Molecular targets of [6]‐gingerol: Its potential roles in cancer chemoprevention

Oyagbemi, Ademola Adetokunbo; Saba, Adebowale Benard; Azeez, O. I.

doi:10.1002/biof.78

Cited by 99 publications

(64 citation statements)

References 109 publications

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“…In addition, the other components of ginger powders or extracts such as paradols were not quantified due to the lack of commercially available standards. Paradols have shown pharmacological effects similar to gingerols and shogaols (36)(37)(38)(39). All these components warrant future studies.…”

Section: Discussionmentioning

confidence: 93%

Examination of the Pharmacokinetics of Active Ingredients of Ginger in Humans

Zick

et al. 2011

AAPS J

106

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Abstract. Ginger extracts have been studied in various clinical trials for different indications. However, the pharmacokinetics of the ginger active constituents in human biological matrices is not well investigated. This study aims to develop a LC-MS/MS method for simultaneous measurement of 6-, 8-, and 10-gingerols and 6-shogaol and study their pharmacokinetics in human plasma and colon tissues. A sensitive LC-MS/MS method was established and validated with a low limit of quantification of 2-5 ng/ mL. The intra-and inter-day accuracy ranged from −7.3% to 10.4% and from −9.4% to 9.8%, respectively. The intra-and inter-day precision ranged from 0.9% to 10.9% and from 2.0% to 12.4%, respectively. The glucuronide and sulfate metabolites of 6-, 8-, and 10-gingerols and 6-shogaol in plasma and colon tissues were quantified after hydrolysis with β-glucuronidase and sulfatase. After oral dosing of 2.0 g ginger extracts in human, free 10-gingerol and 6-shogaol were detected in plasma with peak concentrations (9.5±2.2 and 13.6±6.9 ng/mL, respectively) at 1 h after oral administration, but no free 6-gingerol and 8-gingerol were detected in plasma from 0.25 to 24 h. The peak concentrations of glucuronide metabolites of 6-, 8-, and 10-gingerols and 6-shogaol were 0.47±0.31, 0.17±0.14, 0.37±0.19, and 0.73±0.54 μg/mL at 1 h, respectively. The peak concentrations of the sulfate metabolites of 6-, 8-, and 10-gingerols and 6-shogaol were 0.28±0.15, 0.027±0.018, 0.018±0.006, and 0.047±0.035 μg/mL at 1 h, respectively. Very low concentrations (2-3 ng/mL) of 10-gingerol glucuronide and sulfate were found in colon tissues. Pharmacokinetic analysis showed that half-lives of these four analytes and their metabolites were 1-3 h in human plasma. No accumulation was observed for 6-, 8-, and 10-gingerols and 6-shogaol and their metabolites in both plasma and colon tissues after multiple daily dosing.

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Section: Discussionmentioning

confidence: 93%

Examination of the Pharmacokinetics of Active Ingredients of Ginger in Humans

Zick

et al. 2011

AAPS J

106

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“…Cyclooxygenase (COX) is an important proinflammatory mediator and COX2 is responsible for persistent inflammation [49]. As (S)- [6]gingerol exhibits anti-inflammatory and antioxidant properties [50][51][52] we studied the mechanisms that underlie the anti-inflammatory effects of (S)- [6]-gingerol, isolated in our laboratory, in the IL1 -treated HuH-7 hepatocyte cell model. Pretreatment of HuH-7 cells with (S)- [6]-gingerol for 6 h significantly inhibited IL1 -induced NF-B activity, suggesting that the protective effects of (S)- [6]-gingerol against IL1 -induced inflammation are, at least in part, associated with inhibition of NF-B activation in HuH-7 cells.…”

Section: Effects Of Zingiber Officinale On Inflammatory Markersmentioning

confidence: 99%

Zingiber officinale(Ginger): A Future Outlook on Its Potential in Prevention and Treatment of Diabetes and Prediabetic States

Roufogalis

2014

New Journal of Science

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Diabetes is reaching pandemic levels in both developing and developed countries and requires safe, affordable, and effective therapies. This report summarises work in our laboratory on the effects of Zingiber officinale (ginger) and its components in diabetes models and provides a future outlook on the potential for their use in type 2 diabetes. A high fat diet rat model showed modulation of body weight gain and normalisation of glucose and lipid metabolic disturbances, with reduction of insulin resistance in a high fat-high carbohydrate diet model. Ginger extract inhibits enhanced NF-B in liver of high fat-fed rats through inhibition of the IKK/I B /NF-B classical pathway. The major active component (S) -[6]-gingerol inhibited elevated cytokines in inflamed HuH-7 cells through suppression of COX2 expression and protection against the ROS pathway. Ginger extract and gingerols enhanced glucose uptake in L6 myotubes, by enhancing translocation of GLUT4 to the surface membrane and activation of AMPK 1 through a Ca 2+ /calmodulin-dependent protein kinase kinase pathway. (S)-[6]-Gingerol also enhanced energy metabolism through marked increment of peroxisome proliferator-activated receptor-coactivator-1 (PGC-1 ) gene expression and mitochondrial content in L6 skeletal muscle cells. Future studies will require well designed clinical trials on ginger preparations of defined chemical composition.

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“…Ginger is known to possess antioxidant properties. 6-Gingerol, a natural product of ginger, has been known to possess anti-tumorigenic and pro-apoptotic activities (Oyagbemi et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Effect of methotrexate combined with ginger, silymarin or propolis on the mRNA expression levels of cytochrome P450 oxidoreductase (POR), caspase 3 (CASP-3) and interlukin 6 (IL-6)

Hassan¹,

Ismail²,

Mohamed³

2015

Afr. J. Biotechnol.

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The present study was performed to evaluate the effect of three natural antioxidants on the adverse effect of methotrexate (MTX) in normal liver cells. TaqMan RT-PCR technology was used to estimate the mRNA expression levels for three genes after rats injection with a single dose of 20 mg/kg b.w MTX or the same MTX dose combined with ginger, silymarin or propolis oral administration. The doses of ginger, silymarin or propolis were similar (200 mg/kg b.w) and were daily administrated to rats for 21 days before MTX injection and four days after MTX injection. The three genes were: cytochrome P450 oxidoreductase (POR) that encodes POR enzyme, caspase 3 (CASP-3) that encodes CASP-3 enzyme and interlukin 6 (IL-6) that encodes IL-6 pro-inflammatory cytokine. Results indicate that the used MTX single dose of 20 mg/kg b.w did not significantly affect POR mRNA expression level in rat liver. Moreover the administration of ginger, silymarin or propolis with MTX did not significantly increase or decrease POR mRNA expression level. Results also reveal insignificant increase in CASP-3 mRNA expression level after MTX injection and also after administration of ginger or propolis with MTX. The administration of silymarin with MTX significantly increased the CASP-3 mRNA expression level. IL-6 mRNA expression level was insignificantly upregulated after injection with MTX and also after administration of silymarin with MTX whereas a significantly upregulation in the IL-6 mRNA expression level was reported after administration of ginger or propolis with MTX.

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Molecular targets of [6]‐gingerol: Its potential roles in cancer chemoprevention

Cited by 99 publications

References 109 publications

Examination of the Pharmacokinetics of Active Ingredients of Ginger in Humans

Examination of the Pharmacokinetics of Active Ingredients of Ginger in Humans

Zingiber officinale(Ginger): A Future Outlook on Its Potential in Prevention and Treatment of Diabetes and Prediabetic States

Effect of methotrexate combined with ginger, silymarin or propolis on the mRNA expression levels of cytochrome P450 oxidoreductase (POR), caspase 3 (CASP-3) and interlukin 6 (IL-6)

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