Maclura cochinchinensis (Lour.) Corner Heartwood Extracts Containing Resveratrol and Oxyresveratrol Inhibit Melanogenesis in B16F10 Melanoma Cells.

This study aimed to isolate and purify resveratrol and oxyresveratrol from the heartwoods of Maclura cochinchinensis, and to evaluate their inhibitory effects on melanogenesis in B16F10 murine melanoma cells. A methanol maceration process yielded a crude extract comprising 24.86% of the initial mass, which was subsequently analyzed through HPTLC, HPLC, and LC-MS/MS. These analyses revealed the presence of resveratrol and oxyresveratrol at concentrations of 4.32 mg/g and 33.6 mg/g in the extract, respectively. Initial purification employing food-grade silica gel column chromatography separated the extract into two fractions: FA, exhibiting potent inhibition of both tyrosinase activity and melanogenesis, and FM, showing no such inhibitory activity. Further purification processes led to the isolation of fractions Y11 and Gn12 with enhanced concentrations of resveratrol (94.9 and 110.21 mg/g, respectively) and fractions Gn15 and Gn16 with elevated levels of oxyresveratrol (321.93 and 274.59 mg/g, respectively), all of which significantly reduced melanin synthesis. These outcomes affirm the substantial presence of resveratrol and oxyresveratrol in the heartwood of M. cochinchinensis, indicating their promising role as natural agents for skin lightening.

Relationships between degree of polymerization and activities: A study on condensed tannins from the bark of Ficus altissima.

Condensed tannins were isolated from the bark of Ficus altissima and fractionated into four subcomponents on a Sephadex LH-20 column with 60 %, 80 %, 100 % methanol, and 70 % acetone, separately. Their structures were characterized by MALDI-TOF MS coupled with HPLC-ESI-MS and confirmed to be polymers of B-type procyanidin glucosides, procyanidins, and prodelphinidin glucosides. The degree of polymerization (DP) of these polymers was as high as 21, and the mDPs of the four subcomponents were calculated as 2.4, 6.6, 10.5 and 13.4, respectively. They competitively or noncompetitively suppressed the activities of tyrosinase and α-glucosidase through hydrogen bonding and hydrophobic interaction. And they also showed a powerful antioxidative activity. Correlation analyses verified that the anti-tyrosinase capacity exhibited a significant positive correlation (R2monophenolase = 0.9167 and R2diphenolase = 0.9302) with mDP within the methanol-water system, and the anti-α-glucosidase activity also showed a significant positive correlation with the mDP (R2 = 0.9187). In contrast, the antioxidant capability showed a significant negative correlation with the mDP (R2DPPH = 0.9258, R2ABTS = 0.9372). This study confirmed that condensed tannins from the bark of F. altissima were desirable anti-tyrosinase, anti-α-glucosidase, and antioxidant agents, and elucidated the relationships of their mDP (molecular weight) and activities, which provided a scientific basis for the comprehensive utilization of these polymers in the food, cosmetics, medicine and other fields.

Phytochemical profiling, antioxidant, and tyrosinase inhibitory potential of the Acacia cyclops trunk bark: in vitro combined with in silico approach.

The aim of this study was to analyze the phytochemical profile of Acacia cyclops trunk bark ethyl acetate extract using LC-tandem mass spectrometry for the first time, along with evaluating its antioxidant and anti-tyrosinase properties. Consequently, we determined the total phenolic and flavonoid contents of the extract under investigation and identified and quantified 19 compounds, including phenolic acids and flavonoids. In addition to assessing their antioxidant potential against DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2'-azino-bis-[3-ethylbenzothiazoline-6-sulfonic] acid) assays, in vitro and in silico studies were conducted to evaluate the tyrosinase inhibitory properties of the A. cyclops extract. The ethyl acetate trunk bark extract exhibited a substantial total phenolic content and demonstrated significant antioxidant activity in terms of free radical scavenging, as well as notable tyrosinase inhibitory action (half-maximal inhibitory concentration [IC50] = 14.08 ± 1.10 µg/mL). The substantial anti-tyrosinase activity of the examined extract was revealed through molecular docking analysis and druglikeness prediction of the main selected compounds. The findings suggest that A. cyclops extract holds promise as a potential treatment for skin hyperpigmentation disorders.

Isolation, purification, and biological activities of polysaccharides from Amorpha fruticosa flowers.

The extraction, isolation, structural characterisation and biological activities of polysaccharides from Amorpha fruticosa flowers were investigated. First, the crude polysaccharide AFP was extracted, and two major purified polysaccharide fractions AFP-2 and AFP-3 were isolated. The molecular weight and monosaccharide compositions of AFP-2 and AFP-3 were determined. Then the antioxidant activities of AFP, AFP-2 and AFP-3 were assessed by DPPH radical, ß-Carotene bleaching and hydroxyl radical assays. All three tested polysaccharides showed good antioxidant activity while AFP was the strongest one. The study also showed that AFP, AFP-2 and AFP-3 have good tyrosinase inhibition, moisture absorption and retention activities. The results will provide a helpful reference for the application of polysaccharide from Amorpha fruticosa flowers as a natural cosmetic ingredient.

Optimization, Metabolomic Analysis, Antioxidant Potential andDepigmenting Activity of Polyphenolic Compounds fromUnmature Ajwa Date Seeds (Phoenix dactylifera L.) Using Ultrasonic-Assisted Extraction.

This study sought to optimize the ultrasonic-assisted extraction of polyphenolic compounds from unmature Ajwa date seeds (UMS), conduct untargeted metabolite identification and assess antioxidant and depigmenting activities. Response surface methodology (RSM) utilizing the Box-Behnken design (BBD) and artificial neural network (ANN) modeling was applied to optimize extraction conditions, including the ethanol concentration, extraction temperature and time. The determined optimal conditions comprised the ethanol concentration (62.00%), extraction time (29.00 min), and extraction temperature (50 °C). Under these conditions, UMS exhibited total phenolic content (TPC) and total flavonoid content (TFC) values of 77.52 ± 1.55 mgGAE/g and 58.85 ± 1.12 mgCE/g, respectively, with low relative standard deviation (RSD%) and relative standard error (RSE%). High-resolution mass spectrometry analysis unveiled the presence of 104 secondary metabolites in UMS, encompassing phenols, flavonoids, sesquiterpenoids, lignans and fatty acids. Furthermore, UMS demonstrated robust antioxidant activities in various cell-free antioxidant assays, implicating engagement in both hydrogen atom transfer and single electron transfer mechanisms. Additionally, UMS effectively mitigated tert-butyl hydroperoxide (t-BHP)-induced cellular reactive oxygen species (ROS) generation in a concentration-dependent manner. Crucially, UMS showcased the ability to activate mitogen-activated protein kinases (MAPKs) and suppress key proteins including tyrosinase (Tyr), tyrosinase-related protein-1 and -2 (Trp-1 and -2) and microphthalmia-associated transcription factor (MITF), which associated melanin production in MNT-1 cell. In summary, this study not only optimized the extraction process for polyphenolic compounds from UMS but also elucidated its diverse secondary metabolite profile. The observed antioxidant and depigmenting activities underscore the promising applications of UMS in skincare formulations and pharmaceutical developments.

Eleutherococcus divaricatus Fruits Decrease Hyaluronidase Activity in Blood Serum and Protect from Antioxidative Damages in In Vitro Model.

Fruits are very important dietary components and a source of biologically active compounds used in nutritional pharmacology. Particularly due to the presence of polyphenolic compounds, fruits play an important role in the prevention of diseases of civilization. Therefore, it is important to study the phytochemicals and biological activity of fruits, especially those with a long-standing use in ethnomedicine. In this study, we determined the chemical profile and biological activity of a methanolic extract of the Eleutherococcus divaricatus fruits. Amongst nine polyphenols studied, only chlorogenic acid, protocatechuic acid, and eleutheroside E have been detected. The extract showed a weak anti-hyaluronidase activity from bovine testicular in a range of 9.06-37.70% and quite high for human serum hyaluronidase from children diagnosed with acute leukemia in a range of 76-86%. A weak anti-tyrosinase activity was obtained in a range of 2.94-12.46%. Moreover, the extract showed antioxidant properties against DPPH radical, ABTS radical, and O2•-. In addition, the antioxidant activity of the extract was evaluated by FRAP assay and Fe2+ ion chelation assay. These preliminary studies partially justify the traditional use of the plant in inflammatory- and immune-related diseases, in which hyaluronidase and free radicals can participate. A difference in human serum hyaluronidase inhibition may result from the inter-patient variability. Regardless of that, the results mean that polyphenolic compounds may stimulate activity of hyaluronidase, as well as to protect cells from the oxidative damages. However, further studies in ex vivo and in vivo models are needed, including blood isolated from a larger number of patients.

Cytotoxic, antioxidant, and antiglycation activities, and tyrosinase inhibition using silver nanoparticles synthesized by leaf extract of Solanum aculeatissimum Jacq.

The present study aimed to determine the biological properties of an extract of Solanum aculeatissimum aqueous extract (SaCE) alone as well as silver nanoparticles (AgNPs) generated by green synthesis utilizing S. aculeatissimum aqueous extract (SaCE). These synthesized SaCE AgNPs were characterized using UV-VIS spectrophotometry, scanning transmission electron microscopy (TEM), energy dispersive spectroscopy (EDS), zeta potential (ZP), dynamic light scattering (DLS). Determination of total polyphenols, flavonoids, saponins content was conducted. In addition, high performance liquid chromatography-mass spectrometry (HPLC-MS) was employed to identify constituents in this extract. Antioxidant activity was determined by DPPH radical scavenging and ferric ion reducing power (FRAP) methods. Antiglycation activity was demonstrated through relative mobility in electrophoresis (RME) and determination of free amino groups. The inhibitory activity on tyrosinase was also examined. Molecular docking analyses were performed to assess the molecular interactions with DNA and tyrosinase. The antitumor activity SaCE was also measured. Phytochemical analysis of SaCE and AgNPs showed presence polyphenols (1000.41 and 293.37 mg gallic acid equivalent/g), flavonoids (954.87 and 479.87 mg rutin equivalent/g), saponins (37.89 and 23.01% total saponins), in particular steroidal saponins (aculeatiside A and B). Both SaCE and AgNPs exhibited significant antioxidant (respectively, 73.97%, 56.27% in DPPH test, 874.67 and 837.67 µM Trolox Equivalent/g in FRAP test) and antiglycation activities (72.81 and 67.98% free amino groups, results observed in RME). SaCE and AgNPs presented 33.2, 36.1% inhibitory activity on tyrosinase, respectively. In silico assay demonstrated interaction between steroidal saponins, DNA or tyrosinase. SaCE exhibited antitumor action against various human tumor cells. Data demonstrated that extracts SaCE alone and AgNPs synthesized from SaCE presented biological properties of interest for application in new therapeutic formulations in medicine.

Insights on Juniperus phoenicea Essential Oil as Potential Anti-Proliferative, Anti-Tyrosinase, and Antioxidant Candidate.

In this study, the anti-cancer, anti-tyrosinase, and antioxidant activities of essential oils (EOs) of berries and leaves of Juniperus phoenicea grown wild in North of Tunisia were investigated. The EO yields from leaves and berries were 1.69% and 0.45%, respectively. GC-MS analysis revealed that α-pinene is the predominant component in both EOs (44.17 and 83.56%, respectively). Leaves essential oil presented high levels of ß-phellandrene (18%) and camphene (15%). The EOs displayed cytotoxic effects against MCF-7 breast cancer cell, HT-29 colon cancer, and the normal cells H9C2 cardiomyoblasts. Leaves oil strongly inhibited colon cell line proliferation (IC50 of 38 µg/mL), while berries essential oil was more potent against breast cancerous cells MCF-7 (IC50 of 60 µg/mL). Interestingly, berries essential oil exhibited high ability to inhibit melanin synthesis by inhibiting enzyme mono and diphenolase activities. Overall, the results suggested that the two oils are significant sources of healthy natural chemicals.

Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity.

Tyrosinase inhibitors can reduce melanin production for skin whitening, but some existing products may harm the skin. This study discovered six compounds that inhibit tyrosinase in the mushroom Agaricus bisporus by over 50%. Compound 11 displayed strong inhibition (92.2% and 86.7%) for L-tyrosine and L-DOPA substrates, while compound 13 showed high inhibition (96.0% and 62.0%) for both substrates. Molecular docking simulations revealed compounds 11 and 13 bind at the allosteric site of the enzyme. Xanthone derivatives, based on these findings, hold potential as safe skin whitening agents and for pigmentation-related diseases in the cosmetic industry.

Shoot Cultures of Vitis vinifera (Vine Grape) Different Cultivars as a Promising Innovative Cosmetic Raw Material-Phytochemical Profiling, Antioxidant Potential, and Whitening Activity.

The primary purpose of this work was the initiation and optimization of shoot cultures of different Vitis vinifera L. cultivars: cv. Chardonnay, cv. Hibernal, cv. Riesling, cv. Johanniter, cv. Solaris, cv. Cabernet Cortis, and cv. Regent. Cultures were maintained on 30-day growth cycles using two media, Murashige and Skoog (MS) and Schenk and Hildebrandt (SH), with various concentrations of plant growth regulators. Tested media ('W1'-'W4') contained varying concentrations of 6-benzylaminopurine (BA) in addition to indole-3-butyric acid (IBA) and 1-naphthaleneacetic acid (NAA). High performance liquid chromatography coupled with mass spectrometry (UPLC-MS) was used for metabolomic profiling. In all tested extracts, 45 compounds were identified (6 amino acids, 4 phenolic acids, 13 flavan-3-ols, 3 flavonols, and 19 stilbenoids). Principal component analysis (PCA) was performed to assess the influence of the genotype and medium on metabolic content. PCA showed that metabolic content was mainly influenced by genotype and to a lesser extent by medium composition. MS media variants induced the amino acid, procyanidin, and flavan-3-ol production. In addition, the antioxidant potential and anti-tyrosinase activity was measured spectrophotometrically. The studies on antioxidant activity clearly reveal very high efficiency in reducing free radicals in the tested extracts. The strongest tyrosinase inhibition capacity was proved for shoots cv. Hibernal cultured in SH medium and supplemented with NAA, with an inhibition of 17.50%. These studies show that in vitro cultures of V. vinifera cvs. can be proposed as an alternative source of plant material that can be potentially used in cosmetic industry.

Chemical composition, antioxidant and anti-tyrosinase potentials of Acacia cyclops trunk bark using in vitro and in silico approaches.

The purpose of this paper was to evaluate the phytochemical profile of Acacia cyclops trunk bark methanol extract using LC-MS/MS, as well as to assess its antioxidant and anti-tyrosinase activities. Thus, total phenolic and flavonoid contents of the studied extract were established and 19 compounds were detected and quantified. In addition of their antioxidant potential against DPPH and ABTS assays, in vitro and in silico studies were adopted to evaluate tyrosinase inhibitory property of A. cyclops extract. Methanol trunk bark extract showed significant total phenolic content, antioxidant potential in terms of free radical scavenging, as well as an interesting tyrosinase inhibitory action (IC50= 05.12 ± 0.41 µg/mL). The molecular docking analysis and the drug-likeness prediction of the major selected compounds supported the significant anti-tyrosinase activity of the studied extract. The obtained results suggest that A. cyclops extract could be a promising candidate in the treatment of skin hyperpigmentation disorders.

Plant Extracts as Skin Care and Therapeutic Agents.

Natural ingredients have been used for centuries for skin treatment and care. Interest in the health effects of plants has recently increased due to their safety and applicability in the formulation of pharmaceuticals and cosmetics. Long-known plant materials as well as newly discovered ones are increasingly being used in natural products of plant origin. This review highlights the beneficial effects of plants and plant constituents on the skin, including moisturizing (e.g., Cannabis sativa, Hydrangea serrata, Pradosia mutisii and Carthamus tinctorius), anti-aging (e.g., Aegopodium podagraria, Euphorbia characias, Premna odorata and Warburgia salutaris), antimicrobial (e.g., Betula pendula and Epilobium angustifolium), antioxidant (e.g., Kadsura coccinea, Rosmarinus officinalis, Rubus idaeus and Spatholobus suberectus), anti-inflammatory (e.g., Antidesma thwaitesianum, Helianthus annuus, Oenanthe javanica, Penthorum chinense, Ranunculus bulumei and Zanthoxylum bungeanum), regenerative (e.g., Aloe vera, Angelica polymorpha, Digitaria ciliaris, Glycyrrihza glabra and Marantodes pumilum), wound healing (e.g., Agrimonia eupatoria, Astragalus floccosus, Bursera morelensis, Jatropha neopauciflora and Sapindus mukorossi), photoprotective (e.g., Astragalus gombiformis, Calea fruticose, Euphorbia characias and Posoqueria latifolia) and anti-tyrosinase activity (e.g., Aerva lanata, Bruguiera gymnorhiza, Dodonaea viscosa, Lonicera japonica and Schisandra chinensis), as well as their role as excipients in cosmetics (coloring (e.g., Beta vulgaris, Centaurea cyanus, Hibiscus sabdariffa and Rubia tinctiorum), protective and aromatic agents (e.g., Hyssopus officinalis, Melaleuca alternifolia, Pelargonium graveolens and Verbena officinalis)).

Methoxylated Flavonols and ent-Kaurane Diterpenes from the South African Helichrysum rutilans and Their Cosmetic Potential.

Chromatographic fractionation of a methanol extract of Helichrysum rutilans afforded seven known compounds. The isolated compounds were identified as 5,7,8-trihydroxy-3,6-dimethoxyflavone-8-O-2-methyl-2-butanoate (C-1), 5,7-dihydroxy-3,6,8-trimethoxyflavone (C-2), 5-hydroxy-3,6,7,8-tetramethoxyflavone (C-3), 5-hydroxy-3,6,7-trimethoxyflavone (C-4), ent-kaurenoic acid (C-5), ent-kauran-18-al (C-6), and 15-α-hydroxy-(-)-ent-kaur-16-en-19-oic acid (C-7). Compounds C-1-C-4 demonstrated high antioxidant capacities on ORAC hydroxyl radical (2.114 ± 4.01; 2.413 ± 6.20; 1.924 ± 16.40; 1.917 ± 3.91) × 106; ORAC peroxyl radical (3.523 ± 3.22; 2.935 ± 0.13; 2.431 ± 8.63; 2.814 ± 5.20) × 103 µMTE/g; and FRAP (1251.45 ± 4.18; 1402.62 ± 5.77) µMAAE/g, respectively. Moderate inhibitory activities against Fe2+-induced lipid peroxidation were observed for C-1-C-4 as IC50 values of 13.123 ± 0.34, 16.421 ± 0.92, 11.64 ± 1.72, 14.90 ± 0.06 µg/mL, respectively, while their respective anti-tyrosinase activities with IC50 values of 25.735 ± 9.62, 24.062 ± 0.61, 39.03 ± 13.12, 37.67 ± 0.98 µg/mL were also observed. All compounds demonstrated TEAC values within the range of 1105-1424 µMTE/g. The result is an indication that a methanol extract of H. rutilans might possibly be a good source of natural antioxidants against ailments caused by cellular oxidative stress and as inhibitors against skin depigmentation, as well as possible raw materials needed for slowing down perishable agricultural products. This is the first report on the phytochemical and biological evaluation of H. rutilans.

Characterization of biologically active exopolysaccharide produced by Streptomyces sp. NRCG4 and its anti-Alzheimer efficacy: in-vitro targets.

BACKGROUND: Exopolysaccharides are extremely powerful molecules with a wide range of uses in pharmaceuticals due to their structural and compositional complexity. Marine microorganisms often produce bioactive substances with novel functions and structures because of their special living conditions. Polysaccharides from marine microorganisms are of interest to new drug discovery. RESULTS: The current research focused on the isolation of bacteria from Red Sea, Egypt, that have the ability to produce a new natural exopolysaccharide in order to be examined in treating Alzheimer's illness to obviate side effects of synthetic drugs. Properties of exopolysaccharide (EPS) produced by an isolated Streptomyces strain were investigated for its capability to play as anti-Alzheimer. This strain was identified morphologically, physiologically, and biochemically and actually was confirmed by molecularly 16S rRNA analysis as Streptomyces sp. NRCG4 with accession number MK850242. The produced EPS was fractionated by precipitation 1:4 volumes of chilled ethanol and the third major fraction (1:3) listed as NRCG4, and then the functional groups, MW, and chemical evaluation have been detected via Fourier-transform infrared (FTIR), high-performance gel permeation chromatography (HPGPC), and high-performance liquid chromatography (HPLC). The findings showed that NRCG4 was an acidic EPS composed of mannuronic acid, glucose, mannose, and rhamnose in a molar ratio of 1.2:1.5:2.8:1.0, respectively. NRCG4 Mw was determined to be 4.25 × 105 gmol-1 and the Mn to be 1.97 × 105 gmol-1. Also, the NRCG4 included uronic acid (16.0%) and sulfate (0.0%), but no protein was found. In addition, antioxidant and anti-inflammation activity was measured through various methods. This study confirmed that NRCG4 exopolysaccharide exerted anti-Alzheimer's characters via inhibition of cholinesterase and tyrosinase as well as anti-inflammatory and antioxidant abilities. Additionally, it occurred a potential role in the suppression of Alzheimer's disease risk factors through its antioxidant (metal chelation, radical scavenging capability), anti-tyrosinase and anti-inflammatory characteristics. The anti-Alzheimer's disease efficacy of NRCG4 exopolysaccharide may be assigned to its unique determined chemical composition. CONCLUSIONS: The present study highlighted those exopolysaccharides could be harnessed to improve pharmaceutical industry (anti-Alzheimer, anti-tyrosinase, anti-inflammatory, and antioxidant agents).

Variation in Yield, Chemical Composition and Biological Activities of Essential Oil of Three Curcuma Species: A Comparative Evaluation of Hydrodistillation and Solvent-Free Microwave Extraction Methods.

The essential oils of three medicinally important Curcuma species (Curcuma alismatifolia, Curcuma aromatica and Curcuma xanthorrhiza) were extracted using conventional hydro-distillation (HD) and solvent free microwave extraction (SFME) methods. The volatile compounds from the rhizome essential oils were subsequently analysed by GC-MS. The isolation of essential oils of each species was carried out following the six principles of green extraction and comparison was made between their chemical composition, antioxidant, anti-tyrosinase and anticancer activities. SFME was found to be more efficient than HD in terms of energy savings, extraction time, oil yield, water consumption and waste production. Though the major compounds of essential oils of both the species were qualitatively similar, there was a significant difference in terms of quantity. The essential oils extracted through HD and SFME methods were dominated by hydrocarbon and oxygenated compounds, respectively. The essential oils of all Curcuma species exhibited strong antioxidant activity, where SFME was significantly better than HD with lower IC50 values. The anti-tyrosinase and anticancer properties of SFME-extracted oils were relatively better than that of HD. Further, among the three Curcuma species, C. alismatifolia essential oil showed the highest rates of inhibition in DPPH and ABTS assay, significantly reduced the tyrosinase activity and exhibited significant selective cytotoxicity against MCF7 and PC3 cells. The current results suggested that the SFME method, being advanced, green and fast, could be a better alternative for production of essential oils with better antioxidant, anti-tyrosinase and anticancer activities for application in food, health and cosmetic industries.

Photoprotective and Anti-Aging Properties of the Apical Frond Extracts from the Mediterranean Seaweed Ericaria amentacea.

There is a growing interest in using brown algal extracts thanks to the bioactive substances they produce for adaptation to the marine benthic environment. We evaluated the anti-aging and photoprotective properties of two types of extracts (50%-ethanol and DMSO) obtained from different portions, i.e., apices and thalli, of the brown seaweed, Ericaria amentacea. The apices of this alga, which grow and develop reproductive structures during summer when solar radiation is at its peak, were postulated to be rich in antioxidant compounds. We determined the chemical composition and pharmacological effects of their extracts and compared them to the thallus-derived extracts. All the extracts contained polyphenols, flavonoids and antioxidants and showed significant biological activities. The hydroalcoholic apices extracts demonstrated the highest pharmacological potential, likely due to the higher content of meroditerpene molecular species. They blocked toxicity in UV-exposed HaCaT keratinocytes and L929 fibroblasts and abated the oxidative stress and the production of pro-inflammatory cytokines, typically released after sunburns. Furthermore, the extracts showed anti-tyrosinase and anti-hydrolytic skin enzyme activity, counteracting the collagenase and hyaluronidase degrading activities and possibly slowing down the formation of uneven pigmentation and wrinkles in aging skin. In conclusion, the E. amentacea apices derivatives constitute ideal components for counteracting sunburn symptoms and for cosmetic anti-aging lotions.

Antioxidant and anti-melanogenesis activities of extracts from Leonurus japonicus Houtt.

Leonurus japonicus Houtt is an important anti-skin pigmentation herb used in traditional Chinese medicine. However, the molecular basis for this activity is complex and not fully understood. In this study, water and ethanol extracts and polysaccharide extract from L. japonicus (LJPs) were analyzed by LC-MS/MS and HPLC-DAD separately. Cytotoxicity was analyzed by using CCK-8, antioxidant activity using flow cytometer, anti-MMPs, anti-tyrosinase and signalling pathway analysis using Western blotting to investigate their anti-melanogenesis function. The results showed that the water and ethanol extracts contained alkaloids, flavonoids, and phenolic acids. The LJPs mainly contain glucose, fucose, glucuronic acid, mannose, threonine and arginine, and structure characterization by FITR analyses indicated that LJPs have ß- or α-D-glycosidic bonds and contain pyranose rings. The L. japonicus extracts displayed high cell viability at their maximum concentration. The water extract and polysaccharides significantly reduced lipopolysaccharide (LPS)-induced intracellular reactive oxygen species (ROS) content and exhibited a cytoprotective role. Also, these extracts displayed higher matrix metalloproteinase-2 (anti-MMP-2), anti-MMP-9 and anti-tyrosinase activities. Furthermore, the polysaccharides displayed significantly greater inhibitory effect on intracellular ROS and tyrosinase protein expression than α-arbutin and ursolic acid used for the clinical treatment of skin pigmentation. This study also investigated the polysaccharide inhibition of melanin synthesis by repressing the expression of melanocytic lineage-specific transcription factor (MITF) and melanogenic enzymes via modulation of the phosphoinositide 3-kinase (PI3K-Akt-mTOR) and ß-catenin pathways. The overall results indicate that L. japonicus is a promising candidate for anti-pigmentation treatment.

The anti-melanogenic properties of Swietenia macrophylla king.

Fair flawless skin is the goal for some cultures and the development of irregular skin pigmentation is considered an indication of premature skin aging. Hence, there is a rising demand for skin whitening cosmetics. Thus, this research will be focusing on discovering the anti-pigmentation properties of Swietenia macrophylla seeds. Firstly, the seeds were extracted with ethanol and further fractionate based on their polarity before testing them on zebrafish embryos. The ethanolic extract of the seed demonstrated significant inhibition of both tyrosinase activity and melanin production in the embryos. However, after fractionation, the anti-melanogenic ability was observed to have decreased, signifying that the phytocompounds may be synergistic in nature. Still in the proteomic studies the ethanolic extract and its hexane fraction both induced the downregulation of cathepsin LB and cytoskeletal proteins that have connections to the melanogenic pathway, confirming that S. macrophylla seeds do indeed have anti-pigmentation properties that can be exploited for cosmetic use. Next, limonoids (tetranortriterpenoids found in the seed) were tested for their inhibitory effect against human tyrosinase related protein 1 (TYRP-1) via molecular docking. It was found that limonoids have a stronger binding affinity to TYRP-1 than kojic acid, suggesting that these phytocompounds may have the potential in inhibiting pigmentation. However, this still needs further confirmation before these phytocompounds can be developed into a skin whitening agent. Other assays like ex-vivo or 3D human skin culture can also be used to better study the seeds anti-pigmentation effect on humans.

Preparation, antioxidant and tyrosinase inhibitory activities of chitosan oligosaccharide-hydroxypyridinone conjugates.

Two novel chitosan oligosaccharide (COS)-hydroxypyridone (HPO) conjugates were prepared by reacting chitosan oligosaccharide with 2-chloromethyl-5-hydroxypyridone (HPO), which was synthesized by a series of reactions starting from kojic acid. The degree of substitution of COS-HPO2 reached 1.2, with a yield of 74.9%. The structure of the two conjugates (COS-HPO1 and COS-HPO2) was identified by NMR and FT-IR analysis. The two conjugates showed significantly higher free radical (DPPH•, ABTS+• and •OH) scavenging activity and reducing power than those of COS and HPO (p < 0.05). Both COS-HPO1 and COS-HPO2 possessed significantly stronger tyrosinase inhibitory activity than those of COS, with IC50 values of 0.67 and 0.28 mg/mL for monophenolase, 0.73 and 0.30 mg/mL for diphenolase, respectively. In addition, the conjugates were found to be non-toxic to RAW264.7 macrophages and MRC-5 human lung cells. This work proposes a facile method to enhance the oxidative and tyrosinase inhibitory properties of COS.

assessment of antioxidant, neuroprotective, anti-urease and anti-tyrosinase capacities of leaves extracts.

OBJECTIVE: To characterize the chemical profile of methanolic crude extract and its fractions (Ethyl acetate, n-butanol and aqueous) using liquid chromatography-mass spectrometry (LC-MS) analysis, to evaluate their biological and pharmacological properties: antioxidant (1, 1-diphenyl-2-pycrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic) (ABTS), galvinoxyle free radical scavenging, reducing power, phenanthroline and ß carotene-linoleic acid bleaching assays), enzymes inhibitory ability against several enzymes [acetyl-cholinesterase (AChE), buthyrylcholinesterase (BChE), urease and tyrosinase]. METHODS: Secondary metabolites were extracted from Tamarix africana air-dried powdered leaves by maceration, the crude extract was fractionated using different solvents with different polarities (Ethyl acetate, n-butanol and aqueous). The amount of polyphenols, flavonoids and tannins (hydrolysable and condensed) were determined using colorimetric assays. A variety of biochemical tests were carried out to assess antioxidant and oxygen radical scavenging properties using DPPH, ABTS, galvinoxyle free radical scavenging, reducing power, phenanthroline and ß carotene-linoleic acid bleaching methods. Neuroprotective effect was examined against acetylcholinesterase and buthy-rylcholinesterase enzymes. The anti-urease and anti-tyrosinase activities were performed against urease and tyrosinase enzymes respectively. The extract's components were identified using LC-MS and compared to reference substances. RESULTS: The results indicated that Tamarix africana extracts presented a powerful antioxidant activity in all assays and exhibited a potent inhibitory effect against AChE and BChE as well as urease and tyrosinase enzymes. LC-MS analysis identified amount of eight phenolic compounds were revealed in this analysis; Apigenin, Diosmin, Quercetin, Quercetine-3-glycoside, Apigenin 7-O glycoside, Rutin, Neohesperidin and Wogonin in methanolic extract and its different fractions of Tamarix africana from leaves. CONCLUSIONS: Based on these findings, it is reasonable to assume that Tamarix africana could be considered as a potential candidate for pharmaceutical, cosmetics, and food industries to create innovative health-promoting drugs.