| Description: |
Citrus narirutin fraction (CNF), contained 75% of narirutin, co-administration of CNF with alcohol can alleviate alcohol induced liver damage through preventing lipid formation, protecting antioxidant system and suppressing productions of pro-inflammatory cytokines. Narirutin has anti-inflammatory effect in a murine model of allergic eosinophilic airway inflammation, the mechanism is likely to be associated with a reduction in the OVA-induced increases of IL-4 and IgE. |
| Targets: |
NO | NOS | PGE | COX | TNF-α | NF-kB | MAPK | IL Receptor |
| In vitro: |
| Food Chem Toxicol. 2012 Oct;50(10):3498-504. | | Narirutin fraction from citrus peels attenuates LPS-stimulated inflammatory response through inhibition of NF-κB and MAPKs activation.[Pubmed: 22813871] |
METHODS AND RESULTS:
In this study, we examined the regulatory activity of narirutin fraction from citrus peels on the production of inflammatory mediators managing acute or chronic inflammatory diseases in macrophages. Narirutin fraction inhibited the release, by lipopolysaccharide (LPS)-stimulated macrophages, of nitric oxide (NO) and prostaglandin E2 (PGE2) through suppressing the expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively. The release, by LPS stimulated macrophages, of interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) was also reduced by narirutin fraction in a dose-dependent manner. Furthermore, narirutin fraction inhibited the LPS-mediated activation of nuclear factor-κB (NF-κB) and mitogen-activated protein kinases (MAPKs), which are signaling molecules involved in production of pro-inflammatory factors.
CONCLUSIONS:
As a result of these properties, narirutin fraction has the potential to be used as a functional dietary supplement and effective anti-inflammatory agent. | | Curr Comput Aided Drug Des . 2020;16(5):523-529. | | Structure-based Discovery of Narirutin as a Shikimate kinase Inhibitor with Anti-tubercular Potency[Pubmed: 31654517] | | Abstract
Background: Shikimate pathway is essential for tubercular bacillus but it is absent in mammals. Therefore, Shikimate kinase and other enzymes in the pathway are potential targets for the development of novel anti-tuberculosis drugs.
Objective: In the present study, Shikimate kinase is selected as the target for in silico screening of phytochemicals with an aim to discover a novel herbal drug against Mycobacterium tuberculosis (Mtb).
Methods: A structure-based drug discovery approach is undertaken for the execution of the objective. Virtual screening of phytochemical database NPACT against the target, Shikimate kinase (PDB ID 3BAF), is carried out followed by toxicity and drug-likeness filtration. Finally, a lead, narirutin was selected for in vitro anti-tubercular study.
Results: Narirutin, present in citrus fruits, emerges as the lead. It is considered to be non-toxic with predicted high LD50 value, 12000 mg/kg body weight. The phytochemical is tested for its antitubercular activity in vitro. It has MIC99 62.5 μg/mL against the MtbH37Rv strain.
Conclusion: This is the first-ever report to show anti-tuberculosis potency of narirutin.
Keywords: Molecular docking; Mycobacterium tuberculosis; drug-likeness; narirutin; shikimate kinase; toxicity. |
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| In vivo: |
| Food Chem Toxicol. 2013 May;55:637-44. | | Narirutin fraction from citrus peels attenuates alcoholic liver disease in mice.[Pubmed: 23416143] |
METHODS AND RESULTS:
This study aimed to demonstrate protective activities of the narirutin fraction from peels of Citrus unshiu against ethanol-induced hepatic damage through an animal study. Citrus narirutin fraction (CNF), contained 75% of narirutin, was obtained by an ultra-sonicated extraction and further purification. ICR mice were divided into four groups; normaldiet control, ethanol control (6.5g ethanol/kg), low-CNF (ethanol+150mg CNF/kg) and high-CNF (ethanol+300mg CNF/kg) groups. Consumption of alcohol for 8weeks induced severe liver damage with increases in prognostic indicators such as aspartate transaminase, alanine transaminase in serum whereas co-administration of CNF suppressed their increases. Excessive accumulations in liver TG and TC in ethanol control group were also suppressed by co-administration of CNF. Co-administration of CNF maintained SOD activity, GSH and malondialdehyde levels close to those of the normal diet group. Chronic consumption of alcohol also stimulated abrupt increases in pro-inflammatory cytokines such as nuclear factor (NF)-κB, tumor necrosis factor (TNF)-α and interleukin (IL)-1β in liver otherwise co-administration of CNF effectively suppressed production of these cytokines dose-dependently.
CONCLUSIONS:
These results indicate that co-administration of CNF with alcohol can alleviate alcohol induced liver damage through preventing lipid formation, protecting antioxidant system and suppressing productions of pro-inflammatory cytokines. |
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