Chenopodium album L. and Sisymbrium officinale (L.) Scop.: Phytochemical Content and In Vitro Antioxidant and Anti-Inflammatory Potential

Spontaneous edible plants have an old history of use in popular traditions all around the world, and the rediscovery of these species could also be useful for the search of new drugs. Chenopodium album L. (Amaranthaceae) and Sisymbrium officinale (L.) Scop. (Brassicaceae) are two annual plants traditionally used both as food and herbal remedies against inflammatory disorders. In this work, the potential anti-inflammatory and anti-arthritic activities of these plant species have been investigated, together with their antioxidant potential. The phytochemical composition was assessed as well by means of gas chromatography coupled to mass spectrometry (GC-MS) and high performance thin layer chromatography (HPTLC). The antioxidant properties were assessed using the DPPH and β-carotene bleaching test. The ability of extracts to protect against lipid peroxidation was also examined in rat-liver microsomal membranes. All the samples showed a preservation of antioxidant activity up to 60 min. A significant inhibitory activity on the production of the pro-inflammatory mediator nitric oxide was induced in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells by the dichloromethane fraction of C. album extract, with an IC50 value equal to 81.7 ± 0.9 μg/mL. The same sample showed also a concentration-dependent anti-denaturation effect on heat-treated bovine serum albumin (IC50 = 975.6 ± 5.5 μg/mL), even if the best in vitro anti-arthritic activity was observed for the dichloromethane fraction of S. officinale extract, with an IC50 value of 680.9 ± 13.2 μg/mL.

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Construction of a novel quinoxaline as a new class of Nrf2 activator

10.21203/rs.2.12921/v1 ◽

2019 ◽

Author(s):

Murugesh Kandasamy ◽

Kit-Kay Mak ◽

Thangaraj Devadoss ◽

Punniyakoti Veeraveedu Thanikachalam ◽

Raghavendra Sakirolla ◽

...

Keyword(s):

Docking Studies ◽

Metabolic Stability ◽

Raw 264.7 Cells ◽

Raw 264.7 ◽

New Class ◽

Ic50 Value ◽

Kelch Domain ◽

Anti Inflammatory ◽

Nrf2 Activator

Abstract The transcription factor Nuclear factor erythroid-2-related factor 2 (NRF2) and its principal repressive regulator, the E3 ligase adaptor Kelch-like ECH-associated protein 1 (KEAP1), are critical in the regulation of inflammation, as well as maintenance of homeostasis. Thus, NRF2 activation provides cytoprotection against numerous inflammatory disorders. N-nicotinoylquinoxaline-2-carbohdyrazide (NQC) was designed by combining the important pharmacophoric features of bioactive compounds reported in the literature. NQC was synthesised and characterised using spectroscopic techniques. The compound was tested for its anti-inflammatory effect using LPSEc induced inflammation in mouse macrophages (RAW 264.7 cells). The effect of NQC on inflammatory cytokines was measured using ELISA. The Nrf2 activity of the compound NQC was determined using ‘Keap1:Nrf2 Inhibitor Screening Assay Kit’. To obtain the insights on NQC’s activity on Nrf2, molecular docking studies were performed using Schrodinger suite. The metabolic stability of NQC was determined using mouse, rat and human microsomes. NQC was found to be non-toxic until the dose of 50 µM on RAW 264.7 cells. The NQC showed potent anti-inflammatory effect in an in vitro model of Lipopolysaccharide (LPS) stimulated murine macrophages (RAW 264.7 cells) with an IC50 value 26.13 ± 1.17 µM. The NQC dose-dependently down regulated the pro-inflammatory cytokines (Interleukin (IL)-1β, IL-6 and tumor necrosis factor (TNF)-α) and inflammatory mediator, prostaglandin E2 (PGE2) with IC50 values 13.27 ± 2.37, 10.13 ± 0.58, 14.41 ± 1.83 and 15.23 ± 0.91 µM respectively. Molecular docking studies confirmed the favourable binding of NQC at Kelch domain of Keap-1. It disrupts the Nrf2 interaction with kelch domain of keap 1 and its IC50 value was 4.21 ± 0.89 µM. The metabolic stability studies of NQC in human, rat and mouse liver microsomes revealed that it is quite stable with half-life values; 59.78 ± 6.73, 52.93 ± 7.81, 28.43 ± 8.13 minutes; microsomal intrinsic clearance values; 22.1 ± 4.31, 26.0 ± 5.17 and 47.13 ± 6.34 µL/min/mg protein; respectively. So, rat has comparable metabolic profile with human, thus, rat could be used for predicting the pharmacokinetics and metabolism of NQC in human. NQC is a new class of NRF2 activator with potent in vitro anti-inflammatory activity and good metabolic stability.

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Evaluation of Anti-Inflammatory Properties of Isoorientin Isolated from Tubers of Pueraria tuberosa

Oxidative Medicine and Cellular Longevity ◽

10.1155/2017/5498054 ◽

2017 ◽

Vol 2017 ◽

pp. 1-10 ◽

Cited By ~ 19

Author(s):

Kotha Anilkumar ◽

Gorla V. Reddy ◽

Rajaram Azad ◽

Nagendra Sastry Yarla ◽

Gangappa Dharmapuri ◽

...

Keyword(s):

Cell Line ◽

Antioxidant Properties ◽

Model Systems ◽

Raw 264.7 Cells ◽

Raw 264.7 ◽

Pueraria Tuberosa ◽

Cox 2 ◽

Anti Inflammatory

Inflammation is the major causative factor of different diseases such as cardiovascular disease, diabetes, obesity, osteoporosis, rheumatoid arthritis, inflammatory bowel disease, and cancer. Anti-inflammatory drugs are often the first step of treatment in many of these diseases. The present study is aimed at evaluating the anti-inflammatory properties of isoorientin, a selective cyclooxygenase-2 (COX-2) inhibitor isolated from the tubers of Pueraria tuberosa, in vitro on mouse macrophage cell line (RAW 264.7) and in vivo on mouse paw edema and air pouch models of inflammation. Isoorientin reduced inflammation in RAW 264.7 cell line in vitro and carrageenan induced inflammatory animal model systems in vivo. Cellular infiltration into pouch tissue was reduced in isoorientin treated mice compared to carrageenan treated mice. Isoorientin treated RAW 264.7 cells and animals showed reduced expression of inflammatory proteins like COX-2, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), 5-lipoxygenase (5-LOX), and interleukin 1-β (IL-1-β) both in vitro and in vivo. The antioxidant enzyme levels of catalase and GST were markedly increased in isoorientin treated mice compared to carrageenan treated mice. These results suggest that isoorientin, a selective inhibitor of COX-2, not only exerts anti-inflammatory effects in LPS induced RAW cells and carrageenan induced inflammatory model systems but also exhibits potent antioxidant properties.

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Anti-Inflammatory Activity of Four Triterpenoids Isolated from Poriae Cutis

Foods ◽

10.3390/foods10123155 ◽

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.

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Anti-inflammatory Activity of Mollugo cerviana Methanolic Extract in LPS-induced Acute Inflammatory RAW 264.7 Macrophages

Combinatorial Chemistry & High Throughput Screening ◽

10.2174/1386207324666210302101204 ◽

2021 ◽

Vol 24 ◽

Author(s):

Robina Antony ◽

Jijin Raveendran ◽

Prabath Gopalakrishnan Biju

Keyword(s):

Acute Inflammation ◽

Methanolic Extract ◽

Therapeutic Potential ◽

Indian Subcontinent ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Raw 264.7 Cells ◽

Raw 264.7 ◽

Anti Inflammatory

Background: The management of acute inflammation, which arises from complex biological responses to harmful stimuli, is an important determinant in recovery of the system from an otherwise detrimental outcome such as septicemia. However, the side effects and limitations of current therapeutics necessitate the development of newer and safer alternatives. Mollugo cerviana is a common medicinal herb of the Indian subcontinent and has been traditionally used for its fever mitigating, anti-microbial and hepatoprotective action. We have already reported the rich presence of radical scavenging phytochemicals in the plant extracts and their strong antioxidant properties. Objective: In the present study, we have evaluated the anti-inflammatory effects of methanolic extract (ME) of the areal parts of M. cerviana in a lipopolysaccharide (LPS)-induced acute inflammatory cell culture model. Method: RAW 264.7 mouse macrophages cell were stimulated by the bacterial endotoxin LPS at a concentration of 1 µg/mL. Cytotoxicity and anti-inflammatory potential of ME were carried out. Results: M. cerviana extract concentration up to 150 µg/ml was found to be non-toxic to cells (MTT and NRU assay). LPS induces acute inflammation by binding to TLR-4 receptors, initiating downstream signalling cascade that result in pro-inflammatory cytokine secretion. Extract treatment at 100 µg/ml suppressed LPS-induced gene expression (qPCR) and secretion (ELISA) of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α, and the chemokine CCL2, indicating a dampening of the acute inflammatory cascade. LPS-induced elevation of ROS level (DCFDA method) was significant reduced by extract treatment. Nitric oxide production, as indicated by nitrite level, was significantly reduced post extract treatment. Conclusion: From this study, it is demonstrated that M. cerviana methanolic extract has potent anti-inflammatory effect in the in vitro acute inflammation model of LPS-stimulated RAW 264.7 cells. There is not reported study so far on the anti-inflammatory properties of M. cerviana in an LPS-induced acute inflammatory model which closely mimics a human bacteremia response. Hence, this study highlights the therapeutic potential of this extract as a source of anti-inflammatory lead molecules.

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Molecular Mechanisms Underlying theIn VitroAnti-Inflammatory Effects of a Flavonoid-Rich Ethanol Extract from Chinese Propolis (Poplar Type)

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/127672 ◽

2013 ◽

Vol 2013 ◽

pp. 1-11 ◽

Cited By ~ 21

Author(s):

Kai Wang ◽

Shun Ping ◽

Shuai Huang ◽

Lin Hu ◽

Hongzhuan Xuan ◽

...

Keyword(s):

High Performance ◽

Molecular Mechanisms ◽

Ethanol Extract ◽

Raw 264.7 Cells ◽

Dependent Manner ◽

Anti Inflammatory ◽

Basic Studies ◽

Chinese Propolis

China produces the greatest amount of propolis but there is still lack of basic studies on its pharmacological mechanisms. Our previous study found that ethanol extract from Chinese propolis (EECP) exerted excellent anti-inflammatory effectsin vivobut mechanisms of action were elusive. To further clarify the possible mechanisms underlying the anti-inflammatory effects of Chinese propolis (poplar type), we utilized EECP to analyze its chemical composition and evaluated its potential anti-inflammatory effectsin vitro. High-performance liquid chromatography (HPLC) profile indicated that EECP contained abundant flavonoids, including rutin, myricetin, quercetin, kaempferol, apigenin, pinocembrin, chrysin, and galangin. Next we found that EECP could significantly inhibit the production of NO, IL-1β, and IL-6 in lipopolysaccharide- (LPS-) stimulated RAW 264.7 cells and suppress mRNA expression of iNOS, IL-1β, and IL-6 in a time- and dose-dependent manner. Furthermore, we found that EECP could suppress the phosphorylation of IκBαand AP-1 but did not affect IκBα’s degradation. In addition, using a reporter assay, we found that EECP could block the activation of NF-κB in TNF-α-stimulated HEK 293T cells. Our findings give new insights for understanding the mechanisms involved in the anti-inflammatory effects by Chinese propolis and provide additional references for using propolis in alternative and complementary therapies.

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Antioxidant Action and In Vivo Anti-Inflammatory and Antinociceptive Activities of Myrciaria floribunda Fruit Peels: Possible Involvement of Opioidergic System

Advances in Pharmacological and Pharmaceutical Sciences ◽

10.1155/2020/1258707 ◽

2020 ◽

Vol 2020 ◽

pp. 1-11

Author(s):

Izabelly Bianca da Silva Santos ◽

Bruno Santos dos Santos ◽

João Ricardhis Saturnino de Oliveira ◽

Wêndeo Kennedy Costa ◽

Adrielle Zagmignan ◽

...

Keyword(s):

High Performance ◽

Antioxidant Properties ◽

Chemical Characterization ◽

Opioidergic System ◽

Anti Inflammatory ◽

Inflammatory Action ◽

Monomeric Anthocyanins

This work evaluated the antioxidant properties and in vivo antinociceptive and anti-inflammatory effects of extracts obtained from fruit peels of Myrciaria floribunda (H. West ex Willd.) O. Berg (Myrtaceae). This plant is popularly known in Brazil as Cambuí or camboim. Different extracts were submitted to comparative analysis to determine the content of selected phytochemical classes (levels of total phenols, flavonoids, and monomeric anthocyanins) and the in vitro antioxidant potentials. The extract with higher potential was selected for in vivo evaluation of its antinociceptive and anti-inflammatory action. Finally, the chemical characterization of this extract was performed by high-performance liquid chromatography (HPLC). MfAE (extract obtained using acetone as solvent) showed the higher levels of phenols (296 mg GAE/g) and anthocyanins contents (35.65 mg Cy-3-glcE/g) that were associated with higher antioxidant activity. MfAE also exhibited in vivo anti-inflammatory and analgesic propertiers. This fraction inhibited the inflammatory and neurogenic phases of pain, and this effect was reversed by naloxone (suggesting the involvement of opioidergic system). MfAE reduced the abdominal contortions induced by acetic acid. The HPLC analysis revealed the presence of gallic acid (and its derivatives) and ellagic acid. Taken together, these data support the use of M. floribunda fruit peels for development of functional foods and nutraceutics.

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Cytotoxicity of Eurycomanone and Fargesin in RAW 264.7 Murine Macrophages

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i41a32327 ◽

2021 ◽

pp. 275-284

Author(s):

Hanim Akmar Rosly ◽

Amira Nabila Mat Roof ◽

Salfarina Ramli ◽

Visarut Buranasudja ◽

Pornchai Rojsitthisak ◽

...

Keyword(s):

Inhibitory Concentration ◽

Morphological Changes ◽

New Drugs ◽

Raw 264.7 Cells ◽

Raw 264.7 ◽

Murine Macrophages ◽

Eurycoma Longifolia ◽

Anti Inflammatory ◽

Inflammatory Effect

Bioactive natural compounds derived from plants are the source for the development of new drugs. Numerous in vitro studies have explored the anti-inflammatory effect of eurycomanone and fargesin, derived from Eurycoma longifolia and Flosmagnoliae, respectively. However, before anti-inflammatory investigation is conducted, it is important to obtain the safe doses of these compounds to ensure the validity of the anti-inflammatory results. Therefore, the present study was aimed to investigate the cytotoxicity of eurycomanone and fargesin towards macrophage RAW 264.7. cells to determine the safe doses of these compounds. Different concentrations of eurycomanone and fargesin were subjected to RAW 264.7 cells. The cytotoxicity of the compounds was evaluated by MTT assay and 50% inhibitory concentration (IC50) of these compounds was determined. Morphological changes of RAW 264.7 cells upon exposure to these compounds were also observed. Eurycomanone exhibited its cytotoxic effect by reducing RAW 264.7 cell viability dose-dependently with the IC50 of 94.17 µM. Meanwhile, fargesin had slight cytotoxicity towards RAW 264.7 cells with the IC50 of 173.5µM. Eurycomanone was more cytotoxic towards RAW 264.7 cells compared to fargesin. In conclusion, eurycomanone and fargesin at concentration up to 25 µM, was not toxic to the RAW 264.7 murine macrophages cells and the findings can be applied in the future anti-inflammatory study.

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Natural Anti-inflammatory compounds as Drug candidates in Alzheimer’s disease

Current Medicinal Chemistry ◽

10.2174/0929867327666200730213215 ◽

2020 ◽

Vol 27 ◽

Author(s):

Reyaz Hassan Mir ◽

Abdul Jalil Shah ◽

Roohi Mohi-ud-din ◽

Faheem Hyder Potoo ◽

Mohd. Akbar Dar ◽

...

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Natural Products ◽

Protective Action ◽

New Drugs ◽

Huperzine A ◽

Brain Disorder ◽

Anti Inflammatory

: Alzheimer's disease (AD) is a chronic neurodegenerative brain disorder characterized by memory impairment, dementia, oxidative stress in elderly people. Currently, only a few drugs are available in the market with various adverse effects. So to develop new drugs with protective action against the disease, research is turning to the identification of plant products as a remedy. Natural compounds with anti-inflammatory activity could be good candidates for developing effective therapeutic strategies. Phytochemicals including Curcumin, Resveratrol, Quercetin, Huperzine-A, Rosmarinic acid, genistein, obovatol, and Oxyresvertarol were reported molecules for the treatment of AD. Several alkaloids such as galantamine, oridonin, glaucocalyxin B, tetrandrine, berberine, anatabine have been shown anti-inflammatory effects in AD models in vitro as well as in-vivo. In conclusion, natural products from plants represent interesting candidates for the treatment of AD. This review highlights the potential of specific compounds from natural products along with their synthetic derivatives to counteract AD in the CNS.

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A New Flavonol From Saussurea involucrata With Anti-Inflammatory Activity

Natural Product Communications ◽

10.1177/1934578x211007638 ◽

2021 ◽

Vol 16 (5) ◽

pp. 1934578X2110076

Author(s):

Sheng Pan ◽

Zi-Guan Zhu

Keyword(s):

Nitric Oxide ◽

Aerial Part ◽

Raw 264.7 Cells ◽

Raw 264.7 ◽

Spectroscopic Methods ◽

Soluble Extract ◽

Saussurea Involucrata ◽

Tnf Α ◽

Anti Inflammatory

A new flavonol named 6-(2'',3''-epoxy-3''-methylbutyl)-resokaempferol (1), together with five known compounds (2-6) were isolated from the EtOAc-soluble extract of the aerial part of Saussurea involucrata. Their structures were elucidated on the basis of spectroscopic methods. All compounds were evaluated for their anti-inflammatory effects by measuring the production of nitric oxide (NO) and TNF-α in vitro. Among them, compound 1 showed potential inhibitory activity on the production of NO and TNF-α in LPS-induced RAW 264.7 cells with IC50 values of 48.0 ± 1.5 and 41.4 ± 1.7 µM, respectively.

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