scholarly journals In vitro inhibitory potential of methanolic extract of Celosia argentea var. cristata on tyrosinase, acetylcholinesterase and butyrylcholinesterase enzymes

2015 ◽  
Vol 10 (2) ◽  
pp. 449 ◽  
Author(s):  
Fatima Saqib ◽  
Khalid Hussain Janbaz ◽  
Maryam Khan Sherwani
Keyword(s):  
Neurodegenerative Disorders ◽  
Inhibitory Activity ◽  
Methanol Extract ◽  
Methanolic Extract ◽  
Microtiter Plate ◽  
Tyrosinase Inhibitory Activity ◽  
Skin Hyperpigmentation ◽  
Celosia Argentea ◽  
Inhibitory Potential

<p>In the current study, methanol extract of <em>Celosia argentea</em> var. <em>cristata</em> was tested for its inhibitory potential against tyrosinase, acetylcholinesterase and butyrylcholinesterase enzymes at the concentration of 0.5 mM by ELISA microtiter plate assays. A significant tyrosinase inhibitory activity (63.6%), acetylcholinesterase inhibitory activity (80.3%) and butyrylcholinesterse inhibitory activity (68.24%) was shown by crude methanolic extract of <em>C. argentea</em> var. <em>cristata</em> with respective IC<sub>50 </sub>values of 268.5 ± 0.2 µg/mL, 73.6 ± 0.1 µg/mL and 132.8 ± 0.9 µg/mL. The result of this study reveals the use of <em>C. argentea</em> var. <em>cristata</em> in skin hyperpigmentation, Parkinson’s disease and neurodegenerative disorders like Alzheimer’s disease and dementia.</p>

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.

scholarly journals Evaluation of Antioxidant, Antimicrobial, Antityrosinase and Cytotoxic Potentials of Isatis cappadocica subsp. alyssifoli as a Potent Pharmaceutical Resource

2019 ◽  
pp. 1-12 ◽  
Author(s):  
Meltem Güner ◽  
Seyda Kanbolat ◽  
Nuriye Korkmaz ◽  
Rezzan Aliyazicioglu ◽  
Mahmoud Abudayyak ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Methanol Extract ◽  
Methanolic Extract ◽  
Antioxidant Properties ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Tyrosinase Inhibitor ◽  
Antioxidant Power ◽  
Tyrosinase Inhibitory Activity ◽  
Isatis Cappadocica

Isatis species, which are endemic across most of Turkey, exhibit antibacterial, anticancer and antiviral effects. The aim of this study was to determine of antioxidant, antimicrobial, tyrosinase inhibitor, cytotoxic activities, and phenolic profile of polar extracts of Isatis cappadocica Desv. We analyzed the antioxidant properties of extracts using total phenolic content (TPC), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), and 2,2-diphenylpicrylhydrazyl (DPPH) radical scavenging activity. The phenolic composition of methanolic extract of I. cappadocica was analyzed by reverse phase high performance liquid chromatography (RP-HPLC). Extracts’ antimicrobial properties were evaluated based on the agar well diffusion technique. Tyrosinase inhibitory activity was measured colorimetrically. Methanolic extract yielded better FRAP and CUPRAC results and aqueous extract yielded better DPPH activity. Benzoic acid, and sinapic acid were detected as major phenolic compounds. Methanolic extract was particularly effective against all the bacteria investigated, apart from Yersinia pseudotuberculosis. Methanol extract was exhibited tyrosinase inhibitory activity. The methanol extract has caused to death of cells by dosage in the high concentrations cytotoxic activity on the PC-3 and 3T3 cell lines. The results showed that I. cappadocica could be used as a natural source in the food, cosmetic, and drug industries due to their rich antioxidant, antimicrobial, cytotoxic and tyrosinase inhibitor activities.

Drug Design of Inhibitors of Alzheimer’s Disease (AD): POM and DFT Analyses of Cholinesterase Inhibitory Activity of β-amino di-Carbonyl Derivatives

2019 ◽  
Vol 19 (8) ◽  
pp. 688-705
Author(s):  
Taibi Ben Hadda ◽  
Abdur Rauf ◽  
Hsaine Zgou ◽  
Fatma Sezer Senol ◽  
Ilkay Erdogan Orhan ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
Metal Accumulation ◽  
Microtiter Plate ◽  
Metal Chelation ◽  
Carbonyl Derivatives ◽  
Cholinesterase Inhibitory Activity ◽  
Inhibitory Potential

Background:Since deficit of acetylcholine has been evidenced in the Alzheimer’s disease (AD) patients, cholinesterase inhibitors are currently the most specified drug category for the remediation of AD.Method:In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 μg/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity.Results and Conclusion:All the investigated dicarbonyl compounds exerted none or lower than 30% inhibition against both cholinesterases, whereas compounds 2, 8 and 11 showed 37, 42, 41% of inhibition towards BChE, being the most active. The highest metal-chelation capacity was observed with compound 8 (53.58 ± 2.06%). POM and DFT analyses are in good harmonization with experimental data.

scholarly journals Mammalian Arginase Inhibitory Activity of Methanolic Extracts and Isolated Compounds from Cyperus Species

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1694
Author(s):  
Kamel Arraki ◽  
Perle Totoson ◽  
Alain Decendit ◽  
Andy Zedet ◽  
Justine Maroilley ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Significant Inhibition ◽  
Isolation And Identification ◽  
Vasorelaxant Effect ◽  
Methanolic Extracts ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.

scholarly journals IN VITRO CYTOTOXIC ACTIVITY OF ISOLATED COMPOUNDS FROM VIBURNUM PUNCTATUM BUCH-HAM EX D. DON

2016 ◽  
Vol 9 (1) ◽  
pp. 85
Author(s):  
A. Renjith Alex ◽  
K. Ilango
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Methanol Extract ◽  
Methanolic Extract ◽  
Human Colon ◽  
Human Colon Cancer ◽  
Chloroform Methanol ◽  
Human Colon Cancer Cells

Objective: The main aim of the study was to screen the isolated compounds of Viburnum Punctatum for its in vitro anticancer activity and its percentage viability against HCT 15 (Human Colon Cancer Cells) Cell lines.Methods: Pet ether, Chloroform, Methanol and Aqueous extracts was prepared and assayed for the presence of phytochemicals. Two compounds were isolated from the methanol extract of Viburnum Punctatum by column chromatography such as ME1 (Quercetin) and ME2 (Kaemferol-3-glycoside) characterised by UV, IR, MS, 1H NMR and 13C NMR. The above isolated compounds were subjected to in vitro anticancer activity on HCT 15 cell lines was evaluated by Micro culture Tetrazolium (MTT) assay.Results: ME1 showed significant cytotoxic activity than the ME2 on HCT 15 cells with a percentage viability of 54.60 and 67.18 in the concentration of 10µg/ml and 50µg/ml respectively.Conclusion: On the basis of obtained results, ME1 and ME2 isolated from a methanolic extract of Viburnum Punctatum represent a new group of cytotoxic against HCT 15 Cell lines.

scholarly journals Computational Analysis for Physicochemical Properties of Compounds in Senna auriculata Leaves Methanolic Extract to have Antidiabetic Potentials and their Molecular Interaction with α-amylase

2021 ◽  
pp. 30-42
Author(s):  
Abdulaziz Bin Dukhyil
Keyword(s):  
Molecular Docking ◽  
Physicochemical Properties ◽  
Methanolic Extract ◽  
Natural Compounds ◽  
Physicochemical Analysis ◽  
Dynamics Simulation ◽  
Carbohydrate Hydrolysis ◽  
Catalytic Active Site ◽  
Inhibitory Potential

Aims: Diabetes mellitus (DM) is chronic disorder well known for increased glucose level in blood. This disease can be controlled by inhibiting the enzyme (e.g., α-amylase) involve in carbohydrate hydrolysis. Senna auriculata leaves methanolic extract (SALME) have potential antidiabetic properties and it was also found to be safe in preclinical studies. In this study the aim was to explore the molecular interactions of α-amylase and bioactive compounds in SALME and their physicochemical properties. Methodology: Computational approach such as molecular docking and physicochemical analysis prediction was applied to understand the antidiabetic potential of natural compounds present in SALME. Results: The results showed from physicochemical analysis that out of 11 only 7 compounds are having drug like properties which are orally and intestinally better bioavailable. Furthermore, molecular docking analysis explained that three compounds (C3, C4, and C7) have lower binding energy, ΔG (-8, -9.1, -9.5 kcal/mol) and better binding affinity, Ki (7.31 x 105, 4.68 x 106, and 9.2 x 106 M-1, respectively) than the acarbose ΔG (-7.8 kcal/mol) and Ki (6.18 x 105 M-1), a well-known FDA approved medication for DM. The study also explained the binding pattern that the catalytic residue such as Asp197, Glu233 and Asp300 are involved in stabilizing the natural compounds with in the catalytic active site of target enzyme. Conclusions: From the results it has been concluded that these three compounds found in SALME have better inhibitory potential for α-amylase in comparison with acarbose. Further validation of the findings is required through molecular dynamics simulation, ADME-T study, and in-vitro enzyme inhibition by the purified compounds.

scholarly journals Identification of a Xanthine Oxidase-inhibitory Component from Sophora Flavescens using NMR-based Metabolomics

2013 ◽  
Vol 8 (10) ◽  
pp. 1934578X1300801
Author(s):  
Ryuichiro Suzuki ◽  
Yuka Hasuike ◽  
Moeka Hirabayashi ◽  
Tatsuo Fukuda ◽  
Yoshihito Okada ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Sophora Flavescens ◽  
Vitro Assay ◽  
H Nmr ◽  
Plot Analysis ◽  
Inhibitory Compounds ◽  
Loading Plot

We demonstrate that NMR-based metabolomics studies can be used to identify xanthine oxidase-inhibitory compounds in the diethyl ether soluble fraction prepared from a methanolic extract of Sophora flavescens. Loading plot analysis, accompanied by direct comparison of 1H NMR spectra exhibiting characteristic signals, identified compounds exhibiting inhibitory activity. NMR analysis indicated that these characteristic signals were attributed to flavanones such as sophoraflavanone G and kurarinone. Sophoraflavanone G showed inhibitory activity towards xanthine oxidase in an in vitro assay.

scholarly journals Phosphodiesterase-1 Inhibitory Activity of Two Flavonoids Isolated fromPistacia integerrimaJ. L. Stewart Galls

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Abdur Rauf ◽  
Muhammad Saleem ◽  
Ghias Uddin ◽  
Bina S. Siddiqui ◽  
Haroon Khan ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
In Silico ◽  
Molecular Mechanisms ◽  
Methanolic Extract ◽  
Chemical Constituents ◽  
Folk Medicine ◽  
Chemical Characterization ◽  
Active Constituents ◽  
Isolation And Characterization

Pistacia integerrimais one of twenty species among the genusPistacia. Long horn-shaped galls that develop on this plant are harvested and used in Ayurveda and Indian traditional medicine to make “karkatshringi”, a herbal medicine used for the treatment of asthma and different disorders of respiratory tract. However, until now, the molecular mechanisms of action of “karkatshringi” and its chemical characterization are partially known. This study deals with the isolation and characterization of the active constituents from the methanolic extract ofP. integerrimagalls and it was also oriented to evaluatein vitroandin silicotheir potential enzymatic inhibitory activity against phosphodiesterase-1 (PDE1), a well-known enzyme involved in airway smooth muscle activity and airway inflammation. Our results showed that the methanolic extract ofP. integerrimagalls and some of its active constituents [naringenin (1) and 3,5,7,4′-tetrahydroxy-flavanone (2)] are ablein vitroto inhibit PDE1 activity (59.20 ± 4.95%, 75.90 ± 5.90%, and 65.25 ± 5.25%, resp.) and demonstratein silicoan interesting interaction with this enzymatic site. Taken together, our results add new knowledge of chemical constituents responsible for the biological activity ofP. integerrimaand contextually legitimate the use of this plant in folk medicine.

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

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