scholarly journals Localized Therapy of Vaginal Infections and Inflammation: Liposomes-In-Hydrogel Delivery System for Polyphenols

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 53 ◽  
Author(s):  
May Jøraholmen ◽  
Purusotam Basnet ◽  
Mia Tostrup ◽  
Sabrin Moueffaq ◽  
Nataša Škalko-Basnet
Keyword(s):  
Delivery System ◽  
Ex Vivo ◽  
Radical Scavenging Activity ◽  
In Vitro Release ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
No Production ◽  
Vaginal Infections ◽  
Chitosan Hydrogel ◽  
Anti Inflammatory

Natural polyphenols, such as resveratrol (RES) or epicatechin (EPI), are attractive for treatments of various diseases, including vaginal infections and inflammation, because of their strong anti-oxidative and anti-inflammatory properties. However, their low solubility and consequent poor bioavailability limit their therapeutic uses. To overcome these limitations, a vaginal delivery system comprising either RES or EPI liposomes-in-hydrogel was developed. This system permits therapeutic action of both liposomal polyphenol (RES or EPI) and chitosan-based hydrogel. Liposomes of around 200 nm and entrapment efficiency of 81% and 77% for RES and EPI, respectively, were incorporated into chitosan hydrogel, respectively. Medium molecular weight chitosan (2.5%, w/w) was found to have optimal texture properties and mucoadhesiveness in ex vivo conditions. The in vitro release studies confirmed the sustained release of polyphenols from the system. Both liposomal polyphenols and polyphenols-in-liposomes-in-hydrogel exhibited only minor effects on cell toxicity. EPI showed superior radical scavenging activity at lower concentrations compared to antioxidants vitamin C and E. Anti-inflammatory activity expressed as the inhibitory activity of formulations on the NO production in the LPS-induced macrophages (RAW 264.7) confirmed the superiority of EPI liposomes-in-hydrogel. The plain liposomes-in-hydrogel also exhibited potent anti-inflammatory activity, suggesting that chitosan hydrogel acts in synergy regarding anti-inflammatory effect of formulation.

scholarly journals Probiotic Cell-Free Supernatants Exhibited Anti-Inflammatory and Antioxidant Activity on Human Gut Epithelial Cells and Macrophages Stimulated with LPS

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Stefania De Marco ◽  
Marzia Sichetti ◽  
Diana Muradyan ◽  
Miranda Piccioni ◽  
Giovanna Traina ◽  
...  
Keyword(s):  
Epithelial Cells ◽  
Lactobacillus Reuteri ◽  
Intestinal Inflammation ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Human Colon ◽  
Saccharomyces Boulardii ◽  
Inflammatory Activity ◽  
Industrialized Countries ◽  
Anti Inflammatory

The incidence of inflammatory bowel disease is increasing all over the world, especially in industrialized countries. The aim of the present work was to verify the anti-inflammatory activity of metabolites. In particular, cell-free supernatants ofLactobacillus acidophilus, Lactobacillus casei,Lactococcus lactis, Lactobacillus reuteri, andSaccharomyces boulardiihave been investigated. Metabolites produced by these probiotics were able to downregulate the expression of PGE-2 and IL-8 in human colon epithelial HT-29 cells. Moreover, probiotic supernatants can differently modulate IL-1β, IL-6, TNF-α, and IL-10 production by human macrophages, suggesting a peculiar anti-inflammatory activity. Furthermore, supernatants showed a significant dose-dependent radical scavenging activity. This study suggests one of the mechanisms by which probiotics exert their anti-inflammatory activity affecting directly the intestinal epithelial cells and the underlying macrophages. This study provides a further evidence to support the possible use of probiotic metabolites in preventing and downregulating intestinal inflammation as adjuvant in anti-inflammatory therapy.

scholarly journals Unravelling the Anti-Inflammatory and Antioxidant Potential of the Marine Sponge Cliona celata from the Portuguese Coastline

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 632
Author(s):  
Joana Alves ◽  
Helena Gaspar ◽  
Joana Silva ◽  
Celso Alves ◽  
Alice Martins ◽  
...  
Keyword(s):  
Marine Sponge ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Marine Sponges ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Protective Effects ◽  
Antioxidant Power ◽  
Anti Inflammatory ◽  
Cliona Celata

Inflammation is a double-edged sword, as it can have both protective effects and harmful consequences, which, combined with oxidative stress (OS), can lead to the development of deathly chronic inflammatory conditions. Over the years, research has evidenced the potential of marine sponges as a source of effective anti-inflammatory therapeutic agents. Within this framework, the purpose of this study was to evaluate the antioxidant and the anti-inflammatory potential of the marine sponge Cliona celata. For this purpose, their organic extracts (C1–C5) and fractions were evaluated concerning their radical scavenging activity through 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), ferric reducing antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC), and anti-inflammatory activity through a (lipopolysaccharides (LPS)-induced inflammation on RAW 264.7 cells) model. Compounds present in the two most active fractions (F5 and F13) of C4 were tentatively identified by gas chromatography coupled to mass spectrometry (GC-MS). Even though samples displayed low antioxidant activity, they presented a high anti-inflammatory capacity in the studied cellular inflammatory model when compared to the anti-inflammatory standard, dexamethasone. GC-MS analysis led to the identification of n-hexadecanoic acid, cis-9-hexadecenal, and 13-octadecenal in fraction F5, while two major compounds, octadecanoic acid and cholesterol, were identified in fraction F13. The developed studies demonstrated the high anti-inflammatory activity of the marine sponge C. celata extracts and fractions, highlighting its potential for further therapeutic applications.

scholarly journals Sorbaria kirilowii Ethanol Extract Exerts Anti-Inflammatory Effects In Vitro and In Vivo by Targeting Src/Nuclear Factor (NF)-κB

Biomolecules ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 741 ◽  
Author(s):  
Jiwon Jang ◽  
Jong Sub Lee ◽  
Young-Jin Jang ◽  
Eui Su Choung ◽  
Wan Yi Li ◽  
...  
Keyword(s):  
Signaling Pathways ◽  
Ex Vivo ◽  
Ethanol Extract ◽  
Inflammatory Activity ◽  
No Production ◽  
Nuclear Factor ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Inflammation is a fundamental process for defending against foreign antigens that involves various transcriptional regulatory processes as well as molecular signaling pathways. Despite its protective roles in the human body, the activation of inflammation may also convey various diseases including autoimmune disease and cancer. Sorbaria kirilowii is a plant originating from Asia, with no anti-inflammatory activity reported. In this paper, we discovered an anti-inflammatory effect of S. kirilowii ethanol extract (Sk-EE) both in vivo and in vitro. In vitro effects of Sk-EE were determined with lipopolysaccharide (LPS)-stimulated RAW264.7 cells, while ex vivo analysis was performed using peritoneal macrophages of thioglycollate (TG)-induced mice. Sk-EE significantly reduced the nitric oxide (NO) production of induced macrophages and inhibited the expression of inflammation-related cytokines and the activation of transcription factors. Moreover, treatment with Sk-EE also decreased the activation of proteins involved in nuclear factor (NF)-κB signaling cascade; among them, Src was a prime target of Sk-EE. For in vivo assessment of the anti-inflammatory effect of Sk-EE, HCl/EtOH was given by the oral route to mice for gastritis induction. Sk-EE injection dose-dependently reduced the inflammatory lesion area of the stomach in gastritis-induced mice. Taking these results together, Sk-EE exerts its anti-inflammatory activity by regulating intracellular NF-κB signaling pathways and also shows an authentic effect on reducing gastric inflammation.

scholarly journals Phlorotannins from Fucus vesiculosus: Modulation of Inflammatory Response by Blocking NF-κB Signaling Pathway

2020 ◽  
Vol 21 (18) ◽  
pp. 6897 ◽  
Author(s):  
Marcelo D. Catarino ◽  
Ana Silva ◽  
Maria T. Cruz ◽  
Nuno Mateus ◽  
Artur M.S. Silva ◽  
...  
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Ethyl Acetate Fraction ◽  
Transcriptional Level ◽  
No Production ◽  
Fragmentation Pattern ◽  
Inhibitory Protein ◽  
Brown Macroalgae ◽  
Anti Inflammatory ◽  
Almost All

Due to their large spectrum of bioactive properties, much attention has recently been drawn to phlorotannins—i.e., phenolic compounds characteristic from brown macroalgae. This study aimed to evaluate the antioxidant and anti-inflammatory properties of F. vesiculosus phlorotannin extracts and purified fractions. Overall, the crude extract and its ethyl acetate fraction (EtOAc) showed good radical scavenging activity, particularly towards nitric oxide (NO•). Subsequent subfractions of EtOAc (F1 to F9) with different molecular weights were then shown to inhibit lipopolysaccharide-induced NO• production in macrophages, with stronger effects being observed for fractions of lower MWs. Of the three intracellular markers analyzed, inducible NO• synthase showed the highest sensitivity to almost all the phlorotannin-rich samples, followed by interleukin 1β and cyclooxygenase 2, which was only inhibited by F2. Furthermore, this subfraction inhibited the phosphorylation and degradation of inhibitory protein κBα, thus preventing the activation of NF-κB and blocking the inflammatory cascade at the transcriptional level. This sample was characterized by the presence of a major compound with a deprotonated molecular ion at m/z 507 with a fragmentation pattern coherent with that of a phlorotannin derivative. Overall, this work unveiled some of the mechanistic aspects behind the anti-inflammatory capacity of phlorotannins from F. vesiculosus, endorsing its use as a possible natural source of anti-inflammatory compounds.

scholarly journals IN VITRO ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITIES OF ALCHORNEA CORDIFOLIA (SCHUMACH AND THONN.) MULL. ARG. AND ANTROCARYON KLAINEANUM PIERRE EXTRACTS

2020 ◽  
pp. 129-135
Author(s):  
ROSETTE CHRISTELLE NDJIB ◽  
STEVE VALDI DJOVA ◽  
CHRISTELLE WAYOUE KOM ◽  
AGBOR GABRIEL AGBOR ◽  
AMINA MAMAT ◽  
...  
Keyword(s):  
Concentration Level ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Dry Weight ◽  
Inflammatory Activity ◽  
Phytochemical Screening ◽  
Reducing Activity ◽  
Anti Inflammatory ◽  
Β Carotene

Objective: This study aims to evaluate the in vitro antioxidant, anti-inflammatory activities of the aqueous and hydroethanolic extracts recipe of Alchornea cordifolia and Antrocaryon klaineanum. A preliminary phytochemical screening was carried out. Methods: The total phenols content was determined by the Folin Ciocalteu reagent method, while the antioxidant activity of both extracts was characterized by the 2-2diphenyl-1-picrilhidrazil (DPPH) and β-carotene assays. The anti-inflammatory activity of the extracts was evaluated as the inhibition of Bovine Serum Albumin (BSA) denaturation and antiproteinase activity. Results: The aqueous extracts of Alchornea cordifolia and Antrocaryon klaineanum contained more polyphenols [270 mg Ascorbic acid equivalent (AAE)/g dry weight (dw)] than the hydroethanolic recipe extract (262.41 mg AAE/g dw) at the same concentration level. On the other hand, the aqueous and hydroethanolic recipe extract had the same radical scavenging activity with the antiradical power of 0.851 and 0.830, respectively. Similarly, the recipe extract had the same reducing activity with reducing the power of 94.2±2.03 mg EAA/g dw and 97.4±4.16 mg EAA/g dw for the aqueous and hydroethanolic recipe extract of Alchornea cordifolia and Antrocaryon klaineanum respectively. For the anti-inflammatory activity it was observed that both extracts possess the same activity as Diclofenac® with an IC50 of 50.21 μg/ml. The phytochemical screening of the extracts revealed the presence of alkaloids, flavonoids, carbohydrates, phenols and tannins, which may account for their activities. Conclusion: The plant recipe extract studied possess antioxidant and anti-inflammatory potentials, which may be beneficiary to its consumers.

scholarly journals Amauroderma rugosum(Blume & T. Nees) Torrend: Nutritional Composition and Antioxidant and Potential Anti-Inflammatory Properties

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Pui-Mun Chan ◽  
Gowri Kanagasabapathy ◽  
Yee-Shin Tan ◽  
Vikineswary Sabaratnam ◽  
Umah Rani Kuppusamy
Keyword(s):  
Submerged Culture ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Indigenous Communities ◽  
Antioxidant Potential ◽  
Raw264.7 Cells ◽  
Total Phenolic ◽  
No Production ◽  
Freeze Dried ◽  
Anti Inflammatory

Amauroderma rugosumis a wild mushroom that is worn as a necklace by the indigenous communities in Malaysia to prevent fits and incessant crying by babies. The aim of this study was to investigate the nutritive composition and antioxidant potential and anti-inflammatory effects ofA. rugosumextracts on LPS-stimulated RAW264.7 cells. Nutritional analysis of freeze-dried mycelia ofA. rugosum(KUM 61131) from submerged culture indicated a predominant presence of carbohydrates, proteins, dietary fibre, phosphorus, potassium, and sodium. The ethanol crude extract (EE), its hexane (HF), ethyl acetate (EAF), and aqueous (AF) fractions of mycelia ofA. rugosumgrown in submerged culture were evaluated for antioxidant potential and anti-inflammatory effects. EAF exhibited the highest total phenolic content and the strongest antioxidant activity based on 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. HF showed dose-dependent inhibition of NO production in LPS-stimulated RAW264.7 cells and NO radical scavenging activity. Gas chromatographic analysis of HF revealed the presence of ethyl linoleate and ergosterol, compounds with known anti-inflammatory properties. In conclusion, the nutritive compositions and significant antioxidant potential and anti-inflammatory effects of mycelia extracts ofA. rugosumhave the potential to serve as a therapeutic agent or adjuvant in the management of inflammatory disorders.

scholarly journals Expression of Bioactive Lunasin Peptide in Transgenic Rice Grains for the Application in Functional Food

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2373 ◽  
Author(s):  
Guixing Ren ◽  
Yuqiong Hao ◽  
Yingying Zhu ◽  
Zhenxing Shi ◽  
Gang Zhao
Keyword(s):  
Antioxidant Activity ◽  
Transgenic Rice ◽  
Functional Food ◽  
Radical Scavenging Activity ◽  
Expression System ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Scavenging Activity ◽  
Ic50 Value ◽  
Anti Inflammatory

Lunasin, a bioactive peptide initially isolated from soybean, has anticancer, anti-inflammatory, and antioxidant activity. Due its great application value, lunasin seems to be a candidate gene in improving the nutritional value of crops. In this study, lunasin was inserted into the rice genome to evaluate whether it was feasible to express lunasin using the rice expression system and improve the bioactivity of protein in rice for our needs. We generatedlunasin-overexpressing rice lines, and chose three independent transgenic rice lines for further study. The lunasin content in trans-lunasin rice detected by UPLC-MS/MS was 1.01 × 10−3 g·kg−1 dry rice flour with grease removal in the lunasin extracts. The antioxidant efficacy of LET (lunasin-enriched fraction from trans-lunasin rice) and PEW (peptide-enriched fraction from wild type rice) was compared. Due to the presence of lunasin, LET showed higher (p < 0.05) antioxidant activity than PEW. LET exhibited high DPPH radical scavenging activity (IC50 value, 8 g·L−1), strong ABTS+ radical scavenging activity (IC50 value, 1.18 g·L−1), and great oxygen radical scavenging activity (170 μmol·L−1 Trolox equivalents when the concentration reached 4 g·L−1). Moreover, LET presented significantly higher (p < 0.05) anti-inflammatory activity on macrophage cells, and the NO production and the release of pro-inflammatory cytokines (IL-6, MCP1, and TNF-α) were significantly inhibited by LET. However, because of the low purity, LET showed weaker antioxidant and anti-inflammatory activity when compared to the Lunasin standard. These results suggested that it is feasible to use the rice expression system to express the exogenous lunasin in rice, and lunasin-overexpressing rice seems to be a candidate resource for application in functional food. Rice rich in lunasin is beneficial for human health, and could be used as a functional food in the diets of cancer and obese patients in the future.

scholarly journals Phytochemical analysis, antioxidant, antidiabetic and anti-inflammatory activity of bark of Gardenia latifolia

2019 ◽  
Vol 9 (1) ◽  
pp. 141-145
Author(s):  
Farheen Ansari ◽  
Salaj Khare ◽  
B. K. Dubey ◽  
Amit Joshi ◽  
Amit Jain ◽  
...  
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Inflammatory Activity ◽  
Phytochemical Analysis ◽  
Dpph Radical ◽  
Hydroalcoholic Extract ◽  
Radical Method ◽  
Anti Inflammatory

Gardenia latifolia (Rubiaceae) is commonly known as Indian boxwood or Ceylon boxwood, is a densely foliaceous small tree that occurs throughout the greater parts of Indian common in deciduous forests along the streams. The stem bark and fruits are reported to be used in the treatment of various ailments such as snake bite, skin diseases, stomach pains, caries in humans and ephemeral fever in live stocks. Many beneficial medicinal products are used to treat various serious diseases and disorders like diabetes, cancer and cardiovascular diseases without side effects. Hence our study focused to investigate the phytochemical analysis, quantification of bioactive compounds, in vitro free radical scavenging activity (DPPH radical method), anti-inflammatory activity (Carrageenan induced hind paw oedema ), in vitro anti-diabetic activity by enzyme inhibition activity of bark of Gardenia latifolia (hydroalcoholic extract) which has boundless medicinal properties. The results of this study showed the evidence that the extracts when tested for their phytochemicals and free radical scavenging activity were found to have considerable antioxidant potential. This plant also exhibit better in vitro enzyme inhibitory activity and anti-inflammatory activity. The results of this study indicate that the hydroalcoholic extract of Gardenia latifolia bark has significant pharmacological properties. Keywords: Gardenia latifolia, Phytochemical analysis, DPPH radical method, Anti-inflammatory activity, Anti-diabetic activity

scholarly journals Anti-Inflammatory and Antioxidant Activities ofSalvia fruticosa: An HPLC Determination of Phenolic Contents

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Rima Boukhary ◽  
Karim Raafat ◽  
Asser I. Ghoneim ◽  
Maha Aboul-Ela ◽  
Abdalla El-Lakany
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Inflammatory Activity ◽  
Total Phenolic ◽  
Phenolic Contents ◽  
Aerial Parts ◽  
Phenolic Constituents ◽  
Anti Inflammatory

Objectives.Salvia fruticosaMill. (S. fruticosa) is widely used in folk medicine. Accordingly, the present study was designed to evaluate the antioxidant and anti-inflammatory activities ofS. fruticosa, and to determine the phenolic constituents of its extracts.Methods. The antioxidant activity was determined using 2,2-diphenylpicrylhydrazyl assay. Total phenolic contents were estimated using Folin-Ciocalteu reagent, and high-performance liquid chromatography was performed to identify phenolic constituents. To evaluate the anti-inflammatory activity, carrageenan-induced mouse paw edema was determined plethysmographically.Key Findings. Different plant extracts demonstrated strong radical scavenging activity, where the ethyl acetate extract had the highest value in the roots and the lowest in the aerial parts. This antioxidant activity was correlated to the total phenolic content of different extracts, where rutin and luteolin were the most abundant constituents. Interestingly, both the roots and aerial parts revealed a significant anti-inflammatory activity comparable to diclofenac.Conclusions. This study is the first to demonstrate pharmacologic evidence of the potential anti-inflammatory activity ofS. fruticosa. This activity may partly be due to the radical scavenging effects of its polyphenolic contents. These findings warrant the popular use of the East Mediterranean sage and highlight the potential of its active constituents in the development of new anti-inflammatory drugs.

scholarly journals PHYTOCHEMICAL ANALYSIS AND IN VITRO BIOLOGICAL CHARACTERIZATION OF AQUEOUS AND METHANOLIC EXTRACT OF BACOPA MONNIERI

2016 ◽  
Vol 8 (12) ◽  
pp. 90
Author(s):  
Romana Parveen ◽  
Tooba Naz Shamsi ◽  
Himanshu Kumar ◽  
Sadaf Fatima
Keyword(s):  
Bacterial Infections ◽  
Methanolic Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Bacopa Monnieri ◽  
Inflammatory Activity ◽  
Phytochemical Analysis ◽  
Antioxidant Power ◽  
Anti Inflammatory

<p><strong>Objective</strong>:<strong> </strong>The present study was designed to identify the phytocompounds, to compare the antibacterial, antioxidant, and anti-inflammatory effects of aqueous and methanolic extract of <em>Bacopa monnieri</em>.</p><p><strong>Methods</strong>:<strong> </strong>Antioxidant activity was determined by 1, 1-diphenyl-2-picrylhydrazyl (DPPH), Ferric Reducing Antioxidant Power (FRAP), Super oxide dismutase (SOD), Reduced glutathione (GSH), Catalase assays. Anti-inflammatory activity was measured with inhibition of albumin denaturation and trypsin inhibitory assay. Finally, extracts were tested against various pathogenic bacterial and fungal strains by broth dilution assay and disc diffusion assay respectively.</p><p><strong>Results: </strong>Results showed the presence of alkaloids, flavonoids, phenols, quinines and glycosides etc while steroids and carboxylic acid were absent. The extracts demonstrated free radical-scavenging activity quite comparable with standard ascorbic acid. Methanolic extract exerted comparative higher antioxidant and anti-inflammatory activity than aqueous extract. Both extracts were most effective against <em>Bacillus subtilis</em><em> </em>and lowest inhibition against<em> Staphylococcus aureus</em>.</p><p><strong>Conclusion: </strong>The results obtained clearly indicated a promising potential of <em>B. monnieri</em> for serving as a strong ROS scavenger, might be used as anti-arthritic and strong natural antibiotic agent for effective treatment of various oxidative stressed disorders (cancer, cardiovascular diseases), inflammatory disorders (rheumatoid arthritis) and various bacterial infections.</p>

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