A rapid LC/MS/MS quantitation assay for naringin and its two metabolites in rats plasma

Fang, Tiezheng; Wang, Yonggang; Ma, Yan; Su, Weiwei; Bai, Yang; Zhao, Pengfei

doi:10.1016/j.jpba.2005.07.031

Cited by 94 publications

(66 citation statements)

References 15 publications

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“…The presence of naringin in the plasma demonstrates that the deglycosidation of naringin is not always necessary for its absorption. Previous studies (Fang et al 2006) have administered naringin as a pure compound, whereas in the present study citrus flavanones were administered in the form of a grapefruit extract (as it occurs in nature), in a dose equivalent to that of half a grapefruit. The influence of food matrices must always be considered when interpreting results; it should be borne in mind that they could have been different had pure compounds been used.…”

Section: Discussionmentioning

confidence: 99%

“…Fang et al (2006) have reported plasma concentrations of 3·8, 0·23 and 43·58 mg/ml for naringin, naringenin and naringenin glucuronide respectively after an oral administration of 746·7 mg/kg naringin as a pure compound. In the present study, 70 mg flavanones given as a grapefruit extract were orally administered, and several pharmacokinetic parameters were calculated for naringin and for each of the flavanone metabolites that have been found in dog plasma.…”

Section: Discussionmentioning

confidence: 99%

“…However, the absorption of quercetin glycosides from onions in human subjects (Hollman et al 1995) and the presence of the flavanone glycoside naringin in plasma and urine after oral administration (Ishii et al 2000;Fang et al 2006) have now been demonstrated.…”

mentioning

confidence: 99%

“…Ionspray ionization, together with tandem MS for structural characterization, has become a popular and versatile method for flavonoid analysis (Roura et al 2005;Urpí-Sardà et al 2005;Fang et al 2006).…”

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confidence: 99%

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Absorption and pharmacokinetics of grapefruit flavanones in beagles

et al. 2007

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The present study evaluated the pharmacokinetics of three different grapefruit flavanone forms in dog plasma and demonstrated their absorption after an oral intake of a grapefruit extract; pharmacokinetic parameters of these forms were also determined. Ten healthy beagles were administered 70 mg citrus flavonoids as a grapefruit extract contained in capsules, while two additional dogs were used as controls and given an excipient. The grapefruit flavanone naringin, along with its metabolites naringenin and naringenin glucuronide, was detected in dog plasma. Blood samples were collected between 0 and 24 h after administration of the extract. Naringin reached its maximun plasma concentration at around 80 min, whereas naringenin and naringenin glucuronide reached their maximun plasma concentrations at around 20 and 30 min, respectively. Maximum plasma concentrations of naringin, naringenin and naringenin glucuronide (medians and ranges) were 0·24 (0·05-2·08), 0·021 (0·001 -0·3) and 0·09 (0·034-0·12) mmol/l, respectively. The areas under the curves were 23·16 l (14·04 -70·62) min £ mmol/for nariningin, 1·78 (0·09 -4·95) min £ mmol/l for naringenin and 22·5 (2·74 -99·23) min £ mmol/l for naringenin glucuronide. The median and range values for mean residence time were 3·3 (1·5 -9·3), 2·8 (0·8 -11·2) and 8·0 (2·3 -13·1) h for naringin, naringenin and naringenin glucuronide, respectively. The results of the present study demonstrate the absorption of grapefruit flavanones via the presence of their metabolites in plasma, thus making an important contribution to the field since the biological activities ascribed to these compounds rely on their specific forms of absorption.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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confidence: 99%

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confidence: 99%

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Absorption and pharmacokinetics of grapefruit flavanones in beagles

et al. 2007

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“…The concentration of naringin in the plasma was determined by high-performance liquid chromatography (HPLC) with slight modification of previous methods [17]. Briefly, the plasma samples were loaded into Auto sampler HPLC system (Waters 717 plus, Milford, Mass., USA) that consisted of a 515 HPLC dual pump and a 2487 Dual λ absorbance detector.…”

Section: Methodsmentioning

confidence: 99%

Naringin Exhibits in vivo Prokinetic Activity via Activation of Ghrelin Receptor in Gastrointestinal Motility Dysfunction Rats

2013

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Background and Purpose: Poncirus fructus (PF), also known as the dried immature fruit of Poncirus trifoliata (L.) Raf., has long been used as a cure for the treatment of various gastrointestinal disorders in eastern Asia. Recently, it was reported that naringin, a flavonoid constituent of the PF extract, causes the activation of ghrelin receptor in vitro. Although the ghrelin receptor is involved in the enhancement of intestinal motility, there are no studies as yet involving in vivo action of naringin. Therefore, the purpose of the present study is to investigate whether naringin exhibits a prokinetic effect in vivo. Methods: We measured the intestinal transit rate in rats with gastrointestinal motility dysfunction (GMD) and performed a pharmacokinetic analysis of naringin to investigate the effect of naringin on prokinetic activity in vivo. Results: The results of this study show that the aqueous extract of PF and its constituent naringin have a strong prokinetic activity in GMD rats via activation of the ghrelin receptor. Surprisingly, pharmacokinetic analysis revealed that naringin has low bioavailability (11%), implying that the prokinetic effect of naringin was largely due to the local activation of ghrelin receptor in the intestine rather than a systemic effect after absorption. Indeed, it turned out that intravenous administration of naringin led to a lower prokinetic effect than when administrated orally to rats, indicating that naringin prefers to act on the intestinal wall rather than getting absorbed into the systemic circuit. This local mode of action might be advantageous for preventing possible systemic side effects since naringin is not well absorbed into the system circuit. Conclusions: Naringin exhibits an in vivo prokinetic activity by a preferable local activation of ghrelin receptor. Moreover, we propose that naringin could play a role as a leading compound for the development of ghrelin receptor-based prokinetic agents.

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Metabolism and excretion studies of oral administered naringin, a putative antitussive, in rats and dogs

Liu

Zou

Yang

et al. 2012

Biopharm & Drug Disp

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Naringin, a major active flavonone glycoside from a traditional Chinese medicine Huajuhong, has been demonstrated to have activities such as peripheral antitussive, mucoregulator and anti-inflammatory. The purpose of this study was to elucidate the metabolism and mass balance of orally administered naringin in rats and dogs. After oral administration of naringin to rats and dogs at doses of 42 mg/kg and 12.4 mg/kg, respectively, metabolites in excreta were identified using a LC-Q-TOF system. The major metabolites including naringin, total naringenin (including free naringenin and its conjugates) and 4-hydroxyphenylpropionic acid in excreta were quantified by a LC-MS/MS system. Twenty-two metabolites were identified in dogs and 17 metabolites were detected in rats. The observed routes of naringin metabolism were hydroxylation, methylation, acetylation, hydrogenation, deglycosylation, dehydrogenation, glucuronidation, sulfation, glucosylation, ring-fission, oxidation, glycine conjugation and dehydroxylation. On the basis of these identified metabolites, a comprehensive metabolic pathway of naringin was proposed. About 21% of administered naringin was recovered in rat excreta in the form of naringin, total naringenin and 4-hydroxyphenylpropionic acid, and about 60% was recovered in dog excreta. The levels of 4-hydroxyphenylpropionic acid in excreta were higher than those of naringin and total naringenin, and the quantified metabolites were excreted more through feces, rather than urine. Most of these metabolites were excreted within 36 h post dose. The results of metabolism and excretion studies provide an explanation for future pharmacological and toxicological findings and are the groundwork for clinical studies.

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A rapid LC/MS/MS quantitation assay for naringin and its two metabolites in rats plasma

Cited by 94 publications

References 15 publications

Absorption and pharmacokinetics of grapefruit flavanones in beagles

Absorption and pharmacokinetics of grapefruit flavanones in beagles

Naringin Exhibits in vivo Prokinetic Activity via Activation of Ghrelin Receptor in Gastrointestinal Motility Dysfunction Rats

Metabolism and excretion studies of oral administered naringin, a putative antitussive, in rats and dogs

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