scholarly journals Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1414
Author(s):  
Maria Anghelache ◽  
Mihaela Turtoi ◽  
Anca Roxana Petrovici ◽  
Adrian Fifere ◽  
Mariana Pinteala ◽  
...  
Keyword(s):  
Protocatechuic Acid ◽  
Vascular Inflammation ◽  
Magnetic Core ◽  
Inflammatory Activity ◽  
Adhesion Assay ◽  
Theranostic Nanoparticles ◽  
Mitogen Activated Protein ◽  
Attractive Therapeutic Target ◽  
Anti Inflammatory ◽  
Core Nanoparticles

Vascular inflammation plays a crucial role in the progression of various pathologies, including atherosclerosis (AS), and thus it has become an attractive therapeutic target. The protocatechuic acid (PCA), one of the main metabolites of complex polyphenols, is endowed with anti-inflammatory activity, but its formulation into nanocarriers may increase its bioavailability. In this study, we developed and characterized dextran shell‒iron oxide core nanoparticles loaded with PCA (MNP-Dex/PCA) and assessed their cytotoxicity and anti-inflammatory potential on cells acting as key players in the onset and progression of AS, namely, endothelial cells (EC) and monocytes/macrophages. The results showed that MNP-Dex/PCA exert an anti-inflammatory activity at non-cytotoxic and therapeutically relevant concentrations of PCA (350 μM) as supported by the reduced levels of inflammatory molecules such as MCP-1, IL-1β, TNF-α, IL-6, and CCR2 in activated EC and M1-type macrophages and functional monocyte adhesion assay. The anti-inflammatory effect of MNP-Dex/PCA was associated with the reduction in the levels of ERK1/2 and p38-α mitogen-activated protein kinases (MAPKs) and NF-kB transcription factor. Our data support the further development of dextran shell-magnetic core nanoparticles as theranostic nanoparticles for guidance, imaging, and therapy of vascular inflammation using PCA or other anti-inflammatory compounds.

scholarly journals Antioxidant and Anti-Inflammatory Activities of Flavanones from Glycyrrhiza glabra L. (licorice) Leaf Phytocomplexes: Identification of Licoflavanone as a Modulator of NF-kB/MAPK Pathway

Antioxidants ◽  
2019 ◽  
Vol 8 (6) ◽  
pp. 186 ◽  
Author(s):  
Luca Frattaruolo ◽  
Gabriele Carullo ◽  
Matteo Brindisi ◽  
Sarah Mazzotta ◽  
Luca Bellissimo ◽  
...  
Keyword(s):  
Mapk Pathway ◽  
Antioxidant Properties ◽  
Health Spending ◽  
Glycyrrhiza Glabra ◽  
Inflammatory Activity ◽  
Leaf Extracts ◽  
Mitogen Activated Protein ◽  
Natural Remedies ◽  
Glycyrrhiza Glabra L ◽  
Anti Inflammatory

Inflammation represents an adaptive response generated by injuries or harmful stimuli. Natural remedies represent an interesting alternative to traditional therapies, involving several biochemical pathways. Besides, the valorization of agrochemical wastes nowadays seems to be a feasible way to reduce the health spending and improve the accessibility at bioactive natural compounds. In this context, the chemical composition of three Glycyrrhiza glabra L. (licorice) leaf extracts, obtained through maceration or ultrasound-assisted method (fresh and dried leaves) was investigated. A guided fractionation obtained three main components: pinocembrin, glabranin and licoflavanone. All the extracts showed similar antioxidant properties, evaluated by 2,2′-diphenyl-1-picrylhydrazyl (DPPH) or 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) Diammonium Salt (ABTS) assay, while, among the isolated compounds, licoflavanone exhibited the best antioxidant activity. The anti-inflammatory activity of the extracts and the purified compounds was investigated in lipopolysaccharide (LPS)-stimulated RAW 264.7 murine macrophages. Extract C and licoflavanone showed a good anti-inflammatory activity without affecting cell viability, as they decreased nitrite levels even when used at 12.5 μg/mL (p < 0.005) and 50 μM concentration (p < 0.001), respectively. Interestingly, licoflavanone markedly decreased pro-inflammatory cytokines and cyclooxygenase 2/inducible nitric oxide synthase (COX-2/iNOS) expression levels (p < 0.001). A modulation of nuclear factor kappa B/mitogen-activated protein kinases (NF-kB/MAPK) pathway underlay such behavior, highlighting the potential of this natural compound as a new scaffold in anti-inflammatory drug research.

scholarly journals Anti-Inflammatory Activity of the Phlorotannin Trifuhalol A Using LPS-Stimulated RAW264.7 Cells Through NF-κB and MAPK Main Signaling Pathways

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984979 ◽  
Author(s):  
Kasira Phasanasophon ◽  
Sang Moo Kim
Keyword(s):  
Nitric Oxide ◽  
Ethyl Acetate ◽  
Signaling Pathways ◽  
Ethyl Acetate Fraction ◽  
Inflammatory Activity ◽  
Raw264.7 Cells ◽  
No Production ◽  
Mitogen Activated Protein ◽  
Anti Inflammatory ◽  
Factor Α

Trifuhalol A, a phlorotannin, was extracted from Agarum cribrosum with ethyl acetate and fractionated using Sephadex LH-20 column chromatography (SF1-SF6). The ethyl acetate fraction (EAF) and SF5-containing trifuhalol A exhibited strong inhibitory activity against hyaluronidase. The anti-inflammatory activity of the phlorotannin, EAF, and SF5 was determined through the inhibition of nitric oxide (NO) production in lipopolysaccharide-stimulated RAW264.7 cells. Furthermore, the inhibition of NO production was validated by confirming the appreciable downregulation of inducible nitric oxide synthase expression. Agarum cribrosum phlorotannin also markedly suppressed the expression of cyclooxygenase-2, interleukin (IL)-1β, IL-6, and tumor necrosis factor-α. In addition, the anti-inflammatory action was verified by examining its effects on proinflammatory signaling pathways. The activation of nuclear factor (NF)-κB and mitogen-activated protein kinases (MAPKs) was attenuated via the inhibition of NF-κB p-65, c-Jun N-terminal kinase, extracellular signal-regulated kinase 1/2, and p38 MAPK phosphorylation. Therefore, trifuhalol A is a potential source for either the prevention or the treatment of inflammation.

scholarly journals Prunetin 4′-O-Phosphate, a Novel Compound, in RAW 264.7 Macrophages Exerts Anti-Inflammatory Activity viaSuppression of MAP Kinases and the NFκB Pathway

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6841
Author(s):  
Tae-Jin Park ◽  
Hyehyun Hong ◽  
Min-Seon Kim ◽  
Jin-Soo Park ◽  
Won-Jae Chi ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Map Kinases ◽  
Degradation Process ◽  
Inflammatory Activity ◽  
In Vitro Assays ◽  
Raw 264.7 ◽  
Mitogen Activated Protein ◽  
Anti Inflammatory ◽  
Nfκb Pathway

Biorenovation, a microbial enzyme-assisted degradation process of precursor compounds, is an effective approach to unraveling the potential bioactive properties of the derived compounds. In this study, we obtained a new compound, prunetin 4′-O-phosphate (P4P), through the biorenovation of prunetin (PRN), and investigated its anti-inflammatory effects in lipopolysaccharide (LPS)-treated RAW 264.7 macrophage cells. The anti-inflammatory effect of P4P was evaluated by measuring the production of prostaglandin-E2 (PGE2), nitric oxide (NO), which is an inflammation-inducing factor, and related cytokines such as tumor necrosis factor-α (TNFα), interleukin-1β (IL1β), and interleukin-6 (IL6). The findings demonstrated that P4P was non-toxic to cells, and its inhibition of the secretion of NO—as well as pro-inflammatory cytokines—was concentration-dependent. A simultaneous reduction in the protein expression level of pro-inflammatory proteins such as cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) was observed. Moreover, the phosphorylation of mitogen-activated protein kinases (MAPKs) such as extracellular signal-regulated kinases (ERKs), c-Jun N-terminal kinase (JNK), p38 MAPK (p38), and nuclear factor kappa B (NFκB) was downregulated. To conclude, we report that biorenovation-based phosphorylation of PRN improved its anti-inflammatory activity. Cell-based in vitro assays further confirmed that P4P could be applied in the development of anti-inflammatory therapeutics.

Alpha-Pinene Exhibits Anti-Inflammatory Activity Through the Suppression of MAPKs and the NF-κB Pathway in Mouse Peritoneal Macrophages

2015 ◽  
Vol 43 (04) ◽  
pp. 731-742 ◽  
Author(s):  
Dae-Seung Kim ◽  
Hyun-Ja Lee ◽  
Yong-Deok Jeon ◽  
Yo-Han Han ◽  
Ji-Ye Kee ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Inflammatory Responses ◽  
Inflammatory Diseases ◽  
Peritoneal Macrophages ◽  
Inflammatory Activity ◽  
Potential Candidate ◽  
Alpha Pinene ◽  
Mitogen Activated Protein ◽  
Anti Inflammatory ◽  
Mouse Peritoneal Macrophages

In this study, we found that alpha-pinene (α-pinene) exhibits anti-inflammatory activity through the suppression of mitogen-activated protein kinases (MAPKs) and the nuclear factor-kappa B (NF-κB) pathway in mouse peritoneal macrophages. α-Pinene is found in the oils of many coniferous trees and rosemary. We investigated the inhibitory effects of α-Pinene on inflammatory responses induced by lipopolysaccharide (LPS) using mouse peritoneal macrophages. α-Pinene significantly decreased the LPS-induced production of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), and nitric oxide (NO). α-Pinene also inhibited inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expressions in LPS-stimulated macrophages. Additionally, the activations of MAPKs and NF-κB were attenuated by means of α-pinene treatment. These results indicate that α-pinene has an anti-inflammatory effect and that it is a potential candidate as a new drug to treat various inflammatory diseases.

scholarly journals Luteolin-3′-O-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7393
Author(s):  
Jung-Hwan Kim ◽  
Tae-Jin Park ◽  
Jin-Soo Park ◽  
Min-Seon Kim ◽  
Won-Jae Chi ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Inflammatory Responses ◽  
Mitogen Activated Protein Kinase ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Mitogen Activated Protein ◽  
Anti Inflammatory

Luteolin (LT), present in most plants, has potent anti-inflammatory properties both in vitro and in vivo. Furthermore, some of its derivatives, such as luteolin-7-O-glucoside, also exhibit anti-inflammatory activity. However, the molecular mechanisms underlying luteolin-3′-O-phosphate (LTP)-mediated immune regulation are not fully understood. In this paper, we compared the anti-inflammatory properties of LT and LTP and analyzed their molecular mechanisms of action; we obtained LTP via the biorenovation of LT. We investigated the anti-inflammatory activities of LT and LTP in macrophage RAW 264.7 cells. We confirmed from previously reported literature that LT inhibits the production of nitric oxide and prostaglandin E2, as well as the expression of inducible NO synthetase and cyclooxygenase-2. In addition, expressions of inflammatory genes and mediators, such as tumor necrosis factor-α, interleukin-6, and interleukin-1β, were suppressed. LTP showed anti-inflammatory activity similar to LT, but better anti-inflammatory activity in all the experiments, while also inhibiting mitogen-activated protein kinase and nuclear factor-kappa B more effectively than LT. At a concentration of 10 μM, LTP showed differences of 2.1 to 44.5% in the activity compared to LT; it also showed higher anti-inflammatory activity. Our findings suggest that LTP has stronger anti-inflammatory activity than LT.

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