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Melanocyte stimulating hormone

Cheong-Yong Yun, Seon Mi Ko, Yong Pyo Choi, Beom Joon Kim, Jungno Lee, Jae Mun Kim, Ju Yeon Kim, Jin Yong Song, Song-Hee Kim, Bang Yeon Hwang, Jin Tae Hong, Sang-Bae Han, Youngsoo Kim
Rationale: cAMP up-regulates microphthalmia-associated transcription factor subtype M (MITF-M) and tyrosinase (Tyro) in the generation of heavily pigmented melanosomes. Here, we communicate a therapeutic mechanism of hyperpigmented disorder by α-viniferin, an active constituent of Caragana sinica . Methods: We used cAMP-elevated melanocyte cultures or facial hyperpigmented patches for pigmentation assays, and applied immunoprecipitation, immunobloting, RT-PCR or reporter gene for elucidation of the antimelanogenic mechanism...
2018: Theranostics
Qinghao Jin, Xiang Hua Han, Cheong-Yong Yun, Chul Lee, Jin Woo Lee, Dongho Lee, Mi Kyeong Lee, Sang-Hun Jung, Jin Tae Hong, Youngsoo Kim, Bang Yeon Hwang
Bioassay-guided fractionation of the methanolic extract from the roots of Cynanchum atratum has resulted in the isolation of three new pregnane glycosides (1-3) along with four known compounds (4-7). Their structures were identified by analysis of the spectroscopic data including extensive 2D NMR. All of the isolates were evaluated for their potential to inhibit the melanin production in α-melanocyte stimulating hormone (α-MSH)-activated B16 melanoma cells. Of these, compounds 4-7 dose-dependently inhibited the melanin production with the IC50 values ranging from 4 μM to 33 μM...
January 4, 2018: Bioorganic & Medicinal Chemistry Letters
Hee Jin Jung, Min Jung Lee, Yeo Jin Park, Sang Gyun Noh, A Kyoung Lee, Kyoung Mi Moon, Eun Kyeong Lee, Eun Jin Bang, Yun Jung Park, Su Jeong Kim, Jungho Yang, Sultan Ullah, Pusoon Chun, Young Suk Jung, Hyung Ryong Moon, Hae Young Chung
As part of continued efforts for the development of new tyrosinase inhibitors, (Z)-5-(substituted benzylidene)-2-iminothiazolidin-4-one derivatives (1a - 1l) were rationally synthesized and evaluated for their inhibitory potential in vitro. These compounds were designed and synthesized based on the structural attributes of a β-phenyl-α,β-unsaturated carbonyl scaffold template. Among these compounds, (Z)-5-(3-hydroxy-4-methoxybenzylidene)-2-iminothiazolidin-4-one (1e, MHY773) exhibited the greatest tyrosinase inhibition (IC50 = 2...
March 9, 2018: Bioscience, Biotechnology, and Biochemistry
Gyeong-A Ko, Somi Kim Cho
Phytol (3,7,11,15-tetramethyl-2-hexadecen-1-ol) is an acyclic monounsaturated diterpene alcohol generated from chlorophyll metabolism that exerts anti-inflammatory, antithrombotic, antimicrobial, and antitumor effects. However, the effect of phytol on melanogenesis and the underlying molecular mechanisms of its inhibition remain unknown. Here, we found that phytol suppressed α-melanocyte-stimulating hormone-induced melanogenesis in B16F10 murine melanoma cells without any toxic effects. Phytol significantly attenuated melanin production by reducing the expression of tyrosinase and tyrosinase related protein 1...
February 24, 2018: Chemico-biological Interactions
Thomas A Lutz, Bernd Coester, Lynda Whiting, Ambrose A Dunn-Meynell, Christina N Boyle, Sebastien G Bouret, Barry E Levin, Christelle Le Foll
Amylin phosphorylates ERK (p-ERK) in the area postrema (AP) to reduce eating and synergizes with leptin to phosphorylate STAT3 in the arcuate (ARC) and ventromedial (VMN) hypothalamic nuclei, to reduce food intake and body weight. The current studies assessed potential amylin and amylin-leptin ARC/VMN interactions on ERK signaling and their roles in postnatal hypothalamic pathway development. In amylin knockout (KO) mice, the density of agouti-related protein (AgRP) immunoreactive (IR) fibers in the hypothalamic paraventricular nucleus (PVN) was increased, while the density of α-melanocyte stimulating hormone (αMSH) fibers was decreased...
February 21, 2018: Diabetes
Bonnie C Carney, Jacqueline P McKesey, Dean S Rosenthal, Jeffrey W Shupp
Dyspigmentation in burn scars can contribute to the development of psychosocial complications after injury and can be detrimental to social reintegration and quality of life for burn survivors. Although treatments for skin lightening to treat hyperpigmentation have been well reviewed in the literature, skin-darkening strategies to treat hypopigmentation have not. The following potential treatment options in the context of burn hypertrophic scar will be discussed: use of the melanocyte-keratinocyte transplantation procedure, use of ectopic synthetic analogues of alpha-melanocyte stimulating hormone to initiate melanogenesis, and use of FK506 to induce melanogenesis...
January 2018: Plastic and Reconstructive Surgery. Global Open
Giuseppe Bruschetta, Sungho Jin, Jung Dae Kim, Sabrina Diano
OBJECTIVE: Prolyl carboxypeptidase (PRCP) plays a role in the regulation of energy metabolism by inactivating hypothalamic α-melanocyte stimulating hormone (α-MSH) levels. Although detected in the arcuate nucleus, limited PRCP expression has been observed in the arcuate POMC neurons, and its site of action in regulating metabolism is still ill-defined. METHODS: We performed immunostaining to assess the localization of PRCP in arcuate Neuropeptide Y/Agouti-related Peptide (NPY/AgRP) neurons...
February 8, 2018: Molecular Metabolism
Andrew W Taylor, Tat Fong Ng
The ocular microenvironment has adapted several negative regulators of inflammation to maintain immune privilege and health of the visual axis. Several constitutively produced negative regulators within the eye TGF-β2, α-melanocyte stimulating hormone (α-MSH), Fas ligand (FasL), and PD-L1 standout because of their capacity to influence multiple pathways of inflammation, and that they are part of promoting immune tolerance. These regulators demonstrate the capacity of immune privilege to prevent the activation of inflammation, and to suppress activation of effector immune cells even under conditions of ocular inflammation induced by endotoxin and autoimmune disease...
February 12, 2018: Journal of Leukocyte Biology
Siwei Cai, Qianhui Yang, Mengzhu Hou, Qian Han, Hanyu Zhang, Jiantao Wang, Chen Qi, Qiyu Bo, Yusha Ru, Wei Yang, Zhongxiu Gu, Ruihua Wei, Yunshan Cao, Xiaorong Li, Yan Zhang
BACKGROUND/AIMS: Blood-retinal barrier (BRB) breakdown and vascular leakage is the leading cause of blindness of diabetic retinopathy (DR). Hyperglycemia-induced oxidative stress and inflammation are primary pathogenic factors of this severe DR complication. An effective interventional modality against the pathogenic factors during early DR is needed to curb BRB breakdown and vascular leakage. This study sought to examine the protective effects of α-Melanocyte-stimulating hormone (α-MSH) on early diabetic retina against vascular hyperpermeability, electrophysiological dysfunction, and morphological deterioration in a rat model of diabetes and probe the mechanisms underlying the α-MSH's anti-hyperpermeability in both rodent retinas and simian retinal vascular endothelial cells (RF6A)...
January 25, 2018: Cellular Physiology and Biochemistry
Susanne Grässel, Dominique Muschter
Joint tissues like synovium, articular cartilage, meniscus and subchondral bone, are targets for neuropeptides. Resident cells of these tissues express receptors for various neuroendocrine-derived peptides including proopiomelanocortin (POMC)-derived peptides, i.e., α-melanocyte-stimulating hormone (α-MSH), adrenocorticotropin (ACTH) and β-endorphin (β-ED), and sympathetic neuropeptides like vasoactive intestinal peptide (VIP) and neuropeptide y (NPY). Melanocortins attained particular attention due to their immunomodulatory and anti-inflammatory effects in several tissues and organs...
January 26, 2018: International Journal of Molecular Sciences
Makoto Habara, Nobuko Mori, Yuki Okada, Koh Kawasumi, Nobuhiro Nakao, Yoshikazu Tanaka, Toshiro Arai, Ichiro Yamamoto
Melanocortin 4 receptor (MC4R), which is a member of the G protein-coupled receptor (GPCR) family, mediates regulation of energy homeostasis upon the binding of α-melanocyte-stimulating hormone (α-MSH) in the central nervous system (CNS). Melanocortin 2 receptor accessory protein 2 (MRAP2) modulates the function of MC4R. We performed cDNA cloning of cat MC4R and MRAP2 and characterized their amino acid sequences, mRNA expression patterns in cat tissues, protein-protein interactions, and functions. We found high sequence homology (>88%) with other mammalian MC4R and MRAP2 encoding 332 and 206 amino acid residues, respectively...
January 19, 2018: General and Comparative Endocrinology
Yeong Ro Lee, Ji-Hae Park, Rodrigo Castaneda Molina, Youn Hee Nam, Yeong-Geun Lee, Bin Na Hong, Nam-In Baek, Tong Ho Kang
The excrement of silkworms (Bombyx mori L.), referred to here as silkworm droppings (SDs), is used as a traditional drug in eastern medicine to treat skin diseases such as urticaria and atopy. However, the depigmentation effects of SDs have not previously been evaluated. We focused on the depigmentation effect of a methanol extract of SDs and isolated components of the extract using a zebrafish model system. (+)-Dehydrovomifoliol (M-1), (6R,7E,9R)-9-hydroxy-4,7-megastigmadien-3-one (M-2), (3S,5R,8R)-3,5-dihydroxymegastigma-6,7-dien-9-one (M-3), roseoside (M-4), and citroside A (M-5) were isolated from only SDs extract (SDE), and chemical structures were identified through spectroscopic methods...
January 22, 2018: Archives of Dermatological Research
Yalan Deng, Yuzhong Xiao, Feixiang Yuan, Yaping Liu, Xiaoxue Jiang, Jiali Deng, Geza Fejes-Toth, Aniko Naray-Fejes-Toth, Shanghai Chen, Yan Chen, Hao Ying, Qiwei Zhai, Yousheng Shu, Feifan Guo
Although central nervous system has been implicated in glucocorticoid-induced fat mass gain, the underlying mechanisms are poorly understood. The aim of our current study was to investigate the possible involvement of hypothalamic serum- and glucocorticoid-regulated kinase 1 (SGK1) in glucocorticoid-increased adiposity. It is well-known that SGK1 expression is induced by acute glucocorticoid treatment, interestingly, we found its expression was decreased in the arcuate nucleus of the hypothalamus, including POMC neurons, following chronic dexamethasone (Dex) treatment...
January 10, 2018: Diabetes
Anna C Thomas, Pauline Heux, Chloe Santos, Wisenave Arulvasan, Nita Solanky, Magalie E Carey, Dianne Gerrelli, Veronica A Kinsler, Heather C Etchevers
BACKGROUND: MC1R, a G-protein coupled receptor with high affinity for alpha-melanocyte stimulating hormone (αMSH), modulates pigment production in melanocytes from many species and is associated with human melanoma risk. MC1R mutations affecting human skin and hair color also have pleiotropic effects on the immune response and analgesia. Variants affecting human pigmentation in utero alter the congenital phenotype of both oculocutaneous albinism and congenital melanocytic naevi, and have a possible effect on birthweight...
January 8, 2018: Birth Defects Research
Ki Wung Chung, Hyeong Oh Jeong, Eun Kyeong Lee, Su Jeong Kim, Pusoon Chun, Hae Young Chung, Hyung Ryong Moon
Abnormal pigmentation owing to excessive melanin synthesis can result in serious problems such as freckles, age-spots, and melanoma. Tyrosinase inhibitors have been an interesting target for the treatment of hyperpigmentation because tyrosinase is the rate-limiting enzyme in melanin synthesis. The screening for strong tyrosinase inhibitors led to the finding of the flavonoid galangin, which showed notable inhibitory effects on mushroom tyrosinase. The IC50 value of galangin (3.55±0.39 µM) was lower than that of kojic acid (48...
2018: Biological & Pharmaceutical Bulletin
Rajender K Motiani, Jyoti Tanwar, Desingu Ayyappa Raja, Ayushi Vashisht, Shivangi Khanna, Sachin Sharma, Sonali Srivastava, Sridhar Sivasubbu, Vivek T Natarajan, Rajesh S Gokhale
Endoplasmic reticulum (ER)-plasma membrane (PM) junctions form functionally active microdomains that connect intracellular and extracellular environments. While the key role of these interfaces in maintenance of intracellular Ca2+ levels has been uncovered in recent years, the functional significance of ER-PM junctions in non-excitable cells has remained unclear. Here, we show that the ER calcium sensor protein STIM1 (stromal interaction molecule 1) interacts with the plasma membrane-localized adenylyl cyclase 6 (ADCY6) to govern melanogenesis...
January 8, 2018: EMBO Journal
Yan Wang, Mi-Mi Hao, Ying Sun, Li-Feng Wang, Hao Wang, Yan-Jun Zhang, Hong-Yan Li, Peng-Wei Zhuang, Zhen Yang
When exposed to ultraviolet radiation, the human skin produces profuse reactive oxygen species (ROS), which in turn activate a variety of biological responses. Mounting ROS levels activate tyrosinase by mobilizing α-melanocyte-stimulating hormone in the epidermis and finally stimulates the melanocytes to produce melanin. Meanwhile, the Keap1-Nrf2/ARE pathway, which removes ROS, is activated at increased ROS levels, and antioxidant compounds facilitates the dissociation of Nrf2. In this study, we explored the possible suppressing effects of antioxidant compounds and tyrosine inhibitors on melanin formation and the promotory effects of these compounds on ROS scavenging...
January 4, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Ralf Paus, Silvia Bulfone-Paus, Marta Bertolini
The collapse of the immune privilege (IP) of the anagen hair bulb is now accepted as a key element in AA pathogenesis, and hair bulb IP restoration lies at the core of AA therapy. Here, we briefly review the essentials of hair bulb IP and recent progress in understanding its complexity. We discuss open questions and why the systematic dissection of hair bulb IP and its pharmacological manipulation (including the clinical testing of FK506 and α-melanocyte-stimulating hormone analogs) promise to extend the range of future therapeutic options in AA and other IP collapse-related autoimmune diseases...
January 2018: Journal of Investigative Dermatology. Symposium Proceedings
Kathleen G Mountjoy, Alexandre Caron, Kristina Hubbard, Avik Shome, Angus C Grey, Bo Sun, Sarah Bould, Martin Middleditch, Beau Pontré, Ailsa McGregor, Paul W R Harris, Renata Kowalczyk, Margaret A Brimble, Rikus Botha, Karen M L Tan, Sarah J Piper, Christina Buchanan, Syann Lee, Anthony P Coll, Joel K Elmquist
OBJECTIVE: Regulation of energy balance depends on pro-opiomelanocortin (POMC)-derived peptides and melanocortin-4 receptor (MC4R). Alpha-melanocyte stimulating hormone (α-MSH) is the predicted natural POMC-derived peptide that regulates energy balance. Desacetyl-α-MSH, the precursor for α-MSH, is present in brain and blood. Desacetyl-α-MSH is considered to be unimportant for regulating energy balance despite being more potent (compared with α-MSH) at activating the appetite-regulating MC4R in vitro...
March 2018: Molecular Metabolism
Bonggi Lee, Kyoung Mi Moon, Jong Seung Lim, Yeojin Park, Do Hyun Kim, Sujin Son, Hyoung Oh Jeong, Dae Hyun Kim, Eun Kyeong Lee, Ki Wung Chung, Hye Jin An, Pusoon Chun, Arnold Y Seo, Ju-Hye Yang, Bong-Seon Lee, Jin Yeul Ma, Won-Kyung Cho, Hyung Ryong Moon, Hae Young Chung
Tyrosinase is a key player in ultraviolet-induced melanogenesis. Because excessive melanin accumulation in the skin can induce hyperpigmentation, the development of tyrosinase inhibitors has attracted attention in cosmetic-related fields. However, side effects including toxicity and low selectivity have limited the use of many tyrosinase inhibitors in cosmetics. We synthesized 12 novel 2-(substituted benzylidene)malononitrile derivatives and investigated their anti-melanogenic activities. Of these 12 compounds, 2-(3, 4-dihydroxy benzylidene)malononitrile (BMN11) exhibited the strongest inhibitory activity against tyrosinase (IC50 = 17...
October 31, 2017: Oncotarget
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