Lion's Mane contains kappa agonist
Sciencyst
22 Feb 2014
http://en.wikipedia.org/wiki/Erinacine
Erinacines are isolates of hericium erinaceum (Lion's Mane mushroom).
Erinacine is a kappa opiod receptor agonist.
Erinacines are isolates of hericium erinaceum (Lion's Mane mushroom).
Erinacine is a kappa opiod receptor agonist.
Erinacine Q, a new erinacine from Hericium erinaceum, and its biosynthetic route to erinacine C in the basidiomycete.
Abstract
Erinacines as cyathane-xylosides are known to have potent stimulating activity for nerve-growth-factor synthesis. Our search for new cyathane metabolites from a liquid culture of Hericium erinaceum YB4-6237 resulted in the isolation of a new erinacine named erinacine Q (1). NMR spectrometry and a chemical derivation from erinacine P (2) determined the compound to be a derivative in which the formyl group of erinacine P had been reduced to the hydroxymethyl group. To clarify the biosynthetic relationship between erinacine Q and the others, [1'-13C]erinacine Q ([1'-13C]-1) was chemically derived from [1'-13C]erinacine P ([1'-13C]-2) which had been prepared by feeding [1-13C]-D-glucose to the basidiomycete. The biotransformation of labeled erinacine Q into [1'-13C]erinacine C ([1'-13C]-5) via [1'-13C]erinacine P in this basidiomycete was demonstrated by NMR spectrometry.
→ source (external link)Abstract
Erinacines as cyathane-xylosides are known to have potent stimulating activity for nerve-growth-factor synthesis. Our search for new cyathane metabolites from a liquid culture of Hericium erinaceum YB4-6237 resulted in the isolation of a new erinacine named erinacine Q (1). NMR spectrometry and a chemical derivation from erinacine P (2) determined the compound to be a derivative in which the formyl group of erinacine P had been reduced to the hydroxymethyl group. To clarify the biosynthetic relationship between erinacine Q and the others, [1'-13C]erinacine Q ([1'-13C]-1) was chemically derived from [1'-13C]erinacine P ([1'-13C]-2) which had been prepared by feeding [1-13C]-D-glucose to the basidiomycete. The biotransformation of labeled erinacine Q into [1'-13C]erinacine C ([1'-13C]-5) via [1'-13C]erinacine P in this basidiomycete was demonstrated by NMR spectrometry.
Erinacine E as a kappa opioid receptor agonist and its new analogs from a basidiomycete, Hericium ramosum.
Abstract
A kappa opioid receptor binding inhibitor was isolated from the fermentation broth of a basidiomycete, Hericium ramosum CL24240 and identified as erinacine E (1). Three analogs of 1 were produced by fermentation in other media and by microbial biotransformation. Of these compounds, 1 was shown to be the most potent binding inhibitor. Preliminary SAR studies of these compounds indicated that all functional groups and side chains were required for the activity. Compound 1 was a highly-selective binding inhibitor for the kappa opioid receptor: 0.8 microM (IC50) for kappa, >200 microM for mu, and >200 microM for delta opioid receptor. Compound 1 suppressed electrically-stimulated twitch responses of rabbit vas deferens with an ED50 of 14 microM. The suppression was recovered by adding a selective kappa opioid receptor antagonist nor-binaltorphimine, indicating that 1 is a kappa opioid receptor agonist.
→ source (external link)Abstract
A kappa opioid receptor binding inhibitor was isolated from the fermentation broth of a basidiomycete, Hericium ramosum CL24240 and identified as erinacine E (1). Three analogs of 1 were produced by fermentation in other media and by microbial biotransformation. Of these compounds, 1 was shown to be the most potent binding inhibitor. Preliminary SAR studies of these compounds indicated that all functional groups and side chains were required for the activity. Compound 1 was a highly-selective binding inhibitor for the kappa opioid receptor: 0.8 microM (IC50) for kappa, >200 microM for mu, and >200 microM for delta opioid receptor. Compound 1 suppressed electrically-stimulated twitch responses of rabbit vas deferens with an ED50 of 14 microM. The suppression was recovered by adding a selective kappa opioid receptor antagonist nor-binaltorphimine, indicating that 1 is a kappa opioid receptor agonist.
Ehvam
23 Feb 2014
I've been trying to figure out for myelf what this might mean, but google isn't helping..
Is this a good thing? bad? what does it mean
Is this a good thing? bad? what does it mean
golden1
23 Feb 2014
It might play a part in lion mane's acute subjective effects. Ive taken a lot of lion's mane and I cant say the subtle acute effect really reminds me of salvia, a kappa agonist.
adamh
24 Feb 2014
golden1, do you mean can say or can't say?
"Ive taken a lot of lion's mane and I cant say the subtle acute effect really reminds me of salvia, a kappa agonist."
I've taken it in small doses and never noticed anything.
"Ive taken a lot of lion's mane and I cant say the subtle acute effect really reminds me of salvia, a kappa agonist."
I've taken it in small doses and never noticed anything.
VERITAS INCORRUPTUS
06 Apr 2014
The concentration and bioavailability of the compound likely will make any amount of the herb ingested not of an appreciable amount to engage the KOR significantly. An ED50 of 14uM is fairly weak.
Salvinorin A, the prototypical natural KOR agonist, is orders of magnitude more potent I believe, and of course one needs to use a ROA other than oral
Salvinorin A, the prototypical natural KOR agonist, is orders of magnitude more potent I believe, and of course one needs to use a ROA other than oral
