2-((4-((E)-1-(Hydroxyimino)ethyl)phenyl)amino)-2-oxoethyl Cinnamate

Molbank ◽  
10.3390/m1239 ◽  
2021 ◽  
Vol 2021 (3) ◽  
pp. M1239
Author(s):  
Ioanna-Chrysoula Tsopka ◽  
Dimitra Hadjipavlou-Litina

Cinnamic acid-nitric oxide (NO) donor hybrids have attracted attention, in recent years, as new pharmacological agents to treat multifactorial diseases. In the present study, hybrid oxime 5 was synthesized and its anti-lipid peroxidation and anti-lipoxygenase activities were evaluated. The new compound showed remarkable anti-LOX activity, while its antioxidant activity was quite good in comparison to the appropriate reference compounds. The examined derivative seems to be orally active in accordance to Lipinski’s rule of five. Compound 5 can be considered as a leading structure for the design and synthesis of new hybrids.

Author(s):  
Jane-Rose I. Oche ◽  
Titilayo O. Johnson ◽  
Augustina O. Akinsanmi ◽  
Kiri H. Jaryum ◽  
Timothy Francis

Aim: The aim of this study was to investigate and compare the antioxidative properties of the mistletoe plant obtained from three different host species namely Psidium guajava, Vernonia amygdalina and Moringa olifera lam. Study Design: Experimental Design Place and Duration of Study: Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences and Department of Biochemistry, College of Health Sciences, University of Jos, Nigeria. Methodology: Crude methanolic leaf extracts were studied for their antioxidative properties; Iron reducing and Iron-chelating activities, Nitric oxide (NO) radical and 2,2-diphenyl 1-picrylhydrazyl (DPPH) radical scavenging activities and the lipid peroxidation and thiobarbituric acid reaction (TBAR) methods. One way ANOVA was used for the result analysis with P<.05 for significant difference. Results: Mistletoes from Psidum guajava (MSPG) had significantly higher reducing property (0.16 – 0.20mg/mL); the chelating property of Mistletoes from Moringa olifera (MSMO) was significantly lower (45.7 – 58.9%); DPPH radical scavenging activity had no significant difference; and Nitric oxide scavenging activity was significantly higher in MSPG (72.1% in 75mg/mL) than the extracts from other hosts. MSPG had significantly higher TBAR inhibition using both FeSO4 (77.8% at 125µg/mL) and Sodium nitroprusside (61.6+1.0% at 125µg/mL) with an IC50 of 30.27µg/mL . Extract of Tapinanthus globiferus leaves from Psidium guajava had more antioxidative activities in the TBARs followed by Tapinanthus globiferus leaf extract from Vernonia amygdalina (MSVA). Conclusion: From the study, mistletoes from Psidium guajava had higher antioxidant activity compared to other hosts, which probably justifies its use for treatment of cancer in traditional medicinal practice.


Chemistry ◽  
2020 ◽  
Vol 2 (4) ◽  
pp. 837-848
Author(s):  
Csilla Sepsey Für ◽  
Hedvig Bölcskei

The large originator pharmaceutical companies need more and more new compounds for their molecule banks, because high throughput screening (HTS) is still a widely used method to find new hits in the course of the lead discovery. In the design and synthesis of a new compound library, important points are in focus nowadays: Lipinski’s rule of five (RO5); the high Fsp3 character; the use of bioisosteric heterocycles instead of aromatic rings. With said aim in mind, we have synthesized a small compound library of new spiro[cycloalkane-pyridazinones] with 36 members. The compounds with this new scaffold may be useful in various drug discovery projects.


Biologia ◽  
2012 ◽  
Vol 67 (6) ◽  
Author(s):  
Anjuli Sood ◽  
Charu Kalra ◽  
Sunil Pabbi ◽  
Prem Uniyal

AbstractThe present investigation was carried out to decipher the interplay between paraquat (PQ) and exogenously applied nitric oxide (NO) in Azolla microphylla. The addition of PQ (8 μM) increased the activities of superoxide dismutase (SOD), catalase (CAT), guaiacol peroxidase (GPX), ascorbate peroxidase (APX) by 1.7, 2.7, 3.9 and 1.9 folds respectively than that control in the fronds of Azolla. The amount of H2O2 was also enhanced by 2.7 times in the PQ treated plants than that of control. The supplementation of sodium nitroprusside (SNP) from 8–100 μM along with PQ, suppressed the activities of antioxidative enzymes and the amount of H2O2 compared to PQ alone. The drop in the activity of antioxidative enzymes — SOD, GPX, CAT and APX was highest (39.9%, 48.4%, 41.6% and 41.3% respectively) on the supplementation of 100 μM SNP with PQ treated fronds compared to PQ alone. The addition of NO scavengers along with NO donor in PQ treated fronds neutralized the effect of exogenously supplied NO. This indicates that NO can effectively protect Azolla against PQ toxicity by quenching reactive oxygen species. However, 200 μM of SNP reversed the protective effect of lower concentration of NO donor against herbicide toxicity. Our study clearly suggests that (i) SNP released NO can work both as cytoprotective and cytotoxic in concentration dependent manner and (ii) involvement of NO in protecting Azolla against PQ toxicity.


2011 ◽  
Vol 378-379 ◽  
pp. 423-427 ◽  
Author(s):  
Hai Yan Li ◽  
Wan Zhong Zhang

Abscisic acid (ABA) and sodium nitroprusside (SNP) treatment significantly increased chilling tolerance in maize seedlings. ABA in combination with nitric oxide (NO) donor SNP further enhanced the ABA-induced chilling tolerance. But the addition of NO scavenger 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide (PTIO) nullified the increasing effect of SNP on chilling tolerance. In addition, the combination of ABA and PTIO decreased the ABA-induced chilling tolerance. Measurement of activities of superoxide dismutase (SOD) and catalase (CAT), hydrogen peroxide (H2O2) content and the level of lipid peroxidation (in terms of malondialdehyde) indicated that chilling stress induced an oxidative stress in maize seedlings. ABA treatment enabled maize seedlings to maintain higher SOD and CAT activities and lower level of H2O2 and lipid peroxidation under chilling stress. ABA in combination with SNP further enhanced the ABA-induced increase in SOD and CAT activities and lowered the chilling stress-induced lipid peroxidation in the ABA-treated seedlings. But the addition of PTIO scavenged the increasing effect of SNP. In addition, the combination of ABA and PTIO had a contrary effect with that of ABA and SNP. These results suggest that the ABA-induced chilling tolerance is mediated by NO, NO is involved in ABA-induced chilling tolerance by increasing activities of antioxidant enzymes and reduced endogenous H2O2 accumulation.


2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Mayank Gangwar ◽  
Manish Kumar Gautam ◽  
Amit Kumar Sharma ◽  
Yamini B. Tripathi ◽  
R. K. Goel ◽  
...  

Mallotus philippinensisis an important source of molecules with strong antioxidant activity widely used medicinal plant. Previous studies have highlighted their anticestodal, antibacterial, wound healing activities, and so forth. So, present investigation was designed to evaluate the total antioxidant activity and radical scavenging effect of 50% ethanol fruit glandular hair extract (MPE) and its role on Human Erythrocytes. MPE was tested for phytochemical test followed by its HPLC analysis. Standard antioxidant assays like DPPH, ABTS, hydroxyl, superoxide radical, nitric oxide, and lipid peroxidation assay were determined along with total phenolic and flavonoids content. Results showed that MPE contains the presence of various phytochemicals, with high total phenolic and flavonoid content. HPLC analysis showed the presence of rottlerin, a polyphenolic compound in a very rich quantity. MPE exhibits significant strong scavenging activity on DPPH and ABTS assay. Reducing power showed dose dependent increase in concentration absorption compared to standard, Quercetin. Superoxide, hydroxyl radical, lipid peroxidation, nitric oxide assay showed a comparable scavenging activity compared to its standard. Our finding further provides evidence thatMallotusfruit extract is a potential natural source of antioxidants which have a protective role on human Erythrocytes exhibiting minimum hemolytic activity and this justified its uses in folklore medicines.


Botany ◽  
2019 ◽  
Vol 97 (12) ◽  
pp. 681-690 ◽  
Author(s):  
Masoomeh Nabaei ◽  
Rayhaneh Amooaghaie

Nitric oxide (NO) and melatonin are two biostimulant molecules in plants that not only modulate the growth and development of plants but also confer enhanced tolerance to abiotic stresses. Therefore, in this study, the interactive effects of melatonin and nitric oxide (NO) on seedlings of Catharanthus roseus (L.) G. Don was evaluated under both control and conditions of stress due to Cd. Our results show that both melatonin and sodium nitroprusside (SNP, as an NO donor) significantly improved seedling growth, which was associated with the enhanced concentration of photosynthetic pigments in both the control plants and under Cd-stress conditions. Impacts of both melatonin and SNP were more pronounced in the Cd-stressed plants than control seedlings. The Cd stress increased H2O2 and lipid peroxidation levels in roots. Melatonin, as well as SNP, increased endogenous NO concentration in roots. Both melatonin and SNP enhanced the concentration of proline and the activities of antioxidant enzymes (SOD, POD, APX, CAT) and lowered H2O2 and lipid peroxidation levels in roots of C. roseus plants under Cd stress. These melatonin-induced responses in the roots were suppressed by 4-carboxyphenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide (cPTIO; a specific scavenger of NO), but inhibition of melatonin biosynthesis by p–chlorophenylalanine, could not reverse the protective effects conferred by NO. These outcomes suggest that NO, as a downstream signaling molecule, is implicated in the melatonin-promoted antioxidant responses in roots of C. roseus plants.


1998 ◽  
Vol 274 (1) ◽  
pp. F18-F25 ◽  
Author(s):  
Liguang Chen ◽  
Bao-Hong Zhang ◽  
David C. H. Harris

The potential role of nitric oxide (NO) in iron-induced toxicity was studied in proximal tubule cells in primary culture. NO production ([Formula: see text]/[Formula: see text]) was significantly increased in iron-treated compared with control cells (3.43 ± 0.08 vs. 1.56 ± 0.08 nmol/dish, P < 0.01). NO synthase (NOS) activity was also induced by iron treatment (16.2 ± 2.0 vs. 0.4 ± 0.2 nmol of [Formula: see text]citrulline/mg protein, P < 0.01).l-Arginine, a substrate for NOS, augmented iron-induced NO production and cell damage [lactate dehydrogenase (LDH) leakage], whereas aminoguanidine, an inhibitor of NOS, reduced iron-induced NO production and LDH leakage. Sodium nitroprusside, an exogenous NO donor, induced LDH leakage in a dose-dependent manner, but no effect on lipid peroxidation {malondialdehyde bis[dimethyl acetal] (MDA) production} was observed. Superoxide dismutase and catalase decreased iron-induced MDA production but did not affect LDH leakage or NO production. Dimethylpyrroline N-oxide and desferal prevented MDA production, LDH leakage, and NO production. We concluded that NO is one of the mediators of iron-induced toxicity in proximal tubule cells. NO-induced toxicity is not dependent on lipid peroxidation. This may explain the variable effect of different antioxidants on cell damage and lipid peroxidation in iron-induced cytotoxicity.


2019 ◽  
Vol 2019 ◽  
pp. 1-12
Author(s):  
Aline de Freitas Brito ◽  
Alexandre Sérgio Silva ◽  
Alesandra Araújo de Souza ◽  
Paula Benvindo Ferreira ◽  
Iara Leão Luna de Souza ◽  
...  

The possible mechanism is involved in the effects of Spirulina platensis on vascular reactivity. Animals were divided into sedentary group (SG) and sedentary groups supplemented with S. platensis at doses of 50 (SG50), 150 (SG150), and 500 mg/kg (SG500). To evaluate reactivity, cumulative concentration-response curves were constructed for phenylephrine and acetylcholine. To evaluate the involvement of the nitric oxide (NO) pathway, aorta tissue was preincubated with L-NAME and a new curve was then obtained for phenylephrine. Biochemical analyses were performed to evaluate nitrite levels, lipid peroxidation, and antioxidant activity. To contractile reactivity, only SG500 (pD2=5.6±0.04 vs. 6.1±0.06, 6.2±0.02, and 6.2±0.04) showed reduction in phenylephrine contractile potency. L-NAME caused a higher contractile response to phenylephrine in SG150 and SG500. To relaxation, curves for SG150 (pD2=7.0±0.08 vs. 6.4±0.06) and SG500 (pD2=7.3±0.02 vs. 6.4±0.06) were shifted to the left, more so in SG500. Nitrite was increased in SG150 and SG500. Lipid peroxidation was reduced, and oxidation inhibition was increased in all supplemented groups, indicating enhanced antioxidant activity. Chronic supplementation with S. platensis (150/500 mg/kg) caused a decrease in contractile response and increase in relaxation and nitrite levels, indicating greater NO production, due to decreased oxidative stress and increased antioxidant activity.


2017 ◽  
Vol 9 (2) ◽  
Author(s):  
Raja Sundara rajan ◽  
Ramya I

<p>Assessment of antioxidant activity was imperative in the screening of medicinal plants for potential health benefits. In present study methanol extract of <em>Polygonum glabrum</em> <em> </em>(polygonaceae) was screened for its in vitro antioxidant activity using biologically relevant methodologies which scavenge radicals such as  1,1 diphenyl 2 picryl hydrazyl (DPPH), nitric oxide, hydrogen peroxide, hydroxyl,  superoxide anion and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS). Total reducing ability by conversion of ferric (III) to ferrous (II) and molybdenum (VI) to molybdenum (V), metal ion chelating capacity and anti lipid peroxidation activities were also examined. The antioxidant ability of <em>Polygonum glabrum</em> whole plant extract was found to be in a dose dependent manner. The IC<sub>50</sub> values for scavenging of DPPH<sup>●</sup> and ABTS<sup>●+</sup> free radicals were 13.18 μg/ml and 20.46 μg/ml. For scavenging of nitric oxide, hydrogen peroxide, hydroxyl and superoxide anion radicals, the IC<sub>50</sub> values were found to be 80.22 μg/ml, 33.06 μg/ml, 52.26μg/ml and 36.98 μg/ml respectively. Further, addition of 120μg/ml of plant extract to the reaction mixture produced 50% lipid peroxidation inhibition activity. Commercial antioxidants such as vitamin E, quercetin, butylated hydroxytoluene and ascorbic acid were used as reference compounds. The strong antioxidant activity of <em>Polygonum glabrum</em> may be credited to the presence of triterpenes [beta-hydroxyfriedalanol], phenols        [3-hydroxy-5-methoxystilbene], flavonoids [pinocembrin and pinocembrin-5-methylether], steroids [sitosterol - (6-O-palmitoyl)- 3-O-β-D glucopyranoside and sitosterol-3-O-β-D glucopyranoside], sesqueterpenes [2,3-dihydroxy isodrimeninol] and pigments etc in methanol extract.</p>


2020 ◽  
Vol 12 (1) ◽  
pp. 3-8
Author(s):  
Neha Yadav ◽  
Ajay Pal ◽  
Sonam Sihag ◽  
Nagesh C.R

Background: Syzygium cumini L., commonly known as Jamun, black-plum, and Indian blackberry, is one of the most widely distributed trees in India with booming medical benefits and possesses antioxidant, anticancer and anti-diabetic properties. It belongs to the family Myrtaceae. Despite countless phytochemicals, seeds are not consumed and are the waste part of Jamun fruit. Objective: The objective of this study was to evaluate the antioxidant capacity of phenolics from Jamun seeds against a bundle of oxidant moieties. Methods: The 50% acetone extract of Jamun seeds was investigated for in-vitro antioxidant profiling. Assays include free radical scavenging activity, metal chelation activity, hydroxyl radical scavenging activity, hydrogen peroxide scavenging activity, total antioxidant activity, total reducing power, nitric oxide scavenging activity, and lipid peroxidation inhibition activity. Results: The extract depicted maximum DPPH radical scavenging activity followed by ABTS radical scavenging activity. Hefty metal chelation and nitric oxide scavenging activity were recorded while lipid peroxidation, H2O2, and OH- scavenging activity was intermediate. Conclusion: Jamun seed showed ample antioxidant activity and certifies that it is the right candidate for exploitation as a source of natural antioxidants to counteract autoxidation-induced pathologies or diseases.


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