Antioxidant and ROS inhibitory activities of heterocyclic 2-Aryl-4(3H)-quinazolinone derivatives

Author(s):  
Shahida Perveen ◽  
Syed Muhammad Saad ◽  
Khalid Mohammed Khan ◽  
Muhammad Iqbal Choudhary

Background: Antioxidants are small molecules that prevent or delay the process of oxidations caused by highly reactive free radicals. These molecules are known for their ability to protect various cellular architecture and other biomolecules from oxidative stress and free radicals. Thus, antioxidants play a key role in the prevention of oxidative damages caused by highly reactive free radicals. Method: In the present study, a series of previously synthesized heterocyclic 2-aryl-4(3H)-quinazolinone derivatives 1-25 was screened for antioxidant activity by employing in vitro DPPH and superoxide anion radical scavenging activities. ROS inhibitory activities were also evaluated by serum-opsonized zymosan activated whole blood phagocytes and isolated neutrophils. Cytotoxicity studies were carried out by employing an MTT assay against the 3T3 cell line. Results: Most of the 2-aryl-4(3H)-quinazolinone derivatives showed potent antioxidant activities in superoxide anion radical scavenging assay with IC50 value ranging between 0.57 µM – 48.93 µM, as compared to positive control quercetin dihydrate (IC50 = 94.1± 1.1 µM ). Compounds 5, 6, and 14 showed excellent activity in DPPH assay. Compounds 5-8, 12-15, 17, and 20 showed promising activities in the ROS inhibition assay. All compounds were found to be non-cytotoxic against the 3T3 cell line. Structure antioxidant activity has been established. Conclusion: It can be concluded that most of the heterocyclic 2-aryl-4(3H)-quinazolinone derivatives 1-25 are identified as promising antioxidant agents that are capable of fighting against free radicals and oxidative stress. Thus, they can serve as a lead towards treating oxidative stress and related pathologies.

2014 ◽  
Vol 12 (3) ◽  
pp. 377-385 ◽  
Author(s):  
Vesna Šaponjac ◽  
Dragana Četojević-Simin ◽  
Gordana Ćetković ◽  
Jasna Čanadanović-Brunet ◽  
Sonja Djilas ◽  
...  

AbstractGround spice paprika was extracted with hexane, by conventional Soxhlet procedure (SX oleoresin), and with supercritical carbon dioxide at three different pressures — 20, 30 and 40 MPa (SF20, SF30 and SF40 oleoresins). The effect of extraction method and conditions on the colour intesity of paprika oleoresins, content of α-tocopherol, as well as antioxidant and antiproliferative activity was examined. Hexane showed highest selectivity for paprika pigments (886.02 ASTA), while α-tocopherol showed highest solubility (3846.9 mg kg−1) in supercritical carbon dioxide at 20 MPa. All paprika oleoresins exhibited good superoxide anion radical scavenging activity SF30 being the best superoxide anion radical scavenger. Cell growth activity was evaluated in vitro in human cell lines:cervix epitheloid carcinoma (HeLa), breast adenocarcinoma (MCF7) and colon adenocarcinoma (HT-29). The highest antiproliferative activity was exhibited by SX in MCF7 cell line (IC50=14.28 mg mL−1). Extract SF40 produced significant and selective antiproliferative action towards HeLa cell line. These results suggest that paprika oleoresins, due to high antiradical and tumor cell-inhibiting activity, can be regarded as functional food ingredients.


2013 ◽  
Vol 781-784 ◽  
pp. 1138-1143
Author(s):  
Feng Qiu Wen ◽  
Lang Sheng Pan ◽  
Lei Lei

La (III) complex with apigenin was synthesized and characterized by UV, IR, 1HNMR and thermal analysis. The scavenging activity of the complex on superoxide anion radical (O2-·) and hdroxyl radical (·OH) was also investigated by improved pyrogallic acid way and ortho-oxybenzoic acid way. The results show that the complex had remarkable scavenging effects on O2-· and ·OH, and its scavenging effect on free radicals was better than apigenin.


2013 ◽  
Vol 634-638 ◽  
pp. 1423-1428 ◽  
Author(s):  
Yan Song ◽  
Guo Ping Yu ◽  
Chao Ran Dou ◽  
Hao Wu ◽  
Zhu Gong

The aim of the work was to research antioxidant activity of the anthoyanins extracts of black soybean. The whole soybean through defatted, were to determine the phenolic and anthocyanin contents in black soybean extracts and to examine antioxidant activity of extract against DPPH and ABTS assays, and Ferric Reducing Antioxidant Power (FRAP), and superoxide anion radical scavenging activity. The defatted sample was extracted using ethanol by ultrasonic. The optimum DPPH and ABTS radical scavenging capacity (%) were 68.34% and 70.12%, VC was 59.76% and 95.23%, respectively, and contains high levels of reducing power and superoxide anion radical scavenging activity. The present results indicate that the anthoyanins extract from black soybean has greater anti-oxidative and is useful in functional food and other applications.


2013 ◽  
Vol 807-809 ◽  
pp. 1984-1987 ◽  
Author(s):  
Qin Li ◽  
Chi Zhang

In this article,Cordyceps militaris,that from Hubei and Yunnan,were used as the research objects, to extract seleno-polysaccharide ,then the antioxidant activity of seleno-polysaccharide were determined by reducing power,the scavenging capacity on superoxide anion radical and hydroxyl radical.The results indicated that,the content of selenium in Hubei and Yunnan Cordyceps militaris samples were 210.0μg/g and 57.5μg/g,respectively;the share of Se-polysaccharide in total selenium were 11.086% and 26.713%,respectively,lower degree to turn the selenium organic in Hubei Cordyceps militaris.The reducing power of seleno-polysaccharide from Hubei and Yunnan Cordyceps militaris were 0.0253,0.0297,respectively;two kinds of Cordyceps militaris have certain ability to remove superoxide anion radical and different between them,the seleno-polysaccharide of Yunnan Cordyceps militaris has a better effect to remove superoxide anion radical under different sample amount.About hydroxyl radical,there were no ability to remove it.


2012 ◽  
Vol 583 ◽  
pp. 244-247
Author(s):  
Yong Guang Bi ◽  
Chun Chun Liu

By using spectrophotometric detection of the Chuanxiong polysaccharides on the free radical scavenging. The results show that the Chuanxiong polysaccharides on DPPH radical, hydroxyl radical (HO•) and superoxide anion radical (•) clearance. Scavenging ability with the the Chuanxiong polysaccharide concentration increased, and showed the dose-effect relationship. Concentration of 2.0mg/mL when DPPH radicals clear the rate of 35.61%, while the rate of hydroxyl radicals and superoxide anion radical scavenging, clear the rate of 57.78% and 57.14%. Chuanxiong polysaccharide is an ideal natural antioxidants and good prospects for the development of biomedical composites.


IUBMB Life ◽  
1997 ◽  
Vol 42 (1) ◽  
pp. 35-44 ◽  
Author(s):  
Yasuko Noda ◽  
Akitane Mori ◽  
Lester Packer ◽  
Kazunori Anzai ◽  
Masahiro Kohno ◽  
...  

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