Skin-whitening Agent Research Articles

"Skin Whitening Creams: Cosmetovigilance."

Cosmeceutical products such as skin-lightening agents have been used globally to enhance skin tone and obtain a magnificent outward appearance. The pigment known as melanin, produced by melanocytes, imparts skin color. The Cosmetic Europe survey testifies that most people believe that cosmetics enhance one's quality of life. The most in-demand in the cosmetics industry are skin-whitening agents. Heavy metals and dangerous substances like lead and mercury are present in these skin-brightening cosmetics, which have a long-term effect on important organs and begin asymptomatic. Despite these negative consequences, there is a sizable market for these products due to the desire for fairer skin tones. Cosmetovigilance studies determine the of heavy metals in these preparations, which need to be monitored regularly. This article discusses the toxicity of heavy metals such as nickel, mercury, arsenic, lead, cobalt, and others found in skin-lightening formulas. The acceptable limit for these toxic agents is recognized by several healthcare organizations worldwide.

Cytotoxicity of Ethyl Acetate Extract of Avocado Seeds (Persea americana Mill.) on Mouse Melanoma B16F10 Cell Line

Artificial whitening agents available in the market can cause damage to melanocytes; therefore, a safe and naturally derived skin-whitening agent is needed. Avocado seeds (Persea americana Mill.) are often discarded as waste but possess numerous health benefits. One of the compounds in avocado seeds is catechin, a flavonoid metabolite. This compound has been reported to exhibit antioxidant activity and inhibit tyrosinase to prevent melanin formation, making it suitable for skin-whitening applications. This study aimed to conduct phytochemical screening, assess antioxidant activity using the DPPH method, analyze catechin content using HPLC, and perform cell viability tests using the MTT method from the ethyl acetate extract of avocado seeds. Phytochemical screening has revealed the presence of flavonoids, saponins, and steroids. The DPPH assay yielded an IC50 value of 89.47±0.73 ppm, indicating an intense antioxidant activity, and HPLC detected 0.09% catechin. The MTT test results yielded cell viability percentages ranging from 80-100% at test concentrations of 0.75-25 ppm, with an IC50 value of 61.7 ppm. In conclusion, our results indicate that the ethyl acetate extract from avocado seeds affects cell viability without toxicity, warranting further testing for tyrosinase inhibition in the mouse melanoma B16F10 cell line.

Treatment with Ascorbyl Glucoside-Arginine Complex Ameliorates Solar Lentigos.

Little is known about the anti-pigmenting effects of skin-whitening agents on solar lentigos (SLs). To characterize the anti-pigmenting effects of a newly designed derivative ascorbyl glucoside-arginine complex (AGAC) on SLs, lotions with or without 28% AGAC were applied twice daily for 24 weeks in a double-blind half-face study of 27 Japanese females with SLs. The pigmentation scores and skin colors of previously selected SLs on the right and left sides of the faces of the subjects were evaluated using a photo-scale, a color difference meter and a Mexameter. Treatment with the test lotion elicited a significant decrease in pigmentation scores at 24 weeks compared to week 0, with a significant decrease in pigmentation scores at 24 weeks compared to the placebo lotion. In the test lotion-treated SLs, the lightness (L) and melanin index (MI) values that reflect the pigmentation level significantly increased and decreased, respectively, at 12 and 24 weeks of treatment compared to week 0. Comparisons of increased L values or decreased MI values between the test and placebo lotion-treated SLs demonstrated that the test lotion-treated SLs had significantly higher increased L or decreased MI values than the placebo lotion-treated SLs both at 12 and 24 weeks of treatment. The sum of our results strongly indicates that AGAC is distinctly effective in ameliorating the hyperpigmentation levels of SLs at a level visibly recognizable by the subjects, without any hypo-pigmenting effects or skin problems.

Anti-Melanogenic Effects of Umbelliferone: In Vitro and Clinical Studies.

Melanin overexpression causes skin hyperpigmentation, which is associated with various skin disorders and cosmetic concerns. Umbelliferone, a natural coumarin found widely in plant species, has been noted for its antioxidant and anti-inflammatory effects but has received little attention for its impact on melanogenesis. Here, the effects of umbelliferone on melanogenesis were investigated in vitro and in clinical studies. The results showed that umbelliferone was non-cytotoxic to human skin and B16F10 melanoma cells. It also exhibited significant anti-melanogenic effects, reducing both melanin production and tyrosinase activity in a dose-dependent manner. This effect was achieved through a decrease in tyrosinase mRNA levels. Furthermore, umbelliferone in a formulation was stable under different temperature conditions, and after four weeks of topical application, it significantly decreased the melanin index and increased skin lightness (L*) values compared to those at the baseline. Overall, these findings demonstrate the potential of umbelliferone as a promising skin-lightening agent in the cosmetics industry.

Snow White's tale in nephrology: the emerging threat of skin-whitening creams on kidney health.

The timeless tale of Snow White, with its emphasis on fair skin as a beauty ideal, mirrors a contemporary issue in nephrology: the harmful impact of skin-whitening creams on kidney health. Fairness creams have deeply embedded themselves in global society, driven by a pervasive obsession with lighter skin tones as a symbol of beauty. This widespread use reflects deeply rooted cultural beliefs and social norms, despite the significant health risks associated with these products. Despite regulatory bans, these creams often contain hazardous substances such as hydroquinone, mercury, and arsenic, posing serious health risks. Mercury, a frequent component of these cosmetics, disrupts melanin synthesis by inhibiting tyrosinase, leading to serious health risks, including nephrotoxicity. Chronic exposure to mercury from cosmetics can harm the liver, kidneys, nervous system, and eyes, with the kidneys being particularly vulnerable. This review discusses the link between fairness creams and the occurrence of glomerular diseases. It delves into the mechanisms by which skin-whitening agents cause kidney damage. Mercury can induce kidney damage through direct cellular toxicity and immune-mediated mechanisms. We present evidence from case studies and published studies connecting mercury-containing creams to nephrotic syndrome. Minimal change disease and membranous nephropathy are the most frequently reported glomerular diseases due to these products. Treatment typically involves stopping the use of the creams and chelation therapy, with glucocorticoids and immunosuppressants for non-responsive cases. The prognosis is generally favourable, with high remission rates, and relapses are seldom reported. By highlighting the nephrotoxic effects of skin-whitening creams, this manuscript emphasizes the urgent need for stringent regulatory oversight and increased public awareness to prevent further health complications.

Phytochemical Investigation and Biological Activities of Desmodium heterocarpon Extract as Anti-Tyrosinase: Isolation of Natural Compounds, In Vitro and In Silico Study.

Tyrosinase is an important enzyme in the biosynthesis of melanin. Many skin-whitening agents that inhibit tyrosinase activity from natural sources have been identified because they are harmless and non-toxic. In this work, 114 samples of 54 Fabaceae plants were assessed for their anti-tyrosinase activity using a dopachrome method. The results found that Desmodium heterocarpon stems and roots demonstrated the highest tyrosinase inhibitory activity at 20 µg/mL (92.50 ± 1.09%), whereas the water extract of Artocarpus lacucha and kojic acid demonstrated 87.41 ± 0.61% and 95.71 ± 0.33%, respectively. Six compounds were isolated from this plant, including genistein (1); hexadecanoic acid (2); salicylic acid (3); β-sitosterol-D-glucoside (4); 2,3-dihydroxybenzoic acid (5); and 2,5-dihydroxybenzoic acid (6). Among them, 2,5-dihydroxybenzoic acid demonstrated a potential effect for tyrosinase inhibition with an IC50 of 57.38 µg/mL, while standards of kojic acid and the water extract of A. lacucha showed 2.46 and 0.15 µg/mL, respectively. 2,3-dihydroxybenzoic acid had a similar structure as 2,5-dihydroxybenzoic acid; however, it was shown to have tyrosinase inhibitory activity, with an IC50 of 128.89 µg/mL. Studies using computer simulations confirmed this reservation. The determination of antimicrobial activities found that 2,5-dihydroxybenzoic acid showed the strongest inhibitory activity against Staphylococcus aureus, with MIC and MBC of 5 and 5 µg/mL, respectively. In addition, it inhibited MRSA, S. epidermidis, Propionibacterium acnes, Escherichia coli, and Pseudomonas aeruginosa, with MIC and MBC of 15-30 and 15-40 µg/mL. It showed potential activities against yeast and filamentous fungi, such as Candida albicans, Microsporum gypseum, Trichophyton rubrum, and T. mentagrophytes, with MIC and MFC of 15 µg/mL. So, 2,5-dihydroxybenzoic acid could inhibit tyrosinase activity and microorganisms that cause skin diseases. Therefore, it can be concluded that this plant has advantageous properties that will be investigated and further developed for possible uses, particularly in the cosmetic and pharmaceutical industries.

Glutathione as a skin-lightening agent and in melasma: asystematic review.

Hyperpigmentary disorders, including melasma, are challenging to treat. Glutathione has anti-melanogenic and antioxidant properties, which led to its use as a skin-lightening agent. Our objective was to review the published evidence and literature on the efficacy and safety of glutathione as a skin-lightening agent and in the treatment of melasma. A literature search was done in the PubMed, Embase, and Cochrane library databases using the search terms "glutathione as a skin-lightening agent" and "glutathione in melasma" for the past 10 years. The level of evidence, strength of recommendation, and risk of bias assessment were evaluated. Among various forms of topical glutathione, glutathione 0.5% was significantly more effective compared to glutathione 0.1% and placebo. For glutathione alone versus glutathione plus microneedling, more improvement was seen. Five randomized controlled trials and a single open-arm clinical study on oral glutathione at doses of 250 mg once a day, 250 mg twice a day, and 500 mg once a day showed a significant reduction in the melanin index compared to placebo. The combination of topical 2% glutathione plus oral glutathione was superior to monotherapy alone. There was only one placebo-controlled study on intravenous (IV) glutathione [6/16 (37.5%) vs. 3 (18.7%), (p0.054)]. The risk of bias assessment showed that almost an equal number of studies have low and high risk of bias. Topical versus oral glutathione both provide moderately efficacious skin-lightening outcomes that are localized versus generalized and have minimal versus substantial adverse effects, but they are unsustainable, with variable costs. IV glutathione is contraindicated due to lack of efficacy and side effects. It may work more as an antioxidant in melasma.

α-Arbutin ameliorates UVA-induced photoaging through regulation of the SIRT3/PGC-1α pathway.

Owing to its tyrosinase inhibitory activity, α-arbutin has been added to several skin care products as a skin-lightening agent. However, the protective effect of α-arbutin against ultraviolet A (UVA)-induced photoaging has not been well investigated. The present study was designed to investigate the photoprotective effect and mechanism of α-arbutin against UVA-induced photoaging. In vitro experiments, HaCaT cells were treated with UVA at a dose of 3J/cm2 to evaluate the anti-photoaging effect of α-arbutin. α-Arbutin was found to exhibit a strong antioxidant effect by increasing glutathione (GSH) level and inhibiting reactive oxygen species (ROS) production. Meanwhile, α-arbutin markedly improved the expression of sirtuin 3 (SIRT3) and peroxisome proliferator-activated receptor γ coactivator 1 α (PGC-1α) proteins, initiating downstream signaling to increase mitochondrial membrane potential and mediate mitochondrial biogenesis, and improve mitochondrial structure significantly. In vivo analysis, the mice with shaved back hair were irradiated with a cumulative UVA dose of 10J/cm2 and a cumulative ultraviolet B (UVB) dose of 0.63J/cm2. The animal experiments demonstrated that α-arbutin increased the expression of SIRT3 and PGC-1α proteins in the back skin of mice, thereby reducing UV-induced skin damage. In conclusion, α-arbutin protects HaCaT cells and mice from UVA damage by regulating SIRT3/PGC-1α signaling pathway.

Exploration of Compounds with 2-Phenylbenzo[d]oxazole Scaffold as Potential Skin-Lightening Agents through Inhibition of Melanin Biosynthesis and Tyrosinase Activity.

Inspired by the potent tyrosinase inhibitory activity of phenolic compounds with a 2-phenylbenzo[d]thiazole scaffold, we explored phenolic compounds 1-15 with 2-phenylbenzo[d]oxazole, which is isosterically related to 2-phenylbenzo[d]thiazole, as novel tyrosinase inhibitors. Among these, compounds 3, 8, and 13, featuring a resorcinol structure, exhibited significantly stronger mushroom tyrosinase inhibition than kojic acid, with compound 3 showing a nanomolar IC50 value of 0.51 μM. These results suggest that resorcinol plays an important role in tyrosinase inhibition. Kinetic studies using Lineweaver-Burk plots demonstrated the inhibition mechanisms of compounds 3, 8, and 13, while docking simulation results indicated that the resorcinol structure contributed to tyrosinase binding through hydrophobic and hydrogen bonding interactions. Additionally, these compounds effectively inhibited tyrosinase activity and melanin production in B16F10 cells and inhibited B16F10 tyrosinase activity in situ in a concentration-dependent manner. As these compounds showed no cytotoxicity to epidermal cells, melanocytes, or keratinocytes, they are appropriate for skin applications. Compounds 8 and 13 demonstrated substantially higher depigmentation effects on zebrafish larvae than kojic acid, even at 800- and 400-times lower concentrations than kojic acid, respectively. These findings suggest that 2-phenylbenzo[d]oxazole is a promising candidate for tyrosinase inhibition.

An In‐Depth Review on Recent Progress in Synthetic Approaches and Biological Activities of Thiazol‐2(3H)‐Imine Derivatives

AbstractThis review presents the in‐dept analysis of the synthetic approaches towards thiazol‐2(3H)‐imine and embarks at its various biological properties published during 2000 to 2023. The most important method of synthesis involves the reaction of substituted thioureas and α‐halo carbonyl compounds, and condensation and nucleophilic addition of 2‐amino‐1,3‐thiazoline with aldehydes. Additionally, isothiocyanate‐based multicomponent synthesis, and α‐nitroepoxides have been proved as benign precursors for this motif. Several eco‐friendly and solvent‐free synthesis from diazonium salts, acetylenes, tertiary enaminones and thiosemicarbazides have also been reported. This epitome is a unique combination of synthetic methods as well as biological activities like anti‐inflammatory, anti‐bacterial, anti‐cancer, anti‐leishmanial, anti‐microbial, herbicidal, anti‐HIV, and may be a valuable tool for researchers to tailor the synthetic procedures according to specific target structures and applications. Moreover, this review enlightens the applications of thiazol‐2(3H)‐imine as platelet GPIIB/IIIA receptor antagonists, alkaline phosphatase inhibitors, neurodegenerative drug Pifithrin‐α analogues, and skin whitening agents.

Antioxidant and Skin-Whitening Efficacy of a Novel Decapeptide (DP, KGYSSYICDK) Derived from Fish By-Products.

The skin is vulnerable to damage from ultraviolet rays and oxidative stress, which can lead to aging and pigmentation issues. This study investigates the antioxidant and whitening efficacy of a decapeptide (DP, KGYSSYICDK) derived from marine fish by-products and evaluates its potential as a new skin-whitening agent. DP demonstrated high antioxidant activity, showing comparable or superior performance to Vitamin C (Vit. C) in ferric reducing antioxidant power (FRAP) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging assays. In hydrogen peroxide (H2O2)-treated HaCaT cells, DP increased cell viability and reduced reactive oxygen species (ROS) generation. Furthermore, DP inhibited tyrosinase activity and decreased melanin production in α-melanocyte stimulating hormone (α-MSH)-induced B16F10 melanoma cells in a dose-dependent manner. Reverse transcription polymerase chain reaction (RT-PCR) analysis revealed that DP reduces the mRNA expression of MITF, tyrosinase, and MC1R, thus suppressing melanin production. DP exhibits strong binding interactions with multiple amino acid residues of tyrosinase, indicating potent inhibitory effects on the enzyme. These results suggest that DP possesses significant antioxidant and whitening properties, highlighting its potential as a skin-whitening agent. Future research should focus on optimizing DP's structure and exploring structure-activity relationships.

Glossogyne tenuifolia Essential Oil Prevents Forskolin-Induced Melanin Biosynthesis via Altering MITF Signaling Cascade

Glossogyne tenuifolia (Labill.) Cass. ex Cass (Compositae) is a herbaceous plant that is endemic to Taiwan. Traditional Chinese Medicine has utilized it as a treatment for fever, inflammation, and liver preservation. Recent research has unveiled its bioactivities, including anti-inflammation, anti-cancer, antiviral, antioxidant, anti-fatigue, hepatoprotection, and immune modulation elements. Nevertheless, its effect on skin health remains to be investigated. Thus, we investigated the impact of G. tenuifolia essential oil (GTEO) on forskolin (FRK)-induced melanin biosynthesis and its mechanisms in B16-F10 murine melanoma in vitro. Treatment of GTEO resulted in a substantial decrease in FRK-induced melanin production, accompanied by a significant decrease in tyrosinase mRNA and protein expression levels. Additionally, our data demonstrated that the decrease in tyrosinase expression resulted from the suppression of MITF, as indicated by the reduced movement of MITF into the cell nucleus. Moreover, GTEO prompted a prolonged ERK1/2 activation, leading to the decline of MITF through proteasomal degradation, and it was verified that GTEO had no inhibitory impact on MITF activity in ERK1/2 inhibitor-treated cells. Additional studies demonstrated that α-pinene and D-limonene, which are the primary components in GTEO, showed strong melanin and tyrosinase inhibitory effects, indicating that α-pinene and D-limonene may contribute to its anti-melanogenic effects. Collectively, these data presented compelling proof that GTEO, along with its primary components α-pinene and D-limonene, show great potential as natural sources for developing innovative skin-whitening agents in the field of cosmetics.

Preparation and Evaluation of Nanoemulsion Formulation Containing Kojic Acid and Kojyl 3-aminopropylphosphonic Acid.

The kojyl 3-aminopropylphosphonic acid (KAP) was synthesized by kojic acid (KA) with a 3-aminopropylphosphonic acid. Which is more stable than KA and showed better skin penetration and anti-pigmentation efficacy in melanocytes. However, up till now, there have been no studies aimed at incorporating KAP into an emulsion system and evaluating its effectiveness. We develop a novel skin-lightening agent using KAP as the active ingredient and a low-cytotoxic nanoemulsion as the delivery system in this study. The sorbitan monooleate and polysorbate surfactants with polyethylene glycol (PEG) co-surfactant were used to generate a nanoemulsion system. The transparency and particle size stability over various storage times indicate that the formulated nanoemulsions are suitable for long-term storage. Besides, results demonstrate that the anti-pigmentation function of KA and KAP-containing nanoemulsions (NE-KA and NEKAP) evidently outperformed that of the non-packed KA and KAP group. Despite having the lowest concentration among other treatments, NE-KAP was able to reduce melanin content to approximately 80% of the blank. Our findings suggest that this newly developed nanoemulsion containing KAP could potentially serve as a sustainable alternative to hydroquinone for treating dermal hyperpigmentation disorders in future applications.

The Use of Over-the-Counter (OTC) Skin-Lightening Agents and Their Side Effects Among the Residents of Saudi Arabia: A Cross-Sectional Study.

Over-the-counter (OTC) skin-lightening agents are topical products in the form of lotions, creams, oils, soaps, and serums designed to alter skin pigmentation primarily for cosmetic purposes. The growing misuse and overuse of these products has become a serious public health concern due to their potential adverse effects on human health and their quality of life. This study was cross-sectional in nature, adopting a convenience sampling technique utilizing data from a sample of 408 residents of Arar, Northern Saudi Arabia. The participants completed online questionnaires,distributed through social media means like Telegram, WhatsApp, and Facebook ensuring anonymity. Data was analyzed using SPSS Version 27 to obtain important insights. The sample of the study had a predominance of females 304 (74.5%) while only 104 (25.5%) were males. A substantial proportion of 170 (41.7%) of the participants were aged between 20 and 35 years with more than half (229 (56.2%)) being single and the majority (266 (65.2%))having university and above level of education. More than half (259 (63.5%)) of them indicated that they had bought skin-lightening products without a doctor's prescription. Twenty-eight (10.8%) of the participants had been diagnosed with a condition that increased skin pigmentation before with a substantial proportion (11 (39.3%)) noting that the product contained hydroquinone cream ingredients. The overall prevalence of OTCskin-lightening agents among the participants of Arar, Northern Saudi Arabia was 63.5% (259/408). The study found a significantly high prevalence of use of OTCskin-lightening agents among participants aged 20-35 years (87 (71.3%)) (p=0.031) as well as those who had a university level of education and above (129 (71.3%)) (p=0.001). The findings show that 39 (40.6%) of the female respondents and eight (30.8%) of the male participants experienced adverse effects associated with irritation and redness. Overall, the study found a considerably high prevalence of the use of OTCskin-lightening agents among the participants of Arar, Northern Saudi Arabia. The use of OTCskin-lightening agents was significantly greater among female participants than male participants. The commonly used products contained hydroquinone cream ingredients, which presented adverse effects and complications associated with irritation, redness, and darkening of the skin. It is imperative to launch targeted public awareness campaigns to educate the community, especially women, about the risks associated with OTC skin-lightening agents, promote safer alternatives, and advocate for stricter regulation and control over the sale and distribution of skin-lightening products containing harmful ingredients.

Preparation and characterization of novel nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN) containing coenzyme Q10 as potent antioxidants and antityrosinase agents

We developed novel and optimal Q10-NLC/SLN formulations as antioxidant and anti-tyrosinase agents. The formulations were analyzed for particle size, morphology, entrapment efficiency (EE %), and long-term stability. The in vitro drug release and in vivo skin penetration were evaluated using dialysis bag diffusion and Sprague Dawley (SD) rats, respectively. Cytotoxicity and protecting effects were assessed by AlamarBlue® assay, ROS level by DCFH-DA, and tyrosinase activity by l-DOPA assay, measuring the absorbance at 470 nm. The selected formulations had optimal surface characterizations, including Z-average size, PDI, and Zeta potential ranging from 125 to 207 nm, 0.09–0.22, and −7 to −24, respectively. They also exhibited physiochemical stability for up to 6 months and EE% above 80 %. The lipids ratio and co-Q10 amount as variable factors significantly affected particle size and zeta potential but were insignificant on PDI. The in vitro release diagram showed that Q10-NLC/SLN revealed a fast release during the first 8 h and prolonged release afterward. The in vivo skin permeation revealed a higher accumulative uptake of co-Q10 in the skin for Q10-NLC/SLN compared to Q10 emulsions. Both selected Q10-NLC and Q10-SLN could reduce intracellular ROS after exposure to H2O2. The Q10-NLC was found to be more potent for inhibiting the tyrosinase activity compared to O10-SLN. The results suggest that the new formulations are promising carriers for topical delivery of co-Q10 as an anti-aging and skin-whitening agent.

Illuminating the shadows: an insight into periorbital hyperpigmentation

Periorbital hyperpigmentation (POH), also referred to as periorbital melanosis or dark eye circles, is a common dermatological concern characterized by darkening of the skin around the eyes. This review article aims to comprehensively analyze the current understanding of POH, encompassing its epidemiology, etiopathogenesis, clinical manifestations, diagnosis and available treatment modalities, and focusing on patients’ skin color. The review also consolidates a grading system for POH and emphasizes the importance of accurate diagnosis using clinical examination, assessment scores, Wood’s lamp, ultrasonography, and dermoscopy. Treatment modalities range from non-pharmacological measures to topical agents, including kojic acid, alpha-arbutin, vitamin C, vitamin E, niacinamide, retinoids, and hydrating agents. The manuscript explores the efficacy of various skin-lightening agents, such as hydroquinone, and introduces emerging treatments like caffeine, carotenoids, lactic acid, curcumin, and vitamin K. Additionally, it delves into procedural treatments like chemical peels, lasers, blepharopigmentation, mesotherapy, platelet-rich plasma therapy, fillers, autologous fat transplantation, and surgical interventions. The comprehensive approach to understanding and managing POH presented in this review aims to provide clinicians with valuable insights into the diverse therapeutic options available for this challenging cosmetic concern.

Synthesis and Characterization of Metronidazole and Heterocycle Ester Dyads for Tyrosinase Inhibitory Activity

Tyrosinase is an important copper-based enzyme mainly involved in skin pigmentation. The inhibition of the tyrosinase enzyme attracts importance in cosmetic and medicinal chemistry industry for its applications in skin whitening and anti-browning agents for humans as well as in food, agriculture industries. Imidazole based Metronidazole and its derivatives are widely accepted drug for wide range of diseases. Therefore, the present report involves the synthesis of heterocyclic derivatives of metronidazole and investigation of its efficacy towards the tyrosinase inhibitory activity. A series of metronidazole esters were synthesized and their chemical structures were confirmed using spectral techniques like, infrared spectroscopy (IR), proton nuclear magnetic resonance (1H-NMR), and liquid chromatography-mass spectrometry (LC-MS). All the compounds were evaluated for its tyrosinase inhibitory activity by oxidation of 3,4-dihydroxyphenylalanine in the presence of the synthesized esters(I-VIII) with kojic acid as standard. Among the synthesized compounds, VII (isonicotinic ester) and VIII (quinoline ester) demonstrated significant activity IC50 values 92.5 and 91.8µM respectively. Further molecular docking experiments were carried out for the synthesized compounds with 2y9w protein exhibited greater number of physical interactions for compounds VII and VIII than the other compounds in the series confirming the mushroom tyrosinase activity.

Synthesis and evaluation of coumarin derivatives on antioxidative, tyrosinase inhibitory activities, melanogenesis, and in silico investigations

New coumarin derivatives were designed using a 2-(2-oxo-2H-chromen-4-yl)acetic acid scaffold conjugated with amino acid esters or tyramine. The anti-tyrosinase and anti-lipid peroxidation activities of the synthesized compounds were investigated. Coumarin derivatives 7,9, 11–13, 15–18 showed strong anti-lipid peroxidation activity. Compound 13 exhibited uncompetitive tyrosinase inhibitory activity with an IC50 value of 68.86 µM. Compound 14 (% activity = 123.41) showed stronger tyrosinase activating activity than 8-methoxypsolaren (8-MOP, % activity = 109.46). In silico studies revealed different poses between the inhibitors and activators near the tyrosinase catalytic site. Compounds 13 (25–50 μM) and 14 (25–100 μM) did not show cytotoxicity against B16F10 cells. In contrast to the tyrosinase inhibition assay, compound 13 (50 μM) suppressed melanogenesis in B16F10 cells with two times higher potency than KA (100 μM). Compound 14 at 100 μM showed melanogenesis enhancement in B16F10 cells in a dose-dependent manner, however, inferior to the 8-MOP. Based on the findings, compound 13 and 14 offer potential for development as skin-lightening agents and vitiligo therapy agents, respectively.

Patchouli Alcohol: A Potent Tyrosinase Inhibitor Derived from Patchouli Essential Oil with Potential in the Development of a Skin-Lightening Agent

The inhibitory effects of Pogostemon cablin essential oil (patchouli essential oil, PEO) and its primary bioactive compound, patchouli alcohol (PA), on tyrosinase and melanin were investigated in vitro and ex vivo. Treatment with PEO and PA significantly, as well as dose-dependently, reduced forskolin (FRK)-induced melanin biosynthesis, cellular tyrosinase activity, and tyrosinase (TYR) protein expression. However, the transcriptional levels of TYR and tyrosinase-related proteins (TRP-1 and TRP-2) remained unaffected. These results suggest that PEO and PA may directly interrupt tyrosinase enzyme activity, leading to a reduction in melanin biosynthesis. Further experiments supported this notion, revealing that both PEO and PA significantly and dose-dependently inhibited mushroom tyrosinase activity in both the monophenolase and diphenolase phases. Additionally, an in silico molecular docking analysis was performed, utilizing a homology model of human tyrosinase. In conclusion, these findings strongly suggest that patchouli essential oil and its primary bioactive component, patchouli alcohol, hold promise as potential treatments for hyperpigmentary skin conditions and in the development of cosmetic products designed to lighten the skin.

Future Challenges and Opportunities of Marine Algae in Cosmeceuticals

Abstract: Marine algae have garnered significant attention in the cosmeceutical industry due to their diverse array of bioactive compounds and unique properties. As the demand for sustainable and effective skincare solutions rises, marine algae offer a promising avenue for innovation. This study explores the future challenges and opportunities of utilizing marine algae in cosmeceuticals. One of the foremost challenges lies in the sustainable sourcing and cultivation of marine algae to meet the growing demand while preserving marine ecosystems. Overcoming this challenge requires advancements in biotechnology, including the development of efficient cultivation techniques and sustainable harvesting practice. Cosmetics are widely used by people around the world to protect the skin from external stimuli. Consumer preference towards natural cosmetic products has increased as the synthetic cosmetic products caused adverse side effects and resulted in low absorption rate due to the chemicals’ larger molecular size. The cosmetic industry uses the term “cosmeceutical”, referring to a cosmetic product that is claimed to have medicinal or drug-like benefits. Marine algae are rich in bioactive substances that have shown to exhibit strong benefits to the skin, particularly in overcoming rashes, pigmentation, aging, and cancer. The current review provides a detailed survey of the literature on cosmeceutical potentials and applications of algae as skin whitening, anti-aging, anticancer, antioxidant, antiinflammation, and antimicrobial agents. The biological functions of algae and the underlying mechanisms of all these activities are included in this review. In addition, the challenges of using algae in cosmeceutical applications, such as the effectiveness of different extraction methods and processing, quality assurance, and regulations concerning extracts of algae in this sector were also discussed.