scholarly journals Tyrosinase-Targeting Gallacetophenone Inhibits Melanogenesis in Melanocytes and Human Skin- Equivalents

2020 ◽  
Vol 21 (9) ◽  
pp. 3144 ◽  
Author(s):  
Ji Young Lee ◽  
Jooyun Lee ◽  
Daejin Min ◽  
Juewon Kim ◽  
Hyoung-June Kim ◽  
...  
Keyword(s):  
Human Skin ◽  
Hydrophobic Interactions ◽  
Copper Ions ◽  
Inhibitory Effect ◽  
Compound Library ◽  
Tyrosinase Inhibition ◽  
Skin Model ◽  
Cosmetic Industry ◽  
Key Enzyme ◽  
Computational Molecular Modeling

Demands for safe depigmentation compounds are constantly increasing in the pharmaceutical and cosmetic industry, since the numerous relevant compounds reported to date have shown undesirable side effects or low anti-melanogenic effects. In this study, we reported three novel inhibitors of tyrosinase, which is the key enzyme in melanogenesis, identified using docking-based high throughput virtual screening of an in-house natural compound library followed by mushroom tyrosinase inhibition assay. Of the three compounds, gallacetophenone showed high anti-melanogenic effect in both human epidermal melanocytes and a 3D human skin model, MelanoDerm. The inhibitory effect of gallacetophenone on tyrosinase was elucidated by computational molecular modeling at the atomic level. Binding of gallacetophenone to the active site of tyrosinase was found to be stabilized by hydrophobic interactions with His367, Ile368, and Val377; hydrogen bonding with Ser380 and a water molecule bridging the copper ions. Thus, our results strongly suggested gallacetophenone as an anti-melanogenic ingredient that inhibits tyrosinase.

Increased pro‐collagen 1, elastin, and TGF‐β1 expression by copper ions in an ex‐vivo human skin model

2019 ◽  
Vol 19 (6) ◽  
pp. 1522-1527 ◽  
Author(s):  
Navit Ogen‐Shtern ◽  
Katerina Chumin ◽  
Guy Cohen ◽  
Gadi Borkow
Keyword(s):  
Human Skin ◽  
Copper Ions ◽  
Ex Vivo ◽  
Skin Model ◽  
Tgf Β1

scholarly journals Estimation of Inhibitory Effect against Tyrosinase Activity through Homology Modeling and Molecular Docking

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Daungkamon Nokinsee ◽  
Lalida Shank ◽  
Vannajan Sanghiran Lee ◽  
Piyarat Nimmanpipug
Keyword(s):  
Md Simulation ◽  
Inhibitory Effect ◽  
Human Model ◽  
Mushroom Tyrosinase ◽  
Whitening Agent ◽  
Human Enzyme ◽  
Cosmetic Industry ◽  
Key Enzyme ◽  
Docking Calculations ◽  
Automated Docking

Tyrosinase is a key enzyme in melanogenesis. Generally, mushroom tyrosinase from A. bisporus had been used as a model in skin-whitening agent tests employed in the cosmetic industry. The recently obtained crystal structure of bacterial tyrosinase from B. megaterium has high similarity (33.5%) to the human enzyme and thus it was used as a template for constructing of the human model. Binding of tyrosinase to a series of its inhibitors was simulated by automated docking calculations. Docking and MD simulation results suggested that N81, N260, H263, and M280 are involved in the binding of inhibitors to mushroom tyrosinase. E195 and H208 are important residues in bacterial tyrosinase, while E230, S245, N249, H252, V262, and S265 bind to inhibitors and are important in forming pi interaction in human tyrosinase.

scholarly journals Novel Inhibitory Effect of N-(2-Hydroxycyclohexyl)valiolamine on Melanin Production in a Human Skin Model

2014 ◽  
Vol 15 (7) ◽  
pp. 12188-12195 ◽  
Author(s):  
Bum-Ho Bin ◽  
Yung Joo ◽  
Ai-Young Lee ◽  
Song Shin ◽  
Eun-Gyung Cho ◽  
...  
Keyword(s):  
Human Skin ◽  
Inhibitory Effect ◽  
Skin Model ◽  
Melanin Production

scholarly journals Disinfectant effectiveness against SARS-CoV-2 and influenza viruses present on human skin: model-based evaluation

2021 ◽  
Author(s):  
Ryohei Hirose ◽  
Risa Bandou ◽  
Hiroshi Ikegaya ◽  
Naoto Watanabe ◽  
Takuma Yoshida ◽  
...  
Keyword(s):  
Human Skin ◽  
Influenza Viruses ◽  
Skin Model ◽  
Model Based

scholarly journals Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents

2021 ◽  
Vol 4 (1) ◽  
Author(s):  
Vicky Mody ◽  
Joanna Ho ◽  
Savannah Wills ◽  
Ahmed Mawri ◽  
Latasha Lawson ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dynamics Simulation ◽  
Simulation Studies ◽  
Inhibitory Effects ◽  
Major Threat ◽  
Main Protease ◽  
Approved Drugs ◽  
Fda Approved Drugs ◽  
Computational Molecular Modeling

AbstractEmerging outbreak of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection is a major threat to public health. The morbidity is increasing due to lack of SARS-CoV-2 specific drugs. Herein, we have identified potential drugs that target the 3-chymotrypsin like protease (3CLpro), the main protease that is pivotal for the replication of SARS-CoV-2. Computational molecular modeling was used to screen 3987 FDA approved drugs, and 47 drugs were selected to study their inhibitory effects on SARS-CoV-2 specific 3CLpro enzyme in vitro. Our results indicate that boceprevir, ombitasvir, paritaprevir, tipranavir, ivermectin, and micafungin exhibited inhibitory effect towards 3CLpro enzymatic activity. The 100 ns molecular dynamics simulation studies showed that ivermectin may require homodimeric form of 3CLpro enzyme for its inhibitory activity. In summary, these molecules could be useful to develop highly specific therapeutically viable drugs to inhibit the SARS-CoV-2 replication either alone or in combination with drugs specific for other SARS-CoV-2 viral targets.

scholarly journals Creation of Ionically Crosslinked Tri-Layered Chitosan Membranes to Simulate Different Human Skin Properties

Materials ◽  
2021 ◽  
Vol 14 (7) ◽  
pp. 1807
Author(s):  
Rocío Guerle-Cavero ◽  
Blanca Lleal-Fontàs ◽  
Albert Balfagón-Costa
Keyword(s):  
Elastic Modulus ◽  
Human Skin ◽  
Sodium Tripolyphosphate ◽  
Snow Crab ◽  
Suitable Material ◽  
Cosmetic Industry ◽  
Novel Method ◽  
Current Article ◽  
Chitosan Membranes

In 2023, new legislation will ban the use of animals in the cosmetic industry worldwide. This fact, together with ethical considerations concerning the use of animals or humans in scientific research, highlights the need to propose new alternatives for replacing their use. The aim of this study is to create a tri-layered chitosan membrane ionically crosslinked with sodium tripolyphosphate (TPP) in order to simulate the number of layers in human skin. The current article highlights the creation of a membrane where pores were induced by a novel method. Swelling index, pore creation, and mechanical property measurements revealed that the swelling index of chitosan membranes decreased and, their pore formation and elasticity increased with an increase in the Deacetylation Grade (DDA). Additionally, the results demonstrate that chitosan’s origin can influence the elastic modulus value and reproducibility, with higher values being obtained with seashell than snow crab or shrimp shells. Furthermore, the data show that the addition of each layer, until reaching three layers, increases the elastic modulus. Moreover, if layers are crosslinked, the elastic modulus increases to a much greater extent. The characterization of three kinds of chitosan membranes was performed to find the most suitable material for studying different human skin properties.

Basic Red 51, a permitted semi-permanent hair dye, is cytotoxic to human skin cells: Studies in monolayer and 3D skin model using human keratinocytes (HaCaT)

2014 ◽  
Vol 227 (2) ◽  
pp. 139-149 ◽  
Author(s):  
Thalita B. Zanoni ◽  
Manoela Tiago ◽  
Fernanda Faião-Flores ◽  
Silvia B. de Moraes Barros ◽  
Aalt Bast ◽  
...  
Keyword(s):  
Human Skin ◽  
Human Keratinocytes ◽  
Skin Model ◽  
Hair Dye ◽  
Skin Cells ◽  
Human Skin Cells ◽  
3D Skin

scholarly journals Development and Evaluation of a Topical Anti-Inflammatory Preparation Containing Dodonaea polyandra Extract

2015 ◽  
Vol 18 (4) ◽  
pp. 578 ◽  
Author(s):  
Bradley S Simpson ◽  
Xianling Luo ◽  
Jiping Wang ◽  
Yunmei Song ◽  
David Claudie ◽  
...  
Keyword(s):  
Phase Separation ◽  
Human Skin ◽  
Dosage Form ◽  
Interleukin 1 ◽  
In Vitro Release ◽  
Skin Inflammation ◽  
Skin Model ◽  
Inflammation Model ◽  
Anti Inflammatory

Purpose: We have previously reported that the Australian Northern Kaanju (Kuuku I’yu) medicinal plant Dodonaea polyandra has anti-inflammatory activity. This is attributed largely to the presence of clerodane diterpenoids contained within the leaf resin. We envisaged developing a topical preparation to treat indications relating to skin inflammation. However, it was unknown whether the resin could be incorporated into a suitable dosage form while retaining the therapeutic value demonstrated in previous work. Therefore, the following study was undertaken to assess parameters of safety and efficacy for a prototype formulation containing the leaf resin extracted from D. polyandra. Methods: Using the assessment criteria of optimum appearance, tactile feeling, spreadability and odour, 78 different formulations were developed. Formulation stability was assessed using a centrifugal test with preparations displaying phase separation further modified or re-formulated. A prototype formulation containing 5% w/w plant resin was selected and subjected to in vitro release studies. This was quantified through HPLC analysis using two major bioactive diterpenoids as reference. The prototype formulation was tested for efficacy in a TPA-induced acute murine skin inflammation model as well as a 3D human skin model for irritancy/toxicity (Epiderm™). Results: The prototype resin cream was a chartreuse-coloured homogenous semisolid preparation that was readily spreadable upon contact with skin with no sensation of tackiness, residual greasiness, or irritation. The optimized cream showed no phase separation after 30 min centrifugation at 825 g. In the TPA-induced inflammation model, the resin formulation significantly reduced ear thickness and interleukin-1 beta levels in mouse ear tissue. The 5% w/w resin cream formulation showed no irritancy in a 3D human skin model. Conclusions: Our results demonstrate that bioactive resin from D. polyandra can be formulated into a stable and non-irritant semi-solid dosage form and reduce parameters of acute skin inflammation in vivo. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Human skin model capable of natural shape variation

1988 ◽  
Vol 3 (5) ◽  
pp. 265-271 ◽  
Author(s):  
Koji Komatsu
Keyword(s):  
Human Skin ◽  
Shape Variation ◽  
Skin Model

Molecular characterization of reconstructed skin model by Raman microspectroscopy: Comparison with excised human skin

Biopolymers ◽  
2007 ◽  
Vol 87 (4) ◽  
pp. 261-274 ◽  
Author(s):  
Ali Tfayli ◽  
Olivier Piot ◽  
Florence Draux ◽  
Franck Pitre ◽  
Michel Manfait
Keyword(s):  
Molecular Characterization ◽  
Human Skin ◽  
Raman Microspectroscopy ◽  
Skin Model ◽  
Reconstructed Skin
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