmentation disorders (Melasma) are discussed. Keywords: UV radiation, Hyperpigmentation, Phytochemicals, Cosmeceuticals
Chapter
The terms cosmeceutical and evidence-based may not belong in the same phrase. Cosmeceuticals are considered by many scientists to represent fluff without stuff, and indeed the reader may come to a similar conclusion at the end of this chapter. Nevertheless, it is worthwhile to examine the state of the science for cosmeceuticals as they represent an ever-expanding field in dermatology with perhaps much yet unrealized promise. Cosmeceuticals extend beyond cosmetics to enhance skin functioning, usually aiming to return the skin to a more youthful state. For example, wrinkle-reducing moisturizers, antioxidant serums, and skin-lightening salves all fall into this category. Cosmeceuticals are somewhat confusing, however, as both prescription and over-the-counter (OTC) products have been labeled by this term. Drug cosmeceuticals include topical retinoids for improving dermal collagen production, topical minoxidil for enhanced scalp hair growth, and eflornithine for facial hair growth reduction. These products will not be discussed, as they are not available to the consumer except by prescription. The second category of cosmeceuticals includes OTC drugs, such as sunscreens and antiperspirants. These also are outside the realm of this chapter. The discussion will focus on cosmeceuticals that are topically applied for the purpose of improving skin appearance.
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Kosmeseutikal herbal merupakan kosmetik topikal yang mengandung bahan alami, berasal dari tanaman. Banyak digunakan sebagai Skin Lightening Agent (SLA) dalam penatalaksanaan melasma. Berbagai penelitian telah dilakukan untuk perkembangan kosmeseutikal herbal pada melasma, termasuk penggunaan bahan-bahan alami yang banyak terdapat di Indonesia seperti ekstrak biji mengkudu, ekstrak daun sukun, ekstrak etanol daun pare, ekstrak kulit batang nangka dan gambir. Hasil penelitian tersebut menyatakan bahwa bahan alami dapat digunakan sebagai SLA dalam penatalaksanan melasma melalui berbagai mekanisme interferensi yang mengatur sintesis melanin, mempengaruhi satu atau lebih jalur sintesis melanin. Meskipun beberapa bahan alami tersebut belum diketahui efektivitasnya terhadap pasien melasma, namun dapat dijadikan sebahai bahan penelitian lanjutan sehingga perkembangan kosmeseutikal herbal pada melasma dapat sepenuhnya diketahui.
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Goldstandard für die Behandlung von Pigmentunregelmäßigkeiten der Haut ist nach wie vor Hydrochinon. Aber auch andere Therapien, wie plättchenreiches Plasma, sind in Sicht — deren Wirksamkeit muss sich allerdings in weiteren Studien zeigen.
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Melasma is a common, acquired, symmetrical hypermelanosis. It negatively impacts the patient's quality of life and responds poorly to treatment. Although earlier classified as epidermal and dermal, melasma is now thought to be a complex interaction between epidermal melanocytes, keratinocytes, dermal fibroblasts, mast cells, and vascular endothelial cells. Factors influencing melasma may include inflammation, reactive oxygen species, ultraviolet radiation, genetic factors, and hormones. With a better understanding of the pathogenesis of melasma and the realization that targeting melanin synthesis alone is not very effective, treatments focussing on newly implicated factors have been developed. These include agents targeting hyperactive melanocytes, melanosomal transfer to keratinocytes, defective skin barrier, the mast cells, vasculature, and estrogen receptors as well as drugs with anti-inflammatory and antioxidant activity. Many of these newer agents are botanicals with multimodal mechanisms of action that offer a better safety profile when compared with the conventional drugs. There has also been a focus on oral agents such as tranexamic acid, flutamide, and ascorbic acid. It has been suggested that the "triple therapy of the future" may be a combination of hydroquinone, an antiestrogen and a vascular endothelial growth factor inhibitor, as the "ideal" skin-lightening agent.
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Melasma is a common disorder of hyperpigmentation that affects populations globally and can adversely affect quality of life. Topical therapies—including hydroquinone and nonhydroquinone‐containing formulations—play a central role in the management of melasma. A literature review was conducted using PubMed and Google Scholar. Search keywords included a combination of the following: “melasma,” “chloasma,” and “topical treatment.” We identified and included seminal and high‐quality peer‐reviewed publications, systematic reviews, randomized controlled trials, case series, case reports, consensus statements, and expert opinions. Topical therapies are widely used for the treatment of melasma. Triple combination cream containing hydroquinone, fluocinolone, and tretinoin is the most studied formulation with the strongest evidence among treatment options. Numerous other prescription‐based and nonprescription topical agents, including a growing list of cosmeceuticals, have been used in the treatment of melasma, albeit in smaller studies. A growing range of topical agents is available for the treatment of melasma. While larger, more robust studies are warranted, nonhydroquinone cosmeceuticals may be useful adjuncts or alternatives to the gold standard of triple‐combination hydroquinone cream.
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Extensive melanin production and accumulation inside the skin may result in a number of disorders, among which is acquired hyperpigmentation, such as melasma. Skin hyperpigmentation is attributed to either the increase in the number of melanocytes or the hyperactivity of melanogenic enzymes. Genetic susceptibility, ultraviolet radiation, hormonal remedies as well as the abnormal release of the α-melanocyte stimulating hormone (α-MSH) represent the provoking factors contributing to such disorder. On the account of their prominent localization in skin-exposed areas, hyperpigmentation may possess cosmetic and psychosocial relevance, and subsequently many efforts have been exerted to help rectify this skin disorder. The current review presents the approaches adopted to treat melasma. It also reviews the active molecules counteracting the melanogenesis process and the diverse nanotechnology-based delivery systems, which showed successful topical delivery of hypopigmenting agents for the treatment of melasma.
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Background Ganoderma has been known as a cure for diseases since ancient times, and been used as a medicinal mushroom for more than 2000 years. By many accounts, Ganoderma lucidum extracts from fruit bodies exhibited the comparable tyrosinase inhibition activity. Aims To validate A. cinnamomea mycelia anti‐melanogenesis activity. Ethanolic extracts of A. cinnamomea mycelia were evaluated using in vitro cell‐free tyrosinase assay, cell‐based and zebrafish phenotype‐based method. Meanwhile, safety assessment was also conducted to ensure the feasibility as the novel ingredients in cosmetic and pharmaceutic industries. Methods The major regulatory enzymes being in charge of cutaneous pigmentation, was investigated in both cell‐free and cellular enzyme systems, and in phenotype‐based zebrafish model. A high‐throughput TLC in vitro screening system was introduced to perform the initial evaluation of those with anti‐melanin formation activity. Results Among the fractions, 50% ethanol extracted fraction (AC_Et50_Hex) exhibited highest anti‐melanin formation activity. AC_Et50_Hex (at 100 ppm) reduced 30% intracellular melanin of B16‐F10 cells through suppression of tyrosinase activity and its protein expression. For animal study, not only does AC_Et50_Hex exhibited similar depigmenting efficacy to kojic acid (56.1% vs 52.3%) with lower dosage (50 ppm vs 1400 ppm), but showed less toxicity to zebrafish. Conclusion A. cinnamomea mycelium extracts can be an ideal candidate/substitute for skin‐whitening since kojic acid has been reported with carcinogenic effect. AC_Et50_Hex was recognized as a potential tyrosinase inhibitor throughout in vitro and in vivo analysis studies. The mass production of A. cinnamomea mycelium from agitated fermentation realizes the natural mushroom extracts for commercial application.
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Melasma is a common acquired disorder of symmetric hyperpigmentation that usually affects the face, with females and darker skin types having a higher prevalence. Melasma has an uncertain aetiology, but it is thought to be caused by an increase in melanocyte biological activity rather than an increase in melanocyte amount. Excess or over-pigmentation of the skin causes pigmentary disorders. The amount of collagen, elastin, and melanin in the skin are all factors that contribute to hyper pigmentation. Hypermelanosis may result from an increase in epidermal melanin or a combination of increased epidermal melanin and melanin deposition in the dermis. KEYWORD: Melasma, Melanin, Pigment, Melanocyte. List of abbreviate EDTA Ethylenediaminetetraacetic Acid DOPA Dihydroxyphenylalanine HQ Hydroquinone
Article
Background Hyperpigmentation disorders are commonly encountered in dermatology clinics. The use of prescription-grade and over-the-counter topical lightening agents have increased in popularity, leading to a substantial growth of research over the past decade. Objective We seek to review clinical studies evaluating the use of different Rx-grade and OTC ingredients in treating hyperpigmentation. Methods & Materials: A comprehensive search on PubMed was conducted to identify patient-based evidence on the most common ingredients used as topical lightening agents: arbutin, ascorbic acid, cysteamine, hydroquinone, kojic acid, niacinamide, retinoids, triple-combination therapy. The topicals were classified as either prescription-grade or over-the-counter. Results Varying levels of evidence support the use of topicals in treating hyperpigmentation. There were more clinical trials examining Rx-grade products than OTC products. Mild but tolerated side effects are noted in many of these agents. Conclusion Careful monitoring and adjustment of doses will be needed to maximize skin lightening benefits and minimize side effects.
Chapter
Bioprospecting is a methodical search for natural ingredients and genes in wildlife that have the potential to be turned into industrial products by biological, genetic, and chemical manipulation and without harming nature. Bioprospecting in cosmetics has made leaps from utilizing plant seeds to fungi, from traditional and herbal cosmetics to vegan and natural products made from seaweed and oats. The undiscovered potential of our ecosystem and diverse species has never-ending possibilities of biological value. The chapter aims to outline the various aspects of bioprospecting in cosmetic industry addressing the need to keep in line with various ethical guidelines and enlisting various natural products in use in cosmetic industry.
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Skin whitening is a term used for lightening the complexion of the skin through artificial means like creams, lotions, soaps and injections. Unfortunately, the appeal of these skin bleaching products is based on the obsession of people across the world with skin color. Melanins are produced by specialized cells, termed melanocytes, which are located primarily in the skin, hair bulbs, and eyes. The melanins can be of two basic types: eumelanin’s, which are brown or black, and phaeomelanin’s, which are red or yellow, in mammals typically there are mixtures of both types Increased production and accumulation of melanins characterize number of skin diseases, which include hyperpigmentation such as melanoma, post-inflammatory melanoderma, solar lentigo, etc. Several modalities of treatment for these problems are available including chemical agents or physical therapies. The aim of this review article is to show that some of the skin whitening creams, often sold illegally without a prescription may contain dangerous ingredients that could put people health at risk
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Aloin A/B and aloesin are the major bioactive constituents in the Aloe vera, with diverse pharmacological activities, including anti‐bacterial, anti‐tumour, anti‐inflammatory and intestinal regulation. However, the in vivo metabolism of aloin A/B and aloesin are still unclear. In this study, the metabolic processes of aloin A/B and aloesin in rats were investigated using the ultra‐high performance liquid chromatography coupled with quadrupole time‐of‐flight mass spectrometry (UPLC‐Q‐TOF/MS) and MetaboLynxTM software with Mass defect filter (MDF) technique. Based on the proposed method, the prototype component of three compounds were all detected in the rat plasma, urine and feces. Meanwhile, 25 aloin A/B metabolites (6 phase I, 3 phase II, 16 phase I combined with phase II) and 3 aloesin metabolites (2 phase I and 1 phase II) were detected in rats after oral administration of aloin A, aloin B and aloesin, and the main biotransformation reactions were hydroxylation, oxidation, methylation, acetylation, and glucuronidation. In addition, Aloin A and aloin B can be transformed into each other in vivo and the metabolic profiles of aloin A and aloin B were identical. These results provide essential data for further pharmaceutical researches and clinical application of aloin A/B and aloesin.
Chapter
Research on novel agents from botanicals without the harmful side effects is ongoing and the results are promising. Botanical agents acting as tyrosinase inhibitors include aloe vera extract, rumex occidentalis, and bearberry. Herbal extracts have other actions such as antioxidants, free radical scavengers, and photoprotectants. Some botanicals may have different or several mechanisms of action like melanosome uptake inhibition by keratinocytes and epidermal melanin removal.
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The effects of α- and β-arbutin on the activity of tyrosinases from mushroom and mouse melanoma were examined. α-Arbutin was synthesized from hydroquinone and starch using glucoside synthetase (GSase). β-Arbutin inhibited both tyrosinase activities from mushroom and mouse melanoma. α-Arbutin inhibited only the tyrosinase from mouse melanoma, 10 times as strongly as β-arbutin. The IC50 of α-arbutin was 0.48 mM and its inhibitory mechanism was speculated to be mixed type inhibition, while that of β-arbutin was noncompetitive.
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In humans the major stimulus for cutaneous pigmentation is ultraviolet radiation (UVR). Little is known about the mechanism underlying this response, in part because of the complexity of interactions in whole epidermis. Using a recently developed culture system, human melanocytes were exposed daily to a physiologic range of UVR doses from a solar simulator. Responses were determined 24 hours after the last exposure. There was a dose-related increase in melanin content per cell and uptake of 14C-DOPA, accompanied by growth inhibition. Cells from donors of different racial origin gave proportionately similar increases in melanin, although there were approximately tenfold differences in basal values. Light and electron microscopy revealed UVR-stimulated increases in dendricity as well as melanosome number and degree of melanization, analogous to the well-recognized melanocyte changes following sun exposure of intact skin. Similar responses were seen with Cloudman S91 melanoma cells, although this murine cell line required lower UVR dosages and fewer exposures for maximal stimulation. These data establish that UVR is capable of directly stimulating melanogenesis. Because cyclic AMP elevation has been associated in some settings with increased pigment production by cultured melanocytes, preliminary experiments were conducted to see if the effects of UVR were mediated by cAMP. Both alpha-MSH and isobutylmethylxanthine (IBMX), as positive controls, caused a fourfold increase in cAMP level in human melanocytes and/or S91 cells, but following a dose of UVR sufficient to stimulate pigment production there was no change in cAMP level up to 4 hours after exposure. Thus it appears that the UVR-induced melanogenesis is mediated by cAMP-independent mechanisms.
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We have evaluated the chemotherapeutic potential of 2,4-dihydroxyphenylalanine, a targeted prodrug that can be hydroxylated by tyrosinase (monophenol monooxygenase, EC 1.14.18.1) within melanoma cells to form the cellular toxin 2,4,5-trihydroxyphenylalanine (6-hydroxydopa). 2,4-Dihydroxyphenylalanine proved to be cytotoxic to both B-16 and Cloudman melanoma cells in vitro. The immediate effects of 2,4-dihydroxyphenylalanine included inhibition of DNA, RNA, and protein syntheses. In contrast, no decrease in macromolecular synthesis or viability was seen against cultures of MJY-alpha mammary tumor or L-1210 leukemia, two cell types that do not contain tyrosinase. Within the melanoma cultures, greater cytotoxicity was seen against melanotic (tyrosinase-containing) cells than against amelanotic (tyrosinase-lacking) cells. The cytotoxicity of 2,4-dihydroxyphenylalanine was blocked by 1-phenylthiourea, an inhibitor of tyrosinase. These results show that 2,4-dihydroxyphenylalanine is toxic to melanoma cells and that activation of 2,4-dihydroxyphenylalanine requires the presence of tyrosinase.
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Histochemical (dopa reaction) and electron microscopic studies were carried out to elucidate the nature of the chemical depigmentation produced by hydroquinone (HQ). Depigmentation was induced by topical application or subcutaneous injection of HQ in black guinea pigs. The present study showed that HQ preferentially affected the nonfollicular and follicular melanocyte system. It caused decreased formation of melanosomes, a marked alteration in the internal structure of melanosomes, an increased degradation of melanosomes , and , finally, a destruction of the membranous organelles in the melanocytes. These findings indicate that HQ affects not only the formation, melanization, and degradation of melanosomes, but that it affects also the membraneous structures of melanocytes and eventually causes necrosis of whole melanocytes.
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The Journal of Investigative Dermatology publishes basic and clinical research in cutaneous biology and skin disease.
Article
Arbutin, a naturally occurring beta-D-glucopyranoside of hydroquinone, is effective in the topical treatment of various cutaneous hyperpigmentations characterized by hyperactive melanocyte function. We examined the mechanism of its depigmenting action in human melanocyte cultures. Arbutin inhibited the tyrosinase activity of cultured human melanocytes at noncytotoxic concentrations. It did not affect the expression of tyrosinase mRNA. Melanin production was inhibited significantly by arbutin, as determined by measuring eumelanin radicals with an electron spin resonance spectrometer. The study of the kinetics and mechanism for inhibition of tyrosinase confirms the reversibility of arbutin as a competitive inhibitor of this enzyme. The utilization of L-tyrosine or L-dopa as the substrate suggests a mechanism involving competition with arbutin for the L-tyrosine binding site at the active site of tyrosinase. These results suggest that the depigmenting mechanism of arbutin in humans involves inhibition of melanosomal tyrosinase activity, rather than suppression of the expression and synthesis of tyrosinase.
Article
In the present study, we show that aloesin, which is a low molecular weight ingredients present in Aloe vera, stimulates the proliferation of cultured human hepatoma SK-HEP-1 cells. The incorporation of [3H] thymidine into DNA in the cell cultures was significantly increased at a dose of 10 microM aloesin. The aloesin-induced DNA synthesis appears to require newly synthesized proteins because cycloheximide treatment blocked the DNA synthesis evoked by this compound. We then examined whether this compound increases the intracellular levels of cell cycle regulators by immunoblotting. The data showed that aloesin increased the levels of cyclin E, CDK2, and CDC25A in SK-HEP-1 cells. In addition, immuno-complex kinase assays showed that aloesin up-regulated the enzyme activity of cyclin E/CDK2 kinase in a dose-dependent manner. Collectively, these results suggest that aloesin stimulates the proliferation of SK-HEP-1 cells by inducing the intracellular levels of cyclin E/CDK2 kinase complex and CDC25A, which, together, result in the up-regulation of cyclin E-dependent kinase activity.
Article
In this study, we present evidence that cotreatment of aloesin and arbutin inhibits tyrosinase activity in a synergistic manner by acting through a different action mechanism. Aloesin or arbutin similarly inhibited enzyme activity of human- and mushroom-tyrosinases with an IC50 value of 0.1 or 0.04 mM, respectively. Lineweaver-Burk plots of the enzyme kinetics data showed that aloesin inhibited tyrosinase activity noncompetitively with a Ki value of 5.3 mM, whereas arbutin did it competitively (Maeda, 1996). We then examined whether cotreatment of these agents inhibits the tyrosinase activity in a synergistic manner. The results showed that 0.01 mM aloesin in the presence of 0.03 mM arbutin inhibited activity of mushroom by 80% of the control value and the reverse was also true. The inhibitory effects were calculated to be synergistic according to the Bürgi method. Taken together, we suggest that aloesin along with arbutin inhibits in synergy melanin production by combined mechanisms of noncompetitive and competitive inhibitions of tyrosinase activity.
Article
Research since the 1986 review has largely upheld the therapeutic claims made in the earlier papers and indeed extended them into other areas. Treatment of inflammation is still the key effect for most types of healing but it is now realized that this is a complex process and that many of its constituent processes may be addressed in different ways by different gel components. A common theme running though much recent research is the immunomodulatory properties of the gel polysaccharides, especially the acetylated mannans from Aloe vera, which are now a proprietary substance covered by many patents. There have also been, however, persistent reports of active glycoprotein fractions from both Aloe vera and Aloe arborescens. There are also cautionary investigations warning of possible allergic effects on some patients. Reports also describe antidiabetic, anticancer and antibiotic activities, so we may expect to see a widening use of aloe gel. Several reputable suppliers produce a stabilized aloe gel for use as itself or in formulations and there may be moves towards isolating and eventually providing verified active ingredients in dosable quantities
Article
Inhibition by ALOE extracts of L-dopa oxidation by mushroom-tyrosinase was examined. 2''- O-Feruloylaloesin and aloesin at concentrations of 0.4 microM showed inhibition of 27 and 30%, respectively. Lineweaver-Burk plots of the concentration of L-dopa in the absence and presence of 2''- O-feruloylaloesin, 0.4 and 0.8 microM, showed that this compound inhibits mushroom-tyrosinase noncompetitively. The K (i) value obtained was 8.5 x 10 (-5) M. 2''- O-Feruloylaloesin and aloesin contents were analyzed by a reversed-phase HPLC, and their seasonal variations were observed.
Arbutin: mechanism of its depigmenting action in human melanocyte culture
  • Maeda