scholarly journals Azastilbene Analogs as Tyrosinase Inhibitors: New Molecules with Depigmenting Potential

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Larissa Lavorato Lima ◽  
Rebeca Mól Lima ◽  
Annelisa Farah da Silva ◽  
Antônio Márcio Resende do Carmo ◽  
Adilson David da Silva ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Tyrosinase Inhibitor ◽  
Tyrosinase Inhibition ◽  
Tyrosinase Inhibitory Activity ◽  
Qualitative And Quantitative ◽  
Phenolic Ring ◽  
Tyrosinase Inhibitors ◽  
Resveratrol Analogs ◽  
Better Than

This research has been an effort to develop synthetic resveratrol analogs in order to improve the depigmenting potential of natural resveratrol. Six resveratrol analogs were synthesized and tested for tyrosinase inhibitory activityin vitro, by qualitative and quantitative steps. The results showed the analogCas being the most powerful tyrosinase inhibitor (IA50= 65.67 ± 0.60 μg/mL), followed by the analogsB,E,F,A, andD, respectively. The analogCpresented a tyrosinase inhibition potential better than natural resveratrol (P<0.001). The best depigmenting activity was provided by the presence of hydroxyl in the orthoposition on the second phenolic ring.

Phlorotannins Derived From the Brown Alga Colpomenia bullosa as Tyrosinase Inhibitors

2021 ◽  
Vol 16 (7) ◽  
pp. 1934578X2110213
Author(s):  
Hideyuki Kurihara ◽  
Kazuki Kujira
Keyword(s):  
Inhibitory Activity ◽  
Brown Alga ◽  
Molecular Structures ◽  
Free Form ◽  
Biosynthesis Pathway ◽  
Tyrosinase Inhibitor ◽  
Melanin Biosynthesis ◽  
Tyrosinase Inhibitory Activity ◽  
Tyrosinase Inhibitors ◽  
Potential Use

Tyrosinase catalyzes hydroxylation of L-tyrosine and dehydrogenation of L-DOPA in the melanin biosynthesis pathway. Tyrosinase inhibitors have potential use as cosmetic whitening agents and for preventing seafood deterioration. In this report, tyrosinase inhibitors extracted from brown alga Colpomenia bullosa (Scytosiphonaceae, Scytosiphonales) were investigated. Inhibitory principles were isolated from the extract and identified as phlorotannins, phloroglucinol (1), diphlorethol (2), triphlorethol C (3), which have not been isolated in a free form previously, and fucophlorethol C (4). Compounds 3 and 4 have not been reported previously as tyrosinase inhibitors. Triphlorethol C (3) was the most potent tyrosinase inhibitor among the phlorotannins isolated, whereas isomeric fucophlorethol C (4) displayed the weakest inhibitory activity. The results suggest that molecular structures of phlorotannins strongly affect their tyrosinase inhibitory activity.

scholarly journals Preliminary Screening of Selected Plant Extracts for Anti Tyrosinase Activity

2016 ◽  
Vol 16 (1) ◽  
pp. 18 ◽  
Author(s):  
Vidyalakshmi Subramanian ◽  
Dhamodharan Sahithya
Keyword(s):  
Inhibitory Activity ◽  
Kojic Acid ◽  
Control Cell ◽  
Punica Granatum ◽  
Positive Control ◽  
Tyrosinase Inhibition ◽  
Tyrosinase Inhibitory Activity ◽  
Cassia Angustifolia ◽  
Important Approach

Tyrosinase inhibition is an important approach towards controlling hyper pigmentation. We aimed to screen alcoholic extracts of 11 plants extract for their tyrosinase inhibitory activity. These plants have been used traditionally in the treatment of skin ailments and for the improvement of skin complexion. The extracts were quantified for total phenols, alkaloids and tannins. <em>In vitro</em> tyrosinase inhibition was performed with kojic acid as the positive control. Cell viability was tested on B16 F0 melanoma cells. The extracts of <em>Rosa berberifolia</em>, <em>Punica granatum</em> and <em>Casiia angustifolia</em> showed more than 80% inhibition at 500 mg/ml concentration. Nine of the extracts were also shown to have a high phenolic content greater than 200 mg/g of the plant material. The tyrosinase inhibitory activity of the extracts of <em>Cassia angustifolia, Punica granatum </em>and<em> Rosa berberifolia</em> were comparable with that of the control, kojic acid. The three extracts also showed lesser than 50% cytotoxicity at the concentrations tested. From the screening assays, it is seen that three plants have appreciable tyrosinase inhibitory activity. Hence, these plants may be further evaluated for their use in cosmetics and hyper pigmentation.

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.

scholarly journals Inhibitory Activities of Polyphenolic Extracts of Bangladeshi Vegetables against α-Amylase, α-Glucosidase, Pancreatic Lipase, Renin, and Angiotensin-Converting Enzyme

Foods ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 844
Author(s):  
Razia Sultana ◽  
Adeola M. Alashi ◽  
Khaleda Islam ◽  
Md Saifullah ◽  
C. Emdad Haque ◽  
...  
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Inhibitory Activity ◽  
The Other ◽  
Converting Enzyme ◽  
Inhibitory Activities ◽  
Ash Gourd ◽  
Better Than

The aim of the study was to determine the in vitro enzyme inhibition activities of aqueous polyphenolic extracts of nine popular Bangladeshi vegetables, namely ash gourd, bitter gourd, brinjal, Indian spinach, kangkong, okra, ridge gourd, snake gourd, and stem amaranth. Polyphenolic glycosides were the major compounds present in the extracts. Inhibition of α-amylase (up to 100% at 1 mg/mL) was stronger than α-glucosidase inhibition (up to 70.78% at 10 mg/mL). The Indian spinach extract was the strongest inhibitor of pancreatic lipase activity (IC50 = 276.77 µg/mL), which was significantly better than that of orlistat (381.16 µg/mL), a drug. Ash gourd (76.51%), brinjal (72.48%), and snake gourd (66.82%) extracts were the most effective inhibitors of angiotensin-converting enzyme (ACE), an enzyme whose excessive activities have been associated with hypertension. Brinjal also had a significantly higher renin-inhibitory activity than the other vegetable extracts. We conclude that the vegetable extracts may have the ability to reduce enzyme activities that have been associated with hyperglycemia, hyperlipidemia, and hypertension.

scholarly journals AKTIVITAS INHIBITOR TIROSINASE PADA EKSTRAK ALGA COKELAT SARGASSUM SP. AGARDH ASAL PESISIR LHOK BUBON, KABUPATEN ACEH BARAT

2018 ◽  
Vol 1 (1) ◽  
Author(s):  
Muhammad Gazali
Keyword(s):  
Inhibitory Activity ◽  
Brown Algae ◽  
Methanol Extract ◽  
Kojic Acid ◽  
Bioactive Compound ◽  
Positive Control ◽  
Marine Macroalgae ◽  
Tyrosinase Inhibitor ◽  
Tyrosinase Inhibitory Activity ◽  
New Finding

Seaweeds are marine macro algae that can be found attach to the bottom shallow coastal waters with subsrate as attached media. There are three major groups of seaweeds namely brown algae (Phaeophyta), red (Rhodophyta) and green (Chlorophyta). Sargassum sp is one of brown algae which mostly found in the Lhok Bubon Coastal West of Aceh. Recently, exploration of marine macroalgae as bioactive sources was investigated. Seaweed contains bioactive compound which can serve as a defense from ultraviolet radiation that caused hyperpigmentation effect. The aiming of this study is to analyse the tyrosinase inhibitory activity of Sargassum sp extract from Lhok Bubon Coastal Area, West of Aceh. The results shown that the methanol extract of Sargassum sp possess phytochemical properties such as fenol, alkaloid and triterpenoid. Tyrosinase inhibitory activity of Sargassum sp methanol extract  is the best extract which can be inhibit  monophenolase with  IC50 : 1111.49 µg/ml and IC50 = 1582.31 µg/ml in diphenolase pathway with kojic acid as positive control. Moreover, etyl asetate and n-hexane extract have no activity of tyrosinase inhibitor. Therefore, new finding of tyrosinase inhibitor agent from marine macroalgae Sargassum sp give the fruitfull information for cosmeceutical industry.Keywords : Lhok Bubon, Brown Algae, Sargassum sp, Tyrosinase Inhibitor

scholarly journals POTENSI MAKROALGA PADINA AUSTRALIS (HAUCK 1887) DI BARAT SELATAN ACEH SEBAGAI AGEN INHIBITOR TIROSINASE

2018 ◽  
Vol 5 (1) ◽  
pp. 71
Author(s):  
Mohamad Gazali ◽  
Eri Safutra ◽  
Zulfadhli Zulfadhli
Keyword(s):  
Inhibitory Activity ◽  
Brown Algae ◽  
Methanol Extract ◽  
Bioactive Compound ◽  
Positive Control ◽  
Raw Material ◽  
Marine Macroalgae ◽  
Tyrosinase Inhibitor ◽  
Tyrosinase Inhibitory Activity ◽  
New Finding

Seaweeds are marine macro algae that can be found attach to the bottom shallow coastal waters. There are three major groups of seaweeds namely brown algae (Phaeophyta), red (Rhodophyta) and green (Chlorophyta). Padina australis is one of brown algae which mostly found in the West-South of Aceh coastal Area.  Seaweed contains bioactive compound which can serve as a defense from ultraviolet radiation that caused hyperpigmentation effect The purpose of this study is to analyse the tyrosinase inhibitory activity of P. australis extract from West-South Aceh. The results shown that the methanol extract of P. australis possess phytochemical properties such as flavonoids, tannin and saponin. tyrosinase inhibitory activity of P. australis  methanol extract  is the best extract which can be inhibit monophenolase with  IC50 : 293.520 µg/ml and IC50 = 13.571.067 µg/ml in diphenolase pathway with kojic acid as positive control. Moreover, chloroform and n-hexane extract have no activity of tyrosinase inhibitor. Therefore, new finding of tyrosinase inhibitor agent from marine macroalgae P. australis give the fruitfull information for cosmeceutical industry. P. australis parts could be complementary each other in providing the raw material of cosmetic product.

scholarly journals Identification by shape-based virtual screening and evaluation of new tyrosinase inhibitors

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e4206 ◽  
Author(s):  
Qi Li ◽  
Hongyu Yang ◽  
Jun Mo ◽  
Yao Chen ◽  
Yue Wu ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Inhibitory Activity ◽  
Skin Pigmentation ◽  
Competitive Inhibitor ◽  
Tyrosinase Inhibitor ◽  
Starting Point ◽  
Good Starting Point ◽  
Tyrosinase Inhibitors ◽  
Dopa Formation ◽  
Potent Inhibitory Activity

Targeting tyrosinase is considered to be an effective way to control the production of melanin. Tyrosinase inhibitor is anticipated to provide new therapy to prevent skin pigmentation, melanoma and neurodegenerative diseases. Herein, we report our results in identifying new tyrosinase inhibitors. The shape-based virtual screening was performed to discover new tyrosinase inhibitors. Thirteen potential hits derived from virtual screening were tested by biological determinations. Compound 5186-0429 exhibited the most potent inhibitory activity. It dose-dependently inhibited the activity of tyrosinase, with the IC50 values 6.2 ± 2.0 µM and 10.3 ± 5.4 µM on tyrosine and L-Dopa formation, respectively. The kinetic study of 5186-0429 demonstrated that this compound acted as a competitive inhibitor. We believe the discoveries here could serve as a good starting point for further design of potent tyrosinase inhibitor.

Design and discovery of tyrosinase inhibitors based on a coumarin scaffold

RSC Advances ◽  
2015 ◽  
Vol 5 (114) ◽  
pp. 94227-94235 ◽  
Author(s):  
M. J. Matos ◽  
C. Varela ◽  
S. Vilar ◽  
G. Hripcsak ◽  
F. Borges ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Tyrosinase Inhibitory Activity ◽  
Tyrosinase Inhibitors

A novel series of 3-aryl and 3-heteroarylcoumarins displaying tyrosinase inhibitory activity.

Sign in / Sign up

Export Citation Format

Share Document