Oral pharmacokinetics of baicalin, wogonoside, oroxylin A 7- O -β- d -glucuronide and their aglycones from an aqueous extract of Scutellariae Radix in the rat

Cai, Yu-Dong; Li, Sai; Li, Ting; Zhou, Rui-Na; Wai, Alfred Tai-Seng; Yan, Ru

doi:10.1016/j.jchromb.2015.11.049

Cited by 39 publications

(32 citation statements)

References 45 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The analytes showed multiple peaks in the plasma concentration–time plots, and this phenomenon might be mainly caused by the enterohepatic circulation and the presence of absorption sites along the stomach and different gastrointestinal segments . As shown in Table , the T max values for three glucuronidated metabolites were in the range of 0.16–2 h, which demonstrated that all flavonoids could be quickly absorbed and/or metabolized in the gastrointestinal tract following oral administration of the extract.…”

Section: Resultssupporting

confidence: 93%

Liquid chromatography‐tandem mass spectrometry assay for the simultaneous determination of three major flavonoids and their glucuronidated metabolites in rats after oral administration of Artemisia annua L. extract at a therapeutic ultra‐low dose

Wang

Cai

Liu

et al. 2019

J of Separation Science

View full text Add to dashboard Cite

The traditional antimalarial herb Artemisia annua L., from which artemisinin is isolated, is widely used in endemic regions. It has been suggested that artemisinin activity can be enhanced by flavonoids in A. annua; however, how fast and how long the flavonoids are present in the body remains unknown. In the present study, a rapid and sensitive liquid chromatography with tandem mass spectrometry method was developed and validated for the simultaneous determination of three major flavonoids components, i.e. chrysosplenol D, chrysoplenetin, and artemetin and their glucuronidated metabolites in rats after oral administrations of A. annua extracts at a therapeutic ultra‐low dose. The concentration of the intact form was determined directly, and the concentration of the glucuronidated form was assayed in the form of flavonoids aglycones, after treatment with β‐glucuronidase/sulfatase. The method was linear in the range of 0.5–300.0 ng/mL for chrysoplenetin and artemetin, and 2–600 ng/mL for chrysosplenol D. All the validation data conformed to the acceptance requirements. The study revealed a significantly higher exposure of the flavonoid constituents in conjugated forms in rats, with only trace intact from. Multiple oral doses of A. annua extracts led to a decreased plasma concentration levels for three flavonoids.

show abstract

Section: Resultssupporting

confidence: 93%

Liquid chromatography‐tandem mass spectrometry assay for the simultaneous determination of three major flavonoids and their glucuronidated metabolites in rats after oral administration of Artemisia annua L. extract at a therapeutic ultra‐low dose

Wang

Cai

Liu

et al. 2019

J of Separation Science

View full text Add to dashboard Cite

show abstract

“…In the MS E experiment, a diagnostic fragment ion was detected at m/z 475.0858 (C 15 H 10 O 5 ) in the low‐energy channel, which was the same as the protonated molecule ion of P23, and two diagnostic fragment ions were detected at m/z 299.0580 (C 16 H 11 O 6 ) and 284.0327 (C 15 H 8 O 6 ) in the high‐energy channel, which was the same as those of P23 and P26. Owing to P23, P25, P26 and P32 with the same flavonoid core structure (Figure S5), M25 was tentatively identified as hydroxyl‐wogonoside‐glucuronide (Cai et al, ; Du et al, ).…”

Section: Resultsmentioning

confidence: 99%

“…was the most abundant metabolite in rat plasma owing to its various According to the ClogP values of their potential glycosides in the previous studies (Du et al, 2015, Zhang, Cai, et al, 2015, and 284.0327 (C 15 H 8 O 6 ) in the high-energy channel, which was the same as those of P23 and P26. Owing to P23, P25, P26 and P32 with the same flavonoid core structure ( Figure S5), M25 was tentatively identified as hydroxyl-wogonoside-glucuronide (Cai et al, 2016;Du et al, 2015). (Du et al, 2015).…”

Section: Identification Of Flavonoid-related Metabolitesmentioning

confidence: 99%

Identification of the absorbed components and their metabolites of Tianma‐Gouteng granule in rat plasma and bile using ultra‐high‐performance liquid chromatography combined with quadrupole time‐of‐flight mass spectrometry

Zhang

Duan

Wang

et al. 2019

Biomedical Chromatography

View full text Add to dashboard Cite

Tianma‐Gouteng granule (TGG), a Chinese herbal formula preparation, is clinically used for the treatment of cardio‐cerebrovascular diseases such as hypertension, cerebral ischaemia, acute ischaemic stroke and Parkinson's disease. Although few reports have been published concerning the absorbed prototype components of TGG, the possible metabolic pathways of TGG in vivo remain largely unclear. In this study, a method using UPLC–Q/TOF MS was established for the detection and identification of the absorbed prototype components and related metabolites in rat plasma and bile after oral administration of TGG at high and normal clinical dosages. A total of 68 components were identified or tentatively identified in plasma and bile samples, including absorbed prototypes and their metabolites. The major absorbed components were gastrodin, isorhynchophylline, rhynchophylline, isocorynoxeine, corynoxeine, geissoschizine methyl ether baicalin, baicalein, wogonoside, wogonin, geniposidic acid, leonurine, 2,3,5,4′‐tetrahydroxystilbene‐2‐O‐β‐d‐glucoside and emodin. The main metabolic pathways of these components involved phase I (isomerization, hydrolysis and reduction) and phase II (glucuronidation and sulfation) reaction, and the phase II biotransformation pathway was predominant. The present study provides rich information on the in vivo absorption and metabolism of TGG, and the results will be helpful for further studies on the pharmacokinetics and pharmacodynamics of TGG.

show abstract

“…Scutellaria is a famous traditional Chinese medicine in China, with wogonoside and neobaicalein as its specific constituents (15). The former is a yellow crystal without an obvious melting point (15).…”

Section: Introductionmentioning

confidence: 99%

“…The former is a yellow crystal without an obvious melting point (15). It turns to red brown color when heated to 230˚C and decomposes at 302˚C.…”

Section: Introductionmentioning

confidence: 99%

Wogonoside inhibits cell growth and induces mitochondrial-mediated autophagy-related apoptosis in human colon cancer cells through the PI3K/AKT/mTOR/p70S6K signaling pathway

et al. 2018

View full text Add to dashboard Cite

Abstract. Wogonoside, the main effective constituent of traditional Chinese medicine Scutellaria, belongs to the glucuronide family, with various functions, including detoxification, anti-inflammation and nourishing gallbladder, lowering blood pressure, diuresis and anti-allergic reactions. However, the effects of wogonoside on human colon cancer cells remain unclear. The present study aimed to investigate the anticancer effect of wogonoside on human colon cancer cells in vitro and its anticancer mechanisms. The results demonstrated that wogonoside significantly inhibited cell growth, induced apoptosis and mitochondrial-mediated autophagy of colon cancer cells. Furthermore, the results revealed that wogonoside significantly increased caspase-3 and caspase-9 expression levels, induced apoptosis regulator Bax/Bcl-2 and microtubule-associated protein 1A/1B-light chain 3 protein expression, suppressed the phosphatidylinositol 3 kinase (PI3K)/RAC-α serine/threonine-protein kinase (Akt)/mechanistic target of rapamycin (mTOR)/p70 S6 kinase (p70S6K) signaling pathway and induced p62 protein expression in colon cancer cells. In conclusion, these results demonstrated that wogonoside inhibits cell growth and induces mitochondrial mediated autophagy-related apoptosis in human colon cancer cells through modulation of the PI3K/Akt/mTOR/p70S6K signaling pathway.

show abstract

Oral pharmacokinetics of baicalin, wogonoside, oroxylin A 7- O -β- d -glucuronide and their aglycones from an aqueous extract of Scutellariae Radix in the rat

Cited by 39 publications

References 45 publications

Liquid chromatography‐tandem mass spectrometry assay for the simultaneous determination of three major flavonoids and their glucuronidated metabolites in rats after oral administration of Artemisia annua L. extract at a therapeutic ultra‐low dose

Liquid chromatography‐tandem mass spectrometry assay for the simultaneous determination of three major flavonoids and their glucuronidated metabolites in rats after oral administration of Artemisia annua L. extract at a therapeutic ultra‐low dose

Identification of the absorbed components and their metabolites of Tianma‐Gouteng granule in rat plasma and bile using ultra‐high‐performance liquid chromatography combined with quadrupole time‐of‐flight mass spectrometry

Wogonoside inhibits cell growth and induces mitochondrial-mediated autophagy-related apoptosis in human colon cancer cells through the PI3K/AKT/mTOR/p70S6K signaling pathway

Contact Info

Product

Resources

About