Comparison of metabolic pharmacokinetics of naringin and naringenin in rabbits

Hsiu, Su-Lan; Huang, Tang-Yen; Hou, Yu‐Chi; Chin, Daeje; Chao, Pei‐Dawn Lee

doi:10.1016/s0024-3205(01)01491-6

Cited by 126 publications

(77 citation statements)

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“…For instance, flavanones (i.e. hesperetin and naringenin) have been reported to have plasma elimination half-lives between 1 and 3 h in humans [32,40] and less than 20 min in rabbits [33]. Similar observations have been reported for flavanols (i.e.…”

Section: Introductionsupporting

confidence: 67%

“…The achiral pharmacokinetics of hesperetin, naringenin, eriodictyol and their corresponding glycosides have been reported [8,14,[32][33][34][35][36] as well as their content in different fruits and fruit juices [5]. Furthermore, to our knowledge there are no studies that have properly assessed the urinary pharmacokinetics and/or disposition of these three chiral flavonoids or other polyphenols after oral ingestion of fruit juices or individual flavonoids in humans or rodents.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetics of selected chiral flavonoids: hesperetin, naringenin and eriodictyol in rats and their content in fruit juices

Yáñez

Remsberg

Miranda

et al. 2007

Biopharm & Drug Disp

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The majority of pharmacokinetic studies of individual flavonoids or after ingestion of foodstuffs have overlooked the chirality of some of these xenobiotics. In order to characterize for the first time the stereoselective pharmacokinetics of three flavonoids, hesperetin, naringenin and eriodictyol were intravenously administered (20 mg/kg) to male Sprague-Dawley rats, and their stereospecific content was assessed in various fruit juices. Concentrations in serum, urine and fruit juices were characterized via HPLC and verified by LC/MS. Short half-lives (3-7 h) in serum were observed, while a better estimation of half-life (12-48 h) and the other pharmacokinetic parameters was observed using urinary data. The three flavonoids are predominantly excreted via non-renal routes (fe values of 3-7%), and undergo rapid and extensive phase II metabolism. The (2S)-epimers of the flavonoid glycosides and the S(-)-enantiomers of the aglycones were predominant and in some instances the organic fruit juices had higher concentrations than the conventional fruit juices. This study reports for the first time the stereospecific pharmacokinetics of three chiral flavonoids and their stereospecific content in fruit juices. It also reports for the first time the stereospecific pharmacokinetics of flavonoids employing urine as a more reliable biological matrix.

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Section: Introductionsupporting

confidence: 67%

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of selected chiral flavonoids: hesperetin, naringenin and eriodictyol in rats and their content in fruit juices

Yáñez

Remsberg

Miranda

et al. 2007

Biopharm & Drug Disp

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“…21,22 Consequently, the oral bioavailability of naringin is low (~8%) and its half-life has been estimated to be 2.6 h. 23 In addition, its poor solubility in water hindered its formulation for parenteral use. 24 Thus, alternative naringin formulations such as nanoparticulate systems would be essential to protect the drug against degradation in the gut, improve its bioavailability, and provide a sustained delivery of the drug in the purpose of potentiating its therapeutic efficacy.…”

mentioning

confidence: 99%

Polymeric micelles for potentiated antiulcer and anticancer activities of naringin

Mohamed¹,

Hashim²,

Yusif³

et al. 2018

IJN

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Naringin is one of the most interesting phytopharmaceuticals that has been widely investigated for various biological actions. Yet, its low water solubility, limited permeability, and suboptimal bioavailability limited its use. Therefore, in this study, polymeric micelles of naringin based on pluronic F68 (PF68) were developed, fully characterized, and optimized. The optimized formula was investigated regarding in vitro release, storage stability, and in vitro cytotoxicity vs different cell lines. Also, cytoprotection against ethanol-induced ulcer in rats and antitumor activity against Ehrlich ascites carcinoma in mice were investigated. Nanoscopic and nearly spherical 1:50 micelles with the mean diameter of 74.80±6.56 nm and narrow size distribution were obtained. These micelles showed the highest entrapment efficiency (EE%; 96.14±2.29). The micelles exhibited prolonged release up to 48 vs 10 h for free naringin. The stability of micelles was confirmed by insignificant changes in drug entrapment, particle size, and retention (%) (91.99±3.24). At lower dose than free naringin, effective cytoprotection of 1:50 micelles against ethanol-induced ulcer in rat model has been indicated by significant reduction in mucosal damage, gastric level of malondialdehyde, gastric expression of tumor necrosis factor-alpha, caspase-3, nuclear factor kappa-light-chain-enhancer of activated B cells, and interleukin-6 with the elevation of gastric reduced glutathione and superoxide dismutase when compared with the positive control group. As well, these micelles provoked pronounced antitumor activity assessed by potentiated in vitro cytotoxicity particularly against colorectal carcinoma cells and tumor growth inhibition when compared with free naringin. In conclusion, 1:50 naringin–PF68 micelles can be represented as a potential stable nanodrug delivery system with prolonged release and enhanced antiulcer as well as antitumor activities.

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“…Recently, assay methods for the conjugated metabolites of flavonoids in serum or urine have been developed in our laboratory. [18][19][20][21] The main object of this study was to investigate the urinary pharmacokinetics of the bioactive flavones in Scutellariae Radix after oral administration of a commercial powder to ten healthy male volunteers.…”

mentioning

confidence: 99%

Urinary Pharmacokinetics of Baicalein, Wogonin and Their Glycosides after Oral Administration of Scutellariae Radix in Humans.

Lai¹,

Hsiu²,

Chen³

et al. 2003

Biological & Pharmaceutical Bulletin

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110

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Baicalin, baicalein, wogonoside and wogonin are flavone constituents of Scutellariae Radix with various beneficial biological activities. The purpose of this study was to investigate the urinary pharmacokinetics of these flavones after oral administration of Scutellariae Radix commercial powder. Ten healthy male volunteers received a dose of 5.2 g commercial powder (comparable to 9 g crude drug), respectively. The concentrations of baicalin, baicalein and wogonin in the commercial powder as well as their metabolites in urine were assayed by HPLC method. The glucuronides and sulfates of baicalein and wogonin in urine were hydrolyzed with b b-glucuronidase and sulfatase, respectively. Our results showed that the mean cumulated renal excretion of baicalein glucuronides and sulfates were 43.1؎4.5 m mmol (2.9% of dose) and 64.8؎6.3 m mmol (4.3% of dose), respectively, whereas wogonin glucuronides and sulfates were 21.6؎2.0 m mmol (5.9% of dose) and 20.7؎1.7 m mmol (5.7% of dose), respectively. The result indicated that the renal excretion of conjugated metabolites of wogonin (11.6% of dose) were higher than that of baicalein (7.2% of dose). The baicalein sulfates was predominant than the corresponding glucuronides, whereas wogonin sulfates was comparable to the corresponding glucuronides.

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Comparison of metabolic pharmacokinetics of naringin and naringenin in rabbits

Cited by 126 publications

References 0 publications

Pharmacokinetics of selected chiral flavonoids: hesperetin, naringenin and eriodictyol in rats and their content in fruit juices

Pharmacokinetics of selected chiral flavonoids: hesperetin, naringenin and eriodictyol in rats and their content in fruit juices

Polymeric micelles for potentiated antiulcer and anticancer activities of naringin

Urinary Pharmacokinetics of Baicalein, Wogonin and Their Glycosides after Oral Administration of Scutellariae Radix in Humans.

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