Prostaglandins (PG's) are naturally occurring intercellular messengers. In fact, many of the actions of anabolic substances fail to exert their protein synthesis actions without them. It is a clinical fact that there is a parallel between the rise of some levels of PG's and the degradation of catabolism. So they may in part be the relay between receptor-sites and translation to specific responses, or secondary messengers.
Research has shown a rapid and quite strong direct anabolic action from PG's in muscle cells. If PG's such as PGF-2 and PGE-2 are introduced into muscle cells, protein synthesis occurs at an incredible rate. If insulin is introduced into muscle cells with PGF- 2 or PGE-2 there is a profound synergistic response. This places certain PG's among the most potent of anabolic activators. Perhaps far more so than anabolic steroids. This also suggests that the powerful anabolic actions of IGF-1, insulin, and amino acids are all mediated in one way or another by PG's.
Hang with me here. I need to explain your natural prostaglandin production process. Some prostaglandins called the PGE 2 series are made from a fatty acid found in the plasma membrane of your cells called Arachidonic acid. Under basal or non-training conditions, most of your arachidonic acid is in an esterified (bound) form inside the membrane phospholipids. Since only free (unbound) arachidonic acid can produce prostaglandins of the PGE 2 series, the basal synthesis of them is low. Pretty much like a balance of protein synthesis/degradation is normal (homeostasis). Due to the action of an enzyme called phospholipase A2, The esterified (bound) arachidonic acid is freed. The free arachidonic acid is converted into PGE 2s by another group of enzymes called Cyclooxygenase (COX). COX-1 and COX-2 are both found inside most cells and are responsible for the normal release of PG's. However, COX-2 is not normally present in the cells during basal states. When you train (creating a stress) COX-2 is quickly synthesized which in turn strongly stimulates prostaglandin release. Some PG's are mediators of inflammation, but our focus is upon PGF-2 which is an amazing anabolic stimulator. (COX-2 specific inhibitors such as Celebrex do partially block this activity)
*PG's are not stored like some hormones. They are quickly synthesized and then quickly destroyed. There are no PG reserves.
Cortisol, both natural and synthetic, are powerful PG inhibitors, though synthetic corticoids are even more powerful. Both reduce the activity of COX-1, COX-2, and phospholipase A-2.
A note of interest before I babble on. Intense muscular activity triggers specific muscle prostaglandins and the most intense of all stimuli is pure negative reps with very heavy loads. If you choose an exercise that contains a stretch position such as sissysquats, incline curls, etc., more growth specific PG's are produced. The second most effective natural method of inducing elevated PG production is intense muscular burn. This is because Lactic acid build -up is a PG release stimulator.
Stretching is the third method. Stretching increases intermuscular IGF-1 and FGF (fiber blast growth factor) which triggers PG production.
Prostaglandins have shown up in a synthesized form on the black market since a few years ago. I have personally seen amazing transformations in those who had bravely injected PGF-2 site specifically 3-5 times per day. The injections were administered directly into the muscle group trained that day (usually with a fast-acting insulin such as Humulin R or Humalog). Due to extreme soreness, that body part could not be trained for a few days following injections. Since PGF-2 is site-specific, abdominal enlargement does not seem to occur as with IGF-1.
PGF-2 is the more active PG. Some of the elite group reported dramatic muscular hypertrophy (growth) at a dosage of 1-2 mg each 3-5 times per day. (3-10mg total per day) Side effects were serious soreness throughout the muscle injected. (Like a major cramp far worse than testosterone suspension). It was commonly known to avoid injections of PGF-2 anywhere near the intestines. (PGs of the 2 series will cause smooth muscles such as intestines and stomach to contract majorly. Some have experienced the worst bowel voiding of all times: the shits to end all shits) If injected, a small amount of the PGF-2 would reach the blood stream. This would explain the overall muscular growth reported. The reason, as I have stated prior, the injections were so frequent is due to PG's very short half- life.
Some interesting notes about Prostaglandins
*Using androgens with PG'S were noted to be a bad idea for some individuals even if a legal method could be found. Users often reported that their muscles had difficulty functioning due to serious pumps. The upside was that androgen cycles after PGF-2 cycles became very effective again. According to some available literature, PGF-2 use seems to up- regulate androgen receptor counts at an amazing rate.
*In women PGF-2 use would induce severe menstrual cramping.
*Arachidonic acid is found in red meat in fairly high levels. Unfortunately the activity of an enzyme called 5-Lipooxygenase (5-LO) upon arachidonic acid in the presence of estrogen has been linked to prostate cancer. An interesting finding is that inhibition of the 5-LO enzyme triggers massive apoptosis (programmed cell death) in human prostate cancer cells. Ginger seems to inhibit this enzyme and omega-3 fatty acids have a protective effect against prostate cancer.
As I wrote earlier, training and stretching trigger the release of prostaglandins by acting on the 2 enzymes that are responsible for their formation: Phospholipase A2 is increased which results in higher formation of free (unbound) Arachidonic Acid within muscle cells. Then muscular contractions increase COX-2, which transforms the freed arachidonic acid into PG's. The process can continue for days after a workout. At first, PGF-2 is the most elevated of PG production. FGF-2 synthesis is also elevated but in lower amounts at first. As the training induced muscle injury heals, the amount of PGF-2 production increases progressively. (Which is responsible for much of the anabolic reaction to training) It should be noted that there are several different PG's including PGE-1 which is used as an erectile function drug injected directly into the base of the penis. The result is a sort of inflammation: A woody.
The legal and far less effective but safer way to increase PG's is from the increased intake of essential fatty acids (EFA's). Specifically, Linoleic Acid, which is an OMEGA-6 fatty acid, and Alfa Linolenic Acid which is an Omega-3 fatty acid. Gamma Linoleic Acid (GLA) is another Omega-6 Fatty Acid essential for PGF-2 synthesizes. EFA'S are not just health and performance related. These EFA's are so necessary that without them, your body would simply deteriorate away and you die.
I have been amazed at how lacking many new clients diets are in EFA's. The best ratio seems to be 3:1, or about 6 grams of Omega-3 and 2 grams of Omega-6 fatty acids daily for most hard training bodybuilders. The best supplemental source for both is hemp seed oil. It contains the natural 3:1 ratio. Flax seed oil and evening primrose oil are both good sources, the latter, an excellent GLA provider. Yes, it is possible to test "dirty" for "weed" with enough hemp oil.
L. Rea (2002) - Chemical Muscle Enhancement Bodybuilders Desk Reference