Anti-inflammatory activity of caffeic acid phenethyl ester (CAPE) extracted from Rhodiola sacra against lipopolysaccharide-induced inflammatory responses in mice

Lilium bulbs have long been used as Chinese traditional medicines to alleviate the symptoms of various human inflammatory diseases. However, mechanisms of Lilium bulb-mediated anti-inflammatory activity and the bioactive components in Lilium bulbs remain unknown. In the present study, the anti-inflammatory activity of Lilium bulbs and the underlying mechanism of action were investigated in macrophages using Lilium bulb ethanol extracts (Lb-EE). In a dose-dependent manner, Lb-EE inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and bone marrow-derived macrophages (BMDMs) without causing significant cytotoxicity. Lb-EE also down-regulated mRNA expression of inflammatory genes in LPS-stimulated RAW264.7 cells, which included inducuble nitric oxide synthase (iNOS), cyclooxygenase-2 (COX2), and tumor necrosis factor-[Formula: see text] (TNF-[Formula: see text]). Furthermore, Lb-EE markedly restored LPS-induced morphological changes in RAW264.7 cells to a normal morphology. HPLC analysis identified quercetin, luteolin, and kaempferol as bioactive components contained in Lb-EE. Mechanistic studies in LPS-stimulated RAW264.7 cells revealed that Lb-EE suppressed MyD88- and TRIF-induced NF-[Formula: see text]B transcriptional activation and the nuclear translocation of NF-[Formula: see text]B transcription factors. Moreover, Lb-EE inhibited IKK[Formula: see text]/[Formula: see text]-induced activation of the NF-[Formula: see text]B signaling pathway and IKK inhibition significantly reduced NO production in LPS-stimulated RAW264.7 cells. Taken together, these results suggest that Lb-EE plays an anti-inflammatory role by targeting IKK[Formula: see text]/[Formula: see text]-mediated activation of the NF-[Formula: see text]B signaling pathway during macrophage-mediated inflammatory responses.

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Caffeic acid phenethyl ester attenuates nuclear factor‑κB‑mediated inflammatory responses in M�ller cells and protects against retinal ganglion cell death

Molecular Medicine Reports ◽

10.3892/mmr.2019.10151 ◽

2019 ◽

Cited By ~ 2

Author(s):

Yanwen Jia ◽

Shengqun Jiang ◽

Chen Chen ◽

Guohua Lu ◽

Yang Xie ◽

...

Keyword(s):

Cell Death ◽

Ganglion Cell ◽

Caffeic Acid ◽

Inflammatory Responses ◽

Nuclear Factor Κb ◽

Caffeic Acid Phenethyl Ester ◽

Nuclear Factor ◽

Retinal Ganglion ◽

Retinal Ganglion Cell Death ◽

Ganglion Cell Death

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In vitro and in vivo delivery of atorvastatin: A comparative study of anti-inflammatory activity of atorvastatin loaded copolymeric micelles

Journal of Biomaterials Applications ◽

10.1177/0885328217750821 ◽

2017 ◽

Vol 32 (8) ◽

pp. 1127-1138 ◽

Cited By ~ 9

Author(s):

Sina Andalib ◽

Pezhman Molhemazar ◽

Hossein Danafar

Keyword(s):

Inflammatory Responses ◽

Inflammatory Activity ◽

Lipid Lowering ◽

Precipitation Method ◽

Paw Edema ◽

Scanning Calorimetry ◽

Rat Paw Edema ◽

Anti Inflammatory

Statins have been shown to exert ‘pleiotropic effects’ independent of their cholesterol lowering actions that include anti-inflammatory properties. In this study we synthesized mono methoxy poly (ethylene glycol)–poly (ε-caprolactone) (mPEG-PCL) di block copolymers. The structure of the copolymers was characterized by H nuclear magnetic resonance, Fourier-transform infrared spectroscopy, differential scanning calorimetry and gel permeation chromatography techniques. In this method, atorvastatin was encapsulated within micelles through a single-step nano-precipitation method, leading to the formation of atorvastatin-loaded mPEG-PCL (atorvastatin/mPEG-PCL) micelles. The resulting micelles were characterized further by various techniques such as dynamic light scattering and atomic force microscopy. In this study the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles on acute models of inflammation are analyzed, to compare the effect of indometacin in rats. Carrageenan induces rat paw edema; six animals of each group (10 groups) received indometacin, atorvastatin, and atorvastatin/mPEG-PCL micelles orally 1, 6, 12 and 24 h before carrageenan injection in paw. The paw edema thickness measured at 1, 2, 3 and 4 h after injection and percentage inhibition of edema in various groups were calculated. The results showed that the zeta potential of micelles was about −16.6 mV and the average size was 81.7 nm. Atorvastatin was encapsulated into mPEG-PCL micelles with loading capacity of 14.60 ± 0.96% and encapsulation efficiency of 62.50 ± 0.84%. Atorvastatin and atorvastatin/mPEG-PCL micelles showed significant anti-inflammatory activity in the present study. The anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles was significant in comparison with indometacin. Atorvastatin/mPEG-PCL micelles showed more anti-inflammatory activity than atorvastatin. This study revealed the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles and suggested the statins have a potential inflammatory activity along with its lipid lowering properties. Contrary to anti-inflammatory effects, the pro-inflammatory responses are independent of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition and can be mediated directly by atorvastatin.

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Hydrophilic Phytochelators in Iron Overload Condition

Journal of Nutrition and Food Security ◽

10.18502/jnfs.v4i2.776 ◽

2019 ◽

Author(s):

Zohreh Sajadi Hezaveh ◽

Farzad Shidfar

Keyword(s):

Adverse Effects ◽

Iron Overload ◽

Caffeic Acid ◽

Iron Absorption ◽

Kojic Acid ◽

Inflammatory Activity ◽

Iron Chelators ◽

Natural Iron ◽

Chelating Ability ◽

Anti Inflammatory

Background: Iron overload can cause many complications and damage many organs as well as physiologic functions. Consumption of phetochemicals and flavonoids with iron chelating ability, instead of synthetic iron chelators, can be less harmful and more effective. The aim of this review is to investigate hydrophilic phytochelators in iron overload condition. Methods: In this review, the possible natural iron chelators including quercetin, rutin, bailcalin, silymarin, resveratrol, mimosine, tropolone, curcumine, catechin, kojic acid, and caffeic acid were investigated. Furthermore, the mechanisms through which they chelate iron were discussed. Results: The mentioned antioxidants eliminated excessive iron, decreased iron absorption, exerted antioxidant and anti-inflammatory activity without causing adverse effects and other metal deficiencies in iron overload condition. Conclusion: The combination of synthetic chelators with these antioxidants or their replacement with natural chelators could be possible treatments for iron overload.

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Study on Anti-Inflammatory Activity of Niloticin by Targeting MD-2 Based on Computer-Aided Drug Design and Biolayer Interferometry

Annals of Hematology & Oncology ◽

10.26420/annhematoloncol.2021.1370 ◽

2021 ◽

Vol 8 (10) ◽

Author(s):

Chen G ◽

◽

Liu Y ◽

Zhang M ◽

Xu Y ◽

...

Keyword(s):

Inflammatory Responses ◽

Inflammatory Activity ◽

Myeloid Differentiation ◽

Control Group ◽

Toll Like Receptor ◽

Expression Levels ◽

Biolayer Interferometry ◽

Inflammatory Mechanism ◽

Anti Inflammatory ◽

Cortex Phellodendri

Niloticin is an active compound from Cortex phellodendri, but its antiinflammatory activity has not yet been explored. The aim of the present study was to assess the drug potential of niloticin and to study the MD-2-targeting mechanism of its anti-inflammatory activity. Niloticin’s drug potential was analyzed using the Traditional Chinese Medicine Systems Pharmacology Database. Molecular docking and biolayer interferometry technology were used to explore the anti-inflammatory mechanism of niloticin by targeting myeloid differentiation protein 2 (MD-2), which mediates a series of Toll-Like Receptor (TLR) 4-dependent inflammatory responses. The cytokines involved in the LPSTLR4/ MD-2-NF-κB pathway were evaluated by ELISA, RT-PCR, and western blot. The results showed that niloticin has drug potential and could bind to MD- 2. Niloticin had no impact on cell viability. Niloticin could significantly decrease the levels of NO, IL-6, TNF-a, and IL-1β (P<0.01) induced by LPS. IL-1β, IL-6, iNOS, TNF-a, and COX-2 mRNA expression levels were decreased by niloticin (all P<0.01). Compared with the control group, TLR4, p65, MyD88, p-p65, and iNOS expression levels induced by LPS were suppressed by niloticin (all P<0.01). In conclusion, niloticin is a potential MD-2 antagonist. It might interact with MD-2 to play an anti-inflammatory role by suppressing the activation of the LPS-TLR4/MD-2-NF-κB signaling pathway.

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Anti-Inflammatory Activity of 4-((1R,2R)-3-Hydroxy-1-(4-hydroxyphenyl)-1-methoxypropan-2-yl)-2-methoxyphenol Isolated from Juglans mandshurica Maxim. in LPS-Stimulated RAW 264.7 Macrophages and Zebrafish Larvae Model

Pharmaceuticals ◽

10.3390/ph14080771 ◽

2021 ◽

Vol 14 (8) ◽

pp. 771

Author(s):

Su-Hyeon Cho ◽

SeonJu Park ◽

Hoibin Jeong ◽

Song-Rae Kim ◽

Myeong Seon Jeong ◽

...

Keyword(s):

Nitric Oxide ◽

Inflammatory Responses ◽

Inflammatory Activity ◽

Raw 264.7 Cells ◽

No Production ◽

Raw 264.7 ◽

Dependent Manner ◽

Juglans Mandshurica ◽

Zebrafish Larvae ◽

Anti Inflammatory

Juglans mandshurica Maxim., a traditional folk medicinal plant, is widely distributed in Korea and China. In our previous study, we isolated a new phenylpropanoid compound, 4-((1R,2R)-3-hydroxy-1-(4-hydroxyphenyl)-1-methoxypropan-2-yl)-2-methoxyphenol (HHMP), from J. mandshurica. In the present study, we evaluated the anti-inflammatory activity of HHMP on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells and zebrafish larvae. HHMP significantly inhibited LPS-induced nitric oxide (NO) and prostaglandin E2 production in a dose-dependent manner. Moreover, HHMP treatment considerably suppressed LPS-induced expression of inducible nitric oxide synthase and cyclooxygenase-2. We also demonstrated the mechanisms of HHMP inhibition of inflammatory responses in LPS-stimulated RAW 264.7 cells via Western blot analysis and immunofluorescence staining. Furthermore, HHMP significantly inhibited NO production in LPS-stimulated zebrafish larvae. Consequently, we established that HHMP significantly inhibited the LPS-induced activation of NF-κB and MAPK and the nuclear translocation of p65 in RAW 264.7 cells. Taken together, our findings demonstrate the effect of HHMP on LPS-induced inflammatory responses in vitro and in vivo, suggesting its potential to be used as a natural anti-inflammatory agent.

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A Glycosaminoglycan-Rich Fraction from Sea Cucumber Isostichopus badionotus Has Potent Anti-Inflammatory Properties In Vitro and In Vivo

Nutrients ◽

10.3390/nu12061698 ◽

2020 ◽

Vol 12 (6) ◽

pp. 1698

Author(s):

Leticia Olivera-Castillo ◽

George Grant ◽

Nuvia Kantún-Moreno ◽

Hirian A. Barrera-Pérez ◽

Jorge Montero ◽

...

Keyword(s):

Sea Cucumber ◽

Inflammatory Responses ◽

Ethanol Extract ◽

Inflammatory Activity ◽

Bioactive Constituents ◽

Mouse Ear ◽

Health Promoting ◽

Anti Inflammatory

Sea cucumber body wall contains several naturally occurring bioactive components that possess health-promoting properties. Isostichopus badionotus from Yucatan, Mexico is heavily fished, but little is known about its bioactive constituents. We previously established that I. badionotus meal had potent anti-inflammatory properties in vivo. We have now screened some of its constituents for anti-inflammatory activity in vitro. Glycosaminoglycan and soluble protein preparations reduced 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammatory responses in HaCaT cells while an ethanol extract had a limited effect. The primary glycosaminoglycan (fucosylated chondroitin sulfate; FCS) was purified and tested for anti-inflammatory activity in vivo. FCS modulated the expression of critical genes, including NF-ĸB, TNFα, iNOS, and COX-2, and attenuated inflammation and tissue damage caused by TPA in a mouse ear inflammation model. It also mitigated colonic colitis caused in mice by dextran sodium sulfate. FCS from I. badionotus of the Yucatan Peninsula thus had strong anti-inflammatory properties in vivo.

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