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Sceletium tortuosum - ingredients and uses.

heres what rätsch collected:

preparation and dosage
The processing of Kougoed has only recently been discovered and described in more detail. The collected plant material - it
should be collected in October, because that is when the plant is "strongest" - is between two stones after the harvest
crushed and "fermented" in a sealed jar for a few days.
In the past, animal hoses or
Hemp bags used, today plastic bags have taken their place. First, the bag with the plant material is sent to the
laid sun. During the day, the plant sweats out its juices, which condense on the plastic and later on the plant material
be reabsorbed. At night it cools down.
After 2 to 3 days, the bag is opened and the contents stirred well.
The bag is then closed again and laid out again. On the eighth day after the start of the procedure, the Kougoed
out of the bag and spread out in the sun to dry. Once dry, it can be used. According to
According to the informant, the fresh leaves have no potency, only the "fermented" herb is psychoactive. Then it will continue
crushed or powdered. Presumably by this process the for the genera Sceletiiirri and Mesembryanthernurn
characteristic, high content of oxalic acid significantly reduced.
Oxalic acid can cause severe irritation and allergies.
If you are in a hurry, a fresh plant can also be roasted on red-hot charcoal until it is completely dry and wilted
pulverized (SMITH et al. 1996: 126).
The powder is usually put in the mouth with some alcohol and kept there for about 10 minutes. The himself
collecting saliva can be swallowed beforehand. 2 g of the powder produce a calm after about 30 minutes
Serenity; approx. 5 g of the powder is an anxiolytic dose, with higher doses it can lead to stronger effects (euphoria,
visions) come (SMITH et al. 1996: 126f.).
The crushed plant material can also be smoked pure or mixed with Cannabis sativa (see Smoking Mixtures).
The finely ground powder is said to have been snorted pure or mixed with tobacco (cf. snuff powder).
These and other species have been used as psychoactive additives to beer or to induce fermentation (SMITH et al.
1996:127).
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ingredients
The leaves and stems of the plant contain 0.3 to 0.86% mesembrine (chemical formula C17H,3N03), as well as some
mesembrinine and tortuosamine (SMITH et al.). It also seems to have oxalic acid in the leaves (FROHNE and JENSEN
1992: 1250. It would also be possible that tryptamines occur in the plant.
After all, is in one to the same family
belonging, closely related Delosperma sp. Methyltryptamine (MMT) and NNDMT have been detected (SMITH et al. 1996:
124).
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Effect
South African users cite relief from anxiety and stress as important effects of small doses of Kougoed,
Deepening of social contacts, increase in self-confidence, release from inhibitions and feelings of inferiority.
»Some reported euphoria as well as a feeling of meditative calm.
Some users looked through Kougoed's
The relaxation produced enables one to focus on inner thoughts and feelings or on beauty
to focus on nature. Some informants spoke of increased skin sensitivity to light touch and of
sexual arousal.« (SMITH et al.
1996: 127f.)
At higher doses, especially in combination with Cannabis sativa and alcohol (whisky), slight visions occur.
Chewing some kougoed shortly after smoking cannabis will greatly potentiate the hemp effects. Both the
Effect of tobacco (Nicotiana tabacum) as well as the need for nicotine is reduced by Kougoed.
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2020 - Sceletium tortuosum (Zembrin®) ameliorates experimentally induced anxiety in healthy volunteers

Abstract Objective: To investigate the anxiolytic properties of a standardized extract of Sceletium tortuosum (trademarked-Zembrin®). Methods: Two studies utilized a placebo-controlled, double-blind, between-subject experimental design to investigate the effects of a single dose of Sceletium tortuosum (25 mg, Zembrin®) on laboratory stress/anxiety responding in 20 young healthy volunteers. To elicit feelings of stress/anxiety, participants completed 20 min of the multitasking framework in study 1 and a 5-min simulated public speaking task in study 2. Study 1 measured subjective experiences of mood at baseline, prestress induction, and poststress induction. Study 2 measured subjective experiences of anxiety and physiological indicators of stress (heart rate
and galvanic skin response) at baseline, prestress induction, during stress induction, and poststress induction. Results: A series of analysis of covariances (baseline entered as the covariate) revealed no treatment effect in study 1; however, study 2 revealed subjective anxiety levels to be significantly lower in the Zembrin® group at the prestress induction point and a significant interaction between treatment and time on HR. Taken together, results indicate that a single dose of Zembrin® can ameliorate laboratory stress/anxiety responding in healthy volunteers. Conclusion: We provide the first tentative behavioral evidence to support the anxiolytic properties of Sceletium tortuosum (25 mg Zembrin®).
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2014 - toxicological safety assessment of a standardized extract of Sceletium tortuosum (Zembrin®) in rats

Discussion and conclusion
The present studies are the first formal in vivo toxicological
studies of an extract of S. tortuosum (Zembrin®) and provide supporting
evidence for the safety and tolerability findings in the first
clinical study (Nell et al., 2013). The repeated administration of
Zembrin® for 90 days by gavage toWistar rats resulted in a NOAEL
of 600 mg/kg bw/day. Applying a 100-fold uncertainty factor to compensate
for inter- and intraspecies differences, results can be
extrapolated to an acceptable daily intake of 420 mg by a 70 kg
human. Zembrin® is intended to be used as an ingredient in functional
foods, beverages, and dietary supplements. The recommended
consumption is 25 mg per day. This is 0.357 mg/kg bw/day in a 70 kg
adult, which is 1680 times less than the NOAEL of 600 mg/kg bw/
day. The indigenous classification as a mak, or mild variety, of the
S. tortuosum variety selected for extraction of Zembrin® is supported
by our findings that there were no changes in central nervous
system signs, behavior, activity, weight, or food intake at any of the
doses studied.
In previous safety assessments (Harvey, 2008, unpublished;
Jurkowski, 2008, unpublished), we observed that =100 µg/mL of
Zembrin® had no effect on severalmammalian cell lines and did not
cause genotoxicity in vitro, as revealed by assays for induction of
micronuclei in CHO-K1 and V79 cells, or bacterial reversion in an
Ames test. At 10 µg/mL Zembrin® did partly reduce K+ currents
through hERG channels in whole cell patch clamp experiments although
this concentration is unlikely to be achieved in vivo.
A small series of clinical case studies of subjects who ingested
daily amounts of 50–100 mg of uncharacterized milled S. tortuosum
raw material reported positive findings on mood and feelings of
anxiety (Gericke, 2001), and an in vivo study of an uncharacterized
extract of S. tortuosum in rats demonstrated a positive outcome on
the behavioral effects of restraint stress (Smith, 2011). Positive effects
on well-being, including improved stress coping and improved sleep,
were noted in patient diaries by some participants taking extract
S. tortuosum (Zembrin®) in the first clinical study of this extract (Nell
et al., 2013). A recent double-blind placebo-controlled cross-over
pharmaco-fMRI study of a single 25 mg dose administration of
Zembrin® in healthy university students demonstrated significant
attenuation of amygdala reactivity to fearful faces under low
perceptual load conditions and reduced amygdala–hypothalamus
coupling (Terburg et al., 2013).
The above clinical and preclinical results support the suggested
potential of Zembrin® as beneficial to promotion of a sense
of emotional well-being, calming effect, and stress relief. The present
in vivo toxicological studies on Zembrin®, together with the clinical
evidence of safety and tolerability (Nell et al., 2013) and our
unpublished in vitro safety studies, provide a foundation for future
studies designed to evaluate health-promoting applications of extract
S. tortuosum (Zembrin®) in functional foods, beverages, and dietary
supplements.
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2011 - Pharmacological actions of the South African medicinal and functional food plant Sceletium tortuosum and its principal alkaloids

a b s t r a c t
Ethnopharmacological relevance: The South African plant Sceletium tortuosum has been known for centuries
for a variety of traditional uses, and, more recently, as a possible source of anti-anxiety or
anti-depressant effects. A standardised extract Zembrin® was used to test for pharmacological activities
that might be relevant to the ethnopharmacological uses, and three of the main alkaloids were also
tested.
Materials and methods: A standardised ethanolic extract was prepared from dried plant material, along
with the purified alkaloids mesembrine, mesembrenone and mesembrenol. These were tested on a panel
of receptors, enzymes and other drug targets, and for cytotoxic effects on mammalian cells.
Results: The extract was a potent blocker in 5-HT transporter binding assays (IC50 4.3 g/ml) and had powerful
inhibitory effects on phosphodiesterase 4 (PDE4) (IC50 8.5 g/ml), but not other phosphodiesterases.
There were no cytotoxic effects. Mesembrine was the most active alkaloid against the 5-HT transporter
(Ki 1.4 nM), while mesembrenone was active against the 5-HT transporter and PDE4 (IC50’s < 1 M).
Conclusions: The activity of the Sceletium tortuosum extract on the 5-HT transporter and PDE4 may explain
the clinical effects of preparations made from this plant. The activities relate to the presence of alkaloids,
particularly mesembrine and mesembrenone.
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2014 - Effects of Sceletium tortuosum in rats

Abstract
Ethnopharmacological relevance: Broad historical and current uses in addition to diverse activity on CNS targets may make Sceletium tortuosum a useful therapeutic in a variety of clinical settings. This study sought to more broadly characterize activity of Sceletium tortuosum and mesembrine in a number of common, rodent-based assays that model nociception, depression, anxiety, ataxia, and abuse liability.
Materials and methods: Male Sprague-Dawley were administered Sceletium tortuosum extract products and behavioral responses were evaluated in the conditioned place preference (CPP), hot plate, forced swim, elevated plus, and rotarod tests.
Results and conclusions: Sceletium tortuosum does not cause preference or aversion in CPP. Mesembrine appears to have analgesic properties without abuse liabilities or ataxia. The Sceletium tortuosum fraction has antidepressant properties but does produce ataxia. The ataxia may limit its usefulness as an antidepressant unless the antidepressant activity is associated with one constituent and the ataxia is associated with a separate constituent.
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2016 - High-mesembrine Sceletium extract (Trimesemine™) is a monoamine releasing agent, rather than only a selective serotonin reuptake inhibitor

Abstract
Ethnopharmacological relevance: Extracts from and alkaloids contained in plants in the genus Sceletium have been reported to inhibit ligand binding to serotonin transporter. From this, the conclusion was made that Sceletium products act as selective serotonin-reuptake inhibitors. However, other mechanisms which may similarly result in the anxiolytic or anti-depressant effect ascribed to Sceletium, such as monoamine release, have not been investigated.
Aims of the study: The current study investigated simultaneously and at two consecutive time points, the effect of high-mesembrine Sceletium extract on both monoamine release and serotonin reuptake into both human astrocytes and mouse hippocampal neurons, as well as potential inhibitory effects on relevant enzyme activities.
Materials and methods: Human astrocytes and mouse hippocampal cells were treated with citalopram or Sceletium extract for 15 and 30min, after which protein expression levels of serotonin transporter (SERT) and vesicular monoamine transporter-2 (VAMT-2) was assessed using fluorescent immunocytochemistry and digital image analysis. Efficacy of inhibition of acetylcholinesterase (AChE) and monoamine oxidate-A (MAO-A) activity were assessed using the Ellman and Olsen methods (and appropriate controls) respectively.
Results: We report the first investigation of mechanism of action of Sceletium extract in the context of serotonin transport, release and reuptake in a cellular model. Cell viability was not affected by Sceletium treatment. High-mesembrine Sceletium extract down-regulated SERT expression similarly to citalopram. In addition, VMAT-2 was upregulated significantly in response to Sceletium treatment. The extract showed only relatively mild inhibition of AChE and MAO-A.
Conclusions: We conclude that the serotonin reuptake inhibition activity ascribed to the Sceletium plant, is a secondary function to the monoamine-releasing activity of high-mesembrine Sceletium extract (Trimesemine(TM)).
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really good:

2016 - Mesembrine Alkaloids Review of their Occurrence, Chemistry, and Pharmacology



5 Conclusions
While the pharmacology and mechanism(s) of action for the behavioral effects of the individual
mesembrine alkaloids and preparations containing mixtures of these alkaloids is not entirely clear, it is
evident from in vitro, in vivo, and clinical studies that the main mesembrine alkaloids are bioavailable
CNS-active materials worthy of further study. One current limitation is the lack of commercially available
pure substance and reference materials. Despite the broad screening of an mesembrine alkaloid
mixture followed by testing of the individual alkaloids against the positive hits from the mixture (Harvey
et al., 2011), it would still be of value to broadly screen (affinity and functionality) the individual
alkaloids to better understand their functional activity and selectivity in addition to their potency.
Seldom are CNS drugs completely selective for one target. From the standpoint of developing these
materials or their analogs into therapeutic agents, considerably more study is needed concerning the
ultimate safety of these alkaloids and alkaloid mixtures. Additionally a competitive threat exists from
non-mesembrine compounds that select for the same or multiple CNS targets, such as the dual
serotonin reuptake inhibitors having PDE4 inhibitory activity that have been reported (Cashman and
Ghirmai, 2009; Cashman et al., 2009a, 2009b).
However, from an herbal product perspective, where the safe and effective threshold of a
pharmaceutical product does not need to be met, the trials using standardized commercial preparations
are quite helpful in addressing the issues of safety and tolerability needed for an herbal product. As with
all natural product preparations, QA/QC for the delivery of a consistent product with predictable
biological effects is a considerable challenge. Another issue for the non-prescription use of these
particular preparations is the significant potency as a serotonin reuptake inhibitor. Inappropriate use of
the product or use in combination with other antidepressants or herbal products might lead to serious
interactions or serotonin syndrome. If these products ever see more widespread marketing, then it
would be a priority to address these real possibilities.
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full synthesis of Mesembrine:

2019 - Mesembrine The archetypal psycho-active Sceletium alkaloid
 
2013 - Acute Effects of Sceletium tortuosum (Zembrin), a Dual 5-HT Reuptake and PDE4 Inhibitor, in the Human Amygdala and its Connection to the Hypothalamus

The South African endemic plant Sceletium tortuosum has a long history of traditional use as a masticatory and medicine by San and
Khoikhoi people and subsequently by European colonial farmers as a psychotropic in tincture form. Over the past decade, the plant has
attracted increasing attention for its possible applications in promoting a sense of wellbeing and relieving stress in healthy individuals and
for treating clinical anxiety and depression. The pharmacological actions of a standardized extract of the plant (Zembrin) have been
reported to be dual PDE4 inhibition and 5-HT reuptake inhibition, a combination that has been argued to offer potential therapeutic
advantages. Here we tested the acute effects of Zembrin administration in a pharmaco-fMRI study focused on anxiety-related activity in
the amygdala and its connected neurocircuitry. In a double-blind, placebo-controlled, cross-over design, 16 healthy participants were
scanned during performance in a perceptual-load and an emotion-matching task. Amygdala reactivity to fearful faces under low
perceptual load conditions was attenuated after a single 25 mg dose of Zembrin. Follow-up connectivity analysis on the emotionmatching
task showed that amygdala–hypothalamus coupling was also reduced. These results demonstrate, for the first time, the
attenuating effects of S. tortuosum on the threat circuitry of the human brain and provide supporting evidence that the dual 5-HT
reuptake inhibition and PDE4 inhibition of this extract might have anxiolytic potential by attenuating subcortical threat responsivity.
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paper roll:

2008 - Review on plants with CNS-effects used in traditional South African medicine against mental diseases.pdf
2011 - Pharmacological actions of the South African medicinal and functional food plant Sceletium tortuosum and its principal alkaloids.pdf
2012 - A Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Trial of Extract Sceletium tortuosum (Zembrin) in Healthy Adults.pdf
2013 - Acute Effects of Sceletium tortuosum (Zembrin), a Dual 5-HT Reuptake and PDE4 Inhibitor, in the Human Amygdala and its Connection to the Hypothalamus.pdf
2014 - Effects of Sceletium tortuosum in rats.pdf
2014 - toxicological safety assessment of a standardized extract of Sceletium tortuosum (Zembrin©) in rats.pdf
2015 - A review of commercially important African medicinal plants.pdf
2016 - High-mesembrine Sceletium extract (TrimesemineT) is a monoamine releasing agent, rather than only a selective serotonin reuptake inhibitor.pdf
2016 - Mesembrine Alkaloids Review of their Occurrence, Chemistry, and Pharmacology.pdf
2019 - Mesembrine The archetypal psycho-active Sceletium alkaloid.pdf
2020 - Pharmacology of Herbal Sexual Enhancers A Review of Psychiatric and Neurological Adverse Effects.pdf
2020 - Sceletium tortuosum (Zembrin©) ameliorates experimentally induced anxiety in healthy volunteers.pdf
2021 - A Chewable Cure "Kanna" Biological and Pharmaceutical Properties of Sceletium tortuosum.pdf
 
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