What is Rutin Rutin is a bioflavonoid found in nature  in various plant products, citrus fruits, apples and cranberries. Where it is obtained Rutin is obtained from numerous plants, ...

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What is Rutin

Rutin is a bioflavonoid found in nature  in various plant products, citrus fruits, apples and cranberries.

Where it is obtained

Rutin is obtained from numerous plants, fruits, berries such as blueberry and vegetables, and especially from buckwheat.

What is it for?

Antioxidant

The aim of this study was to evaluate the effect of rutin on oxidative stress and apoptosis induced by H2O2 in human lens epithelial (HLE) cells and the associated mechanisms involved.Cell viability was assessed by 4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide assay and cell apoptosis was determined by flow cytometry, TUNEL assay and DNA fragmentation assay after 24 h treatment of 100 μM H2O2 with or without rutin pretreatment at various concentrations. The level of reactive oxygen species (ROS) was examined using 2',7'-dichlorodihydrofluorescein diacetate by flow cytometry. The activity of superoxide dismutase (SOD) was measured by xanthinoxidase method and the contents of glutathione (GSH) and malondialdehyde (MDA) were quantified by enzyme-linked immunosorbent assay. The expression change of Bcl-2, Bax and caspase-3 at mRNA and protein levels were detected by real-time polymerized chain reaction (RT-PCR) and Western-blot analysis, respectively. Activation and translocation of nuclear factor-kappaB (NF-кB/p65) were examined by Western blot and immunocytochemistry.Rutin pretreatment protected HLE cells from H2O2-induced cell viability decrease and apoptosis. In addition, in the presence of rutin, H2O2-induced intracellular excessive ROS and MDA were attenuated, whereas intracellular SOD and GSH depletion were prevented. Moreover, rutin also inhibited the up-regulation of caspase-3 and Bax expression and rescued down-regulation of Bcl-2 expression. Lastly, rutin blocked the activation and translocation of NF-кB/p65 induced by H2O2.Our results demonstrated that rutin effectively protects HLE cells from H2O2-induced oxidative stress and apoptosis in a dose-dependent manner. The involved mechanisms may be related to the regulation of ROS production, the inhabitation of lipid peroxidation, the protection of intracellular antioxidant system and its modulation of Bcl-2/Bax family and NF-кB/p65 signaling pathway (1).

Anti-inflammatory 

This study investigated the antioxidant activity of one hundred kinds of pure chemical compounds found within a number of natural substances and oriental medicinal herbs (OMH). Three different methods were used to evaluate the antioxidant activity of DPPH radical-scavenging activity, ABTS radical-scavenging activity, and online screening HPLC-ABTS assays. The results indicated that 17 compounds exhibited better inhibitory activity against ABTS radical than DPPH radical. The IC50 rate of a more practical substance is determined, and the ABTS assay IC50 values of gallic acid hydrate, (+)-catechin hydrate, caffeic acid, rutin hydrate, hyperoside, quercetin, and kaempferol compounds were 1.03 ± 0.25, 3.12 ± 0.51, 1.59 ± 0.06, 4.68 ± 1.24, 3.54 ± 0.39, 1.89 ± 0.33, and 3.70 ± 0.15 μg/mL, respectively. The ABTS assay is more sensitive to identifying the antioxidant activity since it has faster reaction kinetics and a heightened response to antioxidants. In addition, there was a very small margin of error between the results of the offline-ABTS assay and those of the online screening HPLC-ABTS assay. We also evaluated the effects of 17 compounds on the NO secretion in LPS-stimulated RAW 264.7 cells and also investigated the cytotoxicity of 17 compounds using a cell counting kit (CCK) in order to determine the optimal concentration that would provide an effective anti-inflammatory action with minimum toxicity. These results will be compiled into a database, and this method can be a powerful preselection tool for compounds intended to be studied for their potential bioactivity and antioxidant activity related to their radical-scavenging capacity (2).

Diabetes

Diabetes and its major risk factor, obesity, have become a world-wide epidemic and cause of suffering for millions of people. There is still no drug of cure for diabetes and the currently available drugs suffer from a number of limitations either due to side effects and/or loss of efficacy during prolonged use. Rutin is one of the most abundant polyphenolic compounds belonging to the flavonoid class. In the present communication, its therapeutic potential for diabetes is critically analysed by reviewing its effect on the various targets of diabetes. The multifunctional nature of rutin including action via antioxidant, anti-inflammatory, organoprotection, etc., mechanisms is outlined through review of evidences from in vitro and in vivo studies (3).

Bowel

Inflammatory bowel disease (IBD), commonly represented by ulcerative colitis and Crohn's disease, is a form of chronic inflammatory disorders of the gastrointestinal system. Its current drug treatment includes the use of antibiotics, 5-aminosalicylates, corticosteroids, immune-modifying agents and biologics such as anti-TNF agents and adhesion molecules blockers. These drugs have inherent problems of efficacy as many IBD sufferers need surgical intervention at some stage, high cost especially for the protein-based drugs, loss of efficacy and unwanted side effects. The discovery of novel drugs including those from natural sources that overcome the above mentioned drawbacks of the current therapy is therefore of great interest. While the flavonoid quercetin with proven antiinflammatory effect failed to show activity in vivo, its glycoside rutin has recently proven to possess a significant IBD therapeutic potential in experimental animals. In this communication, the pharmacological and pharmacokinetic profiles of rutin along with its ability to serve as a prodrug that deliver the bioactive quercetin close to the IBD site are discussed. Potential mechanisms of action far beyond antioxidant effects such as suppression of proinflammatory mediators' release and expression of inflammatory proteins (e.g. adhesion molecules, cyclooxygenase, nitric oxide synthase, etc.) are also scrutinized (4).

Alzheimer's disease

Rutin (quercetin-3-O-rutinoside) is a multifunctional natural flavonoid glycoside with profound effects on the various cellular functions under pathological conditions. Due to the ability of rutin and/or its metabolites to cross the blood brain barrier, it has also been shown to modify the cognitive and various behavioral symptoms of neurodegenerative diseases. In this review, its therapeutic potential for Alzheimer's disease (AD) is evaluated through appraisal of current literatures relevant to the various cellular and molecular targets of the disease. Among the most relevant mechanisms involved are effect on amyloid beta (Aβ) processing, aggregation and action; alteration of the oxidant-antioxidant balance associated with neuronal cell loss; removing the inflammatory component of neurodegeneration, etc. The effect of rutin resulting from its physicochemical features related to effects like metal chelation and bioavailability are also discussed (5).

Alzheimer disease (AD) is a progressive, neurodegenerative disease characterized by extracellular β-amyloid (Aβ) plaques and intracellular neurofibrillary tangles in the brain. Aβ aggregation is closely associated with neurotoxicity, oxidative stress, and neuronal inflammation. The soluble Aβ oligomers are believed to be the most neurotoxic form among all forms of Aβ aggregates. We have previously reported a polyphenol compound rutin that could inhibit Aβ aggregation and cytotoxicity, attenuate oxidative stress, and decrease the production of nitric oxide and proinflammatory cytokines in vitro. In the current study, we investigated the effect of rutin on APPswe/PS1dE9 transgenic mice. Results demonstrated that orally administered rutin significantly attenuated memory deficits in AD transgenic mice, decreased oligomeric Aβ level, increased super oxide dismutase activity and glutathione (GSH)/glutathione disulfide (GSSG) ratio, reduced GSSG and malondialdehyde (MDA) levels, downregulated microgliosis and astrocytosis, and decreased interleukin (IL)-1β and IL-6 levels in the brain. These results indicated that rutin is a promising agent for AD treatment because of its antioxidant, anti-inflammatory, and reducing Aβ oligomer activities (6).

Parkinson's disease

A wide range of neurodegenerative diseases (NDs), including Alzheimer's disease, Parkinson's disease, Huntington's disease, and prion diseases, share common mechanisms such as neuronal loss, apoptosis, mitochondrial dysfunction, oxidative stress, and inflammation. Intervention strategies using plant-derived bioactive compounds have been offered as a form of treatment for these debilitating conditions, as there are currently no remedies to prevent, reverse, or halt the progression of neuronal loss. Rutin, a glycoside of the flavonoid quercetin, is found in many plants and fruits, especially buckwheat, apricots, cherries, grapes, grapefruit, plums, and oranges. Pharmacological studies have reported the beneficial effects of rutin in many disease conditions, and its therapeutic potential in several models of NDs has created considerable excitement. Here, we have summarized the current knowledge on the neuroprotective mechanisms of rutin in various experimental models of NDs. The mechanisms of action reviewed in this article include reduction of proinflammatory cytokines, improved antioxidant enzyme activities, activation of the mitogen-activated protein kinase cascade, downregulation of mRNA expression of PD-linked and proapoptotic genes, upregulation of the ion transport and antiapoptotic genes, and restoration of the activities of mitochondrial complex enzymes. Taken together, these findings suggest that rutin may be a promising neuroprotective compound for the treatment of NDs (7).

Colon cancer

Rutin and Silibinin are active flavonoid compounds, well-known for possessing multiple biological activities. This study reports how Rutin and Silibinin in combination modulate wide range intracellular signaling cascades as evidenced by in-vitro research. Data obtained from preclinical studies provide evidence to be supportive to bridge basic and translational studies. Results suggest that Rutin and Silibinin produce anticancer effects via induction of apoptosis as well as regulating the expressions of genes related to apoptosis, inflammation and MAPK pathway proteins more effectively in combination than individually. This study supports the viability of developing Rutin and Silibinin in combination as a novel therapeutic prodrug for colon cancer treatment and may have a promising role in the development of new anticancer drugs in the future (8).

Skin protection

Skin cancer is related to unprotected exposure to sunlight. Despite the broad expansion of sunscreen market, various researches are focused on the inefficiency and danger of sun products. This study was focused on the development of photoprotective nanoparticulate dermal preparations of the antioxidant flavonoid Rutin (RT). Nanostructured lipid carriers (NLCs) were prepared using different types of lipids. Based on particle size (PS), size distribution (PDI) and Zeta potential (Z) as well as rheological properties, NLC containing Plurol® stearique (NLC-P) and Apifil® (NLC-A) were selected and loaded with different concentrations of RT to form the medicated nanocreams. F4 (NLC-A with 2% RT) attained highest occlusive effect, drug encapsulation and release efficiencies as well as sun protective factor (SPF). Different concentrations of TiO2 were added to F4 aiming to ameliorate the sun protective effect. F7 (containing 5% TiO2) attained the highest SPF and area under the UV absorbance curve and had a critical wavelength above 370 nm, which proved its high efficiency as sunscreen. The in-vitro antioxidant effect of F7 was more than two fold that of the standard antioxidant. This study provides a suitable cosmeceutical lipidic colloidal system of Rutin to be employed as a successful photoprotective preparation (9).

 

Molecular Formula : C₂₇H₃₀O₁₆

Molecular Weight : 610.52

CAS : 153-18-4

Synonyms :

Quercetin 3-rutinoside; Rutin trihydrate;

 

References__________________________

(1) Protective Effect of Rutin Against H₂O₂-Induced Oxidative Stress and Apoptosis in Human Lens Epithelial Cells.

Zhou YF, Guo B, Ye MJ, Liao RF, Li SL.

Curr Eye Res. 2015 Nov 17:1-10. [Epub ahead of print] 

 (2) Antioxidant and Anti-Inflammatory Activity Determination of One Hundred Kinds of Pure Chemical Compounds Using Offline and Online Screening HPLC Assay.

Lee KJ, Oh YC, Cho WK, Ma JY.

Evid Based Complement Alternat Med. 2015;2015:165457. doi: 10.1155/2015/165457. Epub 2015 Oct 4.

(3) The therapeutic potential of rutin for diabetes: an update.

Mini Rev Med Chem. 2015;15(7):524-8.

Habtemariam S1, Lentini G.

(4) Natural Therapies of the Inflammatory Bowel Disease: The Case of Rutin and its Aglycone, Quercetin.

Habtemariam S1, Belai A2.

Mini Rev Med Chem. 2018;18(3):234-243. doi: 10.2174/1389557517666170120152417.

 

(5) Rutin as a Natural Therapy for Alzheimer's Disease: Insights into its Mechanisms of Action.

 

Habtemariam S.

 

 

 

Curr Med Chem. 2016;23(9):860-73. Review

 

(6) Rutin improves spatial memory in Alzheimer's disease transgenic mice by reducing Aβ oligomer level and attenuating oxidative stress and neuroinflammation.

 

Xu PX, Wang SW, Yu XL, Su YJ, Wang T, Zhou WW, Zhang H, Wang YJ, Liu RT.

 

Behav Brain Res. 2014 May 1;264:173-80. doi: 10.1016/j.bbr.2014.02.002. Epub 2014 Feb 7. 

 

(7) Rutin as a Potent Antioxidant: Implications for Neurodegenerative Disorders.

 

Enogieru AB, Haylett W, Hiss DC, Bardien S, Ekpo OE.

 

Oxid Med Cell Longev. 2018 Jun 27;2018:6241017. doi: 10.1155/2018/6241017. eCollection 2018. Review.

 

(8) Synergistic Interaction of Rutin and Silibinin on Human Colon Cancer Cell Line.

 

Nafees S, Mehdi SH, Zafaryab M, Zeya B, Sarwar T, Rizvi MA.

 

 

 

Arch Med Res. 2018 May;49(4):226-234. doi: 10.1016/j.arcmed.2018.09.008. Epub 2018 Oct 9.

 

(9) Rutin nanostructured lipid cosmeceutical preparation with sun protective potential.

 

Kamel R, Mostafa DM. J Photochem Photobiol B. 2015 Sep 4;153:59-66. doi: 10.1016/j.jphotobiol.2015.09.002.

 

Cutaneous biocompatible rutin-loaded gelatin-based nanoparticles increase the SPF of the association of UVA and UVB filters.

 

Oliveira CA, Peres DD, Graziola F, Chacra NA, Araújo GL, Flórido AC, Mota J, Rosado C, Velasco MV, Rodrigues LM, Fernandes AS, Baby AR.

 

Eur J Pharm Sci. 2015 Sep 30;81:1-9. doi: 10.1016/j.ejps.2015.09.016.

 

 

 

 

 

 

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