Prototype Nutrition Ketoforce



The poor bioavailability of (-)-epicatechin and my attempt at getting around it and seeing what it does

By Patrick Arnold


You may have heard of (-)-epicatechin (-epi for short) as my blog reading base I assume has more than the average share of knowledgeable people in the realm of physiology of supplements and drugs.   IF you have not heard of -epi,  it is a natural chemical compound that has lately  been of immense interest  due to several pro health properties.   First and foremost,  is its ability to profoundly increase the functionality of nitric oxide dependent vasodilation and circulatory efficiency (blood flow), right down to the capillary level.   That means efficient infusion of brain, muscle, etc. with oxygen and vital metabolic substrates.  Secondarily, it is a powerful anti-inflammatory and literally eats up reactive oxygen species (ROS)(free radicals) like a chemical pac man.  ROS’ are generated during destructive inflammatory flare ups and mopping them up is essential for minimizing tissue damage and facilitating recovery.    There are a plethora of other benefits as well (i.e. stimulation of mitochondrial activity), likely tied partly to some of these aforementioned fundamental cellular / genomic actions in a downstream fashion.   Oh, and for the muscle crowd it has been shown to raise follistatin and lower myostatin levels in skeletal muscle and increase strength (albeit so far only demonstrated in older people).   Nevertheless, these two signaling molecules, folli and myo, are part of the the TGF beta protein superfamily and are a big deal when it comes to muscle hypertrophy and body composition – so this is nothing to sneeze at.   You muscle heads I know are quite aware of this.

Ok so what’s the problem again.  You read the title so I think you got an idea if you are a one of the more educated readers.  I will explain though in basic detail.    -Epi is found in many food items like tea, and is especially prevalent in chocolate, along with other chemicals in the overall family of “catechins” (several of which have varying remarkable health effects in their own right).   This is great you are thinking.  So why not extract and consume, or gorge on dark chocolates.   Well, you see, -epi like other catechins fall into the overall family of polyphenols.  Polyphenols are ubiquitous natural chemicals that you’re gut microbes and liver are especially good at deactivating when taken orally.   They are deactivated either through the formation of various structurally related -epi breakdown metabolites called SREMS.  Technically these are glucuronide / sulfate conjugated derivatives as well as weird ring fissured stuff, some of which show activity, however probably only after being retransformed into parent -epi at target tissues in the body.

To put all this into perspective, studies have indicated that less than 5% or so unchanged -epi reaches systemic circulation after oral ingestion, and the rest are these derivatives of varying unqualified benefit.

Now oral -epi supplements have been around for a while.   And granted they do work, and have been shown to work (lower blood pressure for example) in some studies.   But this is not a testament to oral -epi being “good enough”.   In my opinion,  it only shows that the stuff is powerful enough to cause measurable physiological effects even if only a little gets into the system.   But what if we were able to get a lot into the system, what would we see then?

How to get “a lot into the system” has been one project of mine.  Now I could always make an injectable out of it, but that’s sort of not convenient and very not legal.   However, I can use the route through the skin which I have done successfully before with various compounds.   This only works for certain things, as many compounds are unsuitable for this, or require formulation technique to overcome obstacles.

Before I detail these obstacles, let me quickly review the science of the skin route.   Its advantages are 1) bypass of gut microbial degradation and liver first pass metabolism which breaks down and/or ties up many compounds (polyphenols especially) and 2) time release effect due to slow transit through the various skin layers to the capillary system in the dermis (obviating the need for multiple daily dosing and allowing for steady state blood levels over time).  Of course there are downsides as well.  Only certain types of compounds qualify as candidates for this sort of delivery, and many of these require “coaxing” of some sort to get appreciable levels through.   Nonetheless, when it comes to things with such terrible oral bioavailability you don’t need to get a ton through to achieve a vast improvement in efficacy

Like I said -epi is problematic.   On the plus side its solubility and molecular weight are pretty good for this delivery.   Still, by itself it wont budge through well (not sure why).   It took some research on my part to discover that there are natural compounds called terpenes which can increase penetration of catechins profoundly.   One of these terpenes demonstrated increases for epicatechin in orders of magnitude which I found remarkable.   A big hurdle was overcome with that discovery

Problem two is in solution this stuff is not stable.   It turns yellow as it breaks down and polymerizes in the presence of light.   Light is everywhere, and even in amber bottles this is still going to happen.   This is a photon induced free radical reaction so the obvious way to minimize this is to include some sort of free radical scavenger in the mix, and something FDA approved as safe would be nice.   I knew exactly what would would do the trick.     Of course the proof is in the pudding so I made a control solution (of  topical liquid not pudding) without the scavenger and one active solution with the scavenger.   The one with the scavenger stayed light colored, while the other turned progressively yellower and darker.

Right now, we have this exact formula bottled and labled and sitting out on the floor.   It will be going on the prototype nutrition site ( and it will be called (-)E spray.   As for my personal experiences with this stuff (which I have been making for months) I initially had a burst of cardio endurance and then over time fat loss in the abdomen.   Then in the skin over the abdomen.  Then other places.   My weight dropped.  People noticed my face and belly bloat had gone and my six pack came back.   Now I won’t lie, I upped the training (this gets easier when something expedites results) and as for the diet, well, made a little better but nothing major.   After xmas and gorging on carbs and fat I got back to Illinois and went to the mirror I use that is a constant and I saw no change.   Granted this was not a one week thing, and the fat loss I experienced was substantial so naturally it’s not gonna happen in one week.   But it is working and it continues to work even as my training and diet have taken the usual holiday nosedive.   Now I have not gotten more or less stronger than I normally would have with my training so I would not call this an anabolic, but I don’t give a damn because I have muscles you can see now.   And one more thing – I am experiencing less aches and pains and my workouts are much faster.

I think that does it.    (-)-Epicatechin, making it work, and what I felt over time using it.   I’d love to see if others see the same results so I can remove any uncertainty I have that I have a winner here






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