Fact Sheet: Oilahuasca P450 Inhibitors (Discussion Thread)

69ron · Sep 05, 2011#12011-09-05T20:18+00:00

This is the discussion thread for the Oilahuasca Activation Wiki article on our sister site HerbPedia.wikidot.com. All of our Fact Sheet threads will be moved to HerbPedia.wikidot.com. This is done to keep them short and to the point so it's easy to find information. I maintain most of the Wiki articles and update them as new data is found.

This discussion thread allows us all to partake in what's listed in the Wiki page. If you see any errors or have discovered new useful P450 inhibitors, this is the place to discuss them.

Just today I saw people talking about cannabidiol. This is not in the fact sheet. This is a CYP2A6 inhibitor found in marijuana. Does anyone know how potent this inhibitor is?

canadianchemistry · Sep 05, 2011#22011-09-05T20:35+00:00

This is the discussion thread for Fact Sheet: Oilahuasca P450 Inhibitors. Fact Sheet threads are always locked. This done to keep them short and to the point so it's easy to find information. I maintain most of the fact sheets and update them as new data is found. Becaue they are locked threads, I made this discussion thread to allow us all to partake in what's listed in the fact sheet. If you see any errors or have discovered new useful P450 inhibitors, this is the place to discuss them.Just today I saw people talking about cannabidiol. This is not in the fact sheet. This is a CYP2A6 inhibitor found in marijuana. Does anyone know how potent this inhibitor is?
-69ron

From first hand experience with Cannabis it's Moderate at Inhibiting it. I recommend NOT to use alone, cannabis also rises PEA and Melatonin levels in the brain. If you smoke tobacco after you had a Joint it's easier to get light-headed I would say that's because of CYP2A6 being inhibited I may be wrong tho.

69ron · Sep 05, 2011#32011-09-05T20:46+00:00

Is there a study that shows how potent it actually is? Knowing it's IC50 value would be very helpful. That way I could compare it to cinnamon oil and other CYP2A6 inhibitors. That would help me categorize it properly.

Does marijuana inhibit any other P450 enzymes?

treppenwitz · Sep 06, 2011#42011-09-05T23:56+00:00

Parsley leaf is high in apigenen and also contains a few other CYP1A2 inhibitors, though I don't know how it compares to German chamomile. Is there any reason why this can't be used to inhibit CYP1A2?

toastus · Sep 06, 2011#52011-09-06T01:53+00:00

SWIM thinks it's possible the PEA release from smoking cannabis interferes with the effects of allylbenzenes. Perhaps SWIM should abstain from cannabis for a while and then try the allyls...

9657874 · Sep 06, 2011#62011-09-06T03:45+00:00

A study from this website states:
The inhibitory effects of CBD on CYP2D6 activity was more potent as compared with those of 16
compounds without nitrogen atom tested, such as progesterone. These
results indicated that CBD caused potent direct CYP2D6 inhibition.
The results state the value of IC50 = 6.52 μM.

69ron · Sep 06, 2011#72011-09-06T10:40+00:00

I didn't know cannabidiol inhibited CYP2D6. That's not good news for people using elemicin.

An IC50 values of 6.52 uM puts cannabidiol in the ballpark of things like grape fruit juice and quinine. That's good for some allylbenzenes like methyl eugenol and methyl chavicol but absolutely terrible for elemicin. That means marijuana usage is incompatible with elemicin. That's too bad.

Sep 06, 2011#82011-09-06T10:58+00:00

Parsley leaf is high in apigenen and also contains a few other CYP1A2 inhibitors, though I don't know how it compares to German chamomile. Is there any reason why this can't be used to inhibit CYP1A2?
-treppenwitz

There's no reason, unless apigenin is weaker than it's reported to be. I have not used apigenin myself yet. I plan to.

Apigenin is in our list of CYP1A2 inhibitors. It's found in German chamomile. I didn't know it was also in Parsley leaf. Parsley leaf also contains myristicin and apiole, a tiny bit.

One source says that common parsley leaf contains nearly 10% apigenin. That's a lot.

Apigenin is supposed to be very potent CYP1A2 inhibitor. It sounds like a good source of apigenin is common parsley. According to the data I read, about 20-50 mg of apigenin should be enough to inhibit CYP1A2. At 10%, that's 200-500 mg of parsley leaf powder. That should easily fit in a size OOO capsule.

We should give Parsley leaf a try. This is great if it works. If so, that gives us three very easy to get CYP1A2 inhibitors: German chamomile oil (5-10 drops), cayenne pepper (500-800 mg), and parsley leaf (200-500 mg).

I will update the fact sheet to include this new information.

Sep 06, 2011#92011-09-06T10:59+00:00

Parsley leaf is high in apigenen and also contains a few other CYP1A2 inhibitors, though I don't know how it compares to German chamomile. Is there any reason why this can't be used to inhibit CYP1A2?
-treppenwitz

There's no reason, unless apigenin is weaker than it's reported to be. I have not used apigenin myself yet. I plan to.

Apigenin is in our list of CYP1A2 inhibitors. It's found in German chamomile. I didn't know it was also in Parsley leaf. Parsley leaf also contains myristicin and apiole, a tiny bit.

One source says that common parsley leaf contains nearly 10% apigenin. That's a lot.

Apigenin is supposed to be very potent CYP1A2 inhibitor. It sounds like a good source of apigenin is common parsley. According to the data I read, about 20-50 mg of apigenin should be enough to inhibit CYP1A2. At 10%, that's 200-500 mg of parsley leaf powder. That should easily fit in a size OOO capsule.

We should give Parsley leaf a try. This is great if it works. That gives us three very easy to use CYP1A2 inhibitors: German chamomile oil (5-10 drops), cayenne pepper (500-800 mg), and parsley leaf (200-500 mg).

I will update the fact sheet to include this new information.

9657874 · Sep 07, 2011#102011-09-07T06:31+00:00

"Just today I saw people talking about cannabidiol. This is not in the
fact sheet. This is a CYP2A6 inhibitor found in marijuana. Does anyone
know how potent this inhibitor is?" - 69ron"Is there a study that shows how potent it actually is? Knowing it's IC50
value would be very helpful. That way I could compare it to cinnamon
oil and other CYP2A6 inhibitors." - 69ron
Oh, 2A6, I was thinking of 2D6. From my searching around on the subject, I have only come up with one report , which states:

"Δ9-THC, CBD, and CBN noncompetitively inhibited coumarin 7-hydroxylase activity of recombinant CYP2A6 with the apparent K i values of 28.9, 55.0, and 39.8 μM, respectively. On the other hand, Δ9-THC, CBD, and CBN inhibited 7-benzoxyresorufin O-debenzylase activity of recombinant CYP2B6 in a mixed fashion with the K i values of 2.81, 0.694, and 2.55 μM, respectively. Because the inhibition of CYP2B6 by CBD was the most potent,
investigation was conducted to determine which moiety of the CBD
structure was responsible for the inhibition.....Δ9-THC, CBD, and CBN showed metabolism-dependent inhibition for CYP2A6 but not for CYP2B6.....These results indicated that Δ9-THC, CBD, and CBN showed differential inhibition against CYP2A6 and CYP2B6."

The report does not show any IC50 values, nor have I found any, and I only know that low values of Ki indicate high inhibiting potency.