Toxicokinetics of cinnamaldehyde in F344 rats

Yuan, Joan; Dieter, Michael P.; Bucher, John R.; Jameson, C. W.

doi:10.1016/0278-6915(92)90109-x

Cited by 60 publications

(41 citation statements)

References 14 publications

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“…Most absorbed cinnamaldehyde is metabolized rapidly to hippuric acid and excreted in urine (Yuan et al, 1992). Thymol is metabolized to thymol sulphate and thymol glucuronide, and approximately 16% of the thymol dose is secreted as these metabolites in urine (Kohlert et al, 2002).…”

Section: Discussionmentioning

confidence: 99%

Effects of cinnamaldehyde and thymol on cytotoxicity, tight junction barrier resistance, and cyclooxygenase-1 and -2 expression in Caco-2 cells

Putaala¹,

Nurminen²,

Tiihonen³

2017

J. Anim. Feed Sci.

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Section: Discussionmentioning

confidence: 99%

Effects of cinnamaldehyde and thymol on cytotoxicity, tight junction barrier resistance, and cyclooxygenase-1 and -2 expression in Caco-2 cells

Putaala¹,

Nurminen²,

Tiihonen³

2017

J. Anim. Feed Sci.

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“…The method utilizes an animal dose and accounts for differences in body weight and body surface area between species to estimate a human dose. A 250-mg/kg dose of t-CA in rats was used for the estimation; this dose resulted in blood concentrations on the order of 1 mg/ml (% 7.6 mM) in rats (Yuan et al, 1992).…”

Section: Downloaded Frommentioning

confidence: 99%

“…Based on our literature search, the systemic t-CA concentration in human blood following oral administration has yet to be reported. In rats, a dose of 250 mg/kg t-CA generated blood concentrations on the order of %7.6 mM (1 mg/ml) (Yuan et al, 1992). Using these data and the body surface area normalization method (Food and Drug Administration, 2005;Reagan-Shaw et al, 2008), the human equivalent dose to generate a similar blood concentration was estimated to be 40.5 mg/kg or 2430 mg of t-CA per day for a 60-kg human.…”

Section: Percentage Of Control Activitymentioning

confidence: 99%

“…Human pharmacokinetic data are not available for t-CA. The oral doses estimated here (32-320 mg) to achieve blood concentrations of 0.1-1 mM in humans are within the t-CA exposure range when cinnamon powder is used for diabetes, based on a method (Reagan-Shaw et al, 2008) to extrapolate pharmacokinetic data from rats (Yuan et al, 1992) to humans. The estimated range of exposure when cinnamon powder (1-10 g/day) is used for diabetes (Kirkham et al, 2009) is 8-275 mg of t-CA, based on the concentration of t-CA in cinnamon powder (Friedman et al, 2000).…”

Section: Tablementioning

confidence: 99%

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Inactivation of CYP2A6 by the Dietary Phenylpropanoid trans-Cinnamic Aldehyde (Cinnamaldehyde) and Estimation of Interactions with Nicotine and Letrozole

Chan¹,

Oshiro²,

Thomas³

et al. 2016

Drug Metabolism and Disposition

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Human exposure to trans-cinnamic aldehyde [t-CA; cinnamaldehyde; cinnamal; (E)-3-phenylprop-2-enal] is common through diet and through the use of cinnamon powder for diabetes and to provide flavor and scent in commercial products. We evaluated the likelihood of t-CA to influence metabolism by inhibition of P450 enzymes. IC 50 values from recombinant enzymes indicated that an interaction is most probable for CYP2A6 (IC 50 = 6.1 mM). t-CA was 10.5-fold more selective for human CYP2A6 than for CYP2E1; IC 50 values for P450s 1A2, 2B6, 2C9, 2C19, 2D6, and 3A4 were 15.8-fold higher or more. t-CA is a type I ligand for CYP2A6 (K S = 14.9 mM). Inhibition of CYP2A6 by t-CA was metabolism-dependent; inhibition required NADPH and increased with time. Glutathione lessened the extent of inhibition modestly and statistically significantly. The carbon monoxide binding spectrum was dramatically diminished after exposure to NADPH and t-CA, suggesting degradation of the heme or CYP2A6 apoprotein. Using a static model and mechanism-based inhibition parameters (K I = 18.0 mM; k inact = 0.056 minute 21

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“…Our group has previously observed cinnamaldehyde-induced proxidant state (Devaraj et al 1992), glutathione depletion and lipid peroxidation in rat liver (Raveendran et al 1993). An earlier report (Yuan et al 1992) has shown that the bioavailability of cinnamaldehyde administered by the oral route to the rats was low in blood since all of the cinnamaldehyde absorbed must pass through the liver before being distributed to the whole system. The low level of cinnamaldehyde that remained in the blood was retained for a long time.…”

Section: Discussionmentioning

confidence: 99%

Effect of the Food Flavour Cinnamaldehyde on the Antioxidant Status of Rat Kidney

Gowder

Devaraj

2006

Basic Clin Pharma Tox

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Cinnamaldehyde, a food flavour, has a high potential for human consumption in India. In this study, we evaluated the effect of cinnamaldehyde on the antioxidant status of the rat kidney. Rats were given cinnamaldehyde orally by gavage at dose levels of 2.14, 6.96, 22.62 and 73.5 mg/kg body weight/day for the period of 10, 30 and 90 days. The non-enzymatic antioxidants ascorbic acid, a-tocopherol and reduced glutathione were decreased while the antioxidant enzymes, superoxide dismutase, glutathione peroxidase and glutathione-s-transferase were increased. Catalase was decreased and thiobarbituric acid-reactive substances were increased only in the kidney of rats treated with cinnamaldehyde at the dose level of 73.5 mg/kg body weight/day during an exposure period of 90 days and not in the kidney of other cinnamaldehyde-treated rat groups. Thus, cinnamaldehyde has an effect on the antioxidant status of rat kidney and its effect is time-and dose-dependent.

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Toxicokinetics of cinnamaldehyde in F344 rats

Cited by 60 publications

References 14 publications

Effects of cinnamaldehyde and thymol on cytotoxicity, tight junction barrier resistance, and cyclooxygenase-1 and -2 expression in Caco-2 cells

Effects of cinnamaldehyde and thymol on cytotoxicity, tight junction barrier resistance, and cyclooxygenase-1 and -2 expression in Caco-2 cells

Inactivation of CYP2A6 by the Dietary Phenylpropanoid trans-Cinnamic Aldehyde (Cinnamaldehyde) and Estimation of Interactions with Nicotine and Letrozole

Effect of the Food Flavour Cinnamaldehyde on the Antioxidant Status of Rat Kidney

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