collection of bioassays of piperine to increase bioavailabilty

hello people, first and foremost i would like to advise against what i'm going to be doing.. anyways i'm sure some of you will know that piperine is one of the main the active constituents in pepper. it is piperine that is responsible for the pungency and bite of pepper. this is actually caused by piperines ability to activate TRPV ion channel TRPV1 on nociceptors (pain sensing nerve cells).

it has also been shown to inhibit certain enzymes (namely CYP3A4 and P-glycoprotein) responsible for roles in the metabolism of some different drugs. it may by this or other mechanism increase bio-availability of certain drugs considerably.
it has been proven to increase the bioavailabilty of curcumin by a staggering 2000% in humans..

now my casual (and *make believe* if you get my drift) venture will include studies on its power to increase bioavailability of certain compounds of interest..:2thumbsup:

i intend to update this thread once each phase of research for each compound of interest is completed.

piperine itself can be easily extracted from black pepper in satisfactory yeilds (like 5-9% of total weight of pepper) using an ethyl alcohol soak, filtration of the resulting solution to remove pepper solids followed by H20 bombing to precipitate freebase piperine which will crystallize over 24hrs-48hrs after which they can be simply filtered out and washed with fresh DH20. this is a reasonable method of extraction in itself but may be combined with multiple recrystallization from ethyl alcohol for extremely pure piperine crystals. such as these;



now with each compound tested i will note my exact doseage of that compound to the mg. and my exact doseage of piperine to the mg.
a report will be written for the events occuring for each substance.

i cannot however, emplore how dangerous this venture may actually be, piperine should never be combined in a haphazard fashion. you read that it increased the bioavailability of curcumin by 2000%. now translate that to *your intended* combination and consider the *possible consequences*. remember this is all unknown territory. now curcumin is a 'curcuminoid' consisting of only carbon, hydrogen and oxygen. no nitrogen. it is not an alkaloid, so i would presume or at least suspect an ability to increase bioavailability of THC and possibly Salvinorin A as they also consist of only these elements. however i am no psychopharmacologist and that statement may be laughable to them, i simply do not know. piperine has very limited research in its interactions with alkaloids.. which interests me greatly.
hence this research.

i have limited knowledge in this field and will be bioassaying (*my mice*) at very low doseages. and recording results created.

i hope my cautious venture will be of some entertainment to you all.

Oxidation:2thumbsup:

 

to the mods;
i posted this here as my piperine combination research will be using synthetic compounds...

 

I cringe when I see a piperine in the compound....

 

hahaha whys that brother?

 

when you take one 2 many anti psychotics and have a bad trip .. I dont even like pepper cream peas anymore..

 

you!? psychotic nah i don't believe you....

 

I was experimenting with a few .. wasnt on anything else at the time. Anti psychotics knocked me down, felt like I was falling backwards..

 

yea i've had avanza- think sorta similar, i'm not sure on the active constituent tho

 

Sounds like a cool expiriment. Keep us posted.

Though I don't think it will do much to THC, or I probably would have noticed something, because I love pepper and pot.

But keep in mind, curcumin is another spice chemical.... a spice potentiating another spice without serious psychoactive effects of it's own (that I know of, anyway) isn't THAT special.

You might consider looking for research on exactly what all enzymes it suppresses, and then what all drugs are related to those enzymes? If that's the route it works by, it could be very easy to predict what it will potentiate.

 

capsaicin ... 8-Methyl-N-vanillyl-trans-6-nonenamide when taken orally has been known to effect the cannabinoid receptor..

 

i dunno roor, considering a good enzyme inhibiting dose of piperine would be 50+mg and theres around 5% of black pepper you'd have to consume some serious pepper to gain full enzyme inhibition.

good advice though thankyou, i will look into the cyp- whatever enzyme and see exactly what it does, i'm reasonably sure its like a transporter that drags molecules from the receptor sites to their doomise by enzymes similar to mao. although this i've not learned from factual reports only from word of mouth with chemist friends, so i'll do some study of my own and see what turns up..:2thumbsup:

though my interpretation is not to trust all the info out there.. i feel that experimentation is ultimate. however i have placebo as my enemy considering it will only be me experiencing the effects.. whoops.. did i say me? i mean my 'mice'......

 

^^^^^^^^this^^^^^^^^^^

piperine is;

5-(3,4-methylenedioxyphenyl)-2,4-pentadienoyl-2-piperidine

love the nomenclature around these parts heh heh

the interests are defintely sparked in me.....

 

check this out, this is one of the enzymes inhibited by piperine

CYP3A4 is a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by glucocorticoids and some pharmacological agents. This enzyme is involved in the metabolism of approximately half the drugs which are used today, including acetaminophen, codeine, ciclosporin, diazepam and erythromycin. The enzyme also metabolizes some steroids and carcinogens.[3] Most drugs undergo deactivation by CYP3A4, either directly or by facilitated excretion from the body. Also, many substances are bioactivated by CYP3A4 to form their active compounds, and many protoxins being toxicated into their toxic forms (for examples - see table below).

 

^^^^^^^^^this^^^^^^^^^

 

I don't understand half of the words in this thread, but good luck any how

 

check this link and look at the substrates.... interesting to say the least

http://en.wikipedia.org/wiki/CYP3A4

 

dont let the vocabulary deter you, it can be overcome. follow this space my friend and all will become apparent> eventually. once i get this ball rolling..:2thumbsup: