Piperine is a spicy alkaloid. A source is black/white pepper with content of about 4-7/5-9%.
Despite it's ubiquitary use as a spice in often not minor amounts, it's seems to have significant effects on the body. It's taste is awful and hence incompatible with most types of food.
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Low level effects:
MAO-A Inhibitor: IC50=20.9µM [1]
MAO-B Inhibitor: IC50=7.0µM [1]
PGP/CYP4A3 Inhibtor [2]
Raise in piperidine levels of blood and brain [3]
High level effects:
CNS depressant effects for electroshock seizures[4, 5, and many other]
Lowering of NA in brain/raise of DOP in some parts/raise of 5-HT in some parts[5]
Antidepressant activity for chronic mild stress[6]
Facts and thoughts:
Piperine is metabolized pretty quickly into piperidine and other obvious metabolites (half life in human ~2h). Piperidine is likely to play a major role in it's effect, though it has stimulant-like effects.
It also enhances the bioavailability of various drugs, but this effect is not that interesting for me.
My experiences:
In combination with Methylphenidate it seemed to exhibit some stimulating effects, which were overall significantly stronger than the ones of MPH itself, but again somehow weird. On it's own (due to extensive use of multiple drugs at this time has just a limited meaning - but most other drugs should have had just a minor effect) it had some weird effects which were somehow sedating. I tried it in very different settings again, but the effects seemed to vary greatly and most likely depend strongly on the different plasma levels of other substances.
But anyway i wasn't able to assign a well defined profile to it. This sounds strange, but it's not difficult for me to do with other substances even in combination.
The doses i used ranged from ~100mg to 500mg. At first it was used pure, then just in form of pepper of which the piperine-content was known.
My questions:
In theory it looks like an interesting addon for multiple drugs - am i right?
Has anyone experience with it and combinations with other drugs?
More pharmacokinetic data on it?
What effects and half life has piperidine?
Do the other metabolites significantly contribute to it's action?
What do you think about this in general?
References:
1. Seon A LEE,a Seong Su HONG,a Xiang Hua HAN,a Ji Sang HWANG,a Gab Jin OH,b Kyong Soon LEE,a
Myung Koo LEE,a, c Bang Yeon HWANG,a and Jai Seup RO*,a
"Piperine from the Fruits of Piper longum with Inhibitory Effect on Monoamine Oxidase and Antidepressant-Like Activity"
Chem. Pharm. Bull. 53(7) 832—835 (2005)
2. Bhardwaj RK, Glaeser H, Becquemont L, Klotz U, Gupta SK, Fromm MF
"Piperine, a major constituent of black pepper, inhibits human P-glycoprotein and CYP3A4"
J. Pharmacol. Exp. Ther. 302 (2): 645–50
3. B. GANESH BHAT and N. CHANDRASEKHARA*
"METABOLIC DISPOSITION OF PIPERINE IN THE RAT"
Toxicology, 44 (1987) 99--106
4. Eun Bang Lee, K u k H y u n Shin and W o n Sick W o o
"Pharmacological Study on Piperine"
Arch. Pharm. Res. 7(2), 127'--132 (1984)
5. A K I T A N E M O R I 1, H I D E A K I K A B U T O 1, AND Y I N - Q U A N P E I 2
"EFFECTS OF PIPERINE ON C O N V U L S I O N S
A N D ON BRAIN SEROTONIN A N D
C A T E C H O L A M I N E L E V E L S IN E1 MICE"
Neurochemical Research, Vol. 10, No. 9, 1985, pp. 1269-1275
6. Song Li a,c,⁎, Che Wang b , Minwei Wang c , Wei Li d , Kinzo Matsumoto e , Yiyuan Tang a
"Antidepressant like effects of piperine in chronic mild stress
treated mice and its possible mechanisms"
Life Sciences 80 (2007) 1373 – 1381
