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Ultimate Guide to Nootropics | Part 6 | Choline

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Choline is an essential nutrient that is found in a variety of foods such as eggs, fish, cauliflower, broccoli and soybeans. As an isolated nutrient, it participates in a wide range of physiological processes, but most importantly it is the main dietary precursor to the neurotransmitter Acetylcholine. It modulates cell integrity and is an important methyl group source. Via these three processes, choline affects many critical biological processes. For example, acetylcholine is highly involved in cognition and inflammation, cell integrity, and is also very important for cognition. This is due to the way it regulates brain tissue formation and maintenance. Choline being a methyl group source affects DNA methylation, which controls a lot of biological processes. Since choline is used in so many different processes, it is possible to develop a choline deficiency if dietary choline levels aren’t sufficient. Due to the fact that choline is a regulator of such important physiological functions, a deficiency could bring a whole host of negative effects with it, such as impaired cognition and the development of non-alcoholic fatty liver disease. Therefore, it is important to maintain adequate choline levels.

To prevent a choline deficiency, it is recommended that men consume 550 mg and women consume 450 mg of choline a day. This can be achieved either through diet or with highly bioavailable choline sources such as alpha-GPC, citicoline, and choline L-bitartrate. The benefit to supplementing with these also reaches far beyond simply correcting a choline deficiency, because even in individuals with adequate choline intake, they can increase cognition, decrease inflammation and increase exercise performance. Thus, supplementing with one of these choline sources will cover all your bases, ensuring that choline levels stay at healthy levels, whilst reaping the auxiliary benefits of them, too. The remainder of this blog will cover all of the different choline sources and their unique auxiliary effects, so that you can select one that will best fit your needs.

Choline L-Bitartrate 

-Prevents Choline deficiencies

-Does not significantly alter brain choline levels

-Enhanced bioavailability

Choline L-Bitartrate is the most basic choline source. By weight it is 41% choline, with the rest being tartaric acid. The tartaric acid enhances the bioavailability of the Choline to the body. However, choline L-bitartrate has a very hard time getting into the brain.

This choline source would be well suited for fixing a choline deficiency and aiding various bodily functions that rely on choline. However, it should not be your main choice if you’re also looking to enhance cognition, due to its limited availability to the brain. That being said, choline L-bitartrate is the most economically friendly source of choline when it comes to reversing deficiencies. It’s just not the most potent version from a cognitive enhancement standpoint. 

Alpha-GPC

- Prevents choline deficiencies

- Most efficient choline source at increasing choline levels in the brain

- Supports the structure of cellular membranes

- Acutely spikes growth hormone secretions, which can enhance exercise performance. 

Alpha-glycerophosphocholine, also known as alpha-GPC, is a naturally occurring choline containing compound which is present in our brains. In our brains, it acts as one of the main precursors for acetylcholine and phospholipid synthesis. It has been shown that when cholinergic neurons are running low on choline for acetylcholine synthesis, they react by breaking down cellular membranes that are made up of choline containing phospholipids. This releases alpha-GPC, which is very readily turned into acetylcholine. Due to this, when alpha-GPC is supplemented, it makes it into the brain rapidly and significantly increases brain acetylcholine levels. In fact, no other choline source is as good at increasing acetylcholine levels in the brain. Furthermore, supplementing with alpha-GPC can increase phospholipid synthesis, because besides choline, it is also a source for glycerophosphate; an important factor in phospholipid synthesis and cellular membrane structure. Thus, alpha-GPC can provide choline for starved cholinergic neurons and rebuild the cellular membranes that have broken down. This makes it a well suited neuroprotective agent in cases of acetylcholine depletion. Taken together, an increase in acetylcholine synthesis, coupled with supporting cellular structures, can result in cognitive enhancement. This is further reinforced by alpha-GPC being a protein Kinase C (PKC) activator, which is a regulator of proteins that are involved in cognition such as the MARCKS proteins.

Alpha-GPC also appears to enhance exercise performance, likely by acutely spiking acetylcholine levels. This can produce two effects. Since acetylcholine is involved with muscle contractions, an increased cholinergic tone could make muscle contractions faster and more powerful. Another possibility is that the spike in acetylcholine, via a catecholaminergic pathway, causes a growth hormone pulse.

This choline source will be well suited for individuals who are wanting to increase both their cognition and physical performance, since those are the applications it is mostly geared towards. However, one precaution has to be taken with alpha-GPC. Rapid increases in acetylcholine appear to sometimes cause bouts of depressive symptoms in some individuals, and this effect has been noted with alpha-GPC. If this occurs, cessation of alpha-GPC will quickly reverse any depressive symptoms.

Citicoline (CDP Choline) 

 - Prevents Choline deficiencies

- Neuroprotective

- Enhances memory and learning

- Anti-addictive

- Increases attention 

Citicoline, like alpha-GPC, is another form of choline that is naturally present in our brains. It functions as the intermediary step in phosphatidylcholine synthesis. Due to this, citicoline can easily make it into brain and is readily converted to acetylcholine by cholinergic neurons. In addition to this, it also aids in the production of phosphatidylcholine, which is an important component of cellular membranes. These effects are all shared by Alpha-GPC, but what makes citicoline unique, is that it is not only a Choline source but it is also a cytidine source. Cytidine is rapidly converted to uridine, which has a lot of positive effects on cognition. Uridine is largely responsible for citicoline’s production of phosphatidylcholine. In addition, it is a P2Y2 agonist, which increase NGF/TrkA signaling. NGF/TrkA signaling is crucial for the maintenance of neuroplasticity and, in combination with increased phosphatidylcholine and acetylcholine synthesis, provides a robust neuroprotective and cognition enhancing effect.

Conclusion

In terms of attenuating a choline deficiency, choline L-bitartrate would be the most straightforward and economically friendly approach. It will reliably increase bodily choline levels; however, it won’t be able to increase brain choline levels to a significant degree. If you wish to attenuate a choline deficiency but want to benefit to a greater degree both mentally and physically then either alpha-GPC or citicoline would be a good choice. If you are after a physical performance boost then alpha-GPC will be a good choice, but if you are looking at a more comprehensive neuroprotectant and cognition enhancer then citicoline would be the preferred choice. 

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