Incarvillateine- stronger analgesic than morphine

[mindperformer]

Incarvillateine has a very strange structure:

The highly substituted 1,3-dicarboxy-cyclobutane Incarvillateine occurs in the chinese plant Incarvillea sinensis with the traditional names Cheron, Jiao hao, Tougucao and Yuan bian zhong. The name of the genus, Incarvillea, came from the botanist Petrus d'Incarville who lived in Peking from 1740 to 1757. The plant is distributed from Yunnan in the south to Siberia in the north and Tibet in the West.

Incarvillea sinensis also contains the macrocyclic spermine alkaloids Incasines A,B, C and Verballocine, the monoterpene alkaloids Incarvilline, Incarvine A,B,C,D and Methoxycarvillateine and the flavonoid Isoliquiritin. It is one of the traditional herbal medicines in China, Tibet and Mongolia and is mainly used to treat rheumatism and relieve pain. Besides it is udes for detoxification, against cough, as laxative, jointache, cramps, eczemas, inflammations in the mouth, carbuncle, skin ailments, spongy gums, ulcers and wounds in chinese medicine.

And against chronic bronchitis, dry cough, lung abscess, otitis media, veneral disease, flatulence and dry faecal in mongolian medicine.

It is used in dosages from 5-15g, cooked in water or external use by a wrap with the dry powder.

The analgesic index (ED50) of Incarvillateine is better than Morphine (1,06-1,33 times) and appears to have a lower ceiling effect than Morphine!

Responsible for the analgesic properties is an agonistic action on mu- and kappa-opioid- receptors and an antagonistic on adenosine-receptors:

http://www.ncbi.nlm....pubmed/16204962

In my experience 2g of the herb were definively analgesic and opioid.

In chinese, mongolian and tibetan medicine many Incarvillea- species are used medicinally, especially as analgesic:

Incarvillea delavayi which contains the analgesic monoterpene alkaloid Delavayine A.

Incarvillea arguta which contains the bacteriostatic and sedative Argutone.

Incarvillea dissectifoliola which contains the monoterpene glycoside Dissectol A.

My Incarvillea sinensis- plants:

And dry Incarvillea delavayi- leaves:

Edited September 9, 2012 by mindperformer

[Alienteaparty]

wow at first i thought it looked kinda like parsley. Sounds interesting never the less. have you tried it?

also you have something a tad cheeky in the bottom right hand corner of the second photo

[mindperformer]

yes, as I wrote 2g of it worked against toothache and were pretty opioid after one hour, but didn't last long (5 hours).

Which cheeky thing do you mean? ;-)

Edited September 9, 2012 by mindperformer

[Acacia King]

Dude! Epic find. She looks like a nice plant to have around too. Similar to a maiden hair fern. How old is the plant?

Do any Aussie members have these plants. Would love to discuss trade or Buy.

Edited September 10, 2012 by Acacia King

[at0m]

Love your posts, Mindperformer. Great stuff!

[Acacia King]

Does Incarvillea delavia contain incarvillateine?

[mindperformer]

the plant was about one year old, it grows quickly. tricky is only the stage shortly after the germination. take sandy soil.

Incarvillea delavayi doesn't contain Incarvillateine, but as I wrote Delavayine A, which is also analgesic but more unexplored

[mindperformer]

More on the habitat and growing conditions:

http://en.cnki.com.cn/Article_en/CJFDTOTAL-GTZY200703052.htm

http://www.amjbot.org/content/92/4/625.full

and the dosage:

http://www.sumobrain.com/patents/jp/Analgesic-action-agent/JP10130157.html

Edited September 27, 2012 by mindperformer

[mindperformer]

1a. Incarvillea sinensis var. sinensis

角蒿(原变种) jiao hao (yuan bian zhong)

Incarvillea sinensis subsp. variabilis (Batalin) Grierson; I. variabilis Batalin.

Leaves variable in shape; flowers pale rose, pale red, or purple. Fl. May-Sep, fr. Oct-Nov. 2n = 22.

* Slopes, fields; 500-2500(-3900) m. W Gansu, Hebei, Heilongjiang, Henan, Nei Mongol, Ningxia, Qinghai, Shaanxi, Shandong, Shanxi, N Sichuan, SE Xizang, NW Yunnan.

I'm sowing seeds of Incarvillea sinensis ssp. variabilis now and wondering if it will have pink flowers and different morphology than my Incarvillea sinensis 'Cheron' last year.

[Thelema]

for god's sake mindperformer, don't you ever EAT any of your plants?? All you seem to post about is theoretical stuff - if you really want to make an input, start eating your plants, performing extractions, finding out useful stuff....

[planthelper]

for god's sake mindperformer, don't you ever EAT any of your plants?? All you seem to post about is theoretical stuff - if you really want to make an input, start eating your plants, performing extractions, finding out useful stuff....

 

thelema, you know i love you, and don't want to upset you, but i am certain your critisism as above is unfounded, mp has reported for example how to make oral sprays, in short back off.

btw, i hardly do bioessays these day's, a massive overdose on a strong halu, scared me off big times, hehehe....

and you know that reporting bioessays, is pretty out of the question, apart from "the boring stuff"....

Edited September 29, 2012 by planthelper

[Thelema]

OK I'll retract my criticism. The stuff mp posts is pretty interesting after all...it would be great though to hear a few more bioassays on stuff like this plant for instance...

[Anodyne]

Besides, mp writes about so goddamn many interesting plants, who could find the time to eat them all? Not to mention all those psychoactive elements...

[mindperformer]

To quote myself

yes, as I wrote 2g of it worked against toothache and were pretty opioid after one hour, but didn't last long (5 hours).

[mindperformer]

I agree with planthelper and Anodyne, it is not possible to test all the thousands of psychoactive materials, but I do what I can, especially with the ones with lower risk.

@ Thelema:

I think you have no idea what I have tested or not, but you already could have known that I tested the Incarvillea (I mentioned in this thread) and some other herbs because I wrote also experiences down, like Kratom, Kanna, Thaumatin and many more. Apart from this I described many traditional uses and reports...

[mindperformer]

More on Incarvillateine:

http://www.bluelight.ru/vb/attachment.php?attachmentid=4798&d=1186685466

http://202.127.145.151/siocl/siocl_0001/HHJdatabank/090707t-3.pdf

Edited September 30, 2012 by mindperformer

[Slocombe]

Bump. Do any aussie members have Incarvillea Sp. for sale or trade?

[shonman]

I wonder if I can obtain a live specimen for my collection in the usa?

[mu!]

I recently ordered some seeds online from Chiltern Seeds. If i'm successful in growing this plant and getting it to flower + seed I'll be sure to make seed available.

[theuserformallyknownasd00d]

Wss has a reasonably priced 20:1 of this extract, what would be the legal status of this?

[Slocombe]

Awesome mu! Can I be first in line :-)

[gwalchgwyn]

Incarvillea delavyi

second pic is backlit by the sun

[Freewheelin]

Very interesting!

Thanks for the info mindperformer and mu

I'll be ordering some seeds from Chiltern tomorrow too.

What does "celiing effect" mean? Is this another way of saying "tolerance" ?

[mu!]

Cultivation details

Easily grown in a deep well-drained sandy but rich soil in full sun[1, 200]. Plants grow better if they are given some shade around midday[200]. Dislikes dry summer soils and winter wet[200]. One report says that this species should be grown in a greenhouse[1] whilst another says that it is hardy to about -15°, tolerating lower temperatures if the roots are well mulched, preferably with dry bracken[200]. The crown of the plant requires protection from slugs in the winter[187]. A very ornamental plant, it usually takes about 1 - 2 years to come into flower from seed[1]. A variable species[214], some forms are perennial whilst others are annual[1]. I. sinensis sinensis is an annual whilst I. sinensis variabilis (Batal.)Grierson is a perennial[200]. Plants are intolerant of root disturbance, it is best to place them in their permanent positions whilst small[200]. The plants will often sulk for several years if they are divided[214].

Propagation

Seed - sow autumn or spring in a greenhouse. Prick out the seedlings into individual pots as soon as they are large enough to handle. Grow on for at least their first winter in a greenhouse and plant out into their permanent positions in spring after the last expected frosts. Division with care in early spring or autumn.

http://www.pfaf.org/user/Plant.aspx?LatinName=Incarvillea+sinensis

mindperformer, does the info above match up with your growing experience?
I got my seeds a couple of days ago so once I have a proper growing space for them (I'll probably go the mini-greenhouse setup to start them off) I'll be starting a grow-diary thread for them.

[Anodyne]

What does "celiing effect" mean? Is this another way of saying "tolerance"

No.

In pharmacology, the term ceiling effect refers to the property of increasing doses of a given medication to have progressively smaller incremental effect (an example of diminishing returns). Mixed agonist-antagonist opioids, such as nalbuphine, serve as a classic example of the ceiling effect; increasing the dose of a narcotic frequently leads to smaller and smaller gains in relief of pain. In many cases, the severity of side effects from a medication increases as the dose increases, long after its therapeutic ceiling has been reached. (link)

So tolerance refers to the way your body adjusts to a drug over time, to require a larger dose for the same effect. The "ceiling effect" refers to the way your body reacts to increasing doses of the same drug, to require a larger increase in dose for a larger effect. So if after six months of taking a drug, you need 100mg/day rather than 30, that is tolerance. But when you're titrating your original dose, maybe you get twice the effect from 20mg as you do from 10, but as you increase the dose, this changes, so that to get double the effect of 20mg, you need to take 60mg - this is happening because you're approaching that ceiling.

In the OP where it says "lower ceiling effect than morphine" I take that to mean a lesser ceiling effect, rather than a lower ceiling. So they're basically saying that if you continue to increase the dose, the effects will continue to increase, at least to a point - and that for incarvillateine the point at which this starts to level out is at a higher level of analgesia than morphine.