What does this work suggest about passiflora for either insomnia or anxiolysis?

Dug out the full text. Can't quote it of course, but I'll summarize.

Open field and elevated maze are long established methods that correlated directly to human studies. Open field in particular, is considered quite useful. These are what they used to measure anxiolytic activity.

Basically, what their chemistry demonstrates is that P. Incarnata, which I know next to nothing about, contains compounds that exert an anxiolytic activity that is antagonized by flumezenil. This implies that some compound within P.I. is active at the "Benzodiazepine" receptor on GABA-A, as this is the major site of activity of flumezenil. Blocking 5HT1A did not reduce any of the measured activities, so this receptor is probably not involved. Basically, what this says is there's a compound in PI that acts like a benzodiazepine.

There are four, perhaps five flavenoid compounds in PI. One they did not detect, that should have been there. What they did was take the plant, separate the chemicals inside out in methanol and water, and run it through HPLC. This compounds, due to their structure, are likely to be the pharmacologically active components.

Depending on the purity they were using, the compound is not likely to be very potent, note the 375mg/kg = approximately 1.5mg/kg Valium for a mouse. It is, however, distinctly active. If I'm reading this correctly, what they did to get that 375mg, was use the above MeOH/H2O extraction on the sample of PascoFlair (one of those crazy German non-regulated herbal things). Basically what this means is that this 375mg has gone through two pretty serious rounds of concentration, so what's in the original plant is NOT there in large quantities. Assuming I'm reading this right. I've been grading things. Grading things written by people who clean microscopes with kimwipes.

Also, they got a U shaped curve, which could imply that it's a partial agonist/antagonist. Or that there's both an agonist, and an antagonist in the mixture as well.

It's probably published in a German medical botany journal because, well, two of the four authors are transplanted germans, and one of the others is presently at a german university.

Pascoe Pharmazeutische Praeparate is somewhat worrisome, as it's one of those companies that basically vendors out various substances branded natural as panaceas, only German. Their laws are strange.

EDIT: Well, U-shaped curve can imply that. It's a possibility, not the only one. We could be getting into the range of.. Hmm.

Let's say there's two substances in the solution. One, is our BzR allosteric agonist. The other, say, binds a noradrenergic receptor in the brain. Say they have dissociation constants (Kd) that are different by about an order of magnitude. Now, at one dose, you've got enough of the BzR agonist for that effect to predominate. But double the dose, and you're getting into the range where you're pushing the 2nd compound, stimulating a noradrenergic receptor.

Anyway, partial agonist/antagonists, or even mixtures can come in handy. Offhand I can think of Buprenorphine. It's an opiate painkiller that it's actually physically impossible to overdose on. We use it, occasionally, for dealing with heroin addicts, and in undergraduate labs that use animals, because you can't trust people who inoculate agar plates without gloves to handle anesthetics without ODing/UDing an animal. And god knows dealing with animals is a big enough pain as it is.

Basically, what this suggests to me is that there's mixed activity in the sample. And this is problematic, because it is not a pure sample, it's a sample with possibly quite a number of active components.

Ideally, they should strip out pure chemicals in here, and do some binding assays to a standard panel of receptors to find out who's doing what, before even approaching the thing in an animal model. But of course, doing so demonstrates that there -are- some interesting properties in there.

The things you read K - amazing.

All this tells us is that the chemicals identified by high pressure liquid chromatography in their passion flower extract worked as well as Valium for frustrated mice. Apparently, the "elevated plus maze" has an anxiety producing effect on test mice. Mouse studies are several steps away from human utility for new pharmaceuticals - as you know. The mechanism of action appears to be mediated by the same receptors affected by benzodiazepines - e.g. the Valium (diazepam).

At the medical center where I trained, we did a similar study regarding anxiety levels in mice. Half the mice were dressed in three piece suits with tight neck ties. The other half were dressed in leisure suits. (It was 1979.) The mice in leisure suits appeared significantly more relaxed as they worked their way through our mazes. There was demonstrably less murine frenzy and frustration. The leisure suit mice also enjoyed a 17% longer life span and a more satisfying social life.

Passiflora Overdose

work suggest passiflora insomnia anxiolysis