Pharmacokinetics of 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol and conjugate metabolites in healthyhuman subjects

Suzanna M. Zick, Zora Djuric, Mack T. Ruffin, Amie J. Litzinger, Daniel P. Normolle, Sara Alrawi, Meihua Rose Feng, Dean E. Brenner

Research output: Contribution to journalArticle

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Abstract

Background: Ginger shows promising anticancer properties. No research has examined the pharmacokinetics of the ginger constituents 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol in humans. We conducted a clinical trial with 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol, examining the pharmacokinetics and tolerability of these analytes and their conjugate metabolites. Methods: Human volunteers were given ginger at doses from 100 mg to 2.0 g (N = 27), and blood samples were obtained at 15 minutes to 72 hours after a single p.o. dose. The participants were allocated in a dose-escalation manner starting with 100 mg. There was a total of three participants at each dose except for 1.0 g (N = 6) and 2.0 g (N = 9). Results: No participant had detectable free 6-gingerol, 8-gingerol, 10-gingerol, or 6-shogaol, but 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol glucuronides were detected. The 6-gingerol sulfate conjugate was detected above the 1.0-g dose, but there were no detectable 10-gingerol or 6-shogaol sulfates except for one participant with detectable 8-gingerol sulfate. The Cmax and area under the curve values (mean ± SE) estimated for the 2.0-g dose are 0.85 ± 0.43, 0.23 ± 0.16, 0.53 ± 0.40, and 0.15 ± 0.12 μg/mL; and 65.6.33 ± 44.4, 18.1 ± 20.3, 50.1 ± 49.3, and 10.9 ± 13.0 μg·hr/mL for 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol. The corresponding tmax values are 65.6 ± 44.4, 73.1 ± 29.4, 75.0 ± 27.8, and 65.6 ± 22.6 minutes, and the analytes had elimination half-lives <2 hours. The 8-gingerol, 10-gingerol, and 6-shogaol conjugates were present as either glucuronide or sulfate conjugates, not as mixed conjugates, although 6-gingerol and 10-gingerol were an exception. Conclusion: Six-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol are absorbed after p.o. dosing and can be detected as glucuronide and sulfate conjugates.

Original languageEnglish (US)
Pages (from-to)1930-1936
Number of pages7
JournalCancer Epidemiology Biomarkers and Prevention
Volume17
Issue number8
DOIs
StatePublished - Aug 1 2008

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Pharmacokinetics
Sulfates
Ginger
Glucuronides
gingerol
shogaol
8-gingerol
Area Under Curve
Volunteers
Clinical Trials

All Science Journal Classification (ASJC) codes

  • Epidemiology
  • Oncology

Cite this

Zick, Suzanna M. ; Djuric, Zora ; Ruffin, Mack T. ; Litzinger, Amie J. ; Normolle, Daniel P. ; Alrawi, Sara ; Feng, Meihua Rose ; Brenner, Dean E. / Pharmacokinetics of 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol and conjugate metabolites in healthyhuman subjects. In: Cancer Epidemiology Biomarkers and Prevention. 2008 ; Vol. 17, No. 8. pp. 1930-1936.
@article{fe3e86cbb0284396877cdfc75828b2ca,
title = "Pharmacokinetics of 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol and conjugate metabolites in healthyhuman subjects",
abstract = "Background: Ginger shows promising anticancer properties. No research has examined the pharmacokinetics of the ginger constituents 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol in humans. We conducted a clinical trial with 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol, examining the pharmacokinetics and tolerability of these analytes and their conjugate metabolites. Methods: Human volunteers were given ginger at doses from 100 mg to 2.0 g (N = 27), and blood samples were obtained at 15 minutes to 72 hours after a single p.o. dose. The participants were allocated in a dose-escalation manner starting with 100 mg. There was a total of three participants at each dose except for 1.0 g (N = 6) and 2.0 g (N = 9). Results: No participant had detectable free 6-gingerol, 8-gingerol, 10-gingerol, or 6-shogaol, but 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol glucuronides were detected. The 6-gingerol sulfate conjugate was detected above the 1.0-g dose, but there were no detectable 10-gingerol or 6-shogaol sulfates except for one participant with detectable 8-gingerol sulfate. The Cmax and area under the curve values (mean ± SE) estimated for the 2.0-g dose are 0.85 ± 0.43, 0.23 ± 0.16, 0.53 ± 0.40, and 0.15 ± 0.12 μg/mL; and 65.6.33 ± 44.4, 18.1 ± 20.3, 50.1 ± 49.3, and 10.9 ± 13.0 μg·hr/mL for 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol. The corresponding tmax values are 65.6 ± 44.4, 73.1 ± 29.4, 75.0 ± 27.8, and 65.6 ± 22.6 minutes, and the analytes had elimination half-lives <2 hours. The 8-gingerol, 10-gingerol, and 6-shogaol conjugates were present as either glucuronide or sulfate conjugates, not as mixed conjugates, although 6-gingerol and 10-gingerol were an exception. Conclusion: Six-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol are absorbed after p.o. dosing and can be detected as glucuronide and sulfate conjugates.",
author = "Zick, {Suzanna M.} and Zora Djuric and Ruffin, {Mack T.} and Litzinger, {Amie J.} and Normolle, {Daniel P.} and Sara Alrawi and Feng, {Meihua Rose} and Brenner, {Dean E.}",
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language = "English (US)",
volume = "17",
pages = "1930--1936",
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Pharmacokinetics of 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol and conjugate metabolites in healthyhuman subjects. / Zick, Suzanna M.; Djuric, Zora; Ruffin, Mack T.; Litzinger, Amie J.; Normolle, Daniel P.; Alrawi, Sara; Feng, Meihua Rose; Brenner, Dean E.

In: Cancer Epidemiology Biomarkers and Prevention, Vol. 17, No. 8, 01.08.2008, p. 1930-1936.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Pharmacokinetics of 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol and conjugate metabolites in healthyhuman subjects

AU - Zick, Suzanna M.

AU - Djuric, Zora

AU - Ruffin, Mack T.

AU - Litzinger, Amie J.

AU - Normolle, Daniel P.

AU - Alrawi, Sara

AU - Feng, Meihua Rose

AU - Brenner, Dean E.

PY - 2008/8/1

Y1 - 2008/8/1

N2 - Background: Ginger shows promising anticancer properties. No research has examined the pharmacokinetics of the ginger constituents 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol in humans. We conducted a clinical trial with 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol, examining the pharmacokinetics and tolerability of these analytes and their conjugate metabolites. Methods: Human volunteers were given ginger at doses from 100 mg to 2.0 g (N = 27), and blood samples were obtained at 15 minutes to 72 hours after a single p.o. dose. The participants were allocated in a dose-escalation manner starting with 100 mg. There was a total of three participants at each dose except for 1.0 g (N = 6) and 2.0 g (N = 9). Results: No participant had detectable free 6-gingerol, 8-gingerol, 10-gingerol, or 6-shogaol, but 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol glucuronides were detected. The 6-gingerol sulfate conjugate was detected above the 1.0-g dose, but there were no detectable 10-gingerol or 6-shogaol sulfates except for one participant with detectable 8-gingerol sulfate. The Cmax and area under the curve values (mean ± SE) estimated for the 2.0-g dose are 0.85 ± 0.43, 0.23 ± 0.16, 0.53 ± 0.40, and 0.15 ± 0.12 μg/mL; and 65.6.33 ± 44.4, 18.1 ± 20.3, 50.1 ± 49.3, and 10.9 ± 13.0 μg·hr/mL for 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol. The corresponding tmax values are 65.6 ± 44.4, 73.1 ± 29.4, 75.0 ± 27.8, and 65.6 ± 22.6 minutes, and the analytes had elimination half-lives <2 hours. The 8-gingerol, 10-gingerol, and 6-shogaol conjugates were present as either glucuronide or sulfate conjugates, not as mixed conjugates, although 6-gingerol and 10-gingerol were an exception. Conclusion: Six-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol are absorbed after p.o. dosing and can be detected as glucuronide and sulfate conjugates.

AB - Background: Ginger shows promising anticancer properties. No research has examined the pharmacokinetics of the ginger constituents 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol in humans. We conducted a clinical trial with 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol, examining the pharmacokinetics and tolerability of these analytes and their conjugate metabolites. Methods: Human volunteers were given ginger at doses from 100 mg to 2.0 g (N = 27), and blood samples were obtained at 15 minutes to 72 hours after a single p.o. dose. The participants were allocated in a dose-escalation manner starting with 100 mg. There was a total of three participants at each dose except for 1.0 g (N = 6) and 2.0 g (N = 9). Results: No participant had detectable free 6-gingerol, 8-gingerol, 10-gingerol, or 6-shogaol, but 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol glucuronides were detected. The 6-gingerol sulfate conjugate was detected above the 1.0-g dose, but there were no detectable 10-gingerol or 6-shogaol sulfates except for one participant with detectable 8-gingerol sulfate. The Cmax and area under the curve values (mean ± SE) estimated for the 2.0-g dose are 0.85 ± 0.43, 0.23 ± 0.16, 0.53 ± 0.40, and 0.15 ± 0.12 μg/mL; and 65.6.33 ± 44.4, 18.1 ± 20.3, 50.1 ± 49.3, and 10.9 ± 13.0 μg·hr/mL for 6-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol. The corresponding tmax values are 65.6 ± 44.4, 73.1 ± 29.4, 75.0 ± 27.8, and 65.6 ± 22.6 minutes, and the analytes had elimination half-lives <2 hours. The 8-gingerol, 10-gingerol, and 6-shogaol conjugates were present as either glucuronide or sulfate conjugates, not as mixed conjugates, although 6-gingerol and 10-gingerol were an exception. Conclusion: Six-gingerol, 8-gingerol, 10-gingerol, and 6-shogaol are absorbed after p.o. dosing and can be detected as glucuronide and sulfate conjugates.

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