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The pharmacology of Polygala tenuiflolia

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Polygala tenuiflolia

While I haven't been able to find the herb locally, Yuan Zhi (Radix Polygale, Chinese senega root) seems to have interesting pharmacological properties. Anyone know if it is available?

Preclinically, Radix Polygalae extract has been shown to demonstrate a rapid-onset antidepressant-like effect. One triterpenoid saponin from the roots, Yuanzhi-1, shows significant affinity towards 5-HT, NE and DA transporters and potent antidepressant-like effects.

3,6'-disinapoyl sucrose from Polygala tenuifolia significantly inhibited MAO-A and MAO-B activity, blocked stress-induced elevations of plasma cortisol, improved hippocampal-dependent learning and memory and rescued stress-induced deficits in hippocampal neuronal plasticity and neurogenesis.

Radix Polygalae extract also displays anti-inflammatory activity towards microglia.

More on the antidepressant properties can be found in this article and in the references:

Preclinical evidence of rapid-onset antidepressant-like effect in radix polygalae extract.

Radix Polygalae (the root of Polygala tenuifolia) is a herb widely used in traditional Asian medicine that is thought to exert a variety of neuropsychiatric effects. Radix Polygalae extract can protect against N-methyl D-aspartate (NMDA) neurotoxicity and induce brain-derived neurotrophic factor (BDNF) expression, suggesting modulatory roles at glutamatergic synapses and possible antidepressant action. In accordance with this hypothesis, Radix Polygalae extract demonstrated antidepressant-like effects in 8-week-old male C57Bl/6 mice by decreasing behavioral despair in the forced swim and tail suspension tasks and increasing hedonic-like behavior in the female urine sniffing test 30 minutes after a single oral administration of 0.1 mg/kg. Reduced latency to acquire a food pellet in the novely suppressed feeding paradigm, without change in anxiety-like behaviors suggested a rapid-onset nature of the antidepressant-like effect. In addition, it decreased the number of failed escapes in the learned helplessness paradigm after two oral administrations 24 hours and 30 minutes before the first test. Finally, it reversed anhedonia as measured by saccharin preference in mice exposed to the chronic stress model after two administrations of 0.1 mg/kg, in contrast to the repeated administration generally needed for similar effect by monoamergic antidepressants. Immobility reduction in tail suspension task was blocked by the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist NBQX, a pattern previously demonstrated by ketamine and other ketamine-like rapid-onset antidepressants. Also similarly to ketamine, Radix Polygalae appeared to acutely decrease phosphorylation of GluR1 serine-845 in the hippocampus while leaving the phosphorylation of hippocampal mTOR serine 2448 unchanged. These findings serve as preclinical evidence that Radix Polygalae extract exerts rapid-onset antidepressant effects by modulating glutamatergic synapses in critical brain circuits of depression and may be worthy of further evaluation as a safe substitute to other rapid-onset antidepressants known to have unacceptable side effects.

References:

Polygalasaponin XXXII from Polygala tenuifolia root improves hippocampal-dependent learning and memory

Anti-inflammatory effects of Polygala tenuifolia root through inhibition of NF-κB activation in lipopolysaccharide-induced BV2 microglial cells.

Possible mechanism of the antidepressant effect of 3,6'-disinapoyl sucrose from Polygala tenuifolia Willd.

Antidepressant-like effects of 3,6′-disinapoyl sucrose on hippocampal neuronal plasticity and neurotrophic signal pathway in chronically mild stressed rats

The discovery of Yuanzhi-1, a triterpenoid saponin derived from the traditional Chinese medicine, has antidepressant-like activity.

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Thanks for the link folias. Sounds like a good product.

Does anyone know if 1:10 extract granules in TCM are what we would call 10:1 or 10x extracts? This store below has a few products but I'm curious if it's a decent extract or mostly fillers?

http://medicineherbsupplier.com.au/store/index.php?route=product/search&search=Yuan%20Zhi

Not that I need the product at the moment but it would be good to know.

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1:10 should be 10%. Sometimes chinese pills are just herb dust rolled into pills with sugar, so 10% herb and 90% sugar.

It could also be that they simply wrote it wrong and meant 10:1 which is 10x, ie 1000%

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Tenuifolins, terpinoids found in this species apparently act as AChE inhibitors as well as increase norepinephrine & dopamine to some extent. possibly worth investigating as a oneirogen if it doesnt cause too much stimulation? youve got my interest peaked :wink:

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Did you ever get to try it out lofty?

Examine has once again done an excellent review of this herb recently.

I finally found the herb at a local TCM shop. My multiple mental health issues and current medications make it hard for me to be a guinea pig for meaningfully testing it out but with a15g decoction of powdered dry herb it seems to be a subtle mood improver. As a warning to others, it was strongly emetic at 30g. These doses are higher than the recommended TCM doses - most stating 3-9 g (dry weight).

One American ebay seller has an extract available which works out to be cheaper than the dried herb from where I found it ($7/100g)

Aside from the intriguing pharmacology, the traditional uses are interesting to consider:

Qualities:
Polygala is one of the truly extraordinary tonic herbs in the entire Asian tonic herbal system. This herb first attained wide use in Taoist circles because it was believed to have powerful mind and spirit developing power. In fact, Polygala root was believed to be an empowering substance in the class with wild Ginseng and Ganoderma in this regard. This root is traditionally used as a Shen tonic to relax the mind, calm the emotions and to aid in the sleep process. However, it does not relax the mind in entirely the same manner as many Shen stabilizing herbs such as Dragon Bone and Polygonum stem.
Instead, many people claim that it enhances dreaming and aids in creative thinking. And it not only aids creative thinking, but the ability to manifest our ideas. In fact, the ancient name for this herb is the “Will Strengthener”. The herb is believed to have the ability to strengthen that part of the psyche which we call the “Will”. Taoists have long claimed using Polygala to strengthen the focus of the mind and to empower our thoughts so that they may be made real. The Taoists taught that our creative visualization, which they called Yi, could be brought to reality by the Will. Therefore the Will had to be strengthened. In fact, the Will was virtually considered to be the fourth Treasure in what was otherwise called the Three Treasures system. Therefore Polygala, as a Will-strengthening herb, ranked extremely high on the list of important herbs in the Taoist pharmacopoeia. These days, Polygala may be used to strengthen the Will of the spiritual seeker, or it may be used to strengthen the Will of the more earth-bound. It is used in formulations to build enough willpower to overcome obstacles and to achieve greater heights. For example, it can be used as the main ingredient in formulas to help stop smoking or even to break other habits, such as drug abuse, overeating or compulsive behavior of any sort. Polygala has the unique power to provide the energy (the “power”) to our Will, so that we can overcome the obstacles that block us from becoming all that we can become. And it not only helps us break old, bad habits, it also helps strengthen our will to do new things, to achieve new heights. It strengthens our Will so that we can start to work on a new project, to start exercising, to start and continue whatever we need to do to grow, to become a great human being. That is the magic of Polygala, the “Will Strengthener”.
Polygala has another unique quality that sets it apart from most other herbs, including the tonic herbs. It has the ability to connect the Kidney (sexual) energy with the Heart (love) energy. It does this by opening the energy flow between the Heart and Kidney known as the Penetrating Vessel. The Penetrating Vessel is one of the energy channels that regulate the functions of the body-mind. It is called a “psychic channel” by the Taoists. Commonly, this vessel is blocked, resulting in a de-linking of our sexual energy and our emotional feelings. It is essential for our true health and well being that feelings of love and the functions of sex are united. Consuming Polygala for a period of time will have this result. The Will Strengthener therefore has a unique power to deepen our experience and our feelings and to bring new levels of happiness into our lives.
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Ive been unemployed the last three months, so id been to broke to bother looking into it. but i believe your post just solved that problem cheers again Alchemica :wink:

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This thread really piqued my interest, so i jumped on my favorite supplement site and grabbed some, im keen to see how it goes :-)

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Thank You very much for this thread / info. This might be of some help in the future for a friend of mine.

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Good to see some others interested in testing it out. I hope it benefits others :)

There's a bit of literature starting to build on saponins as CNS therapeutics in general.

From "Saponins: the phytochemical with an emerging potential for curing clinical depression":

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...there has been an increasing body of preclinical reports exhibiting the potential role of saponins in the cure of clinical depression. In this regard, the total saponins from Areca catechu nut (Abbas et al. 2013), Asparagus racemosus (Singh et al. 2009), Bupleurum falcatum (Sun et al. 2012), Chaihu-jia-longgu-muli-tang (Zhu et al. 2006; Li et al. 2012), Panax ginseng (Dang et al. 2009), Panax notoginseng (Xiang et al. 2011) and Trichopus zeylanicus (Rishikesh et al. 2012) were demonstrated to be antidepressants in rodents using various behavioural paradigms. In similar lines, several active saponins such as bacopasides (bacopaside I, bacopaside II and bacopasaponsin C) obtained from Bacopa monnieri (Zhou et al. 2007; Liu et al. 2013; Rauf et al. 2013), ginsenosides Rb3 (P. notoginseng) (Cui et al. 2012) and Yuanzhi-1 (a triterpenoid saponin isolated from dried root of Polygala tenuifolia) were found to be antidepressants in rodents as well (Jin et al. 2014). However, most of the work was performed on crude extracts and identification of the active saponin contents underlying antidepressant action needs to be explored. Furthermore, the compounds previously known to exhibit antidepressant activity display diverse chemical structures and hitherto no clear correlation has been established between the two. Similarly, there is a dearth of literature reporting the differential effects of steroidal and triterpenoid saponins on antidepressant action.

Saponins and its penetration into central nervous system

Saponins possess several unfavourable properties, such as large molecular weight, hydrophilicity and biliary excretion, leading to low bioavailability and poor penetration into central nervous system (Yu et al. 2012). The bioavailability of saponins is reported to be affected by its species, gastrointestinal digestion and plant combination (Li et al. 2013). Notably, the lipid-based formulations increase the bioavailability of saponins (Xiong et al. 2008). Literature also revealed that the metabolism of saponins by intestinal flora yield metabolites possessing greater ability to cross the membrane barriers of the body (Tawab et al. 2003). In this regard, the intestinal metabolite of ginsenosides, i.e. 20(S)-protopanaxadiol, was reported to exhibit antidepressant-like action in rodents (Xu et al. 2010).Thus, the metabolites of saponins also merit further investigations to characterise their anti-depressant components and development as therapeutic agents. This investigation is crucial in order to devise strategy both to overcome the challenges of bioavailability and penetration of the blood–brain barrier.

† Elevation of monoamines neurotransmitters
† HPA-axis normalisation
† Neurogenesis enhancement
† Reduction in stress-induced apoptosis
† Increase in BDNF and NGF levels
† Alleviation of oxidative stress

Saponins:

- increase the levels of monoamine neurotransmitters in the brain (Dang et al. 2009; Xiang et al. 2011; Abbas et al. 2013).

- decrease serum corticosterone levels, normalising the HPA axis

- inhibit intra-neuronal calcium dynamics thereby preventing excitotoxicity (Zhu et al. 2006; Xiang et al. 2011).

- inhibit stress-induced apoptosis in mice (Liu et al. 2010).

- reduce oxidative stress (Xu et al. 2010).

- increased the expression of BDNF and nerve growth factor (NGF) in the hippocampus of rat brain (Zhu et al. 2006; Dang et al. 2009; Jiang et al. 2012).

Ginseng:

- Ginsenoside Rg1 was reported to enhance neurogenesis in the hippocampus of mice (Jiang et al. 2012).

- Ginseng total saponins reversed the corticosterone-induced decrease in hippocamal BDNF levels via interfering in cAMP response element binding (CREB) signalling pathway (Chen et al. 2014).

- Ginsenoside Rg3 regulates voltage-gated ion channels such as Ca(2+), K(+), and Na(+) channels, and ligand-gated ion channels such as GABAA, 5-HT3, nicotinic acetylcholine, and N-methyl-D-aspartate (NMDA) receptors through interactions with various sites [a]

- Ginsenosides attenuate CNS and HPA dysfunction via peripheral immunomodulation [b, see also: Triterpenes and the immune system]


Bacopa:

- Bacopaside-1-mediated antidepressant activity is attributed partly to reduction in oxidative stress (Liu et al. 2013).

-TPH2 was up-regulated in the hippocampus after the oral treatment of Bacopa monniera leaf extract containing the active compound bacosides. [1]

- Bacopa monnieri and bacoside-A treatment reversed changes to GABAA receptors in epileptic rats [2]

-Treatment with B. monnieri and bacoside A prevented the occurrence of seizures thereby reducing the impairment of GABAergic activity, motor learning, and memory deficits [3].

- Bacoside A3, Bacopaside ll and Bacosaponin C. significantly reduced both expression and development of tolerance to morphine analgesia in mice. Additionally, Bacopa monnieri was found to enhance antinociceptive effect of morphine in intolerant animals [4]

- Bacosides provided a significant reduction of amphetamine-induced stereotype and conditioned avoidance response [5]

- Bacopa extract enhances hippocampus-dependent contextual memory by differentially regulating histone acetylation and protein phosphatases in hippocampus. [6]

- Bacopa monnieri exerts anti-inflammatory effects on cells of the innate immune system in vitro. [7]

- Brahmi has both neuroprotective and cognitive enhancement effects in schizophrenic rat models. [8] Bacosides A and B could be novel neuroprotective compounds for the prevention of cognitive deficits in schizophrenia as they increase VGLUT1 and VGLUT2 expression in a NMDA antagonist model of SCHZ [9, 10]

- A standardized extract of B monnieri was found to be effective in alleviating the symptoms of ADHD in children [11]

- The effects of acute administration of Bacopa monnieri in humans has been studied to a limited extent [12]

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Edited by Alchemica
OCD
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There's a bit of literature starting to build on saponins as CNS therapeutics in general.

Oh- interesting! I don't understand like 99% of the above. But I had a GC/MS workup done on one of my fave .au plants that I find really livens me up ( and kicks hangovers in the arse- Cissus antarctica ) and they found a bunch of novel saponins in it. Was wondering if they could be responsible for the tonic effect

Mind you there was a bunch of other un-ID stuff in there as well. Common with native plant workups.

Love your work. Every time I see a sexy pharmacological or research post here I am so heartened

Edited by Darklight
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This could be a candidate for a trial with piperine


From




_______________________________________________________________________________________________________________________

_____________________________________________________________________________________

Umesh et al, Piperine as a Bioavailability Enhancer

ISSN: 2230-9306 Available online at www.ijrapronline.com

16

Role of Piperine As A Bioavailability Enhancer

*UMESH K PATIL, AMRIT SINGH, ANUP K CHAKRABORTY

People’s Institute of Pharmacy & Research Centre, People’s University, Bhanpur, Bhopal-462037 (M.P.), India

Abstract

Piperine is an alkaloid responsible for the pungency of black pepper and long pepper, along with chavicine (an isomer of

piperine). It has also been used in some forms of traditional medicine and as an insecticide. Long pepper (Piper longum)

and Black pepper (Piper nigrum), the active compound in both Piper longum and Piper nigrum is piperine (1-piperoyl

piperidine) which is responsible for bioenhancing effect. It is shown to possess bioavailability enhancing activity with

various structurally and therapeutically diverse drugs. It has been found that piperine's bioavailability-enhancing

property may be attributed to increased absorption, which may be due to alteration in membrane lipid dynamics and

change in the conformation of enzymes in the intestine. Piperine has been demonstrated to increase the serum levels and

lengthen the serum half lives of some nutritional substances, such as coenzyme Q10 and beta-carotene. The mechanism of

this action is unknown. It is speculated that piperine may act as a so-called thermonutrient and increase the absorption of

certain nutritional substances from the gastrointestinal tract by producing a local thermogenic action. The present review

is an attempt to highlight the bioenhancing ability of piperine when it is given along with various drugs and nutrients

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