Phytochemicals as multi-target inhibitors of the inflammatory pathway- A modeling and experimental study

Devi, Nisha S.; Ramanan, Meera; Paragi-Vedanthi, Padmapriya; Doble, Mukesh

doi:10.1016/j.bbrc.2017.01.046

Cited by 12 publications

(8 citation statements)

References 52 publications

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“…The difference may be due to the type of enzyme used for the test and the concentration of the reacting components. The obtained inhibitory potential of pure ferulic acid and trans-cinnamic acid are in accordance with Devi et al [16], where these polyphenols showed 74.4 and 66.6% of inhibition respectively but in different concentration than in the presented study. The weak activity of ferulic acid as a LOX inhibitor is confirmed by the studies by Landberg et al [5], which showed that low or no inhibition was observed with avenanthramides containing ferulic or para-coumaric acid.…”

Section: Lox Assaysupporting

confidence: 92%

Some Dietary Phenolic Compounds Can Activate Thyroid Peroxidase and Inhibit Lipoxygenase-Preliminary Study in the Model Systems

Habza-Kowalska

Kaczor

Bartuzi

et al. 2021

IJMS

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The presented research concerns the triple activity of trans-cinnamic (tCA), ferulic (FA) and syringic acids (SA). They act as thyroid peroxidase (TPO) activators, lipoxygenase (LOX) inhibitors and show antiradical activity. All compounds showed a dose-dependent TPO activatory effect, thus the AC50 value (the concentration resulting in 50% activation) was determined. The tested compounds can be ranked as follows: tCA > FA > SA with AC50 = 0.10, 0.39, 0.69 mM, respectively. Strong synergism was found between FA and SA. The activatory effects of all tested compounds may result from interaction with the TPO allosteric site. It was proposed that conformational change resulting from activator binding to TPO allosteric pocket results from the flexibility of a nearby loop formed by residues Val352-Tyr363. All compounds act as uncompetitive LOX inhibitors. The most effective were tCA and SA, whereas the weakest was FA (IC50 = 0.009 mM and IC50 0.027 mM, respectively). In all cases, an interaction between the inhibitors carboxylic groups and side-chain atoms of Arg102 and Arg139 in an allosteric pocket of LOX was suggested. FA/tCA and FA/SA acted synergistically, whereas tCA/SA demonstrated antagonism. The highest antiradical activity was found in the case of SA (IC50 = 0.22 mM). FA/tCA and tCA/SA acted synergistically, whereas antagonism was found for the SA/FA mixture.

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Section: Lox Assaysupporting

confidence: 92%

Some Dietary Phenolic Compounds Can Activate Thyroid Peroxidase and Inhibit Lipoxygenase-Preliminary Study in the Model Systems

Habza-Kowalska

Kaczor

Bartuzi

et al. 2021

IJMS

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“…Historically, herbs containing it were used mainly in Asia as yellow colorants to dye paper or various fibers , and as traditional Chinese medicines . Recently, berberine anticancer, anti‐inflammatory, antiviral and antibacterial activities have been reported, as well as a probable cure for diabetes or insomnia . Unfortunately, its low bioavailability is the main problem with medical use .…”

Section: Introductionmentioning

confidence: 99%

Capillary‐HPLC with tandem mass spectrometry in analysis of alkaloid dyestuffs – a new approach

2017

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Development of the identification method of alkaloid compounds in Amur cork tree as well as not examined so far Oregon grape and European Barberry shrubs are presented. The novel approach to separation of alkaloids was applied and the capillary-high-performance liquid chromatography (capillary-HPLC) system was used, which has never previously been reported for alkaloid-based dyestuffs analysis. Its optimization was conducted with three different stationary phases (unmodified octadecylsilane-bonded silica, octadecylsilane modified with polar groups and silica-bonded pentaflourophenyls) as well as with different solvent buffers. Detection of the isolated compounds was carried out using diode-array detector (DAD) and tandem mass spectrometer with electrospray ionization (ESI MS/MS). The working parameters of ESI were optimized, whereas the multiple reactions monitoring (MRM) parameters of MS/MS detection were chosen based on the product ion spectra of the quasi-molecular ions. Calibration curve of berberine has been estimated (y = 1712091x + 4785.03 with the correlation coefficient 0.9999). Limit of detection and limit of quantification were calculated to be 3.2 and 9.7 ng/mL, respectively. Numerous alkaloids (i.e., berberine, jatrorrhizine and magnoflorine, as well as phellodendrine, menisperine and berbamine) were identified in the extracts from alkaloid plants and silk and wool fibers dyed with these dyestuffs, among them their markers.

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“…LPS (the main component of the cell wall of Gram-negative bacteria) is a potent inducer of human T-lymphocyte proliferation as part of host pro-inflammatory response [ 46 ]. In addition, the anti-inflammatory properties of some phytochemicals present in HDHE have been reported [ 47 , 48 , 49 , 50 ]. The use of anti-inflammatory agents is of great importance in the treatment of microbial infection [ 51 , 52 ].…”

Section: Discussionmentioning

confidence: 99%

Himatanthus drasticus Leaves: Chemical Characterization and Evaluation of Their Antimicrobial, Antibiofilm, Antiproliferative Activities

Figueiredo¹,

Santos²,

Castro³

et al. 2017

Molecules

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Plant-derived products have played a fundamental role in the development of new therapeutic agents. This study aimed to analyze antimicrobial, antibiofilm, cytotoxicity and antiproliferative potentials of the extract and fractions from leaves of Himatanthus drasticus, a plant from the Apocynaceae family. After harvesting, H. drasticus leaves were macerated and a hydroalcoholic extract (HDHE) and fractions were prepared. Antimicrobial tests, such as agar-diffusion, Minimum Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) were carried out against several bacterial species. Staphylococcus aureus, Pseudomonas aeruginosa, Listeria monocytogenes and Klebsiella pneumoniae were inhibited by at least one extract or fraction in the agar-diffusion assay (inhibition halos from 12 mm to 30 mm). However, the lowest MIC value was found for HDHE against K. pneumoniae. In addition, HDHE and its fractions were able to inhibit biofilm formation at sub-inhibitory concentrations (780 µg/mL and 1.56 µg/mL). As the best activities were found for HDHE, we selected it for further assays. HDHE was able to increase ciprofloxacin (CIP) activity against K. pneumoniae, displaying synergistic (initial concentration CIP + HDHE: 2 µg/mL + 600 µg/mL and 2.5 µg/mL + 500 µg/mL) and additive effects (CIP + HDHE: 3 µg/mL + 400 µg/mL). This action seems to be associated with the alteration in bacterial membrane permeability induced by HDHE (as seen by propidium iodide labeling). This extract was non-toxic for red blood cell or human peripheral blood mononuclear cells (PBMCs). Additionally, it inhibited the lipopolysaccharide-induced proliferation of PBMCs. The following compounds were detected in HDHE using HPLC-ESI-MS analysis: plumieride, plumericin or isoplumericin, rutin, quercetin and derivatives, and chlorogenic acid. Based on these results we suggest that compounds from H. drasticus have antimicrobial and antibiofilm activities against K. pneumoniae and display low cytotoxicity and anti-proliferative action in PBMC stimulated with lipopolysaccharide.

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Phytochemicals as multi-target inhibitors of the inflammatory pathway- A modeling and experimental study

Cited by 12 publications

References 52 publications

Some Dietary Phenolic Compounds Can Activate Thyroid Peroxidase and Inhibit Lipoxygenase-Preliminary Study in the Model Systems

Some Dietary Phenolic Compounds Can Activate Thyroid Peroxidase and Inhibit Lipoxygenase-Preliminary Study in the Model Systems

Capillary‐HPLC with tandem mass spectrometry in analysis of alkaloid dyestuffs – a new approach

Himatanthus drasticus Leaves: Chemical Characterization and Evaluation of Their Antimicrobial, Antibiofilm, Antiproliferative Activities

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