COX 2 Inhibitors

The Importance of Prostaglandins, or “Worker Bees”

By Ben Fuchs | PharmacistBen

The Importance of Prostaglandins, or "Worker Bees"

Worker Bees. Image credit: Todd Huffman from Phoenix, AZ (Lattice) [CC BY 2.0]

(PharmacistBen) There are 3 main types of hormones that can be distinguished by the speed of their activity, that is, how fast they accomplish their effects. The slowest acting ones, called endocrine hormones travel through the blood starting in structures called glands and accomplish their effects when they reach specific cells. Others called exocrine hormones don’t require a blood highway; rather they are squirted via specialized ducts directly into body cavities like the abdomen or through the skin. The digestive system is especially dependent upon these types of hormones as are the so-called pheromones, chemicals of sexual attraction that are secreted cutaneously into the external environment.

The third hormone category is composed of ultra-fast acting substances called autocrine or paracrine hormones, a term that refers to the fact that, while other hormones that travel through the body or external to it, these substances work in the immediate vicinity of the cells that make them. This allows reactions to happen instantaneously without requiring the brain or the nervous system to be involved. One of the most important of these types of hormones is a class of fatty substances called prostaglandins. It’s hard to really appreciate how unbelievably important these things are.

Prostaglandins and other similar compounds with similar ultra-fast acting functionality (“leukotrienes,” “thromboxanes,” and “nitric oxide,” for example) are the worker bees of the body which is and has to be highly responsive to the environment. Hormones, in general, can be considered to be the mediating element between our environment and our biochemistry; something happens in the environment and a biochemical change is imitated via the activity which functions as a middle man between sights, sounds, and other environmental signals and the body. Prostaglandins and similar substances function in this fashion but much more quickly than other hormones. They’re automatic in the sense that they are a cell response to an environmental change that can occur without the involvement of the brain or glands. This allows them to work super-fast. You see something or think a thought or have an injury and instantly prostaglandins are affected, and a response is initiated. Instantly! And it’s this biochemical instantaneity that gives the body its amazing rapid responsiveness.

In fact, even though many folks haven’t really heard of prostaglandins and less know much about these fatty substances that are essentially an activated form of essential fatty acids, they can be considered among the most powerful and important, if not THE MOST powerful and important molecules in the body and perhaps in all of biology. Even though prostaglandins were initially discovered in the 1930’s, it really wasn’t until the late 20th century that the extreme importance of these molecules was really understood. In fact, even up until 1982, prostaglandin chemistry was so mysterious that that year, the Nobel Prize for Medicine was awarded to a three European physicians for their work in elucidating the diverse and important roles prostaglandins play in the body.

These days, even though prostaglandins are still somewhat unappreciated, drug companies have become quite fond of their money-making potential. Remember, these things are powerful, and blocking them (and sometimes mimicking them) is big bux for the pharmaco medical model. Prostaglandin chemistry is the target for numerous over-the-counter and prescription drugs, most notably anti-inflammatories including aspirin and Motrin and Naprosyn or Aleve, which all work by suppressing or inhibiting the effects of prostaglandins. The most recent prostaglandin drugs are called COX 2 inhibitors, and these work by blocking an enzyme called COX 2 which has the effect of shutting down prostaglandin synthesis. This is a classic example of the utter stupidity and biochemical ignorance of the pharmaco medical model of health. Given the extremily importand nature of prostaglandins, who could ever think blocking their production is an intelligent and therapeutically valid strategy? The reason prostaglandin-blocking medications are the leading cause of drug toxicity and one of the leading causes of drug-induced deaths is because we’re not supposed to me be monkeying around with this stupendously important biochemical family!

Interestingly, while the pharmaco medical model perceives blocking the formation of prostaglandins as somehow beneficial, shutting down inflammation or muscle contractions to reduce cramping, as it turns out, prostaglandin deficiencies are potentially major health issues. A lot of degenerative diseases are associated with prostaglandin deficiencies and when you understand how important the hormone chemicals are, the side effects associated with prostaglandin-blocking drugs are hardly surprising. Think about it: prostaglandins regulate, control, mediate, and are involved with almost every single biochemical reaction in the body. How is it possible NOT to have side effects and toxicity from prostaglandin-blocking drugs? Non-steroidal anti-inflammatory drugs and aspirin are especially recognized for their toxicity to the kidneys and digestive tract and these reactions can be directly attributed to their prostaglandin suppressant activates. Some of you may remember a couple pf years ago Vioxx and Bextra, two COX 2 inhibitor drugs that reduced the production of prostaglandins, had to be taken off the market because of their unfortunate predisposition to causing heart disease. Again the question must be asked: given the wide ranging effect of prostaglandins in the body, given their effects on every single biochemical process, how is it possible that these kinds of drugs CANNOT cause side effects and toxicity? These days, the only COX 2 inhibitor that’s available is Celebrex, and while it apparently doesn’t have the same toxic profile as the other Cox 2 inhibitors that were discontinued, anytime you monkey around with prostaglandin production, you’re asking for trouble.

One of the most significant aspects of prostaglandins is the fact that we can be deficient. In fact, prostaglandin deficiency may be a common denominator in many if not most chronic degenerative and inflammatory disease INCLUDING auto-immunity. Prostaglandin deficiencies may be much more common than anyone recognizes and when we consider the key relationship between essential fatty acids, fat metabolism and fat absorption (or fat MAL absorption) and the production of prostaglandins, this should surprise no one. This is also why improving fat absorption is a key health strategy for reversing almost all chronic degenerative diseases. And it’s why supplementation with essential fatty acids is so important no matter what kind of degenerative health challenges we’re trying to address.

Pretty much all essential nutrients have some relationship to prostaglandin production or activity, and understanding how these things work is critical if we are going to be able to harness and leverage healthy chemistry and mitigate the disease process. The most important point or at least one of the most important points about prostaglandins is the fact that they are forms of essential fatty acids. Basically, we ingest essential fatty acids through foods or supplements, and they get converted into prostaglandins as needed. Prostaglandin deficiency is very common and associated with a lot of if not all degenerative diseases. You can’t take prostaglandins to “up” your prostaglandin levels, but you can use essential fatty acids in foods or supplementally which will ultimately allow you to MAKE more prostaglandins and eliminate deficiency states.

There’s a very interesting essential fat derivative called GLA, which can be thought of as an activated form of omega -6 fats, and which itself is activated to ultimately form prostaglandins. This makes GLA a very helpful supplement for a lot of health issues, especially ones that involve the skin. Borage oil is nature’s best source of GLA and contains around 25 percent or so of the important substance, which is pretty amazing, considering the stuff is so rare. Other good sources of GLA include evening primrose oil and black current oil, but neither has the GLA concentration of the oil that comes from the seeds of the Borage plant which is also known as “starflower”. Hempseed oil has a little GLA and so does barley. Spirulina contains some GLA also, and a little GLA can be made by the body. There’s also a GMO form of safflower oil that has been tweaked genetically and produces super high contents of GLA. Up to 40 percent of GMO safflower oil can be GLA, but of course then you’ll be dealing with genetic modifications that may not be in your long-term health interest. Recently super-high GLA safflower oil has been created via genetic modification which according to the company that developed it, Arcadia Biosciences, is up to 65 percent GLA which is pretty astounding. The primary market for this kind of super high GLA content oil is in the nutritional supplement market and you can expect to see more and more GLA nutritional capsules available that feature this high-tech “creation”. There’s lots of upside to GLA, especially when it comes to skin health, but because inflammation plays such an important role in the disease process and because GLA is such an effective anti-inflammatory, pretty much all health conditions can benefit by GLA supplementation.

The whole nature of anti-inflammation and inflammation, because of its importance and relevance to health and disease is worth spending a couple moments on.

Basically prostaglandins mediate all inflammatory process and also provide a balance to inflammation. The body is constantly balancing opposing biochemical processes. Excitation and Inhibition of brain cells contraction and relaxation of muscles and dilation and constriction of blood vessels are all examples of antagonistic processes that occur in the body and that must be controlled and balanced to keep us healthy. You can add inflammation and anti-inflammation to this list as examples of balancing actions that occur in the body.

The prostaglandin control of this balance is, as you might expect, mediated by opposing types of prostaglandins. There are pro inflammatory prostaglandins and there are anti-inflammatory prostaglandins. The prostaglandins involved with inflammation are derived from Omega-6 EFAs (with the notable exception of GLA, which is anti-inflammatory) and the ones associated with anti-inflammation are associated with Omega-3s. This is why you’ll hear nutritionists and dieticians associate too much inflammation with excess ingestion of Omega -6 containing oils. Omega-3 containing oils are much harder to find in nature and certainly they are much harder to obtain from the standard American diet, which feature vegetable oils derived from Omega-6 grains. It’s generally understood that we should be getting somewhere around 2 or 3 or maybe 4 parts Omega 6 EFAs for every 1 part omega -3 to maintain an optimum relationship between inflammation and anti-inflammation. EFAs are unusual among essential nutrients in the sense that their complexity makes it difficult to assess individual requirements. In other words, no one really knows how much we need of each, how much we need in total, and what the exact proportion of Omega 6s to omega 3’s is appropriate. In day to day real life, lots of factors influence need. If we’re growing or healing or exercising and building muscle, we need more. If we’re not getting enough anti-oxidant, on the other hand, we should probably be using lower daily doses as these fats are unstable and easily destroyed by oxidation. Sometimes EFAs can be displaced by saturated and/or processed fats, so our EFA needs are increased if we’re eating a lot of trans-, hydrogenated or otherwise processed fats. Some disease states, particularly diabetes, can influence how well Omega 6 can get converted into GLA so that prostaglandins can be made. In other words diabetics may not make this conversion effectively leading to GLA deficiency. This makes essential fatty acids especially important for diabetics or even pre-diabetics (which covers most of us).

What is clear is the fact that the Standard American diet, however, is way overloaded with Omega-6 consisting of LA rich oils like soy and safflower and corn. Now, that does not necessarily mean that we’re getting the actual EFAs. Remember, these oils are heavily processed and heated and no one really knows how much Omega 6 we’re getting at the end of the day. In any case, EFA deficiency is probably a much more significant health issue than anyone can guess.. Even something as seemingly trivial and benign as, ambient humidity can have a significant impact on skin biochemistry and that means prostaglandins, which are an early mediator of between the environment and the body and especially the skin. In addition to ambient humidity, the skin is also sensate to temperature, sun, toxicity, and NUTRITIONAL DEFICIENCY!

Posted by Ben Fuchs in Health