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Tissue distribution of naringenin conjugated metabolites following repeated dosing of naringin to rats.

Lin SP, Hou YC, Tsai SY, Wang MJ, Chao PD - Biomedicine (Taipei) (2014)

Bottom Line: Liver contained the highest concentration of naringenin sulfates, followed by spleen, heart, brain and kidney.Naringenin glucuronides were present in liver and kidney, but not in spleen, brain and heart.Conclusion: The bioavailability of naringenin glucuronides and sulfates supported its application for personalized medicine.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, China Medical University, No.91 Hsueh-Shih Road, Taichung, Taiwan.

ABSTRACT

Background: Naringin is a major antioxidant in Citrus fruits and herbs. To clarify molecular forms distributed to various tissues, we investigated tissue distribution of naringin and relevant metabolites in rats after repeated dosing. Methods: Male Sprague-Dawley rats were orally administered naringin (210 mg/kg) twice daily for eight days. At 6 h post the 17(th) dose, various tissues including liver, kidney, heart, spleen and brain were collected and analyzed by HPLC method before and after hydrolysis with β-glucuronidase and sulfatase, individually. Results: The free forms of naringin and naringenin were not detected in all the tissues assayed. Liver contained the highest concentration of naringenin sulfates, followed by spleen, heart, brain and kidney. Naringenin glucuronides were present in liver and kidney, but not in spleen, brain and heart. Conclusion: The bioavailability of naringenin glucuronides and sulfates supported its application for personalized medicine.

No MeSH data available.


Related in: MedlinePlus

Chemical structures of naringin and naringenin.
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Fig1: Chemical structures of naringin and naringenin.

Mentions: Flavonoids, major class of antioxidants, prove interesting to pharmacologists due to various beneficial bioactivities [1,2]. They also draw attention from pharmaceutical researchers via capacity for modulating P-glycoprotein (P-gp) and CYP 3A4 [3-6], both prominent in pharmacokinetics [7, 8]. Naringin (4’, 5, 7-trihydroxyflavanone 7-rhamnoglucoside) is one major flavonoid distributed in Citrus fruits like grapefruit (C. paradisi) or pomelo (C. grandis) and in Chinese herbs like C. aurantium and C. maxima [9]. Numerous in vitro studies report naringin and naringenin, the aglycon of naringin, (structures in Fig. 1) exhibiting benefits: e.g., anticancer [10,11], superoxide scavenging, antioxidation [12,13], antimicrobial effects [14]. Naringin-containing nutraceuticals are increasingly used as dietary supplements, yet based on our prior studies reporting pharmacokinetics of naringin in rabbits and rats, n aringenin sulfates and glucuronides appeared predominately in the blood-stream, with no trace of naringin or naringenin detected [15,16]. Whether bioactivities of naringin and naringenin cited by earlier in vitro study can be extrapolated to in vivo effects remained unanswered [17]. Regarding major forms in various organs, previous studies report tissue distribution of naringin or naringenin in rats [18-20], yet these followed single dose via intravenous or oral route, findings less than consistent. We analyzed distribution of naringin and relevant metabolites in rat tissue after repeated dosing.


Tissue distribution of naringenin conjugated metabolites following repeated dosing of naringin to rats.

Lin SP, Hou YC, Tsai SY, Wang MJ, Chao PD - Biomedicine (Taipei) (2014)

Chemical structures of naringin and naringenin.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4265019&req=5

Fig1: Chemical structures of naringin and naringenin.
Mentions: Flavonoids, major class of antioxidants, prove interesting to pharmacologists due to various beneficial bioactivities [1,2]. They also draw attention from pharmaceutical researchers via capacity for modulating P-glycoprotein (P-gp) and CYP 3A4 [3-6], both prominent in pharmacokinetics [7, 8]. Naringin (4’, 5, 7-trihydroxyflavanone 7-rhamnoglucoside) is one major flavonoid distributed in Citrus fruits like grapefruit (C. paradisi) or pomelo (C. grandis) and in Chinese herbs like C. aurantium and C. maxima [9]. Numerous in vitro studies report naringin and naringenin, the aglycon of naringin, (structures in Fig. 1) exhibiting benefits: e.g., anticancer [10,11], superoxide scavenging, antioxidation [12,13], antimicrobial effects [14]. Naringin-containing nutraceuticals are increasingly used as dietary supplements, yet based on our prior studies reporting pharmacokinetics of naringin in rabbits and rats, n aringenin sulfates and glucuronides appeared predominately in the blood-stream, with no trace of naringin or naringenin detected [15,16]. Whether bioactivities of naringin and naringenin cited by earlier in vitro study can be extrapolated to in vivo effects remained unanswered [17]. Regarding major forms in various organs, previous studies report tissue distribution of naringin or naringenin in rats [18-20], yet these followed single dose via intravenous or oral route, findings less than consistent. We analyzed distribution of naringin and relevant metabolites in rat tissue after repeated dosing.

Bottom Line: Liver contained the highest concentration of naringenin sulfates, followed by spleen, heart, brain and kidney.Naringenin glucuronides were present in liver and kidney, but not in spleen, brain and heart.Conclusion: The bioavailability of naringenin glucuronides and sulfates supported its application for personalized medicine.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, China Medical University, No.91 Hsueh-Shih Road, Taichung, Taiwan.

ABSTRACT

Background: Naringin is a major antioxidant in Citrus fruits and herbs. To clarify molecular forms distributed to various tissues, we investigated tissue distribution of naringin and relevant metabolites in rats after repeated dosing. Methods: Male Sprague-Dawley rats were orally administered naringin (210 mg/kg) twice daily for eight days. At 6 h post the 17(th) dose, various tissues including liver, kidney, heart, spleen and brain were collected and analyzed by HPLC method before and after hydrolysis with β-glucuronidase and sulfatase, individually. Results: The free forms of naringin and naringenin were not detected in all the tissues assayed. Liver contained the highest concentration of naringenin sulfates, followed by spleen, heart, brain and kidney. Naringenin glucuronides were present in liver and kidney, but not in spleen, brain and heart. Conclusion: The bioavailability of naringenin glucuronides and sulfates supported its application for personalized medicine.

No MeSH data available.


Related in: MedlinePlus