Pharmacokinetic study of rutin and quercetin in rats after oral administration of total flavones of mulberry leaf extract

Ouyang, Zhen; Cao, Xu; Wei, Yuan; Zhang, Wei Wan Qi; Zhao, Ming; Duan, Jin Ao

doi:10.1590/s0102-695x2013000500009

Cited by 52 publications

(26 citation statements)

References 6 publications

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“…The outcomes revealed that plasma flavonoids were significantly elevated in rutin-supplemented group, fortunately, without any adverse changes in blood chemistry or indices of liver function. Additionally, Zhang et al ., has reported the absorption and metabolism characteristics of rutin in the intestinal-derived Caco-2 cells (33) and the pharmacokinetics of rutin has been studied in rats after oral administration with the identification of its associated metabolites in urine and feces by Ou-yang et al (34). Furthermore, various antitumor studies have been reported for rutin in rodents.…”

Section: Discussionmentioning

confidence: 99%

Rutin as A Novel c-Met Inhibitory Lead for The Control of Triple Negative Breast Malignancies

Elsayed

Ebrahim

Mohyeldin

et al. 2017

Nutrition and Cancer

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Triple negative breast cancer (TNBC) has high metastatic and mortality potential and lacks effective and selective therapeutic options. Aberrant dysregulation of the receptor tyrosine kinase c-Met promotes TNBC progression, motility and survival and therefore considered a valid therapeutic target. Among various identified anticancer agents, plant polyphenols (PPs) including flavonoids, have been shown to be safe and proven for their antitumor activity through modulating diverse macromolecular targets. This study reports the bioassay-guided identification of the common flavonol glycoside rutin as breast cancer cell proliferation, migration and invasion inhibitor. The cell free Z’-LYTE kinase assay, Western blot and in silico docking experiments uncovered, for the first time, c-Met kinase as a potential mechanistic target for rutin-mediated anticancer effects on TNBC cell lines. Likewise, the intraperitoneal injection of rutin at 30 mg/kg, 3X/week, significantly reduced the growth of the TNBC MDA-MB-231/GFP orthotopic xenograft in nude mouse model. These results clearly designate the functional dietary flavonoid rutin as a potential lead for the prevention and control of c-Met-dependent breast malignancies.

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Section: Discussionmentioning

confidence: 99%

Rutin as A Novel c-Met Inhibitory Lead for The Control of Triple Negative Breast Malignancies

Elsayed

Ebrahim

Mohyeldin

et al. 2017

Nutrition and Cancer

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“…For the oral route of administration, metabolism in the intestinal membrane and the liver is of major concern as it can reduce the systemic bioavailability of the drug (Kushwaha et al 2014). Exposure of drugs to various pH conditions, nature of gut microflora and the presence of various enzymes in gastrointestinal transit also decrease the bioavailability of drugs (Shi et al 2006;Ou-yang et al 2013). It has been reported that the presence of sugar moieties in the molecule structure results in increasing hydrogen bond count, polar surface area and molecular flexibility of the molecules to unfavorable levels of poor membrane permeability (Liu et al 2009).…”

Section: Discussionmentioning

confidence: 99%

Development and validation of HPLC method for vicenin-1 isolated from fenugreek seeds in rat plasma: application to pharmacokinetic, tissue distribution and excretion studies

Kandhare

Bodhankar

Thakurdesai

2016

Pharmaceutical Biology

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Context: Vicenin-1, a flavonol glycoside, has potent platelet aggregation inhibition, antioxidant, radioprotectants and anti-inflammatory activities. Objective: To establish a rapid, simple, precise and sensitive high-performance liquid chromatography (HPLC) method for determination of vicenin-1 in rat plasma, and to investigate the pharmacokinetics, tissue distribution and excretion after a single 60 mg/kg oral dose in rats. Materials and methods: Vicenin-1 was extracted by solid-liquid extraction through Tulsicon V R ADS-400 (0.40-1.2 mm). Chromatographic separation was achieved by HPLC with a C 18 column with a mobile phase composed of water and acetonitrile (75:25 v/v) and a flow rate of 1 mL/min along with UV detection at 210 nm. Results: Good linearity of calibration curve was found between 10.5 and 100.5 lg/mL (R 2 ¼ 0.995) for plasma and tissue, whereas 2.5-500 lg/mL (R 2 ¼ 0.999) for the urine and stool samples. The extraction recoveries were 98.51-99.58% for vicenin-1 in plasma, whereas intra-day and inter-day precision were validated by relative standard deviation (%RSD), that came in the ranges of 1.16-1.79% and 1.28-1.73%, respectively. The pharmacokinetics results showed C max (7.039 lg/mL) and T max (2 h) after oral administration of vicenin-1. Tissue distribution study showed that the highest concentration of vicenin-1 was achieved in the liver followed by the lung. Approximately 24.2% of its administered dose was excreted via urinary excretion route. Conclusion: The first-pass metabolism, poor solubility and presence of reducing sugar moiety in vicenin-1 may decrease its bioavailability. The developed method is sensitive, specific and was successfully applied to the pharmacokinetics, tissue distribution and excretion studies of vicenin-1 in rats.ARTICLE HISTORY

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“…Some examples include the work published by Xu et al () who demonstrated that 68% of naringerin is absorbed in the colon in rat intestinal reperfusion model. In another study, rutin and quercetin were rapidly absorbed and then slowly decreased in rats administered with total flavones from mulberry leaf extract (Ou‐yang et al, ). The half‐lives of elimination ( T 1/2) of vitexin‐4″‐ O ‐glucoside and vitexin‐2″‐ O ‐rhamnoside were found to be 2.53 and 2.32 hr, respectively (Ma et al, ).…”

Section: Pharmacokinetics Of Flavonoidsmentioning

confidence: 98%

Flavonoids as efficient scaffolds: Recent trends for malaria, leishmaniasis, Chagas disease, and dengue

Boniface

Ferreira

2019

Phytotherapy Research

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Endemic in 149 tropical and subtropical countries, neglected tropical diseases (NTDs) affect more than 1 billion people annually with over 500,000 deaths. Among the NTDs, some of the most severe consist of leishmaniasis, Chagas disease, and dengue. The impact of the combined NTDs closely rivals that of malaria. According to the World Health Organization, 216 million cases of malaria were reported in 2016 with 445,000 deaths. Current treatment options are associated with various limitations including widespread drug resistance, severe adverse effects, lengthy treatment duration, unfavorable toxicity profiles, and complicated drug administration procedures. Flavonoids are a class of compounds that has been the subject of considerable scientific interest. New developments of flavonoids have made promising advances for the potential treatment of malaria, leishmaniasis, Chagas disease, and dengue, with less toxicity, high efficacy, and improved bioavailability. This review summarizes the current standings of the use of flavonoids to treat malaria and neglected diseases such as leishmaniasis, Chagas disease, and dengue. Natural and synthetic flavonoids are leading compounds that can be used for developing antiprotozoal and antiviral agents. However, detailed studies on toxicity, pharmacokinetics, and mechanisms of action of these compounds are required to confirm the in vitro pharmacological claims of flavonoids for pharmaceutical applications. Highlights In the current review, we have tried to compile recent discoveries on natural and synthetic flavonoids as well as their implication in the treatment of malaria, leishmaniasis, Chagas disease, and dengue. A total of 373 (220 natural and 153 synthetic) flavonoids have been evaluated for antimalarial, antileishmanial, antichagasic, and antidengue activities. Most of these flavonoids showed promising results against the above diseases. Reports on molecular modeling of flavonoid compounds to the disease target indicated encouraging results. Flavonoids can be prospected as potential leads for drug development; however, more rigorously designed studies on toxicity and pharmacokinetics, as well as the quantitative structure–activity relationship studies of these compounds, need to be addressed.

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Pharmacokinetic study of rutin and quercetin in rats after oral administration of total flavones of mulberry leaf extract

Cited by 52 publications

References 6 publications

Rutin as A Novel c-Met Inhibitory Lead for The Control of Triple Negative Breast Malignancies

Rutin as A Novel c-Met Inhibitory Lead for The Control of Triple Negative Breast Malignancies

Development and validation of HPLC method for vicenin-1 isolated from fenugreek seeds in rat plasma: application to pharmacokinetic, tissue distribution and excretion studies

Flavonoids as efficient scaffolds: Recent trends for malaria, leishmaniasis, Chagas disease, and dengue

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