New ideas about phospholipase A2 and POIS

[Quantum]

In the recent thread created by Nanna1 at http://poiscenter.com/forums/index.php?topic=2502.msg21497#msg21497 , he brought up, among other interesting ideas, the central role that arachidonic acid ( AA) production through the enzyme phospholipase A2 ( PLA2) in the inflammation cascade of POIS, leading to POIS symptoms.

Developing further on this path, I see that PLA2 causes neurological problems not only from AA production, but also from the production of PAF ( platelet activating factor) - see https://en.wikipedia.org/wiki/Phospholipase_A2#Relevance_in_neurological_disorders .

So, I think, that the use of AA synthesis inhibitors, like the omega-3 fatty acid EPA, can be combined with a PAF inhibitor to block neurological symptoms further still.

Natural PAF inhibitors include gingkolides from Ginkgo Biloba, and piperine ( see http://www.sciencedirect.com/science/article/pii/S0367326X1200295X for more info ).   I have just found out that aswagandha is also a natural PLA2 inhibitors - see http://www.medscape.com/viewarticle/538166 , at the end of the article.

There is also the relatively new antihistaminic and PAF inhibitor rupatadine ( brand name Rupafin, Rupax and others), that could be of some interest in POIS symptoms relief ( https://en.wikipedia.org/wiki/Rupatadine ).

I do not think they a PAF antagonist would be highly effective if used alone, but could be a very good part of any pre-pack against POIS.  My preference, of course, goes to natural ones like ginkgolides and aswagandha    So, some gingko biloba and/or aswagandha, with a good source of EPA and DHA, and some antioxidants( curcumin, quercetin, rosemary,...), and some COX and LOX inhibitors, would constitute a good base for the development of a customed pre-pack.


About phospholipase 2 ( PLA2), it is worthy to note that it is inhibited by flavonoids like quercetine and kaempferol  ( https://link.springer.com/article/10.1007/s10822-007-9129-8 )

[romies]

Quantum,

Very interesting point on PAF inhibitors.

Ginkgo Biloba: I may incorporate it into my prepack. I've had Ginkgo Biloba in the past, as a once-daily morning supplement. It has a mild enhancement on short-term memory for me. I do get bruises when I take two in a day, probably indicating nearly complete inhibition for peripheral PLA2.

piperine: bio-piperine already exists in my curcumin formulation.

We will see what happens.

[nanna1]

Has any body tried Pycnogenol(R) or pine bark extract?

Pycnogenol has been shown to have the following properties:
  a. Lowers mRNA expression of COX-2 and LOX-5 (taking 150mg/day for 5 days). [1]
  b. Blocks activity of phospholipase A2. [1]
  c. Inhibits COX-1 and COX-2 (within 30mins of a single dose of 300mg). [2]
  d. Inhibits the release of histamine from mast cells. [3]
  e. Upregulated the body`s antioxidant system (catalase, reduced glutathione and glutathione redox enzyme). [4]
  f. Reduces (smoking-induced) platelet aggregation (both after a single dose 200mg and multiple prior doses 200mg/day). [5]
  g. Improves sperm quality and motility (taking 200mg/day). [6]
  h. In combination with 1.7g L-Arginine Asparate, has been studied to treat erectile disfunction (40mg twice per day). [7]

  The majority of these studies are in-vivo in humans. On paper at least, it seems like Pycnogenol has ideal properties for stopping POIS symptoms. The active components in pine bark extract appear to be α-terpineol, α-pinene, α-pinene and Oligomeric Proanthocyanidins. d-Limonene from lemon peel oil and orange peel oil has similar effects but there is less research on it. [8]

I am curious to know if anybody has experience with this. I am particularlly interested in (e) and (g).

references:
 1. The anti-inflammatory pharmacology of Pycnogenol? in humans involves COX-2 and 5-LOX mRNA expression in leukocytes. (2009)
 2. Inhibition of COX-1 and COX-2 activity by plasma of human volunteers after ingestion of French maritime pine bark extract (Pycnogenol).
 3. Pycnogenol inhibits the release of histamine from mast cells. (2003)
 4. Effects of pycnogenol treatment on oxidative stress in streptozotocin-induced diabetic rats. (2003)
 5. Pine bark extract reduces platelet aggregation. (2000)
 6. Improvement in sperm quality and function with French maritime pine tree bark extract. (2002)
 7. Treatment of erectile dysfunction with pycnogenol and L-arginine. (2003)
 8. A Review on Anti-Inflammatory Activity of Monoterpenes (2013)

[Quantum]

Great post about pine bark extract / Pycnogenol, Nanna!  Well referenced too, as usual 

I have been using pine bar extract for many years, mostly for sport, because it is a potent antioxidant, and I tolerate it very, absolutely no side effects.   It is good for energy, in line with (e) and is good for my joints and muscle ache after sport, which tends to confirm (a), (b) and (c).  It is still part of my sport pre-pack, so I take 100mg of it at least two times a week. 

I have also discovered, through a "side effect", that it promotes nitric oxide production.  I noticed with time that "morning wood" was more stiff than usual when I had taken pine bark extract the day before...  not a bad side effect, though... and this would explain (h)  After realizing this "side effect", last year, it happened that I took it in advance when some sexual activity was planned   Even when taken like 12 hours before, it still gives its little extra, and it also contributes to tame the POIS beast, so it does not hurt     I can add that pomegranate extract has the same "side effect" too.   Resveratrol, too, maybe, but my resveratrol formula contains some pine bark extract, so I cannot be sure if resveratrol itself is a "hardener agent".  ( For anyone wondering, nitric oxide (NO) is a natural vasodilatator in the body, and is essential for the erection process,  and the well known Viagra and Cialis are working through the NO pathway )

I have never realized pine bark extract was also a mast cell stabilizer - thanks for the information.  I have updated my post on natural mast cells stabilizers to include it - see at http://poiscenter.com/forums/index.php?topic=2372.msg19856#msg19856

Pine bark extract could have make it part of my pre-pack, but I didn't have any at hand when I first formulated it.  It was partly because the Pycnogenol brand is expensive.   But now I have found a less expensive pine bark extract that has the same good results for me ( I use https://www.vitacost.com/vitacost-pine-bark-extract-standardized-to-95-polyphenols , which are 100mg caspules).   I use it for POIS "leftover" symptoms, when needed, and it works good, along with other products.

About (g), I cannot tell.  It has been very, very easy for my wife to get pregnant, both time.   First time, it took only one month for her to get pregnant..... it was deliberate form our part, but we thought it could take a little longer than that...hahaha...    So don't worry too much, you may be surprised how easy this could be...lol

 

[Going less Crazy]

I might try pine bark extract one of these days for more energy.  Hope a really sensitive like me can tolerate it though.

[nanna1]

Thanks Quantum for your pine bark extract experience! I just bought some from BulkSupplements.