Search Results (1,655)

Extracted from Ganoderma lucidum mycelium, the developed β-1,3;1,6-glucan rich polysaccharides have the potential to be used during the industrial production of health food products due to their inhibition of metabolic syndrome, immunomodulatory and antitumor activities and other health benefits. Ganoderma active polysaccharides (GAP) have also been found to promote skin health, particularly due to their antioxidant and anti-aging properties. The present study investigates the skin-protective properties of polysaccharides purified from Ganoderma mycelium cultivated using stress-tolerance technology and a fully plant-based medium. The effects of the GAP are investigated in both in vitro and human studies. The results of the study indicate that the developed GAP effectively inhibit 32.4% of tyrosinase activity and 30.6% of melanin production in B16F10 cells. Furthermore, in scratch assays using NIH 3T3 cells, these GAP also promote cell migration and wound healing. In human studies, GAP demonstrated no potential for skin irritation while effectively reducing skin wrinkles, enhancing skin brightness, diminishing erythema, and increasing epidermal hydration. In hot-flux patch-induced erythema experiments, these GAP were found to be capable of alleviating erythema severity by up to 48%. The present study demonstrates that GAP, which can be produced industrially using innovative technologies and is rich in highly water-soluble β-1,3;1,6-glucan with a triple-helix structure, holds potential for application in the skincare industry. Full article

Background: Baeckea frutescens L. (BF) has been reported as a potential natural source for skin-whitening agents. However, its antimelanogenic activity and mechanisms remain unclear. Methods: The antimelanogenic effects of BF were evaluated in α-melanocyte-stimulating hormone (α-MSH)-stimulated B16F10 cells and in zebrafish embryos. Cell viability, intracellular tyrosinase activity and melanin content were measured. Western blot (WB) analysis was used to examine melanogenesis-related proteins. Network pharmacology and molecular docking were performed to predict potential targets and interactions of BF-derived metabolites. Results: The ethanolic extract of BF reduced intracellular tyrosinase activity and melanin content in cells without cytotoxicity. Western blot analysis showed decreased expression of microphthalmia-associated transcription factor (MITF) and its downstream melanogenic enzymes, including tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1), and dopachrome tautomerase (DCT). In addition, BF reduced phosphorylation of protein kinase A (PKA), cAMP responsive element-binding protein (CREB) and extracellular signal-regulated kinase (ERK), suggesting potential suppression of PKA/CREB and ERK signaling pathways. These regulatory effects may contribute to MITF downregulation and subsequent inhibition of melanogenesis. BF reduced melanin accumulation in zebrafish embryos. Network pharmacology and molecular docking analyses further suggested that BF-derived metabolites, particularly bayogenin, may interact with multiple melanogenesis-related targets. Conclusions: BF may inhibit melanogenesis through coordinated modulation of multiple signaling pathways and may represent a promising skin-whitening candidate. Full article

Background/Objectives: Achillea millefolium is a well-known medicinal plant recognized in several pharmacopeias, while the Balkan endemic species Achillea clypeolata lacks a pharmacopeial monograph and remains insufficiently studied despite its traditional use. This study aimed to comparatively evaluate the phytochemical composition and biological potential of both species. Methods: Chemical composition was studied using UHPLC-MS/MS, HPLC, and FT-IR; anti-inflammatory potential was analyzed by erythrocyte membrane stabilization assay (heat- and hypotonicity-induced hemolysis); and enzyme-inhibitory activity was tested against collagenase, elastase, hyaluronidase, and tyrosinase. In addition, antioxidant activity was evaluated using DPPH, ABTS, and DCFDA assays; antimicrobial activity was determined using the broth microdilution method; and cytotoxic potential was investigated by the MTT assay. Results: The major constituents in water–ethanolic extracts were quinic acid derivatives, flavonoids, phenolic acids, and coumarins, with chlorogenic acid, 3,5-dicaffeoylquinic acid, cosmosiin, cynaroside, rutin, and hyperoside as dominant in both species. Extracts exhibited marked anti-inflammatory activity, where A. millefolium provided greater protection under heat-induced hemolysis, and both extracts showed comparable efficacy under osmotic stress. Concentration-dependent inhibition of collagenase, elastase, hyaluronidase, and tyrosinase (concentration from 62.5 to 1000 µg/mL), along with significant antioxidant activity in ABTS and DPPH assays, was observed. In MRC-5 cells, the extracts reduced AAPH-induced ROS levels up to 50 µg/mL, while higher concentrations showed diminished effects. Moderate cytotoxicity was observed, with A. clypeolata displaying stronger effects at 50–100 µg/mL. Both Achillea species exhibited broad-spectrum antimicrobial activity, with pronounced effects against Gram-positive bacteria. Conclusions: The results support the traditional use of Achillea species and highlight A. clypeolata as a promising, yet underexplored, source of bioactive compounds for dermatological and pharmaceutical applications. Full article

Background/Objectives: Skin candidiasis is a key contributor to chronic, non-healing wounds, largely due to persistent microbial infections. Candida species can colonize the skin, form protective biofilms, and interfere with enzyme activity, leading to extracellular matrix degradation, changes in pigmentation, and impaired wound healing. The rising prevalence of antifungal resistance challenges its management, underscoring the need for more effective antifungal therapies. Therefore, this study aimed to assess the antifungal effects and wound-healing potential of essential oils (EOs) from Ferulago spp. Methods: The antifungal activity of the EOs from five Ferulago species was evaluated against Candida spp. and Cryptococcus neoformans. The most active EOs were further investigated for their effects on C. albicans virulence factors, including germ tube formation, as well as biofilm formation and disruption. These effects were assessed using microscopic observation, XTT reduction assay, and crystal violet and safranin stainings. The wound-healing potential of the EOs was evaluated using the scratch-wound assay on fibroblasts and keratinocytes. Additionally, the effect on tyrosinase and elastase activity, was also investigated. Results:F. silaifolia and F. cassia essential oils showed fungicidal activity against Candida spp. and Cryptococcus neoformans. F. silaifolia displayed greater potency, with lower MIC and MLC values. Both oils inhibited key C. albicans virulence factors at sub-MIC concentrations. F. silaifolia EO was more effective in preventing biofilm formation whereas F. cassia EO showed notable tyrosinase inhibitory effect. Conclusions: These findings align with traditional uses and suggest that F. silaifolia and F. cassia EOs exhibit antifungal activity alongside properties associated with wound healing, supporting their potential as topical antifungal agents and thereby justifying further investigation. Full article

This study aims to evaluate the antioxidant and anti-inflammatory potential of dichloromethanic, methanolic and hydroalcoholic extracts of seventeen different selected Balkan medicinal herbs with ethnopharmacological interest, with the goal of identifying the most bioactive candidates for further investigation of their therapeutic efficacy in human diseases. A total of fifty-four extracts were initially screened; due to the high sample number, only the most active samples were advanced to subsequent assays in order to identify bioactive candidates with potential therapeutic efficacy in human diseases. The methanolic extract of Cotinus coggygria showed the highest radical scavenging activity (DPPH: 96.4% inhibition), the hydroalcoholic extract of Hypericum empetrifolium exhibited the most potent iron chelation (IC₅₀: 5.0 μg/mL) and the methanolic extract of Sedum sediforme presented the best anti-inflammatory activity in in vitro assays (LOX IC₅₀: 39.4 μg/mL, COX-1 inhibition: 93.1% and COX-2 inhibition: 94.0%). Furthermore, significant inhibition of tyrosinase and collagenase was observed for the methanolic extract of Cistus creticus (94.2% tyrosinase inhibition, 86.8% collagenase inhibition) and the methanolic extract of Cotinus coggygria (83.1% tyrosinase inhibition, 96.1% collagenase inhibition). In vivo, five promising plant extracts were selected and evaluated for their anti-inflammatory activity using a carrageenan-induced paw edema model in female C57BL/6 mice. The study aimed to assess the in vivo anti-inflammatory potential of these extracts under acute inflammatory conditions. The methanolic extract of Cotinus coggygria proved the most active, significantly reducing paw edema by 34% compared to the non-treated control, indicating a pronounced anti-inflammatory effect and supporting its potential as a source of bioactive compounds with therapeutic relevance. The results of this study indicate that several selected herbal extracts exhibit notable pharmacological activities. Given their antioxidant, anti-inflammatory, and inhibitory properties against enzymes related to skin function, these extracts warrant further in vivo and (pre)clinical investigation for potential use in cosmetic and pharmaceutical products targeting skin disorders associated with inflammation and oxidative stress. Full article

Lotus rectus L. is an underexplored forage legume with reported traditional uses in skin-related conditions. This study aimed to characterize the phytochemical profile of its aqueous leaf extract (LRAE) and to explore its bioactivity in vitro. Phytochemical characterization was carried out using spectrophotometric assays and UHPLC-HRMS/MS. Cytocompatibility was assessed by the resazurin assay in HaCaT keratinocytes and NIH/3T3 fibroblasts, while wound-healing potential was evaluated using a scratch assay. Enzyme inhibitory activities (xanthine oxidase, collagenase, hyaluronidase, and tyrosinase) were determined spectrophotometrically. Antioxidant capacity was assessed using chemical assays (DPPH and ABTS), biologically relevant reactive oxygen species, and metal chelation assays. Antifungal activity was evaluated against clinically relevant yeasts and dermatophytes using standardized macrodilution methods. LRAE showed a relatively high content of flavonoids and proanthocyanidins, particularly flavonol glycosides. The extract was cytocompatible at all tested concentrations and showed an increased closure of the scratched area in vitro. It exhibited antioxidant activity and inhibited xanthine oxidase, while more moderate effects were observed for collagenase and tyrosinase, and minimal activity was detected against hyaluronidase. Antifungal activity was limited, with modest effects observed only against selected dermatophytes at high concentrations. Overall, these findings provide preliminary in vitro evidence of bioactivity associated with the traditional use of this species, supporting further investigation to better characterize the biological relevance of this understudied species. Full article

This study aimed to elucidate the relationship between chemical profiles and in vitro biological activities of essential oils from Cladanthus eriolepis, Asteriscus graveolens, and Teucrium luteum subsp. flavovirens. The chemical composition of these essential oils has been previously reported in our recent publications, revealing distinct chemical profiles with pronounced interspecific variability and identification rates of 83.3%, 96.7%, and 98.1%, respectively. C. eriolepis exhibited a chemical profile rich in aliphatic esters with a mixed monoterpene–sesquiterpene composition dominated by α-pinene (13.0%), isobutyl angelate (10.7%), and 2-methylbutyl angelate (9.5%), whereas A. graveolens was characterized by a high abundance of 6-oxocyclonerolidol (72.5%). T. luteum subsp. flavovirens showed greater chemical complexity, including elemol (16.4%), α-pinene (12.0%), and eudesmol isomers (14.3%). All essential oils exhibited significant biological activities across various in vitro assays. C. eriolepis showed the strongest acaricidal effect (LC₅₀ = 0.539 µL/mL) and notable inhibitory activities against acetylcholinesterase (AChE), tyrosinase, and α-glucosidase (78.4%, 74.6%, and 69.2%, respectively). T. luteum subsp. flavovirens displayed the highest antioxidant capacity (DPPH IC₅₀ = 51.60 µg/mL; FRAP IC₅₀ = 35.53 µg/mL). Overall, variations in chemical profiles strongly influence biological activities, highlighting their potential as multifunctional bioactive sources. Full article

Equisetum ramosissimum Desf. Subsp. debile (Roxb. ex Vaucher) Hauk (E. ramosissimum), exhibits anti-tyrosinase and antioxidant activities. However, identifying the key compounds exhibiting anti-tyrosinase effects and establishing effective protocols for their extraction have not been accomplished. Herein, we investigate and establish an effective extraction method and identify the key bioactive compounds responsible for tyrosinase inhibition. E. ramosissimum was extracted using the microwave-assisted extraction (MAE) method. The MCW4 extract exhibited the highest antioxidant activity (IC₅₀: 90.96 ± 0.515 µg/mL) and TPC (27.23 ± 1.180 mg of GAE/g-crude extract), while the MCW5 extract showed the strongest anti-tyrosinase activity (IC₅₀: 126.48 ± 6.668 µg/mL). LC-MS/MS analysis identified resveratrol isomers, protocatechuic acid, cis-ETRA acid, KF-3-GBS, 1-16:0-lysoPC, and 1-16:0-lysoPE as potential anti-tyrosinase compounds, detected only in MCW4 and MCW5 under the applied extraction and analytical conditions. Molecular docking indicated favorable predicted binding toward human tyrosinase (hTyr) for resveratrol isomers, KF-3-GBS, and 1-16:0-lysoPE. KF-3-GBS was uniquely detected in MCW5. These results suggest that MAE using a solid-to-solvent ratio of 1:16 at 40 °C for 15 min produced an E. ramosissimum extract that exhibited strong tyrosinase inhibitory activity. Kaempferol-3-gentiobioside (KF-3-GBS) demonstrated favorable binding to hTyr in molecular docking analysis, supporting its potential role as a direct tyrosinase inhibitor. Full article

Wound healing involves the coordinated regulation of inflammation, angiogenesis, and extracellular matrix remodeling, processes modulated by natural bioactives. In this context, Chelidonium majus L. (C. majus), a plant rich in alkaloids and flavonoids, remains mechanistically underexplored. This study, therefore, investigates its metabolites using an integrated computational–experimental approach and evaluates their applicability in sericin-based wound-healing systems. A curated database of 83 C. majus bioactive compounds was analyzed using cheminformatics and molecular docking against key wound-healing targets (iNOS, VEGF, MMP-3, and tyrosinase), followed by ADMET and toxicity prediction (StopTox). Selected plant–sericin formulations were subsequently evaluated for wound-healing activity using an in vitro fibroblast scratch assay. Docking revealed strong binding affinities for several metabolites, particularly protopine, kaempferol-3-rutinoside, cynaroside, hesperidin, quercetin-3-rhamnosylrutinoside, and vitexin, indicating multi-target modulation across inflammatory, proliferative, and remodeling phases of tissue repair. ADMET and toxicity analyses predicted favorable dermal safety and pharmacokinetic profiles for most compounds. Consistently, in vitro assays demonstrated that C. majus–sericin systems had fibroblast migration and wound closure in a concentration- and ratio-dependent manner, with improved healing kinetics observed at 150 µg/mL and for formulations containing higher relative proportions of both components. The experimental outcomes supported the pro-angiogenic and matrix-stabilizing mechanisms predicted in silico. Overall, C. majus metabolites exhibit polypharmacological wound-healing activity, supporting their integration into sericin-based systems as a promising strategy for topical therapies. Full article

The aim of this study was to investigate the anti-melanogenic effects and underlying mechanisms of PFRMY (Pro-Phe-Arg-Met-Tyr), a pentapeptide derived from tilapia skin (Oreochromis niloticus), using B16F10 murine melanoma cells. Treatment with PFRMY (1.0 mg/mL) significantly reduced intracellular melanin content and tyrosinase (TYR) activity by 39.55 ± 1.51% and 32.46 ± 1.31%, respectively. RT-PCR and Western blotting analyses revealed that PFRMY suppressed melanogenesis through the α-MSH/PKA/CREB signaling pathway. Notably, PFRMY reversed α-MSH-induced upregulation of key downstream factors including PKA, CREB, MITF, and TYR, while showing minimal effects on the protein expression of MC1R or α-MSH. Molecular docking further suggested that PFRMY binds to MC1R with higher affinity than α-MSH, potentially occupying the ligand-binding site and thereby interfering with downstream signaling. Collectively, these findings demonstrate that PFRMY effectively inhibits melanogenesis by competitively antagonizing the α-MSH/MC1R axis, highlighting its potential as a safe and efficacious ingredient for hyperpigmentation treatment and cosmetic applications. Full article

Marine biofouling remains a major challenge for maritime industries, affecting submerged structures and vessels worldwide. The long-standing reliance on biocidal coatings, together with their documented environmental impacts, has led to increasingly restrictive regulations and an urgent demand for environmentally compatible antifouling (AF) solutions. This study evaluates the AF potential and toxicological profile of two nucleoside analogues, hypoxanthine arabinoside (1′) and 2′-deoxyinosine (2′), selected based on the previously reported non-lethal AF activity of the naturally occurring nucleosides adenosine and 2′-deoxyadenosine from cyanobacteria. Both analogues inhibited the growth of Navicula sp. by approximately 60% without inducing mortality and significantly reduced settlement of Mytilus galloprovincialis plantigrades, with EC₅₀ values of 5.50 µM (1′) and 8.54 µM (2′), and no lethality detected (LC₅₀ > 200 µM). At near-EC₅₀ concentrations, both compounds increased acetylcholinesterase and tyrosinase activities, supported by molecular docking results, suggesting involvement of neurotransmission- and byssal formation-related pathways. Proteomic analysis revealed compound-specific molecular responses. No lethal effects were observed in non-target organisms (LC₅₀ > 32 µM for A. amphitrite and LC₅₀ > 50 µM for A. salina), and environmental fate modelling predicted low bioaccumulation and rapid degradation. Overall, substitution of the amino group by a carbonyl group preserved AF efficacy without increasing toxicity, highlighting nucleosides as promising low-toxicity AF agents. Full article

Cysteine is a sulfur-containing amino acid that plays a central role in skin physiology through thiol-mediated redox regulation and glutathione (GSH) synthesis. It critically influences melanogenesis, collagen homeostasis, and wound healing. However, its clinical application is limited by poor stability and bioavailability. In this review, we provide a mechanistic and comparative analysis of cysteine and its derivatives, including N-acetylcysteine (NAC), cysteinamide (C-NH₂), GSH, and related compounds. These derivatives regulate melanogenesis by modulating dopaquinone pathways and tyrosinase activity, maintain collagen balance by preserving redox-sensitive enzymatic processes, and enhance wound healing through antioxidant and anti-inflammatory mechanisms. Importantly, chemical modifications such as acetylation, amidation, and esterification improve pharmacokinetic properties, enabling more effective intracellular delivery. Furthermore, different derivatives exhibit distinct advantages depending on biological context, highlighting the importance of compound selection. Overall, cysteine derivatives emerge as promising therapeutic candidates for dermatological applications, particularly in pigmentation disorders and impaired wound healing. Future studies should focus on in vivo validation and clinical translation. Full article

Ultraviolet (UV) irradiation induces complex skin damage, including hyperpigmentation, oxidative stress, and alterations in proteins related to keratinocyte differentiation and epidermal barrier-associated status. This study investigated the multifunctional protective effects of Padina arborescens ethanolic extract (PAEE) against skin damage in melanocytes, keratinocytes, and zebrafish. In alpha-melanocyte-stimulating hormone (α-MSH)-stimulated B16F10 cells, PAEE effectively suppressed the protein kinase A (PKA)/cyclic adenosine monophosphate (cAMP) response element-binding protein (CREB) signaling pathway, which was associated with reduced expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, leading to decreased melanin synthesis. PAEE also exhibited photoprotective properties by reducing reactive oxygen species (ROS), inhibiting interleukin-1 beta (IL-1β), and attenuating matrix metalloproteinase-1 (MMP-1) upregulation associated with UVB (ultraviolet B)-induced photodamage in HaCaT keratinocytes. Notably, PAEE restored the UVB-reduced expression of filaggrin and involucrin, representative markers of keratinocyte differentiation and epidermal barrier-associated status, in HaCaT keratinocytes. In zebrafish embryos, PAEE suppressed α-MSH-induced melanin accumulation and UVB-induced ROS generation at non-toxic concentrations. Taken together, these results suggest that PAEE exerts anti-melanogenic and photoprotective effects in cellular and zebrasfish models and may serve as a promising marine-derived ingredient for cosmeceutical applications targeting UVB-related skin damage. Full article

Picnomon acarna (L.) Cass. is a Mediterranean medicinal plant with limited phytochemical and bioactivity characterisation. In this study, methanolic extracts obtained by maceration (MAC), Soxhlet (SOE), and ultrasound-assisted extraction (UAE) were comparatively investigated to determine their phytochemical composition and biological potential. Liquid chromatography–electrospray ionisation–tandem mass spectrometry (LC–ESI–MS/MS) analysis identified and quantified 24 phenolic compounds, with hesperidin, chlorogenic acid, and hyperoside as the dominant constituents. The maceration extract exhibited the highest total phenolic content (29.06 mg GAE/g extract) and showed superior antioxidant performance across six complementary assays [2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing antioxidant power (FRAP), phosphomolybdenum, and ferrous-ion chelation), reflected by the highest relative antioxidant capacity index (RACI = 0.93). Enzyme inhibition assays revealed extraction-dependent activity patterns: Soxhlet and ultrasound extracts demonstrated stronger acetylcholinesterase inhibition (IC₅₀ ≈ 1.23 mg/mL), while Soxhlet extract showed the most potent tyrosinase (AChE) inhibition (IC₅₀ = 1.48 mg/mL). α-Amylase inhibition was comparable among extracts (IC₅₀ = 1.90–2.03 mg/mL). Pearson correlation analysis indicated strong relationships between major phenolics and antioxidant activity. Molecular docking further supported these findings, showing favourable binding affinities of hesperidin, hyperoside, and chlorogenic acid toward α-amylase and acetylcholinesterase, while only chlorogenic acid and hyperoside demonstrated favourable interactions with tyrosinase-related protein-1 (TYRP1), whereas hesperidin did not exhibit a meaningful binding affinity. Overall, the results demonstrate that the extraction strategy significantly influences the phenolic composition and multi-target bioactivity of P. acarna, highlighting its potential as a source of natural antioxidant and enzyme-modulating compounds. Full article

Lippia origanoides Kunth (Verbenaceae family), popularly known in northern Brazil as “Salva-de-Marajó”, is a native plant widely used in traditional medicine and cooking. While previous studies have addressed its antimicrobial and insecticidal properties, its ability to inhibit disease-related enzymes has received limited attention. This study investigated the essential oil (EO) of L. origanoides as a source of enzyme inhibitors relevant to Alzheimer’s disease, metabolic disorders and skin pigmentation disorders. The EO showed strong inhibitory activity against acetylcholinesterase (IC₅₀: 22.9 μg/mL) and α-glucosidase (IC₅₀: 14.6 μg/mL), indicating potential for managing neurodegenerative conditions and diabetes, respectively. Moderate inhibition was observed for lipase, butyrylcholinesterase and tyrosinase. Although carvacrol, the major EO constituent, contributed significantly to these effects, it did not fully explain the observed bioactivity. Bio-guided fractionation revealed that oxygenated compounds were mainly responsible for inhibiting cholinesterases and lipase, whereas α-glucosidase inhibition was associated with hydrocarbon compounds. Both fractions contributed to tyrosinase inhibition, reinforcing the EO’s relevance for treating hyperpigmentation. Furthermore, the EO demonstrated strong antioxidant activity, largely linked to carvacrol and oxygenated constituents. Chemical characterization by GC-MS, GC-FID and enantiomeric analysis strengthened the relationship between composition and bioactivity. Overall, L. origanoides EO emerged as a promising multifunctional natural product for therapeutic and cosmetic applications. Full article