Disease relevance of Scutellarin

• The present study investigated the protective effects of the antioxidant scutellarin against oxidative toxicity induced by glutamate in PC12 cells [1].
• At a concentration of 433muM, scutellarin inhibited 48% of the cell free recombinant HIV-1 RT activity [2].
• A study of the cardioprotective effect of breviscapine during hypoxia of cardiomyocytes [3].
• Overall, SM-470, Cam-300, scutellarin and baicalin inhibited the proliferation of human breast cancer cells and CAL-27 and FaDu cells with different potency [4].
• The results suggest that breviscapine has therapeutic effect on cerebral ischemia and vascular dementia [5].

Psychiatry related information on Scutellarin

• Protective effects of breviscapine on ischemic vascular dementia in rats [5].

High impact information on Scutellarin

• Pharmacokinetics and metabolism of the flavonoid scutellarin in humans after a single oral administration [6].
• The Tmax was late (7.85 +/- 1.62 h), and part of individual pharmacokinetic profiles showed double peaks, which indicated scutellarin could be absorbed into the intestine after hydrolysis to its aglycone by bacterial enzymes [6].
• Moreover, the combination of compounds from different classes offers enhanced potential therapeutic benefits; the combination of SM-470 with scutellarin, Cam-300 or baicalin, augmented the inhibition of cell proliferation [4].
• By comparing the inhibitory effects on p24 antigen, scutellarin was also found to be active against HIV-1(74V) (EC(50) 253muM) and HIV-1(KM018) (EC(50) 136muM) infection with significant difference in potency [2].
• From syncytia inhibition study, the EC(50) of scutellarin against HIV-1(IIIB) direct infection in C8166 cells was 26muM with a therapeutic index of 36 [2].

Chemical compound and disease context of Scutellarin

• AIM: To investigate the neuroprotective effect and mechanisms of scutellarin, a flavonoid extracted from Erigeron breviscapus Hand Mazz, against neuronal damage following cerebral ischemia/reperfusion [7].
• Results: Breviscapine treatment markedly inhibited both an increase of albuminuria and glomeruli hypertrophy and tubulointerstitial injury without modifying mean arterial blood pressure and creatinine clearance [8].

Biological context of Scutellarin

• Additionally, the effect of breviscapine on myocardial oxygen consumption was detected in dog myocardium in vitro [3].
• Prodrugs of scutellarin: Ethyl, benzyl and N,N-diethylglycolamide ester synthesis, physicochemical properties, intestinal metabolism and oral bioavailability in the rats [9].
• The percentage of this H2O2-induced apoptosis in the cells was decreased in the presence of different concentrations of scutellarin [10].
• The brain AUC ratio of breviscapine liposomes to commercial injection was 443.4+/-92.3% [11].
• Intracellular accumulation of ROS, Ca2+ and products of lipid peroxidation, resulting from H2O2 were significantly reduced by scutellarin [10].

Anatomical context of Scutellarin

• CONCLUSION: Scutellarin exerts a potent protective effect against oxidative damage in synaptosomes induced by superoxide [12].
• CONCLUSIONS: Breviscapine may protect the transplanted small intestine against I/R injury during transplantation in rats [13].
• In this study, we demonstrated the effects of breviscapine on vascular dementia (VD) rats, which were mimicked by permanent occlusion of bilateral common carotid arteries [5].
• RESULTS: Scutellarin significantly reduced infarct volume (P<0.05 or P<0.01), ameliorated the neurological deficit and reduced the permeability of the blood-brain barrier (BBB) (P<0.05) [7].
• Differential effects of new breviscapine on arachidonic acid metabolisms in blood cells and endothelial cells [14].

Associations of Scutellarin with other chemical compounds

• A specific, precise and accurate high-performance liquid chromatography (HPLC) method for the determination of aglycone conjugated metabolites of scutellarin in plasma after enzymolysis to scutellarein (the aglycone of scutellarin) was developed and validated [15].
• Glycolamide ester of scutellarin was chosen to investigate the intestinal metabolism and in vivo bioavailability [9].
• Chromatographic separation of scutellarin in plasma was performed on a C18 column, with a mobile phase of acetonitrile-water (23:77, v/v), adjusted to pH 2.5 with 1M phosphoric acid, and rutin was used as an internal standard [16].
• Pretreatment with scutellarin (25-100 micromol/L) significantly ameliorated the oxidative damage of synaptosomes by reducing MDA levels and [Ca2+]i, up-regulating membrane fluidity and restoring Na+/K+-ATPase activity [12].
• Highly water soluble esters of scutellarin with different molecular weight polyethylene glycol (PEG) were synthesized [17].

Gene context of Scutellarin

• Levels of malondialdehyde and protein kinase C activities were markedly higher and antioxidant enzyme activities such as superoxide dismutase, catalase as well as glutathione peroxidase were significantly lower in the kidneys of diabetic rats than of the control group, breviscapine administration markedly remitted these changes [8].
• CONCLUSION: Scutellarin has protective effects for cerebral injury through regulating the expression of NOS isoforms and angiogenic molecules [7].
• Results also showed that hydrogen peroxide increased activity of cNOS, which was markedly inhibited by scutellarin [18].
• Western blot analysis noted that the expression of transforming growth factor beta1 protein was increased 1.8-fold in the kidney in diabetic rats, breviscapine treatment could reduce increased expression of TGF-beta1 protein by 47% [8].
• The aims of the present study were to investigate the regulatory function of scutellarin on production of nitric oxide (NO) as well as activities of constitutive NO synthase (cNOS) and inducible NO synthase (iNOS) in early stages of neuron damage induced by hydrogen peroxide [18].

Analytical, diagnostic and therapeutic context of Scutellarin

• Determination of aglycone conjugated metabolites of scutellarin in rat plasma by HPLC [15].
• Probing the binding of scutellarin to human serum albumin by circular dichroism, fluorescence spectroscopy, FTIR, and molecular modeling method [19].
• Distribution of liposomal breviscapine in brain following intravenous injection in rats [11].
• In vitro release and in vivo pharmacokinetics of MVLs containing breviscapine (bre-MVLs) following intramuscular injection to rats were investigated compared with those of traditional liposomes containing breviscapine (bre-TLs) [20].
• Determination of scutellarin in rat plasma by high-performance liquid chromatography with ultraviolet detection [21].

References