scholarly journals Extract of Ganoderma formosanum Mycelium as a Highly Potent Tyrosinase Inhibitor

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Kai-Di Hsu ◽  
Hong-Jhang Chen ◽  
Chi-Shin Wang ◽  
Chi-Chin Lum ◽  
Shu-Pei Wu ◽  
...  
Biomolecules ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 674
Author(s):  
Shilpi Goenka ◽  
Francis Johnson ◽  
Sanford R. Simon

Skin hyperpigmentation disorders arise due to excessive production of the macromolecular pigment melanin catalyzed by the enzyme tyrosinase. Recently, the therapeutic use of curcumin for inhibiting tyrosinase activity and production of melanin have been recognized, but poor stability and solubility have limited its use, which has inspired synthesis of curcumin analogs. Here, we investigated four novel chemically modified curcumin (CMC) derivatives (CMC2.14, CMC2.5, CMC2.23 and CMC2.24) and compared them to the parent compound curcumin (PC) for inhibition of in vitro tyrosinase activity using two substrates for monophenolase and diphenolase activities of the enzyme and for diminution of cellular melanogenesis. Enzyme kinetics were analyzed using Lineweaver-Burk and Dixon plots and nonlinear curve-fitting to determine the mechanism for tyrosinase inhibition. Copper chelating activity, using pyrocatechol violet dye indicator assay, and antioxidant activity, using a DPPH radical scavenging assay, were also conducted. Next, the capacity of these derivatives to inhibit tyrosinase-catalyzed melanogenesis was studied in B16F10 mouse melanoma cells and the mechanisms of inhibition were elucidated. Inhibition mechanisms were studied by measuring intracellular tyrosinase activity, cell-free and intracellular α-glucosidase enzyme activity, and effects on MITF protein level and cAMP maturation factor. Our results showed that CMC2.24 showed the greatest efficacy as a tyrosinase inhibitor of all the CMCs and was better than PC as well as a popular tyrosinase inhibitor-kojic acid. Both CMC2.24 and CMC2.23 inhibited tyrosinase enzyme activity by a mixed mode of inhibition with a predominant competitive mode. In addition, CMC2.24 as well as CMC2.23 showed a comparable robust efficacy in inhibiting melanogenesis in cultured melanocytes. Furthermore, after removal of CMC2.24 or CMC2.23 from the medium, we could demonstrate a partial recovery of the suppressed intracellular tyrosinase activity in the melanocytes. Our results provide a proof-of-principle for the novel use of the CMCs that shows them to be far superior to the parent compound, curcumin, for skin depigmentation.


2014 ◽  
Vol 98 (22) ◽  
pp. 9389-9398 ◽  
Author(s):  
Cheng-Li Wang ◽  
Chiu-Ying Lu ◽  
Ying-Chao Hsueh ◽  
Wen-Hsiung Liu ◽  
Chun-Jen Chen

2016 ◽  
Vol 18 (6) ◽  
pp. 283-286 ◽  
Author(s):  
Paula García ◽  
Mario O. Salazar ◽  
I. Ayelen Ramallo ◽  
Ricardo L. E. Furlan

2018 ◽  
Vol 44 (4) ◽  
pp. 473-481
Author(s):  
Elif Ayazoglu Demir ◽  
Ahmet Colak ◽  
Aylin Kalfa ◽  
Ahmet Yasar ◽  
Olcay Bekircan ◽  
...  

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.


2018 ◽  
Vol 14 ◽  
pp. 2737-2744 ◽  
Author(s):  
Jacqueline Pollini ◽  
Valentina Bragoni ◽  
Lukas J Gooßen

A convenient and sustainable three-step synthesis of the tyrosinase inhibitor 2-hydroxy-6-tridecylbenzoic acid was developed that starts directly from the anacardic acid component of natural cashew nutshell liquid (CNSL). Natural CNSL contains 60–70% of anacardic acid as a mixture of several double bond isomers. The anacardic acid component was converted into a uniform starting material by ethenolysis of the entire mixture and subsequent selective precipitation of 6-(ω-nonenyl)salicylic acid from cold pentane. The olefinic side chain of this intermediate was elongated by its cross-metathesis with 1-hexene using a first generation Hoveyda–Grubbs catalyst, which was reused as precatalyst in a subsequent hydrogenation step. Overall, the target compound was obtained in an overall yield of 61% based on the unsaturated anacardic acid content and 34% based on the crude CNSL.


2020 ◽  
Vol 10 (5-s) ◽  
pp. 199-204
Author(s):  
Ruchi Gupta ◽  
Rajiv Saxena ◽  
Archana Patidar ◽  
Yashu Chourasiya ◽  
Neelesh Malviya

Tyrosinase (polyphenolic oxidase) is a multifunctional and copper containing enzyme. Tyrosinase is an enzyme which is responsible for melanin biosynthesis which is responsible for color of the skin. Melanin is synthesised in melanocyte cells by melanogenesis process.  Melanogenesis protects skin surface from harmful ultraviolet radiations. Melanin is mainly synthesized in plants, micro organisms and mammalian cells. Melanin pigment is responsible for hyperpigmentation and hypopigmentation. When melanin is present in very less amount it causes local vitiligo and posttraumatic hypopigmentation. When melanin is present in very less amount it causes local vitiligo and posttraumatic hypopigmentation. Abnormal amount of melanin deposit in the specific sites of skin causes abnormal skin colored patches like solar lentigos, chloasma, freckles, post inflammatory hyperpigmentation etc. Tyrosinase is also responsible for color changes in fruits due to enzymatic reactions. Tyrosinase inhibitor compounds are used in cosmetics, food, agriculture science and also used in remedy for imbalance in pigmentations. Some Indian herbal plants and agents like Aloe barbedensis, Crocus sativus, Curcuma longa, Camellia sinensis, Glycyrrhiza glabra, Glycine max, Nelumbo nucifera, Hemidesmus indicus, Vitis Vinifera, Broussonetia papyrifera, resorcinol, arbutin, kojic acid, hydroquinone and ascorbic acid have antityrosinase enzymatic activity. So these plants and inhibitory agents are used in cosmetic industries due to their tyrosinase inhibitory effects or antityrosinase activity or antihyperpigmentation effects. Keywords: Anti-hyperpimentation, Tyrosinase Inhibitor, Melanin, Herbal drugs.


2021 ◽  
Vol 22 (20) ◽  
pp. 11251
Author(s):  
Hsing-Chun Kuo ◽  
Yen-Wenn Liu ◽  
Chi-Chin Lum ◽  
Kai-Di Hsu ◽  
Shin-Ping Lin ◽  
...  

Ganoderma formosanum (GF) is a medicinal mushroom endemic to Taiwan. Previous research established the optimal culture conditions to produce exopolysaccharide rich in β-glucan (GF-EPS) from submerged fermentation of GF. The present study investigated the antitumor effects of GF-EPS in a Lewis lung carcinoma cell (LLC1) tumor-bearing mice model. In the preventive model, GF-EPS was orally administered to mice before LLC1 injection. In the therapeutic model, GF-EPS oral administration was initiated five days after tumor cell injection. The tumor size and body weight of the mice were recorded. After sacrifice, the lymphocyte subpopulation was analyzed using flow cytometry. Spleen tissues were used to analyze cytokine mRNA expression. The results showed that GF-EPS (80 mg/kg) effectively suppressed LLC1 tumor growth in both the preventive and therapeutic models. GF-EPS administration increased the proportion of natural killer cells in the spleen and activated gene expression of several cytokines. Our results provide evidence that GF-EPS promotes tumor inhibition through immunomodulation in tumor-bearing mice.


ChemInform ◽  
2008 ◽  
Vol 39 (35) ◽  
Author(s):  
O. B. Abdel-Halim ◽  
A. M. Marzouk ◽  
R. Mothana ◽  
N. Awadh

Author(s):  
Irmanida Batubara ◽  
Maily Mustofa ◽  
Wulan Tri Wahyuni ◽  
Kilala Tilaar ◽  
Waras Nurcholis ◽  
...  

Xylocarpus granatum is mangrove plant that traditionally used as face powder in Central Sulawesi, Indonesia which related to antioxidant, antiglycation and tyrosinase inhibition activities. This study aimed to evaluate the potency of X. granatum as a tyrosinase inhibitor, antiglycation, and antioxidant. The leaves, stem, stem bark, fruit flesh, fruit peel, and kernel of X. granatum were extracted using ethanol then their tyrosinase inhibition, antiglycation, and antioxidant were evaluated. Tyrosinase inhibition activity was evaluated using in vitro assay with L-tyrosine and L-DOPA as the substrate of monophenolase and diphenolase. Antiglycation activity was studied by measuring the excitation and emission fluorescence from glucose and fructose reaction with Bovine Serum Albumin. Antioxidant activity was measured using the DPPH radical scavenging assay. The result showed that the ethanolic extract of fruit flesh has higher potency as tyrosinase inhibitor (IC50 of 393.8 mg/L and IC50 of 448 mg/L, respectively for monophenolase and diphenolase). Antiglycation assay showed that the ethanolic extract of stem bark provides the strongest antiglycation activity with an IC50 of 118.1 mg/L. Meanwhile, fruit peel provides the strongest antioxidant activity with an IC50 of 5.5 mg/L. Fractionation of ethanolic extracts of each part of X. granatum tree yield fractions with lower bioactivity compared to the crude extract. Moreover, stem extract and fractions from two different locations (Tarakan and Kendari) tend to have different bioactivities strengths.  The stem part of X granatum could be developed as new raw material of cosmetic product in Indonesia, while ethanol as the solvent for extraction, and the different bioactivity of stem extract from different location can be the consideration for the industry to standardize the extract prior to production of final product.


Sign in / Sign up

Export Citation Format

Share Document