Oxyresveratrol extracted from Artocarpus heterophyllus Lam. inhibits tyrosinase and age pigments in vitro and in vivo

2020 ◽  
Vol 11 (7) ◽  
pp. 6595-6607 ◽  
Author(s):  
Jun Li ◽  
Zhenyu Lin ◽  
Xudong Tang ◽  
Guo Liu ◽  
Yunjiao Chen ◽  
...  
Keyword(s):  
Tyrosinase Activity ◽  
Melanin Production ◽  
Artocarpus Heterophyllus

Oxyresveratrol could strongly inhibit tyrosinase activity and decrease melanin production in vitro and in vivo.

Effect of α-melanocyte-stimulating hormone on tyrosinase activity in hair follicular and epidermal melanocytes of the mouse

1988 ◽  
Vol 119 (3) ◽  
pp. 517-522 ◽  
Author(s):  
P. Seechurn ◽  
S. A. Burchill ◽  
A. J. Thody
Keyword(s):  
Tyrosinase Activity ◽  
In Vitro Experiments ◽  
Dorsal Skin ◽  
Wild Type ◽  
Melanocyte Stimulating Hormone ◽  
Tyrosinase Expression ◽  
In Vivo Administration ◽  
Agouti Gene

ABSTRACT In this study, the effect of α-MSH on tyrosinase activity was compared in epidermal and hair follicular melanocytes of mice. It had no effect on epidermal tyrosinase activity in dorsal skin from neonatal non-agouti black mice (C57BL/6J) in both in-vivo and in-vitro experiments. Theophylline and 8-bromocyclic (c)AMP were similarly without effect in in-vitro experiments. In-vivo administration of α-MSH and theophylline for 7 days was also without effect on epidermal tyrosinase activity in ear skin of adult non-agouti mice, and the same was true for α-MSH in wild-type agouti mice. Activation of the epidermal melanocytes in the non-agouti and wild-type agouti mice with ultraviolet radiation also failed to bring about a response to α-MSH and to theophylline in the case of the former. No tyrosinase activity was detected in the epidermis of viable yellow mice (C3H-HeAvy), but, as shown previously, tyrosinase activity was present in the hair follicle when the hair was actively growing and was increased in those mice given either α-MSH or theophylline. α-MSH and theophylline had no such effects on hair follicular tyrosinase activity in the non-agouti mice. The present results suggest that α-MSH- and cAMP-dependent mechanisms have little or no importance in the regulation of tyrosinase expression in mouse epidermal melanocytes. α-MSH may, however, regulate tyrosinase expression in hair follicular melanocytes, but even in these melanocytes its action may be restricted to mice that express the agouti gene. J. Endocr. (1988) 119, 517–522

scholarly journals FGIN-1-27 Inhibits Melanogenesis by Regulating Protein Kinase A/cAMP-Responsive Element-Binding, Protein Kinase C-β, and Mitogen-Activated Protein Kinase Pathways

2020 ◽  
Vol 11 ◽  
Author(s):  
Jinpeng Lv ◽  
Songzhou Jiang ◽  
Ying Yang ◽  
Ximei Zhang ◽  
Rongyin Gao ◽  
...  
Keyword(s):  
Protein Kinase ◽  
The Body ◽  
Tyrosinase Activity ◽  
Mitogen Activated Protein Kinase ◽  
Mushroom Tyrosinase ◽  
Mitogen Activated Protein ◽  
Element Binding Protein ◽  
Responsive Element

FGIN-1-27 is a synthetic mitochondrial diazepam binding inhibitor receptor (MDR) agonist that has demonstrated pro-apoptotic, anti-anxiety, and steroidogenic activity in various studies. Here we report, for the first time, the anti-melanogenic efficacy of FGIN-1-27 in vitro and in vivo. FGIN-1-27 significantly inhibited basal and α-melanocyte-stimulating hormone (α-MSH)-, 1-Oleoyl-2-acetyl-sn-glycerol (OAG)- and Endothelin-1 (ET-1)-induced melanogenesis without cellular toxicity. Mushroom tyrosinase activity assay showed that FGIN-1-27 did not directly inhibit tyrosinase activity, which suggested that FGIN-1-27 was not a direct inhibitor of tyrosinase. Although it was not capable of modulating the catalytic activity of mushroom tyrosinase in vitro, FGIN-1-27 downregulated the expression levels of key proteins that function in melanogenesis. FGIN-1-27 played these functions mainly by suppressing the PKA/CREB, PKC-β, and MAPK pathways. Once inactivated, it decreased the expression of MITF, tyrosinase, TRP-1, TRP-2, and inhibited the tyrosinase activity, finally inhibiting melanogenesis. During in vivo experiments, FGIN-1-27 inhibited the body pigmentation of zebrafish and reduced UVB-induced hyperpigmentation in guinea pig skin, but not a reduction of numbers of melanocytes. Our findings indicated that FGIN-1-27 exhibited no cytotoxicity and inhibited melanogenesis in both in vitro and in vivo models. It may prove quite useful as a safer skin-whitening agent.

scholarly journals Molecular Mechanisms of Anti-Melanogenic Gedunin Derived from Neem Tree (Azadirachta indica) Using B16F10 Mouse Melanoma Cells and Early-Stage Zebrafish

Plants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 330
Author(s):  
Hwang-Ju Jeon ◽  
Kyeongnam Kim ◽  
Chaeeun Kim ◽  
Myoung-Jin Kim ◽  
Tae-Oh Kim ◽  
...  
Keyword(s):  
Skin Color ◽  
Molecular Mechanisms ◽  
Early Stage ◽  
Melanoma Cells ◽  
Ultraviolet Rays ◽  
Melanin Production ◽  
Zebrafish Model ◽  
Mouse Melanoma

Melanogenesis represents a series of processes that produce melanin, a protective skin pigment (against ultraviolet rays), and determines human skin color. Chemicals reducing melanin production have always been in demand in the cosmetic market because of skincare interests, such as whitening. The main mechanism for inhibiting melanin production is the inhibition of tyrosinase (TYR), a key enzyme for melanogenesis. Here, we evaluated gedunin (Ged), a representative limonoid, for its anti-melanogenesis action. Melanin production in vitro was stimulated by alpha-melanocyte stimulating hormone (α-MSH) in B16F10 mouse melanoma cells. Ged reduced α-MSH-stimulated melanin production, inhibiting TYR activity and protein amount. We confirmed this result in vivo in a zebrafish model for melanogenesis. There was no sign of toxicity and malformation of zebrafish embryos during development in all treated concentrations. Ged reduced the number of produced zebrafish embryo pigment dots and melanin contents of embryos. The highly active concentration of Ged (100 µM) was much lower than the positive control, kojic acid (8 mM). Hence, Ged could be a fascinating candidate for anti-melanogenesis reagents.

THE MELANOGENIC RESPONSE TO TESTOSTERONE IN SCROTAL EPIDERMIS: EFFECTS ON TYROSINASE ACTIVITY AND PROTEIN SYNTHESIS

1976 ◽  
Vol 81 (2) ◽  
pp. 435-448 ◽  
Author(s):  
Michael J. Wilson ◽  
Eugene Spaziani
Keyword(s):  
Protein Synthesis ◽  
Specific Protein ◽  
Tyrosinase Activity ◽  
Melanin Synthesis ◽  
Testosterone Treatment ◽  
Pre Treatment ◽  
Inhibitor Of Protein Synthesis ◽  
Rate Limiting

ABSTRACT Pigmentation of the scrotum of the black-pelted rat, as expressed through melanocyte melanogenic activity, is controlled by androgens. Castration decreased in vitro incorporation of [14C] tyrosine into melanin. Testosterone pre-treatment for 4 days increased melanin radioactivity over castrate controls; the increment in vitro was prevented by an inhibitor of protein synthesis (cycloheximide) added to the incubation. However, cycloheximide only partially blocked melanin synthesis when added to tissue from animals hormone treated for 6 days in vivo, and was ineffective in tissue from intacts. Bulk protein synthesis in vitro (incorporation of [14C] tyrosine or -leucine) was not affected by castration or testosterone treatment but was uniformly inhibited by cycloheximide. The data suggest that new synthesis of specific protein in vitro was necessary for initial hormone-stimulation of melanogenesis, but with longer exposure to hormone sufficient protein was pre-synthetized in vivo to permit melanogenesis during incubation with the inhibitor. Radioautographs of epidermis incubated with [14C] tyrosine showed grains concentrated over macromolecular aggregates in melanocytes, a pattern not altered by cycloheximide. Though available for incorporation into general tissue protein. [14C] tyrosine was apparently incorporated preferentially into melanin by melanocytes. DOPA (3,4-dihydroxyphenylalanine) added to incubations in cofactor amounts did not affect decreased melanin synthesis after castration and appears, therefore, not to be rate limiting in that decrease. Tissue uptake of free [14C] tyrosine or — leucine during incubation was lower than normal in castrate epidermis; uptake was elevated by testosterone treatment. Concentrations appeared sufficient in all preparations to suggest that availability is not rate limiting for synthesis of melanin or protein; however, a possible influence on amino acid permeability for melanocytes remains undetermined. Tyrosinase activity was present in both particulate and cytosol fractions of epidermis but decreased significantly after castration only in the cytosol. Testosterone increased particulate activity after 4 days and soluble activity after 9 days of treatment. These and findings above are consistent with a model that tyrosinase is synthesized and incorporated into melanosome structure within 4 days testosterone treatment; with longer treatment synthesis may then exceed that required for melanosome assembly and tyrosinase appears in the soluble milieu.

scholarly journals Assessing the virulence ofCryptococcus neoformanscausing meningitis in HIV infected and uninfected patients in Vietnam

2017 ◽  
Author(s):  
Lam Tuan Thanh ◽  
Dena L. Toffaletti ◽  
Jennifer L. Tenor ◽  
Charles Giamberardino ◽  
Gregory D. Sempowski ◽  
...  
Keyword(s):  
Inflammatory Responses ◽  
Phenotypic Characteristics ◽  
Melanin Production ◽  
Pathogenic Potential ◽  
Virulence Markers ◽  
Tnf Α ◽  
Evolutionary Advantage ◽  
Single Genotype

AbstractWe previously observed a substantial burden of cryptococcal meningitis in Vietnam atypically arising in HIV-uninfected individuals. This disease was associated with a single genotype ofCryptococcus neoformans(Sequence Type (ST)5), which was significantly less common in HIV-infected individuals. Aiming to compare the phenotypic characteristics of ST5 and non-ST5 C. neoformans we selected 30 representative Vietnamese isolates, compared theirin vitropathogenic potential andin vivovirulence. ST5 and non-ST5 organisms exhibited comparable characteristics with respect toin vitrovirulence markers including melanin production, replication at 37°C, and growth in cerebrospinal fluid. However, the ST5 isolates had significantly increased variability in cellular and capsular sizing compared with non-ST5 organisms (p<0.001). Counter-intuitively, mice infected with ST5 isolates had significantly longer survival with lower fungal burdens at day 7 than non-ST5 isolates. Notably, ST5 isolates induced significantly greater initial inflammatory responses than non-ST5 strains, measured by TNF-α concentrations (p<0.001). Despite being generally less virulent in the mouse model, we hypothesize that the significant within strain variation seen in ST5 isolates in the tested phenotypes may represent an evolutionary advantage enabling adaptation to novel niches including apparently immunocompetent human hosts.

Attenuation of In Vitro and In Vivo Melanin Synthesis using a Chinese Herbal Medicine through the Inhibition of Tyrosinase Activity

Phytomedicine ◽  
2021 ◽  
pp. 153876
Author(s):  
Shu-Chun Liu ◽  
Meei-Ling Sheu ◽  
Yi-Ching Tsai ◽  
Yu-Chin Lin ◽  
Ching-Wen Chang ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Chinese Herbal Medicine ◽  
Tyrosinase Activity ◽  
Melanin Synthesis ◽  
Chinese Herbal

EFFECTS OF α-MELANOCYTE-STIMULATING HORMONE AND [8-ARGININE]-VASOTOCIN UPON MELANOGENESIS IN HAIR FOLLICLE MELANOCYTES IN VITRO

1981 ◽  
Vol 91 (3) ◽  
pp. 501-507 ◽  
Author(s):  
ANN LOGAN ◽  
BRIAN WEATHERHEAD
Keyword(s):  
Hair Follicle ◽  
Hair Follicles ◽  
Tyrosinase Activity ◽  
Arginine Vasotocin ◽  
Melanin Production ◽  
Potency Ratio ◽  
Melanin Biosynthesis ◽  
Melanocyte Stimulating Hormone ◽  
Stimulating Hormone

α-Melanocyte-stimulating hormone (α-MSH) has been shown to act directly on the mammalian melanocyte in short-term cultures of hair follicles obtained from the Siberian hamster. Melanogenesis was stimulated through an increase in tyrosinase activity which resulted in an increase in melanin production. The response of hair follicle melanocytes to α-MSH occurred only in follicles taken from moulting animals, implying that they show a discontinuous expression of MSH receptors during the hair follicle growth cycle. Synthetic 1–24 ACTH had no effect on melanogenesis regardless of whether the follicles came from moulting or non-moulting animals. The pineal peptide, [8-arginine]-vasotocin (AVT), inhibited melanin production without a concomitant decrease in tyrosinase activity. In this respect AVT resembled melatonin, although AVT showed a potency ratio of less than half on a molar basis. The action of AVT, like that of melatonin, must ultimately be on some post-tyrosinase step in melanin biosynthesis. In these hair follicle melanocytes AVT seems to bind to specific receptors since neither of the closely related peptides, oxytocin and [8-arginine]-vasopressin, displayed any activity in our culture system.

scholarly journals In Silico Prediction of Tyrosinase and Adenylyl Cyclase Inhibitors from Natural Compounds

2014 ◽  
Vol 9 (2) ◽  
pp. 1934578X1400900
Author(s):  
Pedro Fong ◽  
Henry H. Y. Tong ◽  
Chi M. Chao
Keyword(s):  
Adenylyl Cyclase ◽  
Skin Irritation ◽  
Herbal Medicines ◽  
Skin Permeability ◽  
Pharmacophore Mapping ◽  
Topical Formulation ◽  
Melanin Production ◽  
Skin Whitening

Although many herbal medicines are effective in the treatment of hyperpigmentation, the potency of different constituents remains unknown. In this work, more than 20,000 herbal ingredients from 453 herbs were docked into the crystal structures of adenylyl cyclase and a human homology tyrosinase model using Surflex-Dock. These two enzymes are responsible for melanin production and inhibition of them may attain a skin-whitening effect superior to currently available agents. The essential drug properties for topical formulation of the herbal ingredients, including skin permeability, sensitization, irritation, corrosive and carcinogenic properties were predicted by Dermwin, Skin Sensitization Alerts (SSA), Skin Irritation Corrosion Rules Estimation Tool (SICRET) and Benigni/Bossa rulebase module of Toxtree. Moreover, similarity ensemble and pharmacophore mapping approaches were used to forecast other potential targets for these herbal compounds by the software, SEArch and PharmMapper. Overall, this study predicted seven compounds to have advanced drug-like properties over the well-known effective tyrosinase inhibitors, arbutin and kojic acid. These seven compounds have the highest potential for further in vitro and in vivo investigation with the aim of developing safe and high-efficacy skin-whitening agents.

scholarly journals Identification of Sake Extract as a New Anti-melanogenic Ingredient by in vitro and Clinical Trials

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801
Author(s):  
Jeong-Ah Hwang ◽  
Myeong-Jin Goh ◽  
Eun-Joo Kim ◽  
Myong-Ryul Lee ◽  
Nok-Hyun Park ◽  
...  
Keyword(s):  
Skin Diseases ◽  
Alcoholic Beverage ◽  
Human Keratinocytes ◽  
Equivalent Model ◽  
Dependent Manner ◽  
Melanin Production ◽  
In Vivo Experiments ◽  
Skin Hyperpigmentation

Overproduction of melanin is the cause of skin hyperpigmentation, which is related to several skin diseases and cosmetic concerns. Sake is a Japanese alcoholic beverage produced from rice and water by fermentation, but is little known for its effect on melanogenesis. To identify the effect of sake extract on melanin synthesis, a melanin assay was performed in melan-A murine melanocytes. Sake extract treatment significantly inhibited melanin production in a dose-dependent manner, and tyrosinase, the rate-limiting enzyme of melanogenesis, decreased significantly at the protein level. Further investigations were performed with multiple assay systems; a sake extract reduced melanin production in melan-A/SP-1 murine cell co-culture, and also in MelanoDermTM, a skin equivalent model of human keratinocytes-melanocytes. Finally, subjects were treated with a formula containing the sake extract. Topical application of the sake extract product improved skin lightness (L*) significantly within 7 days. We identified sake extract as a new anti-melanogenic ingredient through in vitro and in vivo experiments. These results suggest that a sake extract can be used to improve skin hyperpigmentation.

scholarly journals Inhibitory Effect of Arctigenin from Fructus Arctii Extract on Melanin Synthesis via Repression of Tyrosinase Expression

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Hwayong Park ◽  
Kwang Hoon Song ◽  
Pil Mun Jung ◽  
Ji-Eun Kim ◽  
Hyunju Ro ◽  
...  
Keyword(s):  
Active Compound ◽  
Gene Promoter ◽  
Inhibitory Effect ◽  
Tyrosinase Activity ◽  
Dependent Manner ◽  
Melanin Content ◽  
Extracellular Signal Regulated Kinase ◽  
Extracellular Signal

To identify the active compound arctigenin in Fructus Arctii (dried seed of medicinal plantArctium lappa) and to elucidate the inhibitory mechanism in melanogenesis, we analyzed melanin content and tyrosinase activity on B16BL6 murine melanoma and melan-A cell cultures. Water extracts of Fructus Arctii were shown to inhibit tyrosinase activity in vitro and melanin content inα-melanocyte stimulating hormone-stimulated cells to similar levels as the well-known kojic acid and arbutin, respectively. The active compound arctigenin of Fructus Arctii displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin content and tyrosinase activity in a dose-dependent manner. Melanogenic inhibitory activity was also identified in vivo with zebrafish embryo. To determine the mechanism of inhibition, the effects of arctigenin on tyrosinase gene expression and tyrosinase promoter activity were examined. Also in addition, in the signaling cascade, arctigenin dose dependently decreased the cAMP level and promoted the phosphorylation of extracellular signal-regulated kinase. This result suggests that arctigenin downregulates cAMP and the tyrosinase enzyme through its gene promoter and subsequently upregulates extracellular signal-regulated kinase activity by increasing phosphorylation in the melanogenesis signaling pathway, which leads to a lower melanin content.

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