Absorption, liver first-pass effect, pharmacokinetics and tissue distribution of calycosin-7- O -ß- d -glucopyranoside (C7G) and its major active metabolite, calycosin, following oral administration of C7G in rats by LC–MS/MS

Tian, Xiaoting; Chen, Shuoji; Zhang, Yuanyuan; Xu, Zhou; Liu, Huan; Hu, Pei; Chen, Zhenyuan; Li, Zhixiong; Huang, Chenggang

doi:10.1016/j.jpba.2017.10.027

Cited by 11 publications

(10 citation statements)

References 10 publications

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“…Studies have shown that the drug concentration of CA in tissues is higher than that of systemic plasma, and the drug concentration in liver, kidney and heart is 212.1, 30.5 and 4.7 times that of systemic plasma. 29 The results of this experiment showed that the drug concentration of CA in normal rat brain tissue is about 2.54 times that in blood, while the drug concentration of CA in brain tissue of model rats is about 4.98 times that in blood, suggesting that CA can be used in the treatment of brain diseases, and cerebral ischemia-reperfusion injury can increase the distribution of CA in brain tissue.…”

Section: Resultsmentioning

confidence: 84%

“…As can be seen from Tables 5 and 6 , the rats in the model group demonstrated lower levels of C max blood , AUC 0-t blood , AUC 0-inf blood , and MRT brain and higher levels of CL blood and C max brain of CG compared to control group following the administration of HGWD, compared to the rats in the normal group, the C max blood was decreased, V blood and V brain of the CA were increased in model rats following the administration of HGWD. According to literature reports, 29 after intragastric administration of CA suspension (administration dose of 120 mg/kg), it was found that the plasma concentration–time curves of CA was double-peaked in the portal vein and systemic plasma, and the first peak time (T max ) appeared at 0.5 h or 1 h, the second T max appears at 4 h, and in this experiment, there is also a double peak in the plasma concentration–time curves of CA of the blood and brain tissues, the first T max appears around at 25 min, and the second T max appeared at about 55 min, indicating that the first T max of CA is due to the absorption of CA contained in the drug, and the second T max may be the formation of CA after the deglycosylation of CG in the intestine and intestinal cells. Studies have shown that the drug concentration of CA in tissues is higher than that of systemic plasma, and the drug concentration in liver, kidney and heart is 212.1, 30.5 and 4.7 times that of systemic plasma.…”

Section: Resultsmentioning

confidence: 99%

Section: Pharmacokinetic Profilesmentioning

confidence: 87%

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<p>Pharmacokinetic Analysis of Huangqi Guizhi Wuwu Decoction on Blood and Brain Tissue in Rats with Normal and Cerebral Ischemia-Reperfusion Injury by Microdialysis with HPLC-MS/MS</p>

Zheng¹,

Shen²,

He³

et al. 2020

DDDT

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The aim of our research was to analyze and compare the pharmacokinetics of paeoniflorin, calycosin, calycosin-7-o-β-d-6-glucoside, and 6-gingerol in the blood and brain tissue of normal and cerebral ischemia-reperfusion injury rats by HPLC-MS/MS method. Methods: The blood and brain tissue samples of normal and middle cerebral artery occlusion (MCAO) rats were compared. The blood and brain tissue samples were collected by using microdialysis technique. The concentrations of paeoniflorin, calycosin, calycosin-7-o-β-d-6-glucoside, and 6-gingerol in blood and brain tissues were determined by the HPLC-MS/MS internal standard method. Results: Compared with the normal group, the model group after the administration of the Huangqi Guizhi Wuwu Decoction showed that C max blood , AUC 0-t blood , and AUC 0-inf blood of paeoniflorin were increased, CL blood , t 1/2 brain , and V brain of paeoniflorin were decreased; C maxblood , AUC 0-tblood , AUC 0-infblood , and average residence time (MRT brain) of calycosin-7-o-β-d-6-glucoside were decreased and the CL blood and C max brain of calycosin-7-o-βd-6-glucoside were increased; C max blood of calycosin was decreased, V blood and V brain of calycosin were increased; C max blood , AUC 0-t blood , AUC 0-inf blood , and MRT brain of 6-gingerol were decreased, CL blood of 6-gingerol was increased. Conclusion: This method is simple, rapid, and sensitive. It is suitable for the pharmacokinetic study of Huangqi Guizhi Wuwu Decoction in the blood and brain tissue of rats. Cerebral ischemia-reperfusion injury increased the content of paeoniflorin, calycosin, calycosin-7-o-β-d-6-glucoside, and 6-gingerol in the blood, affecting the clearance rate of paeoniflorin in the brain, the detention time of calycosin-7-o-β-d-6-glucoside and the 6-gingerol in the brain. In normal and cerebral ischemia-reperfusion rats, the content of paeoniflorin and 6-gingerol in the blood was higher than that in brain tissue, while the content of calycosin, calycosin-7-o-β-d-6-glucoside in the brain tissue was higher than that in blood, suggesting that calycosin and calycosin-7-o-β-d-6-glucoside have brain targeting properties.

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Section: Resultsmentioning

confidence: 84%

Section: Resultsmentioning

confidence: 99%

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<p>Pharmacokinetic Analysis of Huangqi Guizhi Wuwu Decoction on Blood and Brain Tissue in Rats with Normal and Cerebral Ischemia-Reperfusion Injury by Microdialysis with HPLC-MS/MS</p>

Zheng¹,

Shen²,

He³

et al. 2020

DDDT

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show abstract

“…In addition, calycosin was not detected in rat plasma, probably resulting from its strong phase II metabolism in liver. It was often found that high levels of phase II metabolites circulated in blood with trace amounts of aglycone in the pharmacokinetic profiles of isoflavones (Bai, Qu, Lu, Kano, & Yuan, ; Hosoda, Furuta, & Ishii, ; Qu et al, ; Tian et al, ; Wang, Gong, et al, ; Yuan et al, ; Zhang, Qi, Xu, Kano, & Yuan, ). Considerably different pharmacokinetics of CAG and calycosin have been published in the literature after rats were treated with TCM consisting of Huangqi (Liu et al, ; Liu et al, ; Shaw et al, ; Shi et al, ; Tao, Huang, Yang, Li, & Cai, ; Zeng et al, ; Zhang, Yang, Lin, & Hu, ).…”

Section: Resultsmentioning

confidence: 99%

Simultaneous determination of major components of Huangqi–Honghua extract in rat plasma using LC–MS/MS and application to a pharmacokinetic study

Wang

Qiao

et al. 2019

Biomedical Chromatography

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A sensitive and reliable LC-MS/MS method was developed and validated for simultaneous quantification of the major components of Huangqi-Honghua extact in rat plasma, including hydroxysafflor yellow A (HSYA), astragaloside IV (ASIV), calycosin-calycosin-3′-O-sulfate (C-3′-S). After extraction by protein precipitation with acetonitrile and methanol from plasma, the analytes were separated on a Hypersil BDS C 18 column by gradient elution with acetonitrile and 5 mM ammonium acetate. The detection was carried out on a triple quadrupole tandem mass spectrometer equipped with electrospray ionization source switched between negative and positive modes.HSYA was monitored in negative ionization mode from 0 to 4.9 min, and ASIV, CAG, calycosin, C-3′-G and C-3′-S were determined in positive ionization mode from 4.9 to 10 min. The lower limits of quantification of the analytes were 6.25 ng/mL for HSYA, 0.781 ng/mL for CAG and 1.56 ng/mL for ASIV and calycosin. The intra-and inter-assay precision (RSD) values were within 13.43%, and accuracy (RE) ranged from −8.75 to 9.92%. The validated method was then applied to the pharmacokinetic study of HSYA, ASIV, CAG, calycosin, C-3′-G and C-3′-S in rat after an oral administration of Huangqi-Honghua extract.

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“…This indicates that calycosin-7-O- β -glucoside may directly pass through the cell membrane in a prototype form without hydrolysis [ 69 ]. Using Caco-2 cells to study the absorption and transport characteristics of calycosin and its glucoside, it was found that calycosin and calycosin-7-O- β -glucoside are mainly absorbed in the form of passive diffusion, and the absorption process will not be affected by inhibitors of MATEs such as P-gp and MRP2 [ 69 , 70 ]. Calycosin can be metabolized in human liver microsomes to generate two glucuronides.…”

Section: Pharmacokinetics Of Calycosinmentioning

confidence: 99%

Pharmaceutical Values of Calycosin: One Type of Flavonoid Isolated from Astragalus

Gong

Zheng

Yang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Astragalus is a popular Materia Medica in China, and it could be applied in the treatment of various diseases. It contains a variety of chemically active ingredients, such as saponins, flavonoids, and polysaccharides. Plant-derived bioactive chemicals are considered natural, safe, and beneficial. Among the infinite plant-identified and isolated molecules, flavonoids have been reported to have positive effects on human health. Calycosin is the most important active flavonoid substance identified predominantly within this medicinal plant. In recent years, calycosin has been reported to have anticancer, antioxidative, immune-modulatory, and estrogenic-like properties. This review collected recent relevant literatures on calycosin and summarized its potential pharmaceutical properties and working mechanism involved, which provided solid basis for future clinical research.

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Absorption, liver first-pass effect, pharmacokinetics and tissue distribution of calycosin-7- O -ß- d -glucopyranoside (C7G) and its major active metabolite, calycosin, following oral administration of C7G in rats by LC–MS/MS

Cited by 11 publications

References 10 publications

<p>Pharmacokinetic Analysis of Huangqi Guizhi Wuwu Decoction on Blood and Brain Tissue in Rats with Normal and Cerebral Ischemia-Reperfusion Injury by Microdialysis with HPLC-MS/MS</p>

<p>Pharmacokinetic Analysis of Huangqi Guizhi Wuwu Decoction on Blood and Brain Tissue in Rats with Normal and Cerebral Ischemia-Reperfusion Injury by Microdialysis with HPLC-MS/MS</p>

Simultaneous determination of major components of Huangqi–Honghua extract in rat plasma using LC–MS/MS and application to a pharmacokinetic study

Pharmaceutical Values of Calycosin: One Type of Flavonoid Isolated from Astragalus

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