scholarly journals Leathesia difformis Extract Inhibits α-MSH-Induced Melanogenesis in B16F10 Cells via Down-Regulation of CREB Signaling Pathway

2019 ◽  
Vol 20 (3) ◽  
pp. 536 ◽  
Author(s):  
Ga-Young Seo ◽  
Yuna Ha ◽  
Ah-Hyun Park ◽  
Oh Kwon ◽  
Youn-Jung Kim
Keyword(s):  
Therapeutic Agent ◽  
Antioxidant Properties ◽  
Inhibitory Effect ◽  
Melanin Synthesis ◽  
Melanocortin 1 Receptor ◽  
Dopachrome Tautomerase ◽  
Melanocyte Stimulating Hormone ◽  
B16f10 Cells ◽  
Expression Of Genes ◽  
Tyrosinase Related Protein

Leathesia difformis (L.) Areschoug (L. difformis) is a species of littoral brown algae of the class Phaeophyceae. Only a few studies on the apoptotic, antiviral, and antioxidant properties of L. difformis have been reported, and its inhibitory effect on melanin synthesis has not been studied. The aim of this study was to investigate the anti-melanogenic effect of L. difformis extract on α-melanocyte-stimulating hormone (α-MSH)-induced B16F10 melanocytes and its mechanism of action. L. difformis was extracted using 80% ethanol (LDE) and then fractioned between ethyl acetate (LDE-EA) and water (LDE-A). Our data demonstrated that LDE-EA significantly inhibited melanin level and cellular tyrosinase activity in α-MSH-stimulated B16 cells. In addition, the expression of genes associated with melanin synthesis, such as microphthalmia-associated transcription factor (Mitf), tyrosinase (Tyr), tyrosinase-related protein-1 (Trp-1), dopachrome tautomerase (Dct), and melanocortin 1 receptor (Mc1r) was down-regulated by LDE-EA treatment. Moreover, LDE-EA decreased p-CREB levels, which suggests that the inhibition of the cAMP/PKA/CREB pathways may be involved in the anti-melanogenic effect of LDE-EA. Thus, this study revealed that LDE-EA is an effective inhibitor of hyperpigmentation through inhibition of CREB pathways and may be considered as a potential therapeutic agent for hyperpigmentation disorders.

scholarly journals 7,3′,4′-Trihydroxyisoflavone, a Metabolite of the Soy Isoflavone Daidzein, Suppresses α-Melanocyte-Stimulating Hormone-Induced Melanogenesis by Targeting Melanocortin 1 Receptor

2020 ◽  
Vol 7 ◽  
Author(s):  
Ji Hye Kim ◽  
Jae-Eun Lee ◽  
Taewon Kim ◽  
Myung Hun Yeom ◽  
Jun Seong Park ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Intracellular Camp ◽  
Related Protein ◽  
Melanin Production ◽  
Melanocortin 1 Receptor ◽  
Creb Phosphorylation ◽  
Melanocyte Stimulating Hormone ◽  
B16f10 Cells ◽  
Tyrosinase Related Protein ◽  
Stimulating Hormone

7,3′,4′-Trihydroxyisoflavone (7,3′,4′-THIF) is a metabolite of daidzein which is a representative isoflavone found in soybean. Recent studies suggested that 7,3′,4′-THIF exerts a hypopigmentary effect in B16F10 cells, however, its underlying molecular mechanisms and specific target protein remain unknown. Here, we found that 7,3′,4′-THIF, but not daidzein, inhibited α-melanocyte-stimulating hormone (MSH)-induced intracellular and extracellular melanin production in B16F10 cells by directly targeting melanocortin 1 receptor (MC1R). Western blot data showed that 7,3′,4′-THIF inhibited α-MSH-induced tyrosinase, tyrosinase-related protein-1 (TYRP-1), and tyrosinase-related protein-2 (TYRP-2) expressions through the inhibition of Microphthalmia-associated transcription factor (MITF) expression and cAMP response element-binding (CREB) phosphorylation. 7,3′,4′-THIF also inhibited α-MSH-induced dephosphorylation of AKT and phosphorylation of p38 and cAMP-dependent protein kinase (PKA). cAMP and Pull-down assays indicated that 7,3′,4′-THIF strongly inhibited forskolin-induced intracellular cAMP production and bound MC1R directly by competing with α-MSH. Moreover, 7,3′,4′-THIF inhibited α-MSH-induced intracellular melanin production in human epidermal melanocytes (HEMs). Collectively, these results demonstrate that 7,3′,4′-THIF targets MC1R, resulting in the suppression of melanin production, suggesting a protective role for 7,3′,4′-THIF against melanogenesis.

scholarly journals Inhibitory Effects of Cycloheterophyllin on Melanin Synthesis

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2526
Author(s):  
Joong-Hyun Shim
Keyword(s):  
Functional Materials ◽  
Tyrosinase Activity ◽  
Melanin Synthesis ◽  
Activity Assay ◽  
Inhibitory Effects ◽  
Melanin Production ◽  
Messenger Ribonucleic Acid ◽  
B16f10 Cells ◽  
Cell Line Cell ◽  
Tyrosinase Related Protein

This study was performed to clarify the inhibitory effects of cycloheterophyllin on melanin synthesis. In order to elucidate the inhibitory effects of cycloheterophyllin on the B16F10 cell line, cell viability, messenger ribonucleic acid (mRNA) expressions, tyrosinase activity assay, and melanin production assay were measured. The effects of cycloheterophyllin on tyrosinase-related protein 1 (TYRP1)/TYRP2/tyrosinase (TYR)/microphthalmia-associated transcription factor (MITF) mRNA expressions and melanin content were determined. Quantitative real-time RT-PCR showed that cycloheterophyllin decreased the mRNA expression level of TYRP1/TYRP2/TYR/MITF genes and melanin production contents than α-MSH-treated B16F10 cells. The tyrosinase activity assay revealed that cycloheterophyllin decreased the melanin production in the B16F10 cells. These data show that cycloheterophyllin increases the whitening effects in the B16F10 cells; thus, cycloheterophyllin is a potent ingredient for skin whitening. Thus, further research on the mechanism of action of cycloheterophyllin for the development of functional materials should be investigated.

scholarly journals Anti-Melanogenic Effects of Hydroxyectoine via MITF Inhibition by JNK, p38, and AKT Pathways in B16F10 Melanoma Cells

2019 ◽  
Vol 14 (6) ◽  
pp. 1934578X1985852 ◽  
Author(s):  
You C. Chung ◽  
Min-Jin Kim ◽  
Eun Y. Kang ◽  
Yun B. Kim ◽  
Bong S. Kim ◽  
...  
Keyword(s):  
Skin Color ◽  
Inhibitory Effect ◽  
Tyrosinase Activity ◽  
Dependent Manner ◽  
Related Protein ◽  
B16f10 Melanoma ◽  
Melanin Production ◽  
B16f10 Cells ◽  
Dose Dependent ◽  
Tyrosinase Related Protein

Melanin plays a role in determining human skin color of a person, and a large amount of melanin makes the skin color look darkened. The proper amount of melanin formation protects our skin from UV radiation, but excessive melanin production causes hyperpigmentation and leads to freckles, melasma, and lentigo. In this study, we investigated the inhibitory effect of hydroxyectoine on melanogenesis and its mechanism in B16F10 cells. Melanin content and cellular tyrosinase activity were determined. The expression of microphthalmia-associated transcription factor (MITF), and the activities of tyrosinase and other melanogenesis-related enzymes, such as tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2, were also examined. Hydroxyectoine treatment significantly inhibited melanin production and intracellular tyrosinase activity in a dose-dependent manner. Western blot analysis showed that hydroxyectoine also reduced the expressions of tyrosinase and TRP-1. In addition, hydroxyectoine significantly reduced the expression of MITF, a major regulator of melanin production, and inhibited the phosphorylation of p38, c-Jun N-terminal kinase, and activated the protein kinase B. The results demonstrated that hydroxyectoine inhibits the expression of MITF through the inhibition or activation of melanin-related signaling pathways and downregulates melanogenesis by inhibiting melanogenic enzyme expression and tyrosinase activity. Hydroxyectoine has potential value in functional cosmetics applications, such as whitening.

Schisandrin B inhibits α-melanocyte-stimulating hormone-induced melanogenesis in B16F10 cells via downregulation of MAPK and CREB signaling pathways

2020 ◽  
Vol 85 (4) ◽  
pp. 834-841
Author(s):  
Na Zhao ◽  
Xiaoming Su ◽  
He Li ◽  
Zhengyi Li ◽  
Yueyang Wang ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Camp Response Element Binding ◽  
Schisandrin B ◽  
Camp Response Element ◽  
Melanocyte Stimulating Hormone ◽  
B16f10 Cells ◽  
Kinase C ◽  
Element Binding Protein ◽  
Tyrosinase Related Protein ◽  
Stimulating Hormone

ABSTRACT Schisandrin B (Sch B), a lignan compound in Schisandra, possesses antioxidant, anti-inflammatory, and antiobesity activities. The effect of Sch B on melanogenesis and molecular mechanisms are still unknown. Therefore, we aimed to investigate the antimelanogenic effects of Sch B on α-melanocyte-stimulating hormone–induced B16F10 cells and elucidate the underlying molecular mechanisms. We found that Sch B significantly suppressed melanin content and mushroom tyrosinase (TYR) activity. Sch B treatment decreased the expression of TYR, melanocyte-inducing transcription factor (MITF), tyrosinase-related protein (TRP) 1, and TRP2. Moreover, Sch B modulated the phosphorylation of p38, extracellular-regulated protein kinase, c-Jun N-terminal kinase, and cAMP-response element binding protein (CREB), implying that these pathways may be involved in suppressing melanogenesis. Furthermore, we found that Sch B decreased melanogenesis by downregulating MITF and melanogenic enzymes via MAPK and CREB pathways. Overall, these findings indicate that Sch B has the potential use in whitening.

scholarly journals Sesamol Inhibited Ultraviolet Radiation-Induced Hyperpigmentation and Damage in C57BL/6 Mouse Skin

Antioxidants ◽  
2019 ◽  
Vol 8 (7) ◽  
pp. 207 ◽  
Author(s):  
Ya-Jhen You ◽  
Po-Yuan Wu ◽  
Yi-Jung Liu ◽  
Chien-Wei Hou ◽  
Chin-Sheng Wu ◽  
...  
Keyword(s):  
Topical Application ◽  
Skin Pigmentation ◽  
Mouse Skin ◽  
Melanocortin 1 Receptor ◽  
Dopachrome Tautomerase ◽  
B16f10 Cells ◽  
Melanin Index ◽  
Radiation Induced ◽  
L Value ◽  
Related Proteins

Melanin is synthesized through a series of oxidative reactions initiated with tyrosine and catalyzed by melanogenesis-related proteins such as tyrosinase, tyrosinase-related protein-1 (TRP-1), dopachrome tautomerase (TRP-2), and microphthalmia-associated transcription factor (MITF). Our previous study demonstrated that sesamol inhibited melanin synthesis through the inhibition of the melanocortin 1 receptor (MC1R)/MITF/tyrosinase pathway in B16F10 cells. In this study, sesamol was applied to C57BL/6 mouse skin to understand its activity with respect to skin pigmentation. The results indicated that ultraviolet (UV) B-induced hyperpigmentation in the C57BL/6 mouse skin was significantly reduced by topical application of sesamol for 4 weeks. Sesamol reduced the melanin index and melanin content of the skin. In addition, sesamol elevated the brightness (L* value) of the skin. Sesamol also reduced UVB-induced hyperplasia of epidermis and collagen degradation in dermis. In immunohistochemical staining, topical application of sesamol reduced UVB-induced tyrosinase, TRP-1, TRP-2, and MITF expression in the epidermis of the skin. These results demonstrated that sesamol is a potent depigmenting agent in the animal model.

scholarly journals Synthesis of DOTA-pyridine chelates for 64Cu coordination and radiolabeling of αMSH peptide

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Hua Yang ◽  
Feng Gao ◽  
Brooke McNeil ◽  
Chengcheng Zhang ◽  
Zheliang Yuan ◽  
...  
Keyword(s):  
Full Potential ◽  
In Vivo Evaluation ◽  
Melanocortin 1 Receptor ◽  
Melanocyte Stimulating Hormone ◽  
Endogenous Copper ◽  
Coordination Ability ◽  
Copper Chelators ◽  
Cu Complexes ◽  
High Binding Affinity

Abstract Background 64Cu is one of the few radioisotopes that can be used for both imaging and therapy, enabling theranostics with identical chemical composition. Development of stable chelators is essential to harness the potential of this isotope, challenged by the presence of endogenous copper chelators. Pyridyl type chelators show good coordination ability with copper, prompting the present study of a series of chelates DOTA-xPy (x = 1–4) that sequentially substitute carboxyl moieties with pyridyl moieties on a DOTA backbone. Results We found that the presence of pyridyl groups significantly increases 64Cu labeling conversion yield, with DOTA-2Py, −3Py and -4Py quantitatively complexing 64Cu at room temperature within 5 min (1 × 10− 4 M). [64Cu]Cu-DOTA-xPy (x = 2–4) exhibited good stability in human serum up to 24 h. When challenged with 1000 eq. of NOTA, no transmetallation was observed for all three 64Cu complexes. DOTA-xPy (x = 1–3) were conjugated to a cyclized α-melanocyte-stimulating hormone (αMSH) peptide by using one of the pendant carboxyl groups as a bifunctional handle. [64Cu]Cu-DOTA-xPy-αMSH retained good serum stability (> 96% in 24 h) and showed high binding affinity (Ki = 2.1–3.7 nM) towards the melanocortin 1 receptor. Conclusion DOTA-xPy (x = 1–3) are promising chelators for 64Cu. Further in vivo evaluation is necessary to assess the full potential of these chelators as a tool to enable further theranostic radiopharmaceutical development.

scholarly journals Chemical Composition, In Vitro and In Silico Antioxidant Potential of Melissa officinalis subsp. officinalis Essential Oil

Antioxidants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1081
Author(s):  
Matilda Rădulescu ◽  
Călin Jianu ◽  
Alexandra Teodora Lukinich-Gruia ◽  
Marius Mioc ◽  
Alexandra Mioc ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
In Silico ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Melissa Officinalis ◽  
Β Carotene

The investigation aimed to study the in vitro and in silico antioxidant properties of Melissa officinalis subsp. officinalis essential oil (MOEO). The chemical composition of MOEO was determined using GC–MS analysis. Among 36 compounds identified in MOEO, the main were beta-cubebene (27.66%), beta-caryophyllene (27.41%), alpha-cadinene (4.72%), caryophyllene oxide (4.09%), and alpha-cadinol (4.07%), respectively. In vitro antioxidant properties of MOEO have been studied in 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging, and inhibition of β-carotene bleaching assays. The half-maximal inhibitory concentration (IC50) for the radical scavenging abilities of ABTS and DPPH were 1.225 ± 0.011 μg/mL and 14.015 ± 0.027 μg/mL, respectively, demonstrating good antioxidant activity. Moreover, MOEO exhibited a strong inhibitory effect (94.031 ± 0.082%) in the β-carotene bleaching assay by neutralizing hydroperoxides, responsible for the oxidation of highly unsaturated β-carotene. Furthermore, molecular docking showed that the MOEO components could exert an in vitro antioxidant activity through xanthine oxidoreductase inhibition. The most active structures are minor MOEO components (approximately 6%), among which the highest affinity for the target protein belongs to carvacrol.

scholarly journals Effect of Phlorotannins Isolated From Eisenia bicyclis on Melanogenesis in Mouse B16 Melanoma Cells

2021 ◽  
Vol 16 (5) ◽  
pp. 1934578X2110192
Author(s):  
Yuki Ohno ◽  
Shiori Kondo ◽  
Kiho Tajima ◽  
Toshiyuki Shibata ◽  
Tomohiro Itoh
Keyword(s):  
Melanoma Cells ◽  
B16 Melanoma ◽  
Physiological Effects ◽  
Related Protein ◽  
Eisenia Bicyclis ◽  
Melanin Production ◽  
Melanocyte Stimulating Hormone ◽  
B16 Melanoma Cells ◽  
Anti Cancer ◽  
Tyrosinase Related Protein

Phlorotannins isolated from brown algae, such as Eisena bicyclis, have positive physiological effects, including anti-cancer, anti-inflammatory, and anti-Alzheimer’s disease. Although phlorotannins have been shown to inhibit tyrosinase, an enzyme essential for melanogenesis, their effect on melanogenesis remains unexplored. Thus, we isolated phlorotannins from E. bicyclis and examined their effects on α-melanocyte-stimulating hormone (α-MSH)-induced melanogenesis in murine B16 melanoma cells. Both fucofuroeckol-A (FF-A) and phlorofucofuroeckol-A (PFF-A) suppressed α-MSH-induced melanogenesis. Neither inhibited human tyrosinase (TYR) activity, but both inhibited tyrosinase-related protein-2 activity. FF-A downregulated the expression of microphthalmia-associated transcription factor and TYR, which subsequently suppressed melanin production. These results suggest that phlorotannins could be beneficial as melanin control drugs for hyperpigmentation disorders.

Inhibitory effect of brazilein on tyrosinase and melanin synthesis: Kinetics and in silico approach

2015 ◽  
Vol 81 ◽  
pp. 228-234 ◽  
Author(s):  
Hemachandran Hridya ◽  
Anantharaman Amrita ◽  
Mohan Sankari ◽  
C. George Priya Doss ◽  
Mohan Gopalakrishnan ◽  
...  
Keyword(s):  
In Silico ◽  
Inhibitory Effect ◽  
Melanin Synthesis
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