Search Results (32)

Peptide cyclization is a strategy to improve biological stability and functional activity, but direct comparison between linear and cyclic peptides with the same sequence is still limited. In this study, linear (L-CR5) and cyclic (C-CR5) forms were synthesized, and biological functions such as antioxidant, whitening, and anti-wrinkle activity were compared and evaluated. C-CR5 showed about 22.3 times of DPPH radical scavenging activity, which was significantly stronger than L-CR5, and tyrosinase inhibition increased rapidly in C-CR5 to reach inhibition of 95% or more, whereas L-CR5 showed only moderate activity in the same range (about 6.5 times). MMP-1 expression in the evaluation of anti-wrinkle activity did not show a decreasing trend in L-CR5 at all, while C-CR5 showed an anti-wrinkle effect, which was reduced by about 92.8% at 400 μg/mL. As a result of molecular docking analysis, C-CR5 exhibited lower MolDock scores than L-CR5 toward both tyrosinase and MMP-1, indicating a potentially higher binding affinity and improved binding stability. This is expected to be due to reduced structural flexibility and optimized residue directions (especially Tyr and Arg). These results indicate that peptide cyclization is an example of enhanced functional bioactivity of CYGSR and provides a positive case for the structure–activity relationship. Full article

The actinobacterial strain Kitasatospora griseola JNUCC 62 was isolated from volcanic wetland soil at Mulyeongari Oreum, Jeju Island, and taxonomically identified through 16S rRNA gene and whole-genome analyses. The complete genome, assembled from PacBio Sequel I reads, spans 8.31 Mb with a GC content of 72.8% and contains 7265 coding sequences. Comparative genomic indices (Average nucleotide identity, ANI 97.46%; digital DNA–DNA hybridization, dDDH 84.4%) confirmed its conspecific relationship with K. griseola JCM 3339^T. Genome mining using antiSMASH 8.0 revealed 30 biosynthetic gene clusters (BGCs), including polyketide synthase (PKS), non-ribosomal peptide synthetase (NRPS), ribosomally synthesized and post-translationally modified peptide (RiPP), lanthipeptide, and terpene types, accounting for 18.6% of the genome. Several BGCs displayed homology to known formicamycin-, lankacidin-, and lanthipeptide-type clusters, while others were novel or cryptic, reflecting adaptation to the nutrient-poor volcanic environment. Ethyl acetate extraction of the culture broth, especially under tryptophan-supplemented conditions, yielded four metabolites—1-acetyl-β-carboline, perlolyrine, tryptopol, and 1H-pyrrole-2-carboxylic acid—identified by UV and NMR spectroscopy. These compounds correspond to NRPS–PKS hybrid and arylpolyene-type gene clusters predicted in the genome, suggesting precursor-directed biosynthesis of indole and pyrrole alkaloids. The ethyl acetate extract (JNUCC62 EA) exhibited strong antioxidant capacity in the ABTS assay, anti-inflammatory activity via inhibition of nitric oxide (31.09 ± 3.69% of control) and cytokines (IL-6, IL-1β, TNF-α) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages, and anti-melanogenic effects in α-melanocyte-stimulating hormone (MSH)-stimulated B16F10 melanoma cells, where melanin content and tyrosinase activity decreased to 61.49 ± 1.24% and 24.32 ± 0.31% of the control, respectively, without cytotoxicity. A human primary skin irritation test confirmed no irritation up to 50 µg/mL, establishing excellent dermal safety. Collectively, these findings highlight K. griseola JNUCC 62 from Mulyeongari Oreum as a volcanic wetland-derived actinomycete harboring rich biosynthetic potential for novel indole alkaloids with antioxidant, anti-inflammatory, and whitening properties, supporting its development as a safe and multifunctional cosmeceutical ingredient. Full article

Peptides are notable cosmetic ingredients owing to their diverse biological activities and beneficial effects on skin health. Therefore, multifunctional peptides capable of simultaneously exerting antioxidant, whitening, and anti-wrinkle effects are highly desirable. In this study, a scalable and cost-effective chemical synthesis strategy was used for the rapid design and synthesis of linear peptide sequences with skin bioactivity using solid-phase peptide synthesis. Subsequently, liquid-phase peptide synthesis was used to enhance the proteolytic stability and develop a cyclic peptide, cyclic CYGSR (CR5), which was subjected to in vitro biological evaluation. CR5 showed high biocompatibility in water-soluble tetrazolium salt-1 (WST-1) assays, maintaining over 90% cell viability at concentrations up to 400 μg/mL. In the 2,2-Diphenyl-1-picrylhydrazy (DPPH) assay, CR5 exhibited strong antioxidant activity with 83.18% radical scavenging at 200 μg/mL. It also showed 97.79% tyrosinase inhibition at 800 μg/mL, confirming significant whitening potential. Moreover, CR5 inhibited matrix metalloproteinase-1 (MMP-1) expression by 73.55% and increased type I procollagen expression by 44.68% at 400 μg/mL, demonstrating its anti-wrinkle potential. Additionally, molecular docking and dynamic simulation demonstrated stable binding of the peptide to tyrosinase and MMP-1. Collectively, CR5 possesses multifunctional properties with excellent biocompatibility, highlighting its potential as a novel cosmetic active ingredient. Full article

Modern dermocosmetics combine the effectiveness of active substances with the benefits of percutaneous penetration enhancers to address skin issues such as hyperpigmentation. In this study, three bioactive tripeptides (with amino acid sequences CSF, CVL, and CSN) with previously confirmed tyrosinase inhibition activity were synthesized using the solid-phase synthesis method. The structures of the obtained peptides were determined. In addition, elastase in silico and in vitro inhibition assays were carried out. The tripeptides were subsequently encapsulated into liposomes, for which key physicochemical parameters were determined, including size, zeta potential, and encapsulation efficiency. The average diameter of the prepared liposomes was approximately 100 nm across all samples. The prepared carriers were found to be stable and exhibited no cytotoxicity toward reconstructed human epidermis cells. The peptides achieved an encapsulation efficiency of approximately 20–30%, with no significant differences observed between the cationic and anionic vesicles. Liposomes containing the CSF tripeptide, which showed the strongest tyrosinase-inhibiting effect, did not transport the peptide through the human skin in an ex vivo assay to permit quantification in the receptor solution, but facilitated penetration and retention of the tripeptide within the epidermis (4.65 ± 1.81 μg/cm²). These findings suggest that the prepared liposomes may serve as valuable carriers of bioactive tripeptides in anti-aging cosmetics. Full article

Chrono Control Penta is a novel plant derived multifunctional bioactive peptide, which offer a tailored targeted approach to skin health by addressing both pigmentation and aging. Chrono Control Penta inhibits tyrosinase with an IC₅₀ value of 202.8 µM. Additionally, it significantly increased collagen (+87.53%) and elastin (+61.29%) production and secretion (+66.29% and +69.74%, respectively) and decreased the Matrix metalloproteinase-9 (MMP-9) and MMP-2 secretion in aged human dermal fibroblasts, vs. aging condition. At the clinical level, Chrono Control Penta was demonstrated to be already active after 2 weeks, promoting a 9.3% reduction in pigmentation after 6 weeks of use, showing its efficacy in promoting skin complexion. Furthermore, it exhibited significant moisturizing (13.05%), anti-wrinkle (11.55%), and purifying effects (12.45%), as well as firming effects (6.35%), after 6 weeks. The peptide was also well tolerated, with no adverse effects reported in clinical patch tests. This timely study presents novel research on a plant derived peptide, Chrono Control Penta, a significantly contribution to the burgeoning cosmetic peptide market. Our rigorous findings make it a new powerful ingredient, offering a comprehensive solution for skin health, and establishing a strong foundation for future research and application. Full article

Microalgae are a promising source of bioactive compounds, particularly proteins and peptides, with potential applications in skin health and the cosmetic industry. This study investigated the antioxidant and anti-aging properties of peptide fractions derived from Spirulina platensis and Chlorella vulgaris. Both microalgae were cultivated, and their proteins were subsequently extracted, enzymatically hydrolyzed with alcalase, and fractionated through ultrafiltration. Alkaline extraction yielded 82% protein from S. platensis and 72% from C. vulgaris. Enzymatic hydrolysis predominantly yielded <3 kDa peptides, which exhibited strong antioxidant activity reaching 78% for 2,2-diphenyl-1-picrylhidrazol (DPPH), 82% for 2,2′-azinobis-3-etilbenzothiazoline-6-sulfonic acid (ABTS), and 74% for ferric reducing antioxidant power (FRAP), with IC₅₀ values as low as 23.44 µg/mL for ABTS inhibition in C. vulgaris. These peptides also significantly inhibited skin-aging enzymes, showing 84% inhibition of elastase, 90% of collagenase, and 66% of tyrosinase. Mass spectrometry and GNPS molecular networking of the <3 kDa fraction identified several di- and tri-peptides, including Lys-Val, Val-Arg, His-Ile, Lys-Leu, Ile-Leu, and Leu-Phe, Tyr-Phe, and Leu-Gly-Leu, potentially contributing to these bioactivities. These findings suggest that the enzymatic hydrolysis of S. platensis and C. vulgaris proteins provides a sustainable and natural source of bioactive peptides for antioxidant and anti-aging applications in food, pharmaceutical, and cosmetic industries. Full article

Collagen peptides, as a natural source of peptides, possess multiple advantages such as anti-aging, anti-inflammatory properties, tissue repair, and the ability to inhibit melanin production. In this study, type I collagen extracted from pig skin was hydrolyzed with 1% and 3% hydrochloric acid, yielding collagen peptides CPH1 and CPH3. The melanin content and tyrosinase activity in B16F10 cells were compared via direct and paracrine action when CPH1 and CPH3 were used to interfere with melanogenesis. It was found that CPH3 significantly inhibited melanogenesis in B16F10 through the paracrine action involving HaCaT keratinocytes. The intracellular melanin content was measured at 65.23 ± 1.30%, and the mRNA levels of tyrosinase and microphthalmia transcription factor in cells were 55.77 ± 6.09% and 50.70 ± 8.18% of the negative control, respectively. Furthermore, pigment deposition assays in zebrafish showed that, at a concentration of 1.0 mg/mL, CPH3 significantly inhibited melanogenesis compared to the negative control. Finally, tyrosinase inhibitory peptides were identified from CPH3 through peptide segment sequence identification and molecular dynamics simulation. The peptides of Nona-AGPPGFPGA, Octa-APGPVGPA, and Octa-GLPGPPGP have a double effect on the inhibition of tyrosinase and melanin content in B16F10 cells. Full article

Tyrosinase is a key enzyme responsible for the formation of melanin (a natural skin pigment with ultraviolet-protection properties). However, some people experience melanin overproduction, so new, safe, and biocompatible enzyme inhibitors are sought. New tripeptide tyrosinase inhibitors were developed using molecular modeling. A combinatorial library of tripeptides was prepared and docked to the mushroom tyrosinase crystal structure and investigated with molecular dynamics. Based on the results of calculations and expert knowledge, the three potentially most active peptides (CSF, CSN, CVL) were selected. Their in vitro properties were examined, and they achieved half-maximal inhibitory concentration (IC₅₀) values of 136.04, 177.74, and 261.79 µM, respectively. These compounds attach to the binding pocket of tyrosinase mainly through hydrogen bonds and salt bridges. Molecular dynamics simulations demonstrated the stability of the peptid–tyrosinase complexes and highlighted the persistence of key interactions throughout the simulation period. The ability of these peptides to complex copper ions was also confirmed. The CSF peptide showed the highest chelating activity with copper. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay confirmed that none of the test tripeptides showed cytotoxicity toward the reconstructed human epidermis. Our results indicated that the developed tripeptides were non-toxic and effective tyrosinase inhibitors. They could be applied as raw materials in skin-brightening or anti-aging cosmetic products. Full article

Collagen is considered to be an intercellular adhesive that prevents tissue stretching or damage. It is widely utilized in cosmetic skin solutions, drug delivery, vitreous substitutions, 3D cell cultures, and surgery. In this study, we report the development of a green technology for manufacturing collagen peptides from flatfish skin using ultrasound and enzymatic treatment and a subsequent assessment on skin functionality. First, flatfish skin was extracted using ultrasound in distilled water (DW) for 6 h at 80 °C. Molecular weight analysis via high-performance liquid chromatography (HPLC) after treatment with industrial enzymes (alcalase, papain, protamex, and flavourzyme) showed that the smallest molecular weight (3.56 kDa) was achieved by adding papain (0.5% for 2 h). To determine functionality based on peptide molecular weight, two fractions of 1100 Da and 468 Da were obtained through separation using Sephadex™ G-10. We evaluated the effects of these peptides on protection against oxidative stress in human keratinocytes (HaCaT) cells, inhibition of MMP-1 expression in human dermal fibroblast (HDF) cells, reduction in melanin content, and the inhibition of tyrosinase enzyme activity in murine melanoma (B16F10) cells. These results demonstrate that the isolated low-molecular-weight peptides exhibit superior skin anti-oxidant, anti-wrinkle, and whitening properties. Full article

Trigonelline (TRG) is a natural polar hydrophilic alkaloid that is found in many plants such as green coffee beans and fenugreek seeds. TRG potentially acts on multiple molecular targets, including nuclear factor erythroid 2-related factor 2 (Nrf2), peroxisome proliferator-activated receptor γ, glycogen synthase kinase, tyrosinase, nerve growth factor, estrogen receptor, amyloid-β peptide, and several neurotransmitter receptors. In this review, we systematically summarize the pharmacological activities, medicinal properties, and mechanistic actions of TRG as a potential therapeutic agent. Mechanistically, TRG can facilitate the maintenance and restoration of the metabolic homeostasis of glucose and lipids. It can counteract inflammatory constituents at multiple levels by hampering pro-inflammatory factor release, alleviating inflammatory propagation, and attenuating tissue injury. It concurrently modulates oxidative stress by the blockage of the detrimental Nrf2 pathway when autophagy is impaired. Therefore, it exerts diverse therapeutic effects on a variety of pathological conditions associated with chronic metabolic diseases and age-related disorders. It shows multidimensional effects, including neuroprotection from neurodegenerative disorders and diabetic peripheral neuropathy, neuromodulation, mitigation of cardiovascular disorders, skin diseases, diabetic mellitus, liver and kidney injuries, and anti-pathogen and anti-tumor activities. Further validations are required to define its specific targeting molecules, dissect the underlying mechanistic networks, and corroborate its efficacy in clinical trials. Full article

Natural and sustainable anti-aging ingredients have gained attention from the cosmetic industry. This study evaluated the anti-aging potential of a sugarcane straw extract-based (SSE) cosmetic ingredient. First, cytotoxicity tests were assessed in keratinocytes and fibroblast cell lines, and sensitization was carried out through the direct peptide reactivity assay. Subsequently, various anti-aging properties were investigated, including inhibiting skin aging-related enzymes, promoting elastin and hyaluronic acid synthesis, and anti-pollution activity. Finally, a permeability assay using a synthetic membrane resembling skin was conducted. The results demonstrated that the SSE ingredient effectively inhibited elastase (55%), collagenase (25%), and tyrosinase (47%) while promoting hyaluronic acid production at non-cytotoxic and low-sensitizer concentrations. Moreover, it reduced the inflammatory response provoked by urban pollution, as evidenced by decreased levels of IL1-α and IL-6. However, it was observed that the phenolic compounds predominantly reached the skin’s surface, indicating a limited ability to penetrate deeper layers of the skin. Therefore, it can be concluded that the SSE ingredient holds anti-aging properties, albeit with limited penetration into deeper skin layers. Further research and formulation advancements are needed to optimize the ingredient’s ability to reach and exert its effects in deeper skin layers. Full article

Liposomes are self-assembled spherical systems composed of amphiphilic phospholipids. They can be used as carriers of both hydrophobic and hydrophilic substances, such as the anti-aging and wound-healing copper-binding peptide, GHK-Cu (glycyl-L-histidyl-L-lysine). Anionic (AL) and cationic (CL) hydrogenated lecithin-based liposomes were obtained as GHK-Cu skin delivery systems using the thin-film hydration method combined with freeze–thaw cycles and the extrusion process. The influence of total lipid content, lipid composition and GHK-Cu concentration on the physicochemical properties of liposomes was studied. The lipid bilayer fluidity and the peptide encapsulation efficiency (EE) were also determined. Moreover, in vitro assays of tyrosinase and elastase inhibition were performed. Stable GHK-Cu-loaded liposome systems of small sizes (approx. 100 nm) were obtained. The bilayer fluidity was higher in the case of cationic liposomes. As the best carriers, 25 mg/cm³ CL and AL hydrated with 0.5 mg/cm³ GHK-Cu were selected with EE of 31.7 ± 0.9% and 20.0 ± 2.8%, respectively. The obtained results confirmed that the liposomes can be used as carriers for biomimetic peptides such as copper-binding peptide and that the GHK-Cu did not significantly affect the tyrosinase activity but led to 48.90 ± 2.50% elastase inhibition, thus reducing the rate of elastin degeneration and supporting the structural integrity of the skin. Full article

Bioactive peptides have gained significant attention in the cosmetic industry due to their potential in enhancing skin health and beauty. These small protein fragments exhibit various biological activities, such as antioxidant, anti-aging, anti-inflammatory, and antimicrobial activities, making them ideal ingredients for cosmetic formulations. These bioactive peptides are classified into four categories: signal, carrier, neurotransmitter-inhibitory, and enzyme-inhibitory peptides. This review provides insight into applying bioactive peptides in cosmetics and their mechanisms of action (e.g., downregulating pro-inflammatory cytokines, radical scavenging, inhibiting collagen, tyrosinase, and elastase synthesis). The abundant natural origins (e.g., animals, plants, and marine sources) have been identified as primary sources for extractions of cosmetic peptides through various techniques (e.g., enzymatic hydrolysis, ultrafiltration, fermentation, and high-performance liquid chromatography). Furthermore, the safety and regulatory aspects of using peptides in cosmetics are examined, including potential allergic reactions and regulatory guidelines. Finally, the challenges of peptides in cosmetics are discussed, emphasizing the need for further research to fully harness their potential in enhancing skin health. Overall, this review provides a comprehensive understanding of the application of peptides in cosmetics, shedding light on their transformative role in developing innovative and effective skincare products. Full article

Marine macroalgae, such as Padina boergesenii, are gaining recognition in the cosmetics industry as valuable sources of natural bioactive compounds. This study aimed to investigate the biochemical profile of P. boergesenii and evaluate its potential as a cosmetic ingredient. Fourier-transform infrared (FTIR), gas chromatography–mass spectrometry (GCMS), and high-resolution liquid chromatography–mass spectrometry quadrupole time-of-flight (HRLCMS QTOF) analyses were employed to assess the functional groups, phycocompounds, and beneficial compounds present in P. boergesenii. Pigment estimation, total phenol and protein content determination, DPPH antioxidant analysis, and tyrosinase inhibition assay were conducted to evaluate the extracts’ ability to counteract oxidative stress and address hyperpigmentation concerns. Elemental composition and amino acid quantification were determined using inductively coupled plasma atomic emission spectrometry (ICP-AES) and HRLCMS, respectively. FTIR spectroscopy confirmed diverse functional groups, including halo compounds, alcohols, esters, amines, and acids. GCMS analysis identified moisturizing, conditioning, and anti-aging compounds such as long-chain fatty alcohols, fatty esters, fatty acids, and hydrocarbon derivatives. HRLCMS QTOF analysis revealed phenolic compounds, fatty acid derivatives, peptides, terpenoids, and amino acids with antioxidant, anti-inflammatory, and skin-nourishing properties. Elemental analysis indicated varying concentrations of elements, with silicon (Si) being the most abundant and copper (Cu) being the least abundant. The total phenol content was 86.50 µg/mL, suggesting the presence of antioxidants. The total protein content was 113.72 µg/mL, indicating nourishing and rejuvenating effects. The ethanolic extract exhibited an IC₅₀ value of 36.75 μg/mL in the DPPH assay, indicating significant antioxidant activity. The methanolic extract showed an IC₅₀ value of 42.784 μg/mL. Furthermore, P. boergesenii extracts demonstrated 62.14% inhibition of tyrosinase activity. This comprehensive analysis underscores the potential of P. boergesenii as an effective cosmetic ingredient for enhancing skin health. Given the increasing use of seaweed-based bioactive components in cosmetics, further exploration of P. boergesenii’s potential in the cosmetics industry is warranted to leverage its valuable properties. Full article

Anti-pigmentation peptides have been developed as alternative skin-lightening agents to replace conventional chemicals that have adverse effects on the skin. However, the maximum size of these peptides is often limited by their low skin and cell penetration. To address this issue, we used our intra-dermal delivery technology (IDDT) platform to identify peptides with hypo-pigmenting and high cell-penetrating activity. Using our cell-penetrating peptides (CPPs) from the IDDT platform, we identified RMNE1 and its derivative RMNE3, “DualPep-Shine”, which showed levels of α-Melanocyte stimulating hormone (α-MSH)-induced melanin inhibition comparable to the conventional tyrosinase inhibitor, Kojic acid. In addition, DualPep-Shine was delivered into the nucleus and regulated the gene expression levels of melanogenic enzymes by inhibiting the promoter activity of microphthalmia-associated transcription factor-M (MITF-M). Using a 3D human skin model, we found that DualPep-Shine penetrated the lower region of the epidermis and reduced the melanin content in a dose-dependent manner. Furthermore, DualPep-Shine showed high safety with little immunogenicity, indicating its potential as a novel cosmeceutical ingredient and anti-pigmentation therapeutic agent. Full article