Thursday, October 29, 2015

● Kratom (Mitragyna speciosa)




Kratom is the name of a leaf native to Thailand, Malaysia, Indonesia, and Papua New Guinea that comes from the tree known as Mitragyna speciosa.   Kratom is in the same family as Coffee (Rubiaceae) and is botanically related to Corynanthe yohimbe, as well as Uncaria tomentosa and Uncaria rhynchophylla (Cat's claw).  Kratom also shares phytochemicals with Yohimbe and Cat's claw, and contains an extraordinary amount of epicatechin and catechin, two compounds found in Camellia sinensis (Green tea) that possess potent anti-oxidant activity.  In addition to these compounds, kratom also contains two opioid agonists and one opioid antagonist.  Obviously, it is of great potential interest to sufferers of pain, addicts of drugs, and to the field of medicine as a whole.





Kratom has traditionally been used for diarrhea, relieving pain, improving work ethic, depression, and opium detoxification. It contains over 25 known active compounds with the following pharmacological actions: 

● Ajmalicine (Raubasine): Cerebrocirculant, antiaggregant, anti-adrenergic (at alpha-1), sedative, anticonvulsant, smooth muscle relaxer 
● Corynantheidine: Opioid antagonist 
● Corynoxeine: Calcium channel blocker
● Corynoxine A and B: Dopamine mediating anti-locomotives  
● (-)-Epicatechin: Antioxidant, antiaggregant, antibacterial, antidiabetic, antihepatitic, anti-inflammatory, anti-leukemic, antimutagenic, antiperoxidant, antiviral, cancer preventative, alpha-amylase inhibitor  
● 9-Hydroxycorynantheidine: Partial opioid agonist
● 7-Hydroxymitragynine: Analgesic, antitussive, antidiarrheal; primary psychoactive in kratom
● Isomitraphylline: Immunostimulant, anti-leukemic
● Isopteropodine: Immunostimulant
● Mitragynine: Analgesic, antitussive, antidiarrheal, adrenergic, antimalarial, possible (5-HT2A) antagonist (anti-psychotic)
● Mitraphylline: Vasodilator, antihypertensive, muscle relaxer, diuretic, anti-amnesic, possible immunostimulant
● Paynantheine: Smooth muscle relaxer
● Rhynchophylline: Vasodilator, antihypertensive, calcium channel blocker, antiaggregant, anti-inflammatory, antipyretic, anti-arrhythmic, antithelmintic
● Speciociliatine: Weak opioid agonist
● Speciogynine: Smooth muscle relaxer
● Speciophylline: Anti-leukemic
● Tetrahydroalstonine: Hypoglycemic, adrenergic (alpha-2 adrenergic antagonist)


Looking at Kratom's pharmacological profile, it is no wonder that it has been used for a variety of purposes in it's native habitats, specifically Thailand, where the leaf was chewed not only to increase work ethics but as an effective treatment for overcoming the opium addiction that was ravaging the locals. (1)  On August 3, 1943, the government of Thailand passed the Kratom Act 2486. This law makes planting the tree illegal and requires existing trees to be cut down. This law was not found effective, since the tree is indigenous to the country. Before this act was passed, the Thai government was applying duties and collecting taxes from opium users and vendors, causing the habit to become unaffordable for many. This is when Kratom first became noticed by government officials, as the opium users started using the leaf to manage their symptoms of opiate withdrawal and end their addiction. At the beginning of the East Asian War in 1942, the diminishing profits from opium taxation forced the Thai government into action, banning their native tree in the efforts of recovering lost income from the government's taxation of opium.


Police Major General Pin Amornwisaisoradej, a member of the House of Representatives from Lampang in a special meeting on 7 January 1943: 

Taxes for opium are high while kratom is currently not being taxed. With the increase of those taxes, people are starting to use kratom instead and this has had a visible impact on our government’s income. (2)
Sadly, it seems, that a similar situation is occurring today as well. Thanks to Kratom's analgesic and addiction disrupting qualities, it is now being used as an herbal remedy to assist opiate detoxification as well as managing pain symptoms. To many, the leaf is a godsend and is a much safer alternative to pharmaceutical pain killers and anti-depressants. Unfortunately, the herb has not received FDA approval and is relatively unknown to western herbalists. Even more unfortunate, is that the plant has found itself in the hands of the legal high industry, touted as a "euphoric opiate stimulant drug" and not given the proper recognition it deserves as a therapeutic medicinal herb. This irresponsible marketing has recently caused 3 different states to enact legislation on the herb, calling it a "new synthetic drug". It seems that in the haste to put an end to these new & harmful synthetic drugs, Kratom has once again been caught in the crossfire. Hopefully this is just a passing phase, and more research can be given to this wonderful herb that has the potential to improve the lives of many.





Sources:



(1). Asnangkornchai, S. & Siriwong, A. (eds.) 2005. Kratom Plant in Thai Society: Culture, Behavior, Health, Science, Laws.




(2). Series on Legislative Reform of Drug Policies Nr . 13 April 2011 "Kratom in Thailand" Decriminalisation and Community Control? By Pascal Tangua

https://www.tni.org/files/download/kratom-briefing-dlr13.pdf



Originally posted by Akosi


Discuss Kratom on the phytoactive.net forums here: http://phytoactive.net/ethnobotanicals/kratom-mitragyna-speciosa/msg197/#msg197

Kratom leaf powder can be purchased at Meridian Botanicals here: https://meridianbotanicals.com/index.php?main_page=product_info&products_id=243

 

● Brahmi (Bacopa monnieri)

Bacopa monnieri is an ancient Ayurvedic herb that goes by the name Brahmi.  It has traditionally been used in India as a "Medhya Rasayana", or a mind enhancing tonic.  Bacopa is sedative in action, which shows us a bit about how the ideas of intelligence have shifted over time and culture.  Nowadays, stimulants are considered to be more beneficial to the mind, perhaps because the focus of our lives has also been shifted into a work and produce type mindset.  It does make one wonder about what was heralded in ancient India as intelligence and what human traits and characteristics were desirable.




Bacopa has activity as a NMDA antagonist, serotonergic, anti-epileptic, anti-oxidant, nootropic, sedative, anxiolytic, and anti-dopaminergic.

Bacopa is unique in its pharmacology in that it upregulates serotonin synthesis by the enzyme Tryptophan Hydroxylase (TPH2) and by increasing the expression of the serotonin transporter (SERT).


http://www.ncbi.nlm.nih.gov/pubmed/21129470
Bacopa monniera leaf extract up-regulates tryptophan hydroxylase (TPH2) and serotonin transporter (SERT) expression: implications in memory formation. 

Bacopa also shows improvement in spatial learning performance and enhanced memory retention, and when taken for a period of 4-6 weeks, shows promising activity at stimulating neurogenesis, significantly increasing the dendritic intersections and dendritic branching points along the length of both apical and basal dendrites which occur in brain neurons. 

What this means is that when bacopa is taken daily for some time, it strengthens the neuronal networks which send electrical signals to the brain.  Bacopa specifically enhances the networks associated with memory such as the hippocampus and the basolateral amygdala.









http://www.ncbi.nlm.nih.gov/pubmed/21892534

RESULTS AND CONCLUSIONS:

The results showed improvement in spatial learning performance and enhanced memory retention in rats treated with BM extract. There was a significant increase in the dendritic intersections and dendritic branching points along the length of both apical and basal dendrites in rats treated with BM extract for four and six weeks. However, the rats treated with BM extract for two weeks did not show any significant change in hippocampal CA3 neuronal dendritic arborization. We conclude that constituents present in BM extract have neuronal dendritic growth stimulating properties.

Bacopa also has some acetylcholine type activity, believing to function as a mild acetylcholine esterase inhibitor, letting levels of acetylcholine rise higher than normal.  This is not believed to be one of its major effects, but does play a part in the whole spectrum that makes up the total effects of the herb.

Additionally bacopa prevents dopamine induced neurotoxicity making it an excellent low dose companion for stimulant herbs such as mucuna pruriens, and also has adaptogenic type effects, reducing stress.  Bacopa is neuroprotective, prevents neuroinflammation, increases the levels of SOD (super-oxide dimutase), increases cerebral blood flow, has NMDA antagonistic effects, and influences the secretion of endogenous opioids.


Bacopa is strongly sedative in dopamine-high individuals, and initial use of the herb in doses above 1 gram may cause notable feelings of sleepiness or content relaxation in these individuals.  The sedative effects do go away over time but the herb definitely has the potential to negate the desired effects of stimulant herbs.  I prefer low dose bacopa (500 mg raw herb powder) as a daily adjunct with herbal stimulants, and higher doses at night to encourage restful sleep and dreams.  Taking bacopa at night may have potential in re sensitizing the dopamine system, while any supplementation will also sensitive the serotonin system.  I do not personally find bacopa all that useful for work, but dose, individual neurochemistry, and additional substances may produce different results.




Originally posted by Akosi

Discuss Bacopa monneiri on the phytoactive.net forums here: http://phytoactive.net/herbs/bacopa-monnieri-%28brahmi%29-serotonergic-nootropic-meditative-mind-rejuvenative/

Bacopa monneiri herb can be purchased at Meridian Botanicals here https://meridianbotanicals.com/index.php?main_page=product_info&cPath=65&products_id=267



 

Sunday, October 4, 2015

● Intellect tree seeds (Celastrus paniculatus)

Celastrus paniculatus seeds are a very popular herbal smart drug, or Medhya Rasayana with potent nootropic capabilities.  These seeds have been traditionally used as a memory enhancing, antiinflammatory, analgesic, sedative and antiepileptic agent.  The seeds are very popular with Indian students, similar to how American students will use stimulants to help with college.



The seeds are believed to work similar to common nootropics such as piracetam in that they stimulate acetylcholine release or inhibit the metabolism of the acetylcholine esterase enzyme (ACHE).


http://www.tandfonline.com/doi/abs/10.3109/13880200903127391 

The effect of Celastrus paniculatus Willd. (Celastraceae) seed aqueous extract on learning and memory was studied using elevated plus maze and passive avoidance test (sodium nitrite induced amnesia rodent model). The aqueous seed extract was administered orally in two different doses to rats (350 and 1050 mg/kg) and to mice (500 and 1500 mg/kg). The results were compared to piracetam (100 mg/kg, p.o.) used as a standard drug. Chemical hypoxia was induced by subcutaneous administration of sodium nitrite (35 mg/kg), immediately after acquisition training. In elevated plus maze and sodium nitrite-induced amnesia model, Celastrus paniculatus extract has showed statistically significant improvement in memory process when compared to control. The estimation of acetylcholinesterase enzyme in rat brain supports the plus maze and passive avoidance test by reducing acetylcholinesterase activity which helps in memory performance. The study reveals that the aqueous extract of Celastrus paniculatus seed has dose-dependent cholinergic activity, thereby improving memory performance. The mechanism by which Celastrus paniculatus enhances cognition may be due to increased acetylcholine level in rat brain.


In addition to the believed acetylcholine specific effects, celastrus has been shown to inhibit the metabolism of dopamine, serotonin, and norepinephrine, producing a potent anti-depressant effect.


http://ijpsdr.com/pdf/vol2-issue3/3.pdf
 
Oral administration of 1 ml of 5% emulsion of seed oil for 3
days enhanced the learning process in albino rats which was
comparable to that of vasopressin. [28] The memory process
also improved which was more prominent in 7 days treated
animals than in 3 days treated animals. The effects were
comparable to that of vasopressin. [29]
Effects of administration of seed oil on learning and memory
in a passive avoidance model as well as on brain contents of
biogenic amines viz., norepinephrine (NE), dopamine (DA)
and serotonin (5-HT) and their metabolites were studied.
Significant improvement was observed in cognition ability of
the drug treated rats. The drug did not produce any
neurotoxic effect or change in pain threshold in rats. The
contents of NE, DA and 5-HT and their metabolites in the
brain were significantly decreased in the drug treated group.
[30]

Outside of these anti-depressant and cognition enhancing effects, the seeds also show promise as a neuroprotective agent and also are able to enhance neurogenesis, increasing myelination in the brain.  The seeds are also potent anti-oxidants, and even protect the DNA from oxidative stress.

The seeds themselves work instantly when a high enough dose is taken, and also produce a streamlined enhancement of awareness and consciousness when taken long term.  14 days is the recommended timespan to begin to notice the secondary effects of the seeds.  3 grams of seed matter produces an instant lift in awareness, and  6 grams produces a potent anti-depressant effect co-occurring with an enhancement in focus, memory, and awareness.



Originally posted by Akosi

Discuss Celastrus paniculatus on the phytoactive.net forums here: http://phytoactive.net/herbs/celastrus-paniculatus-seeds-(intellect-tree)-nootropic-medhya-rasayana/

Celastrus paniculatus seeds can be purchased at Meridian Botanicals here: https://meridianbotanicals.com/index.php?main_page=product_info&cPath=65&products_id=250

 

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