Synthesis, Antioxidant and Antitumor Activity of Some Substituted 9-Anilinoacridine and 4-Anilinoquinolines Derivatives

2018 ◽  
Vol 15 (6) ◽  
pp. 846-852 ◽  
Author(s):  
Fatimah A. Agili

Background: Acridine and quinoline derivatives have a wide range of biological activities such as antioxidant and antitumor where quinoline derivatives intercalate between base pairs of double-stranded DNA through π-π interactions. Therefore, the development of new compounds with antitumor activity could be an important therapeutic strategy against this metabolic syndrome. Objective: This study was undertaken to synthesize different series of new anilinoacridines and anlinoquinoline with different substituents having biological activity. Materials and Methods: A series of new anilinoacridines and anlinoquinoline with different substituents was prepared by condensation of methyl 3-amino-4-methoxybenzoate hydrochloride with 9- chloroacridine and 4- chloroquinoline to give the target derivatives. Results: New anilinoacridines and anlinoquinoline with different substituents have been synthesized as antioxidant and anti-cancer agents. The structure of the synthesized compounds was confirmed by using spectral methods (FT-IR, 1H-NMR). The antioxidant activity of the synthesized compounds was evaluated by using DPPH radical scavenging ability. Also, the anti-cancer activity was evaluated using lung carcinoma, breast adenocarcinoma and liver carcinoma. The developed compounds 4a, b, 5a,b, 7a,b and 8a,b have shown a potent antioxidant activity. On the other hand, 4a, b, 5a and 7a exhibited the best antitumor activity against both A-549 and MCF7 cancer cells. Conclusion: For the active developed compounds, the most active antioxidant and antitumor one was 4a which registered the highest radical scavenging as well as antitumor activity.

2009 ◽  
Vol 4 (5) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Aneta Wojdyłto ◽  
Jan Oszmiański

Fruits are one of the most important sources of phenolic compounds in our diet. Many of these compounds exhibit a wide range of biological activities, especially antioxidant activity. The objective of this study was to determine the composition and antioxidant activity of phenolic compounds found in fruit juice obtained from buckthorn, flowering quince, rowanberry and hawthorn. Hydroxycinnamic acids (neochlorogenic and chlorogenic acid) and procyanidins were the main phenolics in rowanberry juice. The highest level of flavonols (quercetin derivatives) was found in sea buckthorn. All juices showed strong free-radical scavenging activity against ABTS•+ radicals and ferric reducing ability measured by the FRAP method. The strongest antioxidant activity was found in rowanberry juice, but the lowest was measured in hawthorn and sea buckthorn juices.


Author(s):  
Rukhsana Tabassum ◽  
Muhammad Ashfaq ◽  
Hiroyuki Oku

Abstract:: Quinoline derivatives are considered as broad spectrum pharmacological compounds that exhibit wide range of biological activities. Integration of quinoline moiety can improve its physical and chemical properties and also pharmacological behavior. Due to its wide range of pharmaceutical applications it is very popular compound to design new drugs for treatment of multiple diseases like cancer, dengue fever, malaria, tuberculosis, fungal infections, AIDS, Alzheimer’s disease and diabetes . In this review our major focus is to pay attention on biological activities of quinoline compounds in treatment of these diseases such as, anti-viral, anti-cancer, anti-malarial, anti-bacterial, anti-fungal, anti-tubercular and anti-diabetic.


Author(s):  
SAMRAJ RATTANADILOK NA PHUKET ◽  
TITIMA SANGKAEW ◽  
PIYATIDA CHANAPAN ◽  
SURACHAI TECHAOEI

Objective: The objective of this research was to determine the antioxidant of ß-glucans from an edible mushroom, Schizophyllum commune in Thailand.Methods: The antioxidant activity of ß-glucans was measured in terms of hydrogen donating or radical scavenging ability by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) method,2,2´-azinobis-(3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity analysis, and total phenoliccompounds. The ß-glucans structure was analyzed using Fourier-transform infrared spectrophotometer.Results: The ß-glucans were extracted from S. commune and tested biological activities. Using the Folin–Ciocalteu Reactive method, we found thatthe phenolic compound contents of ethanol extracts of the mushroom sample were 284.41±1.22 mgGAE/g extract. The IC50 radical scavenging ability(DPPH) and IC50 radical scavenging activity (ABTS) of ß-glucans were 0.829±0.006 and 0.724±0.021 mg/mL, respectively.Conclusion: The ß-glucans from S. commune in Thailand showed a potent antioxidant activity and it will be able to apply in pharmaceutical cosmetics.


2020 ◽  
Vol 32 (9) ◽  
pp. 2125-2129
Author(s):  
RAMARAJAN RAJALAKSHMI ◽  
RAJAVEL SANTHI ◽  
THANGARAJ ELAKKIYA

A series of new 4-thiazolidinone derivatives of 2-(4-chlorophenyl)-3-(6-(thiophen-2-yl)-4-p-tolyl-4H-1,3-oxazin-2-yl)- thiazolidin-4-one (7h-m) are synthesized because of its wide range of biological activities.1H & 13C NMR, IR studies were applied for the elucidation of all the synthesized compounds. All the synthesized compounds have been tested for antidiabetic and antioxidant activity in vitro method against standard. The analogs 7h-m was evaluated for α-amylase and α-glucosidase inhibitory potential. The structures of all the compounds have been screened for antioxidant activity using DPPH radical scavenging assay, NO scavenging method. Molecular docking studies were accomplished in addition to understand the binding affinity of those compounds with PDBID 2HR7 which showed that the synthesized derivatives bind in the lively binding site of the target protein


Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1608
Author(s):  
Stephen Lo ◽  
Euphemia Leung ◽  
Bruno Fedrizzi ◽  
David Barker

Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5-O-acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines; and their radical scavenging activity against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.


Coatings ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 604
Author(s):  
Liyan Wang ◽  
Liang Lei ◽  
Kang Wan ◽  
Yuan Fu ◽  
Hewen Hu

Active films based on carboxymethyl chitosan incorporated corn peptide were developed, and the effect of the concentration of corn peptide on films was evaluated. Physicochemical properties of the films, including thickness, opacity, moisture content, color, mechanical properties, water vapor permeability, and oil resistance, were measured. Biological activities of the films, including the antioxidant and antibacterial activities, were characterized in terms of 2, 2-diphenyl-1-picrylhydrazyl free radical scavenging activity, reducing power, the total antioxidant activity, and the filter disc inhibition zone method. The results indicated that the incorporation of corn peptide caused interactions between carboxymethyl chitosan and corn peptide in Maillard reaction and gave rise to the films light yellow appearance. Compared with the Control, the degree of glycosylation, browning intensity, thickness, opacity, tensile strength, antioxidant activity, and antibacterial activity of films were increased, but the elongation, vapor permeability, and oil resistance of films were decreased. The films based on corn peptide and carboxymethyl chitosan can potentially be applied to food packaging.


Marine Drugs ◽  
2021 ◽  
Vol 19 (5) ◽  
pp. 240
Author(s):  
Tatyana A. Pounina ◽  
Tatyana A. Gloriozova ◽  
Nick Savidov ◽  
Valery M. Dembitsky

The review focuses on sulfated steroids that have been isolated from seaweeds, marine sponges, soft corals, ascidians, starfish, and other marine invertebrates. Sulfur-containing steroids and triterpenoids are sourced from sedentary marine coelenterates, plants, marine sediments, crude oil, and other geological deposits. The review presents the pharmacological profile of sulfated steroids, sulfur-containing steroids, and triterpenoids, which is based on data obtained using the PASS program. In addition, several semi-synthetic and synthetic epithio steroids, which represent a rare group of bioactive lipids that have not yet been found in nature, but possess a high level of antitumor activity, were included in this review for the comparative pharmacological characterization of this class of compounds. About 140 steroids and triterpenoids are presented in this review, which demonstrate a wide range of biological activities. Therefore, out of 71 sulfated steroids, thirteen show strong antitumor activity with a confidence level of more than 90%, out of 50 sulfur-containing steroids, only four show strong antitumor activity with a confidence level of more than 93%, and out of eighteen epithio steroids, thirteen steroids show strong antitumor activity with a confidence level of 91% to 97.4%.


2009 ◽  
Vol 2009 ◽  
pp. 1-6 ◽  
Author(s):  
K. Nagendra Prasad ◽  
Jing Hao ◽  
Chun Yi ◽  
Dandan Zhang ◽  
Shengxiang Qiu ◽  
...  

Antioxidant activities of wampee peel extracts using five different solvents (ethanol, hexane, ethyl acetate, butanol and water) were determined by using in-vitro antioxidant models including total antioxidant capability, 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity, reducing power, and superoxide scavenging activity. Ethyl acetate fraction (EAF) exhibited the highest antioxidant activity compared to other fractions, even higher than synthetic antioxidant butylated hydroxyl toluene (BHT). In addition, the EAF exhibited strong anticancer activities against human gastric carcinoma (SGC-7901), human hepatocellular liver carcinoma (HepG-2) and human lung adenocarcinoma (A-549) cancer cell lines, higher than cisplatin, a conventional anticancer drug. The total phenolic content of wampee fraction was positively correlated with the antioxidant activity. This is the first report on the antioxidant and anticancer activities of the wampee peel extract. Thus, wampee peel can be used potentially as a readily accessible source of natural antioxidants and a possible pharmaceutical supplement.


Author(s):  
Ade Chandra Iwansyah ◽  
Rizal M. Damanik ◽  
Lilik Kustiyah ◽  
Muhammad Hanafi

<p><strong>Objective: </strong>The objectives of this research were to evaluate and compare the antioxidant activity; phenolics and flavonoids contents; and chemical composition of some galactopoietic herbs used in Indonesia and to find a possible relationship between antioxidant activity; phenolics, flavonoids and chemical composition of these plants.</p><p><strong>Methods: </strong>A wide range of analytical parameters was studied, including yield; pH; water activity (a<sub>w</sub>); total color difference; phenolics and flavonoids content; moisture; ash; protein; fat; carbohydrate; fiber; calcium; zinc; magnesium; potassium; iron content; and the data were analyzed by partial least squares (PLS) regression analysis and principal component analysis (PCA) to evaluate the correlation between the parameters and classification of the plants. Folin–cioceltaeu assay, aluminum chloride assay and DPPH scavenging assay were used to evaluate of total phenolics content and free radical scavenging activity of the ethanolic extract of galactopoietic herbs.</p><p><strong>Results: </strong>All of the galactagogue herbs, <em>viz</em>. <em>Plectranthus amboinicus </em>(Lour.) (PA), <em>Sauropus androgynus</em> (SA), <em>Moringa oleifera</em> (MO), and <em>Carica papaya</em> leaves (CP) exhibited good results of TPC, TFC and antioxidant activity. MO contained the highest average of total phenolics content (53.89 mg GAE/g). SA with a ratio of total flavonoids to total phenolics (TF/TP) which is 1.59 contained the highest average of total flavonoids and antioxidant activity (IC<sub>50</sub>), 43.63 mg QE/g and 126.13 μg/ml, respectively, followed by MO&gt;CA&gt;PA. Based on PLS and PCA analysis, antioxidant activity correlated with fat, protein, phenolics content, flavonoids content and pH, but only the total flavonoids content correlated strongly with antioxidant activity.<strong></strong></p><p><strong>Conclusion: </strong>This provides useful data about the studied relationships and chemical patterns in some galactopoietic herbs used and provides a helpful tool for understanding much more about the interpretation of results from the experiments and the mechanism of biosynthesis in plants.</p>


2020 ◽  
Vol 8 (1) ◽  
pp. 75-81
Author(s):  
Bui Van Hoai ◽  
Ngo Dai Nghiep ◽  
Dao An Quang ◽  
Nguyen Thi Nam Phuong

Chitosan with 80% degree of deacetylation was hydrolyzed by cellulase of Trichoderma viride to prepare chitooligosaccharides (COSs) by the fractionation of the COSs with ultrafiltration membrane. The antioxidant activities of the COSs were clarified in this study by reducing power and free radical scavenging ability assay by UV-VIS absorption spectrum. The results show that the COS 1 (10,000-5,000 Da), COS 2 (5,000-3,000 Da), COS 3 (3,000-1,000 Da) and COS 4 (less than1,000 Da) segments have antioxidant properties.The antioxidant activitives of the COSs increased with the increment of concentration, and they also depended on molecular weight.


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