Plasma pharmacokinetics and tissue distribution of arctiin and its main metabolite in rats by HPLC-UV and LC-MS

He, Fan; Dou, Deqiang; Sun, Yu; Zhu, Lin; Xiao, Hongbin; Kang, Ting-Guo

doi:10.1055/s-0032-1328294

Cited by 12 publications

(17 citation statements)

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“…Compound 29 generated identical [M + Na] + ions at m / z 557.1993, and the positive MS/MS spectrum gave the fragment ion of m / z 395 [M + Na − glc] + , except that the fragment ion of m / z 137 was also exhibited. According to comparison of the fragmentation pathway and main fragment ions of lignanolides with the literature data (He et al, 2012; Szokol‐Borsodi, Sólyomváry, Molnár‐Perl, & Boldizsár, 2012), compounds 20 and 29 were tentatively assigned as arctigenin and arctiin, respectively. The proposed fragmentation pathways of forsythin and magnolin were described as shown in Figure 4a.…”

Section: Resultsmentioning

confidence: 87%

Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSⁿ and HPLC–UV technique

Yang

Gao

Liu

et al. 2020

Biomedical Chromatography

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Qu‐feng‐sheng‐shi Granules (QFSSG), a common prescription for the treatment of chronic inflammation and allergic rhinitis, is widely used in the clinic as a traditional Chinese medicine. Chemical analysis and quality control studies of this formulation are relatively limited compared with pharmacological studies. In this study, a high‐performance liquid chromatography coupled with electrospray ionization quadrupole time‐of‐flight tandem mass spectrometry (HPLC–ESI–Q/TOF–MSn) was used to identify the components in this prescription. Next, to quantify six major compounds, an HPLC–UV method was developed and validated. The results showed that 53 compounds were identified based on the MSn data, retention time and previous reports, including 17 coumarins, 14 lignans, 10 chromones, nine phenylethanoid glycosides and three other compounds, were identified or tentatively assigned. Contents of six major bioactive compounds (4′‐O‐β‐glucopyranosyl‐5‐O‐methylvisamminol, Prim‐O‐glucosylcimifugin, forsythin, magnolin, imperatorin, isoimperatorin) could be determined by HPLC simultaneously. In addition, the potential anti‐inflammatory activity of six major compounds was determined too, and we found that four compounds (4′‐O‐β‐glucopyranosyl‐5‐O‐methylvisamminol, Prim‐O‐glucosylcimifugin, forsythin, imperatorin) have a potent nitric oxide inhibitory effect. In conclusion, this work provided comprehensive information on the quality control of QFSSG and evaluated the potential biological activity of the main components in QFSSG, which can contribute to understanding and using it more scientifically.

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Section: Resultsmentioning

confidence: 87%

Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSⁿ and HPLC–UV technique

Yang

Gao

Liu

et al. 2020

Biomedical Chromatography

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“…Arctium lappa has been widely used in traditional Chinese medicine to treat inflammation‐related diseases such as cough, cold, and swelling of throat . In the plant, Arc is present as glucoside (arctiin) and Arc is released during the digestive process . Both have been detected in rat plasma after oral administration of arctiin and distributed widely in different tissues including small intestine, stomach, lung, and kidney .…”

Section: Introductionmentioning

confidence: 99%

“…In the plant, Arc is present as glucoside (arctiin) and Arc is released during the digestive process . Both have been detected in rat plasma after oral administration of arctiin and distributed widely in different tissues including small intestine, stomach, lung, and kidney . The anticarcinogenic effect of Arc and arctiin has been demonstrated in several cancers including prostate cancer, associated with the induction of apoptosis, inhibition of proliferation, and modulations of multiple signaling pathways particularly the PI3K/Akt pathway .…”

Section: Introductionmentioning

confidence: 99%

Arctigenin in combination with quercetin synergistically enhances the antiproliferative effect in prostate cancer cells

Wang

Phan

Gordon

et al. 2014

Molecular Nutrition Food Res

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Scope We investigated whether a combination of two promising chemopreventive agents arctigenin and quercetin increases the anti-carcinogenic potency at lower concentrations than necessary when used individually in prostate cancer. Methods and results Androgen-dependent LAPC-4 and LNCaP prostate cancer cells were treated with low doses of arctigenin and quercetin alone or in combination for 48h. The anti-proliferative activity of arctigenin was 10-20 fold stronger than quercetin in both cell lines. Their combination synergistically enhanced the anti-proliferative effect, with a stronger effect in androgen receptor (AR) wild-type LAPC-4 cells than in AR mutated LNCaP cells. Arctigenin demonstrated a strong ability to inhibit AR protein expression in LAPC-4 cells. The combination treatment significantly inhibited both AR and PI3K/Akt pathways compared to control. A protein array analysis revealed that the mixture targets multiple pathways particularly in LAPC-4 cells including Stat3 pathway. The mixture significantly inhibited the expression of several oncogenic microRNAs including miR-21, miR-19b, and miR-148a compared to control. The mixture also enhanced the inhibition of cell migration in both cell lines compared to individual compounds tested. Conclusion The combination of arctigenin and quercetin, that target similar pathways, at low physiological doses, provides a novel regimen with enhanced chemoprevention in prostate cancer.

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“…K i values were calculated to be 16.0 and 76.7 μM for the inhibition of arctiin and arctigenin toward UGT2B15, respectively. After oral administration of arctiin (100 mg/kg), the maximum plasma concentration of arctiin and arctigenin was determined to be 2.5 mg/L (4.68 μM) and 0.2 mg/L (0.54 μM) (He et al , ). Using this value, the [I] / K i values were calculated to be 0.3 and 0.007 for arctiin and arctigenin, respectively.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of UDP-Glucuronosyltransferase (UGT) Isoforms by Arctiin and Arctigenin

et al. 2016

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Arctiin is the major pharmacological ingredient of Fructus Arctii, and arctigenin is the metabolite of arctiin formed via the catalysis of human intestinal bacteria. The present study aims to investigate the inhibition profile of arctiin and arctigenin on important phase II drug-metabolizing enzymes UDP-glucuronosyltransferases (UGTs), indicating the possible herb-drug interaction. In vitro screening experiment showed that 100 μM of arctiin and arctigenin inhibited the activity of UGT1A3, 1A9, 2B7, and 2B15. Homology modeling-based in silico docking of arctiin and arctigenin into the activity cavity of UGT2B15 showed that hydrogen bonds and hydrophobic interactions contributed to the strong binding free energy of arctiin (-8.14 kcal/mol) and arctigenin (-8.43 kcal/mol) with UGT2B15. Inhibition kinetics study showed that arctiin and arctigenin exerted competitive and noncompetitive inhibition toward UGT2B15, respectively. The inhibition kinetic parameters (Ki ) were calculated to be 16.0 and 76.7 μM for the inhibition of UGT2B15 by arctiin and arctigenin, respectively. Based on the plasma concentration of arctiin and arctigenin after administration of 100 mg/kg of arctiin, the [I]/Ki values were calculated to be 0.3 and 0.007 for arctiin and arctigenin, respectively. Based on the inhibition evaluation standard ([I]/Ki < 0.1, low possibility; 0.1 < [I]/Ki < 1, medium possibility; [I]/Ki > 1, high possibility), arctiin might induce drug-drug interaction with medium possibility. Based on these results, clinical monitoring the utilization of Fructus Arctii is very important and necessary. Copyright © 2016 John Wiley & Sons, Ltd.

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Plasma pharmacokinetics and tissue distribution of arctiin and its main metabolite in rats by HPLC-UV and LC-MS

Cited by 12 publications

References 0 publications

Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSⁿ and HPLC–UV technique

Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSⁿ and HPLC–UV technique

Arctigenin in combination with quercetin synergistically enhances the antiproliferative effect in prostate cancer cells

Inhibition of UDP-Glucuronosyltransferase (UGT) Isoforms by Arctiin and Arctigenin

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Plasma pharmacokinetics and tissue distribution of arctiin and its main metabolite in rats by HPLC-UV and LC-MS

Cited by 12 publications

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Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSn and HPLC–UV technique

Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSn and HPLC–UV technique

Arctigenin in combination with quercetin synergistically enhances the antiproliferative effect in prostate cancer cells

Inhibition of UDP-Glucuronosyltransferase (UGT) Isoforms by Arctiin and Arctigenin

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Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSⁿ and HPLC–UV technique

Analysis of chemical constituents and six compounds in Qu‐feng‐sheng‐shi Granules via HPLC–ESI–Q/TOF–MSⁿ and HPLC–UV technique