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

Suzanna M. Zick, Zora Djuric, Mack 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 ; 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 Mack Ruffin and Litzinger, {Amie J.} and Normolle, {Daniel P.} and Sara Alrawi and Feng, {Meihua Rose} and Brenner, {Dean E.}",
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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; 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

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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