Scutellarin‐induced endothelium‐independent relaxation in rat aorta

Pan, Zhenwei; Feng, Tingting; Shan, Luchen; Cai, Benzhi; Chu, Wenfeng; Hui-li, Niu; Lu, Yanjie; Yang, Baofeng

doi:10.1002/ptr.2364

Cited by 72 publications

(36 citation statements)

References 16 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Interestingly enough, vasorelaxant effects were observed at concentrations that were in the same range as flavonoid plasma levels measured in volunteers after oral ingestion of soy protein drinks [15]. Only recently, Pan et al found that the flavonoid scutellarin dosedependently relaxes both endothelium-intact and endotheliumdenuded rat aortic rings [16]. The authors suggested that inhibition of calcium influx might be involved in the observed vasorelaxant effect.…”

Section: Effects Of Flavonoids On Vascular Calcium Currentmentioning

confidence: 78%

Cardiovascular Ion Channels as a Molecular Target of Flavonoids

Scholz

Zitron

Katus

et al. 2010

Cardiovascular Therapeutics

View full text Add to dashboard Cite

SUMMARYFlavonoids are a class of naturally occurring polyphenols abundant in edibles and beverages of plant origin. Epidemiological studies consistently associate high flavonoid intake with a reduced risk for the development of cardiovascular diseases. So far these beneficial effects have been mainly attributed to nonspecific antioxidant and antiinflammatory properties. However, there is an increasing body of evidence that flavonoids specifically target molecular structures including cardiovascular ion channels. Playing a pivotal role in the regulation of vascular tone and cardiac electric activity, ion channels represent a major target for the induction of antihypertensive and cardioprotective effects. Thus, pharmacological properties of flavonoids on cardiovascular ion channels, ion currents and tissue preparations are being increasingly addressed in experimental studies. Whereas it has become clear that cardiovascular ion channels represent an important molecular target of flavonoids, the published data have not yet been systematically reviewed.

show abstract

Section: Effects Of Flavonoids On Vascular Calcium Currentmentioning

confidence: 78%

Cardiovascular Ion Channels as a Molecular Target of Flavonoids

Scholz

Zitron

Katus

et al. 2010

Cardiovascular Therapeutics

View full text Add to dashboard Cite

show abstract

“…It was identified from a local folk prescription more than 30 years ago and is widely used as a microcirculation promoter for the treatment of cardio-cerebrovascular diseases with a large market share in China. In addition to its vasodilator effect (Pan et al, 2008), other pharmacological activities have been reported for S-7-G, including antioxidant (Hong and Liu, 2004), anti-inflammatory (Luo et al, 2008), and neuroprotective …”

Section: Introductionmentioning

confidence: 99%

Absorption and Disposition of Scutellarin in Rats: A Pharmacokinetic Explanation for the High Exposure of Its Isomeric Metabolite

Gao

Chen²,

Zhong³

2011

Drug Metab Dispos

View full text Add to dashboard Cite

ABSTRACT:Scutellarin or scutellarein-7-O-glucuronide (S-7-G) is a flavonoid used in the treatment of cardiovascular diseases. After oral administration to humans, S-7-G can hardly be detected, whereas its isomeric metabolite [scutellarein-6-O-glucuronide (S-6-G)] dominates in plasma. A preliminary study in rats also revealed a low bioavailability of S-7-G, as well as a high plasma concentration of S-6-G. Therefore, the present study tried to explore the possible causes of the unusual pharmacokinetics of scutellarin in humans through investigating the absorption and disposition of S-7-G in rats. After oral administration to rats, S-7-G was largely hydrolyzed in the intestinal tract and was absorbed as aglycone. While passing through the intestinal wall, aglycone was extensively glucuronidated into S-7-G and S-6-G (approximately 20:1), which subsequently entered the mesenteric blood (approximately 15:1). However, because S-7-G exhibited more rapid uptake in hepatocytes, was glucuronidated at a 2.7-fold higher rate in the liver, and was excreted in greater amounts through bile and urine than S-6-G, the S-7-G/S-6-G ratio eventually declined to approximately 1.5:1 in the systemic circulation. Findings revealed that S-7-G cannot be absorbed directly; S-7-G and S-6-G in the body were mostly generated from aglycone in the intestinal wall; a larger amount of S-7-G than S-6-G entered the mesenteric blood at the absorption stage, but the gap between them shrank quickly mainly because of the higher hepatic first-pass elimination of S-7-G. These findings in rats are of great value as reference for further study to accurately interpret the pharmacokinetics of S-7-G in humans.

show abstract

“…Scutellarin has been extensively used for the clinical treatment of cardiovascular and cerebrovascular diseases in China for many years. Pharmacological research indicates that scutellarin is associated with antihypertrophic effects [1] , fibrinolysis and anticoagulant effects [2] , protective effects in the brain and heart [3] , hypercholesterolemia suppression [4] , and endothelium-independent relaxation induction [5] . Scutellarin produces an anti-inflammatory effect via actions on arachidonic acid metabolism [6] .…”

Section: Introductionmentioning

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

Scutellarin‐induced endothelium‐independent relaxation in rat aorta

Cited by 72 publications

References 16 publications

Cardiovascular Ion Channels as a Molecular Target of Flavonoids

Cardiovascular Ion Channels as a Molecular Target of Flavonoids

Absorption and Disposition of Scutellarin in Rats: A Pharmacokinetic Explanation for the High Exposure of Its Isomeric Metabolite

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

Contact Info

Product

Resources

About