Water soluble α‐glycosylated rutin (4G‐α‐D‐glucopyranosyl rutin, monoglucosyl rutin, MR) was used in this study to evaluate its ability to reduce abdominal visceral fat (AVF). We conducted a study ...examining 66 healthy Japanese men and women with a body mass index of ≥23 and <30 kg/m2 for 8 weeks. The subjects were randomly assigned to groups via computer random numbers as follows: MR200 group (MR 200 mg/day), MR400 group (MR 400mg/day), or placebo group. The primary outcome was change in the AVF area after 8 weeks of intervention. The secondary outcomes were effects of MR on total fat and subcutaneous fat of umbilical area, lipid‐related markers, and subjective symptoms. The per‐protocol set analysis involved 18 subjects in the placebo group (7 males and 11 females), 20 subjects in the MR200 group (8 males and 12 females), and 20 subjects in the MR400 group (8 males and 12 females). AVF area in both the MR200 and MR400 groups was reduced at week 8, with changes from the baseline (week 0) significantly higher than the placebo group. Additionally, the MR400 group reported improved subjective symptoms concerning being “worried about abdominal fat” at week 4 compared with the placebo group. These results indicate that the consumption of MR (200 and 400 mg/day) for 8 weeks reduced AVF.
Practical Application
Monoglucosyl rutin, an enzymatically modified form of rutin, is a highly stable and water‐soluble flavonoid widely used in food and beverages to prevent oxidation. The present clinical study demonstrated that it may improve overall health by reducing abdominal visceral fat.
Several lines of evidence suggest that flavonoids that originated from vegetables and medicinal plants have beneficial effects on diabetes by improving glycemic control, lipid profile, and ...antioxidant status. Rutin is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antioxidant, neuroprotective, nephroprotective, and hepatoprotective effects. In this review, the antihyperglycemic property of rutin and its protective effects against the development of diabetic complications are discussed. Proposed mechanisms for the antihyperglycemic effect of rutin include a decrease of carbohydrates absorption from the small intestine, inhibition of tissue gluconeogenesis, an increase of tissue glucose uptake, stimulation of insulin secretion from beta cells, and protecting Langerhans islet against degeneration. Rutin also decreases the formation of sorbitol, reactive oxygen species, advanced glycation end-product precursors, and inflammatory cytokines. These effects are considered to be responsible for the protective effect of rutin against hyperglycemia- and dyslipidemia-induced nephropathy, neuropathy, liver damage, and cardiovascular disorders. Taken together, the results of current experimental studies support the potential of rutin to prevent or treat pathologies associated with diabetes. Well-designed clinical studies are suggested to evaluate advantages and limits of rutin for managing diabetes.
Rutin is a common dietary flavonoid that is widely consumed from plant-derived beverages and foods as traditional and folkloric medicine worldwide. Rutin is believed to exhibit significant ...pharmacological activities, including anti-oxidation, anti-inflammation, anti-diabetic, anti-adipogenic, neuroprotective and hormone therapy. Till date, over 130 registered therapeutic medicinal preparations are containing rutin in their formulations. This article aims to critically review the extraction methods for plant-based rutin and its pharmacological activities. This review provides comprehensive data on the performance of rutin extraction methods and the extent of its pharmacological activities using various in vitro and in vivo experimental models.
Literatures including journals, patents, books and leaflets reporting on rutin from natural resources are systematically reviewed, particularly in the aspect of its extraction methods and biological activities. Factors affecting the efficiency of rutin extraction such as extraction temperature, duration and solvent to sample ratio are presented based on the findings of previous studies. The observed biological activities followed by clear explanation are also provided accordingly.
The biological activities of rutin varied largely dependent on the geographical and plant origins. The complexity of natural rutin has impeded the development of rutin derived drugs. The detail mechanism of rutin in human body after consumption is still unclear. Therefore, studies are intensively carried out both in vitro and in vivo for the better understanding of the underlying mechanism. The studies are not limited to the pharmacological properties, but also on the extraction methods of rutin. Many studies have focused on the optimization of extraction method to increase the extraction yield of rutin. Currently, the performances of modern extraction approaches have also been compared to the conventional heat reflux method as a benchmark.
There are various extraction methods for plant-based rutin ranging from conventional method up to the use of modern techniques such as ultrasound, mechanochemical, microwave, infrared and pressurized assisted methods. However, proper comparison between the methods is very difficult because of the variance in plant origin and extraction conditions. It is important to optimize the extraction method in order to produce high yield and acceptable purity of rutin with a reasonable cost. Even though rutin has been proven to be effective in numerous pharmacological activities, the dosage and toxicity of rutin for such activities are still unknown. Future research should relate the dosage and toxicity of rutin for the ethnobotanical claims based on the underlying mechanisms.
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Non-small cell lung cancer (NSCLC) is one of the major causes of cancer-related mortality globally. Despite the availability of therapeutic options, the improvement in patient survival is yet to be ...achieved. Recent advances in natural product (e.g., Rutin) research, therapeutic nanotechnology and especially the combination of both could aid in achieving significant improvements in the treatment or management of NSCLC. In this study, we explore the anti-cancer activity of Rutin-loaded liquid crystalline nanoparticles (LCNs) in an in vitro model where we have employed the A549 human lung epithelial carcinoma cell line. The anti-proliferative activity was determined by MTT and Trypan blue assays, whereas, the anti-migratory activity was evaluated by the scratch wound healing assay and a modified Boyden chamber assay. We also evaluated the anti-apoptotic activity by Annexin V-FITC staining, and the colony formation activity was studied using crystal violet staining. Here, we report that Rutin-LCNs showed promising anti-proliferative and anti-migratory activities. Furthermore, Rutin-LCNs also induced apoptosis in the A549 cells and inhibited colony formation. The findings warrant further detailed and in-depth anti-cancer mechanistic studies of Rutin-LCNs with a focus towards a potential therapeutic option for NSCLC. LCNs may help to enhance the solubility of Rutin used in the treatment of lung cancer and hence enhance the anticancer effect of Rutin.
Therapeutic benefits of rutin and its nanoformulations Negahdari, Ramin; Bohlouli, Sepideh; Sharifi, Simin ...
Phytotherapy research,
April 2021, 2021-Apr, 2021-04-00, 20210401, Letnik:
35, Številka:
4
Journal Article
Recenzirano
Background
Rutin as a natural flavonoid compound has revealed an extensive range of therapeutic potentials.
Purpose
The current paper is focused on the numerous studies on rutin nanoformulations ...regarding its broad spectrum of therapeutic potentials.
Study and methods
A review was conducted in electronic databases (PubMed) to identify relevant published literature in English. No restrictions on publication date were imposed.
Results
The literature search provided 7,078 results for rutin. Among them, 25 papers were related to the potential biological activities of rutin nanoformulations. Polymeric nanoparticles were the most studied nanoformulations for rutin (14 titles) and lipid nanoparticles (5 titles) were in second place. The reviewed literature showed that rutin has been used as an antimicrobial, antifungal, and anti‐allergic agent. Improving the bioavailability of rutin using novel drug‐delivery methods will help the investigators to use its useful effects in the treatment of various chronic human diseases.
Conclusion
It can be concluded that the preparation of rutin nanomaterials for the various therapeutic objects confirmed the enhanced aqueous solubility as well as enhanced efficacy compared to conventional delivery of rutin. However, more investigations should be conducted to confirm the improved bioavailability of the rutin nanoformulations.
The graphical shows different rutin‐loaded nanomaterials for in vitro, in vivo and, clinical investigations.
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.
Tau pathology is a hallmark of Alzheimer's disease (AD) and other tauopathies. During disease progression, abnormally phosphorylated forms of tau aggregate and accumulate into neurofibrillary ...tangles, leading to synapse loss, neuroinflammation, and neurodegeneration. Thus, targeting of tau pathology is expected to be a promising strategy for AD treatment.
The effect of rutin on tau aggregation was detected by thioflavin T fluorescence and transmission electron microscope imaging. The effect of rutin on tau oligomer-induced cytotoxicity was assessed by MTT assay. The effect of rutin on tau oligomer-mediated the production of IL-1β and TNF-α in vitro was measured by ELISA. The uptake of extracellular tau by microglia was determined by immunocytochemistry. Six-month-old male Tau-P301S mice were treated with rutin or vehicle by oral administration daily for 30 days. The cognitive performance was determined using the Morris water maze test, Y-maze test, and novel object recognition test. The levels of pathological tau, gliosis, NF-kB activation, proinflammatory cytokines such as IL-1β and TNF-α, and synaptic proteins including synaptophysin and PSD95 in the brains of the mice were evaluated by immunolabeling, immunoblotting, or ELISA.
We showed that rutin, a natural flavonoid glycoside, inhibited tau aggregation and tau oligomer-induced cytotoxicity, lowered the production of proinflammatory cytokines, protected neuronal morphology from toxic tau oligomers, and promoted microglial uptake of extracellular tau oligomers in vitro. When applied to Tau-P301S mouse model of tauopathy, rutin reduced pathological tau levels, regulated tau hyperphosphorylation by increasing PP2A level, suppressed gliosis and neuroinflammation by downregulating NF-kB pathway, prevented microglial synapse engulfment, and rescued synapse loss in mouse brains, resulting in a significant improvement of cognition.
In combination with the previously reported therapeutic effects of rutin on Aβ pathology, rutin is a promising drug candidate for AD treatment based its combinatorial targeting of tau and Aβ.
Natural compounds such as bioflavonoids have found application in health care system due to their wide biological activities, high safety margins and lower cost. Rutin , a polyphenolic bioflavonoid ...has shown wide range of pharmacological applications due to its significant antioxidant properties. Conventionally, it is used as antimicrobial, antifungal, and antiallergic agent. However, current research has shown its multispectrum pharmacological benefits for the treatment of various chronic diseases such as cancer, diabetes, hypertension and hypercholesterolemia. Its use is advantageous over other flavonoids as it is a nontoxic and nonoxidizable molecule.
This review focus on various studies done on rutin explaining its broad spectrum pharmacological activities. In addition, this review will also focus on the challenges associated with the drug and various approaches to improve the oral bioavailability of rutin.
Rutin is a highly potent molecule due to its strong antioxidant properties. In the near future, enhancing its bioavailability using novel drug delivery methods having minimum side effects will bring this promising natural molecule to the forefront of therapy for the treatment of various chronic human diseases.
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•Rutin protects against the liver injury induced by HgCl2.•Rutin ameliorated HgCl2-induced hepatic oxidative stress, apoptosis and inflammation.•Rutin reduces the histopathological ...changes and EGFR expression in the HgCl2-induced hepatotoxicity.
Mercury is a global environmental pollutant and is responsible for several organ pathophysiology including oxidative stress-induced liver disorders. Therefore, the present study was conducted to evaluate the potential ameliorative effects of rutin on mercury chloride (HgCl2)-induced hepatotoxicity in adult male rats.
HgCl2 was intraperitoneally injected at a dose of 1.23 mg/kg body weight for 7 days alone or in combination with the orally rutin (50 and 100 mg/kg body weight).
Rutin treatment significantly improved liver function tests alkaline phosphatase (ALP), aspartate aminotransferase (AST) and alanine aminotransferase (ALT), and increased activities of antioxidant defense system catalase (CAT), superoxide dismutase (SOD) and glutathione peroxidase (GPx) and glutathione (GSH) content. The histological alterations and epidermal growth factor receptor (EGFR) expression in the HgCl2-induced liver tissues were decreased by administration of rutin. Furthermore, rutin reversed the changes in levels of apoptosis and inflammation related proteins involving p53, Bcl-2 associated X protein (Bax), B-cell lymphoma-2 (Bcl-2), cytochrome c, nuclear factor kappa B (NF-κB), tumor necrosis factor-α (TNF-α), B-cell lymphoma-3(Bcl-3) and interleukin-1β (IL-1β), and inhibited p38α mitogen-activated protein kinase (MAPK) and cysteine aspartate specific protease-3 (caspase-3) activations.
The data of the present study suggest that rutin effectively suppress HgCl2‐induced hepatotoxicity by ameliorating oxidative stress, inflammation and apoptosis.
•Rutin degradation takes place in 50% methanol.•Rutin degradation in seeds continued after treatment at 140 °C or lyophilisation.•Tartary buckwheat seeds deglycosylated most of ...kaempferol-3-O-rutinoside during 3 h.
Tartary buckwheat achenes are rich in rutin. However, its utilisation as a food is low due to the bitter taste of the products because of the transformation of rutin to quercetin. The aim of this study was to determine the stability of rutin and selected flavonoids, which are influenced by the different sample preparations exposing the achenes to higher temperatures (60 °C, 100 °C, and 140 °C), and also to determine the specificity of the rutin degrading enzymes in Tartary buckwheat. The achenes were directly extracted with methanol pre-extracted with hexane, or lyophilised before extraction. The rutin and quercetin contents were determined by HPLC. The rutin-degrading enzymes in Tartary buckwheat achenes were not inactivated after a heat treatment up to 140 °C acting on them for three hours; neither to lyophilisation nor pre-extraction with hexane. The rutin-degrading enzymes probably caused the deglycosylation of kaempferol-3-O-rutinoside, kaempferol-3-O-β-d-glucoside and piceid. Rutin-degrading enzymes were inactivated with 100% methanol.
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