Effect of captopril on mushroom tyrosinase activity in vitro

2001 ◽  
Vol 1544 (1-2) ◽  
pp. 289-300 ◽  
Author(s):  
Juan Carlos Espín ◽  
Harry J. Wichers
Keyword(s):  
Tyrosinase Activity ◽  
Mushroom Tyrosinase

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 Evaluation ofCinnamomum osmophloeumKanehira Extracts on Tyrosinase Suppressor, Wound Repair Promoter, and Antioxidant

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Man-Gang Lee ◽  
Su-Yu Kuo ◽  
Shih-Yu Yen ◽  
Hsia-Fen Hsu ◽  
Chung-Hang Leung ◽  
...  
Keyword(s):  
Free Radical ◽  
Wound Repair ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Tyrosinase Activity ◽  
Control Group ◽  
Minor Effect ◽  
Petroleum Jelly ◽  
Mushroom Tyrosinase

Cinnamomum osmophloeumKanehira belongs to the Lauraceae family of Taiwan’s endemic plants. In this study,C. osmophloeumKanehira extract has shown inhibition of tyrosinase activity on B16-F10 cellular system first. Whether extracts inhibited mushroom tyrosinase activity was tested, and a considerable inhibition of mushroom tyrosinase activity byin vitroassays was presented. Animal experiments ofC. osmophloeumKanehira were carried out by observing animal wound repair, and the extracts had greater wound healing power than the vehicle control group (petroleum jelly with 8% DMSO, w/v). In addition, the antioxidant capacity ofC. osmophloeumKanehira extractsin vitrowas evaluated. We measuredC. osmophloeumKanehira extract’s free radical scavenging capability, metal chelating, and reduction power, such as biochemical activity analysis. The results showed that a high concentration ofC. osmophloeumKanehira extract had a significant scavenging capability of free radical, a minor effect of chelating ability, and moderate reducing power. Further exploration of the possible physiological mechanisms and the ingredient components of skincare product for skin-whitening, wound repair, or antioxidative agents are to be done.

scholarly journals Novel Anti-Melanogenic Compounds, (Z)-5-(Substituted Benzylidene)-4-thioxothiazolidin-2-one Derivatives: In Vitro and In Silico Insights

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4963
Author(s):  
Heejeong Choi ◽  
Il Young Ryu ◽  
Inkyu Choi ◽  
Sultan Ullah ◽  
Hee Jin Jung ◽  
...  
Keyword(s):  
Active Site ◽  
Kojic Acid ◽  
Docking Simulation ◽  
Tyrosinase Activity ◽  
In Vitro Assays ◽  
Mushroom Tyrosinase ◽  
Tyrosinase Inhibitors ◽  
Melanin Contents ◽  
Human Tyrosinase

To confirm that the β-phenyl-α,β-unsaturated thiocarbonyl (PUSTC) scaffold, similar to the β-phenyl-α,β-unsaturated carbonyl (PUSC) scaffold, acts as a core inhibitory structure for tyrosinase, twelve (Z)-5-(substituted benzylidene)-4-thioxothiazolidin-2-one ((Z)-BTTZ) derivatives were designed and synthesized. Seven of the twelve derivatives showed stronger inhibitory activity than kojic acid against mushroom tyrosinase. Compound 2b (IC50 = 0.47 ± 0.97 µM) exerted a 141-fold higher inhibitory potency than kojic acid. Kinetic studies’ results confirmed that compounds 2b and 2f are competitive tyrosinase inhibitors, which was supported by high binding affinities with the active site of tyrosinase by docking simulation. Docking results using a human tyrosinase homology model indicated that 2b and 2f might potently inhibit human tyrosinase. In vitro assays of 2b and 2f were conducted using B16F10 melanoma cells. Compounds 2b and 2f significantly and concentration-dependently inhibited intracellular melanin contents, and the anti-melanogenic effects of 2b at 10 µM and 2f at 25 µM were considerably greater than the inhibitory effect of kojic acid at 25 µM. Compounds 2b and 2f similarly inhibited cellular tyrosinase activity and melanin contents, indicating that the anti-melanogenic effects of both were due to tyrosinase inhibition. A strong binding affinity with the active site of tyrosinase and potent inhibitions of mushroom tyrosinase, cellular tyrosinase activity, and melanin generation in B16F10 cells indicates the PUSTC scaffold offers an attractive platform for the development of novel tyrosinase inhibitors.

scholarly journals A Newly Authenticated Compound from Traditional Chinese Medicine Decoction Induces Melanogenesis in B16-F10 Cells by Increasing Tyrosinase Activity

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Xiu Juan Xin ◽  
Jiahong Zou ◽  
Tao Zou ◽  
Huoli Shang ◽  
Li Yun Sun
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Cell Number ◽  
Tyrosinase Activity ◽  
Chinese Traditional Medicine ◽  
Inhibition Rate ◽  
Disease Treatment ◽  
Protein Levels ◽  
Stimulation Of

Vitiligo is a kind of skin dysfunction on melanogenesis. The highly prevalent, chronic, and distinctive complexion changes on patients have imposed enormous psychic and economic burden on both individuals and society. Traditional Chinese Medicine (TCM) is a kind of precious source on chronic disease treatment, including skin dysfunctional diseases. In our previous study, a new compound named apigenin-7-butylene glucoside has been authenticated and purified from a prescription of Chinese traditional medicine formula which has been used clinically in vitiligo treatment. The aim of this work is to evaluate the effects of this compound on melanogenesis using melanoma cell B16-F10 in vitro. The results showed that apigenin-7-butylene glucoside had almost no cytotoxicity on B16-F10 cells within a lower dose of 5.0 μg ml-1 and enhanced the melanin level to about 41% and tyrosinase activity to 1.32-fold when compared with controls. The compound showed minor cytotoxicity to B16-F10 cells at the higher concentration of 10 μg ml-1 and 50 μg ml-1, the inhibition rate was 8.4% and 11.8%, and the melanin level and tyrosinase activity showed a decreased trend because of the lower cell number at the higher concentrations. The results indicated that apigenin-7-butylene glucoside was safe to B16-F10 cells within a lower concentration, <5.0 μg ml-1. Incubated with 5.0 ug ml-1of apigenin-7-butylene glucoside for 48 hours, the mRNA and protein levels of Tyr, Trp-1, and Trp-2 genes were all increased except Mitf in B16-F10 cells. The stimulation of apigenin-7-butylene glucoside on melanogenesis of B16-F10 cells through Tyr, Trp-1, and Trp-2 pathway highlighted the potential usage of the compound in vitiligo treatment.

scholarly journals Effect of chrysin omega‐3 and 6 fatty acid esters on mushroom tyrosinase activity, stability, and structure

2018 ◽  
pp. e12728
Author(s):  
Zohreh Jamali ◽  
Gholamreza Rezaei Behbehani ◽  
Karim Zare ◽  
Nematollah Gheibi
Keyword(s):  
Fatty Acid ◽  
Tyrosinase Activity ◽  
Fatty Acid Esters ◽  
Mushroom Tyrosinase ◽  
Omega 3 ◽  
Acid Esters

Investigation of tyrosinase inhibition by some 1,2,4 triazole derivative compounds: in vitro and in silico mechanisms

2018 ◽  
Vol 44 (4) ◽  
pp. 473-481
Author(s):  
Elif Ayazoglu Demir ◽  
Ahmet Colak ◽  
Aylin Kalfa ◽  
Ahmet Yasar ◽  
Olcay Bekircan ◽  
...  
Keyword(s):  
Critical Role ◽  
Docking Studies ◽  
Biosynthesis Pathway ◽  
Mushroom Tyrosinase ◽  
Tyrosinase Inhibitor ◽  
Effective Inhibitor ◽  
Tyrosinase Inhibition ◽  
Triazole Derivative

Abstract Background Tyrosinase plays a central role in the biosynthesis pathway of melanin pigment. Melanin protects human skin against radiation and its unusual levels cause some skin disorders such as pregnancy scar, oldness spots and melanoma. Tyrosinase has also been linked to Parkinson’s and other neurodegenerative diseases. In addition, melanin plays a critical role as a defense molecule for insects during wound healing and is important for their life. Therefore, determination of inhibitor molecules for tyrosinase has a promising potential for therapies of some diseases and is an alternative method for keeping insects under control. Material and methods In this study, 1-hepthyl-3-(4-methoxybenzyl)-4H-1,2,4-triazole-5-one derivative (A6, A8, A15) and 3-(4-chlorophenyl)- 5-(4-methoxybenzyl)-4H-1,2,4-triazole (B5, B9, B13) derivative compounds were evaluated in terms of their potential for mushroom tyrosinase inhibition. IC50 values of these six molecules were determined. Results It was seen that B9 molecule was the most effective inhibitor. Docking studies also nearly supported this end result. Tyrosinase inhibition type and Ki value were found to be uncompetitive and 370.7±0.3 μM, respectively, in the presence of B9 compound. Conclusion These results suggest that B9 compound is a potential tyrosinase inhibitor.

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

ROS-scavenging and Anti-tyrosinase Properties of Crocetin on B16F10 Murine Melanoma Cells

2018 ◽  
Vol 18 (7) ◽  
pp. 1064-1069 ◽  
Author(s):  
Seyed H. Hashemi-Shahri ◽  
Alireza Golshan ◽  
Seyed A. Mohajeri ◽  
Javad Baharara ◽  
Elaheh Amini ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Melanoma Cells ◽  
Biological Properties ◽  
B16 Melanoma ◽  
Tyrosinase Activity ◽  
Crocus Sativus ◽  
Mushroom Tyrosinase ◽  
Ros Scavenging ◽  
Protein Levels ◽  
B16 Melanoma Cells

Background: Crocus sativus (Iridaceae) has been traditionally used in the Iranian folk medicine and as a culinary additive. Major components of the plant that are responsible for biological properties are saffranal, crocin, picrocrocin and crocetin. Although the level of crocetin is not high, some of the important activities of saffron such as antioxidant activity have been attributed to crocetin. Objective: In the present study, we investigated the effects of crocetin on melanogenesis in B16 melanoma cells. Methods: The effect of crocetin on intracellular and mushroom tyrosinase activity and the content of melanin was evaluated spectrophotometrically. Tyrosinase and Microphthalmia-Associated Transcription Factor (MITF) protein levels were compared between Crocetin-treated and control cells after western blot analysis. The antioxidative activity of crocetin was also investigated. Results: Crocetin could inhibit mushroom tyrosinase activity and lower the amount of melanin in B16 melanoma cells. Protein levels of tyrosinase and MITF were also decreased by crocetin. Crocetin also showed antioxidant activity and depleted cellular Reactive Oxygen Species (ROS) content but had no cytotoxicity in alamarBlue® assay. Conclusion: Taken together, decreased tyrosinase activity, melanin content, tyrosinase and MITF proteins levels, and ROS production showed the inhibition of melanogenesis in B16F10 cells by crocetin. Hence, crocetin could be suggested as a potential dermatological whitening agent in skin care products.

Sign in / Sign up

Export Citation Format

Share Document