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1.
Skin Res Technol ; 30(10): e70102, 2024 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-39387830

RESUMO

BACKGROUND: Koenigia alpina (All.) T.M.Schust. & Reveal (alpine knotweed) is a perennial herb belonging to the Polygonaceae family. Several studies have examined Polygonaceae species' potential applications as cosmeceutical materials; however, the potential of K. alpina as a cosmeceutical has not yet been studied. MATERIALS AND METHODS: Hydrogen peroxide (H2O2) and lipopolysaccharide were used to induce an inflammatory response in RAW 264.7 cells. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radicals and H2O2 were used to evaluate the free-radical scavenging activity of K. alpina extract and its protective effect against reactive oxygen species (ROS)-induced cell damage. The whitening, antiaging, and cell proliferation/migration effects of the extracts were evaluated via tyrosinase inhibition, collagenase/elastase inhibition, and wound healing assays, respectively. The anti-inflammatory effect was confirmed by evaluating nitric oxide (NO) production in RAW 264.7 cells. High-performance liquid chromatography (HPLC), UV, and MS/MS were used to determine the main components of the extract and fractions. RESULTS: The ethyl acetate (EA) fraction and its aglycone fraction showed very high free-radical scavenging activities (47.5 and 47.1 µg/mL, respectively). The extract/fractions also showed significant tyrosinase inhibition (IC50 = 0.38 mg/mL in EA fraction), collagenase inhibition (IC50 = 0.21 mg/mL in EA fraction), and elastase inhibition (IC50 = 0.57 mg/mL in aglycone fraction). NO production in lipopolysaccharide-induced RAW 264.7 cells was inhibited by the extract/fractions. The extract also promoted the closure of scratch wounds in HaCaT cells. The K. alpina extract/fractions contained cardamonin, quercetin, and quercitrin. CONCLUSION: K. alpina extracts/fractions showed antioxidant, antiaging, whitening, and anti-inflammatory activities, suggesting they may have potential as antiaging cosmeceuticals.


Assuntos
Anti-Inflamatórios , Extratos Vegetais , Extratos Vegetais/farmacologia , Camundongos , Animais , Células RAW 264.7 , Humanos , Anti-Inflamatórios/farmacologia , Polygonaceae/química , Óxido Nítrico/metabolismo , Proliferação de Células/efeitos dos fármacos , Antioxidantes/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Peróxido de Hidrogênio/farmacologia , Sequestradores de Radicais Livres/farmacologia , Cicatrização/efeitos dos fármacos , Envelhecimento da Pele/efeitos dos fármacos , Movimento Celular/efeitos dos fármacos , Lipopolissacarídeos/farmacologia , Compostos de Bifenilo , Preparações Clareadoras de Pele/farmacologia , Picratos , Monofenol Mono-Oxigenase/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Células HaCaT
2.
Mar Drugs ; 22(9)2024 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-39330301

RESUMO

For thousands of years, pearl and nacre powders have been important traditional Chinese medicines known for their skin whitening effects. To prepare the enzymatic hydrolysates of Hyriopsis cumingii nacre powder (NP-HCH), complex enzymatic hydrolysis by pineapple protease and of neutral protease was carried out after the powder was pre-treated with a high-temperature and high-pressure method. The peptides were identified using LC-MS/MS and picked out through molecular docking and molecular dynamics simulations. Subsequently, the tyrosinase inhibitory and antioxidant properties of novel tyrosinase inhibitory peptides were investigated in vitro. In addition, the enzymatic activity of tyrosinase in B16F10 cells as well as melanin content and antioxidant enzyme levels were also examined. The results showed that a tyosinase inhibitory peptide (Tyr-Pro-Asn-Pro-Tyr, YPNPY) with an efficient IC50 value of 0.545 ± 0.028 mM was identified. The in vitro interaction results showed that YPNPY is a reversible competitive inhibitor of tyrosinase, suggesting that it binds to the free enzyme. The B16F10 cell whitening test revealed that YPNPY can reduce the melanin content of B16F10 cells by directly inhibiting the activity of intracellular tyrosinase. Additionally, it indirectly affects melanin production by acting as an antioxidant. These results suggest that YPNPY could be widely used as a tyrosinase inhibitor in whitening foods and drugs.


Assuntos
Antioxidantes , Melaninas , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase , Peptídeos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Animais , Peptídeos/farmacologia , Peptídeos/química , Peptídeos/isolamento & purificação , Camundongos , Antioxidantes/farmacologia , Antioxidantes/química , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Linhagem Celular Tumoral , Melanoma Experimental/tratamento farmacológico , Simulação por Computador , Espectrometria de Massas em Tandem , Preparações Clareadoras de Pele/farmacologia , Preparações Clareadoras de Pele/química , Preparações Clareadoras de Pele/isolamento & purificação , Simulação de Dinâmica Molecular
3.
Molecules ; 29(17)2024 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-39275009

RESUMO

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.


Assuntos
Melaninas , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase , Preparações Clareadoras de Pele , Animais , Humanos , Camundongos , Agaricales/enzimologia , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Melaninas/biossíntese , Melaninas/antagonistas & inibidores , Estrutura Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Oxazóis/química , Oxazóis/farmacologia , Pironas , Resorcinóis/química , Resorcinóis/farmacologia , Preparações Clareadoras de Pele/farmacologia , Preparações Clareadoras de Pele/química , Relação Estrutura-Atividade , Peixe-Zebra
4.
Soc Sci Med ; 360: 117334, 2024 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-39278013

RESUMO

Deliberate lightening of skin among African women is a complex phenomenon that intersects with cultural identity, health, beauty, and societal influence. The scientific literature has scarcely explored a comprehensive approach by interviewing users of skin lightening products. This article aims to analyze, through a comprehensive approach, the motivations underlying the deliberate lightening of skin among Burkinabe women. The research encompasses a narrative literature review and a qualitative field study in Bobo-Dioulasso, Burkina Faso. It targeted 59 women, categorized into current users, former users, and non-users of skin lightening products. Individual interviews and focus groups were utilized to gather qualitative data. The comprehensive approach enabled contextualization of the phenomenon, focusing on personal and collective motivations, while adhering to ethical principles. Participants gived various motivations for deliberate lightening of skin, including the pursuit of beauty, seduction, and social valorization. The majority used fairthese products to achieve a lightly pigmented, equating it with beauty and allure. Some aimed to enhance their seductive capital or improve their social status. Reasons for discontinuing the practice included awareness of health risks, societal pressure, and unmet objectives. Non-users cited reasons such as attachment to their natural skin tone, health concerns, and financial constraints. Deliberate lightening of skin can be viewed as a strategy to increase various forms of capital: aesthetic, seductive, social, and symbolic. This practice reflects socio-cultural dynamics and environmental influences, emphasizing the role of the body as capital in contemporary society. The findings reveal a heightened awareness among women of their body as a multifaceted capital, convertible into other forms of capital under certain conditions.


Assuntos
Grupos Focais , Motivação , Pesquisa Qualitativa , Humanos , Feminino , Adulto , Burkina Faso , Preparações Clareadoras de Pele , Pigmentação da Pele , Pessoa de Meia-Idade , Beleza , Adulto Jovem
5.
Int J Pharm ; 665: 124731, 2024 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-39306205

RESUMO

Melasma represents an acquired melanogenesis disorder resulting in skin's hyperpigmentation effect. Although several approaches are adopted for melasma treatment, nanotechnology presents the most convenient one. Therefore, the present work aimed to formulate and characterize three nano-vesicular systems namely, liposomes, penetration enhancer containing vesicles (PEVs) and invasomes to enhance the topical delivery of the skin whitening agent; alpha arbutin (α-arbutin) for the treatment of melasma. Liposomes were prepared according to a 23 full factorial design and the selected formula was further employed for the preparation of PEVs and invasomes. Results showed that the three vesicular systems exhibited nano-sizes ranging from 151.95 to 672.5 nm, negative charges ranging from -12.50 to -28.20 mV, high entrapment efficiencies ranging from 80.59 to 99.53 %, good stability and prolonged-release of α-arbutin for 24 h after dispersion in hydrogel form. The deposition study from the vesicular hydrogel confirmed their effectiveness for the drug's accumulation in the skin reaching an average of 1.6-fold higher in the stratum corneum, 1.6-1.8-fold higher in the epidermis, and 1.6-1.8-fold higher in the dermis compared to the free drug dispersion in hydrogel. A preliminary clinical split-face study on patients suffering from melasma revealed that α-arbutin-loaded liposomes and PEVs in hydrogel forms showed better clinical outcomes compared to the free α-arbutin hydrogel as well as to the previously published α-arbutin encapsulated in chitosan nanoparticles and dispersed in hydrogel form. This delineates the aforementioned nano-vesicular systems as effective and clinically superior delivery means for melasma management.


Assuntos
Administração Cutânea , Arbutina , Lipossomos , Melanócitos , Melanose , Absorção Cutânea , Pele , Melanose/tratamento farmacológico , Humanos , Arbutina/administração & dosagem , Melanócitos/efeitos dos fármacos , Melanócitos/metabolismo , Adulto , Feminino , Pele/metabolismo , Nanopartículas/administração & dosagem , Liberação Controlada de Fármacos , Preparações Clareadoras de Pele/administração & dosagem , Preparações Clareadoras de Pele/química , Adulto Jovem , Pessoa de Meia-Idade , Hidrogéis/química , Hidrogéis/administração & dosagem , Animais
6.
Mar Drugs ; 22(8)2024 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-39195491

RESUMO

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.


Assuntos
Antioxidantes , Melaninas , Monofenol Mono-Oxigenase , Preparações Clareadoras de Pele , Animais , Humanos , Camundongos , alfa-MSH/farmacologia , Antioxidantes/farmacologia , Antioxidantes/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Peixes , Células HaCaT , Peróxido de Hidrogênio/farmacologia , Melaninas/biossíntese , Melanoma Experimental/tratamento farmacológico , Melanoma Experimental/metabolismo , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Oligopeptídeos/farmacologia , Oligopeptídeos/química , Estresse Oxidativo/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Receptor Tipo 1 de Melanocortina/metabolismo , Pele/efeitos dos fármacos , Pele/metabolismo , Preparações Clareadoras de Pele/farmacologia , Pigmentação da Pele/efeitos dos fármacos
8.
J Drugs Dermatol ; 23(7): 567-568, 2024 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-38954615

RESUMO

We present a case of a patient with a 10-year history of blue-black macules and patches on the face and an associated history of skin-lightening cream usage. The skin lightening cream contained hydroquinone, which is often associated with exogenous ochronosis (EO). Interestingly, the biopsy did not show characteristic findings of ochronosis, confusing the final diagnosis, however discontinuing the skin-lightening creams halted the progression of the patient's skin lesions supporting a diagnosis of EO. EO presents as asymptomatic hyperpigmentation after using products containing hydroquinone. This condition is most common in Black populations, likely due to the increased use of skin care products and bleaching cream containing hydroquinone in these populations. Topical hydroquinone is FDA-approved to treat melasma, chloasma, freckles, senile lentigines, and hyperpigmentation and is available by prescription only in the US and Canada. However, with the increased use of skin-lightening creams in certain populations, it is important for dermatologists to accurately recognize the clinical features of exogenous ochronosis to differentiate it from similar dermatoses. An earlier diagnosis can prevent the progression to severe presentations with papules and nodules. We summarize the clinical presentations diagnostic features, and treatment pearls, concluding with a discussion of the differential diagnoses.  J Drugs Dermatol. 2024;23(7):567-568.     doi:10.36849/JDD.8248.


Assuntos
Hidroquinonas , Hiperpigmentação , Líquen Plano , Ocronose , Humanos , Ocronose/diagnóstico , Ocronose/induzido quimicamente , Hiperpigmentação/induzido quimicamente , Hiperpigmentação/diagnóstico , Hidroquinonas/efeitos adversos , Hidroquinonas/administração & dosagem , Diagnóstico Diferencial , Líquen Plano/diagnóstico , Líquen Plano/induzido quimicamente , Líquen Plano/tratamento farmacológico , Feminino , Preparações Clareadoras de Pele/efeitos adversos , Preparações Clareadoras de Pele/administração & dosagem , Dermatoses Faciais/diagnóstico , Dermatoses Faciais/induzido quimicamente , Dermatoses Faciais/patologia , Dermatoses Faciais/tratamento farmacológico , Pessoa de Meia-Idade , Creme para a Pele/efeitos adversos , Creme para a Pele/administração & dosagem
9.
J Cosmet Dermatol ; 23(11): 3585-3597, 2024 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-39016678

RESUMO

BACKGROUND: The challenging management of melasma highlights the inadequacies of conventional therapies and their high risk of recurrence. Integrating microneedling for device-assisted drug delivery with tranexamic acid (TA), recognized for its melanin synthesis inhibition, presents a novel approach that warrants further investigation to fully assess its potential in enhancing melasma treatment efficacy. METHODS: Fifty moderate to severe melasma patients participated in this randomized outcome-assessor-blinded controlled trial. Patients were randomly allocated into two main groups. Group A received a modified Kligman formula on one hemi-face on alternate nights for 2 months (A1) and three sessions of microneedling with 10% topical TA on the other hemi-face at 1-month intervals (A2). Group B used the same modified Kligman formula on both sides of the face, with one side additionally receiving three sessions of microneedling with 4% TA (B1) and the opposite side with 10% TA (B2). Primary outcomes were % Modified Melasma Area and Severity Index (mMASI) and % visual analogue scale (VAS) change during 6 month follow-up. Adverse events including post-inflammatory hyperpigmentation (PIH) and treatment tolerability were recorded. RESULTS: Compared to baseline, the mean mMASI reduction immediately after the final session was higher in A1, B1, and B2 (56.84%, 50.88%, and 55.87%, respectively) than in A2, which saw only a 13.16% reduction. Efficacy notably declined after the cessation of treatment across all groups. While the efficacy within groups A1, B1, and B2 was comparable, microneedling with 4% or 10% TA combined with the topical modified Kligman formula proved more potent in patients at a lower risk of PIH. Overall, 22% of patients reported PIH, particularly in the A2 group (28% of hemi-faces), with its occurrence significantly associated with treatment during warmer seasons and in darker skin phototypes. Other adverse events were not observed in any patient. Patient satisfaction was highest in groups B1 and B2, where approximately 72% reported 'excellent' satisfaction. The lowest durability rate (16%) was observed in group A2, while the highest (72%) was seen in group B2, comparable with groups A1 and B1. Treatment tolerability was reported 100% in all groups. CONCLUSION: It was found that the modified Kligman formula outperformed microneedling-TA alone. However, with optimal patient selection, particularly targeting those at lower risk for PIH with lighter skin phototypes and scheduling treatments during less-sunny seasons, combining microneedling with 4% or 10% TA and the modified Kligman formula significantly enhanced efficacy and satisfaction rates compared to conventional topical treatment.


Assuntos
Administração Cutânea , Agulhamento Seco , Melanose , Índice de Gravidade de Doença , Ácido Tranexâmico , Humanos , Melanose/terapia , Ácido Tranexâmico/administração & dosagem , Ácido Tranexâmico/efeitos adversos , Feminino , Adulto , Pessoa de Meia-Idade , Terapia Combinada/métodos , Terapia Combinada/efeitos adversos , Resultado do Tratamento , Agulhamento Seco/efeitos adversos , Agulhamento Seco/métodos , Agulhamento Seco/instrumentação , Agulhas/efeitos adversos , Preparações Clareadoras de Pele/administração & dosagem , Preparações Clareadoras de Pele/efeitos adversos , Masculino , Método Simples-Cego , Satisfação do Paciente , Face , Indução Percutânea de Colágeno
10.
Arch Dermatol Res ; 316(7): 378, 2024 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-38850450

RESUMO

Hydroquinone has been used for years for multiple conditions, including melasma, post-inflammatory hyperpigmentation, dyschromia from photoaging, and solar lentigines. It is known to be a very effective lightening agent, but several concerns have been raised about this widely used agent. The recent U.S. ban on over-the-counter skin lightening products containing hydroquinone has prompted further questioning of the safety of this widely used agent. While there have been prior informative, large-scale reviews on the safety of hydroquinone, new findings have since been reported. Here, we provide an updated review of studies published in the past 15 years on hydroquinone safety.


Assuntos
Hidroquinonas , Preparações Clareadoras de Pele , Hidroquinonas/efeitos adversos , Humanos , Preparações Clareadoras de Pele/efeitos adversos , Hiperpigmentação/induzido quimicamente , Melanose/tratamento farmacológico , Envelhecimento da Pele/efeitos dos fármacos
11.
Nanotechnology ; 35(40)2024 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-38901412

RESUMO

Hyperpigmentation is a skin disorder characterized by excessive production of melanin in the skin and includes dyschromias such as post-inflammatory hyperchromias, lentigens, melasma and chloasma. Topical products containing depigmenting agents offer a less aggressive treatment option for hyperpigmentation compared to methods like chemical peels and laser sessions. However, some of these agents can cause side effects such as redness and skin irritation. Encapsulating these actives in nanosystems shows promise in mitigating these effects and improving product safety and efficacy. In addition, nanocarriers have the ability to penetrate the skin, potentially allowing for targeted delivery of actives to the affected areas. The most commonly investigated nanosystems are nanoemulsions, vesicular nanosystems and nanoparticles, in which different materials can be used to generate different compositions in order to improve the properties of these nanocarriers. Nanocarriers have already been widely explored, but it is necessary to understand the evolution of these technologies when applied to the treatment of skin hyperchromias. Therefore, this literature review aims to present the state of the art over the last 15 years on the use of nanosystems as a potential strategy for encapsulating depigmenting actives for potential application in cosmetic products for skin hyperchromia. By providing a comprehensive overview of the latest research findings and technological advances, this article can contribute to improving the care and quality of life of people affected by this skin condition.


Assuntos
Portadores de Fármacos , Humanos , Portadores de Fármacos/química , Nanopartículas/química , Hiperpigmentação/tratamento farmacológico , Preparações Clareadoras de Pele/administração & dosagem , Preparações Clareadoras de Pele/química , Pele/efeitos dos fármacos , Pele/metabolismo
12.
Am J Clin Dermatol ; 25(5): 717-733, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38896402

RESUMO

Melasma is a chronic, acquired disorder of focal hypermelanosis that carries significant psychosocial impact and is challenging for both the patient and the treating practitioner to manage in the medium to long term. Multiple treatments have been explored, often in combination given the many aetiological factors involved in its pathogenesis. Therapeutic discoveries to treat melasma are a focal topic in the literature and include a range of modalities, with recent developments including updates on visible light photoprotection, non-hydroquinone depigmenting agents, oral tranexamic acid, chemical peels, and laser and energy-based device therapy for melasma. It is increasingly important yet challenging to remain up-to-date on the arsenal of treatments available for melasma to find an efficacious and well-tolerated option for our patients.


Assuntos
Abrasão Química , Melanose , Ácido Tranexâmico , Melanose/terapia , Melanose/diagnóstico , Humanos , Abrasão Química/métodos , Ácido Tranexâmico/uso terapêutico , Terapia a Laser/métodos , Resultado do Tratamento , Preparações Clareadoras de Pele/uso terapêutico , Preparações Clareadoras de Pele/administração & dosagem , Fármacos Dermatológicos/uso terapêutico , Terapia com Luz de Baixa Intensidade/métodos , Terapia com Luz de Baixa Intensidade/instrumentação
13.
J Cosmet Dermatol ; 23(11): 3724-3734, 2024 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-38923657

RESUMO

BACKGROUND: Natural herbs have been widely considered a reservoir for skin-lightening ingredients, but discovery of the effective ingredients from herbs remains a large challenge. AIM: This research aimed to rapidly identify compounds with skin-lightening activity in Chinese herbs. METHODS: The structure information of herbal compounds was collected and selected from the open-source data. High throughput virtual screening (HTVS) and Extra precision (XP) docking modes were used to screen for compounds that could bind to the mushroom tyrosinase involved in melanin synthesis. Furthermore, molecular dynamics (MD) simulations were introduced to assess the binding stability of those compounds with the key target protein. The candidate compounds found by this kind of multidimensional molecular screening were finally tested for their ability to inhibit pigmentation and potential toxicity using an in vivo zebrafish animal model. RESULTS: A Natural Compounds Database was established with 5616 natural compounds. Fourteen compounds with favorable binding capability were screened by the XP docking mode with mushroom tyrosinase and five compounds among them were found to have superior dynamic binding performance through MD simulations. Then the Zebrafish animal experiments revealed that two components, sennoside B (SB) and sennoside C (SC), could significantly inhibit melanogenesis rather than the other three compounds. Meanwhile, there were no obvious side effects observed in SB and SC about the morphology, heart rate, or body length of zebrafish. CONCLUSION: A strategy for rapid screening of compounds with whitening activity has been established, and two potent skin-lightening compounds, SB and SC, have been identified from a vast library of herbal compounds. This study revealed that SB and SC have potential for topical use in skin lightening for the first time. The findings of this study would provide an important theoretical basis for the application of these two compounds in the cosmetic field in the future.


Assuntos
Medicamentos de Ervas Chinesas , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase , Preparações Clareadoras de Pele , Pigmentação da Pele , Peixe-Zebra , Animais , Preparações Clareadoras de Pele/farmacologia , Preparações Clareadoras de Pele/química , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/química , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Pigmentação da Pele/efeitos dos fármacos , Simulação de Dinâmica Molecular , Melaninas , Modelos Animais , Agaricales/química , Ensaios de Triagem em Larga Escala
14.
J Cosmet Dermatol ; 23(9): 3030-3037, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38864461

RESUMO

BACKGROUND: In vitro single-cell experiments may yield inconsistent results compared to clinical trials. To enhance the reliability of cosmetic active ingredient screening, a coculture model of B16F10-HaCaT cells was established in vitro based on the structural characteristics of human skin, thereby improving the credibility of experimental outcomes. Currently, most cosmetic whitening additives primarily target simple efficacy goals such as inhibiting tyrosinase activity or melanin transfer. Therefore, investigating novel and efficient whitening additives has become a prominent research focus. OBJECTIVES: The aim is to establish an in vitro cell coculture model for more reliable experimental results and investigate the mechanism by which Paeonia lactiflora Pall seeds oil inhibits melanin production and transfer. METHODS: The impact of different concentrations of Paeonia lactiflora Pall seeds oil on cocultured cell proliferation rate was assessed using cck8 assay. Tyrosinase inhibition ability in cocultured cells was tested using levodopa as a substrate. Melanin production inhibition ability in coculture cells was evaluated by lysing cells with sodium hydroxide. The effect of Paeonia lactiflora Pall seeds oil on dendrite-related gene expression levels was examined through qPCR analysis. Additionally, Western blotting was employed to study the effect of Paeonia lactiflora Pall seeds oil on dendrite-related protein expression levels. RESULTS: Different concentrations of Paeonia lactiflora Pall seeds oil did not affect the proliferation activity of cocultured cells. A specific concentration of α-MSH increased cell tyrosinase activity, cellular melanin content, as well as Rac1, Cdc42, and PAR-2 gene and protein expression related to dendritic formation. Treatment with a certain concentration of Paeonia lactiflora Pall seeds oil resulted in decreased tyrosinase activity and melanin content in cells along with downregulated expression levels of Rac1, Cdc42, and PAR-2 genes and proteins associated with dendritic formation. CONCLUSIONS: Paeonia lactiflora Pall seeds oil at specific concentrations exhibits the ability to inhibit tyrosinase activity, decrease melanin content, and possesses the potential to impede melanin transfer.


Assuntos
Proliferação de Células , Técnicas de Cocultura , Melaninas , Monofenol Mono-Oxigenase , Paeonia , Óleos de Plantas , Sementes , Preparações Clareadoras de Pele , Paeonia/química , Humanos , Melaninas/biossíntese , Sementes/química , Óleos de Plantas/farmacologia , Monofenol Mono-Oxigenase/metabolismo , Proliferação de Células/efeitos dos fármacos , Preparações Clareadoras de Pele/farmacologia , Camundongos , Animais , Células HaCaT
15.
J Cosmet Laser Ther ; 26(1-4): 26-30, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38879806

RESUMO

Skin whitening is a practice that is used to obtain lighter skin tone and is most prevalent in Africa and Asia. Substances used for this procedure, such as hydroquinone or mercury have a variety of side effects and are banned in several countries. This study examined the popularity of internet searches for terms related to skin whitening and bleaching creams with the use of GoogleTrends (GT). GT was searched globally for the topic "skin whitening" and two terms "hydroquinone cream" and "mercury cream" throughout a 10-year period (01.09.2013-31.08.2023). The popularity of searches increased during the analyzed period. The topic "skin whitening" was most popular in Sudan, Vietnam, and Sri Lanka. The searches were higher for "hydroquinone cream" than "mercury cream" in almost all countries, besides the Philippines and Indonesia. Our study confirms that skin whitening practices are popular, especially among populations with darker skin tone. Despite potentially toxic side effects, creams with hydroquinone and mercury are increasingly searched worldwide. Education about skin whitening and the usage of bleaching substances should be implemented, especially in the regions of Africa and Asia.


Assuntos
Hidroquinonas , Internet , Preparações Clareadoras de Pele , Humanos , Preparações Clareadoras de Pele/efeitos adversos , Hidroquinonas/efeitos adversos , Mercúrio/efeitos adversos , Creme para a Pele/efeitos adversos , Pigmentação da Pele/efeitos dos fármacos
17.
J Ethnopharmacol ; 332: 118388, 2024 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-38796069

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: San-Bai Decoction (SBD) is a classic whitening prescription originally recorded in the 'Introduction to Medicine' of the Ming Dynasty. SBD has been known for invigorating Qi and blood, promoting spleen and stomach, whitening skin, and fading melasma. However, its pharmacodynamic material basis and specific mechanism remain unclear. AIM OF THE STUDY: The aim of this study is to clarify the pharmacodynamic material basis of SBD and its mechanism of removing melasma. MATERIALS AND METHODS: The positive and negative ion mass spectrum data of SBD extract were collected by UHPLC-Q-Exactive Orbitrap MS/MS, imported into Compound Discoverer (CD) 3.1 software, matched through the online database, and manually checked. Finally, the in vitro chemical components of SBD were classified. Similarly, the mass spectrum data of SBD in the serum of normal rats and melasma model rats were also analyzed by CD 3.1 software. The in vitro identified Compound file of SBD was imported into the Expected Compounds and the Generate Expected Compounds project was selected. The SBD compounds were then chosen under the Compound Section. All phase I and II reaction types related to SBD components were selected, and the metabolic platform of CD 3.1 software was utilized to process the results and obtain possible metabolites. The metabolites were scored and products with high scores were subsequently screened. According to literature comparison, the final metabolites of SBD in both normal rats and melasma model rats were determined and comprehensively analyzed. The Melasma model rats were constructed through intramuscular injection of progesterone and ultraviolet radiation B (UVB) irradiation. The preventing and treating effect of SBD on melasma were evaluated by regulating inflammation, epidermal collagen content, and oxidative stress. Additionally, the effect of SBD on the Phosphatidylinositol 3-kinase (PI3K)/Protein kinase B (Akt)/Glycogen synthase kinase 3ß (GSK3ß) pathway was investigated through Western blot (WB) to explore its underlying mechanism on whitening and removing melasma efficacy. RESULTS: Ultimately, 94 components were identified in SBD, including 41 flavonoids, 27 organic acids, and 9 glycosides, 3 terpenoids, 2 amides, 2 aldehydes, 1 phenylpropanoid and 9 other compounds. In the blood of normal rat group, a total of 24 prototype components and 61 metabolites were identified. Similarly, there were19 prototype components and 44 metabolites identified from the blood of melasma model rats. Pharmacodynamic experiment results indicated that SBD effectively reduced the incidence of melasma, prevent the loss of epidermal collagen, and elevate the activity of superoxide dismutase and decrease the malondialdehyde content in both liver and skin. Interestingly, the WB results demonstrated that SBD effectively activated PI3K/Akt/GSK3ß pathway, and down-regulated the expression of melanin-related proteins. CONCLUSIONS: For the first time, the components of SBD extracts, and its prototype components and metabolites in the blood of normal rats and melasma model rats were successfully identified by high-resolution liquid chromatography-mass spectrometry with CD software. Additionally, the differences of in vivo components of SBD between normal rats and melasma model rats were analyzed. The preventive and therapeutic effect of SBD on melasma was verified in the melasma model rats induced by progesterone and UVB irradiation, and its mechanism was related to activating PI3K/Akt/GSK3ß pathway and downregulating the expression of melanin-related proteins. These results provide an experimental foundation for further research on the pharmacodynamic substance basis and pharmacodynamic mechanism of SBD, as well as developing new anti-melasma formula with SBD.


Assuntos
Medicamentos de Ervas Chinesas , Melanose , Ratos Sprague-Dawley , Animais , Melanose/tratamento farmacológico , Ratos , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/química , Masculino , Modelos Animais de Doenças , Feminino , Espectrometria de Massas em Tandem , Cromatografia Líquida de Alta Pressão , Preparações Clareadoras de Pele/farmacologia
18.
J Pharm Biomed Anal ; 246: 116223, 2024 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-38763108

RESUMO

The utilization of Hydroquinone (HQ) in over-the-counter skincare items is subject to restrictions. Consequently, Arbutin (AR) serves as a reliable alternative for addressing hyperpigmentation in non-prescription topical formulations. Nevertheless, AR undergoes decomposition into HQ and p-Benzoquinone (BZ) when exposed to temperature stress, ultraviolet light, or dilution in an acidic environment, all of which can induce skin toxicity. The intention of this paper is to investigate the effect of extraction procedure on the conversion of AR to HQ and or BZ and to evaluate kinetics of AR hydrolysis to HQ. Meanwhile this study aims to evaluate AR and BZ interference with the United States Pharmacopoeia (USP) identification and assessment method for HQ Hydrolytic stress during extraction conditions underwent optimization through systematic screening tests. Subsequent assessment of the residual drug and its degradation products were achieved by HPLC method. The resulting data were meticulously fitted to various kinetic models. To analyze the potential interference of AR in HQ measurement using USP method, the standard concentrations of AR and HQ were analyzed through UV-VIS spectrophotometry. For enhanced certainty, a validated HPLC method analysis was also conducted. Notably, the acid hydrolysis of AR exhibited independence from its initial concentration. So, the hydrolytic degradation of AR exhibited a Zero-order kinetic profile. Furthermore, the proven interference of AR in the UV-VIS spectrophotometry method was identified within the context of the USP method. This study successfully utilized an adopted HPLC method for the concurrent quantification of AR, HQ, and BZ. The potential interference of AR in the UV-VIS spectrophotometric assay for HQ may lead to false results especially for regulatory purposes.


Assuntos
Arbutina , Benzoquinonas , Hidroquinonas , Hiperpigmentação , Arbutina/análise , Arbutina/química , Hidroquinonas/análise , Hidroquinonas/química , Benzoquinonas/química , Benzoquinonas/análise , Cromatografia Líquida de Alta Pressão/métodos , Hidrólise , Preparações Clareadoras de Pele/química , Preparações Clareadoras de Pele/análise , Cinética , Administração Tópica , Espectrofotometria Ultravioleta/métodos
19.
J Cosmet Dermatol ; 23(8): 2750-2756, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38664985

RESUMO

BACKGROUND: In Eastern culture, a fair complexion is the standard of beauty, leading to appearance-related distress among women with darker skin or facial pigmentation. Women seek whitening cosmetics to enhance their skin tone or correct their pigmentation, but their safety and effectiveness are paramount factors to consider. In this study, we evaluated the safety and whitening effects of a compound formula denoted as TEST comprising astaxanthin, nicotinamide, arbutin, and tranexamic acid. METHODS: Primary skin irritation and skin-whitening efficacy were examined. Three qualified melanization areas were treated with TEST, 7% ascorbic acid, or a blank. Skin color, the individual type angle (ITA°), and the melanin index (MI) were compared among treatment areas. RESULTS: TEST did not induce a skin response and exhibited a significantly higher ITA° than the blank, while no significant difference was observed with that of 7% ascorbic acid. Furthermore, the MI of TEST was significantly reduced posttreatment. CONCLUSIONS: TEST could be integrated into spot-fading and skin-whitening cosmeceuticals or functional cosmetics.


Assuntos
Arbutina , Ácido Ascórbico , Melaninas , Niacinamida , Preparações Clareadoras de Pele , Pigmentação da Pele , Raios Ultravioleta , Adulto , Feminino , Humanos , Arbutina/farmacologia , Arbutina/administração & dosagem , Ácido Ascórbico/farmacologia , Ácido Ascórbico/administração & dosagem , Melaninas/metabolismo , Niacinamida/farmacologia , Pele/efeitos dos fármacos , Pele/efeitos da radiação , Pele/metabolismo , Preparações Clareadoras de Pele/farmacologia , Preparações Clareadoras de Pele/administração & dosagem , Pigmentação da Pele/efeitos dos fármacos , Pigmentação da Pele/efeitos da radiação , Raios Ultravioleta/efeitos adversos , Xantofilas/farmacologia , Xantofilas/administração & dosagem
20.
Clin Dermatol ; 42(5): 513-514, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38615979

RESUMO

The skin-lightening (SL) industry has a global reach and is projected to continue to grow over the coming decade. Although SL treatments may be safely prescribed for the treatment of some dermatologic conditions, many over-the-counter SL products contain ingredients that can cause harm to the skin and other organ systems. Given a lack of transparent information to patients and the historical colorist foundation that contextualizes a component of the cosmetic SL industry, dermatologists need to navigate biomedical and ethical concerns when explaining SL products to patients. This commentary briefly outlines the medical ethical issues surrounding this topic and describes avenues by which dermatologists may provide informed patient care that best supports beneficence, justice, autonomy, and nonmaleficence.


Assuntos
Preparações Clareadoras de Pele , Humanos , Preparações Clareadoras de Pele/efeitos adversos , Dermatologia/ética , Pigmentação da Pele
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