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Search Results (520)

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Keywords = tyrosinase inhibitory activity

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24 pages, 2024 KiB  
Article
New Insights into the Synergistic Bioactivities of Zingiber officinale (Rosc.) and Humulus lupulus (L.) Essential Oils: Targeting Tyrosinase Inhibition and Antioxidant Mechanisms
by Hubert Sytykiewicz, Sylwia Goławska and Iwona Łukasik
Molecules 2025, 30(15), 3294; https://doi.org/10.3390/molecules30153294 - 6 Aug 2025
Abstract
Essential oils (EOs) constitute intricate mixtures of volatile phytochemicals that have garnered significant attention due to their multifaceted biological effects. Notably, the presence of bioactive constituents capable of inhibiting tyrosinase enzyme activity and scavenging reactive oxygen species (ROS) underpins their potential utility in [...] Read more.
Essential oils (EOs) constitute intricate mixtures of volatile phytochemicals that have garnered significant attention due to their multifaceted biological effects. Notably, the presence of bioactive constituents capable of inhibiting tyrosinase enzyme activity and scavenging reactive oxygen species (ROS) underpins their potential utility in skin-related applications, particularly through the modulation of melanin biosynthesis and protection of skin-relevant cells from oxidative damage—a primary contributor to hyperpigmentation disorders. Zingiber officinale Rosc. (ginger) and Humulus lupulus L. (hop) are medicinal plants widely recognized for their diverse pharmacological properties. To the best of our knowledge, this study provides the first report on the synergistic interactions between essential oils derived from these species (referred to as EOZ and EOH) offering novel insights into their combined bioactivity. The purpose of this study was to evaluate essential oils extracted from ginger rhizomes and hop strobiles with respect to the following: (1) chemical composition, determined by gas chromatography–mass spectrometry (GC-MS); (2) tyrosinase inhibitory activity; (3) capacity to inhibit linoleic acid peroxidation; (4) ABTS•+ radical scavenging potential. Furthermore, the study utilizes both the combination index (CI) and dose reduction index (DRI) as quantitative parameters to evaluate the nature of interactions and the dose-sparing efficacy of essential oil (EO) combinations. GC–MS analysis identified EOZ as a zingiberene-rich chemotype, containing abundant sesquiterpene hydrocarbons such as α-zingiberene, β-bisabolene, and α-curcumene, while EOH exhibited a caryophyllene diol/cubenol-type profile, dominated by oxygenated sesquiterpenes including β-caryophyllene-9,10-diol and 1-epi-cubenol. In vitro tests demonstrated that both oils, individually and in combination, showed notable anti-tyrosinase, radical scavenging, and lipid peroxidation inhibitory effects. These results support their multifunctional bioactivity profiles with possible relevance to skin care formulations, warranting further investigation. Full article
(This article belongs to the Special Issue Essential Oils—Third Edition)
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21 pages, 2074 KiB  
Article
Preliminary Analysis of Bilberry NaDES Extracts as Versatile Active Ingredients of Natural Dermocosmetic Products: In Vitro Evaluation of Anti-Tyrosinase, Anti-Hyaluronidase, Anti-Collagenase, and UV Protective Properties
by Milica Martinović, Ivana Nešić, Ana Žugić and Vanja M. Tadić
Plants 2025, 14(15), 2374; https://doi.org/10.3390/plants14152374 - 1 Aug 2025
Viewed by 225
Abstract
Bilberry (Vaccinium myrtillus L.) fruits represent the recognized wellspring of bioactive compounds with various documented bioactivities. Although bilberry leaves are often treated as industrial by-products, they also represent a valuable source of phytochemicals with potential dermocosmetic applications. In this study, extracts of [...] Read more.
Bilberry (Vaccinium myrtillus L.) fruits represent the recognized wellspring of bioactive compounds with various documented bioactivities. Although bilberry leaves are often treated as industrial by-products, they also represent a valuable source of phytochemicals with potential dermocosmetic applications. In this study, extracts of bilberry fruits and leaves were prepared using both conventional solvents (water and 50% ethanol) and natural deep eutectic solvents (NaDES) as green, biodegradable alternatives. The aim of this study was to examine the UV protective activity and inhibitory potential of those extracts against some enzymes (tyrosinase, hyaluronidase, collagenase) that are important in terms of skin conditioning and skin aging. The results of in vitro tests have shown the superiority of NaDES extracts compared to conventional extracts regarding all tested bioactivities. In addition, bilberry leaves extracts were more potent compared to fruit extracts in all cases. The most potent extract was bilberry leaf extract made with malic acid–glycerol, which exhibited strong anti-tyrosinase (IC50 = 3.52 ± 0.26 mg/mL), anti-hyaluronidase (IC50 = 3.23 ± 0.30 mg/mL), and anti-collagenase (IC50 = 1.84 ± 0.50 mg/mL) activities. The correlation analysis revealed correlation between UV protective and anti-tyrosinase, UV protective and anti-collagenase as well as between anti-hyaluronidase and anti-collagenase activity. UV protection and anti-tyrosinase activity correlated significantly with chlorogenic acid and hyperoside contents in extracts. The extracts with the best activities also demonstrated a good safety profile in a 24 h in vivo study on human volunteers. Full article
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25 pages, 3359 KiB  
Article
In Vitro and In Silico Evaluation of the Anti-Aging Potential of Eugenia uniflora UAE Extracts
by Desy Muliana Wenas, Berna Elya, Sutriyo Sutriyo, Heri Setiawan, Rozana Othman, Syamsu Nur, Nita Triadisti, Fenny Yunita and Erwi Putri Setyaningsih
Molecules 2025, 30(15), 3168; https://doi.org/10.3390/molecules30153168 - 29 Jul 2025
Viewed by 437
Abstract
Skin aging is a natural biological process that can be accelerated by free radical induction, leading to a reduction in skin elasticity and the formation of wrinkles due to the depletion of elastin. Eugenia uniflora (dewandaru) is a promising plant believed to possess [...] Read more.
Skin aging is a natural biological process that can be accelerated by free radical induction, leading to a reduction in skin elasticity and the formation of wrinkles due to the depletion of elastin. Eugenia uniflora (dewandaru) is a promising plant believed to possess anti-aging properties, primarily attributed to its major constituents, myricitrin and quercetin. This study aimed to investigate the anti-elastase and antioxidant properties of Eugenia uniflora stem bark, ripe fruit, and seed extracts. Extracts were obtained using an ultrasound-assisted extraction (UAE) method with 70% ethanol. Quantitative phytochemical analysis involved measuring the total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity. Bioactive constituents were identified using LC-MS analysis, and their interactions with target enzymes were further evaluated through in silico molecular docking. The results demonstrated that the E. uniflora seed extract exhibited the highest antioxidant activity, with an IC50 of 5.23 µg/mL (DPPH assay) and a FRAP value of 3233.32 µmol FeSO4/g. Furthermore, the ethanolic seed extract showed significant anti-elastase activity with an IC50 of 114.14 µg/mL. Molecular docking predicted strong potential for several compounds as pancreatic elastase inhibitors, including 5-phenylvaleric acid, 2-(3-phenylpropyl)phenol, n-amylbenzene, 2-aminoadipic acid, and traumatin, each showing a prediction activity (PA) value exceeding 0.6. Notably, these compounds also exhibited inhibitory activity against tyrosinase. These findings collectively underscore the significant promise of E. uniflora seed extract as a novel and natural candidate for pharmacocosmeceutical product development, particularly for anti-aging applications. Full article
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23 pages, 8387 KiB  
Article
Solvent Fractionation of Polygonum cuspidatum Sieb. et Zucc. for Antioxidant, Biological Activity, and Chromatographic Characterization
by Yuchen Cheng, Yuri Kang and Woonjung Kim
Int. J. Mol. Sci. 2025, 26(14), 7011; https://doi.org/10.3390/ijms26147011 - 21 Jul 2025
Viewed by 330
Abstract
This study investigated the natural bioactive compounds in Polygonum cuspidatum Sieb. et Zucc. (P. cuspidatum) by fractionating a 70% ethanol extract using n-hexane, chloroform, ethyl acetate, n-butanol, and water. The total polyphenol and flavonoid contents of each fraction were [...] Read more.
This study investigated the natural bioactive compounds in Polygonum cuspidatum Sieb. et Zucc. (P. cuspidatum) by fractionating a 70% ethanol extract using n-hexane, chloroform, ethyl acetate, n-butanol, and water. The total polyphenol and flavonoid contents of each fraction were determined, and their antioxidant activities were evaluated using DPPH, ABTS, and FRAP assays. Additionally, the anti-diabetic potential was assessed via α-glucosidase inhibitory activity, while anti-obesity activity was evaluated using lipase inhibitory activity. The fractions were also tested for tyrosinase and elastase inhibitory activities to assess their skin-whitening and anti-wrinkle potential, and their antibacterial activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa was determined using the agar diffusion method. Finally, bioactive compounds were identified and quantified using HPLC and GC–MSD. The results showed that the ethyl acetate fraction possessed the highest total polyphenol content (0.53 ± 0.01 g GAE/g) and total flavonoid content (0.19 ± 0.02 g QE/g). It also exhibited strong antioxidant activity, with the lowest DPPH radical scavenging IC50 (0.01 ± 0.00 mg/mL), ABTS radical scavenging IC50 (0.06 ± 0.00 mg/mL), and the highest FRAP value (6.02 ± 0.30 mM Fe2+/mg). Moreover, it demonstrated potent enzyme inhibitory activities, including tyrosinase inhibitory activity (67.78 ± 2.50%), elastase inhibitory activity (83.84 ± 1.64%), α-glucosidase inhibitory activity (65.14 ± 10.29%), and lipase inhibitory activity (85.79 ± 1.04%). In the antibacterial activity, the ethyl acetate fraction produced a clear inhibitory zone of 19.50 mm against Staphylococcus aureus, indicating notable antibacterial activity. HPLC-PDA and GC–MSD analyses identified tannic acid and emodin as the major bioactive constituents. These findings suggest that the ethyl acetate fraction of P. cuspidatum extract, rich in polyphenol and flavonoid compounds, is a promising natural source of bioactive ingredients for applications in the food, pharmaceutical, and cosmetic industries. Further research is needed to explore its mechanisms and therapeutic applications. Full article
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22 pages, 4534 KiB  
Article
Upcycled Cocoa Pod Husk: A Sustainable Source of Phenol and Polyphenol Ingredients for Skin Hydration, Whitening, and Anti-Aging
by Aknarin Anatachodwanit, Setinee Chanpirom, Thapakorn Tree-Udom, Sunsiri Kitthaweesinpoon, Sudarat Jiamphun, Ongon Aryuwat, Cholpisut Tantapakul, Maria Pilar Vinardell and Tawanun Sripisut
Life 2025, 15(7), 1126; https://doi.org/10.3390/life15071126 - 17 Jul 2025
Viewed by 726
Abstract
Theobroma cacao L. (cocoa) pod husk, a byproduct of the chocolate industry, has potential for commercial applications due to its bioactive compounds. This study aimed to determine the phytochemical composition, biological activity, and clinical efficacy of a standardized extract. This study compared 80% [...] Read more.
Theobroma cacao L. (cocoa) pod husk, a byproduct of the chocolate industry, has potential for commercial applications due to its bioactive compounds. This study aimed to determine the phytochemical composition, biological activity, and clinical efficacy of a standardized extract. This study compared 80% ethanol (CE) and 80% ethanol acidified (CEA) as extraction solvents. The result indicated that CEA yielded higher total phenolic content (170.98 ± 7.41 mg GAE/g extract) and total flavonoid content (3.91 ± 0.27 mg QE/g extract) than CE. Liquid chromatography–tandem mass spectrometry (LC/MS/MS) identified various phenolic and flavonoid compounds. CEA demonstrated stronger anti-oxidant (IC50 = 5.83 ± 0.11 μg/mL in the DPPH assay and 234.17 ± 4.01 mg AAE/g extract in the FRAP assay) compared to CE. Additionally, CEA exhibited anti-tyrosinase (IC50 = 9.51 ± 0.01 mg/mL), anti-glycation (IC50 = 62.32 ± 0.18 µg/mL), and anti-collagenase (IC50 = 0.43 ± 0.01 mg/mL), nitric oxide (NO) production inhibitory (IC50 = 62.68 μg/mL) activities, without causing toxicity to cells. A formulated lotion containing CEA (0.01–1.0% w/w) demonstrated stability over six heating–cooling cycles. A clinical study with 30 volunteers showed no skin irritation. The 1.0% w/w formulation (F4) improved skin hydration (+52.48%), reduced transepidermal water loss (−7.73%), and decreased melanin index (−9.10%) after 4 weeks of application. These findings suggest cocoa pod husk extract as a promising active ingredient for skin hydrating and lightening formulation. Nevertheless, further long-term studies are necessary to evaluate its efficacy in anti-aging treatments. Full article
(This article belongs to the Special Issue Bioactive Compounds for Medicine and Health)
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23 pages, 4407 KiB  
Article
Integration Viewpoint Using UHPLC-MS/MS, In Silico Analysis, Network Pharmacology, and In Vitro Analysis to Evaluate the Bio-Potential of Muscari armeniacum Extracts
by Nilofar Nilofar, Gokhan Zengin, Mehmet Veysi Cetiz, Evren Yildiztugay, Zoltán Cziáky, József Jeko, Claudio Ferrante, Tina Kostka, Tuba Esatbeyoglu and Stefano Dall’Acqua
Molecules 2025, 30(13), 2855; https://doi.org/10.3390/molecules30132855 - 4 Jul 2025
Viewed by 515
Abstract
The current study investigates the chemical profiling, antioxidant activities, and enzyme inhibitory and cytotoxic potential of the water and methanolic extracts of different parts (flower, leaf, and bulb) of Muscari armeniacum. Chemical profiling was performed using UHPLC-MS/MS. At the same time, different [...] Read more.
The current study investigates the chemical profiling, antioxidant activities, and enzyme inhibitory and cytotoxic potential of the water and methanolic extracts of different parts (flower, leaf, and bulb) of Muscari armeniacum. Chemical profiling was performed using UHPLC-MS/MS. At the same time, different in vitro assays were employed to support the results for antioxidant potential, such as DPPH, ABTS, FRAP, CUPRAC, metal chelation, and PBD, along with the measurement of total phenolic and flavonoid contents. Enzyme inhibition was investigated for cholinesterase (AChE and BChE), α-amylase, α-glucosidase, and tyrosinase enzymes. Additionally, the relative expression of NRF2, HMOX1, and YGS was evaluated by qPCR. LC-MS/MS analysis indicated the presence of some significant compounds, including apigenin, muscaroside, hyacinthacine A, B, and C, and luteolin. According to the results, the highest TPC and TFC were obtained with both extracts of the leaves, followed by the water extract (flower) and methanolic extract of the bulb. In contrast, the methanolic extract from the bulb exhibited the highest antioxidant potential using DPPH, ABTS, CUPRAC, and FRAP, followed by the extracts of leaves. In contrast, the leaf extracts had the highest values for the PBD assay and maximum chelation ability compared to other tested extracts. According to the enzyme inhibition studies, the methanolic extract from the bulb appeared to be the most potent inhibitor for all the tested enzymes, with the highest values obtained for AChE (1.96 ± 0.05), BChE (2.19 ± 0.33), α-amylase (0.56 ± 0.02), α-glucosidase (2.32 ± 0.01), and tyrosinase (57.19 ± 0.87). Interestingly, the water extract from the bulb did not inhibit most of the tested enzymes. The relative expression of NRF2 based on qPCR analysis was considerably greater in the flower methanol extract compared to the other extracts (p < 0.05). The relative expression of HMOX1 was stable in all the extracts, whereas YGS expression remained stable in all the treatments and had no statistical differences. The current results indicate that the components of M. armeniacum (leaves, flowers, and bulb) may be a useful source of natural bioactive compounds that are effective against oxidative stress-related conditions, including hyperglycemia, skin disorders, and neurodegenerative diseases. Complementary in silico approaches, including molecular docking, dynamics simulations, and transcription factor (TF) network analysis for NFE2L2, supported the experimental findings and suggested possible multi-target interactions for the selected compounds. Full article
(This article belongs to the Section Analytical Chemistry)
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27 pages, 7392 KiB  
Article
Skin-Whitening, Antiwrinkle, and Moisturizing Effects of Astilboides tabularis (Hemsl.) Engl. Root Extracts in Cell-Based Assays and Three-Dimensional Artificial Skin Models
by Nam Ho Yoo, Hyun Sook Lee, Sung Min Park, Young Sun Baek and Myong Jo Kim
Int. J. Mol. Sci. 2025, 26(12), 5725; https://doi.org/10.3390/ijms26125725 - 15 Jun 2025
Viewed by 545
Abstract
This study investigated the potential cosmetic properties of the ethyl acetate (EtOAc) fraction obtained from the roots of Astilboides tabularis (Hemsl.) Engl., focusing on skin-whitening, antiwrinkle, and moisturizing effects using cell-based assays and three-dimensional (3D) artificial skin models (Neoderm-ED and Neoderm-ME). The EtOAc [...] Read more.
This study investigated the potential cosmetic properties of the ethyl acetate (EtOAc) fraction obtained from the roots of Astilboides tabularis (Hemsl.) Engl., focusing on skin-whitening, antiwrinkle, and moisturizing effects using cell-based assays and three-dimensional (3D) artificial skin models (Neoderm-ED and Neoderm-ME). The EtOAc fraction showed significant dose-dependent inhibitory activity against tyrosinase (TYR) (72.0% inhibition at 50 µg/mL), comparable to that of kojic acid. In α-melanocyte-stimulating hormone (α-MSH)-stimulated Neoderm-ME artificial skin containing melanocytes, the EtOAc fraction reduced melanin synthesis at concentrations of 50 and 75 µg/mL and decreased melanogenesis-related gene expression, including TYR, microphthalmia-associated transcription factor (MITF), tyrosinase-related protein-1 (TRP-1) and TRP-2. In the antiwrinkle assays, the EtOAc fraction effectively inhibited elastase activity (41.5% inhibition at 10 µg/mL), exceeding the efficacy of ursolic acid. In the Neoderm-ED artificial skin model, the EtOAc fraction reversed structural damage induced by particulate matter (PM10), restoring epidermal thickness and dermal density. This improvement was supported by the increased expression of skin barrier and antiwrinkle genes, including filaggrin, hyaluronic acid synthase-1 (HAS-1), HAS-2, aquaporin-3 (AQP-3), collagen type I alpha 1 chain (COL1A1), elastin, tissue inhibitor of metalloproteinases-1 (TIMP-1), and TIMP-2, as well as decreased expression of matrix metalloproteinases (MMP-1, MMP-3, and MMP-9). Our results indicate that the EtOAc fraction from A. tabularis root has considerable potential as a multifunctional cosmetic. Full article
(This article belongs to the Section Bioactives and Nutraceuticals)
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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 748
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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18 pages, 322 KiB  
Article
Fatty Acid Profile and Some Useful Biological Aspects of Borage, Calophyllum, and Prickly Pear Seed Oils: Implications for Health and Dietary Use
by Florinda Fratianni, Francesca Coppola, Siria Tavaniello, Maria Neve Ombra, Beatrice De Giulio, Nunzio D’Agostino, Gokhan Zengin, Raffaele Coppola and Filomena Nazzaro
Antioxidants 2025, 14(6), 661; https://doi.org/10.3390/antiox14060661 - 30 May 2025
Viewed by 644
Abstract
Seed oils from Borago officinalis (borage), Opuntia ficus-indica (prickly pear), and Calophyllum inophyllum (calophyllum or tamanu) are rich in bioactive fatty acids and have been traditionally used in cosmetic and industrial sectors. This study explored their fatty acid composition and investigated their in [...] Read more.
Seed oils from Borago officinalis (borage), Opuntia ficus-indica (prickly pear), and Calophyllum inophyllum (calophyllum or tamanu) are rich in bioactive fatty acids and have been traditionally used in cosmetic and industrial sectors. This study explored their fatty acid composition and investigated their in vitro antioxidant, anti-arthritic, neuroprotective, and antibiofilm activities. Fatty acid profiles were determined via gas chromatography. Antioxidant activity was assessed using DPPH and ABTS radical scavenging assays. Anti-arthritic potential was measured via bovine serum albumin denaturation. Neuroprotective properties were evaluated through acetylcholinesterase, butirylcholinesterase, and tyrosinase inhibition. Antibiofilm activity against five pathogenic strains was analyzed using crystal violet and MTT assays. Correlation analysis was used to associate fatty acid composition with bioactivity. Prickly pear oil exhibited the highest PUFA content (65.1%), mainly linoleic acid. Calophyllum oil was richer in saturated and monounsaturated fatty acids. All oils showed significant radical scavenging ability, with calophyllum oil showing the lowest DPPH IC50 and borage oil, the highest ABTS activity. Borage and prickly pear oils demonstrated strong anti-arthritic potential. Calophyllum oil showed the most potent AChE inhibition. All oils showed tyrosinase inhibition; however, calophyllum did not show BChE inhibitory activity. Antibiofilm activity was species- and dose-dependent, with Staphylococcus aureus, Escherichia coli, and Acinetobacter baumannii being most affected. Thus, the tested oils exhibited multiple biological activities, influenced by their fatty acid composition. The in vitro antioxidant, anti-arthritic, neuroprotective, and antimicrobial properties support their potential use as functional food ingredients or nutraceuticals, especially for aging-related health concerns. Further in vivo and clinical studies are needed to confirm their efficacy. Full article
(This article belongs to the Section Natural and Synthetic Antioxidants)
22 pages, 517 KiB  
Article
Erica spiculifolia Salisb. (Balkan Heath): A Focus on Metabolic Profiling and Antioxidant and Enzyme Inhibitory Properties
by Reneta Gevrenova, Anna Szakiel, Cezary Pączkowski, Gokhan Zengin, Inci Kurt-Celep, Alexandra Stefanova and Dimitrina Zheleva-Dimitrova
Plants 2025, 14(11), 1648; https://doi.org/10.3390/plants14111648 - 28 May 2025
Viewed by 552
Abstract
Erica spiculifolia Salisb. (formerly Bruckenthalia spiculifolia Benth.) (Balkan heath) is renowned for its traditional usage as a diuretic, anti-inflammatory and antioxidant agent. For the first time, acylquinic acids, flavonoids and numerous proanthocyanidin oligomers were annotated/dereplicated by liquid chromatography–high-resolution mass spectrometry in methanol–aqueous extracts [...] Read more.
Erica spiculifolia Salisb. (formerly Bruckenthalia spiculifolia Benth.) (Balkan heath) is renowned for its traditional usage as a diuretic, anti-inflammatory and antioxidant agent. For the first time, acylquinic acids, flavonoids and numerous proanthocyanidin oligomers were annotated/dereplicated by liquid chromatography–high-resolution mass spectrometry in methanol–aqueous extracts from E. spiculifolia aerial parts harvested at the early and full flowering stage. Chlorogenic acid and proanthocyanidin tetra- and trimer A, B-type together with quercitrin and (+) catechin were the predominant compounds in the semi-quantitative analysis. Neutral triterpenoids, triterpenoid acids and phytosterols were determined in apolar extracts by gas chromatography–mass spectrometry. Triterpenoid acids accounted for 80% of the total triterpenoid content, dominated by ursolic and oleanolic acid, reaching up to 32.2 and 6.1 mg/g dw, respectively. Ursa/olean-2,12-dien-28-oic acids and 3-keto-derivatives together with α-amyrin acetate as a chemotaxonomic marker, α-amyrenone, α- and β-amyrin were evaluated. Total phenolic and flavonoid contents were 83.85 ± 0.89 mg gallic acid equivalents/g and 78.91 ± 0.41 mg rutin equivalents/g, respectively. The extract actively scavenged DPPH and ABTS radicals (540.01 and 639.11 mg Trolox equivalents (TE)/g), possessed high potential to reduce copper and iron ions (660.32 and 869.22 mg TE/g, respectively), and demonstrated high metal chelating capacity (15.57 Ethylenediaminetetraacetic acid equivalents/g). It exhibited prominent anti-lipase (18.32 mg orlistat equivalents/g) and anti-tyrosinase (71.90 mg kojic acid equivalents/g) activity. The extract inhibited α-glucoside (1.35 mmol acarbose equivalents/g) and acetylcholinesterase (2.56 mg galanthamin equivalents/g), and had moderate effects on α-amylase, elastase, collagenase and hyaluronidase. Balkan heath could be recommended for raw material production with antioxidant and enzyme inhibitory properties. Full article
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27 pages, 2278 KiB  
Systematic Review
Current Findings on Allium Species with Melanogenesis Inhibitory Activity
by Mariangela Marrelli, Maria Pia Argentieri, Vincenzo Musolino, Carmine Lupia, Claudia-Crina Toma, Filomena Conforti, Vincenzo Mollace and Giancarlo Statti
Plants 2025, 14(11), 1635; https://doi.org/10.3390/plants14111635 - 27 May 2025
Viewed by 717
Abstract
Allium genus (Amaryllidaceae) is widely distributed in the Northern hemisphere. Some species, including garlic and onion, have been used since ancient times as both food ingredients and medicinal plants. Many reviews deal with the chemical constituents, particularly the typical sulfur compounds, as well [...] Read more.
Allium genus (Amaryllidaceae) is widely distributed in the Northern hemisphere. Some species, including garlic and onion, have been used since ancient times as both food ingredients and medicinal plants. Many reviews deal with the chemical constituents, particularly the typical sulfur compounds, as well as with Allium pharmacological properties, such as antimicrobial, anti-inflammatory, antioxidant, and cytotoxic activities. The bibliographic search performed in this review is mainly focused on the potential role of Allium species in inhibiting melanogenesis, which has been mainly assessed through the evaluation of the inhibitory properties on tyrosinase, the key enzyme in melanin biosynthesis. Two well established models for identifying potential skin-whitening agents have been used to assess the anti-melanogenic effects of Allium species, the mushroom tyrosinase and the murine melanoma B16 cell line. Here, a literature search from Scopus, Web of Science, and PubMed databases has been performed using the keywords “Allium”, “tyrosinase”, “anti-melanogenic”, and “melanogenesis”, combined by means of Boolean operators. Based on selected inclusion criteria, 32 eligible papers have been selected. The aim of this systematic review is to offer an overview of the species for which the ability to affect melanogenesis has been demonstrated to date, highlighting a new and emerging perspective on the potential therapeutic use of Allium species. The biological properties of isolated pure compounds and the negative outcomes have been also considered. Full article
(This article belongs to the Section Phytochemistry)
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25 pages, 1620 KiB  
Article
Laccase-Catalyzed Polymerized Natural Bioactives for Enhanced Mushroom Tyrosinase Inhibition
by Diana Costa, Diana Rocha, Joana Santos, Jennifer Noro, Artur Ribeiro and Carla Silva
Catalysts 2025, 15(5), 481; https://doi.org/10.3390/catal15050481 - 14 May 2025
Viewed by 1355
Abstract
Skin hyperpigmentation disorders, such as melasma, are linked to excessive melanin production, primarily regulated by the enzyme tyrosinase (TYR). While current inhibitors like kojic acid (KA) are effective, they often cause adverse side effects, driving the search for safer andnatural alternatives. This study [...] Read more.
Skin hyperpigmentation disorders, such as melasma, are linked to excessive melanin production, primarily regulated by the enzyme tyrosinase (TYR). While current inhibitors like kojic acid (KA) are effective, they often cause adverse side effects, driving the search for safer andnatural alternatives. This study evaluated the TYR inhibitory potential of bioactive-rich extracts from acorn, cocoa, cork, and eucalyptus, extracted using hydroethanolic (HE) and natural deep eutectic solvents (NADES), and explored the enhancement of their bioactivity through laccase-assisted polymerization. NADES significantly improved extraction yields and preserved bioactive compounds, with cocoa extracts showing the highest TYR inhibition. Laccase-mediated polymerization further enhanced TYR inhibitory activity, particularly of NADES extracts, suggesting a more effective and sustainable approach for skincare applications. The results highlight the potential of combining green chemistry principles with enzymatic catalysis to develop eco-friendly and efficient treatments for hyperpigmentation disorders, offering a promising alternative to conventional methods. Full article
(This article belongs to the Special Issue The Design of Protein-Based Catalysts)
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13 pages, 14458 KiB  
Article
Potential Cutaneous Applications of Boesenbergia rotunda Extract Based on Its In Vitro Anti-Melanogenic and Anti-Fibroproliferative Properties
by Nuntida Salakshna, Wilai Thanasarnaksorn, Phongthon Kanjanasirirat, Kedchin Jearawuttanakul, Napason Chabang, Noppawan Rangkansenee, Uraiwan Panich, Saowalak Thanachaiphiwat, Suparerk Borwornpinyo and Suradej Hongeng
Int. J. Mol. Sci. 2025, 26(9), 4319; https://doi.org/10.3390/ijms26094319 - 1 May 2025
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Abstract
The rhizomes of Boesenbergia rotunda (fingerroot) and its bioactive compound, panduratin A, exhibit potent anti-inflammatory, antioxidant, and anti-proliferative properties. The aim of this study was to investigate the anti-melanogenic (including anti-tyrosinase) effects of B. rotunda extract and panduratin A in B16F10 melanoma cells [...] Read more.
The rhizomes of Boesenbergia rotunda (fingerroot) and its bioactive compound, panduratin A, exhibit potent anti-inflammatory, antioxidant, and anti-proliferative properties. The aim of this study was to investigate the anti-melanogenic (including anti-tyrosinase) effects of B. rotunda extract and panduratin A in B16F10 melanoma cells induced by UVA radiation. The effects of the compounds on fibroblast proliferation and migration were also assessed by scratch wound healing assays in human primary fibroblasts. The results showed that B. rotunda extract and panduratin A significantly reduced tyrosinase activity and cellular melanogenesis induced by UVA radiation in a dose-dependent manner. The compounds also demonstrated inhibitory effects on fibroblast cell migration and proliferation. These findings suggest that B. rotunda extract may have potential therapeutic effects on skin hyperpigmentation and fibroproliferative skin disorders. Full article
(This article belongs to the Section Bioactives and Nutraceuticals)
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23 pages, 2361 KiB  
Article
Tyrosinase Inhibitors Among Flora of Lubelskie Region—Application of Bio-Chromatographic Approach and Zebrafish Model in Bioactivity Screening of Plant Material
by Kamila Kusio-Targońska, Nataliia Kosheva, Krzysztof Kamil Wojtanowski, Katarzyna Gaweł-Bęben, Dimitris Beis and Wirginia Kukula-Koch
Molecules 2025, 30(9), 1979; https://doi.org/10.3390/molecules30091979 - 29 Apr 2025
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Abstract
The whitening potential of natural products is commonly assessed through spectrophotometric assays that colorimetrically measure the inhibitory effects on tyrosinase, a key enzyme in pigment formation. However, these assays fail to provide evidence about the input of individual components into the total activity [...] Read more.
The whitening potential of natural products is commonly assessed through spectrophotometric assays that colorimetrically measure the inhibitory effects on tyrosinase, a key enzyme in pigment formation. However, these assays fail to provide evidence about the input of individual components into the total activity of a mixture like plant extracts. This study introduced chromatographic methods to identify active natural products without isolating them from their mixtures. In this study, various plant extracts of differing polarities (EtOH, 50% EtOH, and HOH) from species growing in the Lubelskie region of Poland were evaluated for their ability to inhibit tyrosinase. The most active extract identified through spectrophotometric assays was a 50% EtOH extract from Matricaria recutita L. (Chamomilla recutita (L.) Rauschert). Subsequent HPLC-MS analysis allowed for the identification of several active compounds from different classes, including organic acids, glycosylated phenolics, and phenolic acids that interacted with the enzyme. The bioactivity of individual components was confirmed through classical spectrophotometric assays, highlighting ferulic acid (IC50 = 0.484 µM), quinic acid (IC50 = 22.90 µM), and citric acid (IC50 = 24.18 µM) as three representatives of different classes of molecules with inhibitory potential. Furthermore, the whitening capacity of the chamomile extract was investigated in a zebrafish model, demonstrating effective pigmentation inhibition in Danio rerio larvae and validating the proposed chromatographic approach. Full article
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18 pages, 2373 KiB  
Article
Yield, Bioactive Compounds, and Antioxidant Potential of Twenty-Three Diverse Microgreen Species Grown Under Controlled Conditions
by Bhornchai Harakotr, Lalita Charoensup, Panumart Rithichai, Yaowapha Jirakiattikul and Patlada Suthamwong
Resources 2025, 14(5), 71; https://doi.org/10.3390/resources14050071 - 27 Apr 2025
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Abstract
Selecting suitable crop species is crucial for optimizing the productivity and nutritional content of microgreens. In this study, twenty-three diverse microgreen species, grown under controlled conditions, were analyzed for yield, bioactive compounds, and antioxidant activities. The microgreens were cultivated on a peat substrate [...] Read more.
Selecting suitable crop species is crucial for optimizing the productivity and nutritional content of microgreens. In this study, twenty-three diverse microgreen species, grown under controlled conditions, were analyzed for yield, bioactive compounds, and antioxidant activities. The microgreens were cultivated on a peat substrate in a controlled environment, with a growth period of 6 to 20 days from planting to harvest. Conditions were maintained at 25 ± 2 °C, a 16 h photoperiod, CO2 concentration of 1000 ppm, relative humidity of 60 ± 2%, and the LED light was set at 330 μmol/m2/s PPFD. Results from the analysis revealed that the yield, bioactive compounds, and antioxidant potential differed significantly among the twenty-three microgreen species. Unfortunately, the superior microgreens exhibiting greater values for all studied traits could not be identified. However, the principal component analysis (PCA) clustered red radish, rat-tailed radish, and Chinese kale microgreens, which were high in both yield and bioactive compounds. In contrast, red holy basil and lemon basil microgreens had high levels of these compounds but low yields. Additionally, a high level of anti-tyrosinase activity was observed in garland chrysanthemum, Chinese mustard, and Chinese cabbage microgreens. Therefore, these microgreen species can be utilized individually or in varying ratios to produce bioactive compounds in different concentrations that are suitable for various applications. The information presented in this study provides valuable insights for health-conscious consumers and growers for selecting superior species with functional implications. Full article
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