Search Results (186)

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

Tuberaria lignosa (Sweet) Samp. (Cistaceae) is a herbaceous species native to southwestern Europe, traditionally used to treat wounds, ulcers, and inflammatory or infectious skin conditions. This study aimed to characterize the phytochemical profile of its aqueous leaf extract and evaluate its skin-related in vitro biological activities. The phenolic composition was determined using UHPLC-HRMS/MS, HPLC-DAD, and quantitative colorimetric assays. Antioxidant activity was assessed against synthetic free radicals, reactive oxygen and nitrogen species, transition metals, and pro-oxidant enzymes. Enzymatic inhibition of tyrosinase, hyaluronidase, collagenase, and elastase were evaluated using in vitro assays. Cytocompatibility was tested on human keratinocytes and NIH/3T3 fibroblasts using MTT and resazurin assays, respectively, while wound healing was evaluated on NIH/3T3 fibroblasts using the scratch assay. Antifungal activity was investigated against several Candida and dermatophyte species, while antibiofilm activity was tested against Epidermophyton floccosum. The extract was found to be rich in phenolic compounds, accounting for nearly 45% of its dry weight. These included flavonoids, phenolic acids, and proanthocyanidins, with ellagitannins (punicalagin) being the predominant group. The extract demonstrated potent antioxidant, anti-tyrosinase, anti-collagenase, anti-elastase, and antidermatophytic activities, including fungistatic, fungicidal, and antibiofilm effects. These findings highlight the potential of T. lignosa as a valuable and underexplored source of bioactive phenolic compounds with strong potential for the development of innovative approaches for skin care and therapy. Full article

This study explores the valorization of agro-industrial by-products—riceberry broken rice (RBR) and soybean meal (SBM)—as cost-effective substrates for enhancing exopolysaccharide (EPS) production by Bacillus tequilensis PS21. Eight Bacillus strains were screened, and B. tequilensis PS21 demonstrated the highest EPS yield (2.54 g/100 mL DW). The EPS displayed a strong antioxidant capacity with 65.5% DPPH and 80.5% hydroxyl radical scavenging, and a FRAP value of 6.51 mg Fe²⁺/g DW. Antimicrobial testing showed inhibition zones up to 10.07 mm against Streptococcus agalactiae and 7.83 mm against Staphylococcus aureus. Optimization using central composite design (CCD) and the response surface methodology (RSM) revealed the best production at 5% (w/v) RBR, 3% (w/v) SBM, pH 6.66, and 39.51 °C, yielding 39.82 g/L EPS. This EPS is a moderate-molecular-weight (11,282 Da) homopolysaccharide with glucose monomers. X-ray diffraction (XRD) showed an amorphous pattern, favorable for solubility in biological applications. Thermogravimetric analysis (TGA) demonstrated thermal stability up to ~250 °C, supporting its suitability for high-temperature processing. EPS also exhibited anticancer activity with IC₅₀ values of 226.60 µg/mL (MCF-7) and 224.30 µg/mL (HeLa) at 72 h, reduced colony formation, inhibited cell migration, and demonstrated anti-tyrosinase, anti-collagenase, and anti-elastase effects. This study demonstrates the successful valorization of agro-industrial by-products—RBR and SBM—for the high-yield production of multifunctional EPS with potent antioxidant, antimicrobial, and anticancer properties. The findings highlight the sustainable potential of these low-cost substrates in supporting the development of green and value-added bioproducts, with promising utilizations across the food, pharmaceutical, and cosmetic sectors. Full article

The treatment of inflammatory bowel diseases (IBDs), particularly ulcerative colitis and Crohn’s disease, remains a challenge. As the available therapeutic options have limited efficacy and various side effect, there is a need to identify new inflammatory modulators that can influence IBD. Natural polyphenols and polyphenol-rich extracts have been found to have preventive and therapeutic potential, including various anti-inflammatory effects. In this study, the inhibition of the formation of mediators associated with intestinal inflammation, remodelling, and angiogenesis by the spent hop extract (SHE), a polyphenol-rich extract from Humulus lupulus L., and its flaxseed polysaccharide-based encapsulates was examined using tumour necrosis factor alpha (TNF-α)-stimulated human small intestinal epithelial (HIEC-6) and large intestinal epithelial (CCD841CoN) cells. Also, we assessed the activity of the tested agents after in the vitro-simulated gastrointestinal digestion process. SHE strongly inhibited the expression of pro-inflammatory cytokines, mainly IL-1β and TNF-α, as well as the expression and activity of type IV collagenases (MMP-2 and MMP-9); these effects resulted from the suppression of NF-κB, ERK and Akt signalling pathways. We also proved the protective effect of encapsulation process against the reduction in the bioaccessibility of SHE, observed under the influence of digestion process. Our results provide initial evidence on the potential utility of SHE and its encapsulates in IBD. Full article

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

The cigarette production from Nicotiana tabacum generates significant amounts of waste, with an estimated 68.31 million tons of pre- and post-harvest waste discarded annually. The pre-harvest waste includes the upper parts of the plant, inflorescences, and bracts, which are removed to help the growth of the lower leaves. This study explores the potential of apical leaves from Nicotiana tabacum var. Virginia, discarded during the budding stage (pre-harvest waste). The leaves were extracted using environmentally friendly solvents (green solvents), including distilled water (DW) and two natural deep eutectic solvents (NaDESs), one consisting of simple sugars, fructose, glucose, and sucrose (FGS) and the other consisting of choline chloride and urea (CU). The anti-inflammatory and anti-aging potential of these green extracts was assessed by the inhibition of key enzymes related to skin aging. The xanthine oxidase and lipoxygenase activities were mostly inhibited by CU extracts with IC₅₀ values of 63.50 and 8.0 μg GAE/mL, respectively. The FGS extract exhibited the greatest hyaluronidase inhibition (49.20%), followed by the CU extract (33.20%) and the DW extract (20.80%). Regarding elastase and collagenase inhibition, the CU extract exhibited the highest elastase inhibition, while all extracts inhibited collagenase activity, with values exceeding 65%. Each extract had a distinct chemical profile determined by LC-ESI-QTOF-MS/MS and spectrophotometric methods, with several shared compounds present in different proportions. CU extract is characterized by high concentrations of rutin, nicotiflorin, and azelaic acid, while FGS and DW extracts share major compounds such as quinic acid, fructosyl pyroglutamate, malic acid, and gluconic acid. Ames test and Caenorhabditis elegans assay demonstrated that at the concentrations at which the green tobacco extracts exhibit biological activities, they did not show toxicity. The results support the potential of N. tabacum extracts obtained with NaDESs as antiaging and suggest their promising applications in the cosmetic and cosmeceutical industries. Full article

This study aims to provide a comprehensive evaluation of the bioactive compounds present in honeysuckle flower (Lonicera japonica Thunb.) extract (HSF) and their remarkable antioxidant activity. A docking simulation was performed to clarify the binding affinities of the identified phytochemicals to enzymes associated with anti-aging and anti-inflammatory activities. In addition, the low-energy nanoemulsions based on optimally formulated polyglycerol fatty acid esters (PGFEs), developed through D-optimality, were designed for the incorporation of HSF extract. The result revealed that HSF is a rich source of diverse phenolic and flavonoid compounds that contribute to its remarkable antioxidant capacity. Molecular docking analysis indicates that its compounds exhibit anti-aging and anti-inflammatory activities, particularly through collagenase, hyaluronidase, and TNF-α inhibition. Furthermore, D-optimality revealed that HSF-loaded nanoemulsions can be fabricated by a surfactant to oil ratio (SOR) of 2:1 with a ratio of low hydrophilic-lipophilic balance (HLB) surfactant to high HLB surfactant (LHR) of 1:2. Polyglyceryl-6 laurate as a high HLB surfactant produced the optimal nanoemulsion with small particle size and possessed an encapsulation efficiency (EE) of 74.32 ± 0.19%. This is the first report to combine D-optimal design-based nanoemulsion development with a multi-level analysis of HSF, including phytochemical profiling, antioxidant evaluation, and in silico molecular docking. These findings highlight that HSF-loaded polyglycerol fatty acid ester-based nanoemulsions could be a skin health-promoting ingredient and effective alternative for a variety of skincare applications. Full article

Characteristic manifestations of skin aging, due to either intrinsic or extrinsic factors, such as ultraviolet (UV) radiation and oxidative stress, include cell senescence, alterations in collagen and elastin networks, and melanogenesis disorders. Natural products are considered a rich source of anti-aging molecules. Accordingly, the screening of a plant extract library from the Greek flora for a panel of biological activities related to skin aging is presented herein. In particular, 52 plant materials extracted using Accelerated Solvent Extraction (ASE) and Supercritical Fluid Extraction (SFE) were assessed for their effects on (1) human skin cell viability, (2) antioxidant activity—using both cell-free and cell-based methods—(3) photoprotective capacity, and (4) interference with collagenase, elastase, and tyrosinase, as well as with proteasomal and lysosomal activities of human skin cells. In vivo phenotypic screens on Danio rerio (zebrafish) embryos were also used for assessing melanogenesis. Many active extracts were identified, some of them for the first time, and others in agreement with previous reports. In general, ASE extracts exhibited higher activities than SFE ones. Seven extracts showed multiple activities, being highly effective in at least four different assays. These data support the potential use of these extracts against skin aging in medicinal and cosmetic applications. Full article

Mitragyna speciosa (kratom) is a traditional medicinal plant rich in bioactive alkaloids and phenolics, known for their antioxidant and anti-aging properties. This study aimed to develop nanoparticle-based topical gels from ethanolic extracts of four kratom varieties, including Kan Daeng (KD), Hang Kang (HK), Tai Bai-yao (KY), and Kan Keaw (KG). Kratom NPs were prepared using a solvent displacement method. The resulting nanoparticles (NPs) exhibited sizes of 201.9–256.2 nm, polydispersity indices (PDI) below 0.3, and a zeta potential between −22.6 and −29.6 mV. The phytochemical analysis revealed that KG and KY extracts contained the highest total phenolic content (TPC) and total flavonoid content (TFC), which were mostly retained after NP formulation. The HPLC analysis confirmed HK as the richest source of mitragynine (9.97 ± 0.10% w/w), while NP formulations displayed slightly reduced levels. Antioxidant activities assessed by DPPH, ABTS, and FRAP assays revealed enhanced radical scavenging in nanoparticle formulations, with IC₅₀ values ranging from 151.23 to 199.87 µg/mL (DPPH) and 207.37 to 272.83 µg/mL (ABTS). All formulations exhibited a significant inhibition of collagenase (80.56 ± 1.60 to 97.23 ± 0.29%), elastase (45.46 ± 6.53 to 52.19 ± 1.20%), and hyaluronidase (83.23 ± 2.34 to 91.67 ± 3.56%), with nanoparticle forms showing superior enzyme inhibition. Notably, nanoparticle formulations exhibited superior inhibitory effects compared to crude extracts. HaCaT cytotoxicity tests confirmed high biocompatibility (IC₅₀ > 700 µg/mL), especially for KD and KG NPs. The NP-loaded gels demonstrated acceptable physicochemical stability after heating/cooling cycle testing, with pH (7.27 to 7.88), viscosity (10.719 to 12.602 Pa·s), and favorable visual and textural properties. In summary, KG and KY cultivars emerged as the most promising cosmeceutical candidates due to their superior phytochemical content, antioxidant capacity, enzyme-inhibitory activities, and formulation performance. These findings support the potential use of KG NP and KY NP-loaded gels as multifunctional cosmeceutical agents for antioxidant protection, anti-aging, and skin rejuvenation. Full article

Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder characterized by impaired glucose regulation. This study evaluated the antioxidant and antidiabetic potential of aqueous extracts from four plant species from the southern Algarve: Aristolochia baetica, Chelidonium majus, Dittrichia viscosa, and Lavandula viridis, using non-cellular in vitro assays. HPLC/PDA was used to identify active compounds. Antioxidant activity was assessed by using TAA, FRAP, RP, and DPPH assays; antidiabetic potential through α-glucosidase and α-amylase inhibition; and wound healing relevance through elastase, collagenase, and lipoxygenase inhibition. D. viscosa showed the highest antioxidant activity (FRAP: 1132.99 ± 19.54 mg TE/g dw; DPPH IC₅₀ = 25.85 ± 0.75 μg/mL) and total phenolic/flavonoid content, with a diverse profile including caffeic and chlorogenic acids, isoquercetin, and quercetin. It also exhibited potent α-glucosidase inhibition (IC₅₀ = 0.61 ± 0.06 mg/mL), outperforming acarbose. L. viridis had the highest total phenolic content (39.04 mg/g), while A. baetica demonstrated the strongest anti-elastase, anti-collagenase, and lipoxygenase activity, suggesting wound-healing potential. C. majus showed the weakest effects. A strong correlation was observed between phenolic content and antioxidant/antidiabetic activity. These findings support further in vivo studies on D. viscosa and A. baetica for potential use in T2DM management and diabetic wound healing. Full article

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

Osteoarthritis (OA), the most common degenerative pathology of the joints, affects mainly elderly people, and it is one of the most important factors causing disability. This study aimed to assess the effect of Juglans regia L. on rats with collagenase-induced knee osteoarthritis comparative with groups with the same disease treated with ellagic acid (EA), indomethacin as positive control and vehicle as negative control. After 2 and 4 weeks of treatment, blood samples were collected in order to evaluate the oxidative stress and inflammation, as well as RANKL and hydroxyproline levels. The results showed that EA improved the systemic antioxidant defense (p < 0.05), decreased the interleukin-6 (IL-6) secretion (p < 0 < 0.05) and RANKL levels (p < 0.01 and p < 0.001) at the same time enhancing hydroxyproline values, particularly after 2 weeks of treatment (p < 0.01). JR extract especially maintained low values of RANKL (p < 0.05) and hydroxyproline levels (p < 0.05), indicating a partial chondroprotective effect compared to EA. In conclusion, the use of EA and JR extract can improve some parameters of bone regeneration in experimental osteoarthritis, suggesting beneficial effects in articular inflammatory diseases. However, further studies are necessary to establish the optimum dose and time of treatment with both compounds in order to obtain optimal therapeutic results. Full article

Hypericum hircinum L., commonly known as goat St. John’s wort or stinking tutsan, is a medicinal plant native to the Mediterranean basin and widespread across Europe and parts of the Middle East. It has a long history of traditional uses in folk medicine to treat respiratory diseases, wounds, and burns and to relieve migraine, rheumatism, and muscular pains. Despite numerous scientific studies shading light on the phytochemical profile and on the beneficial properties of the plant extracts, a comprehensive overview of the current knowledge is missing. In this paper, we summarized the available information on botany, traditional uses, phytochemistry, and pharmacological properties of Hypericum hircinum from peer-reviewed articles published till March 2025 in PubMed, ScienceDirect, Wiley, Springer, ACS, Scielo, and Web of Science databases. The presence of numerous valuable compounds, including terpenes, phenolic acids, flavonoids, and phloroglucinols, is reported as well as the wide range of pharmacological properties, such as antimicrobial, antifungal, antiviral, antidepressant, anti-collagenase, anti-α-glucosidase, and antioxidant activities, together with non-pharmacological properties. The data reported in this review contribute to a deeper understanding of the biological properties of the species and pave the way for further investigation of its potential applications. Full article

Background/Objectives: Conjugation techniques are increasingly valued in food chemistry for enhancing sensory properties, nutritional profiles, and bioactivity, with potential applications in cosmeceuticals. This study aimed to investigate the potential of Glycine max (L.) Merrill oligopeptide–monosaccharide conjugates as active ingredients in cosmeceuticals, emphasizing their biological activities and stability. Methods: G. max isolate was prepared and subsequently hydrolyzed using alcalase to obtain the oligopeptide (OP). The OP was then conjugated with allulose (AL) or mannose (MN) through a controlled humid-dry heating process to produce the conjugates, OPA and OPM, respectively. Their biological activities, including antioxidant, anti-tyrosinase, anti-collagenase, anti-elastase, and anti-hyaluronidase properties, were assessed and compared to the individual components. Additionally, the irritation potential was evaluated using the hen’s egg test on chorioallantoic membrane (HET-CAM). The stability was examined under varying pH levels, temperatures, and light conditions based on their biological activity profiles. Results: OPA demonstrated the highest antioxidant activity, showing the lowest DPPH^• IC₅₀ value of 198.6 ± 2.7 µg/mL along with a strong ferric reducing power of 1.37 ± 0.04 µg FeSO₄/g sample. Besides, OPM showed superior tyrosinase inhibition on both L-tyrosine and L-DOPA substrates, highlighting its potential for skin whitening. Both OPA and OPM significantly enhanced collagenase inhibition, supporting their anti-aging potential. All samples were non-irritating in the HET-CAM test. The conjugates (OPA and OPM) demonstrated enhanced stability against pH, heat, and light compared to OP, AL, and MN. Conclusions: Oligopeptide–monosaccharide conjugation not only improved bioactivity but also enhanced biological stability, suggesting their potential for use in cosmeceutical applications. Full article

Background: Manganese porphyrin, MnTnBuOE-2-PyP⁵⁺ (BMX-001), improves neurologic deficits in experimental ischemic stroke and has the potential to serve as an adjunct with thrombolysis or thrombectomy in stroke patients. In 10–30% of stroke patients following thrombolysis, the hemorrhagic transformation, associated with iron release, occurs. This study aimed to examine the neurologic outcome following the BMX-001 treatment in a mouse intracerebral hemorrhage (ICH) model with relevance to prospective ischemic stroke clinical trials. Methods: Twenty C57Bl6 mice were randomly assigned to groups after surgery and received vehicle or BMX-001 treatment immediately following stereotaxic left striatum collagenase injection. Post-ICH body weight, the Corner test, neurological deficit score, and Rotarod test were examined. Six sham surgery mice serve as a control group. At 72 h, the brain histological evaluation was performed, including hemorrhage size, Prussian blue staining, and the activation of macrophages. Data were collected by a researcher who was blind to groups. Results: No significant difference in body weight, neurological deficits, and hemorrhage size was found between groups. However, BMX-001 reduced the number of macrophages in the hemorrhagic area (48 ± 10 in vehicle, 33 ± 8 in BMX-001, p = 0.008) and the number of cells stained with Prussian blue—an indicator of iron released during hemorrhage (65 ± 22 in vehicle and 41 ± 15 in BMX-001, p = 0.027). Conclusions: The results support the safe use of BMX-001 in stroke patients in combination with thrombolysis or thrombectomy and, moreover, indicate the beneficial anti-inflammatory effect of BMX-001, alike to that previously reported in stroke studies of analogous, similarly redox-active, Mn porphyrins. Full article