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Antioxidant-related parameters and anti-inflammatory and antimicrobial activities against Listeria monocytogenes were assessed in eight North East Spain poplar propolis samples. Propolis extracts (PEs) were obtained using 70% ethanol (PEE) and methanol (PME). Yield and total phenol compounds were higher in PEE. Phenolic acids were analyzed by a high-performance liquid chromatograph–diode array detector. Caffeic and ferulic acids were quantified in all PEE and PME. All samples contained p-coumaric acid (quantified in 6 PEE and in 3 PME). Ascorbic acid was detected in all propolis, but mainly quantified in PME (≤0.37 mg/g PE). Biological properties were tested on PEE. As for antiradical activities, trolox equivalent antioxidant capacity (TEAC) [against 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)•+], ranged between 578 and 4620 µmol trolox/g, 2,2-diphenyl-1-picrylhydrazyl (DPPH) (against DPPH free radical), between 0.049 and 0.094 mg/mL, antioxidant activity against hydroxyl (•OH) radical (AOA), between 0.04 and 11.01 mmol uric acid/g, and oxygen radical absorbance capacity (ORAC) against peroxyl (ROO•) radical between 122 and 3282 µmol trolox/g. Results of TEAC, AOA, and ORAC were significantly correlated. IC50 anti-inflammatory activity ranged from 1.08 to 6.19 mg/mL. Propolis showed higher inhibitory activity against L. monocytogenes CECT934 and L. monocytogenes CP101 by agar well diffusion (P <.05) (10.5 and 10.2 mm, respectively) than against L. monocytogenes CP102 (7.0 mm). Data of this research show that North East Spain propolis may be of interest for pharmaceutical and food industry use. [ABSTRACT FROM AUTHOR]

Objective: Inflammation and oxidative stress are major factors in the development of many disorders. Natural antioxidants present in plants can interrupt, decrease, or reduce the oxidation of components sensitive to oxidative processes by scavenging free radicals and lowering oxidative stress. Most anti-inflammatory agents used in the management of inflammatory disorders diminish oxidative damage. The biological potential of Citrus karna Raf. remains undisclosed, despite its richness in several bioactive compounds. Methods: The methanolic extract was evaluated for quantitative phytochemical analysis and antioxidative efficacy using 1,1-diphenyl-2-picrylhydrazyl radical and hydrogen peroxide scavenging activity. A carrageenan-induced paw edema model was employed to evaluate the anti-inflammatory potential as antioxidants exert anti-inflammatory effects. In silico prediction of activity spectra for substance predictions were performed to understand the possible mechanism of action of phytochemicals. Results: Citrus karna methanolic extract (CKME) showed dosedependent radical scavenging effects. The powerful scavenging activity of CKME could be due to the diverse polyphenolic compounds such as ascorbic acid, beta-carotene, and naringin. In addition, the percentage inhibition of paw edema and swelling was observed in CKME-treated rats and mice, which is the same as that of standard drug-treated groups. The Pa value of ascorbic acid, beta-bisabolene, linalool, and naringin is more than 0.7 which shows that these phytoconstituents might contribute to the anti-inflammatory action of extract samples such as CKME. Conclusions: Our findings shows that CKME possess strong antioxidant and anti-inflammatory effects. The richness of plants in polyphenolics such as flavonoids might be a contributing factor for these potential effects. [ABSTRACT FROM AUTHOR]

The manuscript provides an overview of recent scientific reports on the properties and range of health-promoting effects of acerola (Malpighia emarginata DC) fruits and leaves. Acerola is a natural raw material that, in its unprocessed form, is known to be a rich source of vitamin C and polyphenolic compounds. For this reason, the consumption of acerola may provide a number of health-promoting benefits, particularly related to its strong anti-free radical effects. The review discusses anti-inflammatory and anticancer effects of acerola fruit and leaves as well as its therapeutic effects on selected physiological processes in the human system. Their biochemical mechanisms are also explained. Recommendations for the consumption of acerola in the prevention of inflammatory and free radical diseases are presented. The part of the article devoted to anticancer effects of acerola describes the possibilities of using the edible parts of this raw material to obtain products and preparations of potential use in cancer prevention and therapy. [ABSTRACT FROM AUTHOR]

In the present research, the impact of fermentation with two strains of Lactiplantibacillus plantarum subsp. plantarum (PTCC 1896 and PTCC 1745) on physicochemical properties, antioxidant bioactive compounds, and some health‐promoting features of guava juice was investigated. Results showed a significant (p <.05) decrease in pH, total soluble solids, glucose and fructose residues, vitamin C, and total carotenoids after 32 h of fermentation. Total phenolic content, free radical scavenging abilities, and ferrous reducing power were markedly enhanced during the fermentation process. Moreover, fermented juice represented good enzyme inhibition abilities (α‐amylase and α‐glucosidase) and anti‐inflammatory activities. The initial amount of angiotensin‐converting enzyme inhibitory activity (26.5%) increased to 72.1% and 66.4% in L. plantarum subsp. plantarum 1896 and L. plantarum subsp. plantarum 1745 treatments, respectively. These findings reveal that guava juice fermentation with the studied Lactobacillus strains can be a promising strategy to augment the functional properties of the fruit‐based beverage. [ABSTRACT FROM AUTHOR]

The 1,3,4-oxadiazole derivatives Ox-6a-f have been synthesized by incorporating flurbiprofen moiety with the aim to explore the potential of target molecules to decrease the oxidative stress. The title compounds Ox-6a-f were prepared by simple reactions in which a flurbiprofen –COOH group was esterified with methanol in an acid-catalyzed medium, which was then reacted with hydrazine to afford the corresponding hydrazide. The acid hydrazide was then cyclized into 1,3,4-oxadiazole-2-thiol by reacting with CS2 in the presence of KOH. The title compounds Ox-6a-f were synthesized by the reaction of an –SH group with various alkyl/aryl chlorides, which involves an S-alkylation reaction. The structures of the synthesized Ox-6a-f derivatives were ascertained by spectroscopic data. The in silico molecular docking was performed against target proteins cyclooxygenase-2 COX-2 (PDBID 5KIR) and cyclooxygenase-1 COX-1 (PDBID 6Y3C) to determine the binding affinity of the synthesized compounds with these structures. It has been inferred that most of the synthesized compounds bind well with an active binding site of 5KIR compared to 6Y3C, and especially compound Ox-6f showed excellent binding affinity (7.70 kcal/mol) among all synthesized compounds Ox-6a-f. The molecular dynamic (MD) simulation has also been performed to check the stability of docking complexes of ligands with COX-2 by determining their root mean square deviation and root mean square fluctuation. Little fluctuation was observed in case of Ox-6f, which forms the most stable complex with COX-2. The comprehensive antioxidant potential of the synthesized compounds has been evaluated by determining their free radical scavenging activity, including DPPH, OH, nitric oxide (NO), and iron chelation assay. The derivative Ox-6f showed promising results with 80.23% radical scavenging potential at a dose of 100 µg/mL while ascorbic acid exhibited 87.72% inhibition at the same dose. The anti-inflammatory activity of the final products has also been performed, and inflammatory markers were assayed, such as a thiobarbituric acid-reducing substance, nitric oxide, interleukin-6 (IL-6), and COX-2. The derivatives Ox-6d and Ox-6f displayed higher anti-inflammatory activity, exhibiting 70.56% and 74.16% activity, respectively. The results were compared with standard ibuprofen, which showed 84.31% activity at the same dose, 200 µg/mL. The anti-inflammatory potential has been performed by following the carrageen-induced hind paw edema model, and results showed that derivative Ox-6f exhibited 79.83% reduction in edema volume compared to standard ibuprofen, which reduced 84.31% edema volume. As dry lab and wet lab results confirm each other, it has been deduced that derivative Ox-6f may serve as the lead structure to design potent compounds to address oxidative stress. [ABSTRACT FROM AUTHOR]

Introduction: Herbal products have been widely used for the treatment of diseases throughout the ages. In this research, we investigated antioxidant, antibacterial, anti-adipogenic, and anti-inflammatory activities of methanolic extracts of five ethnomedicinally important plants; namely, Alnus nepalensis, Dryopteris sparsa, Artocarpus lacucha, Litsea monopetala, and Lyonia ovalifolia. Methods: We investigated the DPPH free radical scavenging potential, sensitivity of selected bacterial strains towards the extracts using a disc diffusion assay, anti-inflammatory activity in RAW-264.7 cells, and anti-adipogenic activity by the ORO assay in 3T3-L1 preadipocytes. Results and discussion: The extract of A. nepalensis showed significant antioxidant activity (IC50=4.838 μg/mL), followed by A. lacucha, L. monopetala, and L. ovalifolia, exhibiting comparable IC50 values to that of ascorbic acid (IC50=5.063 μg/mL). Alnus nepalensis also showed good antibacterial activity in disc diffusion methods, with remarkable zones of inhibition in A. baumannii (14.66 mm) and P. mirabilis (15.50 mm) bacterial species. In addition, A. nepalensis was found to increase adipogenesis in 3T3-L1 cells, evidenced by increased lipid deposition in differentiated 3T3-L1 cells. A similar pattern of increased adipogenesis was observed on treatment with L. ovalifolia extracts. On the other hand, A. lacucha effectively reduced lipid deposition in 3T3-L1 cells at 100 μg/mL (75.18± 6.42%) by inhibiting adipogenesis, showing its potential use in the management of obesity. Furthermore, A. lacucha 100 μg/mL (15.91± 0.277 μM) and L. monopetala 75 μg/mL (12.52± 0.05 μM) and 100 μg/mL (11.77± 0.33 μM) significantly inhibited LPS-induced nitric oxide production in RAW 264.7 cells. Also, A. nepalensis and L. ovalifolia inhibited NO production significantly, endorsing their anti-inflammatory potential. Conclusion: The findings from these in-vitro studies suggest that the selected five plants possess remarkable antioxidant, antibacterial, anti-adipogenic, and anti-inflammatory activities. This study opens the door to conduct further advanced in-vivo experiments to find possible lead compounds for the development of valuable therapeutic agents for common health problems. [ABSTRACT FROM AUTHOR]

Litsea belonging to the family Lauraceae, is among the most diverse genera of evergreen shrubs and trees. Litsea is distributed majorly in the Western Ghats of India. Litsea are traditionally used to treat cold, fever, bruises, insect bites and other diseases. The objective of this study was to understand the phytochemistry of the methanol extract of Litsea ghatica stem bark and evaluate it for potential antioxidant activity in an effort to understand the nature of phytoconstituents present in the stem bark. Phytochemical screening of the methanol extract indicated the presence of tannins, phenols, flavonoids, saponins and carbohydrates. The total phenolic and flavonoid content in the methanol extract was determined by Folin Ciocalteau's and aluminum chloride methods, respectively. The antioxidant activity of the methanol extract was evaluated by 2,2-diphenyl-1-picrylhydrazyl, ferric reducing antioxidant power and NO radical scavenging assays. The methanol extract showed significant potential antioxidant activity, namely 93.08 and 95.1 % radical scavenging activity in DPPH assay at 100 ppm for the methanol extract and ascorbic acid, respectively. In FRAP and NO radical scavenging assay, the methanol extract showed dose dependent antioxidant activity reaching maximum at 100 ppm concentration. The anti-inflammatory activity was determined by in vitro albumin denaturation assay using naproxen as the reference standard. The results indicated encouraging anti-inflammatory activity with 18.53% inhibition at 60 ppm of the methanol extract. This preliminary anti-inflammatory data needs to be substantiated with additional in vitro and in vivo studies for conclusive evidence. [ABSTRACT FROM AUTHOR]

Present work involves the green and environmentally benign synthesis of 1,5-benzodiazepines using iodine as a catalyst and PEG-400 as a green solvent at room temperature that gives an excellent yield of products. All the synthesized compounds were screened for their anti-inflammatory, antioxidant, and antidiabetic activity. All the synthesized compounds showed excellent antioxidant activity against DPPH and H2O2 radicals as compared to standard ascorbic acid and even more than standard for SOR and NO radicals. Compound 5h showed the highest % anti-inflammatory activity i.e., 80.73% among the series that was comparable to standard diclofenac sodium whereas compound 5d showed the highest antidiabetic activity i.e., 60.46% which was found potent as compared to standard acarbose. [ABSTRACT FROM AUTHOR]

Traditional Chinese medicine (TCM) has been used for centuries to treat various types of inflammation and tumors of the digestive system. Portulaca oleracea L. (POL), has been used in TCM for thousands of years. The chemical composition of POL is variable and includes flavonoids, alkaloids, terpenoids and organic acids and other classes of natural compounds. Many of these compounds exhibit powerful anti-inflammatory and anti-cancer-transforming effects in the digestive system. In this review, we focus on the potential therapeutic role of POL in NASH, gastritis and colitis and their associated cancers, with a focus on the pharmacological properties and potential mechanisms of action of the main natural active compounds in POL. The information and data on Portulaca oleracea L. and its main active ingredients were collated from various resources like ethnobotanical textbooks and literature databases such as CNKI, VIP (Chinese literature), PubMed, Science Direct, Elsevier and Google Scholar (English literatures), Wiley, Springer, Tailor and Francis, Scopus, Inflibnet. Kaempferol, luteolin, myricetin, quercetin, genistein, EPA, DHA, and melatonin were found to improve NASH and NASH-HCC, while kaempferol, apigenin, luteolin, and quercetin played a therapeutic role in gastritis and gastric cancer. Apigenin, luteolin, myricetin, quercetin, genistein, lupeol, vitamin C and melatonin were found to have therapeutic effects in the treatment of colitis and its associated cancers. The discovery of the beneficial effects of these natural active compounds in POL supports the idea that POL could be a promising novel candidate for the treatment and prevention of inflammation-related cancers of the digestive system. The discovery of the beneficial effects of these natural active compounds in POL supports the idea that POL could be a promising novel candidate for the treatment and prevention of inflammation-related cancers of the digestive system. However, clinical data describing the mode of action of the naturally active compounds of POL are still lacking. In addition, pharmacokinetic data for POL compounds, such as changes in drug dose and absorption rates, cannot be extrapolated from animal models and need to be measured in patients in clinical trials. On the one hand, a systematic meta-analysis of the existing publications on TCM containing POL still needs to be carried out. On the other hand, studies on the hepatic and renal toxicity of POL are also needed. Additionally, well-designed preclinical and clinical studies to validate the therapeutic effects of TCM need to be performed, thus hopefully providing a basis for the validation of the clinical benefits of POL. [Display omitted] • POL is a traditional plant that can treat cancers associated with inflammation of the digestive system. • POL exerts its functions in relation to its active ingredients kaempferol, luteolin, myricetin, quercetin, genistein, EPA, DHA, melatonin, apigenin, genistein, lupeol, vitamin C and others. • The natural active ingredients in POL exhibit primarily antioxidant and anti-inflammatory responses, inhibiting the transformation of inflammation into cancer. [ABSTRACT FROM AUTHOR]

Habb-e-Suranjan (HES), an Unani formulation, has been studied for its anti-inflammatory properties in both in vitro and in vivo experiments. HES is recommended for arthritis, gout, and joint pain. The current endeavor is an attempt to put it to the test and verify its efficacy scientifically. It was tested for DPPH, hydroxyl, and nitric oxide scavenging activities. It was shown that HES had the greatest TAC and FRAC values when compared to catechin and ascorbic acid. HES exhibited DPPH and hydroxyl radical scavenging activity that was dose-dependent. Incubation of sodium nitroprusside solutions in PBS at 25°C for 150 min resulted in the production of nitric oxide. Nitric oxide production was effectively decreased by HES. Anti-inflammatory medications boosted the migration of PMN cells toward the chemoattractant FMLP in an agarose experiment of PMN chemotaxis. In carrageenan-induced rat paw edema, in the HES-treated group, paw thickness was 3.021 ± 0.084 at t = 0 , but it showed an increase in paw inflammation after one hour, i.e., 3.195 ± 0.082 cm which again showed a decrease in paw thickness up to 4th hour, i.e., 3.018 ± 0.078 , 2.98 ± 0.032 , and 2.684 ± 0.061 at t = 2 , 3, and 4, respectively. It showed again getting back to the normal thickness of paw at t = 24 hrs, i.e., 3.029 ± 0.118 cm. It is concluded that the formulation is potent enough and can be used effectively for the treatment of inflammation and associated health issues. Moreover, there is much scope to evaluate its effectiveness using different in vitro and in vivo models. [ABSTRACT FROM AUTHOR]

Psychotria densinervia hydro-ethanolic leaf extract (PHELE) and bark extract (PHEBE) were evaluated for antioxidant, anti-inflammatory, and inhibition of digestive enzymes activities. The antioxidant activity was characterized by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), total phenolic content (TPC), and total flavonoid content (TFC) assays. The anti-inflammatory activity was characterized by protein denaturation and antiproteinase tests, while the inhibition of the enzymes was assessed using α-amylase, α-glucosidase, lipase, and cholesterol esterase activities. PHELE presented low (p < 0.001) IC50 (59.09 ± 5.97 μg/ml) for DPPH compared with ascorbic acid (71.78 ± 6.37 μg/ml) and PHEBE (115.40 ± 1.21 μg/ml). The IC50 of PHELE (262.4 ± 4.46 μg/ml) and PHEBE (354.2 ± 1.97 μg/ml) was higher (p < 0.001) than that of catechin (33.48 ± 2.02 μg/ml) for ABTS. PHELE had high (p < 0.001) FRAP (341.73 ± 21.70 mg CE/g) than PHEBE (150.30 ± 0.32 mg CE/g). PHELE presented (p < 0.001) high TPC (270.05 ± 7.53 mg CE/g) and TFC (23.43 ± 0.032 mg CE/g) than PHEBE (TPC: 138.89 ± 0.91 and TFC: 20.06 ± 0.032 mg CE/g). PHELE showed antiprotein denaturation with IC50 (257.0 ± 7.51 μg/ml) (p < 0.001) and antiproteinase activity (74.37 ± 1.10 μg/ml) lower than PHEBE (316.1 ± 6.02 μg/ml and 177.6 ± 0.50 μg/ml), respectively. Orlistat inhibited lipase (p < 0.001) activity with IC50 (37.11 ± 4.39 μg/ml) lower than PHELE and PHEBE (50.57 ± 2.89 μg/ml and 62.88 ± 1.74 μg/ml, respectively). PHELE inhibited cholesterol esterase with IC50 (34.75 ± 3.87 μg/ml) lower than orlistat (54.61 ± 2.56) and PHEBE (80.14 ± 1.71 μg/ml). PHELE inhibited α-amylase IC50 (6.07 ± 4.05 μg/ml) lower than PHEBE (19.69 ± 6.27 μg/ml) and acarbose (20.01 ± 2.84 μg/ml). Acarbose inhibited α-glucosidase (p < 0.001) activity with IC50 (4.11 ± 3.47 μg/ml) lower than PHELE (24.41 ± 2.84 μg/ml) and PHEBE (38.81 ± 2.46 μg/ml). PHELE presented better antioxidant, anti-inflammatory, and enzyme inhibition activity than PHEBE. [ABSTRACT FROM AUTHOR]

Vitamin C (VC), widely found in vegetables and fruits, operates as an electron donor to perform various biological functions including anti-inflammatory activity. However, the mechanisms by which VC inhibits inflammation remain insufficiently understood. Accordingly, we performed a detail mechanistic study on anti-inflammatory activity of VC at millimolar (pharmacological) concentrations in lipopolysaccharides-stimulated RAW264.7 cells. It was found that VC and its two-electron oxidative product, dehydroascorbate (DHA) constructs an efficient redox cycle with the aid of intracellular glutathione and copper ions, thereby facilitating the generation of reactive oxygen species (ROS) and the ROS-dependent inhibition against the NF-κB-mediated inflammation. [Display omitted] • Mechanisms by which VC at pharmacological concentrations inhibits inflammation are identified. • VC and DHA constructs a redox cycle with the aid of intracellular glutathione and Cu(II) ions. • The redox cycle facilitates the ROS generation. • VC inhibits against the NF-κB-mediated inflammation via the ROS generation. [ABSTRACT FROM AUTHOR]

A green and efficient one-pot has been developed for the synthesis of a series of new diethyl-(((2,3-dihydrobenzo[b][1, 4] dioxin-6yl)amino)(substituted phenyl)methyl) phosphonates (4a-k) by the Kabachinik-Fields reaction of 2,3-dihydrobenzo[b] [1, 4]dioxin-6-amine (1) with various substituted aldehydes (2a-k) and diethyl phosphite (3) using nano ferrite supported glutathione (nano FGT) as catalyst under microwave irradiation and solvent free conditions. The synthesized compounds were evaluated for their antioxidant (DPPH & FRAP) and anti-inflammatory activity studies. Compounds 4b (naphthyl) and 4k (9-anthracenyl) showed highest antioxidant activity than that of standard ascorbic acid in DPPH method. Whereas compounds 4f (3-nitrophenyl), 4h (3-phenoxyphenyl) and 4k (9-anthracenyl) exhibited low IC50 values than that of standard ascorbic acid in and in Ferric Reducing Antioxidant Power (FRAP) studies. Compounds 4a, 4b, 4h, 4i, and 4k have shown strong anti-inflammatory activity against LPS induced cell death in RAW 264.7 cell lines. Molecular docking studies were also carried out against COX-2 showed high binding energies that are in support of their high anti-inflammatory activity. Being the most bioactive compound (4k) stands as promising next future anti-oxidant and anti-inflammatory agent. [ABSTRACT FROM AUTHOR]

A new series of 1-Thiazolyl-2-Pyrazolines 5a-g was accomplished by reacting pyrazolealdehyde with an appropriate aromatic ketone in the presence of PEG-300 as a solvent to yield chalcone. The chalcones reacted with thiosemicarbazide to yield asymmetric 1-thiocarbamoyl pyrazoles. The above formed 1-thiocarbamoyl pyrazoles reacted with appropriate α- haloketones to yield 1-Thiazolyl-2-Pyrazolines. The structural interpretations of newly formed compounds were done by 1H NMR, 13CNMR, IR and mass spectroscopic methods. The newly prepared asymmetric 1-Thiazolyl-2-pyrazoline derivatives were evaluated to their in vitro antioxidant (H2O2, DPPH, SOR and NO radical inhibiting activity) as well as anti-inflammatory activity. The 1-Thiazolyl-2-pyrazoline derivatives 5a-g exhibited moderate to good H2O2 scavenging activity as match up to ascorbic acid. All the 1-Thiazolyl-2-pyrazoline derivatives exhibited excellent SOR scavenging activity except 5 b. All the tested compounds have shown good to excellent, NO radical inhibiting activity. DPPH radical scavenging activity results have shown low antioxidant activity. Also, all the 1-Thiazolyl-2-pyrazoline derivatives were tested for their in vitro anti-inflammatory activity. The compounds 5a, 5 b, 5c, 5f and 5 g were exhibited good anti-inflammatory activity and 5d showed moderate activity while 5e less active as match up to diclofenac sodium as a standard reference. [ABSTRACT FROM AUTHOR]

Bamboo is a perennial, woody grass, belonging to the Poaceae Family. Different bamboo species have been found to have therapeutic applications and studies have shown that bamboo have medicinal uses such as anti-cancer activity, anti-oxidant activity, antimicrobial activity, anti-diabetic activity, anti-inflammatory activity, anti-fertility activity and antihypertensive. In this study, fermented bamboo was used for extraction of phytochemicals and analysis of their antimicrobial and antioxidant activity. The extract was characterized by FTIR. The acetone and methanol extracted yield of 25.78% and 31.08% respectively. The scavenging activity with ascorbic acid for methanol showed 17.3 % for 10 mg/ml whereas no activity for acetone. But extract showed antimicrobial and antioxidant activity. [ABSTRACT FROM AUTHOR]

The Myrciaria dubia (Myrtaceae) fruit is traditionally used to treat malnutrition due to its high levels of vitamin C and phenolic compounds. Because of its composition, this plant is very promising in the research of novel natural treatment for pain disorders. This study analyzed the phytochemical profile of M. dubia juice and assessed its antinociceptive and antiedematogenic potential. The phytochemical profile was determined through high-performance liquid chromatography (HPLC), the oral antinociceptive effect of M. dubia 50% juice (Md50) was evaluated by formalin, hot plate and Complete Freund's Adjuvant tests and the antiedematogenic activity by paw edema. HPLC revealed the presence of ascorbic acid, rutin, and ellagic acid as major compounds. Md50 showed an antinociceptive effect in the acute and chronic phases of the formalin test. In the hot plate test, Md50 also induced an antinociceptive effect of 0.5 up to 6 h, showing antinociceptive and antiedematogenic potential without changing the spontaneous locomotion of animals. All protocols were submitted and approved by the Ethics Committee for use of Animals of the Lutheran University of Brazil (protocol No. 2013-30P). [ABSTRACT FROM AUTHOR]

Background and Aim Deferasirox (Exjade) is an iron-chelating drug used in patients with beta-thalassemia major. Oxidative stress is among f the major causes of nephrotoxicity and its progression. Deferasirox, due to oxidative stress and increased cell apoptosis causes the dysfunction of renal tubules and renal toxicity. According to its antioxidant and anti-inflammatory properties, the present study explored the effect of vitamin C on deferasirox-induced kidney damage. Methods & Materials This study was performed on 30 Wistar rats in 3 groups of control, deferasirox, and deferasirox plus vitamin C. To induce the nephrotoxicity, the intra-peritoneum injection of deferasirox (75 mg/kg/day) was used. After taking plasma from the blood samples of the explored rats, we determined the values of Cr, Na+, K+, Mg+, osmolality, and BUN in the obtained plasma and urine samples. The creatinine clearance, as well as the relative and absolute excretion of sodium and potassium, were also calculated. After separating the two kidneys, they were used for the histologic study with Hematoxylin and Eosin (H&E) staining, as well as Malondialdehyde (MDA) and Ferric Reducing Antioxidant Power (FRAP) biochemical studies. Ethical Considerations This study was approved by the Research Ethics Committee of Arak University of Medical Sciences (Code: IR.ARAKMU.REC.1396.309). Results Cotreatment with deferasirox and vitamin C reduced renal tissue MDA and relative and absolute Na and K excretion and urine osmolarity; this method also increased creatinine clearance and renal tissue FRAP. Conclusion The co-administration of vitamin C presented a significant protective effect on the renal toxicity induced by deferasirox. The protective property of deferasirox is because of the antioxidant impacts of vitamin C in reducing oxidative stress and lipid peroxidation. [ABSTRACT FROM AUTHOR]

Atriplex lindleyi Moq. subsp. inflata from Algeria is known for its traditional use for therapeutic properties. We analysed quantitatively and qualitatively the infusion and diethyl ether, n-butanol and ethereal extracts of A. lindleyi , as well as assessed their acute toxicity, anti-inflammatory, antinociceptive and antioxidant activities. The total phenolic and flavonoid contents were quantified. The anti-inflammatory effect was assessed using a carrageenan-induced paw oedema assay and the antinociceptive effect was evaluated using an acetic acid-induced writhing method. In addition, antioxidant activity was examined by three tests: DPPH, reducing power and phenanthroline assays. The quantity of total phenols in the roots of A. lindleyi was larger than in the aerial parts, while the amounts of total flavonoids were larger in the aerial parts than in the roots. The HPLC profiles allowed us to identify 32 compounds belonging to the phenolic acid and flavonoid classes. Intraperitoneal administration of the infusions and phenolic extracts in mice did not cause any symptoms of toxicity or mortality. Results revealed that the aerial parts and roots of A. lindleyi had potential anti-inflammatory and antinociceptive activities and were higher than diclofenac and paracetamol, respectively. The diethyl ether extract (DEE) of aerial parts and roots showed the greatest antioxidant activity in comparison to the other tested extracts. The phenolic composition attempted to be identified by HPLC confers this plant's pharmacological potential. The antioxidant potential may be due to active ingredients, including ascorbic acid, in the two studied parts of A. lindleyi , which is a bioactive molecule with strong antioxidant properties. Also, detecting salicylic acid, the active antinociceptive ingredient of aspirin, gallic and ferulic acids may justify this subspecies' antinociceptive and anti-inflammatory potentials. [Display omitted] [ABSTRACT FROM AUTHOR]

Three new phenolic glycosides (1 – 3) and a new lignan glycoside (4), together with five known compounds (5 – 9) were isolated from the ethanol extract of the aerial part of Gaultheria leucocarpa var. yunnanensis (Franch.) T.Z.Hsu & R.C.Fang. Their structures were determined on the basis of spectroscopic techniques, experimental and calculated ECD spectra, acid hydrolysis, and enzymatic hydrolysis experiments. All the isolates were evaluated for their anti-inflammatory and antioxidant activities. Compounds 7 and 8 exhibited inhibitory effects against the LPS-induced production of NO with IC 50 of 63.71 and 10.66 μM, respectively, compared to L-NMMA having an IC 50 of 6.95 μM. Besides, compound 7 also represented significant DPPH radical scavenging activity with EC 50 of 18.75 μM, comparable with vitamin C (EC 50 = 15.77 μM). [Display omitted] • Four new (1 – 4) and five known (5 – 9) compounds were isolated from Gaultheria leucocarpa var. yunnanensis. • Compounds 7 and 8 exhibited moderate inhibition against LPS-induced NO production. • Compound 7 showed a comparable DPPH radical scavenging effect to vitamin C. [ABSTRACT FROM AUTHOR]

Synthesis, characterization, antimalarial, antioxidant, anti-inflammatory, molecular docking, DFT, MESP and ADMET studies of thiosemicarbazone ligands-based transition metal(II) complexes. [Display omitted] • Synthesis of new Co(II), Ni(II), Cu(II), Zn(II) complexes from thiosemicarbazone ligands. • Characterization of complexes was done by various analytical techniques. • In vitro antimalarial, antioxidant and anti-inflammatory activities were analyzed. • The Zn(II) complexes (6, 10) were found highly active for biological activities. • Molecular docking, DFT, MESP and ADMET studies were executed to support the in vitro results. Enticed by the current scenario of infectious diseases, eight new Co(II), Ni(II), Cu(II), Zn(II) complexes of thiosemicarbazone ligands were synthesized from benzaldehyde derivatives and 4-(3-fluorophenyl)-3-thiosemicarbazide to ascertain an effective drug for malarial, oxidant, inflammation causing deformities. The compounds (1–10) were characterized by numerous spectral and physical methods which revealed that the complexes have octahedral geometry, amorphous in nature and thermally stable. The antimalarial, antioxidant and anti-inflammatory data highlights that all the compounds (1–10) are remarkably active for malformations of these diseases; and the complexes (5), (6), (10) shows more efficacy to control these ailments while the zinc(II) complex (6) has the highest ability to control the malarial and oxidant dysfunctions with IC 50 value 0.95 ± 0.02 and 2.25 ± 0.06 µM, respectively whereas complexes (6, 10) are highly active for inflammation with IC 50 value 6.86 ± 0.07–7.86 ± 0.01 µM which are comparable with standard drugs (quinine, ascorbic acid and diclofenac sodium). Furthermore, the molecular docking, DFT, MESP and ADMET studies were executed to support the higher antimalarial potency of HL1 ligand (1) and its complexes (3–6) which revealed that the complexes have frequent biological response than their respective ligand (1); and Zn(II) complex (6) is highly efficient for malaria and its effects with various significant computational results like binding interaction, binding energy, binding power, reactivity, no degradation, no carcinogenicity etc. [ABSTRACT FROM AUTHOR]

Background and aim: Defrasirox (Exjade) is an iron chelating drug used in patients with beta thalassemia major. Oxidative stress is one of the most important causes of nephrotoxicity and its progression. Defecirox due to oxidative stress and increased cell apoptosis causes dysfunction of renal tubules and renal toxicity. In this study, according to the antioxidant and anti-inflammatory properties, the effect of vitamin C on kidney damage caused by defrasirox was investigated. Material and methods: This study was performed on 30 Wistar rats in three groups, control group, Deferasirox group and Deferasirox with vitamin C group. Inorder to induce the nephrotoxicity, intra-peritoneum injection of deferasirox(75 mg/kg/day) has been used. After taking plasma from blood samples of the rats, the determination of values of [17]Cr], [Na+], [K+], [Mg+], osmolality, [BUN] in plasma and urine samples performed. The creatinine clearance, relative and absolute excretion of sodium and potassium have been calculated. After separating the two kidneys, they used for histologic study with H&E staining and, MDA and FRAP bichemical study. Results: Cotreatment with deferasirox and vitamin C, reduced renal tissue MDA and relative and absolute Na and K excretion and urine osmolarity also increased creatinine clearance and renal tissue FRAP . Conclusion: Co treatment adminstration of vitamin C has a significant protective effect on the renal toxicity induced by defacirox. The protective ability of deferasirox is because of the antioxidant properties of vitamin C in reducing oxidative stress and reducing lipid peroxidation. [ABSTRACT FROM AUTHOR]

Stink bean (Parkia speciosa Hassk.) grows naturally in tropical regions like Thailand, Malaysia, Indonesia and Philippines. Seed are beneficial as local food and traditional medicine for various treatments. Aims of this study were to evaluate antioxidant activities of stink bean seed dichloromethane and ethanol extracts by DPPH radical scavenging, lipid peroxidation inhibition and nitric oxide radical scavenging assays; and to evaluate in vitro anti-inflammatory activity. Fresh seeds were removed from pods and prepared in powder form, which was extracted by maceration. Total phenolic content (TPC) measurement stink bean seed extracts were done by Folin-Ciocalteu method. DPPH radical scavenging, lipid peroxidation inhibition and NO radical scavenging activity of extracts were evaluated and compared with butylated hydroxytoluene (BHT), α-tocopherol and ascorbic acid, respectively. In vitro inflammatory activity of extracts was evaluated and compared with Diclofenac diethylammonium. Dichloromethane extract (98.43±0.71 mg GAE/100 g) from stink bean seed was higher TPC than ethanol extract (62.01±0.03 mg GAE/100 g). Dichloromethane was exhibited DPPH radical scavenging, lipid peroxidation inhibition and in vitro anti-inflammatory activities; and IC50 were 43.43±3.34, 0.77±0.20 and 428.63±87.33 mg/ml, respectively. While, ethanol extract was exhibited DPPH radical scavenging and NO scavenging activities with IC50 were 46.38±7.14 and 58.00±10.76 mg/ml, respectively. It was implied that seed was exhibited anti-inflammatory activity in hydrophobic condition. This preliminary finding may useful data on different of antioxidant activities and anti-inflammatory activity of stink bean seed extract in different conditions. [ABSTRACT FROM AUTHOR]

Background: Whether hydrocortisone, vitamin C, and thiamine treatment can reduce the mortality of patients with sepsis is controversial.Research Question: To evaluate the efficacy and safety of hydrocortisone, vitamin C, and thiamine combination treatment for patients with sepsis or septic shock (HYVCTTSSS).Study Design and Methods: This single-blind, randomized controlled trial evaluated treatment with hydrocortisone (50 mg every 6 h for 7 days), vitamin C (1.5 g every 6 h for 4 days), and thiamine (200 mg every 12 h for 4 days) vs placebo (normal saline) in patients with sepsis. The intention-to-treat analysis was used. Primary outcome was 28-day all-cause mortality, and secondary outcomes were organ protection, procalcitonin reduction, and adverse events related to hydrocortisone, vitamin C, and thiamine.Results: Eighty patients were randomized to receive combination treatment (n = 40) or normal saline (n = 40). No difference in 28-day all-cause mortality was observed (27.5% vs 35%, respectively; P = .47); however, treatment was associated with a significant improvement of 72-h change in Sequential Organ Failure Assessment score (P = .02). In adverse events analysis, the treatment group exhibited more incidents of hypernatremia (P = .005). In prespecified subgroup analysis, patients of the treatment subgroup diagnosed with sepsis within 48 h showed lower mortality than those in the control subgroup (P = .02). The study was terminated after the midterm analysis.Interpretation: Among patients with sepsis or septic shock, the combination of hydrocortisone, vitamin C, and thiamine did not reduce mortality compared with placebo.Trial Registry: ClinicalTrials.gov; No.: NCT03258684; URL: www.clinicaltrials.gov. [ABSTRACT FROM AUTHOR]

Background: The purpose of the study described here was to evaluate the effects of different supportive treatments - such as antioxidants, immunomodulators, and nonsteroidal anti-inflammatory drugs (NSAIDs) - in mastitic cows treated with intramammary antibiotics on the efficacy of mastitis therapy and fertility indices. Fertility indices, including time to first insemination, conception rate, time between calving and conception (open days), and number of services per conception (insemination index), were evaluated for 300 dairy cows. Sixty cows without apparent clinical signs of mastitis were assigned 100 days after calving to a Control group. Another 240 cows with clinical mastitis were systematically divided into four experimental groups (I–IV) of 60 cows each. All mastitic cows were treated with approved intramammary antibiotics in recommended doses. Cows in Group I were treated with intramammary antibiotics only. Cows in Groups II, III, and IV, received intramammary antibiotic therapy and a single injection with antioxidants, an immunomodulator (lysozyme dimer), or an NSAID (flunixin meglumine), respectively. Results: The lowest treatment efficacy of mastitic quarters and cows was noted in Group I (51.6 and 53.3%; p > 0.05). The best recovery rate was noted in Group II (63.3 and 66.7%; p > 0.05), followed by Group III (58.3 and 60.9%) and Group IV (58.3 and 58.0%; p > 0.05). The above data did not differ statistically (p > 0.05). The animals with mastitis (Groups I–IV) showed prolonged time to first insemination, more open days, higher insemination index, and lower conception rate than the control cows (p < 0.05). The conception rate of healthy cows and of successfully treated cows was insignificantly lower than that of cows required prolonged antibiotic therapy. Supportive treatments improved the mastitis recovery rate compared with intramammary antibiotics only. The efficacy of mastitis treatments affected the reproduction indices: in cows requiring prolonged treatment with antioxidants, a shorter time to first insemination was needed than in other groups (p < 0.05). Fewer days open were observed between the group with antioxidants and the control group (p < 0.05). Conclusions: Clinical mastitis negatively affects reproductive indices (days open, pregnancy rate after first AI, NSC) in dairy cows. Different types of supportive medicine, such as antioxidants (vitamin C and E, and β-carotene), lysozyme dimer, or NSAID can be useful in improving fertility in mastitis cows treated with antibiotic only. It has been proven that each supportive treatment improved antibiotics efficiency and the antibiotic combined with the antioxidants was the most effective treatment. [ABSTRACT FROM AUTHOR]

The impact of feijoa convective drying on the physicochemical characteristics, polyphenol content, antioxidant capacity, and anti-inflammatory activity, as well as the drying parameters (energy consumption and drying rate), were tested. Feijoa fruit slices were dried at 50, 60, and 70 °C, at air velocities of 0.5 and 1 m/s, and at thicknesses of 0.003 m and 0.005 m. The aqueous extracts were used for the determination of bioactivity. Anti-inflammatory activity was determined from the ability of the extracts to counteract and enhance the expression of pro- and anti-inflammatory genes in human THP-1 cells. The best operational drying parameters were found by means of response surface methodology and desirability function. High temperatures, high air velocities and thinner slices obtained the best results for colour, water activity, antioxidant capacity, anti-inflammatory activity and drying rate. Low temperatures, high air velocities, and thinner slices were suitable for the retention of polyphenols, vitamin C, and antioxidant capacity. The optimal conditions were 50.83 °C, 1 m/s air velocity, and 0.003 m thickness. The results indicate that convective drying is a suitable and cost-effective technique to generate functional ingredients while conserving biocompounds and biological activities. • RSM is used to study drying impact on quality and bioactivity properties. • Dried feijoa extracts retain biocomponents, useful in food and pharma. • Convective drying allowed a polyphenols retention of 90%. • Dried feijoa showed antioxidant capacity and anti-inflammatory activity. • Low temperatures improved bioactivity retention. [ABSTRACT FROM AUTHOR]

Hyperglycemia-induced inflammation can greatly increase the risk of periodontal disease in people with diabetes. Low-level laser irradiation (LLLI) has been used for wound healing and anti-inflammation in many cases, and LLLI is known to inhibit the lipopolysaccharide (LPS)-stimulated inflammatory response. However, the therapeutic effect of LLLI in diabetes patients with periodontitis remains unknown. In this study, we cultured human gingival fibroblasts (HGFs) in high-glucose medium (35 mM) to mimic a hyperglycemic environment, and then measured the anti-inflammatory effect of LLLI by assessing the expression of pro-inflammatory genes including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, and IL-8 by quantitative real-time polymerase chain reaction. The results demonstrated no significant inflammatory response in HGFs cultured in mannitol medium and in those treated only with LLLI. However, HGFs cultured only in high-glucose medium showed significantly higher expression of pro-inflammatory cytokine than in those treated together with LLLI. We then observed that LLLI reduced the expression of pro-inflammatory cytokines in HGFs cultured in high-glucose medium by modulating cAMP signaling. We also investigated whether antioxidant (vitamin C) treatment reduced the inflammatory effect of oxidative stress in HGFs cultured in high-glucose medium but found no additive effect upon co-treatment with LLLI, suggesting that LLLI may activate cAMP signaling, but not reactive oxygen species (ROS) signaling, to reduce the high glucose-induced inflammation. In conclusion, LLLI may have an anti-inflammatory effect on HGFs in a high glucose environment and may benefit the treatment of periodontal disease in diabetes patients. [ABSTRACT FROM AUTHOR]

The phytochemical study of the ethanol extract of the leaves and twigs of Rhododendron decorum afforded a new ascorbic acid derivative (1), a new ionone analogue (2), a new ursane-type triterpenoid glucoside (3), and four known compounds (4−7). The structures were elucidated by spectroscopic analyses, including HRESIMS, 1D, and 2D NMR. The anti-neuroinflammatory activities of the compounds were evaluated by measuring inhibitory effects of LPS-induced NO production in BV2 cells. [ABSTRACT FROM AUTHOR]

Aim: Aim of this study was to investigate the influence of an anti‐inflammatory diet on different parameters in patients with gingivitis. Materials and Methods: Thirty patients were randomly allocated to an experimental and a control group stratified by their plaque values. The experimental group had to change to a diet low in processed carbohydrates and animal proteins, and rich in omega‐3 fatty acids, vitamin C, vitamin D, antioxidants, plant nitrates and fibres for 4 weeks. The control group did not change their diet. Both groups suspended interdental cleaning. Periodontal parameters were assessed by a blinded dentist. Serological and subgingival plaque samples were taken at baseline and end. Results: While there were no differences regarding the plaque values, the experimental group showed a significant reduction in gingival bleeding (GI Baseline: 1.04 ± 0.21, GI End: 0.61 ± 0.29, p < 0.05), a significant increase in Vitamin D values and a significant weight loss. There were no inter‐group differences regarding the inflammatory serological parameters, the serological omega fatty acids, nor the subgingival microbiome composition. Conclusion: The evaluated diet could significantly reduce gingivitis in a clinically relevant range, while serological inflammatory parameters and the subgingival microbiome seem to be unaffected in this study duration. (German Clinical Trials Register; DRKS00009888). [ABSTRACT FROM AUTHOR]

A new series of functionalized fused pyridines 4(a–i) and fused pyrido[2,3‐d]pyrimidines 8(a–c) were designed and synthesized through a multi‐component reaction where in pyridine ring formation step plays a key role. All the newly formed compounds were well characterized by spectral techniques such as FTIR, 1HNMR, 13CNMR, HRMS and XRD. The potential therapeutic activities such as anti‐inflammatory activity by protein denaturation and RBC membrane stabilization methods, and anti‐oxidant activity by DPPH scavenging method of the newly synthesized compounds were studied. Interestingly, in‐vitro testing of these compounds reveals that the compounds 4d, 4g, 4i, 8a and 8b showed comparable anti‐inflammatory activity with respect to the standard drug, diclofenac. Similarly, fused pyridine 4f showed excellent anti‐oxidant activity when compared with the standard, ascorbic acid. An efficient synthesis of functionalized spiropyridines and pyrido[2,3‐d]pyrimidines by multi‐component pathway. [ABSTRACT FROM AUTHOR]

Background: The Opuntia spp. have been used in traditional medicine for many centuries. It is used in the management of diseases that involves oxidative stress, especially diabetes, obesity and cancer. Opuntia stricta (Haw) is one of the relatively unknown species in South Africa where it is regarded more as a weed. Because of this, not much is known about its chemical composition. Aim: To determine the chemical composition, antioxidant, anti-inflammatory, and cytotoxic activities of Opuntia stricta cladodes. Methods: The phytochemical composition of acetone, aqueous and ethanol extract of cladodes of Opuntia stricta (Haw), as well as the vitamins A, C and E of its dried weight cladodes and the antioxidant activities, were evaluated using standard in vitro methods. The anti-inflammatory and cytotoxic activities were evaluated using cell-based assays. The phytochemical composition and vitamins were determined spectrophotometrically, while the antioxidant activities were determined by DPPH, nitric oxide, hydrogen peroxide scavenging activity and phosphomolybdenum (total) antioxidant activity. Anti-inflammatory activity was determined using RAW 264.7 cells, while cytotoxicity was determined using U937 cells. Results: The phytochemical composition showed a significant difference in the various extracts. The total phenolics were higher than other phytochemicals in all the extracts used. All the extracts displayed antioxidant activity, while most of the extracts showed anti-inflammatory activity. Only one extract showed cytotoxicity, and it was mild. Conclusion: The results show that the Opuntia stricta is rich in polyphenolic compounds and has good antioxidant activity as well as anti-inflammatory activities. [ABSTRACT FROM AUTHOR]

Protease inhibitors are one of the most promising and investigated subjects for their role in pharmacognostic and pharmacological studies. This study aimed to investigate antioxidant, anti-inflammatory, and antimicrobial activities of trypsin inhibitors (TIs) from two plant sources (Cajanus cajan and Phaseolus limensis). TI was purified from C. cajan (PUSA-992) by ammonium sulfate precipitation followed by ion exchange chromatography. TI from Phaseolus limensis (lima bean trypsin inhibitor; LBTI) was procured from Sigma-Aldrich, St. Louis, Missouri, United States. The antioxidant activity was analyzed by ferric ion reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH). The anti-inflammatory property of TIs was determined by inhibition of albumin denaturation assay. Ascorbic acid and aspirin were used as standards for antioxidant and anti-inflammatory assays, respectively. These TIs were tested against various bacterial and fungal strains. The TIs showed DPPH radical-scavenging activity in a concentration-dependent manner with IC50 values comparable to ascorbic acid. The FRAP values were also observed comparable to ascorbic acid and followed the trend of dose-dependent manner. The half maximal inhibitory concentration (IC50) values of CCTI and LBTI in anti-inflammatory test showed that LBTI is more potent than CCTI. The TIs showed potent antibacterial activity, but apparently no action against fungi. This study has reported the biological properties of CCTI and LBTI for the first time. The results show that TIs possess the ability to inhibit diseases caused by oxidative stress, inflammation, and bacterial infestation. [ABSTRACT FROM AUTHOR]

Pain is an unpleasant subjective feeling having implications on both physical and mental realm. Multiple dimensions of pain involving behavioral, spiritual, emotional, and cognitive changes have been studied and pathways elucidated. It is stressed that the nature in which pain is modulated and perceived at a higher center is a complex phenomenon. One of the main goals of pain modulation is to modify pain to a more tolerable level, rather than its complete eradication. Different pain management interventions were tried but have effects that are more adverse. Till date, the only reliable pain blockers are analgesics and anti-inflammatory drugs in the form of opioids and non-opioids. Despite this, most of the drugs are ineffective at various levels, furthermore, adding to complications. Thus, there is an urgent need for effective intervention with minimal side effects. Ascorbic acid, popularly known as vitamin C, has shown to exhibit promising analgesic properties. The literature is sparse with the usage of the drug in various forms of pain. This review focuses on the dynamics and kinetics of vitamin C and its usage in various forms of pain. With minimal adverse effects, the drug is shown to perform well in different types of pain disorders, thus paving way for alternative interventional agent for pain management. [ABSTRACT FROM AUTHOR]

Ibuprofen is one of the most potent non-steroid anti-inflammatory drugs (NSAIDs) and plays an important role in the treatment of neurodegenerative diseases. However, its poor brain penetration and serious side effects at therapeutic doses, has hindered its further application. Thus, it is of great interest to develop a carrier-mediated transporter (CMT) system that is capable of more efficiently delivering ibuprofen into the brain at smaller doses to treat neurodegenerative diseases. In this study, a dual-mediated ibuprofen prodrug modified by glucose (Glu) and vitamin C (Vc) for central nervous system (CNS) drug delivery was designed and synthesized in order to effectively deliver ibuprofen to brain. Ibuprofen could be released from the prepared prodrugs when incubated with various buffers, mice plasma and brain homogenate. Also, the prodrug showed superior neuroprotective effect in vitro and in vivo than ibuprofen. Our results suggest that chemical modification of therapeutics with warheads of glucose and Vc represents a promising and efficient strategy for the development of brain-targeting prodrugs by utilizing the endogenous transportation mechanism of the warheads. [ABSTRACT FROM AUTHOR]

Background: Sepsis refers to the dysregulated host immune response elicited by microbial infections resulting in life-threatening organ dysfunction. Sepsis represents a medical challenge, since it is associated with a rate of death as high as 60%. Septic shock is strongly associated with vascular dysfunction and elevated pulmonary capillary permeability. We recently reported that the combination of hydrocortisone (HC), ascorbic acid (vitC), and thiamine dramatically improves outcomes and reduces mortality in patients with sepsis. In the present study, we provide experimental evidence in support of the hypothesis that the combination of HC and vitC enhances endothelial barrier function.Methods: Human lung microvascular endothelial cells were exposed to lipopolysaccharide (LPS) in the absence or presence of HC and vitC.Results: LPS alone induced profound hyperpermeability, as reflected in decreased values of transendothelial electrical resistance. vitC alone did not exhibit barrier enhancement properties nor did it affect the LPS-induced hyperpermeability. Similarly, HC alone exhibited only a minor barrier-enhancing and protective effect. Conversely, the combination of HC and vitC, either as before or after treatment, dramatically reversed the LPS-induced barrier dysfunction. The barrier-protective effects of HC and vitC were associated with reversal of LPS-induced p53 and phosphorylated cofilin downregulation and LPS-induced RhoA activation and myosin light chain phosphorylation.Conclusions: These data provide a novel mechanism of endothelial barrier protection and suggest one possible pathway that may contribute to the therapeutic effects of HC and vitC in patients with sepsis. [ABSTRACT FROM AUTHOR]

Helicobacter pylori is recognized as the most common bacterial pathogens colonizing the gastric epithelium of nearly half of the world's population. This bacterium is the main etiological cause of gastroduodenal ulcers, and more importantly as the substantial risk factor for development of gastric cancer. The emergence and rapid increase in the prevalence of multi-drug resistant phenotypes have posed major pitfalls in effectiveness of various treatment regimens and eradication strategies against H. pylori infections. Several natural products and supplementary food components have been reported to have established anti-H. pylori activity. Herein, we review the application and efficacy of some specific natural products and foodstuffs such as milk, bee products (honey and propolis), fish oil, vitamins C and E, and also a nickel free-diet used as anti-H. pylori alternative treatment regimens. [ABSTRACT FROM AUTHOR]

[Display omitted] • Multifunctional C 3 N 4 dots were prepared with urea and L- ascorbic acid by simple hydrothermal method. • Carbon nitride dots exhibited high selectivity and sensitivity for Hg2+ and tetracycline in electrochemical detection. • Cytotoxicity studies with fibroblasts cells and B16 murine melanoma cells indicated the exceptional selective toxicity of C 3 N 4 dots for B16 cells. • Detailed studies have shown that the carbon nitride dot exhibits anticancer properties via chemotherapeutic and photodynamic effects. • In ROS study it became clear that in C 3 N 4 dots, photodynamic effect is prominent than chemotherapic effect. We report the facile single-step synthesis of carbon nitride dots (CND) from l -ascorbic acid and urea as precursors. The as-synthesized carbon dots were water-soluble, displaying green fluorescence in UV light with a high quantum yield. Electrochemical studies manifest carbon nitride dots' excellent stability, sensitivity, and selectivity for mercuric ions and drug tetracycline detection. The former and latter's detection limit is 0.055 µM and 0.18 µM, respectively. Furthermore, cytotoxic studies with the carbon nitride dots exposed its selective toxicity towards cancer cells, which steered anticancer studies on B16 murine melanoma cells. These non-functionalized carbon nitride dots could induce cell death by cell apoptosis derived from chemotherapic and photodynamic effects. [ABSTRACT FROM AUTHOR]

The antioxidant potential of grape ( Vitis vinífera L.) stems has been reported in the last decade although no identification of the individual compounds responsible for such action has been done. In this work, polyphenolic extract of grape stems was processed resorting to semi-preparative HPLC, allowing to obtain 5 purified polyphenols (caftaric acid, malvidin-3- O -glucoside, quercetin-3- O -glucuronide, mailvidin-3- O -(6- O -caffeoyl)-glucoside, and Σ-viniferin), which were fully characterized by HPLC-PDA-ESI-MS n . Isolated compounds were featured on their radical scavenging capacity (DPPH and ABTS), cell viability, anti-inflammatory activity, and capacity to modulate the level of reactive oxygen species, glutathione, lipid peroxidation, and overall oxidative stress in a biological model (human keratinocytes) in vitro , under basal and oxidative conditions. The results obtained noticed the combinations malvidin-3- O -glucoside + Vitamin E and quercetin-3- O -glucuronide + vitamin C as the most effective, allowing to improve the capacity of complete extracts or individual compounds, and being candidates to be used in the development of new functional products. [ABSTRACT FROM AUTHOR]

Background: The global burden of sepsis is estimated as 15 to 19 million cases annually, with a mortality rate approaching 60% in low-income countries.Methods: In this retrospective before-after clinical study, we compared the outcome and clinical course of consecutive septic patients treated with intravenous vitamin C, hydrocortisone, and thiamine during a 7-month period (treatment group) with a control group treated in our ICU during the preceding 7 months. The primary outcome was hospital survival. A propensity score was generated to adjust the primary outcome.Results: There were 47 patients in both treatment and control groups, with no significant differences in baseline characteristics between the two groups. The hospital mortality was 8.5% (4 of 47) in the treatment group compared with 40.4% (19 of 47) in the control group (P < .001). The propensity adjusted odds of mortality in the patients treated with the vitamin C protocol was 0.13 (95% CI, 0.04-0.48; P = .002). The Sepsis-Related Organ Failure Assessment score decreased in all patients in the treatment group, with none developing progressive organ failure. All patients in the treatment group were weaned off vasopressors, a mean of 18.3 ± 9.8 h after starting treatment with the vitamin C protocol. The mean duration of vasopressor use was 54.9 ± 28.4 h in the control group (P < .001).Conclusions: Our results suggest that the early use of intravenous vitamin C, together with corticosteroids and thiamine, are effective in preventing progressive organ dysfunction, including acute kidney injury, and in reducing the mortality of patients with severe sepsis and septic shock. Additional studies are required to confirm these preliminary findings. [ABSTRACT FROM AUTHOR]

Background: Chronic kidney disease (CKD) is a group of heterogeneous abnormalities affecting the function and structure of the kidney and mostly further proceeds to cardiovascular damage prior to end stage renal disease (ESRD). The oxidative insult and inflammatory mediators have some undefined role in CKD and cardiovascular complications. It is therefore, aimed at to pin point the predictive factors in the development of cardiovascular disorder in patients with chronic kidney disease. Methods: Fifty patients of CKD experiencing cardiovascular distress and twenty normal individuals having same age and sex acted as control during these observations. Blood samples (Each 5 ml) were drawn and subjected to centrifugation for 10–15 minutes to separate the serum at 4000-5000rpm. The levels of MDA, GSH, SOD, CAT, VIT C, VIT E, IL-1, TNF-alpha, nitric oxide (NO) and advanced oxidation protein products (AOPPs) were estimated and analyzed. Results: The nitric oxide levels in the CKD patients decreased significantly (13.26±1.25 ng/ml) compared to controls (42.15±5.26 ng/ml). The serum vitamin E and C levels in these patients recorded 2.15±0.25 μg/ml and 0.97±0.09 μg/ml respectively as against their assigned controls which read 6.35±1.22 μg/ml and 3.29±0.25 μg/ml. Furthermore, a significantly higher level of Malondialdehyde (MDA) as1.25±0.07 nmol/ml was observed in CKD patients viz-a-viz relevant control. However, the serum SOD, catalase (CAT) and GSH levels in the same patients registered a significant decline as evident from respective figures 0.07±0.002 μg/dl, 1.22±0.012 μmol/mol, and 3.25±1.05 μg/dl. The control for these was observed as0.99±0.06 μg/dl, 3.19±0.05 μmol/mol, and 8.64±0.03 μg/dL. On the other hand, the IL-1 levels in the CKD patients found quite higher (402.5±18.26 pg/ml). This clearly points to substantial increase in oxidative insult and reduced NO levels leading to the renal and cardiovascular damage. Conclusion: Observations support the fact that the decrease in anti-oxidative capacity accompanied by higher inflammatory mediators in CKD is indicative of oxidative stress, consequently leading to CKD progression, in all probability to cardiovascular insult. The outcome reiterates that strategies be designed afresh to contain CKD progression to cardiovascular complications and ESRD. One way could be to focus on early detection of stress related to the disease. It requires analyzing the factors related to stress, such as the one reported here. Linking these factors with the symptoms could be a crucial step forward. And further, the disease could be monitored in a more disciplined manner. [ABSTRACT FROM AUTHOR]

• Ten compounds have been synthesized and characterized using spectroscopic methods: MS, 1H and 13C NMR and FT-IR. • The DFT and in-silico antidiabetic, antioxidant and anti-inflammatory studies showed good interactions of the compounds with target protein residue compared with standard. • In vivo antidiabetic, antioxidant and anti-inflammatory activities were also studied. The increasing resistance to antidiabetic, antioxidant, and anti-inflammatory drugs are complex and severe health issues these days, as many drugs available on the market are no more effective. The choice for the synthesis of novel dipeptides-sulphonamide hybrid is based on their wide biological properties such as antidiabetic, antioxidant, antimalarial, etc. The base promoted reactions of the L -proline with substituted benzenesulphonyl chloride gave benzenesulphonamides an excellent yield. The condensation reaction of benzenesulphonamides with the carboxamide derivatives using peptide coupling reagents gave targeted products (8a-j). The ten novel compounds were characterized using 1HNMR, 13CNMR, FTIR, and MS spectroscopic techniques. The DFT and in-silico antidiabetic, antioxidant and anti-inflammatory studies showed good interactions of the compounds with target protein residues and a higher dock score in comparison with standard drugs. In vivo antidiabetic, anti-inflammatory and in vitro antioxidant activities were also studied. Estimation of glucose, cholesterol and triacylglycerol levels was carried out and it was observed that compound 8a exhibited significant antidiabetic activity. Compounds 8b, 8c, and 8d also possessed moderate antidiabetic activity. In the in vivo anti-inflammatory studies, compounds 8a inhibited carrageenan-induced rat-paw edema at 94.67 and 91.88% at 0.5 h, and 1 h administration respectively. Compound 8a had excellent antioxidant activity. Compound 8a with IC 50 of 0.992 μg/ml is comparable with that of ascorbic acid at 0.993 μg/ml. This implies that compound 8a can serve as an antioxidant agent compared with ascorbic acid. Calculated DFT parameters agreed significantly with the antidiabetic and anti-inflammatory studies [ABSTRACT FROM AUTHOR]

Phytochemical investigation of the extract of Arctii Fructus led to the isolation and characterization of two new compounds, named arctiisesquineolignan B (1) and arctiiphenolglycoside A (2). Their structures were elucidated by means of spectroscopic methods (UV, IR, HR-ESI-MS, 1D and 2D NMR) and chemical evidence, as well as by comparison with known analogs in the literature. Compound2exhibited stronger antioxidant activity than the positive control ascorbic acid at a concentration of 10 μM. [ABSTRACT FROM AUTHOR]

The phytochemical profile by HPLC-TOF-MS of three blackberry cultivars (‘Jumbo’, ‘Black Satin’ and ‘Dirksen’), adapted to the central-east of Argentina, was determined. The antioxidant capacity by DPPH and FRAP assays, and the effect of the blackberry extracts on lipopolysaccharide (LPS)-induced nitric oxide (NO) production, reactive oxygen species (ROS) production, and biomarkers of inflammation were also evaluated. ‘Dirksen’ fruits exhibited the highest vitamin C content (24 and 14% higher than values found in ‘Black Satin’ and ‘Jumbo’, respectively). However, ‘Jumbo’ and ‘Black Satin’ fruits presented higher total phenolic contents (more than 15%) than ‘Dirksen’. Cyanidin-3- O -glucoside was the main polyphenolic compound quantified in all samples. ‘Jumbo’ and ‘Black Satin’ cultivars exhibited higher antioxidant capacity, and significantly reduced the release of ROS. The mRNA expression levels of cyclooxygenase-2 (Cox-2) and interleukin-6 (IL-6) were reduced consistently (more than 30%) by extracts of both cultivars, and showed slight suppressions on NO production. However, effective inhibition in the gene expression of interleukin-1β (IL-1β) and nitric oxide synthase (iNOS) was not observed by any extract. These results suggest the potential of blackberries cultivars ‘Black Satin’ and ‘Jumbo’ to contribute to a healthy diet, based on their higher polyphenol content, providing higher antioxidant and anti-inflammatory properties. [ABSTRACT FROM AUTHOR]

The antioxidant, anti-inflammatory, acetylcholinesterase (AChE) inhibitory and antimicrobial activities of extract from the Centaurea antiochia Boiss. var. praealta (Boiss. & Bal.) Wagenitz, an endemic plant species from Turkey, were investigated. The results indicated that the extract inhibits FeCl3/ascorbic acid-induced phosphatidylcholine liposome oxidation, scavenges stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radicals, and reduces Fe3+ to Fe2+ in the ferric-reducing antioxidant power (FRAP) assay. The extract inhibited AChE and both cyclooxygenase (COX)-1 and COX-2, which suggests this species might be a potential source of plant-derived anti-inflammatory and anti-AChE substances. The extract may also act as an antimicrobial agent because it inhibited the growth of Gram-positive and Gram-negative bacteria as well as yeast. These findings may scientifically explain some uses of this species in Turkish folk medicine as an antimicrobial, antiinflammatory and wound healing agent. [ABSTRACT FROM AUTHOR]

Ethno-pharmacological relevance Cyperus rotundus L. (Cyperaceae) is a medicinal herb traditionally used to treat various clinical conditions at home such as diarrhea, diabetes, pyresis, inflammation, malaria, and stomach and bowel disorders. Currently, it is one of the most widespread, problematic, and economically damaging agronomic weeds, growing wildly in various tropical and subtropical regions of the world. The present paper summarizes the available information that will aid in future medicine preparation by identifying active ingredients and their mode of action for a specific therapeutic activity using the latest technologies. Material and method This review article is based on the information available on the phytochemical, toxicological, and pharmacological studies on and traditional uses of C. rotundus . The present paper covers the literature available particularly from 2000 to 2015 online (Google Scholar, PubMed, ScienceDirect, Scopus, SpringerLink, and Web of Science) and in books on phytochemistry, ethnopharmacology, and botany of this plant. Results Phytochemical and pharmacological studies revealed the significance of C. rotundus as an antiandrogenic, antibacterial, anticancerous, anticonvulsant, antidiabetic, antidiarrheal, antigenotoxic, anti-inflammatory, antilipidemic, antimalarial, antimutagenic, antiobesity, antioxidant, anti-uropathogenic, hepatoprotective, cardioprotective, neuroprotective, and nootropic agent. This is the most investigated plant worldwide due to the higher concentration of active ingredients in the form of essential oils, phenolic acids, ascorbic acids, and flavonoids in the tuber and rhizomes. Unfortunately, this significant plant species has not been assessed under improved cultivation conditions with the aim of conservation in natural habitats and high quality. Conclusion Reports can be found on the ehtnobotanical use of C. rotundus in atherosclerosis, aging, apoptosis, cancer, cystitis, epilepsy, hirsutism, nociception, prostatitis, and genotoxicity disorders. The phytochemical and pharmacological activities of C. rotundus have supported its traditional as well as prospective uses as a valuable Ayurvedic plant. Previous researches focuses on the phytochemistry, biological properties and clinical application of rhizomes and tubers of C. rotundus . However, such studies on the other parts of this medicinally important plant are still quest to be investigate. Furthermore, future study should aim at confirming the clinical activities and safety of this plant before being used for the development of new therapeutic agent in human subjects. [ABSTRACT FROM AUTHOR]

Increasing demand of shea products (kernels and butter) has led to the assessment of the state-of-the-art of these products. In this review, attention has been focused on macronutrients and micronutrients of pulp, kernels, and butter of shea tree and also the physicochemical properties of shea butter. Surveying the literature revealed that the pulp is rich in vitamin C (196.1 mg/100 g); consumption of 50 g covers 332% and 98% of the recommended daily intake (RDI) of children (4–8 years old) and pregnant women, respectively. The kernels contain a high level of fat (17.4–59.1 g/100 g dry weight). Fat extraction is mainly done by traditional methods that involve roasting and pressing of the kernels, churning the obtained liquid with water, boiling, sieving, and cooling. The fat (butter) is used in food preparation and medicinal and cosmetics industries. Its biochemical properties indicate some antioxidant and anti-inflammatory activities. Large variations are observed in the reported values for the composition of shea products. Recommendations for future research are presented to improve the quality and the shelf-life of the butter. In addition, more attention should be given to the accuracy and precision in experimental analyses to obtain more reliable information about biological variation. [ABSTRACT FROM PUBLISHER]

Introduction: Neutrophils provide the first line of defense of the innate immune system by phagocytosing, killing and digesting bacteria and fungi. During this process, neutrophils produce reactive oxygen species (ROS), which in excess, can damage the cells themselves and surrounding tissues. The carotenoid fucoxanthin (Fc) has been studied concerning its antioxidant and anti-inflammatory actions. Vitamin c (Vc) also demonstrates potent antioxidant action. This study aimed to evaluate the effect of Fc (2 μM) in association with Vc (100 μM) on functional parameters of human neutrophils in vitro. Materials and methods: We evaluated the migration and phagocytic capacity, intracellular calcium mobilization, ROS production (O, HO, HOCl), myeloperoxidase activity, profile of antioxidant enzymes, phosphorylation of p38 MAPK and p65 NFκB subunit, GSH/GSSG ratio and release of pro-inflammatory cytokines (TNF-α and IL-6) in neutrophils under different stimuli. Results: We verified an increase in phagocytic capacity for all treatments, together with an increase in intracellular calcium only in cells treated with Fc and Fc + Vc. ROS production was reduced by all treatments, although Vc was a better antioxidant than Fc. Phosphorylation of the p-65 subunit of NFκB was reduced in cells treated with Fc + Vc and release of TNF-α and IL-6 was reduced by all treatments. These findings indicate that the regulation of inflammatory cytokines by neutrophils is not exclusively under the control of the NFκB pathway. Fc reduced the activity of some antioxidant enzymes, whereas Vc increased GR activity and the GSH/GSSG ratio. Conclusion: In conclusion, the results presented in this study clearly show an immunomodulatory effect of the carotenoid fc alone or in combination with Vc on the function of human neutrophils. [ABSTRACT FROM AUTHOR]

The pathology process in burn injury is both a local and systemic inflammatory reaction, the end result of which is an almost immediate shift of intravascular fluid into the surrounding interstitial space. This occurs as a consequence of changes in vascular permeability as the normal capillary barrier is disrupted by a host of mediators, one of them is histamine. Vitamin C functions as an anti-inflammatory on burn by destroying imizadole ring structure of the histamine molecule. The purpose of this research is to determine the effect of 3000 mg vitamin C infusion on histamine level in severly burnt patients. A randomized pre & posttest control group design. Histamine levels were determined in 16 severely burned patients in burn injury unit of Dr. Soetomo Hospital, Surabaya from June-December 2012 (age 16-65 years old, American Burn Association criteria, 2007). 16 patients were divided into 2 groups; G1 (control, given infusion of vitamin C 2x 400 mg per day for 72 hours) and G2 (vitamin C 3000 mg per day for 72 hours). Variable examined were histamine level of leucocyte, renal function, and blood gas analysis (BGA).Data were analyzed with t test and coupled t test (significant at p<0.05). G1 histamine level was higher than G2 (p<0.05). There were no significant results from renal function analysis and BGA between G1 and G2. The amount of G2 leucocyte was lower than G1 (p=0.045). Giving vitamin C infusion with high dose is able to decrease blood histamine level in severely burnt patient. [ABSTRACT FROM AUTHOR]

Vitamin C deficiency is common during critical illness because of increased requirements, decreased intake, reduced recycling and increased urinary excretion. Vitamin C has multiple key metabolic functions and act synergistically. Vitamin C has important antioxidant, antiinflammatory, and immune-modulating effects, and is an essential cofactor for mono- and dioxygenase enzymes, deficiency can increase the severity of illness and hamper recovery. Several small clinical studies show improvement of organ function or even a reduction in mortality with i.v. vitamin C, but large clinical trials are required. Vitamin A deficiency is more common during infection, and supplementation reduces severe morbidity and mortality from infectious diseases. Vitamin A modulates activities at the cellular level and, via its interrelationship with hormones such as thyroid, insulin, and corticosteroids, has diffuse metabolic effects on the body. Mild vitamin A deficiency may cause fatigue, susceptibility to infections, and infertility. The most common use of vitamin A supplementation is to offset steroids' effect. When considering supplementation, the potential benefits must be weighed against the risk of harm. Vitamin A toxicity can be critical and even result in death. Having more than an average of 1.5 mg a day of vitamin A over many years may affect your bones, making them more likely to fracture when you're older. The evidence for supplementation with vitamin A is currently limited to expert opinion and is not backed up by rigorous trials. [ABSTRACT FROM AUTHOR]

Osteoarthritis (OA) is a degenerative inflammatory condition of the joint cartilage that currently affects approximately 58 million adults in the world. It is characterized by pain, stiffness, and a reduced range of motion with regard to the arthritic joints. These symptoms can cause in the long term a greater risk of overweight/obesity, diabetes mellitus, and falls and fractures. Although the current guidelines for the treatment of OA suggest, as the gold standard for this condition, pharmacological treatment characterized by non-steroidal anti-inflammatory drugs (NSAID), opioids, and cyclooxygenase (COX)-2-specific drugs, a great interest has been applied to nutraceutical supplements, which include a heterogeneous class of molecules with great potential to reduce inflammation, oxidative stress, pain, and joint stiffness and improve cartilage formation. The purpose of this review is to describe the potential application of nutraceuticals in OA, highlighting its molecular mechanisms of actions and data of efficacy and safety (when available). [ABSTRACT FROM AUTHOR]