Pharmacokinetics of Liquiritigenin in Mice, Rats, Rabbits, and Dogs, and Animal Scale-Up

Kang, Hee Eun; Jung, Hye Young; Cho, Yu K.; Kim, So H.; Sohn, Se I.; Baek, Seung Ryel; Lee, Myung G.

doi:10.1002/jps.21702

Cited by 31 publications

(30 citation statements)

References 22 publications

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“…utilizing intravenous dosing of liquiritigenin 20 mg/kg reported approximate plasma half-lives of 5-8 minutes, clearances of 50-70 mL/min/kg, V ss 240-190 mL/kg, and AUC of 290-410 μg.min/mL. Data from the present study parallel these results with respect to AUC (280-385 μg.min/mL) and clearance (30-50 mL/min/kg) but also demonstrated a comparatively greater half-life (0.25-0.43 h) (2526). The very short half-life of liquiritigenin reported by Kang, et al was calculated utilizing plasma samples only, which may underestimate the actual half-life of liquiritigenin and also emphasizes the importance of utilizing urinary data to calculate pharmacokinetic parameters of liquiritigenin as well as similar flavonoids (2526).…”

Section: Discussionsupporting

confidence: 84%

“…The achiral pharmacokinetics of liquiritigenin, and its corresponding glycosides have been reported in the literature (17). Differences in the disposition of an individual enantiomer may result in significant differences in their health benefits or toxic effects in humans (18192021222324252627). The chiral pharmacokinetics of liquiritigenin have only been preliminarily evaluated by our laboratory and one other group.…”

Section: Introductionmentioning

confidence: 99%

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Stereospecific pharmacokinetic characterization of liquiritigenin in the rat

et al. 2017

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Liquiritigenin is a chiral flavonoid present in licorice and other medicinal plants. The nature of its biological fate with respect to the individual enantiomers has not been examined. In this study, we characterize, for the first time, the stereoselective pharmacokinetics of liquiritigenin. Liquiritigenin was intravenously (20 mg/kg) and orally (50 mg/kg) administered to male Sprague-Dawley rats (n = 4 per route of administration). Concentrations in serum and urine were characterized via stereospecific reversed-phase, isocratic HPLC method with UV detection. Serum concentrations were quantified but rapidly fell to undetectable levels. S-liquiritigenin showed a short half-life (0.25-0.54 h), while a better estimation of half-life (26-77 h) and other pharmacokinetic parameters was observed using urinary data. The flavonoid is predominantly excreted via non-renal routes (fe values of 0.16-3.46 %), and undergoes rapid and extensive phase II metabolism. Chiral differences in the chemical structure of the compound result in some pharmacokinetic differences. Serum concentrations rapidly declined, making modeling difficult. S-liquiritigenin showed an increased urinary half-life.

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Section: Discussionsupporting

confidence: 84%

Section: Introductionmentioning

confidence: 99%

Stereospecific pharmacokinetic characterization of liquiritigenin in the rat

et al. 2017

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“…Third, we have found that liquiritigenin does not induce the proliferation of MCF-7 or T47D breast cancer cells (unpublished observations), which is consistent with the results of other studies (Gustafsson et al, 2003). Finally, pharmacokinetics data has demonstrated that liquiritigenin is absorbed well by the intestine amongst rats, with an in vitro blood-brain barrier penetration rate of (29.7±6.8)% within 90 min, similar to that of chloramphenicol (34.0±4.9)%, a known blood-brain barrier and highly penetrative drug (Kupfer et al, 2008;Lu et al, 2008;Kang et al, 2009). Taken together, these observations suggest that liquiritigenin may be a potentially effective therapy for AD.…”

Section: Introductionsupporting

confidence: 82%

Liquiritigenin Attenuates Alzheimer’s-Like Neuropathology in an Amyloid Protein Precursor Transgenic Mouse Model and the Underlying Mechanisms

Liu¹,

Jin²,

Zou³

et al. 2011

Drug Development - A Case Study Based Insight Into Modern Strategies

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“…Institute of Cancer Research (ICR) male mice (7-8 weeks old, weighing 22-34 g) were purchased from Charles River Company Korea (Seoul, South Korea). The procedures used for housing and handling of mice were similar to a method reported previously (Kang et al, 2009).…”

Section: Animalsmentioning

confidence: 99%

Pharmacokinetics of macrolactin A and 7-O-succinyl macrolactin A in mice

Jung¹,

Kim²,

Kwon³

et al. 2013

Xenobiotica

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1. As promising anti-macular degeneration and/or anti-tumour agents, a better understanding of the pharmacokinetics of macrolactin A (MA) and 7-O-succinyl macrolactin A (SMA) is essential. Thus, we evaluated the pharmacokinetics of MA and SMA after intravenous, oral, or intraperitoneal administration of each drug to mice. 2. Both hepatic and extra-hepatic extractions of MA were expected based on the rapid total body clearance (CL) of MA. MA also showed a large steady-state volume of distribution (Vss) in mice. A relatively slower CL (by 54.1%) and smaller Vss (by 85.8%) were observed for SMA than for MA. In accordance with the larger Vss values of MA than of SMA, the mouse tissues studied had good affinity to MA but less affinity to SMA. 3. Both MA and SMA had an extremely low oral extent of absolute bioavailability (F). This could have been a result of the instability of MA and SMA in the gastrointestinal tract, supported by their unstable property in acidic buffer. Gastrointestinal and/or hepatic first-pass extraction of MA and SMA may be other reasons. 4. The pharmacokinetic profiles of both MA and SMA were much improved (greater AUC and F values) following intraperitoneal administration than following oral administration due to avoidance of acidic degradation and/or gastrointestinal first-pass extraction.

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Pharmacokinetics of Liquiritigenin in Mice, Rats, Rabbits, and Dogs, and Animal Scale-Up

Cited by 31 publications

References 22 publications

Stereospecific pharmacokinetic characterization of liquiritigenin in the rat

Stereospecific pharmacokinetic characterization of liquiritigenin in the rat

Liquiritigenin Attenuates Alzheimer’s-Like Neuropathology in an Amyloid Protein Precursor Transgenic Mouse Model and the Underlying Mechanisms

Pharmacokinetics of macrolactin A and 7-O-succinyl macrolactin A in mice

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