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The Polyskull Stack: An herbal Ritalin and an herbal Noopept? -Edefakiel/William Sterog-.

bdnf ngf polygala tenuifolia scutellaria baicalensis

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#1 William Sterog

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Posted 27 June 2016 - 02:37 PM


Scutellaria baicalensis: A Ritalin that increases attention, memory, neurogenesis and neuroprotection while decreasing anxiety?

 

-Attencion promoting effects:

Oroxylin A has shown an ability to block the dopamine transporter (DAT) in a manner similar to methylphenidate, albeit with less potency (similar potency of oroxylin A to atomoxetine).[49] And synthetic derivatives have been made (5,7-Dihydroxy-6-methoxy-4'-phenoxyflavone) with comparable potency than methylphenidate.[50] This is thought to underlie the attention promoting effects observed at 5-10mg/kg oroxylin A (injections) that had a potency similar to 2mg/kg methylphenidate in spontaneous alterations[49] while 1-5mg/kg was slightly less effective at reducing impulsiveness.[49]

-Neurogenesis:

Oroxylin A has been noted to increase CREB and BDNF phosphorylation in cognitively injured mice at 5mg/kg oral intake[51] and mice with beta-amyloid induced memory impairments[52] or to 400% of control mice (no cognitive impairment) at 50μM[53] which is due to activating ERK1/2 (an MAPK),[53][53] this is downstream of GABAA antagonism, as it was mimicked by bicuculline, and blocked by inhibiting NMDA receptors.[53][53]
Due to the above mechanisms, oroxylin A has been noted to stimulate neurogenesis in the hippocampus in a dose-dependent manner when administrated for 7-14 days to otherwise normal mice (5-10mg/kg), with 5mg/kg performing equally to 10mg/kg and 14 days not outperforming 7 days.[54]
Baicalin can enhance neural stem/progenator cell production and hippocampal dependent neurogenesis in rats following cerebral ischemic injury when injected at 50mg/kg daily for three weeks,[55] which is thought to be related to an upregulation of MASH1 expression at 7.5-30µM.

-Neuroprotection.

Heat Shock Protein 70 (HSP70) is an inducible HSP that exert protective effects in neurons[56] with particular efficacy against ischemic damage,[57][58] this neuroprotective property has been noted with baicalin at 200-300mg/kg[59][60][61] and baicalin is known to preserve HSP70 concentrations during ischeia associated with a preservation of ERK phosphorylation (cytoprotective[62][63]) and reducing the phosphorylation of p38 MAPK and JNK (positively mediates cell death[64][63]) resulting in cytoprotective effects.[61]

-Nootropic effects:

In regards to reversing age-related amnesia, scutellaria baicalensis (50-200mg/kg) is slightly more potent than the comparator of 200mg/kg Piracetam over 47 days.[80]
One study assessing the anti-amnesiac properties of Oroxylin A against scopolamine conducted a test in otherwise normal young mice, and while 2.5-20mg/kg trended to improve cognition (passive avoidance) only 5-10mg/kg reached statistical significance.[46]
Some evidence to support the usage of Oroxylin A in improving cognition in otherwise healthy and young rodents, suggesting nootropic effects

-Anxiety:

Baicalein has shown anxiolytic properties in a rat conflict test due to binding to the benzodiazepine binding site of the GABAA receptor[83]

 

 

Polygala Tenuifolia: A Noopept that upregulates NGF, BDNF *and TRKB*, works like an ampakine and have potent antidepressive effects?

-Neurogenesis:

Polygala tenuifolia has been noted to increase nerve growth factor (NGF) secretion when incubated with astroglial cells in the concentration range of 12.5-50μg/mL,[40][39] with most efficacy occurring at a concentration of 25μg/mL.[39] This may be mediated by the onjisaponins (mostly onjisaponins F and G) from the root, which increased NGF secretion in the range of 0.1-10μg/mL.[40]
3,6'-disinapoylsucrose (30-200μM; most potent at 60μM) has been noted to have protective effects against H2O2in vitro via increasing brain-derived neurotrophic factor (BDNF) secretion. This was mediated by CaMKII, ERK1/2, and TrkB, but not PI3K or PKA, signaling.[5] Polygalasaponin XXXII at a low oral dose (2mg/kg) in mice has also shown protective effects against memory loss (induced by scopolamine) with a potency comparable to 0.05mg/kg Huperzine-A.[17] This was due to increased BDNF in the hippocampus and was replicated in vitro at a concentration of 1μM, where ERK and CREB (downstream of BDNF) were activated within four minutes.[17] Tenuifoliside A has also shown BDNF-releasing properties in vitro in a manner dependent on PI3K/ERK activation.[2]

Several individual components of Polygala tenuifolia have been noted to either directly increase BDNF secretion (via PI3K/ERK signaling) or to otherwise preserve BDNF in instances where it would normally be reduced (such as scopolamine-induced amnesia).

[Effect of Polygala tenuifolia Willd YZ-50 on the mRNA expression of brain-derived neurotrophic factor and its receptor TrkB in rats with chronic stress depression]. [Article in Chinese] Sun Y1, Xie TT, Wang DX, Liu P. Author information Abstract OBJECTIVE: To observe the effect of Polygala tenuifolia Willd YZ-50 on the mRNA expression of brain-derived neurotrophic factor (BNDF) and its receptor TrkB in rats with chronic stress depression.es. METHODS: Normal male Wistar rats were divided in to control group, model group, desipramine (20 mg/kg) group, and low and high-dose (2.8 and 5.6 g/kg) YZ-50 groups. The total RNA was extracted from the rats with chronic stress depression, and the mRNA expression of BDNF and TrkB was detected by RT-PCR. RESULTS: Compared with the model group, YZ-50 at both low and high doses significantly increased the mRNA expression of BDNF and TrkB in the hippocampus of rats with chronic stress depression, and the effect was more obvious in the high-dose group (P<0.01). CONCLUSION: YZ-50 can up-regulate the expression of BDNF and TrkB mRNA to promote the recovery of the neurons from chronic stress-induced damages and produces anti-depressant effect.

Oral administration of tenuigenin appears to increase hippocampal activity in otherwise healthy mice, while in models of cognitive deficit there appears to be a preserving effect on hippocampal transmission.

-Neuroprotection:

An oligosaccharide found in the roots of Polygala tenuifolia known as tenuifolisde B (3-10mg/kg oral ingestion), has been noted to confer protection against KCN-induced anoxia and scopolamine-induced amnesia inmice with more potency than an equal dose of tacrine (3-10mg/kg), to such a degree where 10mg/kg of tenuifoliside B improved performance in a passive avoidance test relative to control despite scopolamine.[3] Tenuifoliside A and other oligosaccharide esters such as 3,6'disinapoylsucrose (DISS) also possess a neuroprotective effect in vitro, reducing damage from corticosterone on SY5Y neuroblastoma cells, with peak efficacy at 150µM and 15µM, respectively.[56]

-Depression:

Polygala Tenuifolia: Three Ways To Fight Depression: http://www.longecity...ght-depression/

-AMPA:

The GluR1 subunit of AMPA in rats has been noted to have reduced phosphorylation at Ser-845 30 minutes following oral ingestion of 0.1mg/kg Polygala tenuifolia root which appears to be involved in its antidepressant effects in mice.[8]

The antidepressant effects of Polygala tenuifolia extract (0.1mg/kg oral ingestion in mice) is abolished when AMPA is blocked.[8] This is known to occur with any antidepressant which works via NMDA antagonism such as ketamine or MGS0039.[45][46] Since AMPA blockade does not prevent the effect monoaminergic antidepressants,[47] this suggests that the effect of Polygala tenuifolia on depression is mediated by antiglutaminergic activity.[8] Unlike ketamine, however, Polygala tenuifolia does not activate hippocampal mTOR in neurons,[8] which may (disputably[48]) play a role in NMDA antagonists' antidepressive effects.[49]

-Nootropic effects:

Tenuigenin is another saponin specifically implicated in cognitive enhancement in mice, where 4mg/kg prevented cognitive dysfunction in animals subjected to ovariectomy with a potency comparable to estradiol.[11] Importantly, the effects of tenuigenin are not limited to hormone-compromised mice, as the same 4mg/kg dose improved learning and memory in otherwise healthy mice by enhancing synaptic plasticity.[55]

A dried root extract of Polygala tenuifolia given orally to aging mice at doses of 50-200mg/kg for four weeks alongside testing caused a time- and dose-dependent improvement in cognition associated with the two higher doses (100 and 200mg/kg), with 100mg/kg comparable in efficacy to 3mg/kg galantamine.

In otherwise healthy middle-aged adults 100mg BT-11 thrice daily over the course of four weeks improved immediate word recall relative to placebo, although both short and long term recall improvements (free and cued) assessed by the Korean version of the California Verbal Learning Test (K-CVLT) were not significant.[28] While there were no between-group differences in recognition scores, there was a significant increase in BT-11 treated patients relative to placebo.[28] In a spatial test for working and strategic memory (SOPT) there was a significant improvement noted with BT-11, with a 19% reduction in errors relative to placebo.[28]

Supplementation of BT-11 at 100mg three times a day in elderly adults without cognitive diseases (but with memory complaints) for eight weeks appeared to be able to benefit cognition as assessed by total CEMAD scores and organizational memory.

In elderly adults given the same dose of BT-11 for eight weeks, supplementation showed benefits in total Consortium to Establish a Registry for Alzheimer's Disease Assessment Packet (CERAD) scores, word list learning, and constructional measures (recall and praxis). In contrast, benefits to other parameters such as total MMSE scores, verbal fluency, and recognition did not reach significance and word list recall failed to improve with supplementation.[29]

The Polyskull Stack:

Polygala Tenuifolia + Scutellaria baicalensis.

Increase neurogenesis. 

Increase neuroprotection. 

Increase attention. Increase cognition. 

Increase spatial awareness and organization. 

Decrease anxiety. 

Decrease depression.

Decrease chronic fatigue syndrome:http://www.ncbi.nlm....pubmed/21884774.

Things that you can add:

Acetyl L Carnitine:

Potentiates NGF: http://www.ncbi.nlm..../pubmed/1655307 Increase energy: There are increase in glucose availability in certain brain regions following 25 days oral ingestion of 500mg/kg in otherwise young mice, such as the hippocampal formation (43%) with a decrease in alanine and lactate as well as the cortex (55%) although no changes in lactate occurred.[91]

Other energy molecules including Inositol (30%), Creatine in its phosphorylated form (66%), and phosphorylated adenosine molecules (AMP, ADP, ATP; collectively 23%) were increased over control[91] and the ATPase enzymes (enyzme that uses ATP to fuel metabolic processes) has been noted to be increased in synaptic membranes following infusions of 30-60mg/kg for 28 days.[92]

Rehmannia Glutinosa:

Nogo-A inhibitionhttp://www.dissertat...net/doc/1636787

Nogo-A inhibition and brain regrowth: http://www.longecity...brain-regrowth/

Improving Cognitive Performance By Inhibiting Nogo-A: https://selfhacked.c...-single-switch/


Edited by William Sterog, 27 June 2016 - 02:38 PM.

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#2 LiveWell

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Posted 28 October 2016 - 04:45 AM

Sorry to resurrect an old post.

 

Any updates on the Polygala Tenuifolia + Scutellaria baicalensis stack?



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#3 William Sterog

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Posted 28 October 2016 - 06:41 AM

Sorry to resurrect an old post.

 

Any updates on the Polygala Tenuifolia + Scutellaria baicalensis stack?

 

Actually I have a report on Polygala written here http://www.longecity...e-2#entry790137

 

I haven't tried Skullcap yet, but I read some interesting research about Baicalein a couple of days ago and I'm considering buying it. The only problem is that my stack is getting huge and I'm not comfortable with that.


Edited by William Sterog, 28 October 2016 - 06:50 AM.


#4 LiveWell

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Posted 28 October 2016 - 02:07 PM

Got it. Thanks!



#5 gamesguru

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Posted 29 October 2016 - 01:24 PM

I skimmed Will's post, and what stuck out to me was the fact that he reported benefits to both attention and emotional well-being.  Not sure whether serotonin[1] is involved in attention-deficit, dopamine in emotion dysregulation, or both.

Eur J Pharmacol. 2013 Sep 5;715(1-3):337-44. doi: 10.1016/j.ejphar.2013.05.002. Epub 2013 May 23.

5,7-Dihydroxy-6-methoxy-4'-phenoxyflavone, a derivative of oroxylin A improves attention-deficit/hyperactivity disorder (ADHD)-like behaviors in spontaneously hypertensive rats.

dela Peña IC, Young Yoon S, Kim Y, Park H, Man Kim K, Hoon Ryu J, Young Shin C, Hoon Cheong J.

 

Abstract

Oroxylin A, a major flavonoid in Scutellaria baicalensis, has been shown to alleviate attention-deficit/hyperactivity disorder (ADHD)-like behaviors in the spontaneously hypertensive rat (SHR) model of ADHD. As part of our continuing effort to discover effective ADHD drug candidates, we synthesized a number of oroxylin A derivatives and characterized their biological activities. Among all oroxylin A analogs, compound 7-7 (5,7-dihydroxy-6-methoxy-4'-phenoxyflavone) showed the most remarkable inhibition of dopamine reuptake alike methylphenidate, a dopamine transporter (DAT) blocker and typical drug for ADHD, and oroxylin A. It did not influence norepinephrine reuptake unlike atomoxetine, a selective norepinephrine inhibitor. Moreover, compound 7-7 reduced hyperactivity, sustained inattention and impulsivity in the SHR as measured by the open field, Y-maze and electro-foot shock aversive water drinking tests, respectively. Most drugs that enhance brain dopamine levels (e.g. DAT blockers like cocaine and methylphenidate) produce behavioral effects like those of stimulants causing them to be abused. However, the repeated treatment of compound 7-7 failed to elicit locomotor sensitization in rats, and neither produced conditioned place preference response nor maintained self-administration behavior. Altogether, the present study suggests the promising therapeutic value of compound 7-7 as an ADHD drug. Furthermore, compound 7-7 may be considered as an alternative therapy to psychostimulant ADHD treatments (e.g. amphetamine and methylphenidate) for which use has been deemed controversial due to their abuse liability.


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#6 BieraK

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Posted 13 November 2016 - 03:09 AM

https://www.ncbi.nlm...pubmed/26549702
Do any of you have a good extract from Scutellaria for stacking it with forskolin? Perhaps this could be a good "Chemical induce LTP"



Identification and Characterization of Baicalin as a Phosphodiesterase 4 Inhibitor.
Abstract

Asthma is a chronic inflammatory disease of lung airways, and pharmacological inhibitors of cyclic adenosine monophosphate-specific phosphodiesterase 4 (PDE4) have been considered as therapeutics for the treatment of asthma. However, development of PDE4 inhibitors in clinical trials has been hampered because of the severe side effects of non-selective PDE4 inhibitors. Here, screening of a plant extract library in conjunction with dereplication technology led to identification of baicalin as a new type of PDE4-selective inhibitor. We demonstrated that while rolipram inhibited the enzyme activity of a range of PDE4 subtypes in in vitro enzyme assays, baicalin selectively inhibited the enzyme activity of PDE4A and 4B. In addition, baicalin suppressed lipopolysaccharide-induced TNF-α expression in macrophage where PDE4B plays a key role in lipopolysaccharide-induced signaling. Furthermore, baicalin treatment in an animal model of allergic asthma reduced inflammatory cell infiltration and TNF-α levels in bronchoalveolar lavage fluids, indicating that the antiinflammatory effects of baicalin in vivo are attributable, in part, to its ability to inhibit PDE4.







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