Determination of aglycone conjugated metabolites of scutellarin in rat plasma by HPLC

Huang, Jianming; Li, Ni; Yu, Yunqiu; Weng, Weiyu; Huang, Xubing

doi:10.1016/j.jpba.2005.07.051

Cited by 26 publications

(11 citation statements)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Scutellarin and the unknown metabolite can be hydrolyzed completely by β-glucuronidase from bovine liver (essentially sulfatase-free) but not by sulfatase from Aerobacter aerogenes (no β-glucuronidase activity at pH 7). Huang et al [25] reported that scutellarin was hydrolyzed and transformed into scutellarein. Therefore, after hydrolysis by β-glucuronidase, the scutellarin peak disappeared, but the scutellarein peak increased.…”

Section: Discussionmentioning

confidence: 99%

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

et al. 2011

View full text Add to dashboard Cite

Aim: To study the metabolic and pharmacokinetic profile of scutellarin, an active component from the medical plant Erigeron breviscapus (Vant) Hand-Mazz, and to investigate the mechanisms underlying the low bioavailability of scutellarin though oral or intravenous administration in rats. Methods: HPLC method was developed for simultaneous detection of scutellarin and scutellarein (the aglycone of scutellarin) in rat plasma, urine and feces. The in vitro metabolic stability study was carried out in rat liver microsomes from different genders. Results: After a single oral dose of scutellarin (400 mg/kg), the plasma concentrations of scutellarin and scutellarein in female rats were significantly higher than in male ones. Between the female and male rats, significant differences in AUC, t max2 and C max2 for scutellarin were found. The pharmacokinetic parameters of scutellarin in the urine also showed significant gender differences. After a single oral dose of scutellarin (400 mg/kg), the total percentage excretion of scutellarein in male and female rats was 16.5% and 8.61%, respectively. The total percentage excretion of scutellarin and scutellarein in the feces was higher with oral administration than with intravenous administration. The in vitro t 1/2 and CL int value for scutellarin in male rats was significantly higher than that in female rats. Conclusion:The results suggest that a large amount of ingested scutellarin was metabolized into scutellarein in the gastrointestinal tract and then excreted with the feces, leading to the extremely low oral bioavailability of scutellarin. The gender differences of pharmacokinetic parameters of scutellarin and scutellarein are due to the higher CL int and lower absorption in male rats.

show abstract

Section: Discussionmentioning

confidence: 99%

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

et al. 2011

View full text Add to dashboard Cite

show abstract

“…15,16) It is being widely used in the treatment of ischemic vascular diseases such as cerebral infarction, apoplexy, and coronary heart disease in China. Thus, research on E. breviscapus has become a hot topic in recent years.…”

Section: )mentioning

confidence: 99%

Depigmentation of Melanocytes by (2Z,8Z)-Matricaria Acid Methyl Ester Isolated from Erigeron breviscapus

Luo

Kim

Nguyen

et al. 2009

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

To discover an active skin depigmenting agent, we isolated a novel inhibitor of melanin biosynthesis from the methanol extract of Erigeron breviscapus using a bioactivity-guided fractionation and identified it as (2Z,8Z)-matricaria acid methyl ester by means of spectroscopic analysis. The compound showed strong whitening activity in melan-a cell. Compared with arbutin (IC 50 ‫0.4؍‬ mM) as a positive control, the depigmentation IC 50 value for (2Z,8Z)-matricaria acid methyl ester was 25.4 m mM in B16F10 melanoma cell. Moreover, its inhibitory effect on tyrosinase, the key enzyme of melanogenesis, was examined by in vivo and in vitro tyrosinase assay and Western blot. The results indicate that (2Z,8Z)-matricaria acid methyl ester isolated from Erigeron breviscapus is a promising compound that could be useful for treating hyper-pigmentation as skin-whitening agents.Key words melanin; Erigeron breviscapus; (2Z,8Z)-matricaria acid methyl ester; skin whitening Biol.

show abstract

“…In order to evaluate scientifically the pharmacokinetics and bioequivalence of scutellarin formulations, it is essential to develop a sensitive and reliable analytical assay to determine the concentration of scutellarin in human plasma. Some HPLC methods have been described for the detection of scutellarin in animals given a high oral dosage of scutellarin or injected intravenously (Zhong et al, 2003;Ge et al, 2003;Hao et al, 2005;Huang et al, 2006) and the lower limits of quantification of these assays were mostly above 20 ng/mL. However, the concentration of archetypal scutellarin in human plasma was found to be very low (C max = 5 ng/mL) after oral administration of a clinical dosage (80 mg).…”

Section: Introductionmentioning

confidence: 99%

Retracted: Determination of scutellarin isomer, a predominant metabolite of scutellarin, in human plasma by HPLC/tandem mass spectrometry and its application to a pharmacokinetic study in Chinese healthy volunteers

Xia¹,

Xiong²,

Wang³

2007

Biomedical Chromatography

View full text Add to dashboard Cite

A liquid chromatography/tandem mass spectrometric (LC-MS/MS) method was developed to determine scutellarin isomer, a predominant metabolite of scutellarin, in human plasma for the pharmacokinetic study of scutellarin in Chinese healthy volunteers. Samples were acidified with formic acid and extracted with ethyl acetate. Chromatographic separation was achieved on a C 18 column with the mobile phase of water (containing 0.5% formic acid) and methanol (33:67, v/v). The analytes were detected using an electrospray positive ionization mass spectrometry in the selected reaction monitoring (SRM) mode. The calibration curve was linear over the range of 0.5-200.0 ng/mL and the lower limit of quantification was 0.5 ng/mL. The average extraction recoveries were 81.1 ± 7.5, 84.5 ± 6.9 and 83.4 ± 5.8% at concentrations of 2.0, 20.0 and 100.0 ng/mL, respectively. The intra-and inter-day precisions at three different concentrations were all less than 7.3% and accuracies were within the range 98.9-106.7%. The method described was precise, accurate and successfully applied to evaluate the pharmacokinetics and bioequivalence of scutellarin in 20 Chinese healthy volunteers. The results showed that the main pharmacokinetic parameters between scutellarin guttate pills and tablets had no statistically significant difference and the two formulations were bioequivalent.

show abstract

Determination of aglycone conjugated metabolites of scutellarin in rat plasma by HPLC

Cited by 26 publications

References 10 publications

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

Metabolic and pharmacokinetic studies of scutellarin in rat plasma, urine, and feces

Depigmentation of Melanocytes by (2Z,8Z)-Matricaria Acid Methyl Ester Isolated from Erigeron breviscapus

Retracted: Determination of scutellarin isomer, a predominant metabolite of scutellarin, in human plasma by HPLC/tandem mass spectrometry and its application to a pharmacokinetic study in Chinese healthy volunteers

Contact Info

Product

Resources

About