NO Radical Scavenging Activities Research Articles

Curcumin‐loaded nanoparticles effectively prevent T4‐induced oxidative stress in rat heart

AbstractIn this study, we report the cardioprotective effect of the glycerol monooleate (GMO) based nanocurcumin in both in vitro and in vivo conditions under a hyperthyroid state. The heart is one of the primary target organs sensitive to the action of thyroid hormone, and slight variations in the thyroid hormone serum concentrations result in measurable changes in cardiac performance. Hyperthyroidism‐induced hypermetabolism is associated with oxidative stress and is an important mechanism responsible for the progression of heart failure. Curcumin has been known to play a protective role against oxidative stress‐related diseases like Alzheimer's, asthma, and aging due to its antioxidant properties. Nevertheless, its potent biological activity has been hindered due to its poor bioavailability. To overcome this drawback, a GMO‐based biodegradable nanoparticle (NP) formulation loaded with curcumin has been developed, and the protective effect of curcumin‐loaded NPs was compared against the native drug. Oxidative stress parameters like reactive oxygen species (ROS) release, change in mitochondrial membrane permeability, lipid peroxidation (LPx), lactate dehydrogenase (LDH) release, and the activity and protein expression of the endogenous antioxidant enzymes like superoxide dismutase, catalase (CAT) and glutathione peroxidase were evaluated. The results from in vitro showed that curcumin‐loaded NPs showed better DPPH and NO radical scavenging activity than native curcumin in a concentrations range of 2.5–20 µM. It was also observed that the nanoparticulate curcumin was comparatively more effective than native curcumin in protecting against ROS‐induced membrane damage by reducing LPx and LDH leakage at low concentrations of 5–10 µM. Further, curcumin NPs performed better in facilitating the activities of antioxidant enzymes under in vitro and in vivo conditions with respect to time and concentrations, resulting in reduced cellular ROS levels. In this scenario, we anticipate that curcumin‐loaded NPs can serve as a better antioxidant than its native counterpart in protecting the heart from oxidative stress‐related diseases.

Sesuvium Portulacastrum Potentiates Anticancer Activity by Facilitating the Expression of IRS-1/AKT Signalling: An In vitro Study.

Sesuvium portulacastrum, a coastal medicinal plant with traditional uses has shown promising biological activities including anti-inflammatory, antioxidant and antimicrobial properties. However, the mechanisms of action active ingredients of this plant have not been studied. Aim of the current study is to investigate the anticancer activity of Sesuvium portulacastrum using in vitro and in silico analysis. The in vitro assays included NO radical scavenging activity, total phenolic and flavonoid content determination. The data were analysed by one-way-ANOVA and p<0.05 was considered as statistically significant. The phytochemical analysis showed the presence of tannins, steroids, terpenoids and phenols. Antioxidant activity of S. portulacastrum showed the dose dependent effect of nitric oxide radical scavenging activity. In silico analysis showed a better binding affinity with IR, IRS1 and Akt molecules which demonstrated the action of bioactive compound of S. portulacastrum against IRS-1/AKT signalling pathway.

Yerba Mate as a Protectant against Lipoproteins Oxidation.

Oxidative modification of low-density lipoproteins (LDL) and high-density lipoproteins (HDL) are important factors determining cardiovascular risk. This study investigated the antioxidant mechanisms and potential protective effect of a hydroethanolic extract of yerba mate (Ilex paraguaiensis; EHEM) on the in vitro oxidation of LDL and HDL. EHEM was found to possess ferric reducing power, DPPH free radical scavenging capacity, metal chelating activity, and NO radical scavenging activity. In addition, EHEM reduced the lipoperoxidation induced by α,α'-Azodiisobutyramidine dihydrochloride (AAPH) in HDL and LDL at all tested concentrations. In this study, we demonstrate the antioxidant properties of yerba mate and its phytochemical compounds. These properties may effectively prevent the in vitro oxidation of LDL and HDL molecules, a phenomenon linked to the pathogenesis of atherosclerosis.

A novel peptide derived from Zingiber cassumunar rhizomes exhibits anticancer activity against the colon adenocarcinoma cells (Caco-2) via the induction of intrinsic apoptosis signaling.

This paper presents the initial exploration of the free radical scavenging capabilities of peptides derived from protein hydrolysates (PPH) obtained from Zingiber cassumunar rhizomes (Phlai). To replicate the conditions of gastrointestinal digestion, a combination of pepsin and pancreatin proteolysis was employed to generate these hydrolysates. Subsequently, the hydrolysate underwent fractionation using molecular weight cut-off membranes at 10, 5, 3, and 0.65 kDa. The fraction with a molecular weight less than 0.65 kDa exhibited the highest levels ABTS, DPPH, FRAP, and NO radical scavenging activity. Following this, RP-HPLC was used to further separate the fraction with a molecular weight less than 0.65 kDa into three sub-fractions. Among these, the F5 sub-fraction displayed the most prominent radical-scavenging properties. De novo peptide sequencing via quadrupole-time-of-flight-electron spin induction-mass spectrometry identified a pair of novel peptides: Asp-Gly-Ile-Phe-Val-Leu-Asn-Tyr (DGIFVLNY or DY-8) and Ile-Pro-Thr-Asp-Glu-Lys (IPTDEK or IK-6). Database analysis confirmed various properties, including biological activity, toxicity, hydrophilicity, solubility, and potential allergy concerns. Furthermore, when tested on the human adenocarcinoma colon (Caco-2) cell line, two synthetic peptides demonstrated cellular antioxidant activity in a concentration-dependent manner. These peptides were also assessed using the FITC Annexin V apoptosis detection kit with PI, confirming the induction of apoptosis. Notably, the DY-8 peptide induced apoptosis, upregulated mRNA levels of caspase-3, -8, and -9, and downregulated Bcl-2, as confirmed by real-time quantitative polymerase chain reaction (RT-qPCR). Western blot analysis indicated increased pro-apoptotic Bax expression and decreased anti-apoptotic Bcl-2 expression in Caco-2 cells exposed to the DY-8 peptide. Molecular docking analysis revealed that the DY-8 peptide exhibited binding affinity with Bcl-2, Bcl-xL, and Mcl-1, suggesting potential utility in combating colon cancer as functional food ingredients.

Punica granatum peel extract modulates levofloxacin-induced oxidative stress and testicular damage in rats

Levofloxacin (LEV) is one of the Fluoroquinolones antibiotic groups, which are utilized in the therapy of numerous diseases, particularly in reproductive organs. Punica granatum peel is a waste byproduct rich in phytochemicals that are known for their different biological activities. The current research was designed to assess the capability of pomegranate peel extract (PGPE) in counteracting LEV-induced oxidative stress and testicular injury in rats. Rats groups were divided as follows: control, PGPE (500 mg/kg BW), LEV (300 mg/kg BW), and PGPE plus LEV. Rats were treated orally for two weeks daily. The chemical and nutritional content of Punica granatum peel (PGP) were investigated. GC/MS analysis showed the major phytochemical constituents in PGPE as gallic acid, ellagic acid, 4H-Pyran-4-one, 2,3-dihydro-3,5-dihydroxy-6-methyl, and caffeic acid with DPPH, ABTS, and NO radical scavenging activity, as well as Fe3+- reducing antioxidant activity. Results revealed that LEV increased TBARS and H2O2 concentrations and LDH activity in rat testes significantly. While the activities of antioxidant enzymes, phosphatases, aminotransferases, and reduced glutathione content as well as protein levels, were significantly reduced. Worthy changes in testosterone, luteinizing, and follicle-stimulating hormone levels, as well as sperm characteristics, were also discovered. LEV was also found to trigger apoptosis, as evidenced by elevated p53 and caspase-3 levels and decreased Bcl2 levels. Furthermore, alterations in histological and immunohistochemical PCNA expression were observed in rat testes, confirming the biochemical findings. Furthermore, PGPE pretreatment of LEV-treated rats restored the majority of the tested parameters when compared to the LEV-treated group. In conclusion, pomegranate peel extract had a powerful modulating role against the adverse effects of levofloxacin in rat testes and represents a perspective of the utilization of food waste by-products.

Evaluation of Antioxidant Potential of Asystasia Chelonoides var.chelonoides Nees.(Acanthaceae)

The ethanolic leaf extract of Asystasia chelonoides var. chelonoides Nees. was evaluated using various in vitro and ex vivo assays. Evaluations were made for DPPH radical scavenging activity, NO radical scavenging activity, Super oxide radical scavenging activity ,Ferric Reducing Antioxidant Potential (FRAP) assay, Total antioxidant activity , Reducing Power activity and Lipid Peroxidation inhibition. Over all findings revealed that A.chelonoides leaf exhibited four extracts namely (AC HEX, AC CHL, AC ETH and AC CRD) and were selected for the study, AC ETH and AC CRD showed potent antioxidant activity by inhibiting DPPH radical in a concentration dependent manner . The nitric oxide radical scavenging activity of all the samples increased as their concentration increased from 20 µg/mL to 320 µg/ mL. AC CRD showed its maximum superoxide radical scavenging of 78.56 % at 320 µg/mL and the EC50 was found to be 93.26 µg/mL. The extracts exhibited a dose dependent reducing power activity within the applied concentrations (20 µg/mL to 100 µg/mL) and AC CRD at 100 µg/mL concentration showed highest activity, which was almost comparable to standard ascorbic acid. In FRAP assay the crude extract of A. chelonoides (AC CRD ) showed 138.14 µg trolox equivalent/g of dry extract respectively. Total antioxidant activity of AC CRD, AC HEX, AC CHL and AC ETH were found to be 98.27, 14.86, 20.16 and 72.56 µg of ascorbic acid equivalent/mg of dry extract respectively. A.chelonoides crude extract and ethanolic fraction showed potent inhibition of FeCl2AA stimulated rat liver lipid peroxidation in concentration dependent manner.

Correlation of the free radical and antioxidant activities of Eriobotrya Japonica Lindl. with phenolic and flavonoid contents

This study was conducted to compare the correlations between antioxidant activity and free radicals. Total Polyphenol and Flavonoid contents were the highest 31.97 ± 1.29 mg TAE/g and 96.1 ± 0.31 mg CE/g in hot water extract, respectively. FRAP activity was highest at 559.17 ± 2.69 mg TE/g in 60% EtOH extract. The RC50 values of DPPH and ABTS radical scavenging activity were lowest at 61.96 ± 5.01 μg/mL in 80% EtOH, 73.81 ± 0.16 μg/mL in 60% EtOH, respectively. The RC50 values of hydrogen peroxide scavenging activity and NO radical scavenging activity were lowest at 265.33 ± 3.88 μg/mL in 60% EtOH and 52.51 ± 8.54 μg/mL in hot water extract, respectively. The total polyphenol and flavonoid contents had significant correlation with the free radical scavenging ability and electron donating ability. On the other hand, there was confirmed significant correlation of free radical and antioxidant activities.

In vitro Anti-oxidant and Anti-inflammatory Activity of the Aqueous and Ethanol Leaf Extracts of Clerodendrum phlomidis Linn. F.

Clerodendrum phlomid is was a common shrub of arid plains, low hills, and tropical deserts. It belongs to the family Verbenaceae. Many species of this genus have been documented in traditional system of medicine in India. The roots of the plant have been extensively studied in Ayurveda but in folk and traditional medicine, it is the leaf that finds more application in alleviating many diseases. Oxidation byproducts of metabolism was responsible for many pathophysiological conditions. Anti-oxidants are molecules that quench the free radicals. The present study aims at evaluating the in-vitro anti-oxidant and anti-inflammatory activity of the aqueous and ethanol leaf extract of Clerodendrum phlomidis. The anti-oxidant activity was evaluated by three in vitro models, namely the DPPH radical scavenging activity, hydroxyl radical scavenging activity and NO radical scavenging activity. The anti-inflammatory activity was evaluated by the RBC membrane Inhibition method. The aqueous extract was found to have better anti- oxidant activity than the ethanol extract in DPPH and NO radical scavenging activity. The RBC membrane inhibition method clearly states that the aqueous leaf extract of Clerodendrum phlomidis was found to have a comparatively an effective anti-inflammatory activity than ethanol extract.

Profiling cosmeceutical effects of various herbal extracts through elastase, collagenase, tyrosinase inhibitory and antioxidant assays

• Cotinus coggygria is one of the plant species in terms of cosmeceutical effect. • Active plant species usually have records against skin disorders. • Use of active extracts with different antioxidant mechanisms will be more effective. Plants have been a very rich resource for the development of potentially new drug candidates and also the development of cosmetic products for skincare. The skin produces free radicals or reactive oxygen species through repeated exposure to the sun and these molecules cause oxidative stress and inflammatory reactions in the dermal and epidermal layers of the skin. Matrix metalloproteinases are triggered by aging and in inflamed skin, such as photo-aged skin, skin damage, and wrinkles occurred by collapsing dermal proteins such as collagen and elastin. In the development of plant-based skin whitening products, the first target is to investigate the inhibitors of the tyrosinase enzyme, which provides melanin production. The ethanol extracts of 92 herbal extracts and propolis were tested for their elastase, collagenase, and tyrosinase inhibitory effects using ELISA microtiter assays. Their antioxidant effect was determined using DPPH, DMPD, and NO radical scavenging activity, metal-chelation capacity, FRAP, PRAP, and CUPRAC assays. Total phenolic and flavonoid contents of the extracts were also determined spectrophotometrically. Our results from the screening studies showed that the ethanol extracts prepared from the aerial parts of Lamium purpureum subsp. purpureum, the pericarpium of Garcinia mangostana and Pistacia vera , the flowers of Punica granatum, and the seeds of Vitis vinifera were effective against at least two of these enzymes and therefore, the plant species were selected for further studies.

The Antioxidation Effect of Brown Algae Extract

This study attempted to investigate the functionality of &lt;i&gt;Dactylosiphon bullosus&lt;/i&gt;, &lt;i&gt;Sporochnus radiciformis&lt;/i&gt;, and &lt;i&gt;Zonaria diesingiana&lt;/i&gt; extracts among algae as cosmetic ingredients. For this, antioxidant experiments were performed. &lt;i&gt;D. bullosus&lt;/i&gt;, &lt;i&gt;S. radiciformis&lt;/i&gt; and &lt;i&gt;Z. diesingiana&lt;/i&gt; extracts were prepared with a 70% ethanol concentration to measure antioxidant activities. In terms of DPPH radical scavenging activity, &lt;i&gt;Z. diesingiana&lt;/i&gt; was the highest with 94.20±0.28%. In ABTS radical scavenging activity, &lt;i&gt;Z. diesingiana&lt;/i&gt; was the highest with 96.26±0.98%. In terms of the total phenolic contents and NO radical scavenging activity, &lt;i&gt;Z. diesingiana&lt;/i&gt; was the highest with 47.19±2.07 mg gallic acid/g and 92.87±1.79%, respectively. The above results show that &lt;i&gt;Z. diesingiana&lt;/i&gt; extract has the greatest antioxidant activity, confirming its potential as a cosmetic ingredient.

The Antioxidation Effect of Gracilaria spp. extract

This study examined antioxidant activity for use as a cosmetic material Gracilaria Incurvata, Gracilaria parvispora, and Gracilaria vermiculophylla among the red algae widely used as edible seaweed. For antioxidant activity measurement, extracts were diluted with 70% ethanol to manufacture extracts. In DPPH radical scavenging activity assays, Gracilaria vermiculophylla extract showed the highest figure at 97.27±1.05%. In ABTS radical scavenging activity assays, Gracilaria vermiculophylla extract showed the highest figure at 47.67±2.78%. In total phenolic contents measurement results, Gracilaria vermiculophylla extract showed the highest figure at 75.60±1.40 mg gallic acid/g, but only in the NO radical scavenging activity assay, the Gracilaria incurvata extract showed the highest figure at 95.80±0.33%. As a result, Gracilaria vermiculophylla was the most likely to develop as a cosmetic material in the remaining three antioxidant activity measures in addition to NO radical scavenging activity. Keywords: Gracilaria incurvata; Gracilaria parvispora; Gracilaria vermiculophylla; red algae; seaweed

Stabilization of the ruthenium (II) and -(III) centres by chelating N-donor ligands: Synthesis, characterization, biomolecular affinities and computational studies

Anticancer activities of ruthenium Schiff base metal complexes have been closely correlated to their steric factors and physicochemical properties. The core objectives of our research study were to synthesize and characterize new ruthenium Schiff base compounds derived from cinnamaldehyde, cuminaldehyde or 4-aminoantipyrine. In addition, the stereo-electronic features of the aforementioned metal compounds and two selected previously reported ruthenium Schiff base compounds were related to their antioxidant and biomolecular interaction capabilities. Therefore, we demonstrated the formation of novel mononuclear ruthenium(III) compounds with chelating N-donor ligands: fac-[RuCl3(PPh3)(ap)] (1) (ap = 4-aminoantipyrine), trans-P-[Ru(PPh3)2(cinap)2](PF6) (2) (cinap = 1,5-dimethyl-2-phenyl-4-{[3-phenylprop-2-en-1-ylidene]amino}-1,2-dihydro-3H-pyrazol-3-one) and cis-Cl, trans-P-[RuCl2(PPh3)2(cumbh)] (3) (cumbh = N'-(4-isopropylbenzylidene)benzohydrazide). Structural confirmations were conducted primarily by spectroscopic techniques while the single crystal X-ray analysis revealed the distorted octahedrons of the respective metal compounds. Voltammetry experiments of 1–3 illustrated one-electron quasi-reversible redox waves which are attributed to metal oxidation state interconversions. CT-DNA binding affinities and modes of the novel metal complexes 1–3 as well as the formerly published ruthenium Schiff base compounds, trans-P, cis-Cl-[Ru(pch)Cl2(PPh3)2] (4) (pch = 4-((pyridine-2yl-imino)methylene)-chromone) and cis-[RuCl2(bpap)(PPh3)] (5) (bpap = 2,6-bis-((antipyrine-imino)methylene)pyridine) were experimentally and computationally investigated. The paramagnetism of 1–4 and the proton-donor abilities of all the metal compounds promoted significantly higher NO and DPPH radical scavenging activities than the natural antioxidant, vitamin C. Experimental electronic BSA titrations revealed that the metal compounds are ideal binders which preferentially bind to site IIA. The X-ray and spectroscopic data were supported by the computed data which was simulated using the density functional theory method.

Isolation of potential liver x receptor alpha agonist and antioxidant compounds from Hypericum microcalycinum Boiss. &amp; Heldr.

Background and Aims: Hypericum microcalycinum Boiss. & Heldr. is used for inflammatory diseases in Anatolia. The involvement of liver X receptors (LXRs) and free radicals in inflammatory diseases, activation of LXRs, and high radical contents in cancerous tissue and organs prompted us to determine the radical scavenging and LXRα agonist activity of aqueous fraction of methanol extract and fractions of H. microcalycinum along with the isolation studies from active fractions. Methods: Isolation studies were carried out on chromatographic techniques. DPPH, NO, and SO radical scavenging activity methods were used for the determination of antioxidant activity, and a LXRE reporter gene assay was used for the determination of LXRα agonist activity. Results: While the extract showed weak LXRα agonist activity, phenolic compounds- rich fractions showed moderate activity. DPPH radical scavenging capacities of the extract and some fractions seemed to be very high as well as some isolated compounds. Bioactivity- guided studies resulted in the isolation of catechin (1), epicatechin (2), apigenin-8-C-(2-O-acetyl)- glucopyranoside (3), quercetin-3-O-β-glucopyranoside (4), quercetin-3-O-β-arabinopyranoside (5), kaempferol-3-O-βarabinopyranoside (6), luteolin-8-C-β-glucopyranoside (orientin) (7). Conclusion: According to our results, compounds 1, 2, 4, and 5 may be responsible for the anti-inflammatory effects of H. microcalycinum as a function of LXRα agonist and free radical scavenging effects.

Synthesis, Characterization and Biological Evaluation of Indole-Pyrazole Amalgamated α-Cyano Substituted Chalcones

Indole and pyrazole constitute a major class of biologically active scaffolds. The amalgamation of two or more pharmacophores would generate novel molecular templates that are likely to unveil remarkable biological properties. An efficient and high yielding synthesis of indole-pyrazole integrated α-cyano substituted chalcones and their in vitro antibreast cancer and antioxidant evaluation. The synthesis of a series of indole-pyrazole amalgamated α-cyano substituted chalcones (6a-o) was achieved by reacting substituted 3-cyanoacetyl indole 2 with substituted pyrazole aldehyde 5 in the presence of piperidine. All the newly synthesized compounds have been characterized by IR, 1H NMR and HRMS spectroscopy. Anti-breast cancer evaluation of the synthesized compounds in vitro against MCF-7 cell line revealed high anti-breast cancer activities. Amongst the compounds screened 6f, 6g, 6h, 6c, 6d, 6e, 6i and 6k unveiled excellent activity against breast carcinoma (GI50 <0.1µM) as good as adriamycin (GI50 <0.1µM). The compounds were also screened against the normal Vero monkey cell line and the results demonstrated more selectivity against MCF-7. In other hand, compounds, 6b, 6c, 6d, 6h and 6i have shown moderate DPPH and NO radical scavenging activity. Most of the synthesized compounds exhibited significant antitumor activities. These results further support its safety margin by studying the activity on normal Vero monkey cell line. These results acclaim the possible use of these compounds for the design and development of potent anti-breast cancer agents.

Correlation between antioxidant activity and anti-wrinkle effect of ethanol extracts of Sanguisorba Officinalis L.

Sanguisorba officinalis L., the dried roots of which are referred to as cucumber herb is a perennial herb belonging to the family Rosaceae. This study was showed the correlation between the antioxidant activity and its anti-wrinkle effects of ethanol extraction concentration of S. officinalis L. The extraction yield of the S. officinalis extracts was all 10% or more, which was judged to be economical. 80% ethanol extracts was the highest in total polyphenol and flavonoid contents and the best total antioxidant activity. The correlation between total polyphenol and flavonoid contents and antioxidant activity was 0.830 and 0.872, respectively, with a significant correlation was confirmed. In addition, in 80% ethanol extracts, superoxide anion and NO radical scavenging activities were the most effective. These results validated that the optimum extraction concentration for S. officinalis was 80% ethanol.

Polysaccharides from dandelion (Taraxacum mongolicum) leaves: Insights into innovative drying techniques on their structural characteristics and biological activities

The aim of this study was to well understand the impacts of innovative drying techniques (radio frequency drying and microwave drying) and traditional drying techniques (vacuum drying, freezing drying, and hot air drying) on the structural characteristics and bioactivities of polysaccharides from dandelion leaves (DLPs). Five different DLPs were obtained from dandelion leaves dried by abovementioned drying techniques. Results showed that the structural characteristics and bioactivities of DLPs varied with different drying techniques. The molecular weights, apparent viscosities, molar ratios of constituent monosaccharide, contents of uronic acids, and contents of bonded polyphenolics in DLPs obtained by different drying techniques had noticeable variations, while the types of constituent monosaccharides and the major glycosidic linkages in DLPs were similar. In addition, results showed that DLPs, especially DLP-RF obtained by the radio frequency drying, exhibited remarkable antioxidant activities (ABTS, DPPH, and NO radical scavenging activities), excellent in vitro antiglycation activity, and obvious in vitro inhibitory activity on α-glucosidase. Results from this study suggest that the radio frequency drying can be used as a potential drying technique before extracting DLPs for applications in the functional food and medicine industries.

Isolation and characterization of anti-inflammatory peptides derived from trypsin hydrolysis of microalgae protein (Synechococcus sp. VDW)

ABSTRACTThe Synechococcus sp. VDW peptides were prepared by trypsin digestion, which was then purified by ultrafiltration with molecular weight cut off membranes of 10, 5 and 3 kDa. Among the fractions, the MW <3 kDa fraction exhibited high levels of inhibitory activity toward the NO radical scavenging activities with IC50 values of 34.51 ± 9.8 μg/mL. The MW <3 kDa fraction was purified by reversed-phase HPLC to yield four fractions. The 30–40 min sub-fraction with maximum NO radical scavenging activity (77.50 ± 0.55%) was selected for further analysis by Q-TOF ESI mass spectrometry. Five isolated peptides with amino acid sequences of AILQSYSAGKTK; 1,265.69 Da, ALNKTHLIQTK; 1,265.74 Da, LLVHAPVK; 875.55 Da, IPDAHPVK; 875.48 Da, and VVVLRDGAVQQLGTPR; 1,706.97 Da were identified. The MW <3 kDa fraction showed no cytotoxicity toward RAW264.7 macrophage cells. Quantitative RT-PCR results showed that the MW <3 kDa fraction reduced gene expression of pro-inflammatory cytokines iNOS, TNF-α, COX-2, and IL-6. The peptides isolated from the MW <3 kDa fractions represent potential model peptides to develop natural anti-inflammation food-grade ingredients, drugs, and cosmetic products.

SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL THIAZOLE-PYRAZOLE INTEGRATED CHALCONES AS ANTIOXIDANT AND ANTI-INFLAMMATORY AGENTS

Objective: The objective of the present study was to synthesize the thiazole-pyrazole integrated chalcones and their in vitro antioxidant and anti- inflammatory evaluation.&#x0D; Methods: The designed hybrid thiazole-pyrazole integrated chalcones (3a-j) were synthesized by Claisen–Schmidt reaction of substituted 1-(4-methyl-2-phenylthiazol-5-yl) ethanone and substituted pyrazole aldehyde in the presence of 10% NaOH in ethanol solvent under reflux condition. The chemical structures of synthesized compounds were confirmed by IR, 1H nuclear magnetic resonance (NMR), 13C NMR, and high- resolution mass spectra.&#x0D; Results: All the title compounds were screened for their in vitro antioxidant and anti-inflammatory activity. The screening data indicated that tested compounds showed potent antioxidant activity with moderate anti-inflammatory potential.&#x0D; Conclusion: Antioxidant screening data reveal that most of the synthesized compounds possess excellent 1,1-diphenyl-2-picrylhydrazyl and NO radical scavenging activity. Most of the compounds found to possess marked anti-inflammatory potential by effectively inhibiting the heat-induced albumin denaturation.

Phytochemical, antioxidant, and anti-inflammatory screening of the Egyptian Ulva lactuca methanolic extract

Ulva lactuca is widespread green algae. In some regions, it is used in nutrition. Its nutrients include iron, protein, iodine, vitamins (A, B1, and C) and trace elements. Their extracts showed potential antibacterial, hypolipidemic, cardioprotective and chemoprotective activities. The main chemical constituents of Ulva lactuca methanolic crude extract and its fractions were investigated in this study using different phytochemical and chromatographic methods. Biologically guided fractionation of plants or seaweeds extracts is considered the first step in drug discovery. So, the algal crude extract was fractionated then in vitro bioscreened for the determination of diphenylpicrylhydrazyl (DPPH) antioxidant, (Nitric Oxide) NO radical scavenging and anti-inflammatory activities. Results showed that water fraction was the most active fraction. Phenolic content, detected from HPLC, play a role in the antioxidant activity. Finally, it can be concluded that Ulva water fraction is effective candidate to be used in the treatment of oxidative stress and related disorders

Characterization ofVicia(Fabaceae) seed water extracts with potential immunomodulatory and cell antiproliferative activities

Vicia seeds represent an underutilized source of nutritional and functional components. Besides being rich in proteins, they are also rich in polyphenols, free amino acids, and lectins. These components are enriched in a by-product of the production of protein isolates, a pH 4 soluble extract. Extracts from six Vicia have been analyzed, and NO radical scavenging and antiproliferative activities have been determined. Canavanine was the main free amino acid, while gallic acid derivatives were the most abundant of polyphenols. Fractionation of the extracts by ultrafiltration rendered a lectin-free fraction that exhibited nitric oxide radical scavenging activity. Based on this activity, and in the presence of high levels of polyphenols and canavanine that are inhibitors of inducible nitric oxide synthase, it is proposed that these extracts may have an immunomodulatory effect. In addition, some extracts inhibited proliferation of cancerous Caco-2 cells, further supporting the potential of Vicia extracts as functional components. Practical applications During the production of Vicia protein isolates an aqueous soluble fraction, considered a by-product, is generated which is rich in polar polyphenols, free amino acids, and water soluble proteins that are of interest from a functional point of view. In six Vicia species this aqueous fraction showed NO radical scavenging and cell antiproliferative activity. Hence, these fractions usually considered as a by-product, could be exploited as a source of functional compounds with potential health promoting properties. This could result in the revalorization of Vicia seeds and decrease in the generation of by-products from the process of Vicia protein isolate productions.