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1.
Pediatr Blood Cancer ; 71(4): e30859, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38225622

RESUMO

BACKGROUND: Melanomas of the central nervous system (CNS) based on neurocutaneous melanocytosis (NCM) are exceptionally rare in childhood and have been described only sporadically. Rapidly progressive disease may represent a major challenge for treating physicians, especially given the limited knowledge about this condition. This analysis aimed to increase knowledge about the occurrence and treatment of these malignancies. PROCEDURE: Data on diagnosis, treatment, and outcome of patients aged 0-18 years with CNS melanoma based on NCM recorded in the German Registry for Rare Pediatric Tumors (STEP registry) were analyzed. Additionally, published case reports on this condition were analyzed. RESULTS: In STEP, five patients with leptomeningeal melanoma based on NCM were identified, with a median age at melanoma diagnosis of 3.7 years. Various multimodal treatments were performed: (partial) resection (n = 4), irradiation (n = 2), trametinib (n = 3), different cytostatics (n = 2), and anti-GD2 immunotherapy (n = 1). All patients died between 0.3 and 0.8 years after diagnosis. Including published case reports, 27 patients were identified with a median age of 2.8 years at melanoma diagnosis (range: 0.2-16.6). Fourteen of 16 cases with reported data had a NRAS alteration (88%), particularly NRAS p.Q61K (85%). In the expanded cohort, no patient survived longer than 1 year after diagnosis despite multimodal therapy (including trametinib; n = 9), with a median survival of 0.4 years (range 0.1-0.9). CONCLUSIONS: CNS melanomas based on NCM in childhood are aggressive malignancies without curative treatment to date. Therapeutic approaches must be individualized. Genetic tumor sequencing is essential to improve understanding of tumorigenesis and potentially identify new therapeutic targets.


Assuntos
Neoplasias do Sistema Nervoso Central , Melanoma , Melanose , Síndromes Neurocutâneas , Criança , Humanos , Pré-Escolar , Melanoma/genética , Sistema Nervoso Central/patologia , Síndromes Neurocutâneas/tratamento farmacológico , Síndromes Neurocutâneas/genética , Melanose/tratamento farmacológico , Melanose/etiologia , Neoplasias do Sistema Nervoso Central/complicações
2.
Lipids Health Dis ; 23(1): 138, 2024 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-38734619

RESUMO

BACKGROUND: Skin barrier alterations play a crucial function in melasma development. Past researches have demonstrated variations in lipid content between the epidermis of melasma lesions and normal tissues, along with the varied expression of lipid-related genes in melasma. This study aimed to analyze the lipidome profiles of skin surface lipids (SSL) in patients with melasma before and after treatment to understand associated abnormalities. METHODS: Melasma was treated with tranexamic acid orally and hydroquinone cream topically. Disease was assessed using the Melasma Area and Severity Index (MASI), and the impact to life was evaluated with Melasma Quality of Life (MELASQoL) score. Epidermal melanin particles were observed using reflection confocal microscopy (RCM), whereas epidermal pigment and blood vessel morphology were observed using dermoscopy, and SSL samples were collected. Specific information regarding alterations in lipid composition was obtained through multivariate analysis of the liquid chromatography-mass spectrometry data. RESULTS: After treatment, patients with melasma exhibited decreased MASI and MELASQoL scores (P < 0.001); RCM revealed reduced melanin content in the lesions, and dermoscopy revealed fewer blood vessels. Fifteen lipid subclasses and 382 lipid molecules were identified using lipidomic assays. The expression levels of total lipids, phosphatidylcholine, and phosphatidylethanolamine in the melasma lesions decreased after treatment (P < 0.05). CONCLUSION: This study revealed alterations in the SSL composition after effective melasma treatment, suggesting a compensatory role for lipids in melasma barrier function. The mechanism involving SSL and the lipid barrier, which influences melasma's occurrence, needs further elucidation.


Assuntos
Hidroquinonas , Lipidômica , Melanose , Qualidade de Vida , Humanos , Melanose/tratamento farmacológico , Feminino , Adulto , Hidroquinonas/uso terapêutico , Hidroquinonas/administração & dosagem , Ácido Tranexâmico/uso terapêutico , Pessoa de Meia-Idade , Melaninas/metabolismo , Masculino , Lipídeos/sangue , Lipídeos/análise , Epiderme/metabolismo , Epiderme/efeitos dos fármacos , Epiderme/patologia , Fosfatidiletanolaminas/metabolismo , Fosfatidilcolinas/metabolismo , Pele/patologia , Pele/efeitos dos fármacos , Pele/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos
3.
J Drugs Dermatol ; 23(4): e110-e112, 2024 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-38564390

RESUMO

Tranexamic acid (TXA) is an antifibrinolytic medication largely known for its efficacy in managing menorrhagia, or heavy periods, making it a medication predominantly used by women.


Assuntos
Melanose , Ácido Tranexâmico , Masculino , Humanos , Ácido Tranexâmico/uso terapêutico , Administração Cutânea , Melanose/tratamento farmacológico , Resultado do Tratamento
4.
J Drugs Dermatol ; 23(1): 1266-1270, 2024 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-38206144

RESUMO

BACKGROUND: Dyschromia can be associated with increased production and/or reduced clearance of pigmentation in the skin. Multiple pathways are involved in causality. A novel topical product was recently developed, which contains actives that have been validated through in-vitro and clinical studies to counteract pigmentation related to photodamage, PIH, and melasma. This study further evaluates the safety and efficacy of this product for facial dyschromia during an additional 3-month extension period following the completion of the previous 12-week multi-center trial.  Study Design: Subjects from the previous multi-center trial with mild to severe facial dyschromia at baseline were eligible to participate in this 3-month extension study upon completion of that trial. This extension study evaluated the continued use of the novel topical product with PATH-3 Technology (Alastin Skincare, Carlsbad, CA) over a 3-month period. Subjects who were previously randomized to the novel topical product continued using it and for those previously randomized to hydroquinone 4% discontinued its use. Both cohorts continued daily sunscreen use. Blinded investigators assessed subjects at follow-up visits at 16, 20, and 24 weeks. RESULTS: Twenty-six (26) subjects completed the extension phase of the pivotal trial, with 13 subjects in each of the AL and HQ-BREAK cohorts. Significant improvements were seen within the AL cohort from weeks 12 to 24 for facial dyschromia (P=0.0158) and skin tone/clarity/evenness (P=0.0067), while there were no significant improvements seen in the HQ-BREAK cohort. The HQ-BREAK cohort had more subjects who worsened with facial dyschromia and skin tone/clarity/evenness. For the mMASI, the HQ-BREAK cohort demonstrated regression at week 24 compared to week 12, while the AL cohort instead experienced continued improvement. This difference was found to be significant (P=0.02). No study-related adverse events were reported for either cohort.  Conclusion: A novel topical product designed to counteract various steps in pigmentation pathways using PATH-3 Technology has been demonstrated to be safe and effective in treating facial dyschromia on a long-term basis. In contrast to the significant rebound experienced by subjects with HQ, the AL cohort continued to demonstrate ongoing improvement. J Drugs Dermatol. 2024;23(1):1266-1270.     doi:10.36849/JDD.7622.


Assuntos
Melanose , Transtornos da Pigmentação , Humanos , Pigmentação da Pele , Melanose/diagnóstico , Melanose/tratamento farmacológico , Projetos de Pesquisa , Face
5.
J Drugs Dermatol ; 23(2): 9-16, 2024 02 01.
Artigo em Inglês | MEDLINE | ID: mdl-38306138

RESUMO

BACKGROUND: Modified Kligman's formula (mKF) is the gold standard treatment for melasma; however, its prolonged use is not recommended due to side effects. Cysteamine is a potent, safe, and effective depigmenting agent. Here, we conducted a double-blind, randomized, and placebo-controlled clinical trial to assess the efficacy of cysteamine isobionic-amide -- a complex with enhanced depigmenting efficacy -- and compared it to mKF for the treatment of melasma. METHODS: This study involved a total of 80 patients divided into 3 groups: cysteamine-isobionic amide, placebo, or mKF. The modified Melasma Area Severity Index (mMASI) score and spectrophotometric evaluation were conducted at baseline, week 4, week 8, and week 16. Dermatological assessment, patients’ feedback, and satisfaction including quality-of-life scores were also collected. RESULTS: At week 4, cysteamine isobionic-amide and mKF groups showed an equivalent onset of action in terms of mMASI and skin pigmentation contrast reduction. The 2 groups significantly reduced melasma severity and improved the overall skin condition with a comparable efficacy at week 16. Quality of life of melasma patients was significantly improved in the cysteamine isobionic-amide group at week 8 and further at week 16 (P<0.001) compared to the mKF group. Patients’ feedback and satisfaction were higher with the cysteamine isobionic-amide product compared to mKF. CONCLUSION: Cysteamine isobionic-amide provided a rapid onset of action and was as effective as the mKF for the treatment of melasma. The data suggest that cysteamine isobionic-amide could potentially be an acceptable alternative to mKF for the long-term treatment of melasma. J Drugs Dermatol. 2024;23(2):9-16.  doi:10.36849/JDD.7428.


Assuntos
Cisteamina , Melanose , Humanos , Cisteamina/efeitos adversos , Resultado do Tratamento , Qualidade de Vida , Melanose/diagnóstico , Melanose/tratamento farmacológico , Método Duplo-Cego
6.
J Drugs Dermatol ; 23(1): 1260-1265, 2024 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-38206158

RESUMO

Dyschromia is the result of irregular facial pigmentation. These cutaneous manifestations can have a significant impact on the quality of life of those affected, especially among females and skin of color. In this randomized, double-blinded, two-cell, single-center, 16-week clinical study, all subjects had moderate to severe (scores 4-9 on the modified Griffiths Scale) hyperpigmentation and skin unevenness of the face such that approximately 20% of subjects had post-inflammatory hyperpigmentation (PIH), 40% had overall mottled hyperpigmentation, and 40% had superficial melasma (Superficial Melasma was determined by Wood's Lamp Assessment). Study participants received either Product A (proprietary new formulation - Cysteamine HSA) or Product B (current marketed product - Cyspera®) and used the test product either in the morning or at night, beginning with every other day application, and then advanced to every day, or as tolerated. The results revealed that both Product A (Cysteamine HSA) and Product B (Cyspera®) had statistically significant improvement in facial hyperpigmentation and skin unevenness, however, Product A (Cysteamine HSA) had better tolerability results for scaling, peeling, burning, stinging, erythema, and dryness, indicating that Product A (Cysteamine HSA) outperformed Product B (Cyspera®). J Drugs Dermatol. 2024;23(1):1260-1265.     doi:10.36849/JDD.7584.


Assuntos
Hiperpigmentação , Melanose , Feminino , Humanos , Cisteamina , Hiperpigmentação/diagnóstico , Hiperpigmentação/tratamento farmacológico , Melanose/diagnóstico , Melanose/tratamento farmacológico , Qualidade de Vida , Pele , Método Duplo-Cego
7.
J Drugs Dermatol ; 23(7): 529-537, 2024 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-38954613

RESUMO

BACKGROUND: Melasma is a chronic pigmentary disorder. In this study, an innovative cream combining cysteamine and tranexamic acid (TXA) was assessed. OBJECTIVE: To evaluate the safety, efficacy, and patient satisfaction of a novel nano-formulated cysteamine and TXA combination cream in treating subjects with epidermal melasma. METHODS:   Fifty (50) randomized subjects participated and received cysteamine and TXA combination cream. The cream was applied for 30 minutes daily for a 3-month duration. Treatment effectiveness, safety, patient satisfaction, and adherence were evaluated. RESULTS: A continuous improvement in melasma was observed, with modified Melasma Area and Severity Index (mMASI) scores improving by 40%, 57%, and 63% at 30, 60, and 90 days, respectively. The primary endpoint of a decrease in mMASI scores was met, with 91% of participants experiencing melasma improvement. Patient Satisfaction and Patient Adherence scores indicated satisfaction. Convenience exhibited the strongest correlation with patient adherence.  Conclusion: Nano-formulated cysteamine and TXA combination cream showed significant efficacy in decreasing mMASI score while demonstrating a strong safety profile and patient satisfaction.  J Drugs Dermatol. 2024;23(7):529-537.     doi:10.36849/JDD.7765R1.


Assuntos
Cisteamina , Adesão à Medicação , Melanose , Satisfação do Paciente , Ácido Tranexâmico , Humanos , Melanose/tratamento farmacológico , Melanose/diagnóstico , Cisteamina/administração & dosagem , Cisteamina/efeitos adversos , Ácido Tranexâmico/administração & dosagem , Ácido Tranexâmico/efeitos adversos , Feminino , Adulto , Resultado do Tratamento , Pessoa de Meia-Idade , Masculino , Creme para a Pele/administração & dosagem , Creme para a Pele/efeitos adversos , Administração Cutânea , Índice de Gravidade de Doença , Combinação de Medicamentos , Nanopartículas/administração & dosagem , Adulto Jovem
8.
J Drugs Dermatol ; 23(6): e151-e153, 2024 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-38834215

RESUMO

BACKGROUND: Melasma and post-inflammatory hyperpigmentation (PIH) are common cosmetic dermatologic conditions that predominantly affect patients with skin phototypes III-VI. Comparing treatment coverage for these pigmentary disorders to treatment coverage for acne vulgaris may demonstrate disparities in insurance coverage for diseases that primarily affect patients of color. OBJECTIVE: Describe differences in Medicaid coverage for topical tretinoin for melasma and PIH vs. acne vulgaris in all 50 states and the District of Columbia. METHODS: This is a cross-sectional study of Medicaid insurance plans in all 50 states and the District of Columbia conducted between February 1 and 28, 2023. Data was collected from online publicly available preferred drug lists, prior authorization criteria, and email/telephone inquiries. Information was collected regarding coverage restrictions, including age restrictions, diagnostic restrictions, preferred drug status, and prior authorization requirements. RESULTS: Complete coverage data for all three clinical indications was retrieved from 30 (58.8%) states; partial coverage data for acne vulgaris was retrieved from 16 (31.4%) states; no coverage data was retrieved from 5 (9.8%) states. Of states reporting coverage data, topical tretinoin is covered in 45 (97.8%) states for acne vulgaris and 10 (33.3%) states for melasma and post-inflammatory hyperpigmentation. There was decreased Medicaid coverage of topical tretinoin for acne vulgaris compared to melasma and PIH (P<0.05).  Conclusion: There is differential Medicaid coverage for acne vulgaris compared to pigmentary disorders which disproportionately affect patients of color. Greater advocacy is required to ensure equal treatment for conditions that affect racial minority patients. J Drugs Dermatol. 2024;23(6):e151-e153.     doi:10.36849/JDD.8069e  .


Assuntos
Acne Vulgar , Cobertura do Seguro , Medicaid , Tretinoína , Humanos , Estados Unidos , Acne Vulgar/tratamento farmacológico , Tretinoína/administração & dosagem , Tretinoína/economia , Medicaid/estatística & dados numéricos , Estudos Transversais , Cobertura do Seguro/estatística & dados numéricos , Hiperpigmentação/tratamento farmacológico , Disparidades em Assistência à Saúde/economia , Feminino , Ceratolíticos/administração & dosagem , Ceratolíticos/economia , Melanose/tratamento farmacológico , Masculino
9.
Zhongguo Zhong Yao Za Zhi ; 49(13): 3552-3565, 2024 Jul.
Artigo em Zh | MEDLINE | ID: mdl-39041127

RESUMO

Based on UHPLC-Q-Exactive Orbitrap HRMS coupled with the network pharmacology and molecular docking, the common material basis and molecular mechanisms of Bletillae Rhizoma for melasma, gastrointestinal hemorrhage, lung cancer and bronchoplumonary inflammation as "homotherapy for heteropathy" were explored. The fingerprint of 17 batches of Bletillae Rhizoma from different areas was established using HPLC, and the similarity analysis was carried out. The common chemical components of the 17 batches of Bletillae Rhizoma were identified using UHPLC-Q-Exactive Orbitrap HRMS. Depending on the bioavailability and drug-like properties of the common components, the active chemical components were screened, and then their protein targets were collected using the Traditional Chinese Medicine Database and Analysis Platform(TCMSP) and SwissTargetPrediction database. The protein targets related to diseases were retrieved from the databases DrugBank, TTD and GeneCards to produce a Venn diagram. The shared targets were obtained between drugs and diseases as "homotherapy for heteropathy" targets. The protein-protein interaction(PPI) was analyzed with the STRING database, and KEGG and GO analyses of the "homotherapy for heteropathy" targets were performed using the Bioconductor database. Cytoscape 3.7.2 software was employed to construct the "chemical components of Bletillae Rhizoma-homotherapy for heteropathy targets" network and PPI network, and topological analysis was conducted to screen out the key active chemical components and core targets. Finally, the affinity between the active components and core targets was evaluated using the molecular docking by AutoDock Vina 4.2.6, which verified the interaction between them. Thirteen common peaks were identified by fingerprint chromatography, and the similarity between different batches was 0.941-0.998. Fifty-three chemical components were identified by mass spectrometry in Bletillae Rhizoma, and 18 common chemical constituents were obtained in the 17 batches of Bletillae Rhizoma. Network pharmacologic screening showed that the pharmacodynamic substances of Bletillae Rhizoma for melasma, gastrointestinal hemo-rrhage, lung cancer and bronchoplumonary inflammation with "homotherapy for heteropathy" were 11 compounds, such as polysaccharides, biphenanthrenes, dihydrophenanthrenes and bibenzyls. There were 42 common targets identified for the treatment of different diseases. These targets were involved in biological processes such as cell response to chemical stress, reactive oxygen species and positive regulation of protein kinase B signal transduction. They were also involved in 121 signaling pathways, encompassing vital pathways such as PI3K-Akt, ErbB, Rap1, FoxO, MAPK and estrogen. Molecular docking results showed a strong affinity between the key active components and the core targets. This study provides a preliminary explanation of how Bletillae Rhizoma exerts its therapeutic effect on chloasma, gastrointestinal hemorrhage, lung cancer, and bronchopneumonic lesions as "homotherapy for heteropathy" through a combined action involving multiple components, targets, and pathways. These findings offer a certain theoretical basis for the further deve-lopment and application of Bletillae Rhizoma.


Assuntos
Medicamentos de Ervas Chinesas , Neoplasias Pulmonares , Simulação de Acoplamento Molecular , Farmacologia em Rede , Rizoma , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Cromatografia Líquida de Alta Pressão , Rizoma/química , Neoplasias Pulmonares/tratamento farmacológico , Hemorragia Gastrointestinal/tratamento farmacológico , Melanose/tratamento farmacológico , Orchidaceae/química , Inflamação/tratamento farmacológico , Espectrometria de Massas
12.
J Vis Exp ; (203)2024 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-38314835

RESUMO

Melasma, a common, acquired facial pigmentation skin disorder, presents a straightforward clinical diagnosis but poses challenges in terms of effective management. The precise underlying causes of melasma remain elusive, and the current therapeutic approaches predominantly encompass pharmaceutical and laser interventions, with limited efficacy. Transdermal administration stands as a prevalent treatment method for melasma, often facilitated by the application of microneedles. Among these, tranexamic acid emerges as a frequently employed therapeutic agent. A subset of microneedles, known as roller microneedles, plays a significant role in this approach by delicately puncturing the epidermis with multiple fine needles, synergizing with drug delivery. This methodology not only enhances drug absorption but also augments treatment efficacy while minimizing tissue trauma. These attributes forecast promising avenues for the treatment of melasma. This article primarily introduces the combination of roller microneedle and tranexamic acid solution in the treatment of melasma and demonstrates the efficacy of roller microneedle and tranexamic acid solution in the treatment of melasma through clinical cases.


Assuntos
Melanose , Ácido Tranexâmico , Humanos , Ácido Tranexâmico/uso terapêutico , Administração Cutânea , Resultado do Tratamento , Melanose/tratamento farmacológico , Administração Oral
13.
J Cosmet Dermatol ; 23(2): 681-686, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38111320

RESUMO

OBJECTIVE: To observe the efficacy and safety of supramolecular salicylic acid monotherapy and supramolecular nicotinamide in the treatment of chloasma. METHODS: A total of 28 female patients with chloasma diagnosed in the dermatology outpatient department of our hospital were randomly divided into an experimental group and a control group, with 14 cases in each group. All patients were treated with 30% supramolecular salicylic acid every 2 weeks, for a total of 8 treatments. The experimental group was treated with 10% supramolecular nicotinamide once in the morning and once in the evening, and the control group was a blank control. Before each exfoliation treatment, subjects were photographed with a VISIA skin detector, and skin image analysis and modified melasma area and severity index (MASI) score were performed. RESULTS: According to the MMASI decrease rate (%) before and after treatment, the effective rate of the experimental group was 64.29%, and the effective rate of the control group was 14.29%. The results of the GriffithS10 and VISIA were improved. During the whole treatment, there was one mild adverse reaction in both groups. CONCLUSION: Salicylic acid stripping combined with nicotinamide in the treatment of chloasma is safe and effective, can improve skin conditions, and can be widely applied in clinical practice.


Assuntos
Abrasão Química , Melanose , Humanos , Feminino , Ácido Salicílico/efeitos adversos , Niacinamida/efeitos adversos , Pele , Abrasão Química/métodos , Melanose/tratamento farmacológico , Resultado do Tratamento
14.
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
15.
Int J Biol Macromol ; 270(Pt 2): 132255, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38729504

RESUMO

Melasma is an acquired hypermelanotic condition characterized by the presence of irregular light-to-dark brown macules that primarily manifest on the sun-exposed areas of the skin, particularly the face. The management of melasma poses significant challenges, as it is often recalcitrant to treatment and tends to recur despite successful treatment. In this study, we explored a safe, easy, and effective melasma treatment strategy. A hyaluronic acid (HA)-based microneedle (MN) patch loaded with tranexamic acid (TXA) was designed to deliver the necessary medication for melasma treatment. The MN patch features uniform needles with adequate mechanical strength and effective penetration and solubility in the skin without cytotoxicity. Remarkably, these MNs substantially reduce the thickness of the epidermis of melasma mice, curtail melanin production, and diminish dopachrome tautomerase (DCT) expression.


Assuntos
Ácido Hialurônico , Melanose , Agulhas , Ácido Tranexâmico , Ácido Hialurônico/química , Ácido Hialurônico/farmacologia , Melanose/tratamento farmacológico , Ácido Tranexâmico/administração & dosagem , Ácido Tranexâmico/farmacologia , Animais , Camundongos , Melaninas , Solubilidade , Adesivo Transdérmico , Feminino , Modelos Animais de Doenças , Oxirredutases Intramoleculares
16.
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
17.
J Dermatolog Treat ; 35(1): 2361106, 2024 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38843906

RESUMO

Purpose: This study aimed to evaluate the efficacy of tranexamic acid (TXA) in treating melasma through a meta-analysis and systematic review of randomized controlled trials (RCTs). The study focused on identifying associated adverse effects and comparing TXA's effectiveness with other melasma treatments.Materials and methods: Following PROSPERO and PRISMA guidelines, an extensive electronic search was conducted across four databases for RCTs on TXA use in melasma. Inclusion criteria encompassed full-text English articles with specific outcome measures, while studies with high bias risk or non-English publications were excluded. Data were extracted from 22 relevant studies and analyzed using the RevMan software, with heterogeneity identified using I² statistics and forest plots.Results: A total of 22 studies with 1280 patients were included. TXA was administered orally, topically, or via injection, with treatment durations ranging from 8 weeks to nearly 2 years. TXA significantly reduced melasma severity, evidenced by reductions in MASI, mMASI, MI, and hemi-MASI scores. Oral TXA showed the most substantial decrease in MASI scores, followed by injections and topical applications. However, studies exhibited high heterogeneity, particularly in combined treatments. Adverse effects included gastrointestinal discomfort, skin irritation, and menstrual irregularities.Conclusions: TXA is effective in treating melasma, either alone or combined with other treatments. Despite significant reductions in melasma severity, further research is necessary to standardize TXA administration methods and address long-term effects. The high heterogeneity observed suggests a need for more consistent treatment protocols.


Assuntos
Melanose , Ácido Tranexâmico , Humanos , Administração Cutânea , Administração Oral , Antifibrinolíticos/uso terapêutico , Antifibrinolíticos/administração & dosagem , Melanose/tratamento farmacológico , Ensaios Clínicos Controlados Aleatórios como Assunto , Índice de Gravidade de Doença , Ácido Tranexâmico/uso terapêutico , Ácido Tranexâmico/administração & dosagem , Resultado do Tratamento
18.
J Cosmet Dermatol ; 23(5): 1703-1712, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38327114

RESUMO

BACKGROUND: Melasma is a chronic dermatosis that impacts the patient's quality of life and can present considerable challenges in terms of effective treatment. OBJECTIVE: To evaluate the effectiveness, tolerability, and safety of 5% cysteamine combined with 4% nicotinamide in female subjects with melasma. METHODS: This single-center, single-arm, prospective, open-label study evaluated patients with melasma using a combination cream of 5% cysteamine and 4% nicotinamide in a progressive regimen (60 min in the first month, 120 min in the second month, and 180 min in the third month). RESULTS: Overall, 35 treated subjects exhibited reduced modified Melasma Area and Severity Index (mMASI) (p < 0.001) and decreased MelasQoL scores (p < 0.001), accompanied by improved brightness, luminosity, homogeneity, and spot intensity (p < 0.001). Photographic and colorimetric analysis revealed smaller spots and improved homogeneity. LIMITATIONS: Adherence to progressive daily treatment could not be evaluated long-term. CONCLUSION: A combination cream comprising 5% cysteamine and 4% nicotinamide was effective, tolerable, and safe for treating melasma.


Assuntos
Cisteamina , Combinação de Medicamentos , Melanose , Niacinamida , Índice de Gravidade de Doença , Adulto , Feminino , Humanos , Pessoa de Meia-Idade , Adulto Jovem , Administração Cutânea , Cisteamina/administração & dosagem , Cisteamina/efeitos adversos , Melanose/tratamento farmacológico , Melanose/diagnóstico , Niacinamida/administração & dosagem , Niacinamida/efeitos adversos , Estudos Prospectivos , Qualidade de Vida , Creme para a Pele/administração & dosagem , Creme para a Pele/efeitos adversos , Resultado do Tratamento
19.
Artigo em Inglês | MEDLINE | ID: mdl-38918942

RESUMO

INTRODUCTION: Melasma, a chronic acquired skin pigmentation disorder, is characterized by the presence of irregular-edged brown to gray-brown patches with a symmetrical distribution, primarily on sun-exposed areas such as the face. Topical hydroquinone (HQ) is the gold standard for melasma treatment but has numerous side effects. This study assesses the effectiveness of topical tranexamic acid (TA) as an alternative for melasma treatment. METHODS: In a double-blind, split-face, randomized controlled trial involving 20 subjects, the effectiveness of 3% TA versus 4% HQ cream was evaluated over 8 weeks. The modified melasma area and severity index (mMASI), melanin index, erythema index, and side effects were assessed. Subjective improvement was measured using the patient global assessment (PtGA). RESULTS: A significant decline in the mMASI score was observed at weeks 4 and 8 in both groups compared to baseline. There were no statistically significant differences in PtGA scores between the 3% TA group and the 4% HQ group. CONCLUSIONS: Topical 3% TA is as effective and safe as 4% HQ for treating melasma in the Indonesian population, with potential advantages in terms of side-effect profiles.


Assuntos
Hidroquinonas , Melanose , Ácido Tranexâmico , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Administração Cutânea , Método Duplo-Cego , Hidroquinonas/administração & dosagem , Hidroquinonas/efeitos adversos , Hidroquinonas/uso terapêutico , Melanose/tratamento farmacológico , Índice de Gravidade de Doença , Creme para a Pele/uso terapêutico , Ácido Tranexâmico/administração & dosagem , Ácido Tranexâmico/uso terapêutico , Resultado do Tratamento
20.
J Coll Physicians Surg Pak ; 34(5): 522-526, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38720210

RESUMO

OBJECTIVE: To compare the effectiveness of intense pulsed light (IPL) and intradermal tranexamic acid (TXA) in treating melasma. STUDY DESIGN: A cross-sectional analytical study. Place and Duration of the Study: Department of Dermatology, Dow International Medical College, Dow University Hospital, Karachi, Pakistan, from 15th January to 15th July 2023. METHODOLOGY: A total of 62 patients with melasma, aged 20-50 years, were divided into two groups. Group A (32 patients) received IPL (560 nm filter was used) treatment, and Group B (30 patients) received intradermal TXA. Each group underwent four treatment sessions with varying intervals. Melasma area and severity index (MASI) scores were used to compare the effects of treatment. RESULTS: After a 3-month treatment period, both groups showed reduced mMASI scores compared to baseline with a significant initial difference between Group A (8.6 ± 4.2) and Group B (5.4 ± 2.7, p <0.001). However, post-treatment, there was no significant difference in mMASI scores (Group A: 3.8 ± 2.6; Group B: 3.2 ± 2.0, p = 0.29). IPL treatment (Group A) demonstrated a significant reduction in mMASI scores (57.1 ± 19.7) compared to intradermal TXA treatment (Group B, 42.2 ± 18.8, p = 0.0034). CONCLUSION: Both IPL and intradermal TXA treatments effectively reduced melasma, with IPL exhibiting superior results. However, post-treatment outcomes converged, emphasising the need for personalised approaches considering the unique characteristics of South East Asian skin. KEY WORDS: Intense pulsed light, Melasma, Intradermal tranexamic acid.


Assuntos
Terapia de Luz Pulsada Intensa , Melanose , Ácido Tranexâmico , Humanos , Ácido Tranexâmico/administração & dosagem , Ácido Tranexâmico/uso terapêutico , Melanose/terapia , Melanose/tratamento farmacológico , Adulto , Feminino , Estudos Transversais , Pessoa de Meia-Idade , Resultado do Tratamento , Masculino , Terapia de Luz Pulsada Intensa/métodos , Injeções Intradérmicas , Paquistão , Antifibrinolíticos/administração & dosagem , Antifibrinolíticos/uso terapêutico , Adulto Jovem , Índice de Gravidade de Doença
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