scholarly journals Design, Synthesis and Biological Activities of Some phthalimides Derivatives

2021 ◽  
pp. 50-56
Author(s):  
F. O. Taiwo ◽  
C. A. Obafemi ◽  
E. M. Obuotor ◽  
I. J. Olawuni
Keyword(s):  
Nitric Oxide ◽  
Spectroscopic Analysis ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Design Synthesis ◽  
Ic50 Values ◽  
Magnetic Resonance Spectroscopic Analysis ◽  
Butyryl Cholinesterase ◽  
Oxide Inhibition

Aims: To synthesize some phthalimides derivatives and evaluate the compounds for their possible biological properties. Methods: The substituted phenylisoindoline-1,3-dione were synthesized from the reactions of N-phenyl phthalimide with different substituted aromatic aldehyde. The synthesized compounds were characterized using nuclear magnetic resonance spectroscopic analysis. The Nitric oxide and Ferric reducing antioxidant properties (FRAP) were determined by spectrophochemical method. Results: The IC50 values for all the synthesized compounds were lower than standard, eserine (IC50 = 15 ± 2 µg/mL) against Nitric oxide inhibition. Compounds 3 (FRAP = 205±8 µg/ML) and 6 (FRAP = 118±1 µg/ML) were found to exhibit higher FRAP analysis results which were comparable to the results obtained for serine. (FRAP = 202±7 µg/ML). Conclusion: The considerable activity of the compounds shown by its Nitric oxide and Ferric reducing antioxidant properties (FRAP) makes them good candidates for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.

scholarly journals Synthesis of Some Phenylisoindoline-1,3-Diones and their Acetylcholinesterase and Butyryl Cholinesterase Inhibitory Activities

2021 ◽  
pp. 194-201
Author(s):  
F. O. Taiwo ◽  
C. A. Obafemi ◽  
E. M. Obuotor ◽  
I. J. Olawuni
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Magnetic Resonance ◽  
Cholinesterase Inhibitors ◽  
Spectroscopic Analysis ◽  
Choline Chloride ◽  
Biological Properties ◽  
Active Inhibitor ◽  
Magnetic Resonance Spectroscopic Analysis ◽  
Butyryl Cholinesterase ◽  
Inhibitory Activities

Aims: To synthesize some phthalimides derivatives and evaluate the compounds for their possible biological properties. Methods: The substituted phenylisoindoline-1,3-dione were synthesized from the reactions of N-phenyl phthalimide with different substituted aromatic aldehyde. The synthesized compounds were characterized using nuclear magnetic resonance spectroscopic analysis. The acetylcholinesterase and butyryl cholinesterase inhibitions were determined by Spectro photochemical analysis of acetylthiocholine and butyryl choline chloride. Results: Compounds 6 (IC50 = 30±3 µg/mL) and 4 (IC50 = 141±60 µg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 4 (IC50 = 102±10 µg/mL), 5 (IC50 = 105 ± 20 µg/mL) and 2 (IC50 = 190 ± 10 µg/mL), were found to be most active inhibitor against butyryl cholinesterase. Conclusion: The considerable acetylcholinesterase and butyryl cholinesterase inhibitory activities of the synthesized compounds makes them good candidates for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.

scholarly journals Glycomacropeptide Ameliorates Indomethacin-Induced Enteropathy in Rats by Modifying Intestinal Inflammation and Oxidative Stress

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2351 ◽  
Author(s):  
Daniel Cervantes-García ◽  
Armida I. Bahena-Delgado ◽  
Mariela Jiménez ◽  
Laura E. Córdova-Dávalos ◽  
Vanessa Ruiz-Esparza Palacios ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Intestinal Inflammation ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Lipid Hydroperoxide ◽  
Neutrophil Infiltration ◽  
Clinical Problem ◽  
Intestinal Damage ◽  
Nsaid Enteropathy ◽  
Anti Inflammatory

Nonsteroidal anti-inflammatory drug (NSAID)-induced enteropathy is considered a serious and increasing clinical problem without available treatment. Glycomacropeptide (GMP) is a 64-amino acid peptide derived from milk κ-casein with numerous biological activities. The aim of this study was to investigate the protective effect of GMP on NSAID enteropathy in rats. Enteropathy was induced by seven days oral indomethacin administration. Rats were orally GMP treated from seven days previous and during the establishment of the enteropathy model. Changes in metabolism, hematological and biochemical blood alterations, intestinal inflammation and oxidative damage were analyzed. Integrity barrier markers, macroscopic intestinal damage and survival rate were also evaluated. GMP treatment prevented anorexia and weight loss in animals. Furthermore, prophylaxis with GMP ameliorated the decline in hemoglobin, hematocrit, albumin and total protein levels. The treatment had no therapeutic efficacy on the decrease of occludin and mucin (MUC)-2 expression in intestinal tissue. However, GMP markedly decreased neutrophil infiltration, and CXCL1, interleukin-1β and inducible nitric oxide synthase expression. Nitric oxide production and lipid hydroperoxide level in the small intestine were also diminished. These beneficial effects were mirrored by preventing ulcer development and increasing animal survival. These results suggest that GMP may protect against NSAID enteropathy through anti-inflammatory and antioxidant properties.

scholarly journals Cornus mas L. Stones: A Valuable by-Product as an Ellagitannin Source with High Antioxidant Potential

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4646
Author(s):  
Dominika Przybylska ◽  
Alicja Z. Kucharska ◽  
Iwona Cybulska ◽  
Tomasz Sozański ◽  
Narcyz Piórecki ◽  
...  
Keyword(s):  
Biological Activities ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Raw Material ◽  
Hydrolyzable Tannins ◽  
Cornus Mas ◽  
Fruit Processing ◽  
High Antioxidant Activity ◽  
Total Polyphenolic Content ◽  
First Time

The stone of Cornus mas L. remains the least known morphological part of this plant, whereas the fruit is appreciated for both consumption purposes and biological activity. The stone is considered to be a byproduct of fruit processing and very little is known about its phytochemical composition and biological properties. In this study, the complete qualitative determination of hydrolyzable tannins, their quantitative analysis, total polyphenolic content, and antioxidant properties of the stone of C. mas are presented for the first time. The 37 identified compounds included the following: various gallotannins (11), monomeric ellagitannins (7), dimeric ellagitannins (10), and trimeric ellagitannins (7). The presence of free gallic acid and ellagic acid was also reported. Our results demonstrate that C. mas stone is a source of various bioactive hydrolyzable tannins and shows high antioxidant activity which could allow potential utilization of this raw material for recovery of valuable pharmaceutical or nutraceutical substances. The principal novelty of our findings is that hydrolyzable tannins, unlike other polyphenols, have been earlier omitted in the evaluation of the biological activities of C. mas. Additionally, the potential recovery of these bioactive chemicals from the byproduct is in line with the ideas of green chemistry and sustainable production.

scholarly journals Habitat Affects the Chemical Profile, Allelopathy, and Antioxidant Properties of Essential Oils and Phenolic Enriched Extracts of the Invasive Plant Heliotropium Curassavicum

Plants ◽  
2019 ◽  
Vol 8 (11) ◽  
pp. 482 ◽  
Author(s):  
Ahmed M. Abd-ElGawad ◽  
Abdelsamed I. Elshamy ◽  
Saud L. Al-Rowaily ◽  
Yasser A. El-Amier
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Essential Oils ◽  
Invasive Plant ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Bioactive Constituents ◽  
Chenopodium Murale ◽  
Two Samples ◽  
Ic50 Values

The variation in habitat has a direct effect on the plants and as a consequence, changes their content of the bioactive constituents and biological activities. The present study aimed to explore the variation in the essential oils (EOs) and phenolics of Heliotropium curassavicum collected from the coastal and inland habitats. Additionally, we determined their antioxidant and allelopathic activity against the weed, Chenopodium murale. Fifty-six compounds were identified as overall from EOs, from which 25 components were identified from the coastal sample, and 52 from the inland one. Sesquiterpenes were the main class in both samples (81.67% and 79.28%), while mono (3.99% and 7.21%) and diterpenes (2.9% and 1.77%) represented minors, respectively. Hexahydrofarnesyl acetone, (-)-caryophyllene oxide, farnesyl acetone, humulene oxide, farnesyl acetone C, and nerolidol epoxy acetate were identified as major compounds. The HPLC analysis of MeOH extracts of the two samples showed that chlorogenic acid, rutin, and propyl gallate are major compounds in the coastal sample, while vanilin, quercetin, and 4′,7-dihydroxyisoflavone are majors in the inland one. The EOs showed considerable phytotoxicity against C. murale with IC50 value of 2.66, 0.59, and 0.70 mg mL−1 for germination, root, and shoot growth, respectively from the inland sample. While the coastal sample attained the IC50 values of 1.58, 0.45, and 0.66 mg mL−1. MeOH extracts revealed stronger antioxidant activity compared to the EOs. Based on IC50 values, the ascorbic acid revealed 3-fold of the antioxidant compared to the EO of the coastal sample and 4-fold regarding the inland sample. However, the ascorbic acid showed 3-fold of the antioxidant activity of the MeOH extracts of coastal and inland samples. Although H. curassavicum is considered as a noxious, invasive plant, the present study revealed that EO and MeOH extracts of the H. curassavicum could be considered as promising, eco-friendly, natural resources for antioxidants as well as weed control, particularly against the weed, C. murale.

scholarly journals Selenium-Rich Ricegrass Juice Improves Antioxidant Properties and Nitric Oxide Inhibition in Macrophage Cells

Antioxidants ◽  
2018 ◽  
Vol 7 (4) ◽  
pp. 57 ◽  
Author(s):  
Rattanamanee Chomchan ◽  
Panupong Puttarak ◽  
Adelheid Brantner ◽  
Sunisa Siripongvutikorn
Keyword(s):  
Nitric Oxide ◽  
Antioxidant Properties ◽  
Nitric Oxide Inhibition ◽  
Macrophage Cells ◽  
Oxide Inhibition

scholarly journals Preliminary Biological Study of Two Medicinal Plants used in the Mouhoun Region (Burkina Faso): Boscia angustifolia A. Rich (Caparaceae) and Gardenia erubescens Stapf & Hutch (Rubiaceae)

2019 ◽  
pp. 1-9
Author(s):  
Jotham Yhi-Pênê N’do ◽  
Dramane Pare ◽  
Mahamadi Nikiema ◽  
Adama Hilou
Keyword(s):  
Medicinal Plants ◽  
Burkina Faso ◽  
Traditional Medicine ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Ethanolic Extract ◽  
Biological Properties ◽  
Biological Study ◽  
Microbial Strains ◽  
Reduction Capacity

Aims: Boscia agustifolia and Gardenia erubescens are two medicinal plants widely used in the Mouhoun region. The strong use of these two plants in traditional medicine would be linked to their therapeutic virtues. Study Design: The purpose of this work was to carry out a preliminary biological study on two plants widely used by the population of the Mouhoun region (Burkina Faso) against certain diseases. Place and Duration of Study: The harvest of plant material was made in the Mouhoun region in March 2019. The phytochemistry and the antioxidant tests were carried out at LABIOCA in June 2019. The microorganism tests were carried out at CRSBAN. Methodology: The extracts were obtained by ethanolic maceration. The FRAP method and DPPH were used to evaluate the antioxidant properties of the extracts. The antibiomicrobial activity of the extracts was determined using five microbial strains. Results: The ethanolic extract of Gardenia erubescens bark had antioxidant activity through the iron ion reduction capacity (6.71 ± 1.16 mMol EAA/100 g extract. Boscia angustifolia showed inhibitory activity on the five microbial strains. Conclusion: The biological activities obtained with these extracts could be justified by the presence of active phytochemicals such as flavonoids. These biological properties to constitute a reason based on the strong use of these two plants in traditional medicine.

scholarly journals Design, synthesis and evaluation of biological activities of some novel anti-TB agents with bio-reducible functional group

Bioimpacts ◽  
2019 ◽  
Vol 9 (4) ◽  
pp. 199-209
Author(s):  
Hossein Khani-Meinagh ◽  
Hossein Mostafavi ◽  
Norbert Reiling ◽  
Majid Mahdavi ◽  
Gholamreza Zarrini
Keyword(s):  
Fatty Acid Synthase ◽  
Functional Group ◽  
Biological Activities ◽  
Reduction Reaction ◽  
Log P ◽  
P Value ◽  
Human Leukemia ◽  
Type I ◽  
Design Synthesis ◽  
Ic50 Values

Introduction: With regard to the anti-mycobacterial activity of 2-pyrazinoic acid esters (POEs), recent studies have shown that both pyrazine core and alkyl part of POE interact with the fatty acid synthase type (I) (FAS (I)) precluding a complex formation between NADPH and FAS (I). Methods: Considering this interaction at the reductase site of FAS (I) responsible for reduction of β-ketoacyl-CoA to β-hydroxyacyl-CoA, we hypothesized that POE containing a bioreducible center in its alkyl part might show an increased anti-tubercular activity due to the involvement of FAS (I) in extra bio-reduction reaction. Thus, we synthesized novel POEs, confirmed their structures by spectral data, and subsequently evaluated their anti-mycobacterial activity against Mycobacterium tuberculosis (Mtb) (H37Rv) strain at 10 μg/mL concentration. Results: Compounds 3c, 3j, and 3m showed higher activity with regard to the inhibition of Mtb growth by 45.4, 45.7, and 51.2% respectively. Unexpectedly, the maltol derived POE 3l having the lowest log p value among the POEs indicated the highest anti-mycobacterial growth activity with 56% prevention. Compounds 3c and 3l showed no remarkable cytotoxicity on human macrophages at 10 μg/mL concentration as analyzed by xCELLigence real-time cell analysis. In further experiments, some of the tested POEs, unlike pyrazinamide (PZA), exhibited significant antibacterial and also anti-fungal activities. POEs showed an enhanced bactericidal activity on gram-positive bacteria as shown for Staphylococcus aureus, e.g. compound 3b with a MIC value of 125 μg/mL but not E. coli as a gram-negative bacteria, except for maltol derived POE (3l) that showed an inverse activity in the susceptibility test. In the anticancer activity test against the human leukemia K562 cell lines using MTT assay, compounds 3e and 3j showed the highest cytotoxic effect with IC50 values of 25±8.0 μΜ and 25±5.0 μΜ, respectively. Conclusion: It was found that the majority of POEs containing a bioreducible center showed higher inhibitory activities on Mtb growth when compared to the similar compounds without a bio-reducible functional group.

scholarly journals Metabolomic Profiling and Biological Activities of Pleurotus columbinus Quél. Cultivated on Different Agri-Food Byproducts

Antibiotics ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 1245
Author(s):  
Paola Angelini ◽  
Roberto Maria Pellegrino ◽  
Bruno Tirillini ◽  
Giancarlo Angeles Flores ◽  
Husam B. R. Alabed ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Biological Activities ◽  
Biological Effects ◽  
Antioxidant Properties ◽  
Principal Component ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Ms Analysis ◽  
Quantitative Hplc ◽  
Mushroom Extracts

The genus Pleurotus (Fr.) P. Kumm (Pleurotaceae, Basidiomycota) comprises a cosmopolitan group of mushrooms highly appreciated for their nutritional value and health-promoting benefits. Despite there being many studies about the phytochemical composition of Pleurotus spp., there are very few reports dealing with the phytochemistry, antioxidant and antimicrobial activities of P. columbinus Quél. In this study, a mass spectrometry ultra-performance liquid chromatography mass spectrometry (UHPLC)-QTOF method, coupled with principal component analysis (PCA), was applied to the P. columbinus metabolome in order to investigate the influence of different agri-food residues as growth substrates for P. columbinus cultivation, on the bioactive chemical profile of fruiting bodies and evaluated their potential as antioxidants and antimicrobials. Additionally, a quantitative HPLC-DAD-MS analysis was conducted on phenolic and flavonoid compounds, that could explain, albeit partially, the observed biological effects of P. columbinus extracts. The qualitative metabolic profile identified 97 metabolites, whereas the quantitative HPLC-DAD-MS analysis confirmed the presence of phenolic and flavonoids, in the mushroom extracts, which also showed intrinsic scavenging/reducing and antimicrobial effects. The antibacterial effects were particularly evident against Escherichia coli, whereas Tricophyton and Aspergillus were the dermatophytes more sensitive to the mushroom extracts. The present study supports more in-depth investigations, aimed at evaluating the influence of growth substrate on P. columbinus antimicrobial and antioxidant properties. The extracts from P. columbinus revealed valuable sources of primary and secondary metabolites, thus suggesting potential applications in the formulation of food supplements with biological properties, above all in terms of antioxidant and antimicrobial properties.

scholarly journals Investigation of the Chemical Composition and Antioxidant and Antimicrobial Activities of Lobularia maritima: Potent Therapeutic Applications

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Soumaya Kouidhi ◽  
Oumaima Zidi ◽  
Soukaina Abdelwahed ◽  
Yasmine Souissi ◽  
Najla Trabelsi ◽  
...  
Keyword(s):  
Biological Activities ◽  
Antioxidant Properties ◽  
Extraction Methods ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Aspergillus Ochraceus ◽  
Therapeutic Applications ◽  
Lobularia Maritima ◽  
Promising Source ◽  
Antioxidant And Antimicrobial Activities

Lobularia maritima, commonly known as sweet alyssum, is an annual ornamental halophyte widely spread along the Tunisian seashore. However, little is known about the phytochemical, antioxidant, and antimicrobial activities of Lobularia maritima. The present study aimed to investigate the potential biological properties of different parts (flowers, leaves, roots, and stems) of Tunisian L. maritima using diverse extraction methods. Extracts were then studied for their antioxidant properties, and the highest antioxidant activity was presented in the roots’ fractions. Added to this, flower, leaf, and root fractions showed interesting antimicrobial and antifungal activities against different Gram+ and Gram− bacteria and against Aspergillus ochraceus. Finally, the most active fractions (presenting the highest biological activities) were analyzed using silica gel purification and mass spectrometry coupled to gas chromatography (GC-MS) analysis, and different compounds were identified such as camphor, amide of oleic acids, tributyl acetylcitrate, betulinaldehyde, menthol, 1′-(butyn-3-one-1-yl)-, (1S, 2S, 5R), benzyl benzoate, 7-acetyl-6-ethyl-1,1,4,4-tetramethyltetralin, 2,4-heptadienal, (E,E), and nootkaton-11,12-epoxide. This work represents the first in-depth investigation of the content of bioactive compounds from Lobularia maritima. This species could potentially be a promising source of useful compounds for therapeutic applications.

scholarly journals Antifungal, Antitumoral and Antioxidant Potential of the Danube Delta Nymphaea alba Extracts

Antibiotics ◽  
2019 ◽  
Vol 9 (1) ◽  
pp. 7 ◽  
Author(s):  
Mihaela Cudalbeanu ◽  
Bianca Furdui ◽  
Geta Cârâc ◽  
Vasilica Barbu ◽  
Alina Viorica Iancu ◽  
...  
Keyword(s):  
Laser Scanning ◽  
Antioxidant Properties ◽  
Inhibitory Effect ◽  
Biological Properties ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Danube Delta ◽  
Methanolic Extracts ◽  
Nymphaea Alba ◽  
Ic50 Values

This study aimed to explore for the first time the biological properties such as antifungal, antitumoral and antioxidant of Danube Delta Nymphaea alba (N. alba) leaf and root methanolic extracts. The toxicity studies of N. alba extracts showed no inhibitory effect on wheat seed germination by evaluating the most sensitive physiological parameters (Germination %, Germination index, Vigor index) and using confocal laser scanning microscopy images. The analyzed extracts were found to have high antifungal activity against Candida glabrata with MIC values of 1.717 µg/mL for leaf and 1.935 µg/mL for root. The antitumor activity of the both extracts against A2780/A2780cisR ovarian, LNCaP prostate and MCF-7 breast cancer cells was promising with IC50 values ranging from 23–274 µg/mL for leaf and 18–152 µg/mL for root, and the combination of N. alba extracts with cisplatin showed a synergistic effect (coefficient of drug interaction <1). The antioxidant properties were assessed by β-carotene bleaching, ABTS and FRAP assays and cyclic voltammetry. Quercetin, the most prominent antioxidant, was quantified in very good yields by spectroelectrochemical assay.

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