scholarly journals Depigmentation Activity of Secang (Caesalpinia Sappan L.) Extract Through Tyrosinase, Tyrosinase Related Protein-1 and Dopachrome Tautomerase Inhibition

2019 ◽  
Vol 12 (2) ◽  
pp. 799-808 ◽  
Author(s):  
Ni Putu Linda Laksmiani ◽  
I. Putu Wiratama Nugraha
Keyword(s):  
Ascorbic Acid ◽  
Kojic Acid ◽  
Ethanolic Extract ◽  
Related Protein ◽  
Caesalpinia Sappan ◽  
Dopachrome Tautomerase ◽  
Inhibitory Ability ◽  
Tyrosinase Enzyme ◽  
Tyrosinase Related Protein

Excessive exposure of UV light increase melanin synthesis and cause hyperpigmentation of the skin. The pharmacological activity of secang (Caesalpinia sappan L.) with the main compound, brazilien and brazilin as antioxidants that have potency as free radicals scavenger and directly inhibit tyrosinase activity in the process of melanogenesis. This study aims to determine the inhibitory ability of secang ethanolic extract on tyrosinase enzymes in vitro and evaluate the affinity of brazilein and brazilin as skin depigmentation agents against melanogenesis target protein in silico using molecular docking. In vitro testing using tyrosinase inhibitor assay with L-DOPA as its substrate and calculated the percentage inhibition value and IC50. The IC50 of the extract than compared with the positive control, namely kojic acid and ascorbic acid. Insilico research was carried out using autodock 4.2 program by evaluating the binding energy between the active compound of brazilein and brazilin with melanogenesis protein. Inhibition of the tyrosinase enzyme is showed through the IC50 value from ethanolic extract, kojic acid and ascorbic acid respectively 104 μg/ mL, 44 μg/mL and 37 μg/mL. Binding energy of the molecular docking process between brazilein, brazilin, kojic acid and ascorbic acid with the target protein of melanogenesis enzymes (tyrosinase, tyrosinase related protein 1, and D-Dopachrome tauomerase) are -8.37; -6.56; -5.03; -5.35 kcal/mol in tyrosinase, -7.75; -6.40; -5.32; -5.8 kcal/mol in tyrosinase related proteins 1 and -9.93; -8.26; -5.8; -6.52 kcal/mol in D-Dopachrome tautomerase. Secang ethanolic extract could be developed into a skin lightening agent or depigmentation agent through inhibition of 3 target proteins that induce melanogenesis. Although invitro results show the inhibitory ability of the tyrosinase enzyme is lower than kojic acid and ascorbic acid but in silico, it is seen that brazilein and brazilin in secang ethanolic extract have a stronger affinity compared to kojic acid and ascorbic acid. For this reason, it is necessary to purify the extract into a fraction so that it can get more active ingredients of brazilein and brazilin, and in vitro testing for inhibition of the tyrosinase related protein 1 enzyme, and D-Dopachrome tautomerase.

scholarly journals Tara Tannin Regulates Pigmentation by Modulating Melanogenesis Enzymes and Melanosome Transport Proteins Expression

2020 ◽  
Vol 7 (01) ◽  
pp. e34-e44
Author(s):  
Myra O. Villareal ◽  
Thanyanan Chaochaiphat ◽  
Meriem Bejaoui ◽  
Kozo Sato ◽  
Hiroko Isoda
Keyword(s):  
Skin Color ◽  
Pigment Cell ◽  
Underlying Mechanism ◽  
Mapk Signaling ◽  
Transport Proteins ◽  
Related Protein ◽  
Promoting Effect ◽  
Dopachrome Tautomerase ◽  
Tyrosinase Related Protein

AbstractThe skin color is imparted by the pigment melanin produced in the melanosomes of melanocytes, through the catalytic action of melanogenesis enzymes tyrosinase, tyrosinase-related protein 1, and dopachrome tautomerase. Disruptions in the melanogenesis process may result to hypopigmentation, as observed in cutaneous postinflammatory conditions. Here, the bioactivity of tara tannin, specifically on melanogenesis, was evaluated in vitro using human epidermal melanocytes (HEM) and B16F10 murine melanoma cells in order to determine the possibility that it may be used as a treatment against hypopigmentation. The melanin content of tara tannin-treated B16F10 cells and the expression level of melanogenesis enzymes and melanosome transport proteins were determined. To elucidate the underlying mechanism of tara tannin’s effect on melanogenesis, DNA microarray analysis was performed. Tara tannin significantly increased melanogenesis in both murine and human pigment cell models by upregulating melanogenesis-associated enzymes’ (tyrosinase, tyrosinase-related protein 1, and dopachrome tautomerase) protein and mRNA expression levels, as well as the melanosome transport proteins (myosin Va and RAB27A) expression, both attributed to increased microphthalmia-associated transcription factor (MITF) expression. Global gene expression analysis results revealed the modulation of genes (p≤0.05; fold-change ≥2.0 and ≤−2.0) that are under the transcriptional regulation of MITF and genes relevant for MAPK signaling, metabolic pathways, and cell cycle. Tara tannin has a significant effective melanogenesis-promoting effect, making it a potential therapeutic agent against hypopigmentation disorders. This is the first report on the melanogenesis regulatory effect of tara tannin in vitro.

scholarly journals Virtual Screening of Selected Natural Products as Human Tyrosinase-Related Protein 1 Blockers

2021 ◽  
Author(s):  
Chidi Duru ◽  
Ijeoma Duru ◽  
Chiagoziem Chidiebere
Keyword(s):  
Ascorbic Acid ◽  
Natural Products ◽  
Kojic Acid ◽  
Binding Pocket ◽  
Related Protein ◽  
Melanin Production ◽  
Synthetic Compound ◽  
Skin Lightening ◽  
Tyrosinase Related Protein ◽  
Human Tyrosinase

Many researchers have widely explored the need to replace the harmful compound hydroquinone in skin-lightening creams with more skin-friendly compounds that can give similar results. Some compounds from the plant kingdom have been shown to possess human tyrosinase inhibitory action with no adverse effect on the skin. In this study, the virtual screen of glabridin, kojic acid, arbutin, niacinamide, ascorbic acid, salicin, lactic acid, glutathione, azelaic acid, linoleic acid, glycolic acid, acclaimed to possess this activity as well as the synthetic compound hydroquinone, as human tyrosinase-related protein 1 inhibitor was investigated using computational methods. Site-directed docking was performed at the binding pocket on the enzyme carrying the cocrystallized ligand tropolone. The binding affinity of salicin (-6.7 kcal/mol), a-arbutin (-6.3 kcal/mol), glutathione (-6.2 kcal/mol), ascorbic acid (-5.7 kcal/mol), and niacinamide (-5.7 kcal/mol) were higher than that of the cocrystallized ligand tropolone (-5.5 kcal/mol) and the synthetic skin lightening compound hydroquinone (-4.8 kcal/mol). a-arbutin and glutathione also interacted with similar amino acids units as hydroquinone, suggesting that they followed the exact mechanism of action. These findings strongly corroborate the claim that these natural products could inhibit melanin production and may serve to replace hydroquinone in skin lightening creams.

scholarly journals Anti-melanogenic and Anti-oxidant Activities of an Ethanolic Extract of Kummerowia striata and its active compounds, p-coumaric acid and quercetin

2018 ◽  
Author(s):  
Ju-Hyoung Park ◽  
Jae Yeon Lee ◽  
Young-Rak Cho ◽  
Eun-Kyung Ahn ◽  
Wonsik Jeong ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Ethanolic Extract ◽  
Model Systems ◽  
Dependent Manner ◽  
Melanin Synthesis ◽  
Related Protein ◽  
Anti Oxidant ◽  
Kummerowia Striata ◽  
Tyrosinase Related Protein

Kummerowia striata is a traditional medicine used for the therapy of inflammation-related diseases. Herein, we investigated the anti-melanogenic and antioxidant activities of an ethanolic extract of K. striata (EKS) using a number of in vitro and cell culture model systems. The anti-melanogenic effect was assessed in B16F10 melanoma cells based on melanin synthesis and in vitro tyrosinase inhibitory activity and the anti-oxidant activity assays were performed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2ʹ-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS); EKS exhibited strong anti-oxidant activities in both the assays. The expression of tyrosinase, tyrosinase-related protein 1, tyrosinase-related protein 2, and microphthalmia-associated transcription factor was decreased in a dose-dependent manner at mRNA and protein levels upon treatment with EKS. Notably, EKS did not affect the cell viability at all the EKS concentrations used in this study, indicating that EKS-mediated inhibition of melanin synthesis is not accompanied with cytotoxicity. Collectively, our findings demonstrate, for the first time, that EKS possesses anti-melanogenic and anti-oxidant activities, and suggest that further evaluation and development of EKS as a functional supplement or cosmetic might be useful for skin whitening and for reduction wrinkles.

Retinoic acid as modulator of UVB-induced melanocyte differentiation. Involvement of the melanogenic enzymes expression

1994 ◽  
Vol 107 (4) ◽  
pp. 1095-1103
Author(s):  
C. Romero ◽  
E. Aberdam ◽  
C. Larnier ◽  
J.P. Ortonne
Keyword(s):  
Retinoic Acid ◽  
Sun Exposure ◽  
Transcriptional Level ◽  
Related Protein ◽  
Dopachrome Tautomerase ◽  
Normal Human ◽  
Cis And Trans ◽  
Vitro Effect ◽  
Tyrosinase Related Protein

Retinoic acid (RA) is a hormone-like agent involved in the control of cell differentiation. The most characteristic feature of melanocyte differentiation, melanogenesis, is stimulated by UV radiations. Excessive chronic sun exposure results in irregular skin hypermelanosis that can be partially corrected by topical RA. The basic mechanisms underlying this effect of RA are unknown. To determine whether RA can directly modulate excessive melanin synthesis, we analyzed the in vitro effect of cis- and trans-RA on UVB-induced melanogenesis in S91 mouse melanoma cells and in normal human melanocytes (NHM). In both cells types, the two RA isoforms significantly decreased the UVB-stimulated melanogenesis in term of tyrosinase activity and melanin neosynthesis. To correlate changes in melanogenesis with the expression of melanogenic enzymes, we determined the neosynthesis rate of tyrosinase, tyrosinase-related protein-1 (TRP-1/gp 75) and tyrosinase-related protein-2 (TRP-2/DOPAchrome tautomerase). Here we show that UVB-induced melanogenesis in NHM is related to an increased synthesis of tyrosinase and TRP-1 and to a dramatic decrease of TRP-2 expression. RA inhibition of UVB-induced melanogenesis acts at the post-transcriptional level leading to a decreased tyrosinase and TRP-1 synthesis. We also show that in NHM, inhibition of TRP-2 following UVB-treatment is significantly reversed by RA. This demonstrates a negative correlation between melanogenesis and TRP-2 expression.

Expression of Tyrosinase-related Protein 2/DOPAchrome Tautomerase in the Retinoblastoma

2001 ◽  
Vol 72 (3) ◽  
pp. 225-234 ◽  
Author(s):  
Tetsuo Udono ◽  
Kazuhiro Takahashi ◽  
Ken-ichi Yasumoto ◽  
Miki Yoshizawa ◽  
Kazuhisa Takeda ◽  
...  
Keyword(s):  
Related Protein ◽  
Dopachrome Tautomerase ◽  
Tyrosinase Related Protein

scholarly journals Melanocytes and Pigmentation Are Affected in Dopachrome Tautomerase Knockout Mice

2004 ◽  
Vol 24 (8) ◽  
pp. 3396-3403 ◽  
Author(s):  
Laurence Guyonneau ◽  
Fabien Murisier ◽  
Anita Rossier ◽  
Alexandre Moulin ◽  
Friedrich Beermann
Keyword(s):  
Knockout Mice ◽  
Null Allele ◽  
Coat Color ◽  
Pigment Epithelium ◽  
Retinal Pigment ◽  
Related Protein ◽  
Melanin Content ◽  
Dopachrome Tautomerase ◽  
Exon 1 ◽  
Tyrosinase Related Protein

ABSTRACT The tyrosinase family comprises three members, tyrosinase (Tyr), tyrosinase-related protein 1 (Tyrp1), and dopachrome tautomerase (Dct). Null mutations and deletions at the Tyr and Tyrp1 loci are known and phenotypically affect coat color due to the absence of enzyme or intracellular mislocalization. At the Dct locus, three mutations are known that lead to pigmentation phenotype. However, these mutations are not null mutations, and we therefore set out to generate a null allele at the Dct gene locus by removing exon 1 of the mouse Dct gene. Mice deficient in Dct [Dcttm1(Cre)Bee ] lack Dct mRNA and dopachrome tautomerase protein. They are viable and do not show any abnormalities in Dct-expressing sites such as skin, retinal pigment epithelium, or brain. However, the mice show a diluted coat color phenotype, which is due to reduced melanin content in hair. Primary melanocytes from Dct knockout mice are viable in culture and show a normal distribution of tyrosinase and tyrosinase-related protein 1. In comparison to the knockout, the slaty mutation (Dctslt /Dctslt ) has less melanin and affects growth of primary melanocytes severely. In summary, we have generated a knockout of the Dct gene in mice with effects restricted to pigment production and coat color.

scholarly journals EVALUASI AKTIVITAS INHIBISI XANTIN OKSIDASE DAN KANDUNGAN SENYAWA POLIFENOL DARI EKSTRAK SAPPAN

2018 ◽  
Vol 5 (2) ◽  
pp. 157
Author(s):  
Sri Ningsih ◽  
. Churiyah
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Ethanolic Extract ◽  
Polyphenol Content ◽  
Total Polyphenol ◽  
Caesalpinia Sappan ◽  
Total Polyphenol Content

Evaluation of xanthine oxidase inhibitory activity and polyphenolic content of sappan extractABSTRACTHyperuricemia is a disease that is characterized by a high uric acid level, in which the number of patients tends to increase every year. This research was intended to evaluate the xanthine oxidase (XO) inhibitory activity and determinate the total polyphenol content of heartwood sappan (Caesalpinia sappan L.) extract. The extract was prepared by macerating the dry powder wood using 70% ethanol at room temperature. The quality of ethanolic extract obtained was evaluated based on BPOM guideline. XO inhibitory power was determined by measuring uric acid produced in the xanthine/XO system in vitro. The polyphenol content of the extract was measured using Folin-Ciocalteu reagent spectrophotometrically. The results showed that the quality of sappan semisolid extract fulfilled the required standard. Sappan extract inhibited XO activity by 98% relative to the positive control, allopurinol, at the final extract concentration of 100 µg/mL. The total polyphenol content was 26% of the crude extract. It could be concluded that sappan ethanolic extract has the potential to be developed as an ingredient for hyperuricemia treatment.Keywords: hyperuricemia, sappan, total polyphenol, xanthine, xanthine oxidase ABSTRAKHiperurisemia adalah penyakit yang dicirikan dengan kadar asam urat tinggi dimana prevalensi penderita cenderung meningkat. Penelitian ini bertujuan untuk mempelajari aktivitas esktrak kayu sappan (Caesalpinia sappan L.) dalam menginhibisi enzim XO (xantin oksidase) secara in vitro dan penentuan kadar senyawa polifenol total yang terkandung di dalamnya. Ekstrak dibuat dengan cara maserasi serbuk kayu menggunakan pelarut etanol 70% pada suhu kamar. Kualitas ekstrak dievaluasi mengacu pada parameter karakterisasi ekstrak yang ditetapkan oleh BPOM. Aktivitas inhibisi XO ditetapkan dengan mengukur kadar asam urat yang terbentuk pada sistem xantin/XO in vitro. Kadar polifenol ekstrak diukur menggunakan pereaksi Folin-Ciocalteu secara spektrofotometri. Hasil analisis menyatakan bahwa kualitas ekstrak kental sappan memenuhi persyaratan yang ada. Pengujian inhibisi XO dengan pembanding positif allopurinol pada konsentrasi akhir ekstrak sebesar 100 µg/mL menunjukkan bahwa ekstrak mempunyai kekuatan menginhibisi XO sebesar 98% relatif terhadap pembanding positif allopurinol. Kadar senyawa polifenol total dalam ekstrak sappan sebesar 26% dari ekstrak kasar. Dari penelitian ini dapat disimpulkan bahwa ekstrak sappan mempunyai potensi untuk dikembangkan sebagai bahan untuk mengatasi hiperurisemia.Kata Kunci: hiperurisemia, polifenol total, sappan, xantin, xantin oksidase

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