الملخص
Epimedin B(EB)is one of the main flavonoid ingredients present in Epimedium brevicornum Maxim.,a traditional herb widely used in China.Our previous study showed that EB was a stronger inducer of melanogenesis and an activator of tyrosinase(TYR).However,the role of EB in melanogenesis and the mechanism underlying the regulation remain unclear.Herein,as an extension to our previous investi-gation,we provide comprehensive evidence of EB-induced pigmentation in vivo and in vitro and eluci-date the melanogenesis mechanism by assessing its effects on the TYR family of proteins(TYRs)in terms of expression,activity,and stability.The results showed that EB increased TYRs expression through microphthalmia-associated transcription factor-mediated p-Akt(referred to as protein kinase B(PKB))/glycogen synthase kinase 3β(GSK3β)/β-catenin,p-p70 S6 kinase cascades,and protein 38(p38)/mitogen-activated protein(MAP)kinase(MAPK)and extracellular regulated protein kinases(ERK)/MAPK pathways,after which EB increased the number of melanosomes and promoted their maturation for melanogenesis in melanoma cells and human primary melanocytes/skin tissues.Furthermore,EB exerted repigmentation by stimulating TYR activity in hydroquinone-and N-phenylthiourea-induced TYR inhibitive models,including melanoma cells,zebrafish,and mice.Finally,EB ameliorated monobenzone-induced depigmentation in vitro and in vivo through the enhancement of TYRs stability by inhibiting TYR misfolding,TYR-related protein 1 formation,and retention in the endoplasmic reticulum and then by downregulating the ubiquitination and proteolysis processes.These data conclude that EB can target TYRs and alter their expression,activity,and stability,thus stimulating their pigmentation function,which might provide a novel rational strategy for hypopigmentation treatment in the pharmaceutical and cosmetic industries.
الملخص
Grewia tenax (Forssk.) Fiori (Malvaceae) grows in the Arabian Peninsula and is used for several medicinal purposes. To characterize the dermatological bioactivities of G. tenax in terms of its antimelanoma, antityrosinase and antioxidant activities. Cytotoxicity was assessed by cell proliferation and mitochondrial viability assays. Ability to inhibit mushroom tyrosinase and scavenge free radicals were evaluated by an enzymatic and DPPH scavenging microtiter assay, respectively. Phytochemical analyses were carried out using TLC, HPLC-UV and NMR. The chloroform extract shown significant cytotoxic activity in terms of mitochondrial viability (43 ± 14 µg/mL). We identified lupeol and b-sitosterol as the main active components for the tyrosinase inhibitory activity of the hexane extract. Scavenging activity of the DPPH· radical was confined to the water extract. Extracts from this plant have the potential to be used as a base in the development of cosmeceutical products intended to whiten skin or to combat radical-induced physiopathological processes.
Grewia tenax (Forssk.) Fiori (Malvaceae) crece en la Península Arábiga y se utiliza con varios fines medicinales. Para caracterizar las bioactividades dermatológicas de G. tenax en cuanto a sus actividades antimelanoma, antitirosinasa y antioxidante; la citotoxicidad se evaluó mediante ensayos de proliferación celular y viabilidad mitocondrial. La capacidad para inhibir la tirosinasa de hongo y eliminar los radicales libres se evaluó mediante un ensayo de microtitulación enzimático y de eliminación de DPPH, respectivamente. Los análisis fitoquímicos se realizaron mediante TLC, HPLC-UV y NMR. El extracto de cloroformo mostró una actividad citotóxica significativa en términos de viabilidad mitocondrial (43 ± 14 µg/mL). Identificamos lupeol y b-sitosterol como los principales componentes activos para la actividad inhibitoria de tirosinasa del extracto de hexano. La actividad depuradora del radical DPPH· se limitó al extracto acuoso. Los extractos de esta planta tienen potencial para ser utilizados como base en el desarrollo de productos cosmecéuticos destinados a blanquear la piel o combatir procesos fisiopatológicos inducidos por radicales.
الموضوعات
Cytotoxins/chemistry , Grewia/chemistry , Saudi Arabia , In Vitro Techniques , Monophenol Monooxygenase/pharmacology , Melanoma/therapy , Antioxidants/pharmacologyالملخص
myrsine coriacea (Sw.) R. Br. ex Roem. & Schult. (Primulaceae) conhecida popularmente como capororoquinha ou capororoca, é amplamente distribuída nas regiões sul e sudeste do Brasil. As espécies desse gênero apresentam um potencial antioxidante e anti-inflamatório, que pode ser acessado na busca de novos ativos para o tratamento de desordens pigmentares da pele. Desta forma, este trabalho teve como objetivos avaliar o potencial antitirosinase e antioxidante de extratos e frações de M. coriacea e identificar os possíveis compostos responsáveis por essas atividades. Foram realizados ensaios para avaliar o potencial antioxidante das amostras através do método do DPPH, enquanto a capacidade hipopigmentante das amostras foi avaliado pela inibição da enzima tirosinase. Como complemento, foram determinados os teores de compostos fenólicos totais e flavonoides através dos métodos colorimétricos empregando o reagente Folin-Ciocalteau e AlCl3. Adicionalmente, os extratos de M. coriacea tiveram avaliados seus potenciais citotóxicos utilizando diferentes linhagens tumorais humanas. O perfil fitoquímico de M. coriacea foi analisado por cromatografia a gás acoplada com espectrometria de massas (CG-EM) e cromatografia em camada delgada (CCD) com padrões. Nessas análises foram identificados 34 compostos, sendo o ácido palmítico e o palmitato de etila os compostos majoritários nas amostras de M. coriacea. O extrato bruto das folhas apresentou o maior teor de fenólicos totais, enquanto a fração de acetato de etila das folhas teve o maior teor de flavonoides. Contudo, o extrato bruto dos frutos apresentou a melhor atividade antioxidante de todas as amostras analisadas, apresentando também a melhor atividade antitirosinase. Dentre os compostos anotados, mandenol, ácido -linoleico e o linolenato de etila foram os compostos considerados como possíveis inibidores da tirosinase, com boa interação molecular com a enzima nas análises de ancoragem molecular in silico. Das amostras analisadas com relação a inibição de crescimento frente as células tumorais, a amostra da fração de clorofórmio das folhas foi a que apresentou potencial antitumoral frente as células de adenocarcinoma de cólon (HCT116)
myrsine coriacea (Sw.) R. Br. ex Roem. & Schult. (Primulaceae) popularly known as capororoquinha or capororoca, is widely distributed in southern and southeastern Brazil. Myrsine species have an antioxidant and anti-inflammatory potential, which can be accessed in the search for new actives for the treatment of skin pigmentation disorders. Thus, this work aimed to evaluate the antityrosinase and antioxidant potential from extracts and fractions of M. coriacea and to identify the probable compounds responsible for these activities. Assays were performed to evaluate the antioxidant potential of the samples using the DPPH method, while the hypopigmentation capacity of the samples was evaluated by the tyrosinase inhibition. As a complement, the amounts of total phenolic compounds and flavonoids were determined through colorimetric methods using the Folin-Ciocalteau reagent and AlCl3. Additionally, M. coriacea extracts had their cytotoxic potential evaluated using different human tumor cell lines. M. coriacea phytochemical profile was obtained by gas chromatography coupled with mass spectrometry (GC-MS) and thin layer chromatography (TLC) with standards. In these analyses, 34 compounds were identified, with palmitic acid and ethyl palmitate as the major compounds in M. coriacea samples. The leaf crude extract presented the highest total phenolics contents, while the leaf ethyl acetate fraction had the highest flavonoid amounts. However, the fruit crude extract showed the best antioxidant and antityrosinase activities of all analyzed samples. Among the annotated compounds, mandenol, -linoleic acid and ethyl linolenate were the compounds considered as putative tyrosinase inhibitors, presenting good molecular interaction with the enzyme active site in the in silico molecular docking analysis. The leaf chloroform fraction was the only sample that showed an antitumor potential against colon adenocarcinoma cells (HCT116)
الموضوعات
Monophenol Monooxygenase/analysis , Primulaceae/metabolism , Myrsine/classification , Fruit/classification , Antioxidants/analysis , Mass Spectrometry/methods , Skin Pigmentation/immunology , Chromatography, Thin Layer/methods , Hypopigmentation/pathologyالملخص
Dracaena cochinchinensis (Lour.) S.C. Chen (Chandaeng) is an important traditional medicinal plant used in ancient Thai household remedies. This research focused on investigating the biological properties, including the antibacterial, anti-tyrosinase, antioxidant activities, and phytochemical characteristics of crude Chandaeng extracts. Dried Chandaeng heartwood powder was extracted using ethanol, methanol, and deionized water. The antibacterial activities of the extracts were then tested against skin pathogens, including Cutibacterium acnes (DMST14916), Staphylococcus epidermidis (TISTR518), and Staphylococcus aureus (TISTR321). The ethanolic extract showed antibacterial activity. In a time-kill assay, all bacteria were completely killed after being exposed to it, while the cell membranes were found to have leaked when viewed under a scanning electron microscope. Antioxidant potential was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2¢-azino-bis -3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. According to the findings, the crude ethanolic extract of Chandaeng showed the highest level of antioxidant activity. Furthermore, the potential of the extract to treat skin hyperpigmentation by inhibiting tyrosinase, an important melanin synthesis enzyme, was determined and the ethanolic extract was found to be an anti-tyrosinase agent. Finally, the crude ethanolic extract showed the highest total phenolic compound and flavonoid content. In conclusion, crude Chandaeng extract showed significant potential in activity against skin pathogenic bacteria, antioxidant activity, and tyrosinase inhibition. These properties of the extract could be applied to skincare cosmetics.
الموضوعات
Monophenol Monooxygenase , Dracaena , Enzyme Inhibitors , Anti-Bacterial Agents , Antioxidantsالملخص
@# Objective: To evaluate the effects of phenolic acids (caffeic, ferulic, and coumaric acids) and flavones (luteolin and apigenin) on the proliferation and melanogenesis in murine melanoma B16-F10 cells. Methods: Cell proliferation was determined after 24 and 48 hours of incubation using MTT assay. The effects of these tested compounds on cell cycle progression were analyzed by flow cytometry. Moreover, the melanin content and tyrosinase activity were measured spectrophotometrically at 475 nm. Results: Luteolin and apigenin exhibited significant anti-proliferative activity against B16-F10 cells, while caffeic, ferulic, and coumaric acids induced slight inhibition after 24 and 48 hours of incubation. The tested compounds disturbed cell cycle progression of B16-F10, by a subsequent decrease in G
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OBJECTIVE To stud y the chemical cons tituents of n-butanol part of Qubai tablet and its pharmacodynamic effect on the model of de melanocyte. METHODS The n-butanol part of Qubai tablet was prepared. The chemical constituents were analyzed by ultra-high performance liquid chromatography-mass spectrometry (UPLC-MS). Taking mice B 16 melanoma cells as the research object ,the de melanocyte model was established and divided into model group ,positive control different concentration groups(8-methoxypsoralen 10,50,100,150,200 μmol/L),solvent group (diluted with DMSO )and Qubai tablet n-butanol part different concentration groups (10,50,100,150,200 μmol/L). The number of cells were observed by inverted microscope ,and the cell proliferation rate ,the rate of melanin production and promotion rate of tyrosinase activity were also detected. RESULTS In the positive and negative ion mode ,53 compounds in the n-butanol part of Qubai tablet were preliminarily determined (29 in the positive ion mode ,33 in the negative ion mode ,overlapping 9),of which coumarins accounted for the largest proportion , followed by flavonoids. The n-butanol part of Qubai tablet could significantly increase the number of cells ,which was positively correlated with the action time and administration concentration. It could significantly increase the proliferation rate of cells ,the rate of melanin production and promotion rate of tyrosinase activity (P<0.01). CONCLUSIONS Coumarins and flavonoids may be the material basis for the anti-vitiligo effect of n-butanol part from Qubai tablet ;anti-vitiligo effect of n-butanol part of Qubai tablet may be realized by promoting tyrosinase activity.
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Abstract Passiflora nitida Kunth, an Amazonian Passiflora species, is little studied, although the specie's high biological potential. Herein the plant's pharmacognostic characterization, extract production, antioxidant potential evaluation, and application of this extract in cosmetic products is reported. The physical chemical parameters analyzed were particle size by sieve analysis, loss through drying, extractive yield, total ash content, laser granulometry, specific surface area and pore diameter (SBET), differential scanning calorimetry, thermogravimetry (TG), and wave dispersive X-Ray fluorescence (WDXRF). Total phenol/flavonoid content, LC-MS/MS analysis, DPPH and ABTS antioxidant radical assays, cytotoxicity, melanin, and tyrosinase inhibition in melanocytes test provided evidence to determine the content of the major constituent. P. nitida dry extract provided a fine powder with mesopores determined by SBET, with the TG curve showing five stages of mass loss. The antioxidant potential ranged between 23.5-31.5 mgâmL-1 and tyrosinase inhibition between 400-654 µgâmL-1. The species presented an antimelanogenic effect and an inhibitory activity of cellular tyrosinase (26.6%) at 25 µg/mL. The LC-MS/MS analysis of the spray-dried extract displayed the main and minor phenolic compounds constituting this sample. The results indicate that P. nitida extract has promising features for the development of cosmetic formulations
الموضوعات
Plant Extracts/analysis , Plant Leaves/adverse effects , Cosmetics/classification , Passiflora/classification , Thermogravimetry/methods , X-Rays/adverse effects , Calorimetry, Differential Scanning/methods , Monophenol Monooxygenase/antagonists & inhibitors , Phenolic Compounds , Melanins , Antioxidants/adverse effectsالملخص
Abstract Because it promotes the lightening of pigment spots, tyrosinase inhibition is one of the mechanisms of depigmenting cosmetic products. Considering the adverse effects produced by synthetic depigmenting actives, the search for new therapeutic options is desirable, and plant extracts are possible candidates for hyperpigmentation treatment. Glycolic extracts of Cecropia pachystachya Trécul are, therefore, the focus of this study. Its chemical characterization, antioxidant activity, tyrosinase inhibition, and cell viability were evaluated. Glycolic extracts were obtained by macerating the leaves of C. pachystachya in grain alcohol and glycerin or propylene glycol. Both had a similar chemical constitution, the glycerin being more efficient in concentrating phenolic compounds and flavonoids. Analyses by UHPLC-MS detected quinic acid, chlorogenic acid isomers, proanthocyanidin dimers type B and C, catechin/epicatechin, orientin/isoorientin, isoorientin 2"-O-xyloside, vitexin/isovitexin, and rutin. 5-O-caffeoylquinic acid was then quantified was then quantified, with predominance in the extract produced with propylene glycol. These extracts showed a high antioxidant capacity by the method of DPPH, ß-carotene, and nitric oxide. As for depigmenting activity, both extracts were able to inhibit tyrosinase. Cell viability assay also revealed that the extracts could safely be used in concentrations of ≤ 125 µg/mL. Thus, this study demonstrated for the first time that the glycolic extracts of C. pachystachya have promising chemical and biological characteristics for the development of a multifunctional cosmetic with antioxidant and tyrosinase-inhibition activities
الموضوعات
Cosmetics/classification , Cecropia Plant/adverse effects , Bleaching Agents/classification , Skin Cream/analysis , Plant Extracts/adverse effects , Antioxidants/pharmacologyالملخص
O Brasil é o país que possui a maior diversidade de bambus em todo o continente americano, com mais de 200 espécies catalogadas. Devido à alta resistência e durabilidade, essas espécies são muito utilizadas na construção civil e confecção de móveis e utensílios. No entanto, faltam estudos que investiguem a composição química e as atividades biológicas. Neste projeto foram avaliados extratos etanólicos de folhas e colmos de Guadua chacoensis (Rojas) Londoño & P.M. Peterson e frações em hexano, clorofórmio, acetato de etila e n-butanol. Também se obteve o óleo volátil, mas com um rendimento extremamente baixo (0,00079%). As frações dos extratos apresentaram teores de compostos fenólicos variando entre 1,92 e 15,80 µg EAG/mg. Esses compostos mostraram-se mais abundantes nas amostras de colmos. Em relação ao teor de flavonoides, as folhas apresentaram maior quantidade, variando entre 0,39 e 1,18 µg EQ/mg contra 0,17 a 0,34 µg EQ/mg nos colmos. Investigou-se a atividade antimicrobiana dos extratos, frações e óleo volátil frente cinco microrganismos: Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans e Aspergillus brasiliensis. As amostras demonstraram potencial inibitório moderado a bom contra S. aureus e C. albicans, porém fraca para as demais espécies. Testou-se a capacidade antioxidante frente o radical DPPH e os resultados indicaram atividade antioxidante significativa, especialmente as frações acetato e butanol de colmos. As folhas apresentaram EC50 variando entre 67,5 e 124,0 µg/mL e os colmos entre 40,2 e 124 µg/mL. A inibição da enzima tirosinase, que está associada à produção de melanina, também se mostrou boa a uma concentração de 1 mg/mL, com o extrato bruto de colmos apresentando 43% de inibição, seguido pelas frações acetato (36%) e n-butanol (38%) de folhas. As análises por CG-MS detectaram pelo menos 44 compostos diferentes no óleo volátil, com vários terpenos e sesquiterpenos, e com ß-ionona sendo o componente majoritário (8,75%). As amostras de colmos e folhas apontaram grande diversidade de compostos, cerca de 20 para cada fração, onde os ácidos graxos como ácido palmítico e linoleico e seus ésteres derivados foram os mais abundantes. A análise dos perfis cromatográficos por CCD e CLAE revelaram a presença de ácido p-cumárico nos colmos de G. chacoensis. Esse composto tem relevante atividade antioxidante e de inibição da tirosinase. Também foi possível identificar a quercetagetina-7-O-glicosídeo, uma flavona glicosilada, com propriedades anti-inflamatorias e antidiabéticas. Desta forma, constatou-se que G. chacoensis apresenta grande diversidade de metabólitos secundários com atividades biológicas relevantes, como atividade antioxidante e clareadora, abrindo caminho para investigações mais profundas de suas aplicações, especialmente no segmento de cosméticos e produtos naturais
Brazil is the country with the greatest diversity of bamboo in the entire American continent, with more than 200 species catalogued. Due to their high resistance and durability, they are widely used in home construction and manufacture of furniture and utensils. However, studies investigating chemical composition and biological activities are absent. In this project, ethanol extracts from leaves and stems of Guadua chacoensis (Rojas) Londoño & P.M. Peterson and fractions in hexane, chloroform, ethyl acetate and n-butanol were evaluated. Volatile oil was also obtained, but with an extremely low yield (0.00079%). The fractions of the extracts presented contents of phenolic compounds varying between 1.92 and 15.80 µg GAE/mg. These compounds were more abundant in culm samples. In relation to the flavonoid content, leaves showed a greater amount, varying between 0.39 and 1.18 µg QE/mg against 0.17 to 0.34 µg QE/mg in culms. The antimicrobial activity of extracts, fractions and volatile oil were investigated against five microorganisms: Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans and Aspergillus brasiliensis. The samples showed moderate to good inhibitory potential against S. aureus and C. albicans, but weak for the other species. The antioxidant capacity was tested against the DPPH radical and the results indicated significant antioxidant activity, especially acetate and butanol culm fractions. The leaves presented EC50 varying between 67.5 and 124.0 µg/mL and culms between 40.2 and 124 µg/mL. The inhibition of the enzyme tyrosinase, which is associated with the production of melanin, was also shown to be good at a concentration of 1 mg/mL, with the raw culm extract showing 43% inhibition, followed by acetate (36%) and n-butanol (38%) fractions of leaves. CG-MS analysis detected at least 44 different compounds in volatile oil, with several terpenes and sesquiterpenes, and with ß-ionone being the major component (8.75%). Culm and leaf samples showed great diversity of compounds, about 20 for each fraction, where fatty acids such as palmitic and linoleic acid and their derivative esters were the most abundant. The analysis of the chromatographic profiles by TLC and HPLC revealed the presence of p-coumaric acid in culms of G. chacoensis. This compound has relevant antioxidant and tyrosinase inhibiting activity. It was also possible to identify quercetagetine-7-O-glucoside, a glycosylated flavone, with anti-inflammatory and anti-diabetic properties. Thus, it was found that G. chacoensis presents a great diversity of secondary metabolites with relevant biological activities, such as antioxidant and whitening activity, opening ways for deeper investigations of its applications, especially in the segment of cosmetics and natural products
الموضوعات
Aspergillus/metabolism , Plant Extracts/agonists , Bambusa/adverse effects , Poaceae/chemistry , Antioxidants/analysis , Oils, Volatile/analysis , Chromatography, High Pressure Liquid/instrumentation , Monophenol Monooxygenase/classification , 1-Butanol , Bambusa/chemistryالملخص
The objective of this study was to evaluate biological and phytochemical properties of the aqueous extract from the leaves of Miconia chamissois Naudin (AEMC). Phytochemical properties were assessed by analyzing the chromatographic profile and the polyphenol content of AEMC. Biological properties evaluation was conducted based on cytotoxicity assay and by evaluating the antioxidant, antimicrobial, and enzymatic inhibition activities. Results indicated the presence of phytochemicals in AEMC such as flavonoids and polyphenols, including rutin, isoquercitrin and vitexin derivatives. AEMC showed antioxidant activity, which may be attributed to the high polyphenolic content. Moreover, AEMC demonstrated in vitro enzyme inhibition activity against tyrosinase and alpha-amylase, as well as showed low cytotoxicity. On the other hand, AEMC exhibited weak antimicrobial activity against S. aureusand C. albicans. Thus, AEMC is a promising alternative in search of potential drugs for the treatment of diseases induced by oxidative stress and inflammation, conditions due to hyperpigmentation processes, such as melisma, as well as for diabetes.
El objetivo de este estudio fue detectar las propiedades biológicas y fitoquímicos del extracto acuoso de las hojas de Miconia chamissois Naudin (AEMC). Las propiedades fitoquímicas se evaluaron analizando el perfil cromatográfico y el contenido de polifenoles de AEMC. La evaluación de las propiedades biológicas se realizó en base al ensayo de citotoxicidad y evaluando las actividades de inhibición antioxidante, antimicrobiana y enzimática. Los resultados indicaron la presencia de fitoquímicos en AEMC, como flavonoides y polifenoles, que incluyen derivados de rutina, isoquercitrina y vitexina. AEMC mostró una actividad antioxidante considerable, que puede atribuirse al alto contenido polifenólico. Además, AEMC exhibió actividad de inhibición enzimática in vitro contra tirosinasa y alfa-amilasa, así como mostró baja citotoxicidad. Por otro lado, AEMC demostró actividad antimicrobiana débil contra S. aureusy C. albicans. Por lo tanto, AEMC es una alternativa prometedora en busca de posibles drogas para el tratamiento de enfermedades inducidas por el estrés oxidativo y la inflamación, afecciones debidas a procesos de hiperpigmentación, como el melasma, así como para la diabetes.
الموضوعات
Plant Extracts/pharmacology , Plant Extracts/chemistry , Melastomataceae/chemistry , Flavonoids/analysis , Chromatography, High Pressure Liquid , Chromatography, Thin Layer , Monophenol Monooxygenase/antagonists & inhibitors , alpha-Amylases/antagonists & inhibitors , Polyphenols/analysis , Anti-Infective Agents/pharmacology , Antioxidants/pharmacologyالملخص
Abstract Introduction: Avocado (Persea americana Mill.) is a member of Lauraceae with one-seeded berry fruit and cultivated in all tropical, subtropical regions in the world and in the Southern coast region of Turkey. Oxidative damage caused by UV can trigger inflammation, resulting in serious inflammatory skin diseases including eczema, seborrheic dermatitis, hyperpigmentation and ageing. Enzyme inhibitors involved in melanogenesis, such as tyrosinase, have been used recently for hyperpigmentation and skin diseases in cosmetic products. Objective: This study aimed to evaluate the antioxidant, anti-inflammatory, anti-tyrosinase activities and total polyphenolic contents of the different parts of P. americana fruit. Methods: The fruit was divided into exocarp, mesocarp, seed, and then methanol and n-hexane extracts were prepared. DPPH and ABTS free radical scavenging capacities and inhibitory potentials on lipid peroxidation were determined to investigate the antioxidant potentials of the extracts. Anti-inflammatory activities of the extracts were evaluated by measuring the stabilization level of the human red blood cell membrane. The tyrosinase inhibitory activities of the samples were determined using mushroom tyrosinase. Results: In general methanol extracts possessed remarkable higher DPPH free radical scavenging activities than n-hexane extracts. The highest activity was determined in methanol extracts of seed (4.17 ± 0.04 mg/mL) followed by exocarp (5.25 ± 0.05 mg/mL). Overall methanol extracts possessed higher ABTS free radical scavenging activities than n-hexane extracts. The greatest ABTS free radical scavenging activity was obtained in methanol extracts of seed (0.03 ± 0.01 mg/mL). In the anti-lipid peroxidation assay, the greatest activity was noticed in methanol extracts of seed (7.71 ± 0.36 µg/mL) followed by exocarp (12.12 ± 0.34 µg/mL), while all n-hexane extracts were inactive. Overall methanol extracts exhibited higher anti-inflammatory and antioxidant properties than n-hexane extracts. However, the maximum anti-tyrosinase activity was determined in n-hexane extracts of exocarp (0.40 ± 0.01 mg/mL) followed by seed (0.46 ± 0.01 mg/mL). Conclusions: These extracts are promising candidates for use as natural products-based antioxidant and anti-inflammatory properties in inflammation-related disease, and also anti-tyrosinase properties in dermatological applications.
Resumen Introducción: El aguacate (Persea americana Mill.) es un miembro de Lauraceae, es una baya de una semilla que se cultiva en todas las regiones tropicales y subtropicales del mundo y la región costera sur de Turquía. El daño oxidativo causado por los rayos ultravioleta puede desencadenar inflamación, lo que posteriormente da como resultado enfermedades inflamatorias graves de la piel como eccema, dermatitis seborreica, hiperpigmentación y envejecimiento. Los inhibidores de enzimas implicados en la melanogénesis, como la tirosinasa, se han utilizado recientemente para la hiperpigmentación y enfermedades de la piel en productos cosméticos. Objetivo: Evaluar las actividades antioxidantes, antiinflamatorias, antitirosinasas y los contenidos polifenólicos totales de las partes del fruto de P. americana. Métodos: El fruto se dividió en tres partes: exocarpio, mesocarpio y semilla, y se prepararon extractos de metanol y n-hexano. Se determinaron las capacidades de eliminación de radicales libres de DPPH y ABTS y los potenciales inhibidores sobre la peroxidación de lípidos para investigar los potenciales antioxidantes de los extractos. Las actividades antiinflamatorias de los extractos se evaluaron midiendo el nivel de estabilización de la membrana de los glóbulos rojos humanos. Las actividades inhibidoras de tirosinasa de las muestras se determinaron utilizando tirosinasa de hongos. Resultados: En general, los extractos de metanol poseían actividades de eliminación de radicales libres de DPPH notablemente más altas que los extractos de n-hexano. La actividad más alta se presentó en extractos metanólicos de semilla (4.17±0.04 mg/mL) seguido del exocarpio (5.25±0.05 mg/mL). En general, los extractos de metanol poseían una mayor actividad de eliminación de radicales libres ABTS que los extractos de n-hexano. La mayor actividad captadora de radicales libres de ABTS se obtuvo en extractos metanólicos de semilla (0.03±0.01 mg/mL). En el ensayo de anti-peroxidación lipídica, la mayor actividad se observó en los extractos metanólicos de semillas (7.71±0.36 µg/mL) seguidos del exocarpio (12.12±0.34 µg/mL), mientras que todos los extractos de n-hexano estaban inactivos. En general, los extractos de metanol exhibieron mayores propiedades anti-inflamatorias y antioxidantes que los extractos de n-hexano. Sin embargo, la actividad anti-tirosinasa máxima se determinó en extractos de exocarpio de n-hexano (0.40±0.01 mg/mL) seguido de semillas (0.46±0.01 mg/mL). Conclusiones: Estos extractos son candidatos prometedores como productos naturales debido a sus propiedades antioxidantes y antiinflamatorias para tratar enfermedades relacionadas con la inflamación, y también propiedades antitirosinasas en aplicaciones dermatológicas.
الموضوعات
Persea/chemistry , Antioxidants , Skin , Additives in Cosmetics , Anti-Inflammatory Agentsالملخص
Sophorae Flavescentis Radix,derived from the root of Sophora flavescens in the Leguminosae family,has been widely used in the medicine,agriculture,animal husbandry,and daily chemical industry. A pharmacophore model-based method for rapid discovery of tyrosinase inhibitors( TIs) from S. flavescens was established by molecular docking under Lipinski rules,and verified by enzyme assays. Briefly,the chemical constituent database of S. flavescens( CDSF) was established based on the previous papers. Theoptimal pharmacophore model( OPM) was constructed by DS 2019 on the basis of known active TIs. Eighty-three hits predominated by flavonoids having higher fitting scores with OPM than the positive control were screened out,and subjected to molecular docking based on the three-dimensional structure of tyrosinase crystal protein. The potential TIs such as kurarinone and nor-kurarinone were rapidly discovered from the compounds with higher docking scores than the positive control under the Lipinski rules. The results were verified by the in vitro enzyme assays. The inhibition activities of tyrosinase from non-medicinal parts of S. flavescens were also tested to explore the relationship between the inhibition activity and chemical compositions. This study is expected to provide data support for the comprehensive application and development of S. flavescens and also a new method for the rapid discovery of active substances or functional constituents in the complex systems.
الموضوعات
Animals , Flavonoids , Molecular Docking Simulation , Monophenol Monooxygenase , Plant Extracts/pharmacology , Plant Roots , Sophoraالملخص
A clinical case in which skin and hair color change occurred after sacrococcygeal epidural anesthesia in a nine-month-old Siamese cross queen undergoing ovariohysterectomy (OHE) is described. Six weeks after surgery, during a re-check, it was noted that in the sacrococcygeal region the color of the skin and new hair growth was dark with a color comparable to the color present on the body extremities (muzzle, pinnae, legs, and tail). The skin and new hair growth of the shaved abdomen presented a standard color. The key enzyme of the melanogenic pathway in mammals is tyrosinase (TYR), and the Siamese temperature-sensitive phenotype is the result of genetic mutations that makes TYR function thermolabile. The activity of TYR in these cats is limited to the extremities where the temperature is lower while pigment production is impaired in the other body areas. The trichotomy of the sacrococcygeal region performed during wintertime in an outdoor cat was probably the trigger for increased activity of TYR in this area promoting pigment production. The absence of the same alterations in the abdominal area may be justified by less exposure of that region to the external environment, as well as to the feline habits of sedentarism, that avoid significant cooling in these regions. This report highlights the importance of taking this type of occurrence into account when performing an epidural in the Siamese cat breed. Also, to avoid skin color change in this breed, the authors recommend a midline abdominal instead of a flank approach to perform OHE.(AU)
Descreve-se um caso clínico no qual ocorreu mudança na cor da pele e do pelo após anestesia epidural sacrococcígea numa gata cruzada de raça Siamês de nove meses submetida à ovariohisterectomia (OVH). Seis semanas após a cirurgia, durante uma avaliação pós-operatória, notou-se que na região sacrococcígea, a cor da pele e o crescimento do pelo apresentavam uma cor escura, comparável à das extremidades do corpo (face, orelhas, membros e cauda). A pele e o crescimento do pelo do abdómen, que também havia sido tosquiado, apresentavam uma cor padrão. A enzima chave da via melanogênica em mamíferos é a tirosinase (TYR) e o fenótipo siamês sensível à temperatura é o resultado de mutações genéticas que tornam a função TYR termolábil. A atividade da TYR nestes gatos é limitada às extremidades onde a temperatura é mais baixa, enquanto a produção de pigmento é prejudicada em outras áreas do corpo. A tricotomia da região sacrococcígea realizada durante o inverno nesta gata com acesso livre ao ambiente externo, provavelmente determinou um aumento da atividade da TYR nesta área, promovendo a produção de pigmento. A ausência das mesmas alterações na região abdominal pode ser justificada pela menor exposição desta área do corpo ao ambiente externo, também devido aos hábitos felinos de sedentarismo, que evitam resfriamento significativo nestas regiões. Este relato destaca a importância de se levar em consideração a possibilidade deste tipo de ocorrência quando da realização de uma anestesia epidural nesta raça de gatos. Além disso, os autores recomendam uma abordagem abdominal na linha média ao invés de uma abordagem de flanco para realizar a OVH nesta raça, a fim de evitar a alteração da cor da pele.(AU)
الموضوعات
Animals , Cats , Cats , Clinical Laboratory Techniques , Anesthesia, Epidural/veterinary , Sacrococcygeal Region , Hair Removalالملخص
Objective: The objectives of this study were to quantify γ-oryzanol in an ethanolic extract of Oryza sativa L. Indica (black rice) bran and to evaluate its activity as a tyrosinase inhibitor. Methods: Black rice bran was extracted via maceration in 96% ethanol, and the γ-oryzanol concentration in the extract was measured through high-performance liquid chromatography. The applicability of the extract as a skin lightening agent was determined by evaluating its tyrosinase inhibition activity. Results: The dry rice bran contained 118.572 mg/g of γ-oryzanol, and the extract inhibited tyrosinase activity at an IC50 of 74.8%. Conclusion: The black rice bran extract was sufficiently potent for use in skin lightening formulations.
الملخص
Cellular oxidative stress is caused by an imbalance in the redox status and manifests as hyperpigmentation disorders.Reactive oxygen species, particularly hydrogen peroxide (H2O2) as the highly reactive hydroxyl radicals, promotethe melanin production through the induction of tyrosinase enzyme activity. In this study, the antioxidant activity ofoxyresveratrol was investigated by 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays. In addition, melanin biosynthesis, tyrosinase activity, and cellular oxidants due to thebioactive component, oxyresveratrol, were determined in B16 cells by melanin content assay, cellular tyrosinase activityassay, and the dichloro-dihydro-fluorescein diacetate (DCFH-DA) assay, respectively. Hydrogen peroxide induced themelanogenesis through tyrosinase activity-related cellular oxidants, whereas oxyresveratrol showed a potent antioxidantactivity by DPPH and ABTS assays. At the concentrations of 10 and 12.5 µg/ml, oxyresveratrol significantly inhibitedmelanogenesis in B16 melanoma cells and also suppressed tyrosinase activity and cellular oxidants. Effective doses ofoxyresveratrol inhibit melanogenesis through bioactivity of cellular tyrosinase-related oxidative stress
الملخص
Dentre os crocodilianos com ocorrência no Brasil, o Caiman crocodilus (Linnaeus, 1758) é a espécie de maior frequência, porém sua presença em estudos científicos restringe-se a levantamentos faunísticos, na maioria das vezes. O leucismo, também conhecido como albinismo parcial, é uma anomalia cromática ainda pouco conhecida. Indivíduos portadores dos genes que condicionam a doença apresentam ausência de pigmentação em uma parte ou em todo o corpo, porém os olhos não apresentam alteração. O objetivo deste trabalho foi realizar o primeiro registro de Caiman crocodilus com leucismo no mundo.(AU)
Among crocodilians in Brazil, Caiman crocodilus (Linnaeus, 1758) is the most frequent species, but its presence in scientific studies is mostly restricted to faunal surveys. Leukism, also known as partial albinism, is a still little known chromatic anomaly. Individuals with genes that condition the disease present no pigmentation in one part or in the whole body, but the eyes did not change. The objective of this work was to perform the first record of Caiman crocodilus with leucismo in the world.(AU)
الموضوعات
Animals , Piebaldism/veterinary , Monophenol Monooxygenase , Alligators and Crocodiles , Animals, Wildالملخص
Phenolic compounds are priority pollutants with high toxicity even at low concentrations. Ever-increasingburden of pollutants in major rivers and other water bodies along with stringent environmental legislationand focus on adaptation to eco-friendly treatment approaches have necessitated the need for the removal ofthese phenolics before being discharged to rivers and other freshwater bodies. Compared to physicochemicaltreatment, enzymatic treatment has proven to be the best way to treat various phenolic compounds undermild conditions with different enzymes such as peroxidases, laccases, and tyrosinases. In this study, we havedesigned a simple and efficient method for removal of phenols from effluent wastewater using an immobilizedpreparation of mushroom tyrosinase. The enzyme was isolated from Agaricus bisporus (button mushroom)and partially purified, and subsequently, various immobilization matrices were evaluated for their efficiencyof immobilization, reproducibility, rate of degradation of phenolics, stability, and reusability. Experimentsshowed that the in situ polymerization of acrylamide monomer along with the enzyme gave the most effectiveentrapment with high reproducibility among the tested methods. Immobilized tyrosinase was much more stablethan the free tyrosinase in storage and that the immobilized tyrosinase could even retain about most of itsoriginal activity after repeated use of 10 times in a batch system. This method could provide and an economicaland stabilized immobilized-enzyme method for the removal of phenol in wastewater.
الملخص
The methanol extract of the Balkan endemic species Jurinea tzar-ferdinandii Davidov demonstrated weak antioxidant activity against DPPH⢠and ABTS+⢠and low inhibitory potential against acetylcholinesterase (8.3% Inh.) and tyrosinase (IC50 = 208 ± 8 µg/mL) enzymes. Phytochemical investigation of the extract led to isolation and identification of apigenin, luteolin, apigenin-7-O-glucoside, apigenin-4'-O-glucoside, apigenin-7-O-gentiobioside, luteolin-4'-O-glucoside, rutin, narcissin, chlorogenic and 1,5-dicaffeoylquinic acid. With exception of apigenin and rutin, all isolated compounds are reported for the first time in the representatives of genus Jurinea. The distribution of flavonoids was discussed from chemotaxonomic point of view.
El extracto de metanol de la especie endémica de los Balcanes Jurinea tzar-ferdinandii Davidov demostró una actividad antioxidante débil contra DPPH⢠y ABTS+⢠y un bajo potencial inhibidor contra las enzimas acetilcolinesterasa (8.3% Inh.) tirosinasa (IC50 = 208 ± 8 µg/mL). La investigación fitoquímica del extracto condujo al aislamiento e identificación de apigenina, luteolina, apigenina-7-Oglucósido, apigenina-4'-O-glucósido, apigenina-7-O-gentiobiósido, luteolina-4'-O-glucósido, rutina, narcissin, clorogénico y ácido 1,5- dicafeoilquinico. Con excepción de la apigenina y la rutina, todos los compuestos aislados se informan por primera vez en el género Jurinea. La distribución de flavonoides se discute desde el punto de vista quimiotaxonómico.
الموضوعات
Asteraceae/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Phenols/analysis , Flavonoids/analysis , Cholinesterase Inhibitors , Monophenol Monooxygenase/antagonists & inhibitors , Methanol , Balkan Peninsulaالملخص
Objectives To prepare arbutin phospholipid complex (APC) to improve the skin permeability of arbutin and discuss the formation mechanism of APC. Methods Solvent evaporation method was used to prepare APC. The formation of APC was confirmed by differential scanning calorimetry (DSC), X-ray diffraction (XRD), infrared spectroscopy (IR), 1H nuclear magnetic resonance (1H-NMR), scanning electron microscopy (SEM) and transmission electron microscope (TEM). The solubility, skin permeability and the ability to inhibit tyrosinase of APC were evaluated. Results The analysis showed that the weak interaction between phospholipid and arbutin molecules formed APC. The solubility of arbutin in APC in n-octanol increased from 1.29 µg/mL to 9.54 µg/mL, and the formation of APC effectively increased the lipophilicity of arbutinn. In vitro release study demonstrated that APC exhibited sustained release behavior. Ex vitro penetration studies showed that arbutin was difficult to reach the subcutaneous tissue through the skin, but APC showed strong penetration ability, of which permeation flux was improved from 0.02 mg/cm2 to 0.42 mg/cm2. Enzyme inhibitory activity test showed that the inhibition of APC on tyrosinase activity was 1.85 times of arbutin. Conclusions The formation of the complex improved the bioavailability of arbutin, and the complex held higher application potential for medicinal and cosmetic.
الملخص
Objective: To compare the effects of softeners including ethanol, propylene glycol and mixed alcohol (ethanol-propylene glycol 2:8) on the preparation of glabridin ethosomes (GLA-ES), and provide the selection basis of the softeners for studying the ethosomes of insoluble drugs. Methods: GLA-ES were prepared by injection-ultrasonic binding method with ethanol, propylene glycol and mixed alcohol (ethanol-propylene glycol, 2:8) as softeners. The morphology, size, Zeta potential, entrapment efficiency, stability, and in vitro drug release of GLA-ES were investigated. Tyrosinase activity on melanoma B16-OVA cells were detected to evaluate the inhibition of GLA-ES on the synthesis of melanin, the experiment of potassium ferricyanide reducing power was performed to evaluate the antioxidant effect of GLA-ES, and human epidermal HaCaT cells and rat skin were used for preliminary safety evaluation. Results: GLA-ES were yellow translucent liquid, containing vesicular phospholipid bilayer structure, the average particle size of GLA-Et-ES, GLA-PG-ES and GLA-MA-ES were (34.24 ± 0.29), (62.31 ± 1.66) and (41.20 ± 1.13) nm, respectively; The Zeta potential were (-41.0 ± 1.8), (-32.9 ± 0.2) and (-35.8 ± 1.6) mV, the entrapment efficiency were (91.47 ± 2.39)%, (87.33 ± 1.31)% and (91.39 ± 3.59)%, respectively, which had good stability of storage at 4 ℃ for 20 d, in vitro drug release behaviors of GLA-ES fitted Higuchi equation, implying their sustained release properties. Compared with the glabridin suspension, the inhibitory effects of GLA-Et-ES, GLA-PG-ES and GLA-MA-ES on tyrosinase activity in melanoma B16-OVA cells were increased by 38.07%, 19.58% and 40.42%, respectively. The results of potassium ferricyanide reducing power also showed that GLA-ES had a stronger in vitro antioxidant effect than the glabridin suspension; GLA-ES were nearly nontoxic on normal cells and had no irritation to rat skin. Conclusion: GLA-ES can be obtained by hree kinds of softeners, which can inhibit the synthesis of melanin and enhance the antioxidant effect with good safety. The present research will provide the basis for further developing skin-whitening cosmetics or pharmaceutical external preparation. For the insoluble drugs such as glabridin, when mixed alcohol (ethanol-propylene glycol) was selected as the softener to prepare ethosome, it exhibited better encapsulation efficiency and stability than that of ethanol or propylene glycol as the softener alone.