Betulin-anybody tried it?

[Limpet_Chicken]

Reportedly betulin, derived from the bark of the common birch tree (is it also present in silver birch? there are far more commonly found here than the brown type. Suits me usually mind you, for it means every year brings in a bumper harvest of fly agaric and its parasitic bolete 'friend' Chalciporus piperatus, peppery boletus, which I just love to powder up in my spice grinder with cured fly agaric and throw some in the pot while making chilli con carne
gives it a lovely fire that can't be quite replicated by other spices. If it wasn't a parasite on a mycorrhizal mushroom, I'd suggest it be sold in supermarkets as a spice, as its quite lovely with meat, especially with a bit of fly Amanita. Nature is telling something by bringing these together as a pair%)

Anyhow, betulin itself forms up to 30% dry weight of birch bark although reportedly, its not very orally bioavailable, still, theres no shortage of the stuff if I go looking..(its been extensively explored as a lead compound for developing a really wide range of all kinds of drug, antiretrovirals, antiprotozoals, topoisomerase inhibitors and more besides.



https://www.infona.pl/resource/bwmeta1.element.elsevier-cb41d204-2878-3573-a573-0f2461a158a2

Question-is bicucculine an allosteric or orthosteric GABAa antagonist? which binding site does it hit because its competitive with betulin, I just want to figure out if its likely to be benzo-like or more like a barbiturate/chlormethiazole

 

[serotonin2A]

Bicucculine is a competitive antagonist.

 

[Limpet_Chicken]

I know it is. I wanted to know the specific binding site bicucculine binds to. I know full well WHAT it does, its where it does it that I want to know. Competitive antagonists can bind allosteric sites can't they? making them competitive antagonists of not the primary neurotransmitter at the orthosteric site (Eg an antagonist at GABAa displacing the like of benzos, barbs, loreclezole or neurosteroids, being competitive with the allosteric ligand? or am I barking up the wrong birch tree, so to speak there ?
What do you think about betulin? its definitely a GABA agonist amongst a load of other things, and available for nothing. But the other activities make me a bit...uneasy about it.

Safe enough to bioassay on a test basis you think? with respect to the likes of topoisomerase inhibition specifically. It isn't something I'm exactly planning on making a regular dietary addition, merely,testing/experience purposes.
As it is, afterall available to me for a mere ten to fifteen minute walk and a few trees climbed and branches/twigs lopped off here and there, spreading the cuts over multiple trees to avoid significant damage to any one. Because really, if we take from the wild, we should give back too. And heh, god only knows, those birch trees have to be my favourite tree species I think, as they provide fly Amanita by the sack full, to last me through the following year (I use them for a kitchen spice for cooking, prepared correctly, for eating, cured by heat as a herbal medicine, sedative, sleep aid, endurance booster, helps keep out the bite of cold weather too, in tea form.

Never enough peppery boletes growing with them no matter how far I range in my search for them and fly agaric every year though. I do get enough of the amanitas, just not the parasitic boletes that grow with them.

(if fly agaric is to be eaten itself, it must be repeatedly boiled to leach out the toxins, treat them somewhat like Amanita rubescens, which is a good edible species if sometimes nasty and earthy if you get an old one, as they stay firm for ages even past their best. But it MUST be cooked, after first being twice boiled, and the water thrown out each time. Then cooked and added to a meal or just eaten. This treatment in the case of the blusher, is needed to leach out and destroy a thermolabile haemotoxin known as rubescenslysin, which causes red blood cells to be lysed, raw its poisonous, as is fly agaric, cooked properly both are pretty good eating. Fly agaric tastes REALLY meaty, umami-laden like no other food I have ever tasted. The medicinal tea I prepare from it, tastes almost like a product such as bovril, and STINKS the kitchen out with concentrated essence-of-umami fumes. Like VX for use against vegans

 

[serotonin2A]

You are barking up the wrong birch tree... Antagonists are only described as being competitive for a site if they actually bind to it. So a competitive GABA-A antagonist binds to the same site as GABA (i.e., the orthosteric site). There of course can be negative allosteric modulators (NAMs), but they are by definition non-competitive in relation to GABA. I get your point that someone could be lazy and say a NAM is a competitive antagonist because it competes for the NAM site, but that is very bad terminology -- it would be called a competitive antagonist at the allosteric site, or a GABA-A NAM, but not a GABA-A competitive antagonist.

The way you are using "competitive" makes it meaningless --all antagonists bind somewhere, so by the logic in your post, all antagonists are competitive antagonists.

 

[Limpet_Chicken]

Thats what I meant, a competitive allosteric ligand being competitive for the allosteric site in question with other ligands for that allosteric site.

I wasn't so much using the terminology that way, I just wanted to know if it was correct to do so. Thanks for clearing it up, nice one.

Now lets find out if I'm still barking up the wrong tree trying to eat some. (god, that reads SO strangely, when I look at it..eating trees indeed, because I am not, at least insofar as I know, a beaver)