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.

scholarly journals A New Phenolic Constituent From Carica papaya Flowers and Its Tyrosinase Inhibitory Activity

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1985098
Author(s):  
Giang Thi Kim Lien ◽  
Do Thi Thuy Van ◽  
Dao Hung Cuong ◽  
Pham Hai Yen ◽  
Bui Huu Tai ◽  
...  
Keyword(s):  
Spectral Data ◽  
Inhibitory Activity ◽  
Carica Papaya ◽  
Kojic Acid ◽  
Positive Control ◽  
Natural Source ◽  
Tyrosinase Inhibitory Activity ◽  
Esi Ms ◽  
Phenolic Constituent

A new phenolic (caricapapayol, 1) and 8 known compounds (2-9) were isolated from the flowers of Carica papaya. Their structures were determined by analysis of HR-ESI-MS, NMR spectral data, and comparison with the literature. Among known compounds, compound 2 has not been reported from natural source. Compounds 1, 2, and 4 exhibited tyrosinase inhibitory activity with IC50 values of 14.3 ± 2.7, 25.5 ± 1.9, and 19.8 ± 3.0 µM, respectively, in comparison with positive control kojic acid IC50 11.3 ± 1.6 µM.

Phytochemicals and Tyrosinase Inhibitory Activity from Piper caninum and Piper magnibaccum

2019 ◽  
Vol 25 (4) ◽  
pp. 358-363
Author(s):  
Nur Athirah Hashim ◽  
Farediah Ahmad ◽  
Wan Mohd Nuzul Hakimi Wan Salleh ◽  
Shamsul Khamis
Keyword(s):  
Inhibitory Activity ◽  
Kojic Acid ◽  
Biological Effects ◽  
Positive Control ◽  
Aromatic Plants ◽  
Tyrosinase Inhibitory Activity ◽  
Potential Source ◽  
Phytochemical Constituents ◽  
Reported Data ◽  
Ethyl Acetate Extracts

Background: Piper species are aromatic plants used as spices in the kitchen, but their secondary metabolites have also shown biological effects on human health. In traditional medicine, Piper species have been used worldwide to treat several diseases such as urological problems, skin, liver and stomach ailments, for wound healing, and as antipyretic and anti-inflammatory agents. In the present study, we attempted to isolate the phytochemicals from Piper caninum and Piper magnibaccum and evaluate their tyrosinase inhibitory activity. Methods: Phytochemical constituents of the extracts were investigated using various chromatographic and spectroscopic methods. The structures of the isolated phytochemicals were established by analysis of their spectroscopic data, as compared to that of reported data. Tyrosinase inhibitory activity was also tested on the extracts and selected compounds using mushroom tyrosinase as the enzyme. Results: Fractionation and purification of the extracts of Piper caninum and Piper magni­baccum afforded nine known compounds which were cepharanone A (1), cepharadione A (2), aristolactam AII (3), 5,7-dimethoxyflavone (4), 24-methylenecycloartan-3-one (5), β-sitosterol (6), piperumbellactam A (7), 24S-ethylcholesta-5,22,25-trien-3β-ol (8) and stigmast-3,6-dione (9). Ethyl acetate extracts from leaves of P. magnibaccum gave the highest inhibition value at 48.35%, while the tested compounds displayed weak tyrosinase activity compared to the positive control, kojic acid. Conclusion: These phytochemical results suggested that the extracts could assist as a potential source of bioactive compounds. Further research is needed in which the extract could possibly be exploited for pharmaceutical use.

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 Phenolic Constituents from the Heartwood of Artocapus Altilis and their Tyrosinase Inhibitory Activity

2012 ◽  
Vol 7 (2) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Mai Ha Khoa Nguyen ◽  
Hai Xuan Nguyen ◽  
Mai Thanh Thi Nguyen ◽  
Nhan Trung Nguyen
Keyword(s):  
Phenolic Compounds ◽  
Vanillic Acid ◽  
Inhibitory Activity ◽  
Kojic Acid ◽  
Positive Control ◽  
Coumaric Acid ◽  
Meoh Extract ◽  
Tyrosinase Inhibitory Activity ◽  
Phenolic Constituents ◽  
Inhibitory Activities

From the MeOH extract of the heartwood of Artocapus altilis, thirteen phenolic compounds have been isolated, namely curcumin (1), desmethoxycurcumin (2), retrodihydrochalcone (3), apigenin (4), tangeretin (5), nobiletin (6), O-methyldehydrodieugenol (7), dehydrodieugenol (8), β-hydroxypropiovanillone (9), p-coumaric acid (10), p-hydroxybenzaldehyde (11), vanillin (12), and vanillic acid (13). This is the first report on the presence of these compounds in the heartwood of A. altilis. Compounds 1, 2, and 10 showed more potent tyrosinase inhibitory activities, with IC50 values ranging from 2.3 to 42.0 μM, than the positive control kojic acid (IC50, 44.6 μM). The most active compound, p-coumaric acid (10) (IC50, 2.3 μM), was 22 times more active in tyrosinase inhibitory activity than kojic acid.

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.

scholarly journals Methoxy-Substituted Tyramine Derivatives Synthesis, Computational Studies and Tyrosinase Inhibitory Kinetics

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2477
Author(s):  
Yasir Nazir ◽  
Hummera Rafique ◽  
Naghmana Kausar ◽  
Qamar Abbas ◽  
Zaman Ashraf ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Competitive Inhibition ◽  
Kojic Acid ◽  
Positive Control ◽  
Potential Candidate ◽  
Binding Modes ◽  
Mushroom Tyrosinase ◽  
In Silico Docking ◽  
Human Tyrosinase

Targeting tyrosinase for melanogenesis disorders is an established strategy. Hydroxyl-substituted benzoic and cinnamic acid scaffolds were incorporated into new chemotypes that displayed in vitro inhibitory effects against mushroom and human tyrosinase for the purpose of identifying anti-melanogenic ingredients. The most active compound 2-((4-methoxyphenethyl)amino)-2-oxoethyl (E)-3-(2,4-dihydroxyphenyl) acrylate (Ph9), inhibited mushroom tyrosinase with an IC50 of 0.059 nM, while 2-((4-methoxyphenethyl)amino)-2-oxoethyl cinnamate (Ph6) had an IC50 of 2.1 nM compared to the positive control, kojic acid IC50 16700 nM. Results of human tyrosinase inhibitory activity in A375 human melanoma cells showed that compound (Ph9) and Ph6 exhibited 94.6% and 92.2% inhibitory activity respectively while the positive control kojic acid showed 72.9% inhibition. Enzyme kinetics reflected a mixed type of inhibition for inhibitor Ph9 (Ki 0.093 nM) and non-competitive inhibition for Ph6 (Ki 2.3 nM) revealed from Lineweaver–Burk plots. In silico docking studies with mushroom tyrosinase (PDB ID:2Y9X) predicted possible binding modes in the catalytic site for these active compounds. Ph9 displayed no PAINS (pan-assay interference compounds) alerts. Our results showed that compound Ph9 is a potential candidate for further development of tyrosinase inhibitors.

scholarly journals In Vitro Enzyme Tyrosinase Inhibitory Activity Test on Liquorice Root Extract Cream (Glycyrrhiza glabra L.)

2018 ◽  
Vol 16 (2) ◽  
pp. 150
Author(s):  
Siti Umroh Noor ◽  
Faridah Faridah ◽  
Pamela Magdalena
Keyword(s):  
Kojic Acid ◽  
Ethanol Extract ◽  
Positive Control ◽  
Glycyrrhiza Glabra ◽  
Root Extract ◽  
Inhibition Activity ◽  
Tyrosinase Inhibition ◽  
Skin Whitening ◽  
Glycyrrhiza Glabra L

Liquorice root extract (Glycyrrhiza glabra L.) contains glabridin, an isoflavone substance that has the ability to inhibit the oxidation of L-tyrosin and L-DOPA in the formation of melanin, therefore it can be used as skin whitening. The aim of the study was to determine the potential of the best skin whitening cream using positive control of kojic acid. Formulated 1 blank formula, 3 cream formulas using various concentrations of ethanol extract 70% liquorice roots of (0.01, 0.11, 1.01)% based on the value of tyrosinase inhibition activity in vitro from extracts of (50, 75, 100)%. Spectrophotometric method is used to measure the absorption of dopacrome by a microplate reader which was incubated at 37°C at λ 490 nm for 20 minutes. Oil in water cream was prepared by mixing extract with cream base at a temperature of 70-75°C at a speed of 400 rpm for 25 minutes. Stability test was carried out for 4 weeks at room temperature storage and a temperature of 40°C, evaluated for physical quality. The results of determination of IC50 of kojic acid was 20.88 µg / mL; IC50 of extract variation were (126.75; 1130.90; and 10092.41) µg / mL respectively. Cream has milky white-yellowish color; smell of flowers; soft texture; homogeneous; there is no separation; has type M/A; plastic thixotropic flow properties; has an increasing value including viscosity, spreadability, globule size, and pH, which are respectively (455000-620000)cPs, (2695.82-3545.83)mm2, (54.66-66.27)μm , and (4.44-5.04); tyrosinase inhibition activity in formula 1, 2 and 3 were stored at weeks 0, 2nd  and 4th  were respectively (1.78; -25.74; 22.04)%, (6.74; 6, 12; 4.49)%, and (-28.78; 53.06; 20.32)%. It can be concluded that the cream formula containing liquorice root extract with a concentration of 1.01% is the best formula so it can be used as skin whitening.

scholarly journals Synthesis, Molecular Docking and Tyrosinase Inhibitory Activity of the Decorated Methoxy Sulfonamide Chalcones: in vitro Inhibitory Effects and the Possible Binding Mode

2021 ◽  
Vol 50 (9) ◽  
pp. 2603-2614
Author(s):  
Thawanrat Kobkeatthawin ◽  
Suchada Chantrapromma ◽  
Thitipone Suwunwong ◽  
Lydia Rhyman ◽  
Yee Siew Choong ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Kojic Acid ◽  
Spectral Characteristics ◽  
Binding Mode ◽  
Molecular Docking Study ◽  
Standard Drug ◽  
Tyrosinase Inhibitory Activity ◽  
Chemical Structures

In this study, a series of sulfonamide chalcones derivatives was synthesized and its chemical structures were confirmed by spectral characteristics. The synthesized compounds were evaluated for their tyrosinase inhibitory activities along with molecular docking study. The tyrosinase inhibitory results indicated that compounds 5b, 5c, 5f, 5g and 5h displayed the significant tyrosinase inhibitory activity and comparable to the standard drug (kojic acid). Compound 5c exhibits the most potent tyrosinase inhibition among the synthesized compounds with IC50 = 0.43±0.07 mM, L-DOPA as the substrate, and better than that of the standard kojic acid (IC50 = 0.60±0.20 mM). Molecular docking studies showed that the binding mode of some compounds is in the tyrosinase binding pocket surrounding the copper in the active site. The correlation between the docking results with IC50 values showed that the binding mode prediction of the test compounds would also be convincing. This comprehensive study allows for a possible mechanism for the antityrosinase activity of the sulfonamide chalcones. These sulfonamide chalcones bind to copper atoms of tyrosinase which responsible for the catalytic activity of tyrosinase. These compounds may be used as a lead for rational drug designing for the multi-functional tyrosinase inhibitor.

Tyrosinase Inhibitory Activity of S-Naproxen Derivatives

2019 ◽  
Vol 16 (11) ◽  
pp. 1276-1285
Author(s):  
Ghulam Mohiuddin ◽  
Khalid Mohammed Khan ◽  
Uzma Salar ◽  
Kanwal ◽  
Muhammad Arif Lodhi ◽  
...  
Keyword(s):  
Acetylsalicylic Acid ◽  
Inhibitory Activity ◽  
Kojic Acid ◽  
Moderate Activity ◽  
Tyrosinase Inhibitory Activity ◽  
Active Structure ◽  
Structure Activity ◽  
Tyrosinase Enzyme ◽  
Inhibitory Potential

Background: Tyrosinase enzyme is one of the important targets to reduce melanoma and other skin disorders. Standard inhibitors of tyrosinase enzyme including arbutin and kojic acid are less effective. Some NSAIDs such as acetylsalicylic acid, mefanamic acid, and diclofenac are known to possess inhibitory potential against melanogenesis. The current study deals with the screening of tyrosinase inhibitory potential of S-naproxen derivatives. Methods: Synthetic S-naproxen derivatives 1-33 were evaluated for tyrosinase inhibitory activity in vitro. Results: Six compounds 2, 8, 9, 20, 21, and 29 showed good to moderate activity in the range of (IC50 = 21.05 ± 0.9-53.22 ± 0.7 µM) as compared to the standard kojic acid (IC50 = 16.9 ± 1.3 µM). Compound 9 (IC50 = 21.05 ± 0.9 µM) was found to be significantly active and showed activity close to the standard. Compounds 2 (IC50 = 33.23 ± 1.1 µM), 8 (IC50 = 42.10 ± 1.0 µM), 20 (IC50 = 35.40 ± 0.4 µM), 21 (IC50 = 41.01 ± 0.6 ±M), and 29 (IC50 = 53.22 ± 0.7 µM) were found to be moderately active. Structure-activity relationship (SAR) was rationalized on the basis of different substituents and functionalities present on the main scaffold. Conclusion: This study has identified a number of compounds derived from S-naproxen with comparable tyrosinase inhibitory activity.

Inhibitory effects of bioaccessible anthocyanins and procyanidins from apple, red grape, cinnamon on α-amylase, α-glucosidase and lipase

2020 ◽  
pp. 1-9
Author(s):  
Pınar Ercan ◽  
Sedef Nehir El
Keyword(s):  
Inhibitory Activity ◽  
Digestive Enzymes ◽  
Positive Control ◽  
Anthocyanin Content ◽  
Inhibitory Effects ◽  
Total Anthocyanin ◽  
Total Anthocyanin Content ◽  
Before And After ◽  
Red Grape

Abstract. The goals of this study were to determine and evaluate the bioaccessibility of total anthocyanin and procyanidin in apple (Amasya, Malus communis), red grape (Papazkarası, Vitis vinifera) and cinnamon (Cassia, Cinnamomum) using an in vitro static digestion system based on human gastrointestinal physiologically relevant conditions. Also, in vitro inhibitory effects of these foods on lipid (lipase) and carbohydrate digestive enzymes (α-amylase and α-glucosidase) were performed with before and after digested samples using acarbose and methylumbelliferyl oleate (4MUO) as the positive control. While the highest total anthocyanin content was found in red grape (164 ± 2.51 mg/100 g), the highest procyanidin content was found in cinnamon (6432 ± 177.31 mg/100 g) (p < 0.05). The anthocyanin bioaccessibilities were found as 10.2 ± 1%, 8.23 ± 0.64%, and 8.73 ± 0.70% in apple, red grape, and cinnamon, respectively. The procyanidin bioaccessibilities of apple, red grape, and cinnamon were found as 17.57 ± 0.71%, 14.08 ± 0.74% and 18.75 ± 1.49%, respectively. The analyzed apple, red grape and cinnamon showed the inhibitory activity against α-glucosidase (IC50 544 ± 21.94, 445 ± 15.67, 1592 ± 17.58 μg/mL, respectively), α-amylase (IC50 38.4 ± 7.26, 56.1 ± 3.60, 3.54 ± 0.86 μg/mL, respectively), and lipase (IC50 52.7 ± 2.05, 581 ± 54.14, 49.6 ± 2.72 μg/mL), respectively. According to our results apple, red grape and cinnamon have potential to inhibit of lipase, α-amylase and α-glucosidase digestive enzymes.

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