scholarly journals Acetylcholinesterase inhibitors and antioxidants mining from marine fungi: bioassays, bioactivity coupled LC–MS/MS analyses and molecular networking

2020 ◽  
Vol 2 (4) ◽  
pp. 386-397
Author(s):  
Yingying Nie ◽  
Wencong Yang ◽  
Yayue Liu ◽  
Jingming Yang ◽  
Xiaoling Lei ◽  
...  
Keyword(s):  
Aspergillus Terreus ◽  
Marine Fungi ◽  
Radical Scavenging ◽  
Bioactive Molecules ◽  
Ache Inhibition ◽  
Bioactive Constituents ◽  
Molecular Networking ◽  
Unknown Compound ◽  
Ache Inhibitors ◽  
Larval Toxicity

Abstract Marine fungi are potentially important resources for bioactive lead compounds for discovering new drugs for diseases such as Alzheimer’s disease. In this paper, the combined bioassay model of acetylcholinesterase (AChE) inhibition, 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging, and Artemia larval lethality was used to evaluate the activity and toxicity of 35 marine fungal strains from seas around China. Their bioactive constituents were revealed by thin layer chromatography (TLC) autography, bioactivity coupled LC–MS/MS and Global Natural Products Social Molecular Networking (GNPS). The results show that the extracts of five strains exhibited higher AChE inhibition ratios than the positive control compound, ‘tacrine’, for which the ratio was 89.8% at 200 μg/ml. Six strains displayed both AChE inhibition (inhibition ratios > 20% at 200 μg/ml) and DPPH scavenging activity (scavenging ratios > 30% at 200 μg/ml) together with low Artemia larval toxicity (lethal rates < 12%). TLC autography showed that the fractioned extracts of four strains contained highly diverse and different bioactive constituents, including strains Talaromyces sp. C21-1, Aspergillus terreus C23-3, Trichoderma harzianum DLEN2008005, and Penicillium corylophilum TBG1-17. From the most potent sample F-11-1-b (derived from Aspergillus terreus C23-3), five AChE inhibitors and seven antioxidants were recognized as bioactive molecules by AChE coupled ultrafiltration followed by LC–MS/MS, and LC–MS/MS coupled with DPPH incubation. Furthermore, with the aid of GNPS, the AChE inhibitors were plausibly annotated as territrem analogues including territrems A–C/D, arisugacin A and an unknown compound 4, and the seven antioxidants were assigned as butyrolactone Ι, aspernolide E, a phenolic derivative and possibly unknown compounds 8–10 and 12.

scholarly journals Characterization of Anti-Inflammatory and Antioxidant Constituents from Scutellaria baicalensis Using LC-MS Coupled with a Bioassay Method

Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3617
Author(s):  
Yoo Kyong Han ◽  
Hyunwoo Kim ◽  
Hyeji Shin ◽  
Jiyeon Song ◽  
Mi Kyeong Lee ◽  
...  
Keyword(s):  
Screening Method ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Scutellaria Baicalensis ◽  
No Production ◽  
Dpph Assay ◽  
Bioactive Constituents ◽  
Total Extract ◽  
Molecular Networking ◽  
Bv2 Cells

An effective and previously demonstrated screening method for active constituents in natural products using LC-MS coupled with a bioassay was reported in our earlier studies. With this, the current investigation attempted to identify bioactive constituents of Scutellaria baicalensis through LC-MS coupled with a bioassay. Peaks at broadly 17–20 and 24–25 min on the MS chromatogram displayed an inhibitory effect on NO production in lipopolysaccharide-induced BV2 microglia cells. Similarly, peaks at roughly 17–19 and 22 min showed antioxidant activity with an 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS)/2,2-diphenyl-1- picrylhydrazyl (DPPH) assay. For confirmation of LC-MS coupled with a bioassay, nine compounds (1–9) were isolated from an MeOH extract of S. baicalensis. As we predicted, compounds 1, 8, and 9 significantly reduced lipopolysaccharide (LPS)-induced NO production in BV2 cells. Likewise, compounds 5, 6, and 8 exhibited free radical-scavenging activities with the ABTS/DPPH assay. In addition, the structural similarity of the main components was confirmed by analyzing the total extract and EtOAc fractions through molecular networking. Overall, the results suggest that the method comprised of LC-MS coupled with a bioassay can effectively predict active compounds without an isolation process, and the results of molecular networking predicted that other components around the active compound node may also be active.

scholarly journals Antimicrobial, Antioxidant, and Cytotoxic Activities of Juglans regia L. Pellicle Extract

Antibiotics ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 159
Author(s):  
Floriana D’Angeli ◽  
Giuseppe Antonio Malfa ◽  
Adriana Garozzo ◽  
Giovanni Li Volti ◽  
Carlo Genovese ◽  
...  
Keyword(s):  
Herpes Simplex ◽  
Juglans Regia ◽  
Radical Scavenging ◽  
Fungal Growth ◽  
Bioactive Molecules ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Anion Formation ◽  
Herpes Simplex Viruses

The difficulty to treat resistant strains-related hospital-acquired infections (HAIs) promoted the study of phytoextracts, known sources of bioactive molecules. Accordingly, in the present study, the pharmacological activities of Juglans regia (L.) pellicle extract (WPE) were investigated. The antiviral effect was tested against Herpes simplex virus type 1 and 2, Poliovirus 1, Adenovirus 2, Echovirus 9, Coxsackievirus B1 through the plaque reduction assay. The antibacterial and antifungal activities were evaluated against medically important strains, by the microdilution method. DPPH and superoxide dismutase (SOD)s-like activity assays were used to determine the antioxidant effect. Besides, the extract was screened for cytotoxicity on Caco-2, MCF-7, and HFF1 cell lines by the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. The total phenolic and flavonoid contents were also evaluated. Interestingly, WPE inhibited Herpes simplex viruses (HSVs) replication, bacterial and fungal growth. WPE showed free radical scavenging capacity and inhibited superoxide anion formation in a dose-dependent manner. These effects could be attributed to the high content of phenols and flavonoids, which were 0.377 ± 0.01 mg GE/g and 0.292 ± 0.08 mg CE/g, respectively. Moreover, WPE was able to reduce Caco-2 cell viability, at both 48 h and 72 h. The promising results encourage further studies aimed to better elucidate the role of WPE in the prevention of human infectious diseases.

ASSESSMENT OF PHYTOCHEMICALS, TOTAL PHENOL, FLAVONOID CONTENT AND IN VITRO ANTIOXIDANT PROPERTY OF LARGE CARDAMOM EXTRACTS

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (10) ◽  
pp. 34-41
Author(s):  
Kanthlal S. K. ◽  
Jipnomon Joseph ◽  
Bindhu P. Paul ◽  
Vijayakumar M ◽  
Rema Shree A. B. ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Antioxidant Property ◽  
Bioactive Constituents ◽  
Preliminary Assessment ◽  
Reducing Power Assay ◽  
Large Cardamom

Amomum subulatum, commonly known as large or black cardamom, is a commonly used spice in Indian kitchens and is traditionally used to treat various ailments. To add more knowledge about the medicinal values of the fruit, this study was conducted to evaluate the in vitro antioxidant activities of aqueous, methanol, ethanol, hydro alcohol, ethyl acetate, acetone and chloroform extracts of the fruit. Preliminary assessment was done to detect the presence of phytoconstituents using identification tests. The antioxidant activity was measured by employing methods such as diphenylpicrylhydrazyl (DPPH) radical scavenging assay, total antioxidant activity equivalent to ascorbic acid, reducing power assay and superoxide anion scavenging assay. The antioxidant activities were compared with their respective phenol and flavonoid contents. Preliminary assessment revealed that large cardamom fruit is a good source of all the bioactive constituents as well as phenol and flavonoid essential for medicinal values. The extract obtained by polar solvents showed the highest antioxidant efficacy in relation to its phenol content. Also, all the solvent-soluble fractions showed a concentration-dependent antioxidant effect. Results from our study prove that large cardamom can alleviate oxidative stress, suggesting the potential of large cardamom as a functional food

scholarly journals Thymus algeriensis and Artemisia herba-alba Essential Oils: Chemical Analysis, Antioxidant Potential and In Vivo Anti-Inflammatory, Analgesic Activities, and Acute Toxicity

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6780
Author(s):  
Khadija El Ouahdani ◽  
Imane Es-safi ◽  
Hamza Mechchate ◽  
Mohammed Al-zahrani ◽  
Ashraf Ahmed Qurtam ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Medicinal Plants ◽  
Essential Oils ◽  
Iron Reduction ◽  
Radical Scavenging ◽  
Bioactive Molecules ◽  
Potential Toxicity ◽  
Thymus Algeriensis ◽  
Anti Inflammatory

The study of bioactive molecules of natural origin is a focus of current research. Thymus algeriensis and Artemisia herba-alba are two medicinal plants widely used by the Moroccan population in the traditional treatment of several pathologies linked to inflammation. This study aimed to evaluate the single and combined antioxidant, anti-inflammatory and analgesic effects of the essential oils extracted from these two medicinal plants, and also their potential toxicity. Essential oils were extracted using hydro-distillation in a Clevenger-type apparatus. The antioxidant activity was evaluated by two methods: the scavenging of the free radical DPPH, and the reduction in iron. Anti-inflammatory activity was evaluated by evaluating the edema development induced by carrageenan injecting, while the analgesic power was evaluated according to the number of abdominal contortions induced by the intraperitoneal injection of acetic acid (0.7%). The acute oral toxicity was performed to assess the potential toxicity of the studied EOs, followed by an analysis of the blood biochemical parameters. The results of the two antioxidant tests indicated that our extract mixture exhibits good iron reduction capacity and very interesting DPPH free radical scavenging power, with an IC50 of around 4.38 ± 0.98 μg/mL higher than that of the benchmark antioxidant, BHT. The anti-inflammatory test demonstrated that the mixture administered orally at a dose of 150 mg/kg has a better activity, exceeding that of 1% Diclofenac, with a percentage of maximum inhibition of the edema of 89.99 ± 4.08. The number of cramps in the mice treated with the mixture at a dose of 150 mg/kg is significantly lower (29.80 ± 1.92) than those of the group treated with Tramadol (42.00 ± 2.70), respectively. The toxicity results show no signs of toxicity with an LD50 greater than 150 mg/Kg. These interesting results show that the two plants’ EOs had an important anti-inflammatory, analgesic, and antioxidant activity, and also a powerful synergistic effect, which encourages further in-depth investigations on their pharmacological proprieties.

scholarly journals Comparative phytochemical profiling and effects of Nerium oleander extracts on the activities of murine peritoneal macrophages

2016 ◽  
Vol 68 (3) ◽  
pp. 515-531 ◽  
Author(s):  
Priyankar Dey ◽  
Tapas Chaudhuri
Keyword(s):  
Free Radical ◽  
Leaf Extract ◽  
Radical Scavenging ◽  
Peritoneal Macrophages ◽  
Nerium Oleander ◽  
Gas Chromatography Mass Spectrometry ◽  
Phytochemical Analysis ◽  
Bioactive Constituents ◽  
Root Extracts ◽  
Murine Peritoneal Macrophages

Nerium oleander is a medicinal plant. Apart from its ethnopharmacological uses, pharmacognostic studies have revealed several of its bioactivities. Previously we demonstrated that the phenolic and flavonoid rich extracts of oleander leaf, stem and root possess potent antioxidant and free radical scavenging activities. Moreover, the leaf extract actively modulates the Th1/Th2 cytokine balance and exerts anti-inflammatory activities on murine splenic lymphocytes. Therefore, the present study was designed to evaluate the effect of oleander leaf, stem and root extracts on phagocytosis and the free radical-related activities of murine peritoneal macrophages. In addition, phytochemical profiling was performed using gas chromatography-mass spectrometry (GC-MS). The results demonstrated that the increase in phagocytosis and decrease in myeloperoxidase (MPO) were in the order of leaf>root>stem. The inhibition of cell adhesion, nitric oxide (NO) and elevation of respiratory burst activity was in the order of leaf>stem>root. However, the bioactivities of the leaf extract were much high than those of the stem and root extracts. Phytochemical analysis also revealed the presence of several bioactive constituents in oleander extracts. Therefore, the present study demonstrated that oleander possesses the capacity to modulate macrophage activities and the bioactivities are attributed to the numerous phytochemicals identified in oleander extracts.

scholarly journals ACETYLCHOLINESTERASE INHIBITORY EFFECT OF 3-(1H-INDOL-3-YL)-1, 3-DIPHENYLPROPAN-1-ONE DERIVATIVES

2017 ◽  
Vol 10 (8) ◽  
pp. 83
Author(s):  
Manjunatha K S ◽  
Manu Cp ◽  
Satyanarayan Nd ◽  
Vinay Kn ◽  
Vineetha Ms ◽  
...  
Keyword(s):  
Hydrochloric Acid ◽  
Mode Of Action ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Considerable Degree ◽  
Ache Inhibition ◽  
Ache Inhibitors ◽  
Ellman’S Method ◽  
Inhibition Ability

Objective: The objective of the study is acetylcholinesterase (AChE) inhibitory effect of 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives by Ellman’s method, physostigmine is used as positive control.Method: 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were synthesized by the addition of chalcone (0.25 g, 1 mmol), indole (0.12 g, 1 mmol) in ethanol (5 ml), and concentrated hydrochloric acid (5 mmol %). These earlier synthesized compounds were screened for AChE inhibitors by modifying Ellman’s method.Results: Among the tested compounds, 3a and 3j were found to be having more potential than other compounds with half maximal inhibitory concentration values of 13.64 and 14.3 μg/ml, respectively. Whereas, compounds 3c, 3e, 3g, and 3i exhibited an average AChE inhibition of 16.4, 17.9, 17.6, and 21.1 μg/ml, respectively.Conclusion: The compounds 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were found to be possible lead molecules in AChE inhibition and even though, the molecules were structurally dissimilar to that of the standard, still they exhibited a considerable degree of inhibition and encourage the researchers to look into the mode of action of their inhibition ability against AChE.

scholarly journals Neuroprotective Metabolites from Vietnamese Marine Derived Fungi of Aspergillus and Penicillium Genera

Marine Drugs ◽  
2020 ◽  
Vol 18 (12) ◽  
pp. 608
Author(s):  
Elena V. Girich ◽  
Anton N. Yurchenko ◽  
Olga F. Smetanina ◽  
Phan Thi Hoai Trinh ◽  
Ngo Thi Duy Ngoc ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Secondary Metabolites ◽  
Cell Viability ◽  
Chemical Structure ◽  
Aspergillus Terreus ◽  
Marine Fungi ◽  
2D Nmr ◽  
Natural Source ◽  
Low Molecular Weight ◽  
First Time

Low molecular weight secondary metabolites of marine fungi Aspergillus flocculosus, Aspergillus terreus and Penicillium sp. from Van Phong and Nha Trang Bays (Vietnam) were studied and a number of polyketides, bis-indole quinones and terpenoids were isolated. The structures of the isolated compounds were determined by 1D and 2D NMR and HR-ESI-MS techniques. Stereochemistry of some compounds was established based on ECD data. A chemical structure of asterriquinone F (6) was thoroughly described for the first time. Anthraquinone (13) was firstly obtained from a natural source. Neuroprotective influences of the isolated compounds against 6-OHDA, paraquat and rotenone toxicity were investigated. 4-Hydroxyscytalone (1), 4-hydroxy-6-dehydroxyscytalone (2) and demethylcitreoviranol (3) have shown significant increasing of paraquat- and rotenone-treated Neuro-2a cell viability and anti-ROS activity.

scholarly journals Bioactivities of Centaurium erythraea (Gentianaceae) Decoctions: Antioxidant Activity, Enzyme Inhibition and Docking Studies

Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3795 ◽  
Author(s):  
Laura Guedes ◽  
Pedro B. P. S. Reis ◽  
Miguel Machuqueiro ◽  
Asma Ressaissi ◽  
Rita Pacheco ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antioxidant Activities ◽  
Biological Effects ◽  
Radical Scavenging ◽  
Docking Studies ◽  
Top Down ◽  
Ache Inhibitors ◽  
Shape Complementarity ◽  
In Silico Molecular Docking ◽  
Centaurium Erythraea

Centaurium erythraea is recommended for the treatment of gastrointestinal disorders and to reduce hypercholesterolemia in ethno-medicinal practice. To perform a top-down study that could give some insight into the molecular basis of these bioactivities, decoctions from C. erythraea leaves were prepared and the compounds were identified by liquid chromatography-high resolution tandem mass spectrometry (LC–MS/MS). Secoiridoids glycosides, like gentiopicroside and sweroside, and several xanthones, such as di-hydroxy-dimethoxyxanthone, were identified. Following some of the bioactivities previously ascribed to C. erythraea, we have studied its antioxidant capacity and the ability to inhibit acetylcholinesterase (AChE) and 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR). Significant antioxidant activities were observed, following three assays: free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) reduction; lipoperoxidation; and NO radical scavenging capacity. The AChE and HMGR inhibitory activities for the decoction were also measured (56% at 500 μg/mL and 48% at 10 μg/mL, respectively). Molecular docking studies indicated that xanthones are better AChE inhibitors than gentiopicroside, while this compound exhibits a better shape complementarity with the HMGR active site than xanthones. To the extent of our knowledge, this is the first report on AChE and HMGR activities by C. erythraea decoctions, in a top-down analysis, complemented with in silico molecular docking, which aims to understand, at the molecular level, some of the biological effects ascribed to infusions from this plant.

scholarly journals Triterpenes from Warszewiczia coccinea (Rubiaceae) as Inhibitors of Acetylcholinesterase

2009 ◽  
Vol 4 (10) ◽  
pp. 1934578X0900401
Author(s):  
Angela I. Calderón ◽  
Johayra Simithy ◽  
Giuliana Quaggio ◽  
Alex Espinosa ◽  
Jose Luis López-Pérez ◽  
...  
Keyword(s):  
Free Radical ◽  
Thin Layer ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Spectroscopic Methods ◽  
Ache Inhibitors ◽  
Ache Inhibitory Activity ◽  
Stem Extract ◽  
Layer Chromatography ◽  
Free Radical Scavenging Activities

Seventy-six plant extracts from the Panamanian flora have been screened for acetylcholinesterase (AChE) inhibitors by thin-layer chromatography (TLC) bioautography. The most promising extracts with AChE inhibitory and free radical scavenging activities at 100 μg were those of Tabernaemontana panamensis (Markgr., Boiteau & L. Allorge) Leeuwenb., Pentagonia macrophylla Benth., and Warszewiczia coccinea (Vahl) Klotzsch. Bioguided fractionation of W. coccinea stem extract afforded two triterpenes, 3β,6β,19α-trihydroxy-urs-12-en-28-oic acid (1) and 3β,6β-dihydroxy-olean-12-en-28-oic acid (sumaresinolic acid) (2), with AChE inhibitory activity. Their structures were determined by spectroscopic methods. This is the first report of these bioactive triterpenes in W. coccinea.

scholarly journals Properties of Ginkgo biloba L.: Antioxidant Characterization, Antimicrobial Activities, and Genomic MicroRNA Based Marker Fingerprints

2020 ◽  
Vol 21 (9) ◽  
pp. 3087 ◽  
Author(s):  
Katarína Ražná ◽  
Zuzanna Sawinska ◽  
Eva Ivanišová ◽  
Nenad Vukovic ◽  
Margarita Terentjeva ◽  
...  
Keyword(s):  
Ginkgo Biloba ◽  
Radical Scavenging Activity ◽  
Bacterial Species ◽  
Radical Scavenging ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Bioactive Constituents ◽  
Leaf Extracts ◽  
Minimal Inhibition Concentration ◽  
Fresh Matter ◽  
Antioxidant Power

The aim of this study was to characterize extracts from the leaves of Ginkgo biloba L. from selected Slovakian localities in terms of the content of bioactive constituents, antioxidants and their antimicrobial properties. The results indicated that the content of antioxidants was sample-specific, and this specificity was statistically significant. Ginkgo biloba L. from the locality of Košice had the best activity determined by the free radical scavenging activity (DPPH) (1.545 mg Trolox equivalent antioxidant capacity (TEAC)/g fresh matter (FM)) as well as the molybdenum-reducing antioxidant power (35.485 mg TEAC/g FM) methods. The highest content of total polyphenols (2.803 mg gallic acid equivalent (GAE)/g FM) and flavonoids (4.649 μg quercetin equivalent (QE)/g FM) was also detected in this sample. All samples of G. biloba leaf extracts showed significant antimicrobial activity against one or more of the examined bacterial species, and Staphylococcus aureus subsp. aureus CCM 2461 was found to be the most susceptible (minimal inhibition concentration MIC50 and MIC90 values of 64.2 and 72.2 µg/mL, respectively). Based on the results it was concluded that Ginkgo biloba L. extracts can be used as antimicrobial and antioxidant additives. Selected miRNA-based molecular markers were used to examine the environmental adaptability of Ginkgo biloba L. An almost-complete genotype clustering pattern based on locality was determined in the analysis that involved a species-specific gb-miR5261 marker. Morphologically specific exemplar, cv. Ohatsuki, was excluded.

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