Anti-tyrosinase Effects Research Articles

Antioxidant Activity and Anti-tyrosinase Activity of Nelumbo nucifera Gaertn. Flower Extract Encapsulated in Layered Double Hydroxide

Dermatological problem is mainly caused by reactive oxygen species (ROS) and excessive tyrosinase level in human body. It becomes interesting in the field of biological research which has been attempted to develop new materials from plant extracts to solve this problem. The concern is how those components in the plant extract can be used, protected, and released efficiently during application processes. In this study, we aimed to create a layered double hydroxide (LDH) encapsulating white lotus (Nelumbo nucifera Gaertn.) flower extract (WLE-LDH), investigate the antioxidant and anti-tyrosinase effects of Nelumbo nucifera Gaertn. flower extract encapsulated in the layered double hydroxide (WLE-LDH), and assess the release properties of the nanohybrid. DPPH assay and anti-tyrosinase enzyme assay were performed on methanol extract of N. nucifera and WLE-LDH. The white lotus methanolic extract demonstrated antioxidant activity with an EC50 of 0.17 mg mL-1 and uncompetitive inhibition of tyrosinase with an IC50 of 0.43 mg mL-1. The reconstruction method was used to encapsulate the white lotus flower extract into Mg-Al LDH without isolating the phytochemicals. The successful intercalation of the crude flower extract into the layered structure was confirmed by an increase in the interlayer spacing as indicated by shift in the powder X-ray diffraction pattern. Fourier transform infrared spectroscopy data and SEM image also showed that an encapsulated nanohybrid had been successfully formed. Further, the data of exposure to ultraviolet–visible light suggested that the crude extract of N. nucifera Gaertn. flower was stabilized within the LDH bilayer, protecting its bioactivities. The resulting nanohybrid with bioactive phytoconstituents showed antioxidant activity with an EC50 of 0.58 mg mL-1 and anti-tyrosinase activity with an IC50 of 0.63 mg mL-1. Furthermore, the WLE-LDH sample demonstrated slow and controlled release characteristics with antioxidant activity for up to 3½ h and anti-tyrosinase activity for up to 2½ h. Our findings suggest a promising strategy of its potential applications in the cosmetic and pharmaceutical industries.

Biocompatible Naringin loaded low molecular peptide Nanogels are effective against human melanoma cells.

Melanoma, a type of cancer, has the ability to metastasize and can be fatal. The lack of success in the treatment of melanoma with chemotherapeutic agents and the side effects have led to the search for new agents. Moreover, developing systems that will provide reduce side effects by using biocompatible carriers, may be beneficial. Naringin (NAR), from Citrus plants, has anticancer and anti-inflammatory properties. NAR is useful in formulations where it is used with a carrier due to its low water solubility and bioavailability with few toxicity. This study aimed to evaluate the effects of NAR-loaded peptide based Fmoc-FF nanogels on human melanoma (SK-MEL-30) cells. Characterization of NAR-loaded Fmoc-FF nanogels was carried out. The biocompatibility properties of Fmoc-FF and NAR-loaded nanogels were evaluated in mouse fibroblast (L929) cells, and their cytotoxic effects were evaluated in human melanoma (SK-MEL-30) cells by the MTT method. While the DCF-DA method was used to measure the effects on reactive oxygen species (ROS) release, the changes in oxidative stress biomarkers were examined by spectrophotometric analysis, tyrosinase enzyme activity and inflammation biomarkers were investigated by ELISA method. Comet method was used to evaluate antigenotoxic effects. It has been observed that loading NAR into Fmoc peptide gels may be effective in causing cytotoxic, genotoxic, anti-inflammatory and anti-tyrosinase effects and an increase in ROS release in melanoma cells. These results indicate that NAR-loaded Fmoc-FF gels, which have the feature of easy application to the skin, may be effective in the treatment of melanoma without causing toxic effects.

Phytochemistry, Anti-Tyrosinase, and Anti-Diabetes Studies of Extracts and Chemical Constituents of Dicerothamnus rhinocerotis Leaves

Dicerothamnus rhinocerotis (L.f.) Koekemoer, also known as rhinoceros bush and previously called Elytropappus rhinocerotis (L.f.) Less., is from the Asteraceae plant family. The plant is traditionally used to treat indigestion, stomach ulcers, influenza, and diarrhea. This study was aimed at investigating the phytochemistry, anti-glucosidase, anti-amylase, and anti-tyrosinase effects of D. rhinocerotis as research in this area is limited. The air-dried plant materials were macerated in 80% methanol (MeOH) and fractionated between hexane, dichloromethane (DCM), ethyl acetate (EtOAc), and butanol (BuOH). Column chromatography on silica gel was employed for the isolation of the compounds. A total of six compounds (1–6) were isolated from the fractions viz. acacetin (1), 15-hydroxy-cis-clerodan-3-ene-18-oic-acid (2), acacetin-7-glucoside (3), pinitol (4), apigenin (5), and β-sitosterol-3-O-glycoside (6). Compounds 2–4 and 6 are reported for the first time from this plant. Among the different fractions, the BuOH and EtOAc fractions had strong tyrosinase inhibitory activities with IC50 values of 13.7 ± 1.71 and 11.6 ± 2.68 µg/mL, respectively, while among the isolated compounds, apigenin (5) had the strongest inhibitory activity, with an IC50 of 14.58 µM, which competes favorably with Kojic acid (17.26 µM). The anti-glucosidase assay showed good activity in three of the fractions and compound 5, while the anti-amylase assays did not show significant inhibition activity.

Unveiling the molecular mechanisms of pigmentation control in Queen Loach, Botia dario (Hamilton, 1822): Insights from sesame seed and marigold-induced antityrosinase effects.

Fish pigmentation study can reveal understandings in dermatological research based on functional genomics. Cultured ornamental fish becomes dull coloured and antityrosinase activity through sesame seed may enhance skin colour, which has not been studied. Botia dario is an indigenous fish, having ornamental and aesthetic value and can be studied as a model for fish pigmentation genetics. In this study, fish specimens were fed with 15% marigold petal meal along with 5, 10 and 15% w/w sesame seed in diet. Pigmentation genes, that is, tyr, tyrp1a, asip1, gnaq, kitlga, mc1r, mitf, pax7a, rab38, slc7a11, sox9a, sox10, csf1r, bcdo2 and gsta2 in skin and immunogens, that is, il20, nramp, tlr9 and trail in kidney were studied. Gene expression in tissues revealed enhanced pigmentation and immunity as well as the role of tyr, tyrp1a and asip1 in pigmentation. Immunogenes and blood parameters confirmed the best pigmentation diet. Colorimetric analysis also showed the enhancement of pigmentation. Insights from sesame seed and marigold-induced antityrosinase effects will be applied in aquaculture to develop natural, dietary formulations that will enhance pigmentation in ornamental fish, leading to improved skin colour and market value.

Enhancement of Biological Activities and Phytochemical Compounds of Oryza sativa L. Extract through Probiotic Fermentation

This study aimed to enhance the biological effects and phytochemical content of probiotic fermented red jasmine rice (Oryza sativa L.) extract to apply as a functional ingredient in anti-aging application. In addition, safety evaluation in terms of cytotoxicity and irritation profile were explored. Lactobacillus plantarum and Lactobacillus rhamnosus were used to ferment the aqueous extract of red jasmine rice to produce fermented extracts as BG and LRB, respectively. The biological potentials in terms of antioxidation, anti-enzymatic effects and anti-inflammation with cytotoxicity of fermented extracts were evaluated and compared with nonfermented extract. In addition, alteration in phytochemical constituents of the probiotic-fermented extracts from nonfermented extract were illustrated by synchrotron radiation–based–FTIR microspectroscopy (SR-FT-IR). The results revealed that BG and LRB demonstrated improved antioxidant and anti-tyrosinase effects compared to the control. Additionally, BG and LRB significantly increased the total phenolic contents corresponding to the enhanced biofunctional effects confirmed by SR-FT-IR. Moreover, BG showed a satisfactory safety in human skin cell lines and Hen's egg chorioallantoic membrane. This study implied augmentative effect of probiotic fermentation on the bioactive efficacy of red jasmine rice. Additionally, the safety investigation confirmed that this fermented extract could be used as a functional novel ingredient for anti-aging nutraceutical and cosmetic applications.

Phytochemical Screening of Essential Oils and Ethanolic Extracts of Elsholtzia griffithii Fruits for Cosmeceutical Bioactivity

ABSTRACT The purpose of this study was to examine the chemical composition of essential oil and crude ethanolic extract from the fruits of Elsholtzia griffithii, and to evaluate their cosmeceutical bioactivities such as anti-acne, antioxidant, and anti-tyrosinase effects using in vitro experimental models. The main components of essential oils were neral (48.72%) and geranial (37.34%). Kaempferol, a dietary flavonoid, was found (0.45%) in crude ethanolic extract. The essential oil inhibited Propionibacterium acnes strongly, whereas the crude ethanolic extract demonstrated modest antibacterial action. The essential oil and crude ethanolic extract demonstrated antioxidant and anti-tyrosinase effects.

Evaluation of the bioactivities of turmeric spices of different origins

Our study aimed to compare the in vitro bioactivities of turmeric spice samples obtained from three different sources (India, Pakistan, and Indonesia). Our study involved the determination of total phenolic and flavonoid content, in vitro antioxidant activities, tyrosinase enzyme activity, and antimicrobial activity (Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, and Candida albicans) analyses in three different spice samples. Each spice sample was dissolved in 250 mL of ethanol and stirred on a magnetic stirrer for 36 hours. After filtering out the solid parts, the residues were dissolved again in 250 mL of ethanol separately. This process was repeated three times. After the filtration steps, all filtrates were combined. The remaining solvents in the filtrate were evaporated using an evaporator. The residue of the extracts was placed in Eppendorf tubes and stored in a freezer until use. It has been determined that turmeric of Indian origin, with its high phenolic and flavonoid content, exhibits more potent antioxidant and antityrosinase effects than those from Indonesia and Pakistan. However, antimicrobial activity could not be detected within the studied concentration range of 10 µg/mL to 400 mg/mL.

Evaluation of antioxidant and anti-tyrosinase activities of surfactant and alcohol extracted Combretum Indicum leaves

Combretum Indicum (CI), which contains numerous bioactive compounds, has been used in traditional medicine for a variety of reasons, including the treatment of skin conditions. This study investigates the antioxidant and anti-tyrosinase activities of CI leaves extracted using different surfactants (Triton X-100 and Vitamin E TPGS) at concentrations of 1%, 2%, and 3%, as well as various alcohol solvents (acetone, methanol, and ethanol) at concentrations of 50%, 70%, and 90%. The antioxidant activity of the extracts has been evaluated using Total Phenolic Content (TPC) and 2,2-diphenyl-1-picrylhydrazyl (DPPH), while the anti-tyrosinase activity was assessed through a mushroom tyrosinase inhibition assay. Prior to analysis, CI leaves had been macerated, extracted, and freeze-dried. The research established that ethanol at a concentration of 50% is the optimum solvent to extract CI leaves, as it demonstrated good antioxidant and anti-tyrosinase action with a high percentage of yield and total phenolic content. As a result, the outcomes of this study contribute to a better understanding of the potential applications of CI leaf extract in cosmetics, notably in the treatment of oxidative stress and hyperpigmentation. Further study and development in this field could lead to the creation of effective and natural cosmetic products produced from CI leaves that have antioxidant and anti-tyrosinase effects.

Lycopene-Loaded Solid Lipid Nanoparticles: Preparation, Characterization, ROS-Scavenging, and In vitro Anti-Melanogenesis Evaluations

Background: Lycopene, a natural antioxidant from carotenoids, is produced by plants and microorganisms. It has been investigated in many studies in relation with potential health effects. Objective: Due to the high lipid-solubility of lycopene, its skin penetration is challenged. Therefore, in the present study, lycopene was loaded into lipid nanoparticles to improve penetration and pharmacological properties. Methods: Solid lipid nanoparticles (SLNs) containing lycopene were prepared and anti-tyrosinase properties were studied in the present study. The formulation was investigated in terms of drug release and antityrosinase properties. Determination of encapsulation efficiency was performed directly. Electron microscopy was used to examine the shape of the nanoparticles. Subsequently, the rate of drug release was investigated by the cell diffusion method. The present study applied cytotoxicity tests, cellular tyrosinase inhibition, melanin content, and free radical level to evaluate the effect of formulations on melanogenesis inhibition, and western blot assay was used to determine tyrosinase and MITF levels. Results: The results from particle size investigation for LYC-SLNs were 151.1 ± 2.3, and exploring the data of electron microscopy showed that the shapes of nanoparticles were spherical, and the encapsulation efficiency was 85.76 ± 2.75%. In determining the anti-tyrosinase effects of LYC-SLNs, a significant reduction in cellular tyrosinase activity and melanin and ROS levels were observed; It is also worth noting that LYC-SLNs reduced melanin production with minimal toxicity against melanoma cells. Conclusion: In general, the results confirm that SLNs can be an efficient delivery platform for the topical delivery of lycopene as a natural anti-oxidant and anti-melanogenic agent.

TLC-MS-Bioautographic identification of antityrosinase compounds and preparation of a topical gel formulation from bioactive fraction of RSM optimized alcoholic extract of Rubia cordifolia L. stem.

Rubia cordifolia L., Rubiaceae, is globally reported to treat skin-related problems. The study aimed to assess the antityrosinase potential of RC and the development of gel formulation. AutoDock vina (version V.1.2.0) program package was used for molecular docking to check for the binding affinity of ligands with protein. Response surface methodology (RSM) software was used to optimize extraction parameters for an alcoholic extract of Rubia cordifolia (ARC). The developed HPTLC method for the quantification of purpurin in ARC was validated as per the ICH guidelines, also the bioautographic study for evaluation of antityrosinase effects was performed, anthraquinone enriched fraction (AEF)-loaded gel formulation was developed and so evaluated which could be used to reduce skin pigmentation. Purpurin showed optimum binding affinity (-7.4 kcal/mol) with the molecular target (tyrosinase) when compared to that of standard kojic acid (-5.3 kcal/mol). Quantification of purpurin in ARC, optimized by RSM software was validated and physiologically significant results were observed for the antityrosinase potential of AEF, along with TLC-MS-bioautographic identification for antityrosinase compounds: purpurin (m/z 256.21) and ellagic acid (m/z 302.19). Evaluation of AEF-loaded gel formulation by in vitro and ex vivo permeation studies was performed. ARC extraction parameters optimized by RSM, and bioautographic study helped identify antityrosinase compounds. The development of gel formulation could be a cost-effective option for the treatment of depigmentation in the future.

Unraveling the chemical profile, antioxidant, enzyme inhibitory, cytotoxic potential of different extracts from Astragalus caraganae.

Six extracts (water, ethanol, ethanol-water, ethyl acetate, dichloromethane, and n-hexane) of Astragalus caraganae were studied for their biological activities and bioactive contents. Based on high-performance liquid chromatography-mass spectrometry (HPLC-MS), the ethanol-water extract yielded the highest total bioactive content (4242.90 µg g-1 ), followed by the ethanol and water extracts (3721.24 and 3661.37 µg g-1 , respectively), while the least total bioactive content was yielded by the hexane extract, followed by the dichloromethane and ethyl acetate extracts (47.44, 274.68, and 688.89 µg g-1 , respectively). Rutin, p-coumaric, chlorogenic, isoquercitrin, and delphindin-3,5-diglucoside were among the major components. Unlike the dichloromethane extracts, all the other extracts showed radical scavenging ability in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay (8.73-52.11 mg Trolox equivalent [TE]/g), while all extracts displayed scavenging property in the 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging assay (16.18-282.74 mg TE/g). The extracts showed antiacetylcholinesterase (1.27-2.73 mg galantamine equivalent [GALAE]/g), antibutyrylcholinesterase (0.20-5.57 mg GALAE/g) and antityrosinase (9.37-63.56 mg kojic acid equivalent [KAE]/g) effects. The molecular mechanism of the H2 O2 -induced oxidative stress pathway was aimed to be elucidated by applying ethanol, ethanol/water and water extracts at 200 µg/mL concentration to human dermal cells (HDFs). A. caraganae in HDF cells had neither a cytotoxic nor genotoxic effect but could have a cytostatic effect in increasing concentrations. The findings have allowed a better insight intothe pharmacological potentialof the plant, with respect to their chemical entities and bioactive contents, as well as extraction solvents and their polarity.

Cannabidiol and Minor Phytocannabinoids: A Preliminary Study to Assess Their Anti-Melanoma, Anti-Melanogenic, and Anti-Tyrosinase Properties.

Currently, there is an increased interest from both scientists and consumers in the application of cannabis/hemp/phytocannabinoids in skin-related disorders. However, most previous investigations assessed the pharmacological properties of hemp extracts, cannabidiol (CBD), or tetrahydrocannabinol (THC), with very few studies focusing on minor phytocannabinoids from hemp. In this context, the current work explored the in vitro anti-melanoma, anti-melanogenic, and anti-tyrosinase effects of cannabidiol (CBD) and three minor phytocannabinoids, namely cannabigerol (CBG), cannabinol (CBN), and cannabichromene (CBC). Among the tested human malignant melanoma cells (A375, SH4, and G361), only A375 cells were highly susceptible to the 48 h treatment with the four phytocannabinoids (IC50 values between 12.02 and 25.13 μg/mL). When melanogenesis was induced in murine melanoma B16F10 cells by α-melanocyte stimulating hormone (αMSH), CBD, CBG, and CBN significantly decreased the extracellular (29.76-45.14% of αMSH+ cells) and intracellular (60.59-67.87% of αMSH+ cells) melanin content at 5 μg/mL. Lastly, CBN (50-200 μg/mL) inhibited both mushroom and murine tyrosinase, whereas CBG (50-200 μg/mL) and CBC (100-200 μg/mL) down-regulated only the mushroom tyrosinase activity; in contrast, CBD was practically inactive. The current data show that tyrosinase inhibition might not be responsible for reducing the melanin biosynthesis in α-MSH-treated B16F10 cells. By evaluating for the first time the preliminary anti-melanoma, anti-melanogenic, and anti-tyrosinase properties of CBN and CBC and confirming similar effects for CBD and CBG, this study can expand the utilization of CBD and, in particular, of minor phytocannabinoids to novel cosmeceutical products for skin care.

HPLC/UV Analysis and In Vitro, Promising Antioxidant, Antidiabetic, Anti-Alzheimer, and Anti-Tyrosinase Potentials of the Algerian Pistacia atlantica Desf. Methanolic Extract

The main objective of this work is to evaluate the species Pistacia atlantica by analyzing the chemical composition of the methanolic extract of the plant leaves; then by determining its content on phenolic compounds, flavonoids and condensed tannins; and finally by testing its antioxidant and inhibitory activities against some enzymes involved in several diseases. To identify phenolic compounds, a high-performance liquid chromatography analysis with ultraviolet detector was used; Folin–Ciocalteu trichloroaluminum and vanillin methods were carried out for phenolic compounds, flavonoids, and condensed tannins quantification, respectively. The antioxidant effect was tested by five different methods. Acetylcholinesterase, butyrylcholinesterase, α-glucosidase, and tyrosinase were used to evaluate the inhibitory power of the plant against those enzymes. The results indicated the presence of phenolic compounds in the extract, including phenolic acids and flavonoids. The total phenolic compounds, flavonoids, and condensed tannins contents obtained, respectively, were equal to 36.089 ± 0.047 mg equivalent of galic acid per gram, 0.775 ± 0.01 mg equivalent of quercetin per gram, and 5.44 ± 0.5 mg of equivalent catechin per gram of dry plant. High antioxidant activity was observed and it was expressed by IC50 ranging from 3.50 ± 0.05 to 11.11 ± 4.03 μg/ml and concentrations at absorbance 0.5 from 0.84 ± 0.08 to 54.57 ± 0.24 μg/ml values. Strong antidiabetic effect was recorded which far exceeds the effect of acarbose, and interesting anti-Alzheimer and anti-tyrosinase effects were noted.

Recovery of High Valuable Bioactive Molecules from Vaccinium myrtillus L. Bioresidues

PurposeThe interest in using bioresidues produced by the agri-food industry is increasingly intrinsic to the world economy. As such, researchers started to look for new ways to enhance its use, developing innovations to transform these residues into high-value raw materials with industrial application, promoting the circular economy concept.MethodsTherefore, pruning residues from the production of Vaccinium myrtillus L. could be an interesting exploitation field, given its position as a superfood due to its well-known antioxidant properties. The antioxidant, antibacterial, anti-inflammatory, anti-tyrosinase, and cytotoxicity potentials of aqueous and hydroethanolic extracts of V. myrtillus aerial parts were evaluated.ResultsFrom the obtained results, ultrasound-assisted and maceration extracts were found to be as effective as, if not more effective than, conventional antibiotics against methicillin-resistant Staphylococcus aureus. Aside from antibacterial activity, the extracts also showed antioxidant and anti-tyrosinase effects, which were found to be favourably related to the level of caffeoylquinic acid derivatives.ConclusionThe obtained results highlight the bioactive potential and the importance of exploiting this bio residue as a novel candidate for industrial application, taking advantage of their biological properties.Graphical

Evaluation of anti-oxidant and antimelanogenic effects of the essential oil and extracts of Rosa × damascena in B16F10 murine melanoma cell line.

Rosa × damascena Herrm. belonging to the Rosaceae family has demonstrated anti-inflammatory and anti-oxidant effects previously. Excessive production of free radicals and activation of tyrosinase enzyme caused by UV induces excessive concentration of melanin pigment and skin spots in the long term. Therefore, finding natural sources with anti-oxidant and antityrosinase effects helps to regulate the melanogenesis process. In the current research, we investigated the antimelanogenic, anti-oxidant, and anti-tyrosinase effects of its essential oil, methanol extract (MeOH), and different fractions including n-hexane, dichloromethane (CH2Cl2), n-butanol (BuOH), ethyl acetate (EtOAc), and H2O of R. × damascena in B16F10 cell line. For this purpose, impacts of extracts and essential oil of R. × damascena were investigated on cell viability, cellular tyrosinase, melanin content, mushroom tyrosinase, reactive oxygen species (ROS) production, as well as the amount of tyrosinase protein in the B16F10 murine melanoma cell line. Essential oil, MeOH, and different fractions of R. × damascena were not cytotoxic on B16F10 cells. However, they had significant reducing effects on mushroom tyrosinase activity, melanin content, and ROS production. Also, there is a significant decrease in tyrosinase protein levels at 200 µg/ml but not at other concentrations. Therefore, the essential oil, MeOH, and different fractions of R. × damascena had promising antimelanogenic activity via repression of mushroom tyrosinase activity and ROS production.

Evaluation of the Antioxidant, Cytoprotective and Antityrosinase Effects of Schisandra chinensis Extracts and Their Applicability in Skin Care Product.

Plant extracts have been widely used for skin care for many centuries, and nowadays, they are commonly applied for the development and enrichment of new cosmetic preparations. The present study aimed the assessment of the biological activity of aqueous Schisandra chinensis extracts as a potential ingredient of skin care products. The aspects studied involved the ability to neutralize free radicals, impact on viability and metabolism of keratinocytes, as well as tyrosinase inhibitory potential. Our study showed that aqueous S. chinensis extracts have a positive effect on keratinocyte growth and have high antioxidant potential and strong tyrosinase inhibitory activity. UPLC-MS analysis revealed that three groups of phenolic compounds were predominant in the analyzed extract, including lignans, phenolic acids and flavonoids and protocatechiuc and p-coumaryl quinic acids were predominant. Moreover, microwave-assisted extraction, followed by heat reflux extraction, was the most effective for extracting polyphenols. Furthermore, a prototypical natural body washes gel formulation containing the previously prepared extracts was developed. The irritation potential and viscosity were assessed for each of the formulations. The study demonstrated that the addition of these extracts to body wash gel formulations has a positive effect on their quality and may contribute to a decrease in skin irritation. In summary, S. chinensis aqueous extracts can be seen as an innovative ingredient useful in the cosmetic and pharmaceutical industry.

Study of the Cosmetic Potential Uses of Plants from Mayotte as Skin Care Agents through the Screening of Their Biological Activities

(1) The island of Mayotte, located in the Indian Ocean, possesses remarkable biodiversity. In a previous ethnobotanical study, we already highlighted 69 different plant species used in traditional medicine. Among those, 21 were traditionally employed for skin care by the local populations. The present study aimed to better understand the traditional use of those plants by investigating their in vitro biological activities and, more specifically, their anti-lipoxygenase, antioxidant and anti-tyrosinase properties. (2) These three activities were, respectively, determined by lipoxygenase inhibition, DPPH-reducing potency, and anti-tyrosinase activity assays. (3) Results revealed high biological activities for several plant species, with some of them displaying one strong single activity, while others had at the same time anti-lipoxygenase, antioxidant and anti-tyrosinase effects. (4) Those in vitro biological activities agreed with the traditional use of those plants by the local population. It also highlights the high potential of those species from Mayotte in the development of new cosmetic ingredients for the treatment of many skin affections, such as eczema.

Characteristics and in vitro anti skin aging activity and UV radiation protection of morin loaded in niosomes.

One of the dermatologic problems in elderly people is skin aging, which is a natural and complex biological process. Morin is a flavonoid with high radical scavenging activity as well as antityrosinase effects but its low water solubility has restricted its application. This research aimed to develop, characterize, and optimize morin niosomes composed of non-ionic surfactants, and evaluate the in vitro UV protection and antiaging effectiveness. Niosomes were prepared by the film hydration method with sorbitan monostearate (Span® 40), polyoxyethylenesorbitan monopalmitate (Tween® 40), and cholesterol. The niosomes were characterized in terms of size, zeta potential, morphology, in vitro release behavior, and drug entrapment efficiency (EE). Afterward, antiaging activity, including antityrosinase, antioxidant, intracellular reactive oxygen species (ROS) scavenging, and sun protection factor (SPF) were evaluated. The optimized niosomes appeared as unilamellar vesicles with a spherical shape, with size, zeta potential, and EE values of 6.13 ± 0.40 μm, -0.81 ± 0.32 mV, and 89.35% ± 2.80%, respectively. The noisome formulation remained stable at -4°C for 3 months. The release profiles of morin loaded in niosomes revealed the extended release over 8h and followed zero-order release kinetics. Morin-loaded niosomes exhibited no significant toxicity toward the L929 cell line. The niosome loaded with morin showed anti skin aging activity, including antityrosinase effects (IC50=13.17 ± 1.58 μg/ml), antioxidant (IC50=28.49 ± 2.05 μg/ml), and ROS scavenging activity. For 1% and 5% (w/w) morin niosomes in eucerin base cream, the SPF was 39.03 ± 1.01 and 38.15 ± 0.82, respectively, whereas the noisome-free morin cream exhibited an SPF of 4.47 ± 0.56. Morin-loaded niosome has been shown to provide sun protection and antiaging effects, suggesting that it could be used in pharmaceutical and cosmetic products.

590 Biological and in-silico characterization of pyrazole and pyrazolone derivatives: Identifies novel anti-skin cancer, antioxidant and tyrosinase inhibitory agents

The psychosocial burden akin to cutaneous conditions such as cancer and hyperpigmentation disorders, make their management very sensitive. Current therapeutic interventions, are associated with side-effects, cost, invasiveness and bioavailability issues. Herein, 26 new pyrazole and pyrazolone compounds were synthesized via microwave-assisted reactions and their pharmacokinetic parameters ADMET predicted by in-silico methods. In addition, these compounds were evaluated for their anti-proliferative, antioxidant, anti-tyrosinase effects.

Acylated sucroses and butenolide analog from the leaves of Tripterygium wilfordii Hook. f. and their potential anti-tyrosinase effects

Three undescribed acylated sucroses (1–3), one undescribed butenolide analog (4) along with three known compounds (5–7) were isolated from the aqueous EtOH extract of the dried leaves of Tripterygium wilfordii. Their structures were elucidated on the basis of spectroscopic analyses, electron circular dichroism (ECD) techniques, and saccharide hydrolysis. All the isolated compounds were tested for their anti-tyrosinase effects. Among them, 6 exhibited similar inhibitory effects on tyrosinase with IC50 values of 0.073 mM comparing to arbutin. Additionally, the possible mechanism of the interaction between 6 and the active site of tyrosinase was explored by molecular docking.