scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

2020 ◽  
Vol 11 (4) ◽  
pp. 6262-6267
Author(s):  
Krishnamoorthy Meenakumari ◽  
Giridharan Bupesh ◽  
Mayur Mausoom Phukan

The foods from plants were known to ensure against degenerative diseases and maturing because of their antioxidant activitycredited to their high content. Information on antioxidant activity of Indian medicinal plant is abundant. To the best of our knowledge, biological properties have not been accounted in the literature for this species of . As a point, this is the first results to assess the anti-oxidant activity of the plant which belongs to the family . The antioxidant activity of Methanol, , Ethyl acetate and Aqueous extracts of E. was determined using the DPPH free radical scavenging activity, ABTS radical scavenging activity and reducing power assay. The DPPH scavenging activity showed higher activity observed in extract (63%) of E. than (54%), (44%) and aqueous (30%). the ABTS assay inhibition in extract (58%) than (43%), (38%) and aqueous (32%) extracts. The reducing power assay of different extracts was increased in extract (54%) than (40%), (34%) and aqueous (28%) extracts. Overall, the and ethyl acetate extract had higher antioxidant properties than other extract. However, in this study, extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.


2020 ◽  
Vol 2 (3) ◽  
pp. 653-662
Author(s):  
Rokiman Letsara ◽  
Rigobert Andrianantenaina ◽  
Gédéon Ngiala Bongo ◽  
Colette Masengo Ashande ◽  
Mahendra Ilmi S Matondang ◽  
...  

The World Health Organization reported that at least 80% of populations rely on traditional medicine and medicinal plants for their primary health care. Due to their phytochemical compounds, the plants of the Aloe genus are reported to have high potential antiCovid-19 (and antioxidant properties. The aim of this study is to evaluate the in vitro antioxidant activity of some Malagasy endangered species of Aloe genus. The ethanolic extract of few Aloe of Madagascar leaf extracts was fractionated by liquid-liquid partition using hexane. In total 18 different fractions from 9 species have been used to determine their antioxidant activity through in vitro model by using 2,2-Diphenyl-1-picrylhydrazyl (DPPH) assay. Both hexanic extract and aqueous extract displayed antioxidant activities in four species. The most evident antioxidant activity was expressed by A. helenae.


2020 ◽  
Vol 103 (2) ◽  
pp. 422-427
Author(s):  
Agata Święciło ◽  
Kamila Rybczyńska-Tkaczyk

Abstract Background: In addition to nutrients, plant raw materials for food production should also contain substances with beneficial biological properties, which unquestionably include antioxidant compounds. Among the numerous methods of determining the antioxidant properties of samples of plant material, biological methods that provide information about not only the in vivo antioxidant potential of samples but also their metabolism and bioavailability are increasingly valued. Objective: The aim of the study was to assess the antioxidant properties of extracts from large cranberry (Vaccinium macrocarpon) obtained from different producers. Methods: Biologically active compounds were extracted from cranberry fruits using water alone and ethyl alcohol–water in proportions of 1+1 and 4+1 (v/v) as solvents. The following were determined in the extracts: content of phenolic compounds and anthocyanins, total antioxidant capacity based on reduction of the ABTS+• [2,20-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid)] radical cation, and antioxidant properties as reflected by the growth of a Saccharomyces cerevisiae Δsod1 mutant in a liquid hypertonic environment. The growth parameters of this Δsod1 mutant, monitored by a method exploiting a color reaction with resazurin, reflected the antioxidant properties of the extracts. Results: The ethanol–water cranberry extracts showed higher content of polyphenols, anthocyanins, and total antioxidants expressed as Trolox equivalent, determined on the basis of ABTS+• reduction. Conclusions: The antioxidant properties determined by the bioassay did not respond strongly to the data obtained in the in vitro chemical and biochemical assays, because they were more closely associated with the batch of fruit than with the type of solvent used to extract phytochemicals.


2017 ◽  
Vol 15 (1) ◽  
pp. 82-91
Author(s):  
Daniela Batista ◽  
Pedro L. Falé ◽  
Maria L. Serralheiro ◽  
Maria-Eduarda Araújo ◽  
Catarina Dias ◽  
...  

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.


Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1090
Author(s):  
Ramona Figat ◽  
Anita Śliwińska ◽  
Anna Stochmal ◽  
Agata Soluch ◽  
Magdalena Sobczak ◽  
...  

Traditional medicinal plants are an important source of active compounds with potential antimutagenic activity. Polyscias filicifolia Bailey (Araliaceae) is a South Asian traditional herb used as an adaptogenic and cardiac drug. Extracts of P. filicifolia contain a wide range of biologically active compounds like phenolic acids and triterpenoid saponins. In the present study. antigenotoxic potential of three naturally occurring phenolic acids and extracts of P. filicifolia growing in vitro with the addition of elicitors was evaluated against direct (4-nitroquinoline-N-oxide (4NQO) and mitomycin C (MMC)) and indirect mutagens (2-aminoanthracene (2AA)). The evaluation was made using a bacterial umu-test. Moreover, the ability to prevent photogenotoxicity induced by chlorpromazine (CPZ) under UVA irradiation was measured. The phytochemical profiling of examined extracts revealed the presence of numerous compounds with the prevelance of chlorogenic, caffeic, and ferulic acid derivatives; however, saponin fractions were also determined. The antioxidant potential of extracts strictly correlated with their composition. The tested extracts exhibited high antigenotoxic activity if the assay was performed with 2AA and metabolic activation. Moreover, the extracts slightly decreased the MMC-induced genotoxicity. However, an increase of the genotoxic effect was observed in the assay performed with 4NQO. In addition, photo-antigenotoxic activity was observed. In our study, phenolic acids exhibited lower activity than the extracts.


2021 ◽  
Vol 37 (3) ◽  
pp. 3-10
Author(s):  
L.I. Nikolaeva

Bifidobacteria occupy a special place among various representatives of normal human microbiota. A wide range of probiotic preparations has been obtained based on cultivated strains of various bifidobacteria of the intestinal microbiota. A number of scientific publications noted the immunomodulatory, anticarcinogenic, and antiviral properties of bifidobacteria in vitro and in vivo. Recently, progress has been made in the research and application of this group of microorganisms in genetic engineering. It was established that vaccines against viral and bacterial infections and antitumor substances can be developed on the basis of various strains of bifidobacteria. Bifidobacteria can also be used as adjuvants for other vaccines, as well as delivery systems for biologically active substances to tumors. The prospects for the use of bifidobacteria for the development of recombinant vaccines are discussed. bifidobacteria, medical and biological properties, recombinant vaccines, drug delivery, adjuvants, plasmids This work was funded by the Epidemiology and Microbiology National Research Center. The authors are grateful to V. V. Kuprianov for valuable comments on the text of the review.


Antioxidants ◽  
2019 ◽  
Vol 8 (6) ◽  
pp. 197 ◽  
Author(s):  
Guadalupe Firpo ◽  
María L. Ramírez ◽  
Martín S. Faillace ◽  
Maria dos R. Mendes de Brito ◽  
Ana P. S. Correia Lima e Silva ◽  
...  

The growing interest in the chemistry of unsaturated ring-fused 1,3-heterocycles, in this particular case 1,3-oxazines, arise in part from their versatile pharmacological applications. In the present article, the evaluation of the in vitro and ex vivo antioxidant activity of two cyclohexene-fused oxazines is discussed. The in vitro antioxidant activity was evaluated by trapping the ABTS and hydroxyl radicals as well as the inhibition of the enzyme acetyl-cholinesterase and hemolysis of erythrocytes by 2,2’-Azobis(2-amidinopropane) dihydrochloride (AAPH). The results suggest that both unsaturated 1,3-oxazines are auspicious sources of biologically active compounds with good antioxidant properties. In addition, a comprehensive analysis of the interaction between these heterocycles with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radicals, as well as the measurements of redox potential, provided evidence for a mechanism of antioxidant activity that takes place through electron transfer (ET) processes.


Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 89
Author(s):  
Chiara Lambruschini ◽  
Ilaria Demori ◽  
Zeinab El Rashed ◽  
Leila Rovegno ◽  
Elena Canessa ◽  
...  

The Ugi four-component reaction employing naturally occurred ferulic acid (FA) is proposed as a convenient method to synthesize feruloyl tertiary amides. Applying this strategy, a peptoid-like derivative of ferulic acid (FEF77) containing 2 additional hydroxy-substituted aryl groups, has been synthesized. The influence of the configuration of the double bond of ferulic acid and feruloyl amide on the antioxidant activity has been investigated thanks to light-mediated isomerization studies. At the cellular level, both FA, trans and cis isomers of FEF77 were able to protect human endothelial cord vein (HECV) cells from the oxidative damage induced by exposure to hydrogen peroxide, as measured by cell viability and ROS production assays. Moreover, in steatotic FaO rat hepatoma cells, an in vitro model resembling non-alcoholic fatty liver disease (NAFLD), the molecules exhibited a lipid-lowering effect, which, along with the antioxidant properties, points to consider feruloyl amides for further investigations in a therapeutic perspective.


2021 ◽  
Vol 17 (5) ◽  
pp. 43-52
Author(s):  
A. A. Skhalyakhov ◽  
Kh. R. Siyukhov ◽  
Z. T. Tazova ◽  
L. V. Lunina

In the last decade the attitude of socially active people to their own health has changed significantly. The desire to lead a healthy lifestyle forms consumers’ demand for proper balanced nutrition, products enriched with natural biologically active substances of unconventional plant materials, systematic consumption of which can not only reduce the risk of alimentary diseases, but also protect a person from oxidative stress, which is the predecessor of many serious illnesses. Among the wide range of chemical compounds that make up plant materials, a special place is occupied by compounds of antioxidant action, such as flavonoids, phenol carboxylic acids, vitamins C and E. The aim of the research was to study the qualitative composition and quantitative content of natural antioxidants in some types of medicinal and technical plant materials of the Republic of Adygea to determine the possibility of their use in the production of functional food products. The content of biologically active compounds that determine the antioxidant properties of plant materials was determined using «Kapel 105 «M» capillary electrophoresis system and JASCO 875-UV liquid chromatograph. Antioxidant activity was measured by the amperometric method with Tsvet Yauza-01-AA analyzer. According to the results of the research, it has been found that Echinacea purpurea herb (1,09 g / dm3) and walnut leaves (0,96 g / dm3) exhibit a high antioxidant activity (in terms of gallic acid), which is due to the high concentration of natural antioxidants of the phenolic type. Due to these properties this plant raw materials can be used as enriching ingredients for the production of various groups of food products for functional purposes.


2019 ◽  
Vol 5 (4) ◽  
pp. 270-277 ◽  
Author(s):  
Vijay Kumar ◽  
Simranjeet Singh ◽  
Ragini Bhadouria ◽  
Ravindra Singh ◽  
Om Prakash

Holoptelea integrifolia Roxb. Planch (HI) has been used to treat various ailments including obesity, osteoarthritis, arthritis, inflammation, anemia, diabetes etc. To review the major phytochemicals and medicinal properties of HI, exhaustive bibliographic research was designed by means of various scientific search engines and databases. Only 12 phytochemicals have been reported including biologically active compounds like betulin, betulinic acid, epifriedlin, octacosanol, Friedlin, Holoptelin-A and Holoptelin-B. Analytical methods including the Thin Layer Chromatography (TLC), High-Performance Thin Layer Chromatography (HPTLC), High-Performance Liquid Chromatography (HPLC) and Liquid Chromatography With Mass Spectral (LC-MS) analysis have been used to analyze the HI. From medicinal potency point of view, these phytochemicals have a wide range of pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, and anti-tumor. In the current review, it has been noticed that the mechanism of action of HI with biomolecules has not been fully explored. Pharmacology and toxicological studies are very few. This seems a huge literature gap to be fulfilled through the detailed in-vivo and in-vitro studies.


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