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 -- J.R.R. Tolkien The Children of Hurin
- Myricetin -


General Information:

Names: Myricetin, Cannabiscetin, Myricetol, Myricitin
Wikipedia entry: http://en.wikipedia.org/wiki/Myricetin
Dr. Ray Shahelien entry: http://www.raysahelian.com/myricetin.html

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Observations:

...Quercetin and structurally related flavonoids (myricetin, fisetin, luteolin)...

This flavonoid,an extract of the Chinese bayberry (Myrica rubra) plant, is under intense study in several universities. Dr. Chad Dickey and his team patented their formulation in 2010, anticipating a breakthrough treatment for tauopathies using this.
http://www.sumobrain.com/patents/wipo/Materials-methods-reduction-proteintau/WO2012012798A2.pdf Began mid-May, 2012.

One person diagnosed with CBD has found good results using Myricetin 100 mg tabs, two at bedtime and two in a.m.  Reports profound improvement in speech after taking myricetin about 10 days. Apraxia improved but improvements are subtle.


"Myricetin is being studied in several university labs because it is both low toxicity and reduces intracellular tau levels in a different way compared to curcumin, fisetin , and trehalose--to the extent that world-class tau researcher Dr. Chad Dickey's group has patented one formulation of this extract of the Bayberry plant... In my experience, the Longvida curcumin and the myricetin are the most powerful elements of this complementary regimen..."
http://www.sumobrain.com/patents/wipo/Materials-methods-reduction-protein-tau/WO2012012798A2.pdf

lecithin/quercetin preparation

http://www.mobilereagents.com/ gives blood-brain barrier info for chemicals

PMID: 15611092 Myricetin is actually better than MB for inhibiting tau filament formation (IC50s of 1.2 and 1.9 microM).

USDA Database for the Flavonoid Content of Selected Foods
http://www.nal.usda.gov/fnic/foodcomp/Data/Flav/flav.pdf
http://www.nal.usda.gov/fnic/foodcomp/Data/Flav/Flav02-1.pdf
http://lpi.oregonstate.edu/infocenter/phytochemicals/flavonoids/

Flavonoid Content of Vegetables
http://www.nal.usda.gov/fnic/foodcomp/Data/Other/AICR03_VegFl

Myricetin and Neurodegnerative:

Myricetin and brai health [Myricetin and brain health]

Excitotoxicity is the pathological process by which nerve cells are damaged by glutamate, when receptors for the excitatory neurotransmitter glutamate, such as the NMDA receptor, are overactivated. Excitotoxins, high levels of glutamate, reactive oxygen species generation or caspase-3 activation can cause excitotoxicity by allowing high levels of calcium ions to enter the cell. The high level of calcium in the cells activates a enzymes that can damage cell structures, resulting in diseases such as Alzheimer. A study conducted by Y Shimmyo and coworkers at Kyoto University showed that myricetin was a potent anti-neurodegenerative compound and may contribute to the discovery of a drug against neurodegeneration [1]. The scientists came to that conclusion after investigating the effect of myricetin on neurons. They found that myricetin reduced the excitotoxicity by different pathways. Myricetin modulated the NMDA receptor by phosphorylation, resulting in a reduced intracellular calcium level. Myricetin also inhibited ROS production caused by glutamate and reduced glutamate-induced activation of caspase-3.

A study by the Qingdao University, China, concluded that myricetin had protective effect on the toxicity of neurotoxin 6-hydroxydopamine by suppressing iron toxicity [2]. The main use of 6-hydroxydopamine is to induce Parkinsonism in laboratory animals to test new medicines for treating Parkinson's disease in humans. The scientists studied the effects of myricetin on 6-hydroxydopamine-induced neurodegeneration in the substantia nigra-striatum system and found that myricetin restored the dopamine content in the striatum.

[1] Three distinct neuroprotective functions of myricetin against glutamate-induced neuronal cell death: involvement of direct inhibition of caspase-3. J Neurosci Res. 2008 Jun;86(8):1836-45

[2] Myricetin reduces 6-hydroxydopamine-induced dopamine neuron degeneration in rats. Neuroreport. 2007 Jul 16;18(11):1181-5.

http://www.phytochemicals.info/phytochemicals/myricetin/brain-health.php

Myricetin affords protection against peroxynitrite-mediated DNA damage and hydroxyl radical formation.
Chen W, Li Y, Li J, Han Q, Ye L, Li A.
Food Chem Toxicol. 2011 Sep;49(9):2439-44. Epub 2011 Jun 30.
Source: College of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou 310035, China.
Abstract
Peroxynitrite has been extensively implicated in the pathogenesis of various forms of neurodegenerative disorders via its cytotoxic effects, this study was undertaken to investigate whether the neuroprotective effect of myricetin is associated with inhibition of peroxynitrite-mediated DNA damage, a critical event leading to peroxynitrite elicited cytotoxicity. We observed that peroxynitrite can cause DNA damage in ϕX-174 plasmid DNA and rat primary astrocytes. The presence of myricetin at physiological concentration was found to significantly inhibit DNA strand breakage induced by both peroxynitrite and its generator 3-morpholinosydnonimine (SIN-1). Moreover, the consumption of oxygen caused by SIN-1 was found to be decreased in the presence of myricetin, indicating that myricetin might affect the auto-oxidation of SIN-1. Furthermore, EPR spectroscopy demonstrated that the formation of DMPO-hydroxyl radical adduct (DMPO-OH) from peroxynitrite, and that myricetin inhibited the adduct signal in a concentration-dependent manner. Taken together, these results demonstrate for the first time that myricetin can inhibit peroxynitrite-mediated DNA damage and hydroxyl radical formation.
PMID: 21741426 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/21741426
Full Text: http://hnjzxbs.com/Myricetin%20affords%20protection%20against%20peroxynitrite-mediated%20DNA%20damage%20and%20hydroxyl%20radical%20formation.pdf

Myricetin is also known as Cannabiscetin, Myricetol, Myricitin [check these!]
http://www.altiusdirectory.com/Lifestyle/myricetin-supplements.html

Multiple System Atrophy (MSA):

“…alpha-synuclein (alphaS)…  Lewy body diseases (LBD) and multiple system atrophy (MSA)…”

Antioxidant compounds have potent anti-fibrillogenic and fibril-destabilizing effects for alpha-synuclein fibrils in vitro.
Ono K, Yamada M.
J Neurochem. 2006 Apr;97(1):105-15. Epub 2006 Mar 8.
Source: Department of Neurology and Neurobiology of Aging, Kanazawa University Graduate School of Medical Science, Kanazawa, Japan.
Abstract
The aggregation of alpha-synuclein (alphaS) in the brain has been implicated as a critical step in the development of Lewy body diseases (LBD) and multiple system atrophy (MSA). Various antioxidants not only inhibit the formation of beta-amyloid fibrils (fAbeta), but also destabilize preformed fAb in vitro. Using fluorescence spectroscopy with thioflavin S and electron microscopy, here we examined the effects of the antioxidants nordihydroguaiaretic acid, curcumin, rosmarinic acid, ferulic acid, wine-related polyphenols [tannic acid, myricetin, kaempferol (+)-catechin and (-)-epicatechin], docosahexaenoic acid, eicosapentaenoic acid, rifampicin and tetracycline on the formation of alphaS fibrils (falphaS) and on preformed falphaS. All molecules, except for docosahexaenoic acid and eicosapentaenoic acid, dose-dependently inhibited the formation of falphaS. Moreover, these molecules dose-dependently destabilized preformed falphaS. The overall activity of the molecules examined was in the order of: tannic acid=nordihydroguaiaretic acid=curcumin=rosmarinic acid=myricetin>kaempferol=ferulic acid>(+)-catechin=(-)-epicatechin>rifampicin=tetracycline. These compounds with anti-fibrillogenic as well as antioxidant activities could be key molecules for the development of preventives and therapeutics for LBD and MSA as well as Alzheimer's disease.
PMID: 16524383 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/16524383

Curcumin reduces α-synuclein induced cytotoxicity in Parkinson's disease cell model
Min S Wang1,2, Shanta Boddapati1, Sharareh Emadi1 and Michael R Sierks1*
* Corresponding author: Michael R Sierks sierks@asu.edu
Author Affiliations
1 Department of Chemical Engineering, Arizona State University, Tempe, AZ 85287-6006 USA
2 Department of Chemistry, University of Colorado Denver, Denver, CO 80217-3364 USA
BMC Neuroscience 2010, 11:57 doi:10.1186/1471-2202-11-57
http://www.biomedcentral.com/1471-2202/11/57

Curcumin reduces alpha-synuclein induced cytotoxicity in Parkinson's disease cell model.
Wang MS, Boddapati S, Emadi S, Sierks MR.
BMC Neurosci. 2010 Apr 30;11:57.
Source: Department of Chemical Engineering, Arizona State University, Tempe, AZ 85287-6006, USA.
Abstract
BACKGROUND:

Overexpression and abnormal accumulation of aggregated alpha-synuclein (alphaS) have been linked to Parkinson's disease (PD) and other synucleinopathies. alphaS can misfold and adopt a variety of morphologies but recent studies implicate oligomeric forms as the most cytotoxic species. Both genetic mutations and chronic exposure to neurotoxins increase alphaS aggregation and intracellular reactive oxygen species (ROS), leading to mitochondrial dysfunction and oxidative damage in PD cell models.

RESULTS:

Here we show that curcumin can alleviate alphaS-induced toxicity, reduce ROS levels and protect cells against apoptosis. We also show that both intracellular overexpression of alphaS and extracellular addition of oligomeric alphaS increase ROS which induces apoptosis, suggesting that aggregated alphaS may induce similar toxic effects whether it is generated intra- or extracellulary.

CONCLUSIONS:

Since curcumin is a natural food pigment that can cross the blood brain barrier and has widespread medicinal uses, it has potential therapeutic value for treating PD and other neurodegenerative disorders.
PMID: 20433710 [PubMed] PMCID: PMC2879277
http://www.ncbi.nlm.nih.gov/pubmed/20433710
Full text: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2879277/?tool=pubmed
            http://www.biomedcentral.com/content/pdf/1471-2202-11-57.pdf

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Known sources:
    http://www.vitacost.com/source-naturals-myricetin-100-mg-60-tablets

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Natural sources:

Walnuts, blueberries (2.66 milligrams (mg) per 100 grams (g)), cranberries (6.78mg per 100g) and red onions (2.7mg per 100g)
[ Don’t know where they got these numbers from: Article Source: http://EzineArticles.com/6206018]

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References:

Multifunction of myricetin on A beta: neuroprotection via a conformational change of A beta and reduction of A beta via the interference of secretases.
Shimmyo Y, Kihara T, Akaike A, Niidome T, Sugimoto H.
J Neurosci Res. 2008 Feb 1;86(2):368-77.
Source: Department of Neuroscience for Drug Discovery, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan.
Abstract
Myricetin (3,3',4',5,5',7-hexahydroxyflavone) is classified as a flavonoid with strong antioxidant effects. Oxidative stress plays a key role in various neurological diseases such as ischemia and Alzheimer's disease (AD). To elucidate whether myricetin could counter the progress of AD, we examined the effects of myricetin on neurotoxicity induced by beta-amyloid (A beta), a component of senile plaques in the AD brain. We found that cultured rat primary cortical neurons treated for 48 hr with A beta1-42 (1 microM) induced significant neuronal injury. Conformationally altered A beta1-42 caused apoptotic changes, such as nuclear fragmentation, as shown by DAPI staining. Pre- and simultaneous administration of myricetin and A beta1-42 reduced A beta neurotoxicity in a concentration-dependent manner. By using circular dichroism spectroscopy and a thioflavin T binding assay, we show that myricetin (10 microM, 48 hr) prevented structural changes in A beta1-42 from a random coil to a beta-sheet-rich structure. A beta1-42-induced apoptotic changes and caspase-3 activation were reduced by myricetin treatment. Furthermore, we determined that administration of myricetin significantly decreased A beta1-40 and A beta1-42 levels in culture media. These effects were based on two mechanisms: the activation and up-regulation of alpha-secretase (ADAM10) protein levels as indicated by fluorescence resonance energy transfer (FRET) assay and immunoblot analysis and the direct binding and inhibition of beta-secretase (BACE-1) indicated by cell-free FRET assays. Evidently, myricetin has multiple functions to counter the progress of AD by the reduction of A beta production and the detoxification of A beta through a structural change.
PMID: 17722071 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/17722071

Phenolic compounds prevent amyloid β-protein oligomerization and synaptic dysfunction by site specific binding
Kenjiro Ono1, Lei Li2, Yusaku Takamura3, Yuji Yoshiike4, Lijun Zhu2, Fang Han2, Xian Mao2, Tokuhei Ikeda1, Jun-ichi Takasaki1, Hisao Nishijo3, Akihiko Takashima4, David B. Teplow5, Michael G. Zagorski2 and Masahito Yamada1
First Published on March 5, 2012, doi: 10.1074/jbc.M111.325456 jbc.M111.325456.
First Published on March 5, 2012, doi: 10.1074/jbc.M111.325456 April 27, 2012 The Journal of Biological Chemistry, 287, 14631-14643.
Abstract
Cerebral deposition of amyloid β-protein (Aβ) is an invariant feature of Alzheimer's disease (AD), and epidemiological evidence suggests that moderate consumption of foods enriched with phenolic compounds reduce the incidence of AD. We previously reported that the phenolic compounds myricetin (Myr) and rosmarinic acid (RA) inhibited Aβ aggregation in vitro and in vivo. To elucidate a mechanistic basis for these results, we analyzed the effects of five phenolic compounds in the Aβ aggregation process and in oligomer-induced synaptic toxicities. We now report that the phenolic compounds blocked Aβ oligomerization, and Myr promoted significant NMR chemical shift changes of monomeric Aβ. Both Myr and RA reduced cellular toxicity and synaptic dysfunction of the Aβ oligomers. These results suggest that Myr and RA may play key roles in blocking the toxicity and early assembly processes associated with Aβ through differently binding.
http://www.jbc.org/content/early/2012/03/08/jbc.M111.325456
Full Text: http://www.jbc.org/content/early/2012/03/08/jbc.M111.325456.full.pdf+html
http://www.jbc.org/content/287/18/14631.full.pdf+html

Myricetin: A Naturally Occurring Regulator of Metal-Induced Amyloid-β Aggregation and Neurotoxicity
Alaina S. DeToma1,†, Dr. Jung-Suk Choi2,†, Joseph J. Braymer1, Prof. Dr. Mi Hee Lim 1,2,*Article first published online: 28 APR 2011
DOI: 10.1002/cbic.201000790
http://onlinelibrary.wiley.com/doi/10.1002/cbic.201000790/abstract

Myricetin: a naturally occurring regulator of metal-induced amyloid-β aggregation and neurotoxicity.
DeToma AS, Choi JS, Braymer JJ, Lim MH.
Chembiochem. 2011 May 16;12(8):1198-201. doi: 10.1002/cbic.201000790. Epub 2011 Apr 28.
Source: Department of Chemistry, University of Michigan, Ann Arbor, MI 48109-1055, USA.
PMID: 21538759 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/21538759

[From a post “Myricetin suppresses iron neurodegeneration”
 http://forum.lowcarber.org/archive/index.php/t-339842.html
See alsoIron metabolism in Parkinsonian syndromes.
 http://www.ncbi.nlm.nih.gov/pubmed/16817199 (double check this link!)
CBD is a Parkinsonian Syndrome]

Myricetin reduces 6-hydroxydopamine-induced dopamine neuron degeneration in rats.
Ma ZG, Wang J, Jiang H, Liu TW, Xie JX.
Neuroreport. 2007 Jul 16;18(11):1181-5.
Source: Department of Physiology, Faculty of Medicine, Neuroscience Research Center of Shandong Province, Qingdao University, Qingdao, Shandong, PR China.
Abstract
The effects of myricetin on 6-hydroxydopamine (6-OHDA)-induced neurodegeneration in the substantia nigra-striatum system were investigated. By high-performance liquid chromatography electrochemical detection, we showed that the dopamine content in the striatum decreased after 6-OHDA treatment, which could be restored by myricetin. The immunohistochemistry and semiquantitative reverse transcription-PCR studies showed that myricetin could prevent the 6-OHDA-induced decrease of tyrosine hydroxylase positive neurons and the tyrosine hydroxylase mRNA expression in the substantia nigra. Perls' iron staining study further demonstrated that myricetin prevented the 6-OHDA-induced increase of iron-staining cells in the substantia nigra. These results suggested that the protective effects of myricetin on the toxicity of 6-OHDA could be attributed to the myricetin-suppressed iron toxicity.
PMID: 17589323 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/17589323

Iron metabolism in Parkinsonian syndromes.
Berg D, Hochstrasser H.
Mov Disord. 2006 Sep;21(9):1299-310.
Source: Hertie Institute of Clinical Brain Research and Department of Medical Genetics, University of Tübingen, Germany. daniela.berg@uni-tuebingen.de
Abstract
Growing evidence suggests an involvement of iron in the pathophysiology of neurodegenerative diseases. Several of the diseases are associated with parkinsonian syndromes, induced by degeneration of basal ganglia regions that contain the highest amount of iron within the brain. The group of neurodegenerative disorders associated with parkinsonian syndromes with increased brain iron content can be devided into two groups: (1) parkinsonian syndromes associated with brain iron accumulation, including Parkinson's disease, diffuse Lewy body disease, parkinsonian type of multiple system atrophy, progressive supranuclear palsy, corticobasal ganglionic degeneration, and Westphal variant of Huntington's disease; and (2) monogenetically caused disturbances of brain iron metabolism associated with parkinsonian syndromes, including aceruloplasminemia, hereditary ferritinopathies affecting the basal ganglia, and panthotenate kinase associated neurodegeneration type 2. Although it is still a matter of debate whether iron accumulation is a primary cause or secondary event in the first group, there is no doubt that iron-induced oxidative stress contributes to neurodegeneration. Parallels concerning pathophysiological as well as clinical aspects can be drawn between disorders of both groups. Results from animal models and reduction of iron overload combined with at least partial relief of symptoms by application of iron chelators in patients of the second group give hope that targeting the iron overload might be one possibility to slow down the neurodegenerative cascade also in the first group of inevitably progressive neurodegenerative disorders
PMID: 16817199 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/16817199

[ This one makes me sad because I knew about the iron connection.  Myricetin was available in 2008, but I didn’t know about it. ]

Phenolic compounds prevent Alzheimer's pathology through different effects on the amyloid-beta aggregation pathway.
Hamaguchi T, Ono K, Murase A, Yamada M.
Am J Pathol. 2009 Dec;175(6):2557-65. Epub 2009 Nov 5.
Source: Department of Neurology and Neurobiology of Aging, Kanazawa University Graduate School of Medical Science, Takara-machi, Kanazawa, Japan.
Abstract
Inhibition of amyloid-beta (Abeta) aggregation is an attractive therapeutic strategy for Alzheimer's disease (AD). Certain phenolic compounds have been reported to have anti-Abeta aggregation effects in vitro. This study systematically investigated the effects of phenolic compounds on AD model transgenic mice (Tg2576). Mice were fed five phenolic compounds (curcumin, ferulic acid, myricetin, nordihydroguaiaretic acid (NDGA), and rosmarinic acid (RA)) for 10 months from the age of 5 months. Immunohistochemically, in both the NDGA- and RA-treated groups, Abeta deposition was significantly decreased in the brain (P < 0.05). In the RA-treated group, the level of Tris-buffered saline (TBS)-soluble Abeta monomers was increased (P < 0.01), whereas that of oligomers, as probed with the A11 antibody (A11-positive oligomers), was decreased (P < 0.001). However, in the NDGA-treated group, the abundance of A11-positive oligomers was increased (P < 0.05) without any change in the levels of TBS-soluble or TBS-insoluble Abeta. In the curcumin- and myricetin-treated groups, changes in the Abeta profile were similar to those in the RA-treated group, but Abeta plaque deposition was not significantly decreased. In the ferulic acid-treated group, there was no significant difference in the Abeta profile. These results showed that oral administration of phenolic compounds prevented the development of AD pathology by affecting different Abeta aggregation pathways in vivo. Clinical trials with these compounds are necessary to confirm the anti-AD effects and safety in humans.
PMID: 19893028 [PubMed] PMCID: PMC2789642
http://www.ncbi.nlm.nih.gov/pubmed/19893028
Full Text:  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2789642/?tool=pubmed

Potent anti-amyloidogenic and fibril-destabilizing effects of polyphenols in vitro: implications for the prevention and therapeutics of Alzheimer's disease.
Ono K, Yoshiike Y, Takashima A, Hasegawa K, Naiki H, Yamada M.
J Neurochem. 2003 Oct;87(1):172-81.
Source: Department of Neurology and Neurobiology of Aging, Kanazawa University Graduate School of Medical Science, Kanazawa 920-8640, Japan.
Abstract
Cerebral deposition of amyloid beta-peptide (Abeta) in the brain is an invariant feature of Alzheimer's disease (AD). A consistent protective effect of wine consumption on AD has been documented by epidemiological studies. In the present study, we used fluorescence spectroscopy with thioflavin T and electron microscopy to examine the effects of wine-related polyphenols (myricetin, morin, quercetin, kaempferol (+)-catechin and (-)-epicatechin) on the formation, extension, and destabilization of beta-amyloid fibrils (fAbeta) at pH 7.5 at 37 degrees C in vitro. All examined polyphenols dose-dependently inhibited formation of fAbeta from fresh Abeta(1-40) and Abeta(1-42), as well as their extension. Moreover, these polyphenols dose-dependently destabilized preformed fAbetas. The overall activity of the molecules examined was in the order of: myricetin = morin = quercetin > kaempferol > (+)-catechin = (-)-epicatechin. The effective concentrations (EC50) of myricetin, morin and quercetin for the formation, extension and destabilization of fAbetas were in the order of 0.1-1 micro m. In cell culture experiments, myricetin-treated fAbeta were suggested to be less toxic than intact fAbeta, as demonstrated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Although the mechanisms by which these polyphenols inhibit fAbeta formation from Abeta, and destabilize pre-formed fAbetain vitro are still unclear, polyphenols could be a key molecule for the development of preventives and therapeutics for AD.
PMID: 12969264 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/12969264

Three distinct neuroprotective functions of myricetin against glutamate-induced neuronal cell death: involvement of direct inhibition of caspase-3.
Shimmyo Y, Kihara T, Akaike A, Niidome T, Sugimoto H.
J Neurosci Res. 2008 Jun;86(8):1836-45.
Source: Department of Neuroscience for Drug Discovery, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan.
Abstract
The excitatory neurotransmitter glutamate can accumulate in the brain and is thought to be involved in the etiology of many neurodegenerative disorders, including ischemia and Alzheimer disease. Therefore, it is important to search for compounds that reduce glutamate neurotoxicity. This glutamate-mediated excitotoxicity is caused by intracellular Ca2+ overload via the N-methyl-D-aspartate receptor NMDAR), reactive oxygen species (ROS) generation, and caspase-3 activation. Here we show that the natural flavonoid myricetin inhibited glutamate-induced excitotoxicity and protected neurons by multiple, distinct pathways. First, myricetin affected modulation of the NMDAR by phosphorylation, causing a subsequent reduction in glutamate-induced intracellular Ca2+ overload. Second, myricetin inhibited the ROS production caused by glutamate. Finally, glutamate-induced activation of caspase-3 was reduced by myricetin treatment. Moreover, myricetin directly interacted with the active site of caspase-3 via three hydrogen bonds and inhibited its activity. We conclude that myricetin inhibited glutamate-induced neuronal toxicity by multiple biochemical pathways. These results show that myricetin is a potent antineurodegenerative compound and may contribute to the discovery of a drug with which to combat neurodegeneration.
PMID: 18265412 [PubMed - indexed for MEDLINE]
http://www.ncbi.nlm.nih.gov/pubmed/18265412

Anti-inflammatory activity of myricetin-3-O-beta-D-glucuronide and related compounds.
A Hiermann, H W Schramm, S Laufer
Inflamm Res. 1998 Nov ;47 (11):421-7  9865500  Cit:9
Institute of Pharmacognosy, University of Graz, Austria. alois.hiermann@kfunigraz.ac.at

OBJECTIVE AND DESIGN: The anti-inflammatory effect of myricetinglucuronide (MGL) was investigated and structurally-related compounds were compared to examine the structure/activity-relationship in carrageenan-induced rat paw edema. MATERIALS AND SUBJECTS: In vitro studies were performed using rat basophilic leukemia (RBL-1) cells, human polymorphonuclear leukocytes (PMNL), COX-1 from ram seminal vesicle, COX-2 from sheep placenta and human venous blood. For the in vivo tests male Wistar rats were used, for the ex vivo test perfused rabbit ears. TREATMENT: 1-300 microg/kg MGL or myricetinmethylglucuronate and 0.1-5 mg/kg other related compounds administered p.o.(carrageenan edema). 5, 50 and 150 microg/kg MGL p.o. for 14 days (Freund's adjuvant arthritis), 5 and 50 microg/kg p.o. for 6 days (ulceration). METHODS: Anti-inflammatory effects were measured in carrageenan edema and in adjuvant arthritis. Incidence of gastric lesions was tested in an ulcerogenicity model in vivo. Influence on COX was determined in the perfused rabbit ear, in PMNL and in a test assay using COX-1 and COX-2. 5-LOX activity was studied using PMNL and RBL-1. The influence on platelet aggregation was evaluated measuring light transmission. RESULTS: MGL exerted a marked and dose-dependent anti-inflammatory effect in acute (carrageenan edema, ED50 15 microg/kg, indomethacin ED50 10 mg/kg) and chronic (adjuvant arthritis, inhibition at 150 microg/kg 18.1 % left paw, 20.6% right paw, indomethacin 3 mg/kg 18.0% and 19.4%)) models of inflammation. In the perfused rabbit ear 1 microg MGL inhibited the release of PGI2, PGD2 and PGE2 to the same extent as 1 microg indomethacin. The inhibition of COX-1 in the intact cell system was IC50 = 0.5 microM, that of indomethacin 0.0038 microM. In the isolated enzyme preparations of COX-1 and COX-2 the IC50 was 10 microM and 8 microM, that of indomethacin 9.2 mM and 2.4 microM. In the RBL-1 and PMNL test assay the inhibition of 5-LOX was 0.1 microM and 2.2 microM. An orally administered dose of 50 microg/kg/day induced no gastric ulcers in rats treated for 6 days. The investigations on carrageenan edema showed a close relationship between the structure of MGL and the anti-inflammatory effect. CONCLUSIONS: MGL is a COX-1, COX-2 and 5-LOX inhibitor. In view of the moderate in vitro activity and the very potent in vivo activity an additive mechanism must be involved. Small changes in the molecular structure lead to the loss or reduction of the anti-inflammatory activity.
Keywords: pmnl; mgl; cox; lox; microm; anti-inflammatory; microg/kg; rbl; carrageenan; indomethacin; edema; adjuvant arthrity; anti-inflammatory activity; rabbit ear; paw;
http://lib.bioinfo.pl/paper:9865500

Myricetin suppresses iron neurodegeneration
http://forum.lowcarber.org/showthread.php?t=339842

USDA Database for the Flavonoid Content of Selected Foods
http://www.nal.usda.gov/fnic/foodcomp/Data/Flav/flav.pdf

http://www.nal.usda.gov/fnic/foodcomp/Data/Flav/Flav02-1.pdf

http://lpi.oregonstate.edu/infocenter/phytochemicals/flavonoids/

Flavonoid Content of Vegetables
http://www.nal.usda.gov/fnic/foodcomp/Data/Other/AICR03_VegFlav.pdf

Search keywords: Myricetin and Neurodegnerative:

Myricetin and brai health [sic.  Should be: Myricetin and brain health This article needs to be summarized before publication!!!!!]
Excitotoxicity is the pathological process by which nerve cells are damaged by glutamate, when receptors for the excitatory neurotransmitter glutamate, such as the NMDA receptor, are overactivated. Excitotoxins, high levels of glutamate, reactive oxygen species generation or caspase-3 activation can cause excitotoxicity by allowing high levels of calcium ions to enter the cell. The high level of calcium in the cells activates a enzymes that can damage cell structures, resulting in diseases such as Alzheimer. A study conducted by Y Shimmyo and coworkers at Kyoto University showed that myricetin was a potent anti-neurodegenerative compound and may contribute to the discovery of a drug against neurodegeneration [1]. The scientists came to that conclusion after investigating the effect of myricetin on neurons. They found that myricetin reduced the excitotoxicity by different pathways. Myricetin modulated the NMDA receptor by phosphorylation, resulting in a reduced intracellular calcium level. Myricetin also inhibited ROS production caused by glutamate and reduced glutamate-induced activation of caspase-3.

A study by the Qingdao University, China, concluded that myricetin had protective effect on the toxicity of neurotoxin 6-hydroxydopamine by suppressing iron toxicity [2]. The main use of 6-hydroxydopamine is to induce Parkinsonism in laboratory animals to test new medicines for treating Parkinson's disease in humans. The scientists studied the effects of myricetin on 6-hydroxydopamine-induced neurodegeneration in the substantia nigra-striatum system and found that myricetin restored the dopamine content in the striatum.
[1] Three distinct neuroprotective functions of myricetin against glutamate-induced neuronal cell death: involvement of direct inhibition of caspase-3. J Neurosci Res. 2008 Jun;86(8):1836-45
[2] Myricetin reduces 6-hydroxydopamine-induced dopamine neuron degeneration in rats. Neuroreport. 2007 Jul 16;18(11):1181-5.
http://www.phytochemicals.info/phytochemicals/myricetin/brain-health.php

Myricetin affords protection against peroxynitrite-mediated DNA damage and hydroxyl radical formation.
Chen W, Li Y, Li J, Han Q, Ye L, Li A.
Food Chem Toxicol. 2011 Sep;49(9):2439-44. Epub 2011 Jun 30.
Source: College of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou 310035, China.
Abstract
Peroxynitrite has been extensively implicated in the pathogenesis of various forms of neurodegenerative disorders via its cytotoxic effects, this study was undertaken to investigate whether the neuroprotective effect of myricetin is associated with inhibition of peroxynitrite-mediated DNA damage, a critical event leading to peroxynitrite elicited cytotoxicity. We observed that peroxynitrite can cause DNA damage in ϕX-174 plasmid DNA and rat primary astrocytes. The presence of myricetin at physiological concentration was found to significantly inhibit DNA strand breakage induced by both peroxynitrite and its generator 3-morpholinosydnonimine (SIN-1). Moreover, the consumption of oxygen caused by SIN-1 was found to be decreased in the presence of myricetin, indicating that myricetin might affect the auto-oxidation of SIN-1. Furthermore, EPR spectroscopy demonstrated that the formation of DMPO-hydroxyl radical adduct (DMPO-OH) from peroxynitrite, and that myricetin inhibited the adduct signal in a concentration-dependent manner. Taken together, these results demonstrate for the first time that myricetin can inhibit peroxynitrite-mediated DNA damage and hydroxyl radical formation.
PMID: 21741426 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/21741426
Full Text: http://hnjzxbs.com/Myricetin%20affords%20protection%20against%20peroxynitrite-mediated%20DNA%20damage%20and%20hydroxyl%20radical%20formation.pdf

Multifunction of myricetin on Aβ: Neuroprotection via a conformational change of Aβ and reduction of Aβ via the interference of secretases
Yoshiari Shimmyo, Takeshi Kihara,Akinori Akaike,Tetsuhiro Niidome,Hachiro Sugimoto
Article first published online: 24 AUG 2007
DOI: 10.1002/jnr.21476
http://onlinelibrary.wiley.com/doi/10.1002/jnr.21476/abstract;jsessionid=1A49187547845BCF178B87CDE637FCE0.d04t02?systemMessage=Wiley+Online+Library+will+be+disrupted+on+7+July+from+10%3A00-12%3A00+BST+%2805%3A00-07%3A00+EDT%29+for+essential+maintenance&userIsAuthenticated=false&deniedAccessCustomisedMessage

Multifunction of myricetin on A beta: neuroprotection via a conformational change of A beta and reduction of A beta via the interference of secretases.
Shimmyo Y, Kihara T, Akaike A, Niidome T, Sugimoto H.
J Neurosci Res. 2008 Feb 1;86(2):368-77.
Source: Department of Neuroscience for Drug Discovery, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan.
Abstract
Myricetin (3,3',4',5,5',7-hexahydroxyflavone) is classified as a flavonoid with strong antioxidant effects. Oxidative stress plays a key role in various neurological diseases such as ischemia and Alzheimer's disease (AD). To elucidate whether myricetin could counter the progress of AD, we examined the effects of myricetin on neurotoxicity induced by beta-amyloid (A beta), a component of senile plaques in the AD brain. We found that cultured rat primary cortical neurons treated for 48 hr with A beta1-42 (1 microM) induced significant neuronal injury. Conformationally altered A beta1-42 caused apoptotic changes, such as nuclear fragmentation, as shown by DAPI staining. Pre- and simultaneous administration of myricetin and A beta1-42 reduced A beta neurotoxicity in a concentration-dependent manner. By using circular dichroism spectroscopy and a thioflavin T binding assay, we show that myricetin (10 microM, 48 hr) prevented structural changes in A beta1-42 from a random coil to a beta-sheet-rich structure. A beta1-42-induced apoptotic changes and caspase-3 activation were reduced by myricetin treatment. Furthermore, we determined that administration of myricetin significantly decreased A beta1-40 and A beta1-42 levels in culture media. These effects were based on two mechanisms: the activation and up-regulation of alpha-secretase (ADAM10) protein levels as indicated by fluorescence resonance energy transfer (FRET) assay and immunoblot analysis and the direct binding and inhibition of beta-secretase (BACE-1) indicated by cell-free FRET assays. Evidently, myricetin has multiple functions to counter the progress of AD by the reduction of A beta production and the detoxification of A beta through a structural change.
PMID:17722071 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/17722071

Inhibition of Heparin-induced Tau Filament Formation by Phenothiazines, Polyphenols, and Porphyrins*
Sayuri Taniguchi
http://www.jbc.org/content/280/9/7614.full
Full Text: http://www.jbc.org/content/280/9/7614.full.pdf+html

Inhibition of heparin-induced tau filament formation by phenothiazines, polyphenols, and porphyrins.
Taniguchi S, Suzuki N, Masuda M, Hisanaga S, Iwatsubo T, Goedert M, Hasegawa M.
J Biol Chem. 2005 Mar 4;280(9):7614-23. Epub 2004 Dec 17.
Source: Department of Molecular Neurobiology, Tokyo Institute of Psychiatry, Tokyo Metropolitan Organization for Medical Research, 2-1-8 Kamikitazawa, Setagaya-ku, Tokyo 156-8585, Japan.
Abstract
Tau protein is the major component of the intraneuronal filamentous inclusions that constitute defining neuropathological characteristics of Alzheimer's disease and other tauopathies. The discovery of tau gene mutations in familial forms of frontotemporal dementia has established that dysfunction of the tau protein is sufficient to cause neurodegeneration and dementia. Here we have tested 42 compounds belonging to nine different chemical classes for their ability to inhibit heparin-induced assembly of tau into filaments in vitro. Several phenothiazines (methylene blue, azure A, azure B, and quinacrine mustard), polyphenols (myricetin, epicatechin 5-gallate, gossypetin, and 2,3,4,2',4'-pentahydroxybenzophenone), and the porphyrin ferric dehydroporphyrin IX inhibited tau filament formation with IC(50) values in the low micromolar range as assessed by thioflavin S fluorescence, electron microscopy, and Sarkosyl insolubility. Disassembly of tau filaments was observed in the presence of the porphyrin phthalocyanine. Compounds that inhibited tau filament assembly were also found to inhibit the formation of Abeta fibrils. Biochemical analysis revealed the formation of soluble oligomeric tau in the presence of the inhibitory compounds, suggesting that this may be the mechanism by which tau filament formation is inhibited. The compounds investigated did not affect the ability of tau to interact with microtubules. Identification of small molecule inhibitors of heparin-induced assembly of tau will form a starting point for the development of mechanism-based therapies for the tauopathies.
PMID: 15611092 [PubMed - indexed for MEDLINE]
http://www.ncbi.nlm.nih.gov/pubmed/15611092
Full Text: http://www.jbc.org/content/280/9/7614.long

[A long list of citations from some site in Japan]

http://omicspace.riken.jp/PosMed/search?actionType=searchexec&condition=GeneIds&geneIds1=MGI:97180&keyword=microtubule&posSelectMode=false&rankScore=squ

[Patent by Genentech, Inc.  What exactly are they patenting???]
Modulation of Axon Degeneration
United States Patent Application 20110256150
http://www.freepatentsonline.com/y2011/0256150.html

Structure-activity relationship of flavonoids derived from medicinal plants in preventing methylmercury-induced mitochondrial dysfunction.
Franco JL, Posser T, Missau F, Pizzolatti MG, Dos Santos AR, Souza DO, Aschner M, Rocha JB, Dafre AL, Farina M.
Environ Toxicol Pharmacol. 2010 Nov 1;30(3):272-278.
Source: Departamento de Bioquímica Centro de Ciências Biológicas Universidade Federal de Santa Catarina, Florianópolis - SC, Brazil.
Abstract
In the present study, we investigated the potential protective effects of three flavonoids (myricetin, myricitrin and rutin) derived from medicinal plants against methyl mercury (MeHg)-induced mitochondrial dysfunction in vitro... Overall, the results suggest that MeHg-induced mitotoxicity is associated with oxidative stress. The ability of myricetin to prevent MeHg-induced oxidative damage in brain mitochondria renders this flavonoid a promising molecule for further in vivo studies in the search for potential antidotes to counteract MeHg-induced neurotoxicity.
PMID: 21127717  [PubMed]
PMCID:  PMC2992974
http://www.ncbi.nlm.nih.gov/pubmed/PMC2992974
Full text: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2992974/?tool=pubmed

Neuroprotection by flavonoids.
Dajas F, Rivera-Megret F, Blasina F, Arredondo F, Abin-Carriquiry JA, Costa G, Echeverry C, Lafon L, Heizen H, Ferreira M, Morquio A.
Braz J Med Biol Res. 2003 Dec;36(12):1613-20. Epub 2003 Nov 17.
Source: Departamento de Neuroquimica, Instituto de Investigaciones Biol gicas Clemente Estable, Universidade da Republica, Montevideo, Uruguay.
Abstract
The high morbidity, high socioeconomic costs and lack of specific treatments are key factors that define the relevance of brain pathology for human health and the importance of research on neuronal protective agents. Epidemiological studies have shown beneficial effects of flavonoids on arteriosclerosis-related pathology in general and neurodegeneration in particular. Flavonoids can protect the brain by their ability to modulate intracellular signals promoting cellular survival. Quercetin and structurally related flavonoids (myricetin, fisetin, luteolin) showed a marked cytoprotective capacity in in vitro experimental conditions in models of predominantly apoptotic death such as that induced by medium concentrations (200 M) of H2O2 added to PC12 cells in culture. Nevertheless, quercetin did not protect substantia nigra neurons in vivo from an oxidative insult (6-hydroxydopamine), probably due to difficulties in crossing the blood-brain barrier. On the other hand, treatment of permanent focal ischemia with a lecithin/quercetin preparation decreased lesion volume, showing that preparations that help to cross the blood-brain barrier may be critical for the expression of the effects of flavonoids on the brain. The hypothesis is advanced that a group of quercetin-related flavonoids could become lead molecules for the development of neuroprotective compounds with multitarget anti-ischemic effects.
PMID: 14666245 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/14666245
Full text: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2003001200002&lng=en&nrm=iso&tlng=en

Inhibition of heparin-induced tau filament formation by phenothiazines, polyphenols, and porphyrins.
Taniguchi S, Suzuki N, Masuda M, Hisanaga S, Iwatsubo T, Goedert M, Hasegawa M.
J Biol Chem. 2005 Mar 4;280(9):7614-23. Epub 2004 Dec 17.
Source: Department of Molecular Neurobiology, Tokyo Institute of Psychiatry, Tokyo Metropolitan Organization for Medical Research, 2-1-8 Kamikitazawa, Setagaya-ku, Tokyo 156-8585, Japan.
Abstract
Tau protein is the major component of the intraneuronal filamentous inclusions that constitute defining neuropathological characteristics of Alzheimer's disease and other tauopathies. The discovery of tau gene mutations in familial forms of frontotemporal dementia has established that dysfunction of the tau protein is sufficient to cause neurodegeneration and dementia. Here we have tested 42 compounds belonging to nine different chemical classes for their ability to inhibit heparin-induced assembly of tau into filaments in vitro. Several phenothiazines (methylene blue, azure A, azure B, and quinacrine mustard), polyphenols (myricetin, epicatechin 5-gallate, gossypetin, and 2,3,4,2',4'-pentahydroxybenzophenone), and the porphyrin ferric dehydroporphyrin IX inhibited tau filament formation with IC(50) values in the low micromolar range as assessed by thioflavin S fluorescence, electron microscopy, and Sarkosyl insolubility. Disassembly of tau filaments was observed in the presence of the porphyrin phthalocyanine. Compounds that inhibited tau filament assembly were also found to inhibit the formation of Abeta fibrils. Biochemical analysis revealed the formation of soluble oligomeric tau in the presence of the inhibitory compounds, suggesting that this may be the mechanism by which tau filament formation is inhibited. The compounds investigated did not affect the ability of tau to interact with microtubules. Identification of small molecule inhibitors of heparin-induced assembly of tau will form a starting point for the development of mechanism-based therapies for the tauopathies.
PMID: 15611092 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/15611092
Full text: http://www.jbc.org/content/280/9/7614.long


Cell culture protection and in vivo neuroprotective capacity of flavonoids.
Dajas F, Rivera F, Blasina F, Arredondo F, Echeverry C, Lafon L, Morquio A, Heizen H.
Neurotox Res. 2003;5(6):425-32.
Source: Department of Neurochemistry, Instituto de Investigaciones Biológicas Clemente Estable, Avda Italia 3318, 11600 Montevideo, Uruguay. fdajas@iibce.edu.uy
Abstract
Flavonoids are an important group of recognized antioxidants ubiquitous in fruits, vegetables and herbs. There are epidemiological evidences for the stroke-protecting capacity of flavonoids and while the neuroprotective power of complex extracts rich in flavonoids like those of Ginkgo biloba, green tea or lyophilized red wine have been demonstrated in several studies, neuroprotection by individual flavonoids has been poorly studied in vivo. The neuroprotective capacity of individual flavonoids was studied in PC12 cells in culture and in a model of permanent focal ischemia (permanent Middle Cerebral Artery Occlusion - pMCAO). In the in vivo experiments, flavonoids were administered in lecithin preparations to facilitate the crossing of the blood brain barrier. The simultaneous incubation of PC12 cells with 200 micro M hydrogen peroxide (H2O2) and different flavonoids for 30 min resulted in a conspicuous profile: quercetin, fisetin, luteolin and myricetin significantly increased cell survival while catechin, kaempherol and taxifolin did not. Quercetin was detected in brain tissue 30 min and 1 h after intraperitoneal administration. When one of the protective flavonoids (quercetin) and one of those that failed to increase PC12 cell survival (catechin) were assessed for their protective capacity in the pMCAO model, administered i.p. 30 min after vessel occlusion, quercetin significantly decreased the brain ischemic lesion while catechin did not. It is concluded that when administered in liposomal preparations, flavonoids structurally related to quercetin could become leads for the development of a new generation of molecules to be clinically effective in human brain ischemia.
PMID: 14715446 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/14715446


Flavonoid permeability across an in situ model of the blood-brain barrier.
Youdim KA, Qaiser MZ, Begley DJ, Rice-Evans CA, Abbott NJ.
Free Radic Biol Med. 2004 Mar 1;36(5):592-604.
Source:  Antioxidant Research Group, Wolfson Centre for Age-Related Diseases, Centre for Neuroscience Research, Guy's King's and St Thomas's School of Biomedical Sciences, King's College, London SE1 1UL, UK.
Erratum in Free Radic Biol Med. 2004 May 15;36(10):1342.
Abstract
Understanding mechanisms associated with flavonoid neuroprotection is complicated by the lack of information on their ability to enter the CNS. This study examined naringenin and quercetin permeability across the blood-brain barrier (BBB), using in vitro (ECV304/C6 coculture) and in situ (rat) models. We report measurable permeabilities (P(app)) for both flavonoids across the in vitro BBB model, consistent with their lipophilicity. Both flavonoids showed measurable in situ BBB permeability. The rates of uptake (K(in)) into the right cerebral hemisphere were 0.145 and 0.019 ml min(-1) g(-1) for naringenin and quercetin, respectively. Quercetin K(in) was comparable to that of colchicine (0.006 ml min(-1) g(-1)), a substrate for P-glycoprotein (P-gp). Preadministration of the P-gp inhibitor PSC833 or GF120918 (10 mg/kg body wt) significantly increased colchicine K(in), but only GF120918 (able to inhibit breast cancer resistance protein, BCRP) affected K(in) for quercetin. Naringenin K(in) was not affected. The influence of efflux transporters on flavonoid permeability at the BBB was further studied using MDCK-MDR1 and immortalized rat brain endothelial cells (RBE4). Colchicine, quercetin, and naringenin all showed measurable accumulation (distribution volume, V(d) (microl/mg protein)) in both cell types. The V(d) for colchicine increased significantly in both cell lines following coincubation with either PSC833 (25 microM) or GF120918 (25 microM). Both inhibitors also caused an increase in naringenin V(d); by contrast only GF120918 coincubation significantly increased quercetin V(d). In conclusion, the results demonstrate that flavonoids are able to traverse the BBB in vivo. However, the permeability of certain flavonoids in vivo is influenced by their lipophilicity and interactions with efflux transporters.
PMID: 14980703 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/14980703

Flavonoids and the aging brain.
Schmitt-Schillig S, Schaffer S, Weber CC, Eckert GP, Müller WE.
J Physiol Pharmacol. 2005 Mar;56 Suppl 1:23-36.
Source: Institute of Pharmacology (ZAFES), Biocenter Niederursel, University of Frankfurt, Frankfurt am Main, Germany.
Abstract
Like in all other organs, the functional capacity of the human brain deteriorates over time. Pathological events such as oxidative stress, due to the elevated release of free radicals and reactive oxygen or nitrogen species, the subsequently enhanced oxidative modification of lipids, protein, and nucleic acids, and the modulation of apoptotic signaling pathways contribute to loss of brain function. The identification of neuroprotective food components is one strategy to facilitate healthy brain aging. Flavonoids were shown to activate key enzymes in mitochondrial respiration and to protect neuronal cells by acting as antioxidants, thus breaking the vicious cycle of oxidative stress and tissue damage. Furthermore, recent data indicate a favorable effect of flavonoids on neuro-inflammatory events. Whereas most of these effects have been shown in vitro, limited data in vivo are available, suggesting a rather low penetration of flavonoids into the brain. Nevertheless, several reports support the concept that flavonoid intake inhibits certain biochemical processes of brain aging, and might thus prevent to some extent the decline of cognitive functions with aging as well as the development or the course of neurodegenerative diseases. However, more data are needed to assess the true impact of flavonoids on brain aging.
PMID: 15800383 [PubMed]
http://www.ncbi.nlm.nih.gov/pubmed/15800383
Full text: http://www.jpp.krakow.pl/journal/archive/03_05_s1/pdf/23_03_05_s1_article.pdf

Note… myricetin can induce apoptosis in cancer cells.

http://pi3kaktblog.com/2011/10/10/myricetin-can-inhibit-pi3k-and-induce-apoptosis-in-pancreatic-cancer/

Myricetin induces pancreatic cancer cell death via the induction of apoptosis and inhibition of the phosphatidylinositol 3-kinase (PI3K) signaling pathway.
Cancer Lett. 2011 Sep 28;308(2):181-8. Epub 2011 Jun 14.
Phillips PA, Sangwan V, Borja-Cacho D, Dudeja V, Vickers SM, Saluja AK.
Source: Department of Surgery, University of Minnesota, Minneapolis, 55455, United States.
Abstract
Pancreatic cancer is the fourth leading cause of cancer related deaths and is a disease with poor prognosis. It is refractory to standard chemotherapeutic drugs or to novel treatment modalities, making it imperative to find new treatments. In this study, using both primary and metastatic pancreatic cancer cell lines, we have demonstrated that the flavonoid myricetin induced pancreatic cancer cell death in vitro via apoptosis, and caused a decrease in PI3 kinase activity. In vivo, treatment of orthotopic pancreatic tumors with myricetin resulted in tumor regression and decreased metastatic spread. Importantly, myricetin was non-toxic, both in vitro and in vivo, underscoring its use as a therapeutic agent against pancreatic cancer.
PMID: 21676539
http://www.ncbi.nlm.nih.gov/pubmed/21676539

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