Alchemica
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Posts posted by Alchemica
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I've been interested in this plant as a potential pro-cognitive but wonder if it could also have merits in augmenting plant medicines.
Convolvulus plauricalis (Shankpushpi) has nootropic, neuroprotective, anti-depressant, anti-stress, anti-inflammatory, anti-oxidant, anti-convulsant, anxiolytic, analgesic, spasmolytic, aphrodisiac, sedative, anti-Alzheimer's, and anti-Parkinson’s activity.
The most notable constituents are tropane alkaloids. Only convolamine has been identified, but other alkaloids (convoline, convolidine, convolvine, confoline, convosine, etc) found in other species from this family are probably present. Convolamine is a potent positive
modulator of the sigma-1 receptor [1] Scopoletin, kampferol and β-sitosterol were also found in significant amountsWhile I'm interested in the neuroprotective, pro-cognitive effects, the action of sigma-1 positive modulation makes me ponder if it may be an effective novel admixture - σ1R modulation seems to have a useful therapeutic augmentation effect of serotonergics etc and it's often used as a polyherbal remedy.
[1] Crouzier L, Meunier J, Carles A, Morilleau A, Vrigneau C, Schmitt M, Bourguignon JJ, Delprat B, Maurice T. Convolamine, a tropane alkaloid extracted from Convolvulus plauricalis, is a potent sigma-1 receptor-positive modulator with cognitive and neuroprotective properties. Phytother Res. 2024 Feb;38(2):694-712. https://doi.org/10.1002/ptr.8068.
[2] Balkrishna A, Thakur P, Varshney A. Phytochemical Profile, Pharmacological Attributes and Medicinal Properties of Convolvulus prostratus - A Cognitive Enhancer Herb for the Management of Neurodegenerative Etiologies. Front Pharmacol. 2020 Mar 3;11:171. https://doi.org/10.3389%2Ffphar.2020.00171
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6 hours ago, fyzygy said:
In that case I'll definitely be hunting for roots. Do mesembrine alkaloids (like SSRIs) inhibit the effects of other psychoactive plant medicines? Or would they (like MAOIs) potentiate them? I have my suspicions, but wonder what others might be able to report.
I haven't personally explored combinations but I've in a limited way heard of 'useful' potentiation of 5-HT1A/2A agonists but one would want to be cautious re adverse interactions. Definitely wouldn't combine with MAOIs. Mesembrine seems very atypical as a SSRI, if it is even one [1]. Depending on the alkaloid profile, it may be more a monoamine releaser through VMAT2 etc and different studies have pointed to that effect. Coupled with the PDE4 inhibition it may "enhance 5-HT2AR signaling by increasing cAMP levels"
[1] https://doi.org/10.1016/j.jep.2015.11.034 -
Roots may be a more interesting option, that's where the researchers have been looking for antidepressant potential.
It's undisputedly much milder and requires higher doses but given it has traditional use as an anxiolytic and anti-inflammatory (Garden of Eden), it's got some potential merits if other options are less available. Keep in mind it's devoid of mesembrine, initial results that it had 13.6% the mesembrine of Sceletium were later disputed, instead has other alkaloids
1.8g alkaloid was obtained from 250g of dried roots. Considering 100mg/kg alkaloid fraction i.p. was found to be antidepressant in rats [1], which may be excessive, ~16mg/kg may potentially be needed for human antidepressant effects. 4,5-dihydro-4'-O-methylsceletenone and 4'-O-methylsceletenone were the dominant alkaloids in the root @ 0.235%, stems had ~ 0.1% [2].
Said, A. A. E., Ali, T. F. S., Attia, E. Z., Ahmed, A. S. F., Shehata, A. H., Abdelmohsen, U. R., & Fouad, M. A. (2020). Antidepressant potential of Mesembryanthemum cordifolium roots assisted by metabolomic analysis and virtual screening. Natural Product Research, 35(23), 5493–5497. https://doi.org/10.1080/14786419.2020.1788019
A study of Mesembryanthemaceae alkaloids (2006) Candice Delphine Gaffney https://def-sa.com/wp-content/uploads/2020/08/Gaffney_Candice_D_2006_0.pdf
aptenia | PDF Host -
Keen to hear people list off dietary/nutritional interventions they've found benefit from for mental or cognitive health. Trying to write up a more comprehensive list than what I can currently find elsewhere, early days let me know if you think of other additions
https://1drv.ms/x/s!AiE8pZSRNVehlH63pwhJE5ags31C?e=y8b8zy-
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Found this to be a good review. Not suggesting self-medication using plants as a standalone to replace conventional pharmacotherapy but particularly think it may have some merits as adjunctive treatment, particularly if one sticks with more benign phytochemicals in line with more dietary-type modifications etc
Alternative Therapy of Psychosis: Potential Phytochemicals and Drug Targets in the Management of Schizophrenia
https://doi.org/10.3389/fphar.2022.895668
Anti-schizophrenic drugs have variable efficacy in different patients, with often poor efficacy and sometimes with debilitating side-effects. There is a great need of more efficacious and safer remedies. Phytochemicals offer potential and diverse alternatives to allopathic anti schizophrenic medicines due to their wide array of biological activities such as anti-inflammatory activity, anti-oxidant potential, affecting neurotransmission, and modulating cell signaling pathways
Possible factors?
- genetic and environmental factors, prenatal infections
- neurochemical factors (dopamine, gamma-aminobutyric acid (GABA) and glutamate, serotonin and noradrenaline
- interplay of neuro inflammation, oxidative stress, cell signaling pathways and abnormal immune system activation
Phytochemicals playing a beneficial role?
- Phytochemicals showing efficacy against schizophrenia belong to different phytochemical classes such as alkaloids, tannins, glycosides, phenolic acids, flavonoids, terpenes, terpenoids and essential oils. -
Best talking with your Dr but as an adjunct, not to be considered medical advice:
Omega-3's seem pretty mood stabilising in most studies "sources state that omega-3s may have a mood stabilising effect and help with short-term symptoms of bipolar disorder"
Dietary ketosis seems very stabilising, maybe could add some MCTs to your diet if you can't go full keto
Lithium is natural, while high doses are only good suggested under medical supervision, some people find low dose lithium orotate can have some benefits
N-acetyl-cysteine seems to have some 'leveling effects' and evidence for it's use in diverse mental health conditions
5-HTP or tryptophan might level out some emotional volatility
If it's anxious distress, maybe something like oral lavender oil capsules you can get at the chemist which has similar levels of effect size on such as SSRIs and BZDs
I found L-tetrahydropalmatine leveling
Something like theanine? Taurine, Glutamine etc. Calming herbs. Whole range of more calming things out there that might dampen excitatory neurotransmission a bit for you
Considered something like inositol? You need quite high doses and the level of evidence as a mood stabiliser isn't great but it's benign
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5 hours ago, saguaro said:
What is meant by interact with native double helical DNA in this instance? As far as I'm aware MTXs aren't mutagens, MTX actions should be accounted for by acute signalling mechanisms and effects on transcription.
They "... interact with all the base pairs of DNA (A-T; G-C) and phosphate group through hydrogen bond (H-bond) interaction." Probably similar to things like beta-carbolines that interact in the way below. Other ones like coralyne and berberine also form a complex with DNA, probably by intercalation, giving rise to therapeutic effects in things like cancer.
Johnson, I.M., Prakash, H., Prathiba, J., Raghunathan, R., Malathi, R. Spectral analysis of naturally occurring methylxanthines (theophylline, theobromine and caffeine) binding with DNA. PLoS One 2012, 7, e50019. https://doi.org/10.1371/journal.pone.0050019
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Anyone used theobromine for a sustained period and found it useful for attention deficits? The cacao flavonols would likely be synergistic over theobromine alone
It's only an animal model study so far but potentially an option
Theobromine improves hyperactivity, inattention, and working memory via modulation of dopaminergic neural function in the frontal cortex of spontaneously hypertensive rats
https://doi.org/10.1039/D4FO00683F
While it has a nonselective PDE inhibition effect greater than caffeine, oral theobromine inhibits mTOR signalling in vivo which is of relevance to multiple conditions [1] and elevates cerebral brain-derived neurotrophic factor and facilitates learning in animal models [2] and orally supplemented, it upregulates the pathways in the mPFC, which may then improve working memory in animal models [3].
MTXs act through a variety of different molecular mechanisms: mobilization of intracellular calcium, inhibition of phosphodiesterases (PDEs), modulation of gamma-amino butyric acid (GABAA) receptors, inhibition of high affinity ATP-dependent cyclic nucleotide transporters and antagonism of adenosine receptors. The plasma levels that could be reached under dietary regimes and the fact that MTXs readily cross the blood-brain barrier indicate that these drugs inhibit adenosine receptors in the CNS; higher doses may be required to mobilize intracellular calcium, inhibit PDEs or modulate GABAA receptors, or to unselectively inhibit ABCC5 and ABCC4 transporters. Moreover, despite the physiological relevance, also under scrutiny is how caffeine, theobromine and theophylline are able to interact with native double helical DNA
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On 02/05/2024 at 4:58 PM, fyzygy said:
What is an easy source of pinene terpenes?
Theres Aus shops like this Home - My Terpenes Australia
For pinenes, I tend to use frankincence essential oil unless you can get the pure terpene - ~30-60% α-pinene. There seems to be different enantiomers in different oils which needs to be taken into account. Even between B. carterii and B. sacra there seems to be different pinene enantiomers.
α-pinene: anti-inflammatory via PGE1, acetylcholinesterase inhibitor - aiding memory, positive modulator of GABAA receptors at BZD sites. α-pinene was observed to initiate soothing physiological and behavioural responses with a significant impact on physiological and psychological relaxation.
(1R)-(+)-α-pinene was more prevalent than (1S)-(−)-α-pinene in pine oils
(+)-α-Pinene was the predominant enantiomer in most rosemary, this is intriguing as (-)-α-pinene displays partial modulation of GABAA-BZD receptors and direct binding to the BZD binding site of GABAA receptor while the (+)- enantiomer is less characterised.
α-Pinene shows anti-metastatic and anti-tumor activities. Moreover, it seems to be anti-inflammatory, anti-oxidant and an anti-allergic bronchodilator and can produce anxiolytic and hypnotic effects via the GABAergic system (α-PN shows anxiolytic and hypnotic effects upon inhaled administration. α-PN evokes its hypnotic action through direct binding to GABAA as a partial modulator at the benzodiazepine binding site
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I've played around a bit with terpenes/Citrus oils, even making a transdermal spray. I find they get more interesting as synergistic blends.
Komiya and colleagues (2006) observed that lemon oil vapor inhalation causes an anti-stress effect by modulating serotonergic and dopaminergic in addition to GABAergic systems in mice. Limonene enhances neurotransmitter release and could inhibit HPA activity under physical stress, It may act via regulating dopamine levels and 5-HT receptor function, along with GABAA activity.
Citrus essential oils have been utilised widely in traditional medicine"Improvements in neuroendocrine, neurotrophic, and monoaminergic systems are related to the antidepressant effects of limonene". It produces antidepressant-like effects that seems to be mediated by 5-HT and dopamine neurotransmission and is an agonist for adenosine A(2A) receptors.Lemon essential oils showed strong ability to improve memory in animal modelsIt is suggested "metabolites of these monoterpene compounds contained in citrus essential oils have a stronger effect on monoamine release from brain tissue than the monoterpene compounds themselves"
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3 minutes ago, fyzygy said:
I've been propagating this for a while now, but have no experience with consumption. How does it taste? Grows well from cutting, but not from seed, in my (limited) experience.
No experience with consumption myself either but maybe I need to expel some bad spirits....-
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Doing lots of cuttings of this at the moment, if someone wants to grow it get in touch here. No WA/TAS.
QuoteThe traditional healers use Iresine herbstii with the ritual aim to expel bad spirits from the body. Furthermore, Iresine herbstii was used in association with other plants, such as Trichocereus pachanoi, for divination, to diagnose diseases, and to take possession of another identity.
Tea has been prepared from the leaves, rich in antioxidants.
Iresine herbstii (Amaranthaceae), traditionally called “cimora se˜ norita”, is used in black magic (De Feo, 2003) and in association with San Pedro for magic rituals (Friedberg, 1959; Dobkin De Rios, 1977; De Feo, 2003), to diagnose illness, and to take possession of another identity (Cruz-Sanchez, 1948). Its leaves are claimed, for external use, a skin depurative, whereas the aerial part decoction is known to be an antipyretic (De Feo, 2003).
- anti-inflammatory, cytotoxic and apoptotic activities and antioxidant activity
- affinity for the 5-HT1AR
- affinity for 5-HT2C receptor and for D1 receptor (MeOH extract)
- lower affinity for D1 and higher affinity for D2 receptors (Aq. extract)
- presumable antagonist action on D1 and D2 receptors by Iresine (both extracts)Leaves: 2,5-Dimethoxy-6,7-(methylenedioxy)-isoflavone; acylated betacyanins
Roots: oleanolic acid and its saponins. An alcoholic extract of the root showed the presence of amino acids, steroids, triterpenoids, alkaloids and coumarins.
https://doi.org/10.1016/j.jep.2005.11.022
https://doi.org/10.1076/phbi.34.3.184.13212
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On 29/03/2024 at 8:00 PM, Alchemist said:
Galantamine is the real deal for lucid dreams. It worked again last night.
Unfortunately the more easily available huperizine A is useless for me. Took up to 400 mcg and simply felt weird the next day.
DMAE , 50mg eq. freebase for a week did nothing for dreams either.
Calea has done nothing in the past, but I never took it after sleeping for 4 hours first , like needs to be done for galantamine. So I will be giving that a go in a few days, after the G has cleared from the system.
Galantamine is interesting as it functions as both an AChE inhibitor and positive allosteric modulator of a7-nAChRs, I found it quite cognitively interesting but wasn't looking for lucid dreams. On the contrary, huperzine A seems more to be AChE/NMDARs.
Your DMAE dose seems personally quite low but I can see there being challenges using it with sleep as some people find it activating. As the bitartrate 250mg-500mg may be more typical, eq, dimethylaminoethanol freebase ~186mg at the upper dose.
Out of interest, have you explored something like CDP-choline as a cholinergic? It seems to have procognitive effects mediated by predominately a7-nAChR activation. More recently there's been interest in coupling AChE inhibition with CDP-choline or alpha-GPC for dementias and that seems to be an effective augmentation, so perhaps that could be possible to cautiously augment huperzine A with such, in theory.
I have some Silene undulata 98% triterpenoid saponins extract from the SAB store, if you want a bit in an envelope no cost send me a PM. It didn't get as frothy as expected (presumptive test for saponins) but did form a lasting sort of foam to some extent.
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There's been a bit of research into fermentation of different plants with either lactic acid bacteria or yeasts. I've tried to summarise a bit of it here
The Science of Fermented Fruits, Veggies and Plant Medicines - Pharmacology, Chemistry & Medicine - The Corroboree (shaman-australis.com)The bacteria and yeasts are in a way potentially mildly psychoactive, hence their often-termed action as "psychobiotics". I've only tried milk kefir, which is interesting in it's own way, as the kefir peptides are too mildly psychoactive but you're right, fermenting a plant into the mix is an interesting concept and worth exploring more.
There's the classic example of Sceletium which I've tried to explore here with yeasts
yeasts to encourage bioconversion.pdf
QuoteAlongside the nutritional and psychobiotic effect, a diversity of peptides from casein are released by kefir including at least 5 opioid peptides. Opioid effects have been also reported following oral administration of casein hydrolysates. The peptides may exhibit anxiolytic-like and cognition enhancing activities. Kefir peptides may also act as anti-oxidants, immunomodulators and anti-obesity agents
Let us know if you do any experimenting
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Stuck with this for awhile and there's been the slow but gradual return of some seemingly simple cognitive functions when used catalytically with effort and attempting to retrain my mind.
For example, I was unable to sit and watch something as simple as a short youtube clip and follow the video. I've lately got back into watching inspirational short videos that I'm enjoying and can now watch something like a 30min clip which was previously totally unfeasible. I've started to embrace the need to do a lot more simple cognitive remediation in my day, for example getting back into colouring in an adult colouring books etc as an activityIt hasn't all been linear for recovering some levels of very basic functionality, the cognitive fatigue associated with essentially retraining and forging some new connections of some basic cognitive functions has been extreme and literally left me floored and sometimes come at the expense of maintaining functionality in other domains.
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There seems to be several factors that limit berberine's bioavailability to the <1% mark:
- poor absorption
- extensive metabolism
- efflux back to the intestinal lumen by the action of permeability glycoprotein (P-glycoprotein, P-gp)
As piperine from black pepper works on the cytochrome metabolism and P-gp level, it may very well be worth considering but haven't seen it done
Things that have been studied are detailed here
the phospholipid-berberine complexes including things like encapsulating it in lecithin seem to have some significant effects on bioavailability in studies but wasn't able to personally tell how effective it was, lets just say I had lots of experiments happening.
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12 hours ago, Ishmael Fleishman said:
Has anyone used Berberine and to what effect?
Thanks for the writeup.
I explored a long time ago, also made up a mix of berberine hydrochloride with lecithin trying to improve it's bioavailability and was interested in it's CNS effects and beneficial metabolic effects, the CNS effects particularly related to it's sigma-1 agonism, prolyl oligopeptidase activity and monoaminergic effects
Berberine may offer benefit in the control of psychotic and depressive symptoms, along with metabolic side effects. It has a broad range of CNS relevant pharmacological actions, including sigma-1 agonism, acetylcholinesterase inhibition and a range of neuroprotective effects including neurotrophin-mediated neuroprotection (NGF). There are some limitations to its use, including bioavailability and difficulties in reaching active levels in the CNS. “The potential use in schizophrenia was suggested when berberine was found to act as a D2-receptor antagonist, although it was also noted that dopamine level was increased in the brain as partly responsible for its antidepressant mechanism. It is unclear if these influences on dopamine level and action may counter each other, diminishing the proposed antipsychotic effect. Future studies may also elucidate whether berberine will exacerbate extrapyramidal motor symptoms due to the blockade of D2 receptors. On the other hand, it was proposed that the anxiolytic effect of berberine resulted from its antagonism at 5-HT2 receptor. This finding may indicate less severe motor side effects, if there are any, when berberine is used as an antipsychotic since atypical antipsychotics also act via 5-HT2 receptor blockade. A possible advantage of berberine over other antipsychotics is its ability to inhibit prolyl oligopeptidases, the activity of which is elevated in psychosis and not targeted by antipsychotics at present.”
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1 hour ago, fyzygy said:
Sounds promising. I hope the positive effects increase over time.Which Acorus species (and plant parts) have you been concentrating your efforts on?
I'm just using a likely high asarone Acorus calamus essential oil. I don't want to make it a long-term addition but something to get out of a rut. Early days but small subjectively useful shifts, combined with little lifestyle shifts when I can seem to help slightly. I get very rigid in my routines and behaviours, so if this is a way to potentially plasticise my mind and behavioural repertoire a bit that could be good
QuoteWould sub-lingual also work while avoiding toxic effects?
That could be useful and possibly minimise toxicity? I know some people simply chew the calamus rhizome, that seems to be the suggested way to use the Japanese Sweet Flag SAB sells for stimulant effects. This intranasal spray is a bit more full on with quite significant levels of asarone which I think would be hard to reach via plain herb
QuoteVariegated sweet flag, I think you mentioned that it had been traditionally used among Japanese to treat stuttering?
Yeah that one's Acorus gramineus, it's got a diverse range of constituents that have interesting pharmacology aside from asarones. Still, whilst it seems to have quite prominent TCM use etc, I'd probably stick with chewing it etc as you mention
My notes on A. gramineus
QuoteAcorus gramineus is a traditional medicine used to treat various disorders including cognitive disorders where of all the traditional Chinese medicines used in treating cognitive disorders, the rhizome appears with the highest frequency. In TCM it has an action of "calming heart and inducing tranquilisation"It contains β-asarone, α-asarone and other phenylpropenes as well as lignans, along with aporphine-type alkaloids with the essential oil having NMDA receptor antagonist-like action and possibly increases NE, DA and 5-HT, also decreasing the activity of acetylcholinesterase. A water extract demonstrated specific binding to striatal dopamine D1 and D2 receptors and competed with [3H]muscimol for specific binding to the GABA binding site of cortex GABAA receptor-
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A few days in and perhaps the most robust change has been with potential anti-addictive activity, for me being able to say no to smoking which resurged recently and I wasn't able to get on top of (EDIT less sustained anti-addictive potential than I'd hoped). The regulation of neurotrophins, particularly GDNF [1], seems to have quite profound effects on addictive processes, the GDNF pathway implicated in the anti-addictive action of things like ibogaine. Some stability in mood developed over the extreme negative mood states and even some uplift, whilst still having profound motivational deficits and ability to initiate and maintain goal-directed activity. Been trying to have glimmers of sustained attention to focus on tasks like watching short bursts of movies or TV shows which is still incredibly challenging
As the administration via intranasal pathways directly into the olfactory bulb is likely to target the neurotrophic activity directly into the OFC and frontal lobes, it interests me how it could impact severe hypofrontality [2] particularly with regard to OFC functioning where damage can cause neurobehavioural issues
For a long time I've been walking around like a headless chook with aberrant motor functions, this seems to reduce the 'headless chook' wandering a bit
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Thanks for your input and kind words DL. Hope you get some improvement of your residual symptoms.
Initially there's not much robust acute improvement but symptoms were severe at baseline so not expecting quick results. If anything perhaps some destabilisation of mood etc but I sometimes feel that can be a part of the 'solve et coagula' of life. I particularly wonder if, as a significant portion of my symptoms was through an inhalation suicide attempt, this might be a very direct way to target the damaged pathways, particularly into the OFC, quite directly.They did some research using aromatherapy for inhalant abuse, this is like the next level up, intranasal aromatherapy.
A novel approach of substitution therapy with inhalation of essential oil for the reduction of inhalant craving: A double-blinded randomized controlled trial -
Very limited availability of these two
Mind Mend Cognitive Blend
https://pdfhost.io/v/wIuDteWuV_mind_mend
Polyphenol blend
https://pdfhost.io/v/2XXhGA8me_polyphenol_blend-
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I have a small quantity of research material left over from my brief TLC study on it, if anyone is curious to do any complimentary research on it let me know. There are no studies I can find on possible alkaloid constituents yet.
Heteropterys angustifolia - A preliminary TLC study
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Nose-to-brain delivery of asarones for CNS conditions?
Ayurvedic medicine and traditional Chinese medicine (TCM) use Acorus preferably to treat central nervous system (CNS) related diseases such as epilepsy, insanity, mental weakness, or insomnia, Calamus has been widely used internally in both Chinese and Ayurvedic medicine for degenerative central nervous system disorders associated with communication, focus, memory and learning but there are concerns regarding the safety of such orally.The ability of asarones to induce such a broad range of neurotrophic factors (NGF, BDNF, GDNF, CNTF in a dose-dependent manner), alongside other neuroprotective and neurorestorative pharmacological actions, intrigues me.
Pharmacologically, α- and β-asarone at lower doses (<50 mg/kg) exhibits a wide range of therapeutic activities such as antidepressant, antianxiety, anti-Alzheimer, and anti-Parkinson effects [1].Asarones as a therapeutic are limited by poor absolute bioavailability when administered orally, less than 10%, because it is highly lipophilic and has poor solubility in water, coupled with extensive gastrointestinal and/or hepatic first-pass metabolism.
There are concerns potentially harmful effects, such as genotoxicity particularly through accumulation in the liver where "both α- and β-asarone can cause hepatomas and might possess mutagenic, genotoxic, carcinogenic, and teratogenic effects". Because the amounts of asarone accumulated in liver may reflect its hepatotoxicity, there is special significance to reducing the amount of asarone in liver.
Quote"The development of more efficient systems to deliver α- and β-asarone to their biological targets, particularly the brain, might allow for effective localized biological action while minimizing toxicity."
Efforts have been centred on exploring nose-to-brain delivery of asarones, particularly as nanoemulsions [1,2] In humans, 20mg asarone has been added to memantine for AD [3]
Quote"Drugs can travel from the olfactory epithelium in the nasal cavity straight into brain tissue via the olfactory bulb which gives intranasal administration special significance for brain diseases"
"...intranasal administration of asarone showed significant nose-to-brain transport, especially in the olfactory bulb, and such treatment yields equivalent or higher concentrations in other brain tissues compared to intravenous or oral administration"
I'm personally curious as to whether a simple spray of asarones emulsified in water with a polysorbate emulsifier, delivered via a nasal spray bottle may be simple enough to make a readily available nose-to-brain delivery system "polysorbates [are] a promising excipient to increase drug concentration in both plasma and brain via intranasal route".The main beneficial actions of asarones, as described by [1], are summarised as:
" (1) antioxidant properties; (2) the regulation of various neuroprotective signaling pathways; (3) the reduction of aggregate formation and promotion of the clearance of pathogenic protein aggregates; (4) anti-inflammatory properties; (5) the inhibition of microglial activation; (6) the activation of NTFs-mediated neuroprotection; and (7) the modulation of neurotransmitter levels associated with behavioural functions and neuronal cell survival."
Actions of asarones on the CNS, taken from [1]
Normal vs diseased brain aspects
Asarone functions as a neuroprotective effect in both in vivo and in vitro models of neurodegeneration- Enhance BDNF via TrkB and activate the ERK pathway, triggering antidepressant-like effects
- Significantly promoted the expression and secretion of neurotrophins, such as nerve growth factor (NGF), BDNF, and GDNF, in a dose-dependent manner. Also effects on CNTF
- Maintain equilibrium between glutamate and GABA in the hippocampus, enhancing learning and memory abilities. β-asarone induced the high potentiation of GABAARs
-Anxiolytic effects of asarone were partially due to maintaining the balance between excitatory/inhibitory transmissions and attenuating neuronal hyper-excitability of excitatory neurons in the basolateral amygdala.
- modulates microglial morphological dynamics, may functionally relate to its influence on neurogenesis
- Other monoaminergic effects, particularly antidepressant effects mediated by noradrenergic (α1 and α2 adrenoceptors) and serotonergic (particularly, 5-HT1A receptors) systems.
- Enhances tyrosine hydroxylase activity with relevance to Parkinson'sMy current line of thinking is to make an emulsion of a polysorbate emulsifier with calamus oil 1:1 in water and explore that. Any input appreciated.
1:1:2 Calamus EO:polysorbate solubiliser:saline administered by nasal spray has got quite a strong bit of burn to it but not totally intolerable.
Nasal sprays are normally less than 140uL/spray meaing at 25% EO concentration {assume 80% asarones), about 28mg asarone per spray may be possible. Even at that dose, each spray is quite painful but it may be feasible to - via multiple doses scattered through the day - reach a therapeutic dose of asarones intranasally with such.
References:
Balakrishnan, R.; Cho, D.-Y.; Kim, I.-S.; Seol, S.-H.; Choi, D.-K. Molecular Mechanisms and Therapeutic Potential of α- and β-Asarone in the Treatment of Neurological Disorders. Antioxidants 2022, 11, 281. https://doi.org/10.3390/antiox11020281
Lu, J., Fu, T., Qian, Y., Zhang, Q., Zhu, H., Pan, L., Zhang, M. (2014). Distribution of α-asarone in brain following three different routes of administration in rats. European Journal of Pharmaceutical Sciences, 63, 63–70. . https://doi.org/10.3390/10.1016/j.ejps.2014.06.006Pan L, Zhou J, Ju F, Zhu H. Intranasal delivery of α-asarone to the brain with lactoferrin-modified mPEG-PLA nanoparticles prepared by premix membrane emulsification. Drug Deliv Transl Res. 2018 Feb;8(1):83-96. doi: https://doi.org/10.1007/s13346-017-0438-8.
Dong, Haiying; Wu, Shuqin; Hu, Nan; Xing, Guihua (2018) Efficacy of tenuigenin and β-asarone as augmentations for memantine in the treatment of Alzheimer’s disease https://doi.org/10.1097/WNR.0000000000000952
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Following up with a TLC comparison to Tabernaemontana pandacaqui (Banana Bush) seeds
T. pandacaqui | PDF Host
Sceletium substitutes? Mesembryanthemum cordifolia tests poorly for mesembrine alkaloids ...
in Cacti & Succulents
Posted
Even Lampranthus spp. has been commercially sold as 'Chinese Kanna', so not sure about that?
