Pharmacokinetics of S-Allyl-l-cysteine in Rats Is Characterized by High Oral Absorption and Extensive Renal Reabsorption

The Journal of Nutrition
Hirotaka AmanoKenji Itoh

Abstract

S-Allylcysteine (SAC) is a key component of aged garlic extract, one of many garlic products. However, information on its pharmacokinetics has been scant except for data from a few animal studies. We designed this study to determine the overall pharmacokinetics of SAC in rats. After oral or intravenous administration of SAC to rats at a dose of 5 mg/kg, the plasma concentration-time profile of SAC and its metabolites, as well as the amounts excreted in bile and urine, were analyzed by using liquid chromatography tandem mass spectrometry. After oral administration, SAC was well absorbed with a bioavailability of 98%. Two major metabolites of SAC, N-acetyl-S-allylcysteine (NAc-SAC) and N-acetyl-S-allylcysteine sulfoxide (NAc-SACS), were detected in plasma, but their concentrations were markedly lower than those of SAC. SAC was metabolized to a limited extent, but most of the orally absorbed SAC was excreted into urine in the form of its N-acetylated metabolites. The amounts of SAC, NAc-SAC, and NAc-SACS excreted in urine over 24 h were 2.9%, 80%, and 11% of the orally administered SAC, respectively. The very low renal clearance (0.016 L ⋅ h(-1) ⋅ kg(-1)) of SAC indicated that it undergoes extensive renal reabsorption. These resul...Continue Reading

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Citations

Oct 22, 2016·Journal of Natural Medicines·Naoaki Morihara, Atsuko Hino
Jan 13, 2017·Current Pharmaceutical Design·Spyridon PetropoulosGeorgia Ntatsi
Feb 6, 2020·Experimental and Therapeutic Medicine·Yasuhiro Kosuge
Jul 30, 2019·Journal of Food Biochemistry·Cheng ZhangXichun Peng
Dec 11, 2020·Seminars in Cancer Biology·Danielle De GreefAnupam Bishayee
Jul 11, 2020·Biochimica Et Biophysica Acta. General Subjects·Prachi GuptaAshwani Mittal

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