Simultaneous quantification of 5 main components of Psoralea corylifolia L. in rats’ plasma by utilizing ultra high pressure liquid chromatography tandem mass spectrometry

Gao, Qianqian; Xu, Zisheng; Zhao, Genhua; Wang, Heng; Weng, Zebin; Pei, Ke; Wu, Li; Cai, Baochang; Chen, Zhipeng; Li, Weidong

doi:10.1016/j.jchromb.2015.12.044

Cited by 25 publications

(12 citation statements)

References 20 publications

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“…Meanwhile, it account for 0.157~0.363% of the dried seed weight . Pharmacokinetics studies indicated that CA could be rapidly absorbed into plasma and brain, and with poor bioavailability (Gao et al, 2016;Yang et al, 2018b), while it could undergo massive glucuronidation and sulfation reactions (Geng et al, 2014;Wang et al, 2015a). However, few researches were reported about the metabolism involving CYP and UGT enzymes.…”

Section: Discussionmentioning

confidence: 99%

“…At present, CA were proved to be absorbed in plasma after intragastric administration of Psoralea corylifolia or Psoralea corylifolia-containing herbal prescriptions (Geng et al, 2014;Wang et al, 2015a). Furthermore, the pharmacokinetics results indicated that the maximal plasma concentration (C max ) of CA were 8.87 ng/mL at a single dose of Psoralea corylifolia extract at 2.0 g/kg (Gao et al, 2016), whereas the C max value was 1.70 ng/mL after oral administration of Psoralea corylifolia extract at 1.2 g/kg (Yang et al, 2018b). Besides, the distribution concentrations of CA at different nuclei varied at one determined time point (ranging from 260.63 to 493.29 ng·h/g), but the overall trends were basically similar to the plasma concentration-time results (Yang et al, 2018b).…”

Section: Introductionmentioning

confidence: 93%

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Metabolism and disposition of corylifol A from Psoralea corylifolia: metabolite mapping, isozyme contribution, species differences and identification of efflux transporters for corylifol A-O-glucuronide in HeLa1A1 cells

Yang

et al. 2020

Xenobiotica

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2020): Metabolism and disposition of corylifol A from Psoralea corylifolia: metabolite mapping, isozyme contribution, species differences, and identification of efflux transporters for corylifol A-O-glucuronide in HeLa1A1 cells, Xenobiotica, Abstract 1. Corylifol A (CA), a phenolic compound from Psoralea corylifolia, possessed several biological properties but poor bioavailability. Here we aimed to investigate the roles of cytochromes P450s (CYPs), UDP-glucuronosyltransferases (UGTs) and efflux transporters in metabolism and disposition of CA. 2. Metabolism of CA were evaluated in HLM, expressed CYPs and UGTs. Chemical inhibitors and shRNA-mediated gene siliencing of multidrug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP) were performed to assess the roles of transporters in CA disposition. 3. Three oxidated metabolites (M1-M3) and two glucuronides (M4-M5) were detected. The intrinsic clearances (CL int ) values of M1 and M4 in HLM were 48.10 and 184.03 μL/min/mg, respectively. Additionally, CYP1A1, 2C8 and 2C19 were identified as main contributors with CL int values of 13.01~49.36 μL/min/mg, while UGT1A1, 1A7, 1A8 and 1A9 were with CL int values ranging form 85.01 to 284.07 μL/min/mg. Furthermore, activity correlation analysis proved CYP2C8, UGT1A1 and 1A9 were main active hepatic isozymes. Besides, rats and monkeys were appropriate model animals. Moreover, dipyridamole and MK571 both could significantly inhibit M4 efflux. Gene silencing results also indicated MRP4 and BCRP were major contributors in HeLa1A1 cells. 4. Taken together, CYPs, UGTs, MRP4 and BCRP were important determinants of CA A c c e p t e d M a n u s c r i p t pharmacokinetics.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 93%

Metabolism and disposition of corylifol A from Psoralea corylifolia: metabolite mapping, isozyme contribution, species differences and identification of efflux transporters for corylifol A-O-glucuronide in HeLa1A1 cells

Yang

et al. 2020

Xenobiotica

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“…Actually, its maximum plasma concentration is very low and less than 10 ng/ml (about 30 nM). [1,12,13] In addition, it is shown that bavachin could be distributed almost evenly to the brain cerebral nuclei after quickly absorbed into rat plasma (t max = 1 h). [13] Poor plasma exposure entails a huge obstacle to exert the pharmacological action, because the plasma C max values are significantly less than the EC 50 values of bavachin on oestrogen-like activity.…”

Section: Introductionmentioning

confidence: 99%

Characterization of metabolic activity, isozyme contribution and species differences of bavachin, and identification of efflux transporters for bavachin-O-glucuronide in HeLa1A1 cells

Yang

et al. 2020

Journal of Pharmacy and Pharmacology

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Objectives Bavachin is a bioactive natural flavonoid with oestrogen-like activity. Here, we aimed to investigate its metabolic and disposal fates involving in CYPs, UGTs and efflux transporters. Methods Phase I metabolism and glucuronidation were performed by human liver microsomes (HLM). Reaction phenotyping and activity correlation analysis were performed to identify the main CYP and UGT isozymes. Chemical inhibition and gene knock-down approaches were employed to explore the function of BCRP and MRPs. Key findings Five phase I metabolites (M1-M5) and three glucuronides (G1-G3) were identified. The CL int values for M4 and G1 by HLM were 127.99 and 1159.07 μl/min per mg, respectively. Reaction phenotyping results suggested CYP1A1 (208.85 μl/min per mg) and CYP2C9 (107.51 μl/min per mg), and UGT1A1 (697.19 μl/min per mg), UGT1A7 (535.78 μl/min per mg), UGT1A8 (247.72 μl/min per mg) and UGT1A9 (783.68 μl/min per mg) all participated in the metabolism of bavachin. In addition, activity correlation analysis also supported the results above. Furthermore, the metabolism exhibited marked species differences, and rabbits were the appropriate model animals. Moreover, MRP4 was identified as the main contributor based on chemical inhibition and gene silencing approaches. Conclusions CYP1A1 and CYP2C9, UGT1A1, UGT1A7, UGT1A8 and UGT1A9, and MRP4 all played important roles in the metabolism and disposition of bavachin.

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“…Meanwhile, simultaneous quantification of multiple effective components in P. corylifolia L. has been performed by HPLC (Qiao et al, ) and UPLC (Wang, Yao, et al, ; Wang, Lv, et al, ). Gao et al () developed a rapid and accurate UPLC/MS/MS method for simultaneous determination of five main flavonoid components in rat plasma. Capillary electrophoresis coupled with mass spectrometric detection (CE‐MS) may be used for the determination of isomeric compounds in Psoraleae Fructus as well for its high speed, simplicity and low cost (Zhang and Chen, ), but the sensitivity of CE is relatively poor and the repeatability of separation may be affected by electrodialysis.…”

Section: Introductionmentioning

confidence: 99%

Qualitative analysis of Psoraleae Fructus by HPLC‐DAD/TOF‐MS fingerprint and quantitative analysis of multiple components by single marker

Luan

Shen

Liu

et al. 2017

Biomedical Chromatography

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A variety of bioactive substances may account for the recognized efficacy and wide clinical application of Psoraleae Fructus in China. A high-performance liquid chromatography-diode array detector (HPLC-DAD) fingerprint method was developed to present the comprehensive phytochemical profile of the crude drug. Thirteen major compounds were separated and identified by HPLC coupled with time-of-flight mass spectrometry (HPLC/TOF-MS), namely psoralenoside (PO), isopsoralenoside (IPO), psoralen (PS), isopsoralen (IPS), neobavaisoflavone (NBF), bavachin (BC), corylin (CN), bavachromene (BCM), psoralidin (PD), isobavachalcone (IBC), bacachinin (BCN), corylifol A (CA) and bakuchiol (BK). Then quantitative analysis of multiple components by single marker (QAMS) was applied in content determination of PO, IPO, PS, IPS, BC, IBC, BCN, CA and BK, with NBF as the internal standard. The calculation results indicated no significant difference from the traditional external standard method (p > 0.05, RSD < 2.62%), suggesting that QAMS is a reliable and convenient method for content determination of multiple chemical compositions, especially when there is a shortage of reference substances. In conclusion, simultaneous qualitative and quantitative analysis of Psoraleae Fructus may be fulfilled through the newly proposed method of QAMS combined with HPLC-DAD/TOF-MS fingerprint.

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Simultaneous quantification of 5 main components of Psoralea corylifolia L. in rats’ plasma by utilizing ultra high pressure liquid chromatography tandem mass spectrometry

Cited by 25 publications

References 20 publications

Metabolism and disposition of corylifol A from Psoralea corylifolia: metabolite mapping, isozyme contribution, species differences and identification of efflux transporters for corylifol A-O-glucuronide in HeLa1A1 cells

Metabolism and disposition of corylifol A from Psoralea corylifolia: metabolite mapping, isozyme contribution, species differences and identification of efflux transporters for corylifol A-O-glucuronide in HeLa1A1 cells

Characterization of metabolic activity, isozyme contribution and species differences of bavachin, and identification of efflux transporters for bavachin-O-glucuronide in HeLa1A1 cells

Qualitative analysis of Psoraleae Fructus by HPLC‐DAD/TOF‐MS fingerprint and quantitative analysis of multiple components by single marker

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