Nitric Oxide Production In RAW Research Articles

Curcubinoyl flavonoids from wild ginseng adventitious root cultures

Wild ginseng (Panax ginseng) adventitious root cultures were prepared by elicitation using methyl jasmonate and investigated further to find new secondary metabolites. Chromatographic fractionation of wild ginseng adventitious root cultures led to the isolation of eleven compounds. The chemical structures of isolated compounds were identified as four known flavanone derivatives (1–4), one new curcubinoyl derivative, jasmogin A (5) and six new curcubinoyl-flavanone conjugates, jasmoflagins A-F (6–11) by extensive spectroscopic analysis. Newly isolated curcubinoyl derivatives showed inhibitory activity against lipopolysaccharide-stimulated nitric oxide production in RAW 264.7 macrophages. Therefore, our present study suggested that elicitor stimulated plant cell cultures might contribute to the production of new metabolites.

Structural basis for the regulation of inducible nitric oxide synthase by the SPRY domain-containing SOCS box protein SPSB2, an E3 ubiquitin ligase

Relatively high concentration of nitric oxide (NO) produced by inducible nitric oxide synthase (iNOS) in response to a variety of stimuli is a source of reactive nitrogen species, an important weapon of host innate immune defense. The SPRY domain-containing SOCS box protein 2 (SPSB2) is an E3 ubiquitin ligase that regulates the lifetime of iNOS. SPSB2 interacts with the N-terminal region of iNOS via a binding site on the SPRY domain of SPSB2, and recruits an E3 ubiquitin ligase complex to polyubiquitinate iNOS, leading to its proteasomal degradation. Although critical residues for the SPSB2-iNOS interaction have been identified, structural basis for the interaction remains to be explicitly determined. In this study, we have determined a crystal structure of the N-terminal region of iNOS in complex with the SPRY domain of SPSB2 at 1.24 Å resolution. We have resolved the roles of some flanking residues, whose contribution to the SPSB2-iNOS interaction was structurally unclear previously. Furthermore, we have evaluated the effects of SPSB2 inhibitors on NO production using transient transfection and cell-penetrating peptide approaches, and found that such inhibitors can elevate NO production in RAW264.7 macrophages. These results thus provide a useful basis for the development of potent SPSB2 inhibitors as well as recruiting ligands for proteolysis targeting chimera (PROTAC) design.

Bioactive-guided isolation and identification of oligostilbenes as anti-rheumatoid arthritis constituents from the roots of Caragana stenophylla

Ethnopharmacological relevanceThe roots of Caragana stenophylla have been used as folk medicine due to the functions of activating blood, diuresis, analgesic and tonicity, especially in treating rheumatoid arthritis and hypertension. However, the anti-rheumatoid arthritis mechanisms and bioactive ingredients have not previously been fully investigated. Aim of the studyThe aim of this study was to assess the anti-rheumatoid arthritis effects of the roots of Caragana stenophylla ethanol extract (EC), elucidate its mechanism of action and identify its active substances. Materials and methodsAnti-rheumatoid arthritis activity of EC was assessed using type II-collagen induced arthritis in rats. Arthritis severity was evaluated by foot paw volume, arthritis index, joint swelling degree and histopathology. The serum inflammatory cytokines and matrix metalloproteinases (MMPs) were also detected by immunohistochemical analysis. In addition, the protein expression of IκB, p-IκB, iNOS and COX-2 was analyzed by western blot. RAW 264.7 macrophage cells were employed to assess the anti-inflammatory effects of fractions and compounds in vitro. UPLC-Q-TOF-MS was adopted to appraise the ingredients of the active fraction of the roots of C. stenophylla. Furthermore, various chromatographic techniques and spectroscopic methods were used for isolation and structure elucidation of compounds. ResultsThe results showed that EC could reduce type II collagen-induced rheumatoid arthritis model arthritic score and histopathology markedly at dose of 240 mg/kg. Besides, EC could suppress the levels of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, IL-17, and TNF-α) and matrix metalloproteinases (MMP-3, MMP-9), and the expression levels of COX-2, p-IκB and iNOS also were declined. While, the levels of IL-10 and IκB were increased. The ethyl acetate fraction exhibited potent inhibitory effects against nitric oxide production in RAW 264.7 macrophage cells. Eleven main components including 1 flavonoid and 10 oligostilbenes from active fraction were isolated by mass directed chromatographic techniques. Their structures were determined on the basis of various spectroscopic methods and by comparison with the published NMR data. ConclusionThe roots of C. stenophylla attenuated arthritis severity, restored serum cytokine imbalances by regulating NF-κB signaling pathway in type II collagen-induced rheumatoid arthritis model. Oligostilbenes were essential ingredients in ethyl acetate extract of C. stenophylla roots. Stilbenes and flavonoids should be responsible for its anti-rheumatoid arthritis activities.

Polyacetylene glucosides from the florets of Carthamus tinctorius and their anti-inflammatory activity

Five previously undescribed polyacetylene glucosides, namely, four C10- and one C14-acetylenes, together with three known analogues, were isolated from the florets of Carthamus tinctorius L. The structures of these novel compounds were elucidated to be (5R)-5-acetoxy-8,10,12-tetradecatriyne-1-O-β-D-glucopyranoside, (2Z)-decaene-4,6,8-triyne-1-O-β-D-glucopyranoside, (8Z)-1-[(3-O-β-D-glucosyl)-isovaleroyloxy]-8-decaene-4,6-diyne, (8Z)-decaene-1-isovaleroyloxy-4,6-diyne-10-O-β-D-glucopyranoside, and (2E,8E)-decadiene-4,6-diyne-1-O-β-D-glucopyranoside via spectroscopic and chemical methods. All of the isolated compounds were tested for cytotoxicity against cancer cell lines, antibacterial activity, and inhibitory effects on the lipopolysaccharide (LPS)-induced nitric oxide (NO) production. The results showed that (5R)-5-acetoxy-8,10,12-tetradecatriyne-1-O-β-D-glucopyranoside significantly inhibited LPS-induced NO production in RAW264.7 cells in a dose-dependent manner.

Evaluation of the efficacy of ethanol leaf extract of Helichrysum petiolare Hilliard and B.L. Burtt against skin aging

Purpose: To determine the efficacy of Helichrysum petiolare ethanol leaf extract against skin aging.Methods: The cytotoxic potential of the plant extract towards human dermal fibroblast (MRHF) cells was determined by Hoechst 33342/Propidium iodide (PI) staining. Effect of H. petiolare extract on reactive oxygen species (ROS) levels in MRHF cells and NO (nitric oxide) production in RAW 246.7 cells activated by LPS (lipopolysaccharides) was investigated. The inhibitory effect of the extract againstcollagenase, elastase, tyrosinase and protein glycation was also evaluated.Results: The extract did not display cytotoxicity towards MRHF cells at the tested concentrations when compared to the trend seen with the untreated control (p < 0.05). The extract caused a significant decrease (p < 0.05) in ROS levels in MRHF cells in a concentration-dependent manner and also demonstrated a reduction in NO production in RAW cells with no toxicity. Furthermore, the extract produced a weak inhibition of collagenase, elastase and tyrosinase activities when compared to the corresponding positive controls, but effectively inhibited protein glycation at the tested concentrations.Conclusion: The findings suggest that the ethanol leaf extract from H. petiolare has the potential to mitigate skin aging and therefore needs to be further investigated for possible clinical applications.
 Keywords: Cytotoxicity, Efficacy, Helichrysum petiolare, MRHF cells, Oxidative stress, Protein glycation; skin aging

Sesquiterpenoids from Chrysanthemum indicum with Inhibitory Effects on NO Production.

Three new guaianolide lactones (1-3) and four new 9-oxonerolidol glucosides (5-8) together with 20 known compounds were isolated from the MeOH extract of the flowers of Chrysanthemum indicum. Their structures were elucidated based on the interpretation of NMR, HRESIMS, and electronic circular dichroism (ECD) data along with acid hydrolysis. Of the isolates, sesquiterpenoids 1-4 and 15 and flavones 17 and 18 exhibited inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide production in RAW 264.7 cells with IC50 values in the range 0.2-27.0 μM.

Diterpenoids and Diacetylenes from the Roots of Aralia cordata with Inhibitory Effects on Nitric Oxide Production.

Bioactivity-guided isolation of a MeOH extract of Aralia cordata led to the isolation of four new ent-pimarane diterpenoids (1-4) and a diacetylene (5) together with 21 known compounds (6-26). Their structures were established based on the interpretation of one- and two-dimensional NMR and HRESIMS data. The absolute configurations of the new isolates were determined by electronic circular dichroism data analysis, single crystal X-ray diffraction, and Mosher's esterification method. All compounds exhibited inhibitory effects on lipopolysaccharide-induced nitric oxide production in RAW 264.7 macrophages with IC50 values ranging from 1.1 to 69.4 μM.

The anti-inflammatory and analgesic activities of the ethyl acetate extract of Viburnum taitoense Hayata

Ethnopharmacological relevanceViburnum taitoense Hayata has been used as folk medicine by the minority people in Southwestern China for a long history, especially in Guangxi Zhuang Autonomous Region. The minority in Guangxi including Zhuang, Miao and Yao people use the ethanol extract of V. taitoense Hayata to treat the fracture, kill the pain of rheumatism because of its definite therapeutic effects. Aim of the studySo far, the scientific investigation of V. taitoense Hayata is done very little. Here, we first prepared the ethyl acetate extract of V. taitoense (EEVt), secondly measured the contents of phenols, flavonoids, and terpenoids in EEVt, and thirdly, the anti-inflammatory and analgesic activities of EEVt were investigated by invitro model of RAW 264.7 cells and invivo models of inflammation and pain in rats and mice. Materials and methodsThe contents of phenols, flavonoids, and terpenoids in EEVt were determined by UV spectrophotometry, respectively. The anti-inflammatory effect of EEVt (5, 25, 50, 100, and 200 μg/mL) in vitro was tested by determining its inhibitory effect on the nitric oxide production of RAW264.7 cells activated by lipopolysaccharide (LPS). The anti-inflammatory and analgesic effects of EEVt in vivo were investigated in the following experimental rats and mice models: carrageenan-induced paw edema, corton-oil-induced ear edema, acetic acid writhing test, and formalin pain test. ResultsThe contents of total phenolic, total flavonoids, and total triterpenoids in V. taitoense were measured to be 3.46 ± 0.04%, 2.38 ± 0.04%, and 14.96 ± 0.17%, respectively. In vitro test showed that EEVt at different tested dosages (5, 25, 50, 100, and 200 μg/mL) had no significant toxicity to RAW264.7 macrophages. At dosages of 37.5 and 75 μg/mL of EEVt significant inhibitory (p < 0.001) on the productions of nitric oxide (NO). High dosage (200 μg/mL) of EEVt displayed highly significant inhibitory (p < 0.001) on the productions of proinflammatory cytokines IL-6, IL-1β, and TNF-α from the LPS-induced RAW264.7 macrophages. EEVt showed obvious anti-inflammatory activity at different time points after carrageenan injection (p < 0.05) in vivo test, and its anti-inflammatory activity reached the strongest 4 h. Similarly, through the ear swelling test, EEVt (200 mg/kg) showed significant (p < 0.05) anti-inflammatory activity. Besides, formalin and acetic acid writhing experiments also showed that EEVt has significant (p < 0.05) analgesic activity. ConclusionEEVt was confirmed to be definite anti-inflammatory and analgesic effects, and the phytochemicals of EEVt was disclosed to be rich in triterpenoids, which was worthy to be further investigated.

Sulfated Mesona chinensis Benth polysaccharide enhance the immunomodulatory activities of cyclophosphamide-treated mice

Abstract A sulfated polysaccharide (SMP) from the Mesona chinensis Benth was successfully obtained and its immunomodulatory effects were evaluated. Results showed that SMP exhibited the proliferation effects in splenocytes in vitro and ameliorated the impaired of splenocytes in Cy-treated mice. SMP induced the production of nitric oxide (NO), interleukin (IL) −2, interferon-γ (IFN-γ), increased the expression of antioxidant enzymes (SOD and CAT), and reduced the production of malondialdehyde (MDA) in Cy-treated mice, as well as improved the blood index, body weight and organ index. In addition, SMP enhanced the viability of RAW264.7 macrophages and increased the secretion of IL-6, IL-1β and tumor necrosis factor-α (TNF-α) and production of NO in RAW264.7 cells. Furthermore, SMP binds to TLR4 (Toll-like Receptor 4) to promote RAW264.7 to produce cytokines, thereby exerting immunoregulatory function. These data indicated that SMP act a pivotal part in immunomodulatory and could be used as functional foods.

Anti-inflammatory effect of neo-lignan isoamericanin A via suppression of NF-κB in liposaccharide-stimulated RAW 264.7 cells

Purpose: To investigate the potential anti-inflammatory effects of the seeds of Opuntina humifusa and its active constituents.Methods: The extract of O. humifusa seeds was tested for the inhibition of nitric oxide (NO) production in liposaccharide (LPS)-stimulated RAW 264.7 cells using Griess reagent. The active constituents were isolated using bioassay-guided isolation methods. The effects of the active constituent on NO, proinflammatory cytokines, nuclear factor-kappa B (NF-κB) and nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor (IκB) were evaluated by enzyme-linked immunosorbent assay (ELISA) and western blot analysis.Results: The seed extract of O. humifusa significantly attenuated LPS-induced NO production in RAW 264.7 cells (p &lt; 0.05). Bioassay-guided fractionation resulted in the isolation of isoamericanin A as an active constituent. Isoamericanin A reduced LPS-induced production of NO, iNOS, and proinflammatory cytokines (TNF-α and IL-6) in a concentration-dependent manner (p &lt; 0.05). Furthermore, the effect was accompanied by decreased translocation of NF-κB from the cytosol to the nucleus and the decreased phosphorylation of IκB in the cytosol induced by LPS (p &lt; 0.05).Conclusion: The seed extract of O. humifusa and its active constituent, isoamericanin A, have antiinflammatory effects in LPS-stimulated RAW 264.7 cells, suggesting that they have potentials as antiinflammatory agents.&#x0D; Keywords: Opuntia humifusa seeds, Isoamericanin A, Nitric oxide, RAW 264.7 cells, NF-kappa B

Terpenoid and phenolic derivatives from the aerial parts of Elsholtzia rugulosa and their anti-inflammatory activity

Seven undescribed terpenoids, including three pairs of enantiomers, named (±)-rugulolides A−C, and one cyclopentenone derivative, named rugulolide D, together with twenty-six known compounds, were isolated from the aerial parts of Elsholtzia rugulosa. The chiral separation of rugulolides A−C was achieved by high-performance liquid chromatography using the chiral column. Their structures were elucidated unambiguously based on comprehensive spectroscopic analysis in conjunction with electronic circular dichroism (ECD) and single-crystal X-ray diffraction experiments. Rugulolides A−D are rare naturally occurring terpenoid derivatives featuring a methylated α,β-unsaturated-γ-lactone or a cyclopent-2-en-1-one nucleus. All the isolates were evaluated for their inhibitory effects on lipopolysaccharide-induced nitric oxide production in RAW264.7 cell, among them, four compounds showed moderate inhibition with IC50 values ranging from 12.46 to 23.10 μM.

Lactobacillus paraplantarum THG-G10 as a potential anti-acne agent with anti-bacterial and anti-inflammatory activities

Cutibacterium acnes (formerly Propionibacterium acnes) is the main bacterium targeted for the prevention and medical treatment of acne vulgaris. Lactic acid bacteria (LAB) are a group of microorganisms classified by their ability to produce lactic acid through fermentation. Although the activities of LAB have been studied, their potential anti-acne effects are not well known. Here, Lactobacillus paraplantarum THG-G10, which has anti-bacterial activity against C. acnes, was isolated from traditional Kimchi in Republic of Korea. The anti-acne effects of dried cell-free supernatant of L. paraplantarum THG-G10 (DC-G10) were evaluated by determining its anti-microbial and anti-inflammatory activities. Anti-microbial activity was examined by a broth dilution assay: 25 mg/ml of DC-G10 inhibited the growth of C. acnes KCTC 5012 and KACC 1194; salicylic acid and benzoyl peroxide for acne treatment inhibited the growth of C. acnes KCTC 5012 and KACC 11946 at concentrations of 1.25 and 7.5 mg/ml, respectively; and tea tree oil inhibited the growth of C. acnes KCTC 5012 but not the growth of C. acnes KACC 11946 at 50 mg/ml. Anti-inflammatory activity was evaluated by a nitric oxide (NO) assay: only DC-G10 and ascorbic acid reduced LPS-induced NO production in RAW 264.7 cells in a dose-dependent manner. In addition, the toxicities of erythromycin, salicylic acid, benzoyl peroxide, tea tree oil, and DC-G10 were examined in HaCaT cells and normal human dermal fibroblasts (NHDFs). In these cells, the cytotoxic effects of DC-G10 were weaker than the effects of erythromycin, benzoyl peroxide, and ascorbic acid. Furthermore, scanning electron microscopy revealed that DC-G10 induces deleterious morphological changes in the bacterial cell membrane. These results demonstrate that DC-G10 may be an effective and safe treatment for acne vulgaris.

Anti-inflammatory principles from Balanophora laxiflora

Eighteen known compounds, including lignans, phenylpropanoids, triterpenoids, and phytosterols, were isolated from Balanophora laxiflora (Balanophoraceae). The inhibitory activities of these compounds on the production of nitric oxide (NO), a pro-inflammatory mediator, were evaluated. Compounds isolariciresinol (1), ethyl caffeate (13) and ferulic aldehyde (16) showed potent to mild inhibitory activities on LPS-stimulated NO production in RAW 264.7 macrophages with IC 50 values of 0.81, 7.29, and 98.67 μM, respectively. The results showed that compound 1 had a potent effect on TNF-α production with an IC 50 value of 0.87 μM, but practically no effect on IL-6 synthesis. In addition, an inhibitory effect of compound 1 on nuclear factor-κB (NF-κB) activation was shown by the repression of LPS-stimulated β-lactamase reporter activity. Taken together, these results demonstrated that compound 1 modulates the production of inflammatory mediators through the attenuation of NF-κB transcription signaling.

Enhanced production and immunomodulatory activity of levan from the acetic acid bacterium, Tanticharoenia sakaeratensis

Levan is a fructose polymer with β-(2 → 6) glycosidic linkages. It is produced by several microorganisms, and due to its potential biotechnological and industrial applications, various levan-producing bacteria with different levels of production efficiencies have been reported. We investigated the levan-producing ability of the acetic acid bacterium, Tanticharoenia sakaeratensis. The exopolysaccharides produced by the bacterium under a sucrose environment were characterized as levan by FT-IR, and 1H and 13C NMR. The molecular weight of levan thus produced range from 1.0 × 105–6.8 × 105 Da. The maximum yield of levan from T. sakaeratensis is 24.7 g·L−1 in a liquid medium containing 20% (w/v) sucrose and incubated at 37 °C, 250 RPM for 35 h. The levan produced by T. sakaeratensis can promote nitric oxide production in RAW264.7 macrophage cells in a concentration-dependent manner, suggesting it has immunomodulatory effects. Our study reveals that T. sakaeratensis can be potentially employed as a new source of levan for industrial applications.

Coumarin derivatives from the leaves and twigs of Murraya exotica L. and their anti-inflammatory activities

Fifteen previously undescribed coumarin derivatives, murratins A−M, including two pairs of coumarin enantiomers with a cyclopropane unit, two benzocoumarins, a dimeric coumarin, and eight C-8-substituted coumarins, together with six known analogues were isolated from the extract of the leaves and twigs of Murraya exotica L., a medicinal plant named “Jiulixiang” in Chinese. Their structures were elucidated on the basis of comprehensive analysis of 1D and 2D NMR and HRMS spectroscopic data, and the absolute configurations were assigned via comparison of the specific rotations, the ECD exciton coupling method, comparison of experimental and calculated ECD data, and the ECD data of in situ formed transition metal complexes. All the isolates were evaluated for their inhibitory effects on lipopolysaccharide-induced nitric oxide production in RAW 264.7 cells, and five coumarin derivatives showed moderate inhibitory activities. The possible mechanism for NO inhibition of undescribed bioactive compounds was deduced to interact with iNOS protein via molecular docking. The above results shed some light on a better understanding of the traditional anti-inflammation effect of M. exotica and coumarins are disclosed to be its potential anti-inflammatory constituents.

Anti-Inflammatory Activity of Antimicrobial Peptide Periplanetasin-5 Derived from the Cockroach Periplaneta americana.

Previously, we performed an in silico analysis of the Periplaneta americana transcriptome. Antimicrobial peptide candidates were selected using an in silico antimicrobial peptide prediction method. It was found that periplanetasin-5 had antimicrobial activity against yeast and grampositive and gram-negative bacteria. In the present study, we demonstrated the anti-inflammatory activities of periplanetasin-5 in mouse macrophage Raw264.7 cells. No cytotoxicity was observed at 60 μg/ml periplanetasin-5, and treatment decreased nitric oxide production in Raw264.7 cells exposed to lipopolysaccharide (LPS). In addition, quantitative RT-PCR and enzyme-linked immunosorbent assay revealed that periplanetasin-5 reduced cytokine (tumor necrosis factor-α, interleukin-6) expression levels in the Raw264.7 cells. Periplanetasin-5 controlled inflammation by inhibiting phosphorylation of MAPKs, an inflammatory signaling element, and reducing the degradation of IκB. Through LAL assay, LPS toxicity was found to decrease in a periplanetasin-5 dose-dependent manner. Collectively, these data showed that periplanetasin-5 had antiinflammatory activities, exemplified in LPS-exposed Raw264.7 cells. Thus, we have provided a potentially useful antibacterial peptide candidate with anti-inflammatory activities.

Analgesic action of Rubimaillin in vitro and in vivo

Pain, a common symptom in clinics, is a serious impediment to quality of life. The analgesic drugs presently in use have poor efficacy, and are associated with undesirable side effects. Rubimaillin (Rub) is a naphthoquinone compound extracted from Chinese herbal medicine, and it has various biological activities. In this study, the analgesic effect of Rub, and its mechanism of action were investigated using glacial acetic acid-induced mice writhing model and a mice model of neurogenic and inflammatory bipolar pain. Analgesic effects were measured in different experimental groups. In vitro, RAW 264.7 cells were used to investigate the release of nitric oxide (NO), iNOS and COX-2 protein in RAW 264.7 cells stimulated with lipopolysaccharide (LPS). The results revealed that Rub reduced the number of acetic acid-induced writhing in mice, inhibited formalin-induced biphasic pain response, and suppressed the production of NO in RAW 264.7 cells. The mechanisms involved in the analgesic and anti-inflammatory effects of rub may be related to the inhibition of cyclooxygenase-2 (COX-2), endogenous inflammatory mediators, and reduction in the content of pain-induced mediators.

A new lignan glucoside from root of Paeonia lactiflora

A new lignan glucoside,(+)-fragransin A_2-4-O-β-D-glucopyranoside(1), has been isolated from the dry root of Paeonia lactiflora by column chromatography on silica gel, Sephadex LH-20, and MCI-gel resin, as well as preparative RP-HPLC. The structure of the new compound was elucidated by spectroscopic data analysis(MS, UV, IR, CD, 1 D and 2 D NMR) and chemical method. Compound 1 showed moderate inhibition against lipopolysaccharide induced nitric oxide production in RAW264.7 macrophages, with an IC_(50) value of 21.3 μmol·L~(-1).

Anti-inflammatory xanthone derivatives from Garcinia delpyana

Two new xanthones delpyxanthone A (1) and delpyxanthone B (3), together with four known ones, gerontoxanthone I (2), α-mangostin (4), cowanin (5) and cowanol (6) were isolated from the stem bark of Garcinia delpyana. The chemical structures of 1–6 were established mainly using nuclear magnetic resonance (NMR) and mass spectrometry (MS). The anti-inflammatory activity of the isolated compounds was evaluated against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 cells in vitro. Compounds 1–4 showed significant inhibitory activity against the LPS-induced NO production in RAW264.7 cells with IC50 values ranging from 14.5 to 28.2 μM, but the others were inactive. The results suggested that G. delpyana and its constituents might be potential anti-inflammatory agents on RAW 264.7 cells.

Functionalised Flouroquinolones as a Potentially Novel Class of Anti-inflammatory and Anti-glycation Compounds; Synthesis and Pharmacological Appraisal

New synthetic 36 fluoroquinolones (FQs) have been developed. Their anti-inflammatory and 2,2-diphenyl-1-picrylhydrazyl (DPPH)- and nitric oxide (NO)- radicals scavenging propensities were delineated in vitro. The anti-inflammation related NO radical scavenging bioactivities of new FQs compounds against lipopolysaccharide (LPS)-prompted NO production in RAW 264.7 macrophages were examined using the Griess assay. Selectively nitro FQ compound 2-AnisCEtA exerted an exceedingly superior anti-inflammatory effects (p<0.001 vs. indomethacin IC50 value of 103.35±4.4 μM) while 7 nitro FQs, 10 reduced FQs and 9 triazolo FQs were moderately more efficacious than indomethacin. The remaining 9 Compounds could display appreciable anti-inflammatory capacity. Unequivocally their DPPH radical scavenging effects were of substantially lesser efficacy than ascorbic acid. Using 400 μM methylglyoxal as the choice glucotoxicity concentration in RAW264.7 macrophages; it was shown that 18 out of 36 FQs could exhibit an exceedingly more superior than or significantly comparable cytoprotection against methylglyoxal-induced carbonyl toxicity to antiglycation aminoguanidine. Suggestively dual modulation of glycation-inflammation can be linked with FQs lipophilicity-chelating properties. FQs can serve as scaffolds for the development and designing of new druggable deglycation and antiglycation therapeutic candidates via duality of antiglycation-antiinflammatory capacities.