Acetylcholine esterase inhibitory activity of green synthesized nanosilver by naphthopyrones isolated from marine-derived Aspergillus niger

Aspergillus niger metabolites exhibited a wide range of biological properties including antioxidant and neuro-protective effects and some physical properties as green synthesis of silver nanoparticles AgNP. The present study presents a novel evidence for the various biological activities of green synthesized AgNPs. For the first time, some isolated naphtho-γ-pyrones from marine-derived Aspergillus niger, flavasperone (1), rubrofusarin B (2), aurasperone A (3), fonsecinone A (4) in addition to one alkaloid aspernigrin A (7) were invistigated for their inhibitory activity of acetylcholine esterase AChE, a hallmark of Alzheimer’s disease (AD). The ability to synthesize AgNPs by compounds 3, 4 and 7 has been also tested for the first time. Green synthesized AgNPs were well-dispersed, and their size was ranging from 8–30 nm in diameter, their morphology was obviously spherical capped with the organic compounds. Further biological evaluation of their AChE inhibitory activity was compared to the parent compounds. AgNps dramatically increased the inhibitory activity of Compounds 4, 3 and 7 by 84, 16 and 13 fold, respectively to be more potent than galanthamine as a positive control with IC50 value of 1.43 compared to 0.089, 0.311 and 1.53 of AgNPs of Compounds 4, 3 and 7, respectively. Also compound 2 showed moderate inhibitory activity. This is could be probably explained by closer fitting to the active sites or the synergistic effect of the stabilized AgNPs by the organic compouds. These results, in addition to other intrinsic chemical and biological properties of naphtho-γ-pyrones, suggest that the latter could be further explored with a view towards other neuroprotective studies for alleviating AD.

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Design, Synthesis and Biological Evaluation of of Novel Anticancer Agent tert-butyl 1-phenyl-3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.781-784.2211 ◽

2013 ◽

Vol 781-784 ◽

pp. 2211-2214

Author(s):

Biao Shi ◽

Yi Qian Wang ◽

Yao Yang ◽

Peng Yu ◽

Kui Lu

Keyword(s):

Biological Activities ◽

Biological Properties ◽

Biological Evaluation ◽

Nmr Spectrum ◽

Design Synthesis ◽

H Nmr ◽

Growth Inhibitory ◽

Wide Range ◽

New Compounds ◽

Synthesis And Biological Evaluation

Indole and its derivatives extensively exist in nature, which showed a wide range of biological activities. Recently, there is a growing tendency to develop some new methods for the synthesis of novel indole derivatives and to study their biological properties. In this paper, we would like to report the design, synthesis and biological evaluation of a novel series of tricyclic indoles by employing Pictet-Spengler reaction as key step. All the target compounds were synthesized in four steps in 68-78% overall yield, which were characterized by 1H-NMR spectrum. All this new compounds were tested in an MTT assay on HepG2 and K562 and HT-29. Two of them showed tumor cell growth inhibitory good activity.

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1,4-Diazepines: A Review on Synthesis, Reactions and Biological Significance

Current Organic Synthesis ◽

10.2174/1570179416666190703113807 ◽

2019 ◽

Vol 16 (5) ◽

pp. 709-729 ◽

Cited By ~ 4

Author(s):

Muhammad A. Rashid ◽

Aisha Ashraf ◽

Sahibzada S. Rehman ◽

Shaukat A. Shahid ◽

Adeel Mahmood ◽

...

Keyword(s):

Biological Activities ◽

Biological Significance ◽

Biological Evaluation ◽

Wide Range ◽

Pharmaceutical Industries ◽

Biological Aspects ◽

Synthetic Routes ◽

Biological Attributes ◽

Synthesis Reactions ◽

Potential Use

Background:1,4-Diazepines are two nitrogen containing seven membered heterocyclic compounds and associated with a wide range of biological activities. Due to its medicinal importance, scientists are actively involved in the synthesis, reactions and biological evaluation of 1,4-diazepines since number of decades.Objective:The primary purpose of this review is to discuss the synthetic schemes and reactivity of 1,4- diazepines. This article also describes biological aspects of 1,4-diazepine derivatives, that can be usefully exploited for the pharmaceutical sector.Conclusion:This review summarizes the abundant literature on synthetic routes, chemical reactions and biological attributes of 1,4-diazepine derivatives. We concluded that 1,4-diazepines have significant importance due to their biological activities like antipsychotic, anxiolytic, anthelmintic, anticonvulsant, antibacterial, antifungal and anticancer. 1,4-diazepine derivatives with significant biological activities could be explored for potential use in the pharmaceutical industries.

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Nω-Hydroxy-L-arginine and Its Homologues. Chemical and Biological Properties. A Review

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc20040499 ◽

2004 ◽

Vol 69 (3) ◽

pp. 499-510 ◽

Cited By ~ 1

Author(s):

Petra Beranová ◽

Karel Chalupský ◽

Gustav Entlicher

Keyword(s):

Inhibitory Activity ◽

Biological Activities ◽

Biological Effects ◽

Biological Properties ◽

No Synthase ◽

Point Of View ◽

No Donor ◽

Good Substrate ◽

No Formation ◽

Vasorelaxant Activity

Nω-Hydroxy-L-arginine (NOHA) is a stable intermediate in NO formation from L-arginine catalyzed by NO synthase (NOS). Apparently, NOHA can be released and serve as a stable reserve NO donor (as a substrate of NOS) or transported and exert its own biological effects. It shows endothelium-dependent as well as endothelium-independent vasorelaxant activity. The latter case indicates that NOHA can be metabolized by pathways independent of NOS. These possibilities are discussed in detail. Of the available NOHA homologues homo-NOHA is a good substrate of NOS while nor-NOHA seems to be a very poor substrate of this enzyme. On the contrary, nor-NOHA exerts arginase inhibitory activity 20 times higher than NOHA whereas homo-NOHA is inactive. Detailed investigation of biological activities of NOHA and its homologues seems to be promising from the pharmacological point of view. A review with 43 references.

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A Review of the Traditional Uses, Phytochemistry and Biological Activities of the Genus Santolina

Planta Medica ◽

10.1055/a-0585-6153 ◽

2018 ◽

Vol 84 (09/10) ◽

pp. 627-637 ◽

Cited By ~ 3

Author(s):

Rosa Tundis ◽

Monica Loizzo

Keyword(s):

Biological Activities ◽

Biological Properties ◽

Future Research ◽

Chemical Profile ◽

Bioactive Constituents ◽

Mediterranean Flora ◽

Traditional Uses ◽

Ancient Times ◽

Analgesic Activities ◽

First Time

AbstractThe genus Santolina is a taxonomically complex group of plant species widely distributed in the Mediterranean flora and used in traditional medicine since ancient times for their biological properties, including antimicrobial, anti-inflammatory, antispasmodic, digestive, and analgesic activities. Phytochemical investigations of Santolina species have revealed the presence of terpenoids as the main bioactive constituents of the genus. Coumarins and flavonoids were also identified. This review deals, for the first time, with information on the traditional uses, chemical profile, and biological properties of plants of the genus Santolina in order to provide input for future research prospects.

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

Molecules ◽

10.3390/molecules25204646 ◽

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.

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Synthesis and Biological Evaluation of New Hydrazone Derivatives of Quinoline and Their Cu(II) and Zn(II) Complexes againstMycobacterium tuberculosis

Bioinorganic Chemistry and Applications ◽

10.1155/2015/153015 ◽

2015 ◽

Vol 2015 ◽

pp. 1-14 ◽

Cited By ~ 18

Author(s):

Mustapha C. Mandewale ◽

Bapu Thorat ◽

Dnyaneshwar Shelke ◽

Ramesh Yamgar

Keyword(s):

Mycobacterium Tuberculosis ◽

Metal Complexes ◽

Inhibitory Activity ◽

Biological Properties ◽

Biological Evaluation ◽

Fluorescence Properties ◽

Synthesis And Biological Evaluation ◽

Derivatives Of

A new series of quinoline hydrazone derivatives and their metal complexes have been synthesized and their biological properties have been evaluated againstMycobacterium tuberculosis(H37 RV strain). Most of the newly synthesized compounds displayed 100% inhibitory activity at a concentration of 6.25–25 μg/mL, againstMycobacterium tuberculosis. Fluorescence properties of all the synthesized compounds have been studied.

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Characterization of Andean Blueberry in Bioactive Compounds, Evaluation of Biological Properties and in vitro Bioaccessibility

10.20944/preprints202009.0055.v1 ◽

2020 ◽

Author(s):

Nieves Baenas ◽

Jenny Ruales ◽

Diego A. Moreno ◽

Daniel Alejandro Barrio ◽

Carla M. Stinco ◽

...

Keyword(s):

Antioxidant Capacity ◽

Bioactive Compounds ◽

Biological Activities ◽

In Vitro Digestion ◽

Biological Properties ◽

Wide Range ◽

Zebrafish Embryogenesis

Andean blueberries are wild berries grown and consumed in Ecuador which contain high values of bioactive compounds, mainly anthocyanins, with powerful antioxidant activity. The aim of this study was to evaluate the profile and contents of (poly)phenols and carotenoids in Andean blueberry by HPLC-DAD-MSn and determine a wide range of its biological activities. The antioxidant capacity of this fruit was evaluated in vitro by three different methods and in vivo using the zebrafish animal model, also the toxicity effect was determined by the zebrafish embryogenesis test. Besides, the antimicrobial activity and the capacity of Andean blueberry to produce hemagglutination in blood cells were evaluated. Finally, the bioaccessibility of (poly)phenols and related antioxidant capacity were determined in the different phases of an in vitro digestion. The global results indicated no toxicity of Andean blueberry, weakly bacteriostatic activity, and high contents of anthocyanins and antioxidant capacity, which were partially bioaccesible in vitro (~ 50 % at the final intestinal step), contributing to the knowledge of its health benefits for consumers and its potential use in the food and pharmaceutical industry as functional ingredient.

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An Overview of Bioactive 1,3-Oxazole-Containing Alkaloids from Marine Organisms

Pharmaceuticals ◽

10.3390/ph14121274 ◽

2021 ◽

Vol 14 (12) ◽

pp. 1274

Author(s):

Jinyun Chen ◽

Sunyan Lv ◽

Jia Liu ◽

Yanlei Yu ◽

Hong Wang ◽

...

Keyword(s):

Nitrogen Atom ◽

Chemical Synthesis ◽

Biological Activities ◽

Structural Features ◽

Biological Properties ◽

Therapeutic Agents ◽

Marine Organisms ◽

Chemical Structures ◽

First Time ◽

Oxazole Derivatives

1,3-Oxazole chemicals are a unique class of five-membered monocyclic heteroarenes, containing a nitrogen atom and an oxygen. These alkaloids have attracted extensive attention from medicinal chemists and pharmacologists owing to their diverse arrays of chemical structures and biological activities, and a series of 1,3-oxazole derivatives has been developed into therapeutic agents (e.g., almoxatone, befloxatone, cabotegravir, delpazolid, fenpipalone, haloxazolam, inavolisib). A growing amount of evidence indicates that marine organisms are one of important sources of 1,3-oxazole-containing alkaloids. To improve our knowledge regarding these marine-derived substances, as many as 285 compounds are summarized in this review, which, for the first time, highlights their sources, structural features and biological properties, as well as their biosynthesis and chemical synthesis. Perspective for the future discovery of new 1,3-oxazole compounds from marine organisms is also provided.

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Phytochemical Profile and Biological Properties of Colchicum triphyllum (Meadow Saffron)

Foods ◽

10.3390/foods9040457 ◽

2020 ◽

Vol 9 (4) ◽

pp. 457 ◽

Cited By ~ 3

Author(s):

Biancamaria Senizza ◽

Gabriele Rocchetti ◽

Murat Ali Okur ◽

Gokhan Zengin ◽

Evren Yıldıztugay ◽

...

Keyword(s):

High Performance ◽

Biological Activities ◽

Reducing Power ◽

Extraction Methods ◽

Biological Properties ◽

Leaf Extracts ◽

Antioxidant Power ◽

Phytochemical Profile ◽

First Time

In this work, the phytochemical profile and the biological properties of Colchicum triphyllum (an unexplored Turkish cultivar belonging to Colchicaceae) have been comprehensively investigated for the first time. Herein, we focused on the evaluation of the in vitro antioxidant and enzyme inhibitory effects of flower, tuber, and leaf extracts, obtained using different extraction methods, namely maceration (both aqueous and methanolic), infusion, and Soxhlet. Besides, the complete phenolic and alkaloid untargeted metabolomic profiling of the different extracts was investigated. In this regard, ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) allowed us to putatively annotate 285 compounds when considering the different matrix extracts, including mainly alkaloids, flavonoids, lignans, phenolic acids, and tyrosol equivalents. The most abundant polyphenols were flavonoids (119 compounds), while colchicine, demecolcine, and lumicolchicine isomers were some of the most widespread alkaloids in each extract analyzed. In addition, our findings showed that C. triphyllum tuber extracts were a superior source of both total alkaloids and total polyphenols, being on average 2.89 and 10.41 mg/g, respectively. Multivariate statistics following metabolomics allowed for the detection of those compounds most affected by the different extraction methods. Overall, C. triphyllum leaf extracts showed a strong in vitro antioxidant capacity, in terms of cupric reducing antioxidant power (CUPRAC; on average 96.45 mg Trolox Equivalents (TE)/g) and ferric reducing antioxidant power (FRAP) reducing power (on average 66.86 mg TE/g). Interestingly, each C. triphyllum methanolic extract analyzed (i.e., from tuber, leaf, and flower) was active against the tyrosinase in terms of inhibition, recording the higher values for methanolic macerated leaves (i.e., 125.78 mg kojic acid equivalent (KAE)/g). On the other hand, moderate inhibitory activities were observed against AChE and α-amylase. Strong correlations (p < 0.01) were also observed between the phytochemical profiles and the biological activities determined. Therefore, our findings highlighted, for the first time, the potential of C. triphhyllum extracts in food and pharmaceutical applications.

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Phytochemical Characterization and Biological Evaluation of the Aqueous and Supercritical Fluid Extracts from Salvia sclareoides Brot

Open Chemistry ◽

10.1515/chem-2017-0011 ◽

2017 ◽

Vol 15 (1) ◽

pp. 82-91

Author(s):

Daniela Batista ◽

Pedro L. Falé ◽

Maria L. Serralheiro ◽

Maria-Eduarda Araújo ◽

Catarina Dias ◽

...

Keyword(s):

Linoleic Acid ◽

Supercritical Fluid ◽

Antioxidant Properties ◽

Biological Properties ◽

Biological Evaluation ◽

Cyclooxygenase 1 ◽

Wide Range ◽

Anti Inflammatory ◽

Β Carotene

AbstractPlants belonging to the genus Salvia (Lamiaceae) are known to have a wide range of biological properties. In this work, extracts obtained from the aerial parts of Salvia sclareoides Brot. were evaluated to investigate their chemical composition, toxicity, bioactivity, and stability under in vitro gastrointestinal conditions. The composition of the supercritical fluid extract was determined by GC and GC-MS, while the identification of the infusion constituents was performed by HPLC-DAD and LC-MS. The in vitro cytotoxicity of both extracts (0-2 mg/mL) was evaluated in Caco-2 cell lines by the MTT assay. The anti-inflammatory and anticholinesterase activities were determined through the inhibition of cyclooxygenase-1 and acetylcholinesterase enzymes, while β-carotene/linoleic acid bleaching test and the DPPH assays were used to evaluate the antioxidant activity. The infusion inhibited cyclooxygenase-1 (IC50 = 271.0 μg/mL), and acetylcholinesterase (IC50 = 487.7 μg/ mL) enzymes, also demonstrated significant antioxidant properties, as evaluated by the DPPH (IC50 = 10.4 μg/mL) and β-carotene/linoleic acid (IC50 = 30.0 μg/mL) assays. No remarkable alterations in the composition or in the bioactivities of the infusion were observed after in vitro digestion, which supports the potential of S. sclareoides as a source of bioactive ingredients with neuroprotective, anti-inflammatory and antioxidant properties.

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