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Keywords = skin-brightening

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18 pages, 1052 KiB  
Article
Impact of Kickxia elatine In Vitro-Derived Stem Cells on the Biophysical Properties of Facial Skin: A Placebo-Controlled Trial
by Anastasia Aliesa Hermosaningtyas, Anna Kroma-Szal, Justyna Gornowicz-Porowska, Maria Urbanska, Anna Budzianowska and Małgorzata Kikowska
Appl. Sci. 2025, 15(15), 8625; https://doi.org/10.3390/app15158625 - 4 Aug 2025
Viewed by 361
Abstract
The growing demand for natural and sustainable skincare products has driven interest in plant-based active ingredients, especially from in vitro cultures. This placebo-controlled study investigated the impact of a facial cream containing 2% Kickxia elatine (L.) Dumort cell suspension culture extract on various [...] Read more.
The growing demand for natural and sustainable skincare products has driven interest in plant-based active ingredients, especially from in vitro cultures. This placebo-controlled study investigated the impact of a facial cream containing 2% Kickxia elatine (L.) Dumort cell suspension culture extract on various skin biophysical parameters. The cream was applied to the cheek once daily for six weeks on 40 healthy female volunteers between the ages of 40 to 49. The evaluated skin parameters including skin hydration, transepidermal water loss (TEWL), erythema intensity (EI), melanin intensity (MI), skin surface pH, and skin structure, wrinkle depth, vascular lesions, and vascular discolouration. The results indicated that significant improvements were observed in skin hydration (from 40.36 to 63.00 AU, p < 0.001) and there was a decrease in TEWL score (14.82 to 11.76 g/h/m2, p < 0.001), while the skin surface pH was maintained (14.82 to 11.76 g/h/m2, p < 0.001). Moreover, the K. elatine cell extract significantly improved skin structure values (9.23 to 8.50, p = 0.028), reduced vascular lesions (2.72 to 1.54 mm2, p = 0.011), and lowered skin discolouration (20.98% to 14.84%, p < 0.001), indicating its moisturising, protective, brightening, and soothing properties. These findings support the potential use of K. elatine cell extract in dermocosmetic formulations targeting dry, sensitive, or ageing skin. Full article
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25 pages, 7428 KiB  
Article
Sialic Acid-Loaded Nanoliposomes with Enhanced Stability and Transdermal Delivery for Synergistic Anti-Aging, Skin Brightening, and Barrier Repair
by Fan Yang, Hua Wang, Dan Luo, Jun Deng, Yawen Hu, Zhi Liu and Wei Liu
Pharmaceutics 2025, 17(8), 956; https://doi.org/10.3390/pharmaceutics17080956 - 24 Jul 2025
Viewed by 378
Abstract
Objectives: Sialic acid (SA), a naturally occurring compound abundantly found in birds’ nests, holds immense promise for skincare applications owing to its remarkable biological properties. However, its low bioavailability, poor stability, and limited skin permeability have constrained its widespread application. Methods: [...] Read more.
Objectives: Sialic acid (SA), a naturally occurring compound abundantly found in birds’ nests, holds immense promise for skincare applications owing to its remarkable biological properties. However, its low bioavailability, poor stability, and limited skin permeability have constrained its widespread application. Methods: To overcome these challenges, SA was encapsulated within nanoliposomes (NLPs) by the high-pressure homogenization technique to develop an advanced and efficient transdermal drug delivery system. The skincare capabilities of this novel system were comprehensively evaluated across multiple experimental platforms, including in vitro cell assays, 3D skin models, in vivo zebrafish studies, and clinical human trials. Results: The SA-loaded NLPs (SA-NLPs) substantially improved the transdermal penetration and retention of SA, facilitating enhanced cellular uptake and cell proliferation. Compared to free SA, SA-NLPs demonstrated a 246.98% increase in skin retention and 1.8-fold greater cellular uptake in HDF cells. Moreover, SA-NLPs protected cells from oxidative stress-induced damage, stimulated collagen synthesis, and effectively suppressed the secretion of matrix metalloproteinases, tyrosinase activity, and melanin production. Additionally, zebrafish-based assays provided in vivo evidence of the skincare efficacy of SA-NLPs. Notably, clinical evaluations demonstrated that a 56-day application of the SA-NLPs-containing cream resulted in a 4.20% increase in L*, 7.87% decrease in b*, 8.45% decrease in TEWL, and 4.01% reduction in wrinkle length, indicating its superior brightening, barrier-repair, and anti-aging effects. Conclusions: This multi-level, systematic investigation strongly suggests that SA-NLPs represent a highly promising transdermal delivery strategy, capable of significantly enhancing the anti-aging, barrier-repair, and skin-brightening properties of SA, thus opening new avenues for its application in the fields of dermatology and cosmeceuticals. Full article
(This article belongs to the Special Issue Lipid/Polymer-Based Drug Delivery Systems)
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19 pages, 4889 KiB  
Article
The Antioxidant and Skin-Brightening Effects of a Novel Caffeic Acid Derivative, Caffeic Acid-3,4-Dihydroxyphenylpropanolester
by Kyu-lim Kim, Ju-hee Jeon, Yeonjoon Kim and Kyung-Min Lim
Antioxidants 2025, 14(7), 806; https://doi.org/10.3390/antiox14070806 - 29 Jun 2025
Viewed by 670
Abstract
Caffeic acid (CA) is a naturally occurring polyphenol antioxidant found in coffee, tea, fruits, and vegetables, known for its strong antioxidant, anti-inflammatory, and anti-aging properties. However, its cosmetic application is limited because of poor dermal absorption due to its high polarity. This study [...] Read more.
Caffeic acid (CA) is a naturally occurring polyphenol antioxidant found in coffee, tea, fruits, and vegetables, known for its strong antioxidant, anti-inflammatory, and anti-aging properties. However, its cosmetic application is limited because of poor dermal absorption due to its high polarity. This study aimed to evaluate the antioxidant and skin-brightening effects of a novel lipophilic CA derivative, CAD (caffeic acid-3,4-dihydroxyphenylpropanolester). CAD was synthesized by conjugating CA with 3,4-DHPEA, a lipophilic antioxidant derived from olive oil. In both DPPH and ABTS assays, CAD exhibited more potent antioxidant activity than CA. In B16F10 melanoma cells, CAD significantly inhibited melanin production without cytotoxicity at concentrations lower than those required for CA. Cellular assays using DCF-DA staining demonstrated that CAD effectively reduced intracellular ROS levels. Mechanistic studies revealed that CAD inhibited tyrosinase activity and downregulated the expression of TYR, TRP-1, and TRP-2. Additionally, CAD suppressed MITF phosphorylation, along with reduced phosphorylation of ERK and JNK, elucidating its anti-melanogenic mechanism. Importantly, CAD showed dose-dependent skin-brightening effects in the 3D human skin model Melanoderm™, as evidenced by increased lightness and histological evaluation. In conclusion, CAD demonstrates strong potential as a safe and effective antioxidant and skin-brightening agent for cosmetic applications. Full article
(This article belongs to the Special Issue Methodologies for Improving Antioxidant Properties and Absorption)
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19 pages, 1591 KiB  
Article
Exploring Anti-Inflammatory and Anti-Tyrosinase Potentials and Phytochemical Profiling of Cannabis sativa Stems Byproducts
by Pannita Kongtananeti, Desy Liana, Hla Myo, Anuchit Phanumartwiwath and Chitlada Areesantichai
Sci 2025, 7(2), 77; https://doi.org/10.3390/sci7020077 - 3 Jun 2025
Viewed by 823
Abstract
Cannabis sativa L. has been traditionally used for its therapeutic properties, particularly in treating various skin conditions. This study explores the in vitro anti-aging potential of five distinct parts of C. sativa L. (inflorescence, seed, leaf, stem, and root) by analyzing their bioactive [...] Read more.
Cannabis sativa L. has been traditionally used for its therapeutic properties, particularly in treating various skin conditions. This study explores the in vitro anti-aging potential of five distinct parts of C. sativa L. (inflorescence, seed, leaf, stem, and root) by analyzing their bioactive compounds and biological activities. Ultrasound-assisted extraction was employed using ethyl acetate as an extracting solvent, followed by chemical characterization via gas chromatography-mass spectrometry (GC-MS/MS) and liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOF-MS/MS) analyses. The biological assessment included antioxidant, anti-inflammatory, anti-tyrosinase activities, and cytotoxicity evaluations. The inflorescence extract demonstrated the antioxidant activity, with a half-maximal inhibitory concentration (IC50) value of 3,849.01 ± 5.25 µg/mL against DPPH radicals and 31.19 ± 0.96% inhibition of NO radicals at 1.25 mg/mL. Notably, the stem extract exhibited the highest anti-tyrosinase activity, with an IC50 value of 0.01 ± 0.00 mg/mL, and significantly inhibited 5-lipoxygenase (5-LOX) activity with an IC50 value of <0.024 µg/mL. All extracts showed no cytotoxicity on HaCaT cells at a concentration of 10 µg/mL, indicating their potential safety for dermatological applications. The stem extract was abundant in phytosterols, triterpenoids, diterpenoids, unsaturated fatty acids, and phenolic compounds, which likely contribute to its anti-inflammatory and anti-tyrosinase effects. These findings suggest that the stem, traditionally considered as waste, could be a valuable raw material for developing dermatological treatments with strong anti-inflammatory and skin-brightening effects. Full article
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16 pages, 2991 KiB  
Article
Lysine Carboxymethyl Cysteinate, as a Topical Glutathione Precursor, Protects Against Oxidative Stress and UVB Radiation-Induced Skin Damage
by Ping Gao, Xue Xiao, Xiao Cui, Hong Zhang and Xuelan Gu
Antioxidants 2025, 14(5), 606; https://doi.org/10.3390/antiox14050606 - 17 May 2025
Cited by 1 | Viewed by 990
Abstract
Lysine carboxymethyl cysteinate (LCC) is a synthetic substance obtained via lysine salification of S-carboxymethyl-cysteine. LCC has emerged as a promising glutathione (GSH) precursor. In this study, we sought to determine whether LCC could boost GSH levels and protect skin against oxidative stress. Experiments [...] Read more.
Lysine carboxymethyl cysteinate (LCC) is a synthetic substance obtained via lysine salification of S-carboxymethyl-cysteine. LCC has emerged as a promising glutathione (GSH) precursor. In this study, we sought to determine whether LCC could boost GSH levels and protect skin against oxidative stress. Experiments utilizing primary human keratinocytes and skin tissue samples revealed that LCC significantly increased endogenous GSH levels. LCC was able to pass through the stratum corneum and reach deep into the epidermis, where it enhanced the production of key metabolites involved in GSH biosynthesis. Then, the efficacy of LCC on skin protection was explored. LCC demonstrated protective effects by shielding keratinocytes from blue-light-induced oxidative stress and preventing ultraviolet B (UVB)-induced barrier disruption and pigmentation in a pigmented living skin equivalent (pLSE) model. In addition to its antioxidant properties, LCC also reduced the production of inflammatory mediators. Together, these findings underscore the multifaceted role of LCC in bolstering the natural antioxidant defenses of skin and preventing the accumulation of irreversible damage from the environment, thereby positioning it as a promising candidate for advancing skin health. Full article
(This article belongs to the Special Issue Glutathione and Health: From Development to Disease)
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12 pages, 1503 KiB  
Article
The Anti-Acne and Reduction of Hyperpigmentation Effects of Products Containing Retinol, Niacinamide, Ceramides, and Dipotassium Glycyrrhizinate in Chinese Women
by Zheng Kuai, Wenna Wang, Jiahong Yang, Xiaofeng He, Yi Yi, Hequn Wang, Yijie Zheng and Yunfei Ai
Cosmetics 2025, 12(2), 69; https://doi.org/10.3390/cosmetics12020069 - 8 Apr 2025
Cited by 2 | Viewed by 4574
Abstract
Acne vulgaris is a dermatological condition characterized by the hyperkeratinization of sebaceous follicles, which can further lead to post-inflammatory hyperpigmentation. Considering the intricate pathophysiology of acne, it is essential to develop novel topical therapies that are capable of targeting multiple underlying mechanisms of [...] Read more.
Acne vulgaris is a dermatological condition characterized by the hyperkeratinization of sebaceous follicles, which can further lead to post-inflammatory hyperpigmentation. Considering the intricate pathophysiology of acne, it is essential to develop novel topical therapies that are capable of targeting multiple underlying mechanisms of acne. The objective of this study was to study the effect of products containing retinol, niacinamide, ceramides, and dipotassium glycyrriszinate on acne-related markers. A total of 43 women with acne skin (including sensitive skin) were enrolled. To evaluate the effect of test products on acne-related indicators following 4 weeks of use, this study combined clinical assessments of skin condition (acne lesion counts), instrumental assessments (skin gloss), and photo tracking using VISIA-CR and Primos CR systems, which encompass metrics such as a*, ITA°, skin area (%) covered by sebum spots, and the presence of sebum spots. Adverse reactions were also assessed. After 4 weeks of treatment, significant reductions were observed in both the inflammatory acne lesion count and non-inflammatory acne lesion count, while there was also a significant decrease in skin redness a* and skin area (%) covered by sebum spots and a significant increase in skin brightness ITA° and gloss. No adverse events occurred during the entire testing process. In summary, the daily application of products containing retinol, niacinamide, and ceramides not only improves acne-related symptoms but also alleviates post-inflammatory hyperpigmentation caused by acne, which suggests that such products have the potential to meet the dual needs of brightening and acne care. Full article
(This article belongs to the Section Cosmetic Dermatology)
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14 pages, 1786 KiB  
Article
Enhancing Niacinamide Skin Penetration via Other Skin Brightening Agents: A Molecular Dynamics Simulation Study
by Kamolrat Somboon, Choon-Peng Chng, Changjin Huang and Shikhar Gupta
Int. J. Mol. Sci. 2025, 26(4), 1555; https://doi.org/10.3390/ijms26041555 - 12 Feb 2025
Cited by 1 | Viewed by 7961
Abstract
Niacinamide, a derivative of vitamin B3, has been shown to reduce skin pigmentation (i.e., acting as a brightening agent) and inflammatory responses such as dermatitis and acne vulgaris. However, niacinamide is a hydrophilic compound and poor partitioning to the lipid matrix in the [...] Read more.
Niacinamide, a derivative of vitamin B3, has been shown to reduce skin pigmentation (i.e., acting as a brightening agent) and inflammatory responses such as dermatitis and acne vulgaris. However, niacinamide is a hydrophilic compound and poor partitioning to the lipid matrix in the uppermost layer of the skin (the stratum corneum or SC) limits its delivery to the skin. This necessitates the use of penetration enhancers to increase its bio-availability. In this study, we used computer simulations to investigate the skin penetration of niacinamide alone and in combination with other brightening agents that are also shown to be skin penetration enhancers, namely undecylenoyl phenylalanine (Sepiwhite®), bisabolol, or sucrose dilaurate. Molecular dynamics simulations were performed to reveal molecular interactions of these brightening agents with a lipid bilayer model that mimics the SC lipid matrix. We observed minimal penetration of niacinamide into the SC lipid bilayer when applied alone or in combination with any one of the three compounds. However, when all three compounds were combined, a notable increase in penetration was observed. We showed a 32% increase in the niacinamide diffusivity in the presence of three other brightening agents, which also work as penetration enhancers for niacinamide. These findings suggest that formulations containing multiple brightening agents, which work as penetration enhancers, may improve skin penetration of niacinamide and enhance the effectiveness of the treatment. Full article
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20 pages, 1733 KiB  
Article
New Insights into Common Bean (Phaseolus vulgaris L.) Sprouts: Pilot Studies on the Formulation of a Cosmeceutical Based on Micellar Extracts Bean Sprouts
by Katarzyna Wojciechowska, Ewelina Rostkowska, Grażyna Ginalska, Łukasz Zimmer and Ewa Poleszak
Appl. Sci. 2025, 15(4), 1831; https://doi.org/10.3390/app15041831 - 11 Feb 2025
Viewed by 984
Abstract
The search for new active plant ingredients is crucial for the development of innovative cosmetic products. Micellar extracts from plant raw materials are not yet widely popular in cosmetics; however, scientific reports suggest that this form of extract is superior to standard extracts [...] Read more.
The search for new active plant ingredients is crucial for the development of innovative cosmetic products. Micellar extracts from plant raw materials are not yet widely popular in cosmetics; however, scientific reports suggest that this form of extract is superior to standard extracts due to its enhanced ability to solubilize active compounds, improve their stability, and facilitate better penetration into the skin. For this reason, our research focuses on an innovative in its applicative form micellar extract from common bean sprouts (Phaseolus vulgaris L.) with a favorable composition and promising biological activity. The aim of this study was to develop a cream formulation containing this extract and evaluate its effects using in vivo tests. Six formulations were assessed for their physicochemical properties, and a comparative analysis was conducted against a reference cream and placebo cream. For the in vivo efficacy tests, the cream, which exhibited optimal physicochemical properties and long-term stability, was selected and tested on a group of 45 volunteers. The evaluation utilized Multi-Probe Adapter Systems to compare the cream with the micellar extract, a placebo cream (cream without the extract), and a reference antiaging cream. Results demonstrated that the formulation with micellar extract exhibited superior moisturizing, antiaging, and skin-brightening properties compared to the control groups. After 12 weeks of application, the micellar extract cream improved skin hydration by 22.31%, while the placebo cream showed only a 3.52% increase, and the reference cream achieved a 13.96% improvement. The antiaging effect, assessed based on improvements in skin elasticity parameters (R2 and R5), showed increases of 13.30% and 12.33% for the micellar extract cream, compared to 8.5% and 2.32% for the placebo cream and 6.38% and 3.82% for the reference cream, respectively. In conclusion, the common bean sprouts micellar extract shows potential as an effective active ingredient for skin care products, highlighting its promising applications in the cosmetics industry. Full article
(This article belongs to the Special Issue Advanced Phytochemistry and Its Applications)
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15 pages, 1573 KiB  
Article
Clinical Efficacy of Belight3TM on Dark Spot Pigmentation in Caucasian Subjects
by Francesco Tursi, Line Pourtau, Gloria Roveda, Ileana De Ponti, David Gaudout, Benjamin Moras, Camille Pouchieu and Vincenzo Nobile
Cosmetics 2025, 12(1), 27; https://doi.org/10.3390/cosmetics12010027 - 5 Feb 2025
Viewed by 3198
Abstract
Belight3TM, a nutricosmetic formulation containing polyphenol-rich extracts, has previously been demonstrated to be safe and effective in brightening skin color and dark spots in a clinical study involving Asian volunteers. The aim of this study was to investigate the efficacy of [...] Read more.
Belight3TM, a nutricosmetic formulation containing polyphenol-rich extracts, has previously been demonstrated to be safe and effective in brightening skin color and dark spots in a clinical study involving Asian volunteers. The aim of this study was to investigate the efficacy of this formulation in lightening dark spots in a Caucasian population, which is characterized by lighter skin pigmentation and greater visibility of hyperpigmentation, as well as to determine whether the supplementation increased sensitivity to UV exposure. A randomized, double-blind, placebo-controlled clinical study was conducted on 66 male and female participants with skin phototype I to III, all exhibiting facial hyperpigmentation. The color of selected dark spots was assessed using spectrophotometry to measure the L* value of the CIELab color space and the Individual Typology Angle (ITA). L* and ITA levels of dark spots were significantly increased after 6 and 12 weeks of Belight3TM treatment (respectively by +1.2% and +2.5% for L* and by 12.1% and 22.5% for ITA), and this lightening effect was significantly higher than the placebo after 12 weeks (p < 0.05 for L*; p < 0.001 for ITA). Clinical evaluation of skin complexion evenness and dark spot visibility were also improved in subjects receiving the Belight3TM treatment, achieving a significant difference with the placebo after 12 weeks. No changes in MED or skin redness were observed during this study. This study confirmed the safety and efficacy of Belight3TM in lightening dark spots in a Caucasian population without increasing UV sensitivity. Full article
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20 pages, 1493 KiB  
Article
Green Extraction of Bioactives from Curcuma longa Using Natural Deep Eutectic Solvents: Unlocking Antioxidative, Antimicrobial, Antidiabetic, and Skin Depigmentation Potentials
by Jelena Jovanović, Marko Jović, Jelena Trifković, Katarina Smiljanić, Uroš Gašić, Maja Krstić Ristivojević and Petar Ristivojević
Plants 2025, 14(2), 163; https://doi.org/10.3390/plants14020163 - 8 Jan 2025
Cited by 4 | Viewed by 2106
Abstract
This study evaluates the efficiency of 20 Natural Deep Eutectic Solvents (NADES) formulations for extracting curcuminoids and other bioactive compounds from turmeric and emphasize their ability to preserve and enhance antioxidant, antimicrobial, antidiabetic, and skin depigmentation effects. The NADES formulations, prepared using choline [...] Read more.
This study evaluates the efficiency of 20 Natural Deep Eutectic Solvents (NADES) formulations for extracting curcuminoids and other bioactive compounds from turmeric and emphasize their ability to preserve and enhance antioxidant, antimicrobial, antidiabetic, and skin depigmentation effects. The NADES formulations, prepared using choline chloride (ChCl) combined with sugars, carboxylic acids, glycerol, amino acids, urea, polyols, and betaine, were assessed for their extraction efficiency based on the total phenolic content and curcumin concentration. Fourier transform infrared spectroscopy was employed to characterize the synthesized NADES and confirm their chemical composition. Bioactivity evaluations included antioxidant assays (ABTS and DPPH), antidiabetic tests (α-amylase inhibition), antimicrobial assays, and skin depigmentation (tyrosinase inhibition). The results demonstrated that NADES significantly enhanced the extraction efficiency and bioactive properties of turmeric extracts compared to water as a conventional green solvent. NADES 18 (ChCl/1,2-propanediol/water 1:1:1) and NADES 19 (glycerol/betaine/water 1:1:3) exhibited the highest extraction yields, with curcumin concentrations of 30.73 ± 1.96 mg/g and 31.70 ± 2.02 mg/g, respectively, outperforming water (26.91 ± 1.72 mg/g), while NADES 17 (ChCl/1,2-propanediol/water 0.5:3:0.5:5) and NADES 20 (glycerol/lysine/water 1:1:3) exhibited the most potent antioxidant activity. Furthermore, NADES 14 (ChCl/lactic acid/water 1:2:5) demonstrated the strongest tyrosinase inhibition (98.7%), supporting its potential for skin-brightening applications, including notable α-amylase inhibition exceeding 90%. This study aligns with the principles of green chemistry, as NADES are effective and sustainable solvents for natural product extraction. The presenting benefits of improved extraction efficiency and enhanced bioactivities position NADES as a promising and eco-friendly approach for developing efficient bioactive compound extraction methodologies. Full article
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11 pages, 3947 KiB  
Article
In Vivo Application of the Effects of Red-to-Near-Infrared Light Spectroscopy on Skin-Brightening and Anti-Aging Properties via LED Facial Masks
by Sunghoon Lee, Mohammad M. Afandi, Jungah Lee and Jongsu Kim
Cosmetics 2025, 12(1), 4; https://doi.org/10.3390/cosmetics12010004 - 1 Jan 2025
Viewed by 2303
Abstract
Most people want effective anti-aging and skin-brightening products. Although red-to-near-infrared (R/NIR) spectroscopy has recently been used in cosmetology, its practical use with high efficacy for anti-aging and skin brightening remains challenging. Herein, we aimed to determine the efficacy and improvement effects of a [...] Read more.
Most people want effective anti-aging and skin-brightening products. Although red-to-near-infrared (R/NIR) spectroscopy has recently been used in cosmetology, its practical use with high efficacy for anti-aging and skin brightening remains challenging. Herein, we aimed to determine the efficacy and improvement effects of a newly developed anti-aging and skin-brightening facial mask. A face study was conducted to assess efficacy and improvement effectiveness, with 21 female volunteers with oily, dry, and normal skin conditions applying the product under study (CF Magic Mask) to their face for 4-week periods. The dermatologist investigator evaluated the skin brightness, skin elasticity, eye wrinkles, dead skin cells on the scalp, dermal density, face lifting, scalp sebum, and global appearance. The mean skin-brightening and anti-aging parameters were improved (p < 0.05) after the use of the newly developed CF Magic Masks for 4-week periods. Significantly, the scalp sebum and dead skin cells on the scalp showed the greatest improvement, being reduced by about 26.71% and 21.96%, respectively. The global assessment by the volunteers showed moderate efficacy and preference, with no adverse effects or skin irritation indicated after the use of the test product. Full article
(This article belongs to the Special Issue Skin Anti-Aging Strategies)
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20 pages, 3311 KiB  
Article
Novel Tripeptides as Tyrosinase Inhibitors: In Silico and In Vitro Approaches
by Michał Dymek, Dawid Warszycki, Sabina Podlewska and Elżbieta Sikora
Int. J. Mol. Sci. 2024, 25(24), 13509; https://doi.org/10.3390/ijms252413509 - 17 Dec 2024
Cited by 2 | Viewed by 1754
Abstract
Tyrosinase is a key enzyme responsible for the formation of melanin (a natural skin pigment with ultraviolet-protection properties). However, some people experience melanin overproduction, so new, safe, and biocompatible enzyme inhibitors are sought. New tripeptide tyrosinase inhibitors were developed using molecular modeling. A [...] Read more.
Tyrosinase is a key enzyme responsible for the formation of melanin (a natural skin pigment with ultraviolet-protection properties). However, some people experience melanin overproduction, so new, safe, and biocompatible enzyme inhibitors are sought. New tripeptide tyrosinase inhibitors were developed using molecular modeling. A combinatorial library of tripeptides was prepared and docked to the mushroom tyrosinase crystal structure and investigated with molecular dynamics. Based on the results of calculations and expert knowledge, the three potentially most active peptides (CSF, CSN, CVL) were selected. Their in vitro properties were examined, and they achieved half-maximal inhibitory concentration (IC50) values of 136.04, 177.74, and 261.79 µM, respectively. These compounds attach to the binding pocket of tyrosinase mainly through hydrogen bonds and salt bridges. Molecular dynamics simulations demonstrated the stability of the peptid–tyrosinase complexes and highlighted the persistence of key interactions throughout the simulation period. The ability of these peptides to complex copper ions was also confirmed. The CSF peptide showed the highest chelating activity with copper. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay confirmed that none of the test tripeptides showed cytotoxicity toward the reconstructed human epidermis. Our results indicated that the developed tripeptides were non-toxic and effective tyrosinase inhibitors. They could be applied as raw materials in skin-brightening or anti-aging cosmetic products. Full article
(This article belongs to the Section Molecular Biophysics)
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17 pages, 5874 KiB  
Article
Development of Transethosomes Loaded with Fruit Extract from Carissa carandas L. as a Brightening and Anti-Aging Cosmeceutical Ingredient
by Sitthiphong Soradech, Worawan Tiatragoon, Phongsapak Phanphothong, Kanyarat Ouamkan, Pattarawadee Kengkwasingh, Supatjaree Ruengsomwong, Somkamol Intawong and Thanchanok Muangman
Cosmetics 2024, 11(6), 199; https://doi.org/10.3390/cosmetics11060199 - 21 Nov 2024
Cited by 2 | Viewed by 2244
Abstract
The ethanolic extract of Carissa carandas L. (ECE) inhibited the enzyme tyrosinase, enhanced the proliferation of normal human dermal fibroblast cells, and increased the formation of collagen type I, indicating possible anti-aging and whitening effects. However, the stratum corneum acts as a rate-limiting [...] Read more.
The ethanolic extract of Carissa carandas L. (ECE) inhibited the enzyme tyrosinase, enhanced the proliferation of normal human dermal fibroblast cells, and increased the formation of collagen type I, indicating possible anti-aging and whitening effects. However, the stratum corneum acts as a rate-limiting stage in the absorption of herbal extracts through the skin, resulting in limited absorption of ECE via the skin, which affects the efficacy of ECE. The purpose of this study was to develop ECE encapsulated in transethosomes for improved skin penetration as a novel brightening and anti-aging cosmeceutical ingredient. Transethosomes were successfully developed using the sonication technique, with a suitable formulation including 1.00% (w/w) phosphatidylcholine, 0.10% (w/w) polysorbate 80 and 28.55% (v/v) ethanol. The physicochemical properties, encapsulation efficacy, in vitro skin permeation and toxicity of ECE-loaded transethosomes were also investigated. The result showed that the percentages of encapsulation of ECE loaded in transethosomes increased slightly with higher concentrations of the ECE. When compared to the liquid extract, the ECE loaded in transethosomes significantly increased (p < 0.05) skin penetration. Furthermore, ECE loaded with transethosomes showed low cytotoxicity in normal human dermal fibroblast cells and caused no skin irritation when evaluated on reconstructed human epidermal skin. Given these abilities, it is evident that transethosomes containing ECE are highly effective anti-aging and skin-whitening agents, making them a promising new cosmeceutical ingredient. Full article
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30 pages, 6947 KiB  
Article
Epigallocatechin Gallate Enzymatic Alpha Glucosylation Potentiates Its Skin-Lightening Activity—Involvement of Skin Microbiota
by Cloé Boira, Emilie Chapuis, Laura Lapierre, Daniel Auriol, Cyrille Jarrin, Patrick Robe, Jean Tiguemounine, Amandine Scandolera and Romain Reynaud
Molecules 2024, 29(22), 5391; https://doi.org/10.3390/molecules29225391 - 15 Nov 2024
Viewed by 2205
Abstract
(1) Background: Ultraviolet radiation takes part in photoaging and pigmentation disorders on skin. Epigallocatechin gallate (EGCG) is a well-known brightening and photoprotective compound but it faces limitations in terms of stability and solubility. (2) Methods: A more stable and water-soluble glucoside called EGCG-G1 [...] Read more.
(1) Background: Ultraviolet radiation takes part in photoaging and pigmentation disorders on skin. Epigallocatechin gallate (EGCG) is a well-known brightening and photoprotective compound but it faces limitations in terms of stability and solubility. (2) Methods: A more stable and water-soluble glucoside called EGCG-G1 was obtained by enzymatic glucosylation of EGCG. In vitro and ex vivo experiments evaluated EGCG-G1 skin penetration, antioxidant activity, and antimelanogenic properties compared to EGCG. This gene expression study characterized the pathways impacted by EGCG-G1. Four clinical studies covering phototypes I to V, at various ages, and different skin areas, using several tools, were conducted to assess the effect of EGCG-G1 on skin hyperpigmentation and tone. The impact of glucoside on skin microbiota, especially Lactobacillus sp., was assessed through in vitro and in vivo investigations. (3) Results: EGCG-G1 better penetrated the epidermis than EGCG due to a possible interaction with GLUT1. EGCG-G1 presented similar antioxidant activity to that of EGCG and decreased melanogenesis through the inhibition of 13 genes, including MITF. The skin Lactobacillus population increased with EGCG-G1, which promoted bacterial growth in vitro as prebiotic, and induced the release of a microbial brightening metabolite. Clinical trials demonstrated EGCG-G1 to decrease hyperpigmented spots and increase skin brightness and homogeneity in a large panel of phototypes, outperforming EGCG and vitamin C. (4) Conclusions: Glucosylation of EGCG maintained its photoprotective antioxidant properties and enhanced penetration across the epidermis. EGCG-G1 demonstrated brightening properties on all skin types by down-regulation of melanogenesis pathways and indirectly by skin microbiota stimulation. Full article
(This article belongs to the Section Food Chemistry)
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15 pages, 1995 KiB  
Article
In Vitro Bioactivity of Australian Finger Lime Cultivars as an Initial Evaluation of Their Nutraceutical Potential
by Joel B. Johnson, Parbat Raj Thani, Si-Yuan Chen, Janice S. Mani, Michael E. Netzel and Mani Naiker
Nutraceuticals 2024, 4(4), 596-610; https://doi.org/10.3390/nutraceuticals4040032 - 24 Oct 2024
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Abstract
There is increasing interest in Australian finger lime (Citrus australasica) due to its nutritional and bioactive potential. In this study, polar extracts from five finger lime cultivars were investigated for their potential bioactivity using a range of assays: antioxidant capacity (total [...] Read more.
There is increasing interest in Australian finger lime (Citrus australasica) due to its nutritional and bioactive potential. In this study, polar extracts from five finger lime cultivars were investigated for their potential bioactivity using a range of assays: antioxidant capacity (total phenolic content (TPC), ferric reducing antioxidant power (FRAP), and cupric reducing antioxidant capacity (CUPRAC)), total monomeric anthocyanin content (TMAC), anti-diabetic activity (α-glucosidase and α-amylase inhibition), anti-Alzheimer activity (acetylcholinesterase inhibition), Skin-whitening activity skin-brightening activity (tyrosinase inhibition), and anti-inflammatory activity (COX-2 inhibition). Commercial Tahitian lime was used as a “control” (comparison). The TPC ranged from 328 to 779 mg GAE/100 g dry weight (DW) in the pulp (compared to 1043 mg GAE/100 g for Tahitian lime) and from 755 to 1048 mg GAE/100 g in the peel (1704 mg GAE/100 g for Tahitian lime). A similar range of variation was seen for FRAP, ranging from 114 to 436 mg TE/100 g DW in the pulp (422 mg TE/100 g for Tahitian lime) and 259 to 495 mg TE/100 g DW in the peel (491 mg TE/100 g for Tahitian lime). Similarly, the TFC was generally lower in finger lime pulp (100–392 mg QE/100 g DW) compared to Tahitian lime (312 mg QE/100 g). The polar extracts did not show any significant inhibition of α-glucosidase, α-amylase, tyrosinase, or COX-2. One finger lime variety showed moderate (>50%) inhibition of acetylcholinesterase (AChE) at the highest concentration screened (~1500 mg/L), as did Tahitian lime. Additionally, in silico docking against acetylcholinesterase suggested that some of the polyphenols present, including catechin, quercetin-3-glucoside, and cyanidin-3-glucoside, could potentially dock to AChE and inhibit it. This is the first time the species has been investigated for many of these bioactive properties, and also the first time in silico docking has been performed to explore which potential compounds from this species could provide its bioactivity. Although little bioactivity was generally found across the applied bioassays, these findings nevertheless provide important basic data for future research and any claims about the potential health benefits of Australian finger lime. Full article
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