Displacement of Bilirubin from Albumin in Plasma from Jaundiced Newborns. An <i>In Vitro</i> Study of Purified Chinese Herbal Constituents and Sulfisoxazole

Soligard, H; Bratlid, Dag; Cao, Chunyu; Liang, Aihua; Nilsen, Odd G.

doi:10.1002/ptr.3402

Cited by 6 publications

(2 citation statements)

References 22 publications

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“…It was reported that about 80% of the world’s population use herbs to cover their need for drugs [2]. The reason may be that herbal therapeutic efficacy is mild and broad, and the incidence of adverse reactions is relatively low in comparison with synthetic drugs [3].…”

Section: Introductionmentioning

confidence: 99%

Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats

Gao

Liu

et al. 2014

PLoS ONE

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Baicalin has been used as mainly bioactive constituent of about 100 kinds of traditional Chinese medicines in Chinese pharmacopoeia. The effect of baicalin on cytochrome P450 should be paid more attention because baicalin was used widely. The aim of this study was to investigate whether baicalin could inhibit CYP1A2 in pooled human liver microsomes (HLMs) and in rats in vivo and the gene polymorphisms could affect inter-individual variation in IC50 in 28 human livers. Phenacetin was used as probe of CYP1A2. Kinetic parameter of CYP1A2 and IC50 of baicalin on CYP1A2 to each sample were measured and the common CYP1A2 polymorphisms (−3860G>A and −163C>A) were genotyped. The results showed that baicalin exhibited a mixed-type inhibition in pooled HLMs, with a Ki value of 25.4 µM. There was substantial variation in Km, Vmax, CLint of CYP1A2 and IC50 of baicalin on CYP1A2 (3∼10-fold). The range was from 26.6 to 114.8 µM for Km, from 333 to 1330 pmol·min−1·mg−1protein for Vmax and from 3.8 to 45.3 µL·min−1·mg−1 protein for CLint in HLMs (n = 28). The Mean (range) value of IC50 in 28 HLMs was 36.3 (18.9 to 56.1) µM. The genotypes of −3860G>A and −163C>A had no significant effect on the inhibition of baicalin on CYP1A2. The animal experiment results showed that baicalin (450 mg/kg, i.v.) significantly decreased the Cmax and CL of phenacetin, and increased C60 min, t1/2, Vd and AUC (P<0.05). There were significant correlations between percentage of control in C60 min, t1/2, CL, AUC of phenacetin and Cmax of baicalin in 11 rats (P<0.05). Protein binding experiments in vitro showed that baicalin (0–2000 mg/L) increased the unbound phenacetin from 14.5% to 28.3%. In conclusion, baicalin can inhibit the activity of CYP1A2 in HLMs and exhibit large inter-individual variation that has no relationship with gene polymorphism. Baicalin can change the pharmacokinetics of phenacetin in rats.

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Section: Introductionmentioning

confidence: 99%

Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats

Gao

Liu

et al. 2014

PLoS ONE

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“…Displacement binding experiments also can be a guidance to reasonably predict clinical toxic and side effect of active herbal components. Soligard et al used purified Chinese herbal constituents and sulfisoxazole to displace the bilirubin from HSA from jaundiced newborns [ 147 ]. The positive inhibitor control sulfisoxazole increased plasma unbound fraction by an average of 60%, while, no displacement phenomena that neferine, sinomenine, tetrahydropalmitine and notoginsenoside showed up.…”

Section: Methods To Investigate the Interaction Between Active Herbalmentioning

confidence: 99%

Study on the interaction between active components from traditional Chinese medicine and plasma proteins

Jiao

Wang

Jiang

et al. 2018

Chemistry Central Journal

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Traditional Chinese medicine (TCM), as a unique form of natural medicine, has been used in Chinese traditional therapeutic systems over two thousand years. Active components in Chinese herbal medicine are the material basis for the prevention and treatment of diseases. Research on drug-protein binding is one of the important contents in the study of early stage clinical pharmacokinetics of drugs. Plasma protein binding study has far-reaching influence on the pharmacokinetics and pharmacodynamics of drugs and helps to understand the basic rule of drug effects. It is important to study the binding characteristics of the active components in Chinese herbal medicine with plasma proteins for the medical science and modernization of TCM. This review summarizes the common analytical methods which are used to study the active herbal components-protein binding and gives the examples to illustrate their application. Rules and influence factors of the binding between different types of active herbal components and plasma proteins are summarized in the end. Finally, a suggestion on choosing the suitable technique for different types of active herbal components is provided, and the prospect of the drug-protein binding used in the area of TCM research is also discussed.

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Inhibition of Rat CYP1A2 and CYP2C11 by Honokiol, a Component of Traditional Chinese Medicine

Sun

et al. 2019

Eur J Drug Metab Pharmacokinet

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Displacement of Bilirubin from Albumin in Plasma from Jaundiced Newborns. An In Vitro Study of Purified Chinese Herbal Constituents and Sulfisoxazole

Cited by 6 publications

References 22 publications

Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats

Inhibition of Baicalin on Metabolism of Phenacetin, a Probe of CYP1A2, in Human Liver Microsomes and in Rats

Study on the interaction between active components from traditional Chinese medicine and plasma proteins

Inhibition of Rat CYP1A2 and CYP2C11 by Honokiol, a Component of Traditional Chinese Medicine

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