Collagenase Inhibitor Research Articles

Bioactivities and phenolic composition of Limonium boitardii Maire and L. cercinense Brullo & Erben (Plumbaginaceae): two Tunisian strict endemic plants

ABSTRACT Limonium genus is traditionally used in North Africa for disease treatment and in cosmetic. This study investigates for the first time the antioxidant, anti-inflammatory and enzyme inhibitory activities of two Tunisian endemic plants, L. boitardii and L. cercinense. Analysis of phenolic compounds was carried out by using RP-HPLC. Total phenolic and flavonoid contents, antioxidant activity (antiradical, reducing and total antioxidant activities), tyrosinase and α-glucosidase, collagenase inhibition activities were determined. Inhibiting of NO release in LPS-stimulated macrophages was assessed. L. cercinense exhibited strong antioxidant and anti-inflammatory effects. In the tyrosinase and α-glucosidase inhibitor activity tests, the two species were highly active, especially L. cercinense. High total phenolic and flavonoid contents were recorded in L. cercinense and myricitrin, myricetin, myricetin 3-O-β-D-galatopyranoside, luteolin 7-O-glucoside and rutin were the main phenolics in both species. The results obtained render L. boitardii and L. cercinense as valuable new natural sources for cosmetic and pharmacological applications.

Dietary polyphenol oleuropein and its metabolite hydroxytyrosol are moderate skin permeable elastase and collagenase inhibitors with synergistic cellular antioxidant effects in human skin fibroblasts

Oleuropein (OLE) and hydroxytyrosol (HT) are dietary polyphenols with skin beneficial effects but their effects on skin-ageing-related enzymes are not clear. Herein, we evaluated their inhibitory effects on elastase and collagenase. OLE and HT (62.5–1 000 μM) showed moderate anti-elastase and anti-collagenase effects (5.1–26.3%, 5.8–12.2% and 12.6–31.0%, 11.6–31.9% inhibition, respectively). Combinations of OLE and HT (1:1 ratio) exerted synergistic inhibitory effects on elastase, which were supported by their combination index (CI), kinetic assay and computational docking. Moreover, HT (100 μM) reduced hydrogen peroxide (H2O2)-induced cytotoxicity and reactive oxygen species (ROS) in human dermal fibroblast cells by 21.8 and 15.2%, respectively. In addition, combinations of OLE and HT (6.25/6.25–100/100 μM) exerted synergistic cytoprotective effects by reducing ROS levels by 7.6–37.3% with CIs of 0.17–0.44, respectively. The findings from this study support the cosmeceutical activities of OLE and HT but further research is warranted to evaluate their anti-skin-ageing effects using in vivo models.

Green synthesis of magnesium nanoparticles mediated from Rosa floribunda charisma extract and its antioxidant, antiaging and antibiofilm activities

Flower based nanoparticles has gained a special attention as a new sustainable eco-friendly avenue. Rosa floribunda charisma belongs to modern roses with bright yellow, red flowers with marvellous rose scent. Different methods were used for the extraction of its floral scent such as hexane, microwave, and solid-phase micro-extraction. The latter was the most efficient method for the extraction of phenyl ethyl alcohol, the unique scent of roses. In the current study, magnesium nanoparticles (RcNps) have been synthesized using Rosa floribunda charisma petals that have privileges beyond chemical and physical routs. RcNps formation was confirmed using UV–Visible (UV–Vis) Spectroscopy, Fourier Transform Infrared Spectroscopy (FTIR), High Resolution-Transmission Electron Microscope (HR-TEM), Field Emission-Scanning Electron Microscope (FE-SEM), Energy dispersive X-ray (EDX), X-ray Diffractometer (XRD), and X-ray photoelectron spectroscopy (XPS). HR-TEM images detected the polyhedral shape of RcNps with a diverse size ranged within 35.25–55.14 nm. The resulting RcNps exhibited a high radical scavenging activity illustrated by inhibition of superoxide, nitric oxide, hydroxyl radical and xanthine oxidase by by IC50 values 26.2, 52.9, 31.9 and 15.9 µg/ml respectively as compared to ascorbic acid. Furthermore, RcNps at concentration of 100 µg/ml significantly reduced xanthine oxidase activity (15.9 ± 0.61 µg/ml) compared with ascorbic acid (12.80 ± 0.32 µg/ml) with p < 0.05. Moreover, RcNps showed an excellent antiaging activity demonstrated by inhibition of collagenase, elastase, hyaluronidase and tyrosinase enzymes in a dose-dependent manner with IC50 values of 58.7 ± 1.66 µg/ml, 82.5 ± 2.93 µg/ml, 191.4 ± 5.68 µg/ml and 158.6 ± 5.20 µg/ml as compared to EGCG respectively. RcNps also, exhibited a promising antibacterial activity against three skin pathogens delineate a significant threat to a public health, as Staphylococcus epidermidis, Streptococcus pyogenes, and Pseudomonas aeruginosa with MIC of 15.63, 7.81, 31.25 µg/ml as compared to ciprofloxacin (7.81, 3.9 and 15.63 µg/ml). Moreover, RcNps suppressed the formation of biofilms with minimum biofilm inhibitory concentrations 1.95, 1.95, 7.81 µg/ml against the fore mentioned strains, respectively. Overall, our findings indicate that Rosa floribunda nanoparticles could be used as a leading natural source in skin care cosmetic industry.

(-)-Loliolide Isolated from Sargassum horneri Abate UVB-Induced Oxidative Damage in Human Dermal Fibroblasts and Subside ECM Degradation.

Ultraviolet (UV) B exposure is a prominent cause of skin aging and a contemporary subject of interest. The effects are progressing through the generation of reactive oxygen species (ROS) that alter cell signaling pathways related to inflammatory responses. The present study evaluates the protective effects of (7aR)-6-hydroxy-4,4,7a-trimethyl-6,7-dihydro-5H-1-benzofuran-2-one (HTT) isolated from the edible brown algae Sargassum horneri against UVB protective effects in human dermal fibroblasts (HDFs). HTT treatment dose-dependently suppressed intracellular ROS generation in HDFs with an IC50 of 62.43 ± 3.22 µM. HTT abated UVB-induced mitochondrial hyperpolarization and apoptotic body formation. Furthermore, UVB-induced activation of key nuclear factor (NF)-κB and mitogen-activated protein kinase signaling proteins were suppressed in HTT treated cells while downregulating pro-inflammatory cytokines (interleukin-1β, 6, 8, 33 and tumor necrosis factor-α). Moreover, HTT treatment downregulated matrix metalloproteinase1, 2, 3, 8, 9 and 13 that was further confirmed by the inhibition of collagenase and elastase activity. The evidence implies that HTT delivers protective effects against premature skin aging caused by UVB exposure via suppressing inflammatory responses and degradation of extracellular matrix (ECM) components. Extensive research in this regard will raise perspectives for using HTT as an ingredient in UV protective ointments.

Anti-small cell lung cancer and collagenase inhibition properties of hydroxysafflor yellow A

IntroductionHydroxysafflor yellow A is the major active chemical ingredient of Carthamus tinctorius L. (safflower), which is widely used in patients with cardiovascular and cerebrovascular diseases in China.Material and methodsIn our study, the inhibitory effect of hydroxysafflor yellow A on collagenase showed a lower value, IC50 = 78.81 µg/ml. In the cellular and molecular part of the recent study, the cells treated with hydroxysafflor yellow A were assessed by MTT assay for 48 h as regards the cytotoxicity and anti-small cell lung cancer effects on SBC-3, DMS273, and DMS114 cell lines.ResultsThe viability of small cell lung cancer cell lines decreased dose-dependently in the presence of hydroxysafflor yellow A. The IC50 values of hydroxysafflor yellow A were 539, 432, and 416 µg/ml against SBC-3, DMS273, and DMS114 cell lines, respectively. A molecular docking study was carried out for evaluation of the biological activity of hydroxysafflor yellow A against the collagenase H from Clostridium histolyticum.ConclusionsThe results of the docking calculations revealed the considerable binding affinity of the inhibitor to the enzyme with a docking score of –9.238 (kcal/mol). This remarkable binding affinity could be attributed to the number of hydrogen bonds and hydrophobic contacts, which are 6 and 10, respectively.

Collagenase and Tyrosinase Inhibitory Effect of Isolated Constituents from the Moss Polytrichum formosum.

Mosses from the genus Polytrichum have been shown to contain rare benzonaphthoxanthenones compounds, and many of these have been reported to have important biological activities. In this study, extracts from Polytrichum formosum were analyzed in vitro for their inhibitory properties on collagenase and tyrosinase activity, two important cosmetic target enzymes involved respectively in skin aging and pigmentation. The 70% ethanol extract showed a dose-dependent inhibitory effect against collagenase (IC50 = 4.65 mg/mL). The methanol extract showed a mild inhibitory effect of 44% against tyrosinase at 5.33 mg/mL. Both extracts were investigated to find the constituents having a specific affinity to the enzyme targets collagenase and tyrosinase. The known compounds ohioensin A (1), ohioensin C (3), and communin B (4), together with nor-ohioensin D (2), a new benzonaphthoxanthenone, were isolated from P. formosum. Their structures were determined by mass spectrometry and NMR spectroscopy. Compounds 1 (IC50 = 71.99 µM) and 2 (IC50 = 167.33 µM) showed inhibitory activity against collagenase. Compound 1 also exhibited inhibition of 30% against tyrosinase activity at 200 µM. The binding mode of the active compounds was theoretically generated by an in-silico approach against the 3D structures of collagenase and tyrosinase. These current results present the potential application from the moss P. formosum as a new natural source of collagenase and tyrosinase inhibitors.

A Newfangled Collagenase Inhibitor Topical Formulation Based on Ethosomes with Sambucus nigra L. Extract.

Sambucus nigra L. (S. nigra) is a shrub widespread in Europe and western Asia, traditionally used in medicine, that has become popular in recent years as a potential source of a wide range of interesting bioactive compounds. The aim of the present work was to develop a topical S. nigra extract formulation based on ethosomes and thus to support its health claims with scientific evidence. S. nigra extract was prepared by an ultrasound-assisted method and then included in ethosomes. The ethosomes were analyzed in terms of their size, stability over time, morphology, entrapment capacity (EC), extract release profile, stability over time and several biological activities. The prepared ethosomes were indicated to be well defined, presenting sizes around 600 nm. The extract entrapment capacity in ethosomes was 73.9 ± 24.8%, with an interesting slow extract release profile over 24 h. The extract-loaded ethosomes presented collagenase inhibition activity and a very good skin compatibility after human application. This study demonstrates the potential use of S. nigra extract incorporated in ethosomes as a potential cosmeceutical ingredient and on further studies should be performed to better understand the impact of S. nigra compounds on skin care over the time.

Front Cover: Phosphonate as a Stable Zinc‐Binding Group for “Pathoblocker” Inhibitors of Clostridial Collagenase H (ColH) (ChemMedChem 8/2021)

Front Cover: Phosphonate as a Stable Zinc‐Binding Group for “Pathoblocker” Inhibitors of Clostridial Collagenase H (ColH) (ChemMedChem 8/2021)

Bioactivities of Karanda (Carissa carandas Linn.) fruit extracts for novel cosmeceutical applications.

ABSTRACTThe aim of this research was to determine the total phenolic content (TPC), antioxidation, antiaging, and antibacterial activities of Carissa carandas Linn., and aims at the novel plant sources which is utilized for their cosmeceutical applications. The two conditions (fresh and dried) and three stages (unripe, ripe, and fully ripe) of C. carandas were extracted by ethanolic maceration. Folin–Ciocalteu assay was used for determining the TPC. 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays were used for estimating antioxidant activity. The inhibitory tyrosinase activities were measured using the modified dopachrome assay. Antiaging was evaluated by inhibition of collagenase and elastase, and antibacterial activities. The result of six extracts from C. carandas showed that the highest phenolic content and elastase inhibition of the fresh fruit in fully ripe stage were 100.31 ± 2.64 mg GAE/g extract and 14.11% ± 0.95%, respectively. The fresh fruit in the unripe stage showed that the strongest percentage of DPPH IC50 and collagenase inhibitory activity were 29.11 ± 0.23 μg/mL and 85.94% ± 2.21%, respectively. The ethanolic extract of unripe dried fruit exhibited the highest antioxidant activity in the of ABTS assay, with an IC50 of 0.17 ± 0.01 μg/mL. The MBC displayed the dried fruit ripe stage anti Cutibacterium acnes, Staphylococcus epidermidis, and Staphylococcus aureus strains were 25.0, 25.0, and 16.25 mg/mL, respectively. The fresh fruit in the ripe stage showed that the strongest inhibition tyrosinase was 93.88% ± 5.64%. The conclusion of this research indicates that the fresh fruit of C. carandas fruit extracts has high potential as a novel cosmeceuticals’ applications to antiaging and skin whitening. The dried fruit in ripe stage extract has the most effective ingredient for antiacne products.

Phosphonate as a Stable Zinc-Binding Group for "Pathoblocker" Inhibitors of Clostridial Collagenase H (ColH).

Microbial infections are a significant threat to public health, and resistance is on the rise, so new antibiotics with novel modes of action are urgently needed. The extracellular zinc metalloprotease collagenase H (ColH) from Clostridium histolyticum is a virulence factor that catalyses tissue damage, leading to improved host invasion and colonisation. Besides the major role of ColH in pathogenicity, its extracellular localisation makes it a highly attractive target for the development of new antivirulence agents. Previously, we had found that a highly selective and potent thiol prodrug (with a hydrolytically cleavable thiocarbamate unit) provided efficient ColH inhibition. We now report the synthesis and biological evaluation of a range of zinc‐binding group (ZBG) variants of this thiol‐derived inhibitor, with the mercapto unit being replaced by other zinc ligands. Among these, an analogue with a phosphonate motif as ZBG showed promising activity against ColH, an improved selectivity profile, and significantly higher stability than the thiol reference compound, thus making it an attractive candidate for future drug development.

Evaluation of the efficacy of ethanol leaf extract of Helichrysum petiolare Hilliard and B.L. Burtt against skin aging

Purpose: To determine the efficacy of Helichrysum petiolare ethanol leaf extract against skin aging.Methods: The cytotoxic potential of the plant extract towards human dermal fibroblast (MRHF) cells was determined by Hoechst 33342/Propidium iodide (PI) staining. Effect of H. petiolare extract on reactive oxygen species (ROS) levels in MRHF cells and NO (nitric oxide) production in RAW 246.7 cells activated by LPS (lipopolysaccharides) was investigated. The inhibitory effect of the extract againstcollagenase, elastase, tyrosinase and protein glycation was also evaluated.Results: The extract did not display cytotoxicity towards MRHF cells at the tested concentrations when compared to the trend seen with the untreated control (p &lt; 0.05). The extract caused a significant decrease (p &lt; 0.05) in ROS levels in MRHF cells in a concentration-dependent manner and also demonstrated a reduction in NO production in RAW cells with no toxicity. Furthermore, the extract produced a weak inhibition of collagenase, elastase and tyrosinase activities when compared to the corresponding positive controls, but effectively inhibited protein glycation at the tested concentrations.Conclusion: The findings suggest that the ethanol leaf extract from H. petiolare has the potential to mitigate skin aging and therefore needs to be further investigated for possible clinical applications.&#x0D; Keywords: Cytotoxicity, Efficacy, Helichrysum petiolare, MRHF cells, Oxidative stress, Protein glycation; skin aging

Therapeutic potential of selected South African macrofungi in diabetic wound healing: An in vitro evaluation

Diabetic wounds frequently undergo impaired and prolonged wound healing due to cellular dysfunction. Treatment options, however, remain limited, non-specific, and generally unsuccessful. The potential of medicinal mushrooms in treating several diseases have been exploited by traditional folk medicines for centuries yet very little scientific evidence to support these practices exists. To explore natural products as potential therapeutics to treat diabetic wounds and encourage more research on this topic, this study sought out to screen the potential of four wild mushroom species (Pisolithus tinctorius, Russula capensis, Imleria badia and Pleurotus ostreatus) as suitable diabetic wound healing therapies. This was achieved using various in vitro models characteristic of the diabetic state including LPS and glycated gelatin to mimic bacterial infection and protein glycation, respectively. Activities screened include antioxidant (FRAP and DPPH), collagenase inhibition, immune modulatory capacity in RAW 264.7 macrophages (NO production, NO scavenging, COX-2, M1/M2 polarisation and phagocytosis) as well as MRHF fibroblast migration. In vitro toxicity screening revealed negligible toxicity for all of the tested aqueous and ethanolic extracts with a mildly cytostatic response recorded for P. tinctorius. P. tinctorius also demonstrated strong pro-inflammatory activity in RAW 264.7 macrophages (NO production and COX-2) however, in the presence of LPS the opposite effect was observed owing to strong NO scavenging capabilities while the pro-inflammatory nature of R. capensis aqueous extract was found to be due to the presence of bacterial endotoxins. Overall, different mushroom species presented divergent macrophage responses with the ethanol extract of R. capensis producing the most favourable effects with respect to established diabetic wounds due to its capacity to attenuate inflammation, promote macrophage transition from a pro-inflammatory to a wound healing phenotype, re-establish the phagocytic activity of macrophages and stimulate dermal fibroblast cell migration.

Study on patterned photodynamic cross-linking for keratoconus

PurposeThis study examined the patterned treatment of corneal collagen cross-linking (CXL) for keratoconus to reduce the complications caused by ultraviolet (UV) irradiation. By modifying the method of UV irradiation during the cross-linking process, cross-linking with a special structure is achieved, and the cross-linking effect is analyzed and compared to that of traditional cross-linking. By constructing an animal model of keratoconus, the process and effect of corneal cross-linking can be investigated more fundamentally. These studies provide valuable references for future cross-linking precision improvement and specialization. MethodBy injecting exogenous collagenase into the corneal stroma of rabbits, the balance between collagenase and collagenase inhibitor in the corneal stroma was disrupted, the collagen fiber structure of the cornea was broken to simulate the pathogenesis of keratoconus, and an animal model of keratoconus was thus constructed. Two custom cross-linking patterns were designed with reference to the cable dome structure, and these two special patterns were irradiated and cross-linked by a DMD chip. The cross-linking effect was evaluated by optical coherence tomography (OCT), corneal topography and corneal biaxial tensile tests. The experimental rabbits were divided into four groups: group A, cross-linking of the bird's nest structure; group B, cross-linking of the honeycomb structure; group C, cross-linking of the traditional spot structure; and group D, normal (without modeling and cross-linking). ResultFollowing collagenase treatment, the collagen fiber structure of the rabbit cornea was destroyed, the central thickness of the cornea was reduced, the mechanical properties of the cornea were weakened, and no keratitis, ulcers or haze occurred. After the three cross-linking treatments, the morphology of the cornea improved, the density of the stromal layer increased, and the mechanical properties were enhanced. For the improvement of keratoconus mechanical properties, the average relative difference (Δ) of the four outcome measures was 61.98% for bird's nest cross-linking versus keratoconus (Wilcoxon rank sum test, P = 0.024), 16.13% for honeycomb cross-linking versus keratoconus (Wilcoxon rank sum test, P = 0.025), and 21.07% for traditional spot cross-linking versus keratoconus (Wilcoxon rank sum test, P = 0.014). All these differences are statistically significant. ConclusionAll three methods of cross-linking can improve the morphology and tissue structure of keratoconus and significantly improve the biomechanical properties of the cornea. Among them, the corneal cross-linking of the bird's nest structure attains the best biomechanical properties, followed by the corneal cross-linking of the traditional spot structure and of the honeycomb structure. This suggests that similar or better cross-linking effects can be achieved by designing custom structures with less UV exposure. This provides a direction for future research on better and more accurate pattern cross-linking treatments.

Anti-Aging Potential of Extracts from Washingtonia filifera Seeds.

The aim of this study was to test the inhibitory effect of fruit extracts from Washingtonia filifera on skin aging-related enzymes. The pulp extracts did not exert a significant enzyme inhibition while seed extracts from W. filifera exhibit anti-elastase, anti-collagenase, and anti-tyrosinase activities. Tyrosinase was mildly inhibited while a stronger effect was observed with respect to elastase and collagenase inhibition. Alcoholic extracts provided better results than aqueous extracts. Among them, methanol extracts showed the prominent enzyme inhibitory activities being IC50 value for elastase and collagenase comparable and even better than the reference compound. The inhibition mode of the most active extracts was investigated by Lineweaver-Burk plot analysis. Seed extracts from W. filifera were also investigated for their photo-protective effect by Mansur equation and the antioxidant activity of W. filifera extract was evaluated in oxidative-stressed cells. To evaluate the safety of the extract, the effect on cell viability of human keratinocytes cells was analyzed. Methanol extract presented the best photo-protective effect and exerted an antioxidant activity in a cellular system with no cytotoxic effect. The overall results demonstrate that W. filifera extracts are promising sources of bioactive compounds that could be used in cosmetic and pharmaceutical preparation.

Secondary metabolites changes in germinated barley and its relationship to anti-wrinkle activity

The purpose of this research was to identify metabolite change during barley (Hordeum vulgare) germination and reveal active principles for the anti-wrinkle activity. Barley was germinated with deionized water (DW) and mineral-rich water (MRW) for the comparison of the effect of mineral contents on the metabolites changes during germination. The effects of germinated barley extracts (GBEs) on collagen production and collagenase inhibition were evaluated in vitro using human dermal fibroblasts (HDFs). A pronounced anti-wrinkle activity was observed in the test group treated with the MRW-GBEs. In order to find out the active components related to the anti-wrinkle activity, an orthogonal projection to latent structure-discriminant analysis (OPLS-DA) was performed, using the data from secondary metabolites profiling conducted by UPLC–PDA–ESI–MS. The anti-wrinkle activity of MRW-GBEs was revealed to be associated with the increase of oligomeric compounds of procyanidin and prodelphinidin, indicating that it can be used as an active ingredient for anti-wrinkle agents.

In Vitro Anti-Collagenase Activity and Total Phenolic Content Of Five Selected Herbs: A Review

Etlingera elatior, Persicaria odorata, Centella asiatica, Senna alata and Phyllanthus emblica were reviewed for their in vitro anti-collagenase activity and its total phenolic contents. Plant herbs play a vital role to promote the production of collagen which is the component of the skin. Different solvents during plant extraction and various plant parts were used to determine anti-collagenase properties and total phenolic content. Generally, anti-collagenase assay and Folin-Ciocalteu method were used to determine the anti-collagenase activity and total phenolic content, respectively. The extracts of these herbs have the potential of inhibiting collagenase activity and they possess total phenolic content. The total phenolic was found to be important elements in collagenase inhibition activity other than flavonoid. The selected herbs are popular in Malaysia and this review can be a useful reference or information for future application in pharmaceutical, food and cosmetics fields.&#x0D; Keywords: Anti-collagenase activity, total phenolic contents; plant Extraction; flavonoids

Mycosporine-Like Amino Acids from Marine Resource.

In the last 10 years, a great number of publications (both regular papers and reviews) have been published on the interesting molecules—mycosporine-like amino acids (MAAs). Despite significant advances in the research of MAAs, current overviews in the recent publications involving MAA research still need reporting. The aim of this Special Issue is to join, as an interdisciplinary approach, the photochemical and photobiological aspects, with emphasis on new natural resources to obtain both algae and zooplankton MAAs, advances in methodology of extraction and chemical identification of new MAAs. Finally, this Special Issue reviews the bioactivities of MAAs including UVR screen, antioxidant, immunostimulant, growth factor, DNA protection, inhibition of collagenase, elastase and hyaluronidase, and anti-photoaging, among others, and their potential use as nutracosmeceutic molecules (i.e., oral and topic photoprotector).

IN VITRO ANTI-WRINKLE AND TYROSINASE INHIBITORY ACTIVITIES OF GRAPEFRUIT PEEL and STRAWBERRY EXTRACTS

The research aims to analyse the antioxidant, anti-tyrosinase and anti-wrinkle activities from grapefruit (Citrus Maxima L) and strawberry extracts. Samples were extracted by maceration using 96% ethanol and ethyl acetate, subsequently. The Ferric Reducing Antioxidant Power (FRAP) and β-carotene bleaching (BCB) were used to measure the antioxidant activity. The effect of anti-wrinkle was determined by testing the inhibition of elastase and collagenase enzyme, while anti-tyrosinase activity was analysed using mushroom tyrosinase enzyme. The results showed that strawberry extracts in ethanolic (SE) and ethyl acetate (SEA) have antioxidant activity in FRAP (EC50 = 404.39 ± 3.27 µg / mL and 1978.65 ± 37.25 µg/mL) and BCB (IC50 = 292.30 ± 4.69 µg/mL and 671.11 ± 6.74 µg/mL). Whereas the grapefruit peel extracts both in ethanolic (GPE) and ethyl acetate (GPEA) have antioxidant activity in FRAP (EC50 219.47 ± 71.96 µg / ml and 309.44 ± 95.76 µg/ml) and BCB (EC50 245.19 ± 162.47 µg/ml and 567.54 ± 95.31 µg/ml). As positive standards for FRAP antioxidant analysis were quercetin and vitamin C which has IC50 respectively 18.97 ± 4.50 µg/mL and 24.47 ± 1.44 µg/mL. While in BCB analysis, Butylated Hydroxy Toluene (BHT) used as positive standard (IC50 38.68 ± 5.70 µg/mL). The samples of SE, SEA, GPE and GPEA showed tyrosinase inhibitory activity which the IC50 values were respectively 492.68 ± 1.43; 2658 ± 48.08; 3312.5 ± 222.74; 2985.17 ± 122.80 µg/ml. Kojic acid (IC50 111.52 ± 0.42 µg/ml) is used as positive standard in this study. In addition, SE, SEA, GPE and GPEA were able to inhibit elastase and collagenase enzymes, although their activities were still lower than the positive standard used in this study. Elastastinal in concentration 50 µg/mL giving elastase inhibition about 71.71 ± 0.81 µg/mL, while vitamin C in the same concentration showed collagenase inhibition about 66.79 ± 1.23 µg/mL. It can be concluded that the extract of strawberry and grapefruit peel has antioxidant, anti-tyrosinase and anti-wrinkle activity through inhibition of elastase and collagenase enzymes; thus, they can be used as antiaging cosmetic ingredients.

주정박의 미용 소재로서의 기능성 분석

The purpose of this study is to analyze the functional effects of Dried Distiller's Grains with Solubles (DDGS) as an ethanol-based byproduct in order to find the applicability of DDGS as a cosmetic material and to improve its value. In the anti-oxidation test, based on DPPH and ABTS radical scavenging assay, anti-oxidation activity was found, and ABTS radical scavenging activity was improved. Given that, anti-oxidation effects seemed to be attributable to hydrophilic substances, rather than hydrophobic substances. According to the whitening effect analysis through Tyrosinase inhibition assay, a 25% inhibition activity was found using a concentration of 10㎎/ ㎖. In the collagenase inhibition activity test, for the analysis on the wrinkle-care effect, a 70% inhibition activity was found using a 6㎎/㎖ concentration; in the elastase inhibition activity test, a 96% inhibition activity was found using the 100㎎/㎖ concentration. The water extract from the DDGS sample did not have better whitening or wrinkle-care effects than the positive control group arbutin and EGCG (epigallocatehin gallate). However, when it was compared with brown rice and barley, its anti-oxidation, whitening, and wrinkle-care effects did not fall much. It indicates that DDGS, mainly used as animal feed, is applicable as a cosmetic material.

P.076 Synaptic proteome changes in the hippocampus of prenatally immune-challenged adult mice correspond to behavioural impairments reminiscent of neuropsychiatric developmental disorders

Droplet-based microfluidics holds enormous potential for transforming high-throughput drug screening. Miniaturization through droplets in combination with automation contributes to reduce reagent use and analysis time as well as minimizing or eliminating labor-intensive steps leading to associated reductions in cost. In this paper, we demonstrate the potential of automated and cost-effective microfluidic droplet-generating technology in the context of an enzymatic activity assay for screening collagenase inhibitors. Experimental results show reproducible and accurate creation and mixing of droplet combinations resulting in biochemical data comparable to data produced by an industry standard instrument. This microfluidic platform that can generate and combine multiple droplets represents a promising tool for high-throughput drug screening.