Estrogenic and Neuroprotective Properties of Scutellarin from<i>Erigeron breviscapus</i>: A Drug against Postmenopausal Symptoms and Alzheimer's Disease

Zhu, Judy Ting Ting; Choi, Roy Chi Yan; Li, Jun; Xie, Heidi Qunhui; Bi, Cathy W. C.; Cheung, Anna Wing Han; Dong, Tina T. X.; Zhi, Jiang; Chen, Ji J.; Tsim, Karl Wah Keung

doi:10.1055/s-0029-1185776

Cited by 39 publications

(17 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The compound has also been shown to have some anti-HIV effects [7] and to attenuate hepatocellular damage [8] . It is interesting that scutellarin exhibits weak estrogenic properties [9,10] , similar to genistein and apigenin. Many phytoestrogen compounds, such as genistein, apigenin, daidzein, glycitein, and their metabolites, have been demonstrated pharmacokinetic differences between male and female in humans and rats.…”

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

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

show abstract

“…In addition, flavones, one of the major components of HE, have been shown to possess neuroprotective effects [9] and inhibit formation of reactive oxygen species [47][48][49][50] . Furthermore, Scu can inhibit Aβ aggregation and prevent cell death induced by Aβ in cultured PC12 cells [1,3] . In this study, the rats were injected with Aβ to induce learning and memory dysfunction and then treated with Scu extracted from HE in order to investigate the effects of the compound on learning and memory function, expression of nAChRs and the activity of ChE.…”

Section: Wwwchinapharcom Guo Ll Et Almentioning

confidence: 99%

“…Interestingly, scutellarin (Scu) is a major component of flavonoids in HE (over 40% of the total flavonoids: 5,6,4',7-glucuronyl oxyflavone). Several basic research and clinical studies have shown that Scu plays an important role in combating neurotoxi city [1,7,8] . Alzheimer's disease (AD) is one of the most devastating diseases of the central nervous system (CNS).…”

Section: Introductionmentioning

confidence: 99%

“…Herba Erigerontis (HE), a Chinese medicinal herb derived from Erigeron breviscapus (vant) Hand-Mazz, has been used to effectively treat brain and cardiovascular disorders [1] . Flavonoids, a large group of natural compounds found in HE, have been considered as substitutes for estrogen [2] and proven to have neuroprotective effects [3][4][5][6] .…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Scutellarin protects against Aβ-induced learning and memory deficits in rats: involvement of nicotinic acetylcholine receptors and cholinesterase

Guo

Guan

Wang³

2011

Acta Pharmacol Sin

View full text Add to dashboard Cite

Aim: To examine the protective effects of scutellarin (Scu) on rats with learning and memory deficit induced by β-amyloid peptide (Aβ). Methods: Fifty male Wistar rats were randomly divided into 5 groups: control, sham operation, Aβ, Aβ+Scu, and Aβ+piracetam groups. Aβ 25-35 was injected into the lateral ventricle (10 μg each side). Scu (10 mg/2 mL) or piracetam (10 mg/2 mL was intragastrically administered per day for 20 consecutive days following Aβ treatment. Learning and memory was assessed with Morris water maze test. The protein and mRNA levels of nicotinic acetylcholine receptor (nAChR) α4, α7, and β2 subunits in the brain were examined using Western blotting and real-time PCR, respectively. The activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in the brain and plasma were measured using Ellman's colorimetric method. Results: In Aβ group, the escape latency period and first platform cross was significantly increased, and the total number of platform crossings was significantly decreased, as compared with the control and the sham operation groups. Both Scu and piracetam treatment significantly reduced the escape latency period and time to cross platform, and increased the number of platform crosses, but there were no significant differences between Aβ+Scu and Aβ+piracetam groups. In Aβ group, the protein levels of nAChR α4 and α7 subunits in the cerebral cortex were significantly decreased by 42%-47% and 58%-61%, respectively, as compared to the control and the sham operation groups. Scu treatment caused upregulation of α4 and α7 subunit proteins by around 24% and 30%, respectively, as compared to Aβ group, but there were no significant differences between Aβ+Scu and Aβ+piracetam groups. The protein level of nAChR β2 subunit had no significant difference among different groups. The mRNA levels of nAChR α4, α7, and β2 subunits were not significantly changed. In Aβ group, the activities of AChE and BuChE in the brain were significantly increased, but were significantly decreased in the plasma, as compared to the control and the sham operation groups. Scu or piracetam treatment restored the activities in brain and plasma nearly to the levels in the control group. Conclusion: The results suggest that Scu may rescue some of the deleterious effects of Aβ, possibly by stimulating nAChR protein translation and regulating cholinesterase activity.

show abstract

“…In experimental studies, it has been reported to have estrogenic and neuroprotective properties. [15] Breviscapine has been reported to attenuate neuroapoptosis and regulate the protein expression related to apoptosis after transient focal cerebral ischemia at a dose of 50-100 mg/kg in rats. [16] Neuroprotective effects of scutellarin on brain ischemic injury-induced apoptosis have been reported to be associated with inhibition of PARP-dependent mitochondrial dysfunction and subsequent translocation of the apoptosisinducing factor pathway.…”

mentioning

confidence: 99%

Closed Gateways — Can Neuroprotectants Shield the Retina in Glaucoma?

Velpandian

2010

Drugs R D

View full text Add to dashboard Cite

Neuroprotection for glaucoma is a therapeutic approach that aims to prevent optic nerve damage or cell death. An appropriate drug that reaches an adequate concentration across the blood retinal barrier is expected to shield the retina in glaucoma. Several in vitro and in vivo attempts in experimental models indicate the possibility of successful neuroprotection. However, clinical trials might not show the same level of neuroprotection as a result of subtherapeutic concentrations of the drug in the eye. The study by Zhong et al. in this issue of Drugs in R&D could not attribute the observed improvement in visual field indices to any one of the individual active constituents of Erigeron breviscapus (vant.) Hand. Mazz. (EBHM). One of the major constituents of EBHM is scutellarin, which is known to have poor oral bioavailability and an unclear ability to penetrate inside the eye. Therefore, before recognizing EBHM as a neuroprotectant in glaucoma for further clinical studies and practice, its active constituents and their pharmacokinetics (systemic as well as ocular) need to be explored.Neuroprotection as a pharmacological strategy to shield retinal ganglion cell death has been a popular approach adopted by many researchers. Yet, its effectiveness in preventing retinal ganglion cell death and thereby preserving vision in patients with primary open-angle glaucoma has not been demonstrated. [1] Mitochondria are abundant in the unmyelinated part of the retinal ganglion cell axons to meet the higher energy demand for nerve conduction and for the maintenance of optimum neuronal function. [2] Ischemia to the optic nerve head region can cause ganglion cell death at different rates. Therefore, effective intraocular pressure (IOP) control and blocking intracellular death triggers are both viable options. The right pharmacologic agent with a meaningful intraocular penetration would rationalize the neuroprotection strategy in glaucoma.For the last three decades, several attempts have been made to establish a successful neuroprotectant for glaucoma using various in vitro and in vivo models. A comprehensive PubMed search with the MeSH terms ''glaucoma'' and ''neuroprotection'' revealed the following compounds, factors and plant extracts: NMDA receptor antagonists (memantine, dexanabinol), an a2-adrenergic receptor agonist (brimonidine), an a 1 -and b-adrenergic receptor antagonist with a nitric oxide donor (nipradilol), an angiotensin II type 1 receptor blocker (candesartan), a prostaglandin-related compound (tafluprost), calcium channel blockers (nilvadipine and cilnidipine), a sodium channel blocker (phenytoin), a dual COMMENTARY Drugs R D 2010; 10 (2): 93-96

show abstract

Estrogenic and Neuroprotective Properties of Scutellarin fromErigeron breviscapus: A Drug against Postmenopausal Symptoms and Alzheimer's Disease

Cited by 39 publications

References 18 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

Scutellarin protects against Aβ-induced learning and memory deficits in rats: involvement of nicotinic acetylcholine receptors and cholinesterase

Closed Gateways — Can Neuroprotectants Shield the Retina in Glaucoma?

Contact Info

Product

Resources

About