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1.
Molecules ; 29(17)2024 Aug 30.
Article in English | MEDLINE | ID: mdl-39274964

ABSTRACT

The present investigation was performed to figure out the chemical constituents and biological potential of polar extracts (AcOEt and BuOH) from Achillea ligustica, a medicinal species of the Asteraceae family. Liquid chromatography quadrupole time-of-flight mass spectrometry (LC-Q-TOF-MS) was utilized to conduct a preliminary analysis of the phytochemical profiles of the AcOEt and BuOH extracts. The analysis revealed the existence of twenty compounds in the AcOEt extract and twenty-two in the BuOH extract, classified into various types of secondary metabolites. Subsequently, the exudate from the plant yielded five flavonoids, including two 6-methoxyflavonols identified for the first time in this genus. The isolation of compounds from AcOEt and BuOH extracts was achieved through the combined use of column chromatography (silica gel and Sephadex LH-20) and preparative TLC chromatography. The structures have been elucidated using 1D and 2D NMR spectroscopy, alongside comparisons with research data. Our study measured the total phenolic and flavonoid contents and carried out a comprehensive range of antioxidant tests using DPPH, GOR, CUPRAC, reducing power, and O-phenanthroline assays. Both extracts exhibited considerable antioxidant potential and contained high levels of phenolic and flavonoid compounds. The photoprotective effect of the AcOEt and BuOH extracts was evaluated in vitro by measuring the sun protection factor. Both extracts exhibited a high capacity for UV radiation absorption. Consequently, this plant presents an intriguing prospect for future research focused on incorporating it into photoprotective cosmetic products and pharmaceutical formulations.


Subject(s)
Achillea , Antioxidants , Flavonoids , Phenols , Plant Extracts , Achillea/chemistry , Antioxidants/chemistry , Antioxidants/pharmacology , Plant Extracts/chemistry , Plant Extracts/pharmacology , Phenols/chemistry , Phenols/analysis , Phenols/pharmacology , Flavonoids/chemistry , Flavonoids/pharmacology , Flavonoids/analysis , Phytochemicals/chemistry , Phytochemicals/pharmacology , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology
2.
Sci Prog ; 107(3): 368504241272454, 2024.
Article in English | MEDLINE | ID: mdl-39119690

ABSTRACT

UV filters in current sunscreen formulations can have negative effects on human health, such as endocrine disruption and allergic reactions, as well as on the environment, including bioaccumulation and coral health toxicity. As a result, there is a need to find alternative compounds that serve as safer and more ecofriendly active ingredients. This study successfully isolated actinomycetes from the octocoral Eunicea fusca and assessed their potential as producers of photoprotective compounds. The use of bio-based chemical agents, particularly natural products, has been a highly effective strategy for discovering bioactive compounds, especially in marine invertebrates and their associated microbiota. Eighteen bacterial isolates were obtained and subsequently employed to prepare raw methanolic extracts from seven-day submerged cultures in Zobell marine broth. The resulting extracts were screened for 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity and characterized by total phenolic and flavonoid content measurements. After screening, the Gordonia hongkongensis EUFUS-Z928-derived raw extract exhibited the best antioxidant profile, i.e. DPPH and ABTS radical scavenging of 4.93 and 6.00 µmol Trolox per gram of extract, respectively, and selected for further photoprotection-related analysis. Thus, this extract demonstrated a UV-absorbing capacity of 46.33% of the in vitro sun protection factor calculated for 30 µg/mL oxybenzone but did not exhibit any cytotoxicity on human dermal fibroblasts (HDFa cell line) at concentrations up to 500 µg/mL. The liquid chromatography-mass spectrometry chemical characterization of this extract showed compounds with structural features associated with free radical scavenging and UV absorption (i.e. photoprotection-related activities). These findings highlighted the potential of the microbiota associated with E. fusca and confirmed the feasibility of exploiting its metabolites for photoprotection-related purposes.


Subject(s)
Anthozoa , Sunscreening Agents , Sunscreening Agents/pharmacology , Sunscreening Agents/chemistry , Anthozoa/microbiology , Animals , Actinobacteria/metabolism , Actinobacteria/chemistry , Humans , Ultraviolet Rays , Antioxidants/pharmacology , Antioxidants/chemistry , Phenols/chemistry , Phenols/pharmacology , Flavonoids/chemistry , Flavonoids/pharmacology
3.
Int J Mol Sci ; 25(15)2024 Aug 03.
Article in English | MEDLINE | ID: mdl-39126045

ABSTRACT

Isoamyl 4-methoxycinnamate (IMC) is widely used in various fields because of its exceptional UV-filter properties. However, due to its cytotoxicity and anti-microbial degradability, the potential eco-environmental toxicity of IMC has become a focus of attention. In this study, we propose a host-guest supramolecule approach to enhance the functionality of IMC, resulting in a more environmentally friendly and high-performance materials. Sulfobutyl-ß-cyclodextrin sodium salt (SBE-ß-CD) was used as the host molecule. IMC-SBE-ß-CD supramolecular substances were prepared through the "saturated solution method", and their properties and biosecurity were evaluated. Meanwhile, we conducted the AOS tree evaluation system that surpasses existing evaluation approaches based on apoptosis, oxidative stress system, and signaling pathways to investigate the toxicological mechanisms of IMC-SBE-ß-CD within human hepatoma SMMC-7721 cells as model organisms. The AOS tree evaluation system aims to offer the comprehensive analysis of the cytotoxic effects of IMC-SBE-ß-CD. Our findings showed that IMC-SBE-ß-CD had an encapsulation rate of 84.45% and optimal stability at 30 °C. Further, IMC-SBE-ß-CD promoted cell growth and reproduction without compromising the integrity of mitochondria and nucleus or disrupting oxidative stress and apoptosis-related pathways. Compared to IMC, IMC-SBE-ß-CD is biologically safe and has improved water solubility with the UV absorption property maintained. Our study provides the foundation for the encapsulation of hydrophobic, low-toxicity organic compounds using cyclodextrins and offers valuable insights for future research in this field.


Subject(s)
Ultraviolet Rays , beta-Cyclodextrins , Humans , beta-Cyclodextrins/chemistry , beta-Cyclodextrins/pharmacology , Cell Line, Tumor , Apoptosis/drug effects , Cinnamates/chemistry , Cinnamates/pharmacology , Oxidative Stress/drug effects , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology
4.
Chem Res Toxicol ; 37(8): 1344-1355, 2024 Aug 19.
Article in English | MEDLINE | ID: mdl-39095321

ABSTRACT

This study introduces a novel cheminformatic read-across approach designed to identify potential environmental obesogens, substances capable of disrupting metabolism and inducing obesity by mainly influencing nuclear hormone receptors (NRs). Leveraging real-valued two-dimensional features derived from chemical fingerprints of 8435 Tox21 compounds, cluster analysis and subsequent statistical testing revealed 385 clusters enriched with compounds associated with specific NR targets. Notably, one cluster exhibited selective enrichment in peroxisome proliferator-activated receptor γ (PPARγ) agonist activity, prominently featuring methoxy cinnamate ultraviolet (UV) filters and obesogen-related compounds. Experimental validation confirmed that 2-ethoxyethyl 4-methoxycinnamate, an organic UV filter cinoxate, could selectively bind to PPARγ (Ki = 18.0 µM), eliciting an obesogenic phenotype in human bone marrow-derived mesenchymal stem cells during adipogenic differentiation. Molecular docking and further experiments identified cinoxate as a potent PPARγ full agonist, demonstrating a preference for coactivator SRC3 recruitment. Moreover, cinoxate upregulated transcription levels of genes encoding lipid metabolic enzymes in normal human epidermal keratinocytes as primary cells exposed during clinical usage. This study provides compelling evidence for the efficacy of cheminformatic read-across analysis in prioritizing potential obesogens, showcasing its utility in unveiling cinoxate as an obesogenic PPARγ agonist.


Subject(s)
Molecular Docking Simulation , PPAR gamma , PPAR gamma/agonists , PPAR gamma/metabolism , Humans , Obesity/drug therapy , Obesity/metabolism , Cinnamates/pharmacology , Cinnamates/chemistry , Molecular Structure , Keratinocytes/drug effects , Keratinocytes/metabolism , Mesenchymal Stem Cells/drug effects , Mesenchymal Stem Cells/metabolism , Sunscreening Agents/pharmacology , Sunscreening Agents/chemistry , Ultraviolet Rays
5.
Pharm Res ; 41(7): 1475-1491, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38992234

ABSTRACT

OBJECTIVE: Zinc Oxide nanoparticles (ZnO NPs) are used widely in nowadays personal care products, especially sunscreens, as a protector against UV irradiation. Yet, they have some reports of potential toxicity. Silica is widely used to cage ZnO NPs to reduce their potential toxicity. Vitamin C derivative, Magnesium Ascorpyl Phosphate (MAP), is a potent antioxidant that can efficiently protect human skin from harmful impacts of UV irradiation and oxidative stress. The combination of silica coated ZnO NPs and MAP nanovesicles could have potential synergistic protective effect against skin photodamage. METHODS: Silica coated ZnO NPs and MAP nanovesicles (ethosomes and niosomes) were synthesized, formulated, and evaluated as topical gels. These gel formulations were evaluated in mice for their photoprotective effect against UV irradiation through histopathology and immuno-histochemistry study. Split-face clinical study was conducted to compare the effect of application of silica coated ZnO NPs either alone or combined with MAP nanovesicles. Their photoprotective action was evaluated, using Antera 3D® camera, for melanin level, roughness index and wrinkles depth. RESULTS: Silica coated ZnO NPs when combined with MAP nanovesicles protected mice skin from UV irradiation and decreased the expression of the proinflammatory cytokines, NF-κB. Clinically, silica coated ZnO NPs, alone or combined with MAP nanovesicles, could have significant effect to decrease melanin level, roughness index and wrinkles depth with higher effect for the combination. CONCLUSION: A composite of silica coated ZnO NPs and MAP nanovesicles could be a promising cosmetic formulation for skin protection against photodamage signs such as hyperpigmentation, roughness, and wrinkles.


Subject(s)
Ascorbic Acid , Silicon Dioxide , Skin , Sunscreening Agents , Ultraviolet Rays , Zinc Oxide , Zinc Oxide/chemistry , Zinc Oxide/pharmacology , Zinc Oxide/administration & dosage , Animals , Silicon Dioxide/chemistry , Ultraviolet Rays/adverse effects , Mice , Humans , Ascorbic Acid/chemistry , Ascorbic Acid/pharmacology , Ascorbic Acid/administration & dosage , Ascorbic Acid/analogs & derivatives , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Sunscreening Agents/administration & dosage , Skin/drug effects , Skin/radiation effects , Skin/metabolism , Female , Antioxidants/pharmacology , Antioxidants/chemistry , Antioxidants/administration & dosage , Nanoparticles/chemistry , Skin Aging/drug effects , Skin Aging/radiation effects , Male , Adult , Middle Aged
6.
Pharm Res ; 41(8): 1613-1620, 2024 Aug.
Article in English | MEDLINE | ID: mdl-39044045

ABSTRACT

PURPOSE: The aim of this study was to examine the ability of sunscreen active ingredients to inhibit in vitro drug metabolism via cytochrome P450 (CYP) enzymes and drug uptake transporters. METHODS: Metabolism assays with human liver microsomes were conducted for CYP2C9, CYP2D6 and CYP3A4 using probe substrates warfarin, bufuralol and midazolam, respectively. Uptake transporter assays with transfected cell lines were conducted for OAT3, OCT2 and OATP1B1 with probe substrates estrone-3-sulfate, metformin and rosuvastatin, respectively. Six sunscreen active ingredients, avobenzone, enzacamene, oxybenzone, octinoxate, trolamine, and homosalate, were evaluated up to their aqueous solubility limits in the assays. RESULTS: None of the sunscreen active ingredients inhibited CYP2D6 or CYP3A4 activities in the microsomes at concentration ranges up to tenfold higher than their known clinical total plasma levels. Only enzacamene, oxybenzone and trolamine were found to be inhibitory to CYP2C9 activity with IC50 values of 14.76, 22.46 and 154.7 µM, respectively. Avobenzone, enzacamene, homosalate and octinoxate were not inhibitory to the uptake transporters at the evaluated concentrations. Oxybenzone was inhibitory to OAT3 and OCT2 with IC50 values of 39.93 and 42.77 µM, respectively. Trolamine also inhibited uptake in OAT3 and OCT2 transfected cells with IC50 values of 448.1 and 1376 µM, respectively. CONCLUSIONS: Although enzacamene, oxybenzone and trolamine inhibited CYP2C9 and the renal transporters OAT3 and OCT2 in vitro, their IC50 values exceeded total plasma levels found in clinical studies. Therefore, it is unlikely that these sunscreen active ingredients in sunscreen products will inhibit the metabolism or transport of co-administered drugs in consumers.


Subject(s)
Drug Interactions , Microsomes, Liver , Sunscreening Agents , Humans , Sunscreening Agents/pharmacokinetics , Sunscreening Agents/metabolism , Sunscreening Agents/pharmacology , Microsomes, Liver/metabolism , HEK293 Cells , Cytochrome P-450 CYP2D6/metabolism , Cytochrome P-450 Enzyme Inhibitors/pharmacology , Cytochrome P-450 CYP3A/metabolism
7.
Photochem Photobiol ; 100(5): 1527-1530, 2024.
Article in English | MEDLINE | ID: mdl-38828502

ABSTRACT

The field of sun protection is quickly changing and the research article by Douki et al., published in the current issue of Photochemistry and Photobiology, reported key experimental data that will certainly help the development of better sun care products. Mutagenic photoproducts (CPDs, cyclobutane pyrimidine dimers and 6-4PPs, pyrimidine-6-4-pyrimidone photoproducts) were formed in the reconstructed human epidermis (RHE) by UVB (312 nm) irradiation, and their concentrations were detected by HPLC-MS/MS as a function of time after the UVB treatment. RHE had been previously exposed or not (control) to blue light (427 nm). Both CPDs and 6-4PPs were shown to last longer in blue-light irradiated RHE, proving the inhibition of the DNA repair by blue light exposure. This is a highly relevant information because sunscreens allow people to enjoy longer periods under the sun and consequently, to endure very high doses of blue light. The work also reported results obtained with RHEs previously treated with a sunscreen formulation containing a broadband filter that offers blue-light protection. Interestingly, authors observed that the DNA repair was not significantly inhibited in RHE previously treated with the sunscreen offering broadband protection. Readers will find a scientifically sound proof of the importance of blue-light protection in sun care products.


Subject(s)
DNA Repair , Sunscreening Agents , Humans , DNA Repair/drug effects , Sunscreening Agents/pharmacology , Sunscreening Agents/chemistry , Skin/radiation effects , Skin/drug effects , Light , Ultraviolet Rays/adverse effects , Pyrimidine Dimers
8.
J Biophotonics ; 17(8): e202400107, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38937980

ABSTRACT

The skin surface lipids (SSLs) film, composed of sebum and keratinocyte membrane lipids, is crucial to the barrier function of the stratum corneum (SC). The first part of this study investigated the impact of solar radiation on the SC based on a novel hydration and dehydration approach using Raman spectroscopy. The SSLs were found to absorb solar light, and thus participate to the protection of the skin surface. However, the protective function of the SSLs may be limited and is dependent to the heterogenous distribution of SSLs over the body surface. To ensure comprehensive protection, synergistic measures such as the application of solar filters are necessary. In this second part of the study, we have evaluated the limits of the protection capacity of SSLs and explored the protective action of a solar filters on both SSLs composition and the water hydration and dehydration kinetics in the SC.


Subject(s)
Water , Water/metabolism , Humans , Sunlight , Epidermis/radiation effects , Epidermis/metabolism , Spectrum Analysis, Raman , Skin/radiation effects , Skin/metabolism , Sunscreening Agents/pharmacology
9.
Molecules ; 29(12)2024 Jun 12.
Article in English | MEDLINE | ID: mdl-38930851

ABSTRACT

Bletilla striata is the dried tuber of B. striata (Thund.) Reichb.f., which has antibacterial, anti-inflammatory, anti-tumor, antioxidant and wound healing effects. Traditionally, it has been used for hemostasis therapy, as well as to treat sores, swelling and chapped skin. In this study, we used the ultraviolet (UV) absorbance rate of B. striata extracts as the index, and the extraction was varied with respect to the solid-liquid ratio, ethanol concentration, ultrasonic time and temperature in order to optimize the extraction process for its sunscreen components. The main compounds in the sunscreen ingredients of Baiji (B. striata) were analyzed using ultra-high-performance liquid chromatography combined with quadrupole time-of-flight tandem mass spectrometry. The sunscreen properties were subsequently evaluated in vitro using the 3M tape method. The results show that the optimal extraction conditions for the sunscreen components of B. striata were a solid-liquid ratio of 1:40 (g/mL), an ethanol concentration of 50%, an ultrasonic time of 50 min and a temperature of 60 °C. A power of 100 W and an ultrasonic frequency of 40 Hz were used throughout the experiments. Under these optimized conditions, the UV absorption rate of the isolated sunscreen components in the UVB region reached 84.38%, and the RSD was 0.11%. Eighteen compounds were identified, including eleven 2-isobutyl malic acid glucose oxybenzyl esters, four phenanthrenes, two bibenzyl and one α-isobutylmalic acid. An evaluation of the sunscreen properties showed that the average UVB absorption values for the sunscreen samples from different batches of B. striata ranged from 0.727 to 1.201. The sunscreen ingredients of the extracts from B. striata had a good UV absorption capacity in the UVB area, and they were effective in their sunscreen effects under medium-intensity sunlight. Therefore, this study will be an experimental reference for the extraction of sunscreen ingredients from the B. striata plant, and it provides evidence for the future development of B. striata as a candidate cosmetic raw material with UVB protection properties.


Subject(s)
Orchidaceae , Plant Extracts , Sunscreening Agents , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Sunscreening Agents/isolation & purification , Orchidaceae/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/isolation & purification , Chromatography, High Pressure Liquid , Ultrasonic Waves , Tandem Mass Spectrometry , Humans , Ultraviolet Rays
10.
Molecules ; 29(12)2024 Jun 11.
Article in English | MEDLINE | ID: mdl-38930846

ABSTRACT

Grape marc is a by-product resulting from the winemaking industry that still contains beneficial compounds that can be valorized. Thus, we report here the possibility of using polyphenolic extracts of grape marc origin to obtain sun protection creams. The extractions were performed in ethanol and acetone solutions using pomace from different grape varieties (Merlot, Bläufrankisch, Feteasca Neagra, Isabella) as a raw material. The obtained extracts were analyzed in order to determine the total phenolic content, the antioxidant activity, and the sun protection factor (SPF) via Mansur spectrophotometric assay. The best results were achieved using 70% ethanol in water as a solvent. The extracts with the highest potential photoprotective effects are from the Merlot variety (SPFspectrophotometric = 7.83 ± 0.76). The sunscreens were prepared using the 70% ethanolic extract of the Merlot variety evaporated to dryness, redissolved in either distilled water or ethanol. The SPF estimated in vitro via the COLIPA method showed values of 14.07 ± 1.50 and 11.46 ± 1.32 for the aqueous and ethanolic extracts, respectively, when working with a cream to polyphenolic extract a ratio of 1/1 (w/w). At the same time, the use of aqueous polyphenolic extracts ensures the better stability of creams compared with the ethanolic ones.


Subject(s)
Antioxidants , Plant Extracts , Sunscreening Agents , Vitis , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Vitis/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Cosmetics/chemistry , Polyphenols/chemistry , Polyphenols/pharmacology , Wine/analysis , Biological Products/chemistry , Biological Products/pharmacology , Sun Protection Factor
11.
ACS Appl Mater Interfaces ; 16(25): 32649-32661, 2024 Jun 26.
Article in English | MEDLINE | ID: mdl-38865694

ABSTRACT

Ultraviolet (UV) filters are the core ingredients in sunscreens and protect against UV-induced skin damage. Nevertheless, their safety and effectiveness have been questioned in terms of their poor photostability, skin penetration, and UV-induced generation of deleterious reactive oxygen species (ROS). Herein, an organic UV filter self-framed microparticle sunblock was exploited, in which quercetin (QC) and hexachlorocyclotriphosphazene (HCCP) were self-constructed into microparticles (HCCP-QC MPs) by facile precipitation polymerization without any carriers. HCCP-QC MPs could not only significantly extend the UV shielding range to the whole UV region but also remarkably reduce UV-induced ROS while avoiding direct skin contact and the resulting epidermal penetration of small-molecule QC. Meanwhile, HCCP-QC MPs possess a high QC-loading ability (697 mg g-1) by QC itself as the microparticles' building blocks. In addition, there is no leakage issue with small molecules due to its covalently cross-linked structure. In vitro and vivo experiments also demonstrated that the HCCP-QC MPs have excellent UV protection properties and effective ROS scavenging ability without toxicity. In summary, effective UV-shielding and ROS scavenging ability coupled with excellent biocompatibility and nonpenetration of small molecules make it a broad prospect in skin protection.


Subject(s)
Free Radical Scavengers , Organophosphorus Compounds , Polymers , Reactive Oxygen Species , Skin , Sunscreening Agents , Ultraviolet Rays , Organophosphorus Compounds/chemistry , Organophosphorus Compounds/pharmacology , Polymers/chemistry , Polymers/pharmacology , Skin/drug effects , Skin/radiation effects , Skin/metabolism , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacology , Reactive Oxygen Species/metabolism , Animals , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Humans , Mice , Quercetin/chemistry , Quercetin/pharmacology
12.
J Drugs Dermatol ; 23(5): 366-375, 2024 May 01.
Article in English | MEDLINE | ID: mdl-38709706

ABSTRACT

OBJECTIVE:   This study aimed to investigate the ultraviolet (UV) protection/repair benefits of a patented Amino Acid Complex (AAComplex). METHODS: I) AAComplex was incubated with dermal fibroblasts, with/without UVA, and collagen I was measured with a GlasBoxPlus device. II) A lotion, with/without AAComplex (1%) was applied topically to skin explants, following UVA irradiation, and quantified for health-related biomarkers (TNFalpha, histamine, and MMP-1). III) A broad spectrum sunscreen with SPF 46 and a skincare serum containing AAComplex (2%) were assessed using epidermal equivalents, in the presence of UV irradiation, for effects on IL-1alpha, thymine dimers, Ki-67, filaggrin and Nrf2. RESULTS: I) Collagen I synthesis in dermal fibroblasts was significantly decreased after UVA compared to without UV. The presence of AAComplex prevented this decrease. II) UVA irradiation of skin explants increased histamine, TNFα, and MMP-1. Hydrocortisone aceponate cream significantly decreases all 3 biomarkers. AAComplex contained lotion also significantly decreased all 3 biomarkers, the no AAComplex control lotion only reduced histamine. III) With the regimen of sunscreen + AAComplex contained skincare serum, the significant reduction in IL-1alpha was observed along with a complete recovery of Ki-67 and stimulation of filaggrin and Nrf2T. No thymine dimer positive cell was observed indicating the most positive skin impact from the regiment.  Conclusion: This research using different human skin models demonstrated that AAComplex can provide protection and damage repair caused by UV, at the ingredient level also when formulated in a serum or lotion formula. Skin may be best protected from UV damage when the regimen is used.   J Drugs Dermatol. 2024;23(5):366-375. doi:10.36849/JDD.7916.


Subject(s)
Fibroblasts , Filaggrin Proteins , Matrix Metalloproteinase 1 , NF-E2-Related Factor 2 , Tumor Necrosis Factor-alpha , Ultraviolet Rays , Humans , Ultraviolet Rays/adverse effects , Fibroblasts/drug effects , Fibroblasts/radiation effects , Fibroblasts/metabolism , Matrix Metalloproteinase 1/metabolism , Tumor Necrosis Factor-alpha/metabolism , Skin/radiation effects , Skin/drug effects , Skin/metabolism , Sunscreening Agents/administration & dosage , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Amino Acids/administration & dosage , Amino Acids/pharmacology , Amino Acids/chemistry , Interleukin-1alpha/metabolism , Histamine/blood , Skin Cream/administration & dosage , Biomarkers/metabolism , Collagen Type I , Intermediate Filament Proteins/metabolism , Ki-67 Antigen/metabolism , Pyrimidine Dimers , Cells, Cultured
13.
Plant Physiol Biochem ; 212: 108744, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38781638

ABSTRACT

The most recent evaluation of the impacts of UV-B radiation and depletion of stratospheric ozone points out the need for effective photoprotection strategies for both biological and nonbiological components. To mitigate the disruptive consequences of artificial sunscreens, photoprotective compounds synthesized from gram-negative, oxygenic, and photoautotrophic prokaryote, cyanobacteria have been studied. In a quest to counteract the harmful UV radiation, cyanobacterial species biosynthesize photoprotective metabolites named as mycosporine-like amino acids (MAAs). The investigation of MAAs as potential substitutes for commercial sunscreen compounds is motivated by their inherent characteristics, such as antioxidative properties, water solubility, low molecular weight, and high molar extinction coefficients. These attributes contribute to the stability of MAAs and make them promising candidates for natural alternatives in sunscreen formulations. They are effective at reducing direct damage caused by UV radiation and do not lead to the production of reactive oxygen radicals. In order to better understand the role, ecology, and its application at a commercial scale, tools like genome mining, heterologous expression, and synthetic biology have been explored in this review to develop next-generation sunscreens. Utilizing tactical concepts of bio-nanoconjugate formation for the development of an efficient MAA-nanoparticle conjugate structure would not only give the sunscreen complex stability but would also serve as a promising tool for the production of analogues. This review would provide insight on efforts to produce MAAs by diversifying the biosynthetic pathways, modulating the precursors and stress conditions, and comprehending the gene cluster arrangement for MAA biosynthesis and its application in developing effective sunscreen.


Subject(s)
Amino Acids , Cyanobacteria , Sunscreening Agents , Ultraviolet Rays , Sunscreening Agents/metabolism , Sunscreening Agents/pharmacology , Cyanobacteria/metabolism , Amino Acids/metabolism
14.
Int J Biol Macromol ; 267(Pt 2): 131462, 2024 May.
Article in English | MEDLINE | ID: mdl-38614163

ABSTRACT

The rapid development of the industry has led to the destruction of the earth's ozone layer, resulting in an increasingly serious problem of excessive ultraviolet radiation. Exploring effective measures to address these problems has become a hot topic. Lignin shows promise in the design and preparation of anti-ultraviolet products due to its inherent properties. However, it is important to investigate way to enhance the reactivity of lignin and determine its application form in related products. In this study, phenolic reactions with tea polyphenols were conducted through acid-catalyzed conversion, utilizing organic solvent lignin as the primary material. The phenolic hydroxyl content of the original lignin increased significantly by 218.8 %, resulting in notable improvements in UV resistance and oxidation resistance for phenolic lignin. Additionally, micro-nanocapsule emulsions were formed using phenolic lignin particles as surfactants through ultrasonic cavitation with small-molecule sunscreens. A bio-based sunscreen was prepared with phenolated lignin micro-nanocapsules as the active ingredient, achieving an SPF 100.2 and demonstrating excellent stability. The sunscreen also exhibited strong antioxidant properties and impermeability, ensuring user safety. This research offers a current solution for improving the application of lignin in sunscreens while also broadening the potential uses of plant-based materials in advanced functional products.


Subject(s)
Lignin , Oxidation-Reduction , Polyphenols , Sunscreening Agents , Tea , Ultraviolet Rays , Lignin/chemistry , Polyphenols/chemistry , Catalysis , Tea/chemistry , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Acids/chemistry
15.
Photochem Photobiol Sci ; 23(5): 853-869, 2024 May.
Article in English | MEDLINE | ID: mdl-38613600

ABSTRACT

Synthetic sunscreen offers protection against excessive exposure to ultraviolet (UV) radiation from the sun, and protects the skin from possible damage. However, they have low efficacy against the formation of reactive oxygen species (ROS), which are highly reactive molecules that can be generated in the skin when it is exposed to UV radiation, and are known to play a role in oxidative stress, which can contribute to skin aging and damage. Thus, there is an ongoing search for sunscreens that do not have these negative effects. One promising source for these is natural products. Therefore, the current patent review summarizes topical formulations made from natural compounds that have antioxidant properties and can be used as photoprotective or anti-aging agents, either using a single natural extract or a combination of extracts. The review reports basic patent information (applicant country, type of applicant, and year of filing) and gives details about the invention, including its chemical composition, and the in vitro and in vivo tests performed. These patents describe natural products that can be used to protect the skin and validate their efficacy, and safety, in addition to standardizing their formulations. The compositions described illustrate the consistent innovation in the use of natural products to protect against UV damage and photoaging disorders, a promising field which is receiving growing global recognition.


Subject(s)
Biological Products , Sunscreening Agents , Ultraviolet Rays , Sunscreening Agents/pharmacology , Sunscreening Agents/chemistry , Humans , Biological Products/chemistry , Biological Products/pharmacology , Ultraviolet Rays/adverse effects , Patents as Topic , Skin/drug effects , Skin/radiation effects , Skin Aging/drug effects , Skin Aging/radiation effects , Antioxidants/pharmacology , Antioxidants/chemistry , Animals , Plant Extracts/pharmacology , Plant Extracts/chemistry
16.
Article in English | MEDLINE | ID: mdl-38518984

ABSTRACT

Benzophenone chemicals (BPs) have been developed to prevent the adverse effects of UV radiation and they are widely contaminated. 11ß-Hydroxysteroid dehydrogenase 1 (11ß-HSD1) catalyze the conversion of inactive glucocorticoid to active glucocorticoid, playing critical role in many physiological function. However, the direct effect of BPs on human, pig, rat, and mouse 11ß-HSD1 remains unclear. In this study, we screened the inhibitory strength of 12 BPs on 4 species, and performed the structure-activity relationship (SAR) and in silico docking analysis. The inhibitory potency of BPs was: for human 11ß-HSD1, BP6 (IC50 = 18.76 µM) > BP8 (40.84 µM) > BP (88.89 µM) > other BPs; for pig 11ß-HSD1, BP8 (45.57 µM) > BP6 (59.44 µM) > BP2 (65.12 µM) > BP (135.56 µM) > other BPs; for rat 11ß-HSD1, BP7 (67.17 µM) > BP (68.83 µM) > BP8 (133.04 µM) > other BPs; and for mouse 11ß-HSD1, BP8 (41.41 µM) > BP (50.61 µM) > other BPs. These BP chemicals were mixed/competitive inhibitors of these 11ß-HSD1 enzymes. The 2,2'-dihydroxy substitutions in two benzene rings play a key role in enhancing the effectiveness of inhibiting 11ß-HSD1, possibly via increasing hydrogen bond interactions. Docking analysis shows that these BPs bind to NADPH/glucocorticoid binding sites and forms hydrogen bonds with catalytic residues Ser and/or Tyr. In conclusion, this study demonstrates that BP chemicals can inhibit 11ß-HSD1 from 4 species, and there are subtle species-dependent difference in the inhibitory strength and structural variations of BPs.


Subject(s)
11-beta-Hydroxysteroid Dehydrogenase Type 1 , Benzophenones , Molecular Docking Simulation , Animals , Benzophenones/chemistry , Benzophenones/pharmacology , 11-beta-Hydroxysteroid Dehydrogenase Type 1/antagonists & inhibitors , 11-beta-Hydroxysteroid Dehydrogenase Type 1/metabolism , 11-beta-Hydroxysteroid Dehydrogenase Type 1/chemistry , Humans , Structure-Activity Relationship , Rats , Mice , Swine , Sunscreening Agents/chemistry , Sunscreening Agents/pharmacology , Sunscreening Agents/toxicity , Enzyme Inhibitors/pharmacology , Enzyme Inhibitors/chemistry , Species Specificity , Ultraviolet Rays
17.
Environ Pollut ; 349: 123840, 2024 May 15.
Article in English | MEDLINE | ID: mdl-38537797

ABSTRACT

Benzophenone-3 (BP3) is a common ingredient in personal care products (PCPs) due to its well-established effectiveness in absorbing UV radiation. Sunscreen products are among the most widely used PCPs-containing BP3 applied to the skin, resulting in significant human exposure to BP3 primarily through a dermal application. In the present work, we have tested the action of three environmentally relevant concentrations of BP3 (2, 20 and 200 µg/L) on an in vitro model of implantation of murine blastocysts and on migration ability of the human trophoblast cell line Swan 71. We showed that BP3 caused a significant reduction of blastocyst expansion and a delayed hatching in a non-monotonic way. Besides, embryos displayed a delayed attachment in the three BP3 groups, resulting in a smaller implantation area on the 6th day of culture: BP3(2) (0.32 ± 0.07 mm2); BP3(20) (0.30 ± 0.08 mm2) and BP3(200) (0.25 ± 0.06 mm2) in comparison to the control (0.42 ± 0.07 mm2). We also found a reduced migration capacity of the human first-trimester trophoblast cell line Swan 71 in a scratch assay when exposed to BP3: the lowest dose displayed a higher uncovered area (UA) at 6h when compared to the control, whereas a higher UA of the wound was observed for the three BP3 concentrations at 18 and 24 h of exposure. The changes in UA provoked by BP3 restored to normal values in the presence of flutamide, an androgen receptor (AR) inhibitor. These results indicate that a direct impairment on early embryo implantation and a defective migration of extravillous trophoblast cells through the androgen receptor pathway can be postulated as mechanisms of BP3-action on early gestation with potential impact on fetal growth.


Subject(s)
Benzophenones , Cell Movement , Embryo Implantation , Sunscreening Agents , Trophoblasts , Ultraviolet Rays , Benzophenones/toxicity , Sunscreening Agents/toxicity , Sunscreening Agents/pharmacology , Trophoblasts/drug effects , Cell Movement/drug effects , Mice , Animals , Humans , Embryo Implantation/drug effects , Blastocyst/drug effects , Female , Cell Line
18.
ACS Appl Mater Interfaces ; 16(13): 15798-15808, 2024 Apr 03.
Article in English | MEDLINE | ID: mdl-38507684

ABSTRACT

Sunscreens play a crucial role in protecting the skin from ultraviolet (UV) damage. However, present commercial sunscreens have a tendency to generate free radicals in the UV window, resulting in serious inflammatory responses and health problems. In this study, we demonstrate that silk fibroin microspheres (SFMPs) assembled from regenerated silk fibroin (SF) could scavenge free radicals while preventing UV irradiation and thus present a promising sunscreen. The SFMP reflected more UV light than SF and presented a higher stability than that of organic commercial sunscreens. In vitro analysis proved that SFMP could more efficiently scavenge the hydroxy radical and reduce the intracellular reactive oxygen than titanium dioxide (TiO2). In vivo experiments exhibited that SFMP provided stronger skin protection against UV irradiation than commercial sunscreens and TiO2. Furthermore, SFMP treatment significantly inhibited the skin inflammatory response. This work suggests that the SFMP has great potential to be developed into a biosafe sunscreen.


Subject(s)
Bombyx , Fibroins , Animals , Fibroins/pharmacology , Sunscreening Agents/pharmacology , Microspheres , Free Radicals , Silk
19.
J Oleo Sci ; 73(2): 121-134, 2024.
Article in English | MEDLINE | ID: mdl-38311403

ABSTRACT

Factors influencing on in vitro evaluation of UV protecting ability of sunscreens were analyzed. It was found that any factors making the sunscreen layer spatially inhomogeneous, such as directional viscous fingering during the sunscreen application, dewetting of applied sunscreen layer, and the surface roughness of the standard PMMA plate, alter the UV transmittance. New application procedure and new type of flat hydrophilic plate were developed for inhibiting the generation of spatial inhomogeneity in applied sunscreen layer. The method created by the combination of these newly developed technologies succeeded in providing reliable and reproducible in vitro evaluation of UV protecting ability.


Subject(s)
Sunscreening Agents , Ultraviolet Rays , Sunscreening Agents/pharmacology , Viscosity , Hydrophobic and Hydrophilic Interactions , In Vitro Techniques
20.
Int J Mol Sci ; 25(3)2024 Jan 24.
Article in English | MEDLINE | ID: mdl-38338710

ABSTRACT

Sunlight, despite its benefits, can pose a threat to the skin, which is a natural protective barrier. Phototoxicity caused by overexposure, especially to ultraviolet radiation (UVR), results in burns, accelerates photoaging, and causes skin cancer formation. Natural substances of plant origin, i.e., polyphenols, flavonoids, and photosynthetic pigments, can protect the skin against the effects of radiation, acting not only as photoprotectors like natural filters but as antioxidant and anti-inflammatory remedies, alleviating the effects of photodamage to the skin. Plant-based formulations are gaining popularity as an attractive alternative to synthetic filters. Over the past 20 years, a large number of studies have been published to assess the photoprotective effects of natural plant products, primarily through their antioxidant, antimutagenic, and anti-immunosuppressive activities. This review selects the most important data on skin photodamage and photoprotective efficacy of selected plant carotenoid representatives from in vivo studies on animal models and humans, as well as in vitro experiments performed on fibroblast and keratinocyte cell lines. Recent research on carotenoids associated with lipid nanoparticles, nanoemulsions, liposomes, and micelles is reviewed. The focus was on collecting those nanomaterials that serve to improve the bioavailability and stability of carotenoids as natural antioxidants with photoprotective activity.


Subject(s)
Skin Neoplasms , Ultraviolet Rays , Animals , Humans , Ultraviolet Rays/adverse effects , Antioxidants/pharmacology , Antioxidants/metabolism , Skin/metabolism , Keratinocytes , Carotenoids/pharmacology , Carotenoids/metabolism , Skin Neoplasms/metabolism , Sunscreening Agents/pharmacology
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