scholarly journals Pilloin, A Flavonoid Isolated from Aquilaria sinensis, Exhibits Anti-Inflammatory Activity In Vitro and In Vivo

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3177 ◽  
Author(s):  
Yun-Chen Tsai ◽  
Sin-Ling Wang ◽  
Mei-Yao Wu ◽  
Chia-Huei Liao ◽  
Chao-Hsiung Lin ◽  
...  
Keyword(s):  
Mitogen Activated Protein Kinase ◽  
Inflammatory Activity ◽  
Flavonoid Compound ◽  
Raw 264.7 ◽  
Aquilaria Sinensis ◽  
Raw 264.7 Macrophages ◽  
Tnf Α ◽  
Anti Inflammatory

Flavonoids, widely present in medicinal plants and fruits, are known to exhibit multiple pharmacological activities. In this study, we isolated a flavonoid compound, pilloin, from Aquilaria sinensis and investigated its anti-inflammatory activity in bacterial lipopolysaccharide-induced RAW 264.7 macrophages and septic mice. Pilloin inhibited NF-κB activation and reduced the phosphorylation of IκB in LPS-stimulated macrophages. Moreover, pilloin significantly suppressed the production of pro-inflammatory molecules, such as TNF-α, IL-6, COX-2 and iNOS, in LPS-treated RAW 264.7 macrophages. Additionally, pilloin suppressed LPS-induced morphological alterations, phagocytic activity and ROS elevation in RAW 264.7 macrophages. The mitogen-activated protein kinase-mediated signalling pathways (including JNK, ERK, p38) were also inhibited by pilloin. Furthermore, pilloin reduced serum levels of TNF-α (from 123.3 ± 7 to 46.6 ± 5.4 ng/mL) and IL-6 levels (from 1.4 ± 0.1 to 0.7 ± 0.1 ng/mL) in multiple organs of LPS-induced septic mice (liver: from 71.8 ± 3.2 to 36.7 ± 4.3; lung: from 118.6 ± 10.6 to 75.8 ± 11.9; spleen: from 185.9 ± 23.4 to 109.6 ± 18.4; kidney: from 160.3 ± 11.8 to 75 ± 10.8 pg/mL). In summary, our results demonstrate the anti-inflammatory potential of pilloin and reveal its underlying molecular mechanism of action.

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.

scholarly journals In Vitro and In Vivo Anti-Inflammatory Effects of Sulfated Polysaccharides Isolated from the Edible Brown Seaweed, Sargassum fulvellum

Marine Drugs ◽  
2021 ◽  
Vol 19 (5) ◽  
pp. 277
Author(s):  
Lei Wang ◽  
Hye-Won Yang ◽  
Ginnae Ahn ◽  
Xiaoting Fu ◽  
Jiachao Xu ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Brown Seaweed ◽  
Sulfated Polysaccharides ◽  
Raw 264.7 ◽  
Raw 264.7 Macrophages ◽  
Sargassum Fulvellum ◽  
Pharmaceutical Industries ◽  
Anti Inflammatory

In the present study, the in vitro and in vivo anti-inflammatory effects of the sulfated polysaccharides isolated from Sargassum fulvellum (SFPS) were evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and zebrafish. The results indicated that SFPS improved the viability of LPS-stimulated RAW 264.7 macrophages from 80.02 to 86.80, 90.09, and 94.62% at the concentration of 25, 50, and 100 µg/mL, respectively. Also, SFPS remarkably and concentration-dependently decreased the production levels of inflammatory molecules including nitric oxide (NO), tumor necrosis factor-alpha, prostaglandin E2, interleukin-1 beta, and interleukin-6 in LPS-treated RAW 264.7 macrophages. In addition, SFPS significantly inhibited the expression levels of cyclooxygenase-2 and inducible nitric oxide synthase in LPS-treated RAW 264.7 macrophages. Furthermore, the in vivo test results indicated that SFPS improved the survival rate of LPS-treated zebrafish from 53.33 to 56.67, 60.00, and 70.00% at the concentration of 25, 50, and 100 µg/mL, respectively. In addition, SFPS effectively reduced cell death, reactive oxygen species, and NO levels in LPS-stimulated zebrafish. Taken together, these results suggested that SFPS possesses strong in vitro and in vivo anti-inflammatory activities, and could be used as an ingredient to develop anti-inflammatory agents in the functional food and pharmaceutical industries.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF KNEMA ATTENUATA (HOOK. F. AND THOMSON) WARB ETHANOLIC STEM BARK EXTRACT IN ALBINO WISTAR RATS

2019 ◽  
pp. 330-334
Author(s):  
SUPRIYA RAJA H
Keyword(s):  
Stem Bark ◽  
Inflammatory Activity ◽  
Assay Method ◽  
Bark Extract ◽  
Raw 264.7 ◽  
Myeloperoxidase Activity ◽  
Stem Bark Extract ◽  
Anti Inflammatory

Objective: Knema attenuata (Myristicaceae), popularly known as “wild nutmeg,” is an endemic tree species from Western Ghats, which has been used in folk medicine. Conventionally, the stem bark of K. attenuata is used for treating inflammatory conditions without any scientific information available for the same. The present study was undertaken to evaluate the anti-inflammatory activity of the ethanolic stem bark extract (ESBE) of K. attenuata using in vivo and in vitro screening models. Methods: The ethanolic extract of stem bark was prepared by soxhlation, and its cytotoxicity in RAW 264.7 cell line was assessed using MTT assay method. In vivo anti-inflammatory effect of extract was estimated in rats using carrageenan-induced paw edema model and cotton pellet-induced granuloma model. The in vitro anti-inflammatory activity of the extract was evaluated by cyclooxygenase and lipoxygenase inhibition assay, estimation of myeloperoxidase activity, and determination of cellular nitrite levels in lipopolysaccharide-stimulated RAW 264.7 macrophage cells. Results: Toxic symptoms were not observed for the ESBE. The extract demonstrated significant anti-inflammatory activity in both in vivo and in vitro models. The anti-inflammatory action exhibited by the extract was a result of the inhibition of leukocyte migration and nitric oxide pathway and partially by inhibition of mediators such as prostaglandins and leukotrienes. Conclusion: Findings from the study provide the evidence for the popular use of stem bark extract of K. attenuata as a potential anti-inflammatory agent.

scholarly journals Anti-Inflammatory Activity of Four Triterpenoids Isolated from Poriae Cutis

Foods ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 3155
Author(s):  
Lijia Zhang ◽  
Mengzhou Yin ◽  
Xi Feng ◽  
Salam A. Ibrahim ◽  
Ying Liu ◽  
...  
Keyword(s):  
High Speed ◽  
High Performance ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Dose Dependent

In this study, triterpenoid compounds from Poriae Cutis were separated by high-speed countercurrent chromatography (HSCCC) and identified using ultra-high performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry (UHPLC-QTOF-MS/MS) and nuclear magnetic resonance (NMR). The in vitro anti-inflammatory activities of the purified triterpenoids on RAW 264.7 cells were also investigated. Triterpenoids, poricoic acid B, poricoic acid A, dehydrotrametenolic acid, and dehydroeburicoic acid were obtained; their levels of purity were 90%, 92%, 93%, and 96%, respectively. The results indicated that poricoic acid B had higher anti-inflammatory activity than those of poricoic acid A by inhibiting the generation of NO in lipopolysaccharide (LPS)-induced RAW 264.7 cells. However, dehydrotrametenolic acid and dehydroeburicoic acid had no anti-inflammatory activity. In addition, the production of cytokines (TNF-α, IL-1β, and IL-6) in cells treated with poricoic acid B decreased in a dose-dependent manner in the concentration range from 10 to 40 μg/mL. The results provide evidence for the use of Poriae Cutis as a natural anti-inflammatory agent in medicines and functional foods.

scholarly journals Enhanced anti-inflammatory effect of resveratrol and EPA in treated endotoxin-activated RAW 264.7 macrophages

2012 ◽  
Vol 108 (9) ◽  
pp. 1562-1573 ◽  
Author(s):  
Victor Pallarès ◽  
Damien Calay ◽  
Lídia Cedó ◽  
Anna Castell-Auví ◽  
Martine Raes ◽  
...  
Keyword(s):  
Epigallocatechin Gallate ◽  
No Production ◽  
Raw 264.7 ◽  
Fish Food ◽  
Antioxidant Genes ◽  
Raw 264.7 Macrophages ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Macrophages play an important role in immunogenic challenges by producing reactive oxygen species, NO and proinflammatory cytokines that can aggravate and propagate local inflammation. Multiple mechanisms regulate these inflammatory processes. NF-κB and activator protein 1 pathways are crucial in the expression of proinflammatory genes, such as TNF-α, IL-1 (α or β) and -6. Some polyphenols, which are present in beverages, vegetables and fruits, and PUFA, which are present in marine oils and fish food, possess anti-inflammatory effects in vivo and in vitro. Our aim in the present study was to assess whether polyphenols and PUFA have synergistic anti-inflammatory effects in murine macrophages in vitro. Inflammation in RAW 264.7 macrophages was induced by lipopolysaccharide at 100 ng/ml. The treatments with molecules were performed by co-incubation for 19 h. A NO production assay by Griess reaction, a phosphoprotein assay by Pathscan ELISA kit and gene expression analysis using the TaqMan® Low-density Array for ninety-one genes related to inflammation, oxidative stress and metabolism were performed to assess the synergistic anti-inflammatory effects of polyphenols, epigallocatechin gallate and resveratrol (Res; 2·5 μg/ml), and the PUFA, DHA and EPA (30 μm). Adding Res+EPA had an enhanced anti-inflammatory effect, in comparison with EPA and Res alone, leading to decreased NO levels; modulating the phospho-stress activated protein kinase/Jun N-terminal kinase (P-SAPK/JNK) level; down-regulating proinflammatory genes, such as IL, chemokines, transcription factors; and up-regulating several antioxidant genes. Therefore, this combination has a stronger anti-inflammatory effect than either of these molecules separately in RAW macrophages.

scholarly journals Efficient In Vitro and In Vivo Anti-Inflammatory Activity of a Diamine-PEGylated Oleanolic Acid Derivative

2021 ◽  
Vol 22 (15) ◽  
pp. 8158
Author(s):  
Fatin Jannus ◽  
Marta Medina-O’Donnell ◽  
Veronika E. Neubrand ◽  
Milagros Marín ◽  
Maria J. Saez-Lara ◽  
...  
Keyword(s):  
Oleanolic Acid ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Tetradecanoyl Phorbol Acetate ◽  
Tnf Α ◽  
Effective Therapeutic Strategy ◽  
Anti Inflammatory ◽  
Inflammatory Action

Recent evidence has shown that inflammation can contribute to all tumorigenic states. We have investigated the anti-inflammatory effects of a diamine-PEGylated derivative of oleanolic acid (OADP), in vitro and in vivo with inflammation models. In addition, we have determined the sub-cytotoxic concentrations for anti-inflammatory assays of OADP in RAW 264.7 cells. The inflammatory process began with incubation with lipopolysaccharide (LPS). Nitric oxide production levels were also determined, exceeding 75% inhibition of NO for a concentration of 1 µg/mL of OADP. Cell-cycle analysis showed a reversal of the arrest in the G0/G1 phase in LPS-stimulated RAW 264.7 cells. Furthermore, through Western blot analysis, we have determined the probable molecular mechanism activated by OADP; the inhibition of the expression of cytokines such as TNF-α, IL-1β, iNOS, and COX-2; and the blocking of p-IκBα production in LPS-stimulated RAW 264.7 cells. Finally, we have analyzed the anti-inflammatory action of OADP in a mouse acute ear edema, in male BL/6J mice treated with OADP and tetradecanoyl phorbol acetate (TPA). Treatment with OADP induced greater suppression of edema and decreased the ear thickness 14% more than diclofenac. The development of new derivatives such as OADP with powerful anti-inflammatory effects could represent an effective therapeutic strategy against inflammation and tumorigenic processes.

scholarly journals In Vitro and In Vivo Anti-Inflammatory Activity of Tetrastigma Sulcatum Leaf Extract, Pure Compound and Its Derivatives

2021 ◽  
Author(s):  
Ravindra Jagannath Waghole ◽  
Ashwini Vivek Misar ◽  
Neha Shashikant Kulkarni ◽  
Feroz Khan ◽  
Dattatraya Gopal Naik ◽  
...  
Keyword(s):  
Proinflammatory Cytokines ◽  
Crude Extract ◽  
Leaf Extract ◽  
Inflammatory Activity ◽  
No Production ◽  
Pure Compound ◽  
Tnf Α ◽  
Anti Inflammatory

Abstract The severity and perseverance of the inflammation have been demonstrated in many health conditions. The limitations of existing medications, propose the need for newer alternative anti-inflammatory medications. In our earlier studies, we demonstrated the topical anti-inflammatory potential of crude ethanolic extract of Tetrastigma sulcatum leaves and its fractions. In the present study, we further explored anti-inflammatory activity of T. sulcatum extract, fractions, pure compound and its derivatives using in vitro and in vivo bioassay techniques. We attempted to isolate a pure compound from leaf extract and was identified as Friedelan-3β-ol (CI) and its derivatives Friedelinol acetate (C II) and Friedelinol methyl ether (C III) were synthesized. Treatment with crude extract and its fractions demonstrated a significant reduction in the mRNA expression levels of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) and nitric oxide (NO) production in LPS-stimulated inflammation in RAW 264.7 cells. Likewise, compounds CI, CII and CIII showed a similar pattern of significant inhibition of proinflammatory cytokines and NO production. In vivo study in Carrageenan induced paw-inflammatory mice model demonstrated reduced paw oedema and proinflammatory cytokines levels in a dose-dependent manner upon treatment of extract, its fractions, pure compound (CI), and their derivatives (CII and CIII.). The docking study showed all the compounds (CI, CII and CIII) share common residues with Dexamethasone. TNF- α exhibited the most interacting residues with the compounds. The present study confirmed the T. sulcatum ’s anti-inflammatory activity, suggesting Friedelan-3β-ol as an active component in a crude extract.

scholarly journals Inhibition of Skin Inflammation by Scytonemin, an Ultraviolet Sunscreen Pigment

Marine Drugs ◽  
2020 ◽  
Vol 18 (6) ◽  
pp. 300
Author(s):  
Moo Rim Kang ◽  
Sun Ah Jo ◽  
Hyunju Lee ◽  
Yeo Dae Yoon ◽  
Joo-Hee Kwon ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nuclear Translocation ◽  
Skin Inflammation ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Blue Green Algae ◽  
Tnf Α ◽  
Anti Inflammatory

Scytonemin is a yellow-green ultraviolet sunscreen pigment present in different genera of aquatic and terrestrial blue-green algae, including marine cyanobacteria. In the present study, the anti-inflammatory activities of scytonemin were evaluated in vitro and in vivo. Topical application of scytonemin inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear swelling in BALB/c mice. The expression of tumor necrosis factor-α (TNF-α) and inducible nitric oxide synthase (iNOS) was also suppressed by scytonemin treatment in the TPA-treated ear of BALB/c mice. In addition, scytonemin inhibited lipopolysaccharide (LPS)-induced production of TNF-α and nitric oxide (NO) in RAW 264.7 cells, a murine macrophage-like cell line, and the mRNA expressions of TNF-α and iNOS were also suppressed by scytonemin in LPS-stimulated RAW 264.7 cells. Further study demonstrated that LPS-induced NF-κB activity was significantly suppressed by scytonemin treatment in RAW 264.7 cells. Our results also showed that the degradation of IκBα and nuclear translocation of the p65 subunit were blocked by scytonemin in LPS-stimulated RAW 264.7 cells. Collectively, these results suggest that scytonemin inhibits skin inflammation by blocking the expression of inflammatory mediators, and the anti-inflammatory effect of scytonemin is mediated, at least in part, by down-regulation of NF-κB activity. Our results also suggest that scytonemin might be used as a multi-function skin care ingredient for UV protection and anti-inflammation.

scholarly journals Pediococcus pentosaceus-Fermented Cordyceps militaris Inhibits Inflammatory Reactions and Alleviates Contact Dermatitis

2018 ◽  
Vol 19 (11) ◽  
pp. 3504 ◽  
Author(s):  
Ha-Kyoung Kwon ◽  
Min-Jung Song ◽  
Hye-Ji Lee ◽  
Tae-Sik Park ◽  
Moon Kim ◽  
...  
Keyword(s):  
Contact Dermatitis ◽  
Cordyceps Militaris ◽  
Raw 264.7 ◽  
Raw 264.7 Macrophages ◽  
Pediococcus Pentosaceus ◽  
Inflammatory Reactions ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Cordyceps militaris is a medicinal mushroom used to treat immune-related diseases in East Asia. We investigated the anti-inflammatory effect of the extract of C. militaris grown on germinated Rhynchosia nulubilis (GRC) fermented with Pediococcus pentosaceus ON89A isolated from onion (GRC-ON89A) in vivo as well as in vitro. The anti-inflammatory effect of GRC-ON89A was investigated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. The total polyphenol content (TPC) and total flavonoid content (TFC) in the GRC-ON89A ethanol extract were significantly increased compared to that in GRC. GRC-ON89A hexane fraction (GRC-ON89A-Hex) inhibited the release of nitric oxide (NO) compared to that of the LPS-treated control without cytotoxicity in LPS-stimulated RAW 264.7 macrophages. GRC-ON89A-Hex decreased the inducible NO synthase (iNOS), cyclooxygenase 2 (COX2), and tumor necrosis factor (TNF)-α mRNA expression in LPS-stimulated RAW 264.7 macrophages. In addition, pre-treatment with GRC-ON89A-Hex significantly inhibited LPS-stimulated phosphorylation of mitogen-activated protein kinases (MAPKs) and nuclear factor (NF)-κB. To induce allergic contact dermatitis (ACD), 1-fluoro-2, 4-dinitrofluorobenzene (DNFB) was applied to the surface of the right ears of C57BL/6N mice. GRC-ON89A reduced the ear swelling and thickness in DNFB-induced ACD mice. This study demonstrates the potential usefulness of GRC-ON89A as an anti-inflammatory dietary supplement or drug.

scholarly journals Anti-Inflammatory Comparison of Melatonin and Its Bromobenzoylamide Derivatives in Lipopolysaccharide (LPS)-Induced RAW 264.7 Cells and Croton Oil-Induced Mice Ear Edema

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4285
Author(s):  
Pimpichaya Sangchart ◽  
Panyada Panyatip ◽  
Teerasak Damrongrungruang ◽  
Aroonsri Priprem ◽  
Pramote Mahakunakorn ◽  
...  
Keyword(s):  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
In Vivo Models ◽  
Raw 264.7 Macrophages ◽  
Ear Edema ◽  
Croton Oil ◽  
Anti Inflammatory

The pineal gland is a neuroendocrine organ that plays an important role in anti-inflammation through the hormone melatonin. The anti-inflammatory effects of melatonin and its derivatives have been reported in both in vitro and in vivo models. Our previous study reported the potent antioxidant and neuroprotective activities of bromobenzoylamide substituted melatonin. In silico analysis successfully predicted that melatonin bromobenzoylamid derivatives were protected from metabolism by CYP2A1, which is a key enzyme of the melatonin metabolism process. Therefore, the anti-inflammatory activities of melatonin and its bromobenzoylamide derivatives BBM and EBM were investigated in LPS-induced RAW 264.7 macrophages and croton oil-induced ear edema in mice. The experiments showed that BBM and EBM significantly reduced production of the inflammatory mediators interleukin-6 (IL-6), prostaglandin E2 (PGE2), and nitric oxide (NO) in a dose-dependent manner, but only slightly affected TNF-α in LPS-induced RAW 264.7 macrophages. This suggests that modifying melatonin at either the N1-position or the N-acetyl side chain affected production of NO, PGE2 and IL-6 in in vitro model. In the croton oil-induced mouse ear edema model, BBM, significantly decreased ear edema thickness at 2–4 h. It leads to conclude that bromobenzoylamide derivatives of melatonin may be one of the potential candidates for a new type of anti-inflammatory agent.

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