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https://www.readbyqxmd.com/read/28340400/pharmacoinformatics-exploration-of-polyphenol-oxidases-leading-to-novel-inhibitors-by-virtual-screening-and-molecular-dynamic-simulation-study
#1
Mubashir Hassan, Qamar Abbas, Zaman Ashraf, Ahmed A Moustafa, Sung-Yum Seo
Polyphenol oxidases (PPOs)/tyrosinases are metal-dependent enzymes and known as important targets for melanogenesis. Although considerable attempts have been conducted to control the melanin-associated diseases by using various inhibitors. However, the exploration of the best anti-melanin inhibitor without side effect still remains a challenge in drug discovery. In present study, protein structure prediction, ligand-based pharmacophore modeling, virtual screening, molecular docking and dynamic simulation study were used to screen the strong novel inhibitor to cure melanogenesis...
March 15, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28333105/anti-melanogenic-properties-of-greek-plants-a-novel-depigmenting-agent-from-morus-alba-wood
#2
Eliza Chaita, George Lambrinidis, Christina Cheimonidi, Adamantia Agalou, Dimitris Beis, Ioannis Trougakos, Emmanuel Mikros, Alexios-Leandros Skaltsounis, Nektarios Aligiannis
In therapeutic interventions associated with melanin hyperpigmentation, tyrosinase is regarded as a target enzyme as it catalyzes the rate-limiting steps in mammalian melanogenesis. Since many known agents have been proven to be toxic, there has been increasing impetus to identify alternative tyrosinase inhibitors, especially from natural sources. In this study, we investigated 900 extracts from Greek plants for potential tyrosinase inhibitive properties. Among the five most potent extracts, the methanol extract of Morus alba wood (MAM) demonstrated a significant reduction in intracellular tyrosinase and melanin content in B16F10 melanoma cells...
March 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28303328/effects-of-palmitoyl-kvk-l-ascorbic-acid-on-skin-wrinkles-and-pigmentation
#3
Hyeong Mi Kim, Hyo Sun An, Jung-Soo Bae, Jung Yun Kim, Chi Ho Choi, Ju Yeon Kim, Joo Hyuck Lim, Joon-Hun Choi, Hyunnam Song, Sung Ho Moon, Young Jun Park, Shin-Jae Chang, Sun Young Choi
Wrinkle formation and abnormal pigmentation are major clinical alterations associated with skin aging. As the aim of our study was to investigate the effects of palmitoyl-KVK-L-ascorbic acid on skin aging, the anti-wrinkle and depigmentation effects of palmitoyl-KVK-L-ascorbic acid were evaluated by measuring collagen expression in dermal fibroblast cells and inhibition of melanogenesis in B16F1 cells, respectively. The anti-aging effect of palmitoyl-KVK-L-ascorbic acid cream was also evaluated against a placebo cream in a clinical trial...
March 16, 2017: Archives of Dermatological Research
https://www.readbyqxmd.com/read/28283753/cosmetic-applications-of-glucitol-core-containing-gallotannins-from-a-proprietary-phenolic-enriched-red-maple-acer-rubrum-leaves-extract-inhibition-of-melanogenesis-via-down-regulation-of-tyrosinase-and-melanogenic-gene-expression-in-b16f10-melanoma-cells
#4
Hang Ma, Jialin Xu, Nicholas A DaSilva, Ling Wang, Zhengxi Wei, Liangran Guo, Shelby L Johnson, Wei Lu, Jun Xu, Qiong Gu, Navindra P Seeram
The red maple (Acer rubrum) is a rich source of phenolic compounds which possess galloyl groups attached to different positions of a 1,5-anhydro-D-glucitol core. While these glucitol-core containing gallotannins (GCGs) have reported anti-oxidant and anti-glycative effects, they have not yet been evaluated for their cosmetic applications. Herein, the anti-tyrosinase and anti-melanogenic effects of a proprietary phenolic-enriched red maple leaves extract [Maplifa(™); contains ca. 45% ginnalin A (GA) along with other GCGs] were investigated using enzyme and cellular assays...
March 10, 2017: Archives of Dermatological Research
https://www.readbyqxmd.com/read/28279786/miltefosine-is-fungicidal-to-paracoccidioides-spp-yeast-cells-but-subinhibitory-concentrations-induce-melanisation
#5
Diego Conrado Pereira Rossi, Cristina de Castro Spadari, Joshua Daniel Nosanchuk, Carlos Pelleschi Taborda, Kelly Ishida
Paracoccidioidomycosis (PCM) is a systemic mycosis caused by the dimorphic fungi Paracoccidioides spp. The duration of antifungal treatment ranges from months to years and relapses may nevertheless occur despite protracted therapy. Thus, there remains an urgent need for new therapeutic options. Miltefosine (MLT), an analogue of alkylphospholipids, has antifungal activity against species of yeast and filamentous fungi. The aim of this study was to evaluate the antifungal effects of MLT on the yeast forms of Paracoccidioides brasiliensis and Paracoccidioides lutzii...
March 6, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28278663/melanogenesis-inhibitors-from-coix-lacryma-jobi-seeds-in-b16-f10-melanoma-cells
#6
Yhiya Amen, Enos Tangke Arung, Mohamed S Afifi, Ahmed F Halim, Ahmed Ashour, Ryoji Fujimoto, Takahiro Goto, Kuniyoshi Shimizu
An adenine derivative, 9-β-D-glucopyranosyl adenine, reported for the first time from a natural source, in addition to nine known compounds were isolated from the seeds of Coix lacryma-jobi. Their structures were elucidated based on extensive spectroscopic and chemical studies. The isolated compounds and the ethanol extract have been assayed for melanin inhibition using B16-F10 melanoma cell line. The results of our study suggested the potential use of Coix lacryma-jobi seeds as a skin whitening agent and reveal the seeds to be a rich source of important phytochemicals with melanogenesis inhibitory activity...
February 16, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28271633/pheomelanogenesis-is-promoted-at-a-weakly-acidic-ph
#7
Kazumasa Wakamatsu, Ayano Nagao, Miu Watanabe, Kenta Nakao, Shosuke Ito
The diversity of pigmentation in the skin, hair and eyes of humans has been largely attributed to the diversity of pH in melanosomes with an acidic pH being proposed to suppress melanin production, especially eumelanogenesis. We previously showed that an acidic pH greatly suppresses the late stage of eumelanogenesis after the dopachrome stage. The oxidation of tyrosine by tyrosinase in the presence of cysteine forms cysteinyldopa isomers, which are further oxidized to give rise to pheomelanin via benzothiazine intermediates...
March 8, 2017: Pigment Cell & Melanoma Research
https://www.readbyqxmd.com/read/28268138/chemical-and-bioactivity-of-flavanones-obtained-from-roots-of-dalea-pazensis-rusby
#8
María D Santi, Mariana A Peralta, Caterine S Mendoza, José Luis Cabrera, María G Ortega
Two new prenylated flavanones, pazentin A (3',4'-dihydroxy-6,2'-diprenylpinocembrin, 1) and pazentin B [4'-hydroxy-2'-methoxy-5'-(1‴, 1‴-dimethylallyl)-6-prenylpinocembrin, 2] together with two known ones (3 and 4) previously isolated from other Dalea species were obtained from the benzene extract of Dalea pazensis Rusby roots. The compounds were evaluated in vitro for their inhibition on mushroom tyrosinase enzyme and in relation to their effect on melanogenesis in B16 murine melanoma cells, by using a spectrophotometric method...
February 27, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28241436/gomisin-n-inhibits-melanogenesis-through-regulating-the-pi3k-akt-and-mapk-erk-signaling-pathways-in-melanocytes
#9
Jae Kyoung Chae, Lalita Subedi, Minsun Jeong, Yong Un Park, Chul Young Kim, Hakwon Kim, Sun Yeou Kim
Gomisin N, one of the lignan compounds found in Schisandra chinensis has been shown to possess anti-oxidative, anti-tumorigenic, and anti-inflammatory activities in various studies. Here we report, for the first time, the anti-melenogenic efficacy of Gomisin N in mammalian cells as well as in zebrafish embryos. Gomisin N significantly reduced the melanin content without cellular toxicity. Although it was not capable of modulating the catalytic activity of mushroom tyrosinase in vitro, Gomisin N downregulated the expression levels of key proteins that function in melanogenesis...
February 22, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28204812/the-lactoferricin-b-derived-peptide-lfb17-34-induces-melanogenesis-in-b16f10-cells
#10
Hsiu-Chin Huang, Hsuan Lin, Min-Chuan Huang
Lactoferricin B (LfcinB), a peptide of bovine lactoferrin (LfB), exhibits multiple biological functions, including antimicrobial, antiviral, antioxidant and immunomodulatory activities. However, the role of LfcinB-related peptides in melanogenesis remains unclear. In this study, a set of five LfcinB-related peptides was examined. We found that LfB17‑34, an 18-mer LfcinB-derived peptide, increased melanogenesis in B16F10 melanoma cells without significantly affecting cell viability. LfB17‑34 increased in vitro tyrosinase activity and melanin content in a dose-dependent manner...
March 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28192140/action-of-2-2-4-4-tetrahydroxybenzophenone-in-the-biosynthesis-pathway-of-melanin
#11
Antonio Garcia-Jimenez, Jose Antonio Teruel-Puche, Pedro Antonio Garcia-Ruiz, Jose Berna, Jose Neptuno Rodríguez-López, Jose Tudela, Francisco Garcia-Canovas
2,2',4,4'-tetrahydroxybenzophenone (Uvinul D50), a sunscreen used in cosmetics, has two effects in the melanin biosynthesis pathway. On the one hand, it acts a weak inhibitor of tyrosinase and on the other, it accelerates the conversion of dopachrome to melanin. Uvinul D50 was seen to behave as a weak competitive inhibitor: apparent constant inhibition=2.02±0.09mM and IC50=3.82±0.39mM established in this work. These values are higher than those in the bibliography, which tend to be undersetimated. This discrepancy could be explained by the reaction of Uvinul D50 with the dopachrome produced from l-tyrosine or l-dopa, which would interfere in the measurement...
May 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28185012/the-synergistic-effect-of-maltose-enhances-the-anti-melanogenic-activity-of-acarbose
#12
Bum-Ho Bin, Sung Tae Kim, Jinhyuk Bhin, Kyounghee Byoun, Tae Ryong Lee, Eun-Gyung Cho
Melanocytes play an important role in maintaining epidermal homeostasis by producing melanin and protecting the skin from harmful environmental factors. However, excessive up- or down-regulation of melanin production often causes hyper- or hypo-pigmented disorders, respectively, which affect the patient's quality of life. Therefore, various strategies for modulating melanin levels have been developed by the pharmaceutical and cosmetic industries. We reported previously that voglibose, which is a well-known anti-hyperglycemic agent, could be used as an anti-melanogenic agent by inhibiting α-glucosidase activity and reducing tyrosinase protein levels...
April 2017: Archives of Dermatological Research
https://www.readbyqxmd.com/read/28182699/bifunctional-effects-of-o-methylated-flavones-from-scutellaria-baicalensis-georgi-on-melanocytes-inhibition-of-melanin-production-and-intracellular-melanosome-transport
#13
Michiko Kudo, Kumiko Kobayashi-Nakamura, Kentaro Tsuji-Naito
The growing interest in skin lightening has recently renewed attention on the esthetic applications of Chinese herbal medicine. Although Scutellaria baicalensis Georgi is used for antipyretic and antiinflammatory purposes, its whitening effect remains unclear. This study reports three major findings: (1) S. baicalensis has a potent inhibitory effect on melanogenesis; (2) wogonin and its glycoside are the active components of S. baicalensis; and (3) O-methylated flavones from S. baicalensis, such as wogonin, inhibit intracellular melanosome transport...
2017: PloS One
https://www.readbyqxmd.com/read/28174022/the-evolution-and-genetics-of-carotenoid-processing-in-animals
#14
REVIEW
David P L Toews, Natalie R Hofmeister, Scott A Taylor
Coloration is one of the most conspicuous traits that varies among organisms. Carotenoid pigments are responsible for many of the red, orange, and yellow colors in the natural world and, at least for most animals, these molecules must be acquired from their environment. Identifying genes important for carotenoid transport, deposition, and processing has been difficult, in contrast to the well-characterized genes involved in the melanogenesis pathways. We review recent progress in the genetics of carotenoid processing, advances owing in part to the application of high-throughput sequencing data...
February 4, 2017: Trends in Genetics: TIG
https://www.readbyqxmd.com/read/28165370/plumbagin-suppresses-%C3%AE-msh-induced-melanogenesis-in-b16f10-mouse-melanoma-cells-by-inhibiting-tyrosinase-activity
#15
Taek-In Oh, Jeong-Mi Yun, Eun-Ji Park, Young-Seon Kim, Yoon-Mi Lee, Ji-Hong Lim
Recent studies have shown that plumbagin has anti-inflammatory, anti-allergic, antibacterial, and anti-cancer activities; however, it has not yet been shown whether plumbagin suppresses alpha-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis to prevent hyperpigmentation. In this study, we demonstrated that plumbagin significantly suppresses α-MSH-stimulated melanin synthesis in B16F10 mouse melanoma cells. To understand the inhibitory mechanism of plumbagin on melanin synthesis, we performed cellular or cell-free tyrosinase activity assays and analyzed melanogenesis-related gene expression...
February 3, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28165285/lactoferrin-inhibits-melanogenesis-by-down-regulating-mitf-in-melanoma-cells-and-normal-melanocytes
#16
Nanase Ishii, Mizuyuki Ryu, Yasushi A Suzuki
The aim of this study was to evaluate the effect of bovine lactoferrin (bLf) on melanin-producing cells and to elucidate its mechanism of action. We tested the anti-melanogenic effect of bLf on a 3-dimensional cultured pigmentation skin model and confirmed a 20% reduction in pigmentation, suggesting that bLf was transdermally absorbed and it suppressed melanin production. Treatment of human melanoma cells with bLf resulted in a significant, dose-dependent suppression of melanin production. Apo-bLf and holo-bLf suppressed melanogenesis to the same degree as bLf...
February 2017: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
https://www.readbyqxmd.com/read/28152530/the-preventive-effect-of-coffee-compounds-on-dermatitis-and-epidermal-pigmentation-after-ultraviolet-irradiation-in-mice
#17
Yurika Yamate, Keiichi Hiramoto, Eisuke F Sato
BACKGROUND: Ultraviolet (UV) irradiation is well known to promote inflammation and pigmentation of skin. UVB mainly affects dermatitis and pigmentation. Coffee contains a number of polyphenols, such as caffeic acid (CA) and chlorogenic acid (CGA) but their in vivo bioactivity for photobiology remains unclear. METHODS: C57BL/6j male mice were irradiated with UVB (1.0 kJ/m2/day) for 3 days. Five days after the final session of UVB irradiation, the dorsal skin, ear epidermis, and blood samples were analyzed to investigate the inflammatory factors, melanogenesis factors and related hormones...
2017: Skin Pharmacology and Physiology
https://www.readbyqxmd.com/read/28133910/tranexamic-acid-in-treatment-of-melasma-a-comprehensive-review-of-clinical-studies
#18
REVIEW
Mohammad Taraz, Somayeh Niknam, Amir Houshang Ehsani
Melasma is a human melanogenesis dysfunction that results in localized, chronic acquired hyperpigmentation of the skin. It has a significant impact on appearance, causing psychosocial and emotional distress, and reducing the quality of life of the affected patients. Tranexamic acid (TA) is a plasmin inhibitor used to prevent abnormal fibrinolysis to reduce blood loss and exerts its effect by reversibly blocking lysine binding sites on plasminogen molecules, thus inhibiting plasminogen activator (PA) from converting plasminogen to plasmin...
January 30, 2017: Dermatologic Therapy
https://www.readbyqxmd.com/read/28130732/zebrafish-phosvitin-derived-peptide-pt5-inhibits-melanogenesis-via-camp-pathway
#19
Yuan-Yuan Liu, Xiu-Rong Su, Shou-Sheng Liu, Shuang-Shuang Yang, Cheng-Yan Jiang, Yu Zhang, Shicui Zhang
Zebrafish phosvitin-derived peptide Pt5, consisting of the C-terminal 55 residues of phosvitin, has been shown to have an antimicrobial-immunomodulatory activity comparable to phosvitin. Here, we showed clearly that Pt5 had the capacity to inhibit tyrosinase (TYR) activity and melanin biosynthesis, and this inhibition was independent of cell proliferation and cytotoxic effects. Incubation of fluorescein isothiocyanate (FITC)-labeled Pt5 with B16F10 melanoma cells revealed that Pt5 was localized in the cytoplasm of the cells...
January 27, 2017: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/28127878/melanin-is-effective-in-protecting-fast-and-slow-growing-fungi-from-various-types-of-ionizing-radiation
#20
Claudia Pacelli, Ruth A Bryan, Silvano Onofri, Laura Selbmann, Igor Shuryak, Ekaterina Dadachova
Melanin is a ubiquitous pigment with unique physicochemical properties. The resistance of melanized fungi to cosmic and terrestrial ionizing radiation suggests that melanin also plays a pivotal role in radioprotection. In this study, we compared the effects of densely-ionizing deuterons and sparsely-ionizing X-rays on two microscopic fungi capable of melanogenesis. We utilized the fast-growing pathogenic basiodiomycete forming an induced DOPA-melanin, Cryptococcus neoformans (CN); and the slow-growing environmental rock-inhabiting ascomycete synthesizing a constitutive DHN-melanin, Cryomyces antarcticus (CA); melanized and non-melanized counterparts were compared...
January 27, 2017: Environmental Microbiology
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