Caffeine is a very fascinating compound, which plays an enormous role in human civilization. In fact, it is thought that caffeine is the most widely consumed psychoactive substance on the planet! From a quick espresso, to hours long tea ceremonies, almost every culture on earth integrates caffeinated plants into their daily lives. What’s especially interesting to note, is that these caffeinated plants seem quite different from each other. However, they actually have quite a lot in common!
Unexpected Origins of Caffeine
Caffeine biosynthetic pathways developed in various species of flowering plants, most surprisingly in fact, various citrus species! Thus it is no surprise that the majority of caffeine-containing plants are in fact flowering plants. Coffee flowers are probably the last thing you think of when drinking a roasty cup of coffee, but the coffee tree does in fact display some beautiful flowers!
These flowering plants attract pollinators through scents and the nectar contained in the flowers. Recent research in fact found that when the scent of a citrus flower is combined with a very small amount of caffeine in the nectar, bees are more likely to remember the flower and return to it. Research has even indicated that small doses of caffeine actually have a cognition and productivity enhancing effect on bees! However, in higher concentrations, caffeine is a deterrent for bees, and other insects. Calibrated at just the right level though, and beneficial pollinators like bees can come back to get their fix of caffeinated nectar over and over, while pests are kept at bay by the deterrent effects of caffeine.
Clearly, caffeine serves a very important role for these flowering plants, and thus it is no surprise that caffeine is found in numerous different species of plants. However, humans aren’t buzzing around slurping down caffeinated nectar, so how did humans first come into contact with this energizing compound?
How Did Humans Discover Caffeine?
This is where things get tricky, and there are lots of different theories as to how humans first came into contact with caffeine. One common theory is that once humans discovered fire, and were able to heat up water, they started making water infusions of various leaves. This makes quite a lot of sense, a cup of tea is wonderful, but chewing on tea leaves is not a very pleasant experience. Additionally, caffeine is highly water soluble in the context of hot water. Caffeine is found in the leaves of lots of different plant species, which are found throughout the world. For example, Camelia sinensis (Asia), Ilex paraguariensis (South America), Ilex vomitoria (North America) and Coffea arabica (Middle East & Africa) leaves all contain caffeine and all seem to have a long established history of the leaves being used to brew infusions with.
Caffeine in Ancient Rituals
More than likely however, the first uses of caffeine containing plants likely were spiritual/ceremonial. These beverages would have acquired tastes, and would not be nutritious while demanding quite a bit of effort to make. However, caffeine, especially in ancient times would have had mind blowing effects on the consumers of these mystical leaf infusions. This would especially be the case for leaves that are especially rich in caffeine, such as the Ilex species. In fact, Ilex vomitoria and Ilex cassine have historically been used ceremonially by various different Native American groups, in a ceremonial beverage referred to as “black drink”.
Early Use of Caffeine
Other caffeine containing plants certainly seem to have been utilized ceremonially too. Theobroma cacao for example comes to mind, having been a highly important botanical for the ancient Mayans. Tea and even coffee have traditionally also been used ritualistically. One thing that all of these caffeine containing plants however seem to have in common, is that more often than not, they are made into beverages using hot water to extract bioactive molecules, of which caffeine is one of the primary bioactives! Thus, there likely is something to the theory that our first encounters with caffeine were facilitated via the discovery of hot water!
Fire’s Role in Coffee Evolution
Fire also, of course, led to the discovery of coffee which gets its characteristic flavors and properties, from fermentation, drying and most importantly, roasting processes. Coffee is much more complex and advanced than other caffeine preparations due to this, which in contrast mostly consists of picking leaves, drying them and infusing them in hot water. However, as civilization progressed, so did technological advancements in caffeinated products.
We often overlook the complexity of coffee—from cultivation and processing to drying, shipping, roasting, and brewing, it’s intricate.
Artisanal Coffee Cultivation Process
For top-quality coffee, it must grow at high altitudes, making hand-picking necessary, though challenging due to terrain. Sort the coffee cherries by density and extract the seeds from the cherry. Next, ferment and occasionally wash the seeds to eliminate the mucilage surrounding them. Dry the seeds in open air until they reach the ideal moisture level.
Coffee Bean Journey: From Harvest to Brew
Then the seeds have a coating of parchment on them, which needs to be removed. Green coffee beans, now obtained, are shipped worldwide to roasters. Roasters then take the processed coffee beans, and meticulously roast them, in a process where the coffee bean itself starts to function as a bioreactor that generates bioactive compounds. They then end up in the hands of homebrewers or professional baristas who need to precisely grind the beans to within exacting particle size standards. Next, dial in grind sizes to achieve the perfect cup of coffee. Humans have certainly spent A LOT of time, money and effort into making that morning cup of coffee many of us drink.
Caffeine’s Origin Story: From Coffee Beans to Isolation
Our obsession with coffee is vast, and has been the case for a long time. Thus, it is unsurprising that caffeine was first isolated from coffee beans, and in fact, this is where caffeine gets its name from. The actual isolation of caffeine is quite a fascinating story too, and resulted from the unlikely liaison of a poet and a chemist! At the time caffeine was isolated from coffee beans, coffee remained a luxury item, seldom consumed by the average person.
Thus, it was quite incredible that one of the most famous poets at the time, Johann Wolfgang von Goethe had quite the affinity for both coffee and science. Impressed by Runge’s demonstration, where he dilated a cat’s pupils with atropine, Goethe gave him a bag of coffee beans. Goethe’s purpose in the transaction was for Runge to isolate the then-unknown compound responsible for coffee’s distinctive properties. After experimentation, Runge successfully isolated caffeine, initially dubbing it “Kaffebase” (“coffee base”).
Synergies Of Caffeine Within Caffeine Containing Plants
When Runge isolated caffeine from coffee beans, he only discovered part of why coffee is stimulating. Over the years, we have discovered that coffee contains a plethora of psychoactive compounds. For instance, it harbors methylxanthines like theophylline and paraxanthine, akin to caffeine, albeit in minute amounts. Coffee beans’ beta-carbolines inhibit MAO enzymes, potentially amplifying caffeine’s stimulant effects, adding intrigue to their composition. Coffee beans also contain the unique compound trigonelline, which appears to have significant mood promoting effects.
Exploring other caffeine-containing beverages reveals caffeine’s frequent companionship with various bioactive compounds. Consider green tea: caffeine paired with L-theanine, alongside catechins such as EGCG and epicatechin, enriching its composition. Yerba mate frequently harbors abundant methylxanthines like theophylline and theobromine, complementing its high caffeine content. Yerba mate boasts various polyphenols and flavonoids such as rutin and quercetin, influencing caffeine’s effects. Theobroma cacao, notable for theobromine and caffeine, also contains endocannabinoid compounds like anandamide, adding to its intriguing profile.
Caffeine: Isolation and Synthesis
Plants always accompany caffeine with diverse bioactive compounds, altering its effects. Runge’s isolation of caffeine from coffee beans prompted focused research on caffeine in total isolation. Pure caffeine’s prominence surged with Hermann Emil Fischer’s 1895 total synthesis, making it easily accessible and widely used. Commercialization of pure synthetic caffeine took time, but its widespread availability followed swiftly, appearing ubiquitously. Synthetic caffeine is very cheap and abundant, so it’s easy to make pure caffeine products.
Pure isolated caffeine feels lackluster compared to traditional sources like coffee, yerba mate, or tea, subjectively speaking. Commercial energy drinks, typically with synthetic or isolated caffeine, also feature various bioactive compounds like taurine and B-vitamins.
Caffeine’s Effects: Personal Observations
Emiel, Noo-tropics.eu specialist, finds notable variations in effects between isolated caffeine and preferred delivery methods like coffee and yerba mate. In fact, I’ve even noticed stark differences in effects between different cultivars of coffee, and even coffees from different origins. For example, coffee beans from Ethiopia tend to feel smoothly stimulating with a prominent mood brightening effect. On the flipside, coffee beans from Columbia tend to have a much zippier and focusing effect for me. I recently brought this up on a reddit thread, and discovered others had experienced these differences too. I’ve even noticed that the type of coffee extraction makes a big difference too.
Espresso feels full-bodied, strong, motivating, and mood-boosting, while filter coffee tends to feel cleaner, stimulating, and focusing. This is somewhat independent of caffeine content, because contrary to popular belief, espresso actually contains less caffeine than filter coffee! James Hoffman recently demonstrated this brilliantly in a remarkable video.
This clearly demonstrates that caffeine appears to be highly modifiable by other compounds. Espresso extraction, under high pressure, may efficiently extract non-caffeine bioactive compounds like beta-carbolines from coffee beans compared to percolation. Caffeine remains a prime candidate for designing nootropic stacks, offering a versatile foundation for further exploration and innovation. Exploring beyond natural sources of caffeine, let’s delve into novel combinations achievable with pure isolated caffeine!
Synergies Of Caffeine With Other Plants & Compounds
When crafting caffeine stacks, primary goals include enhancing potency or smoothing effects for optimal results. For example, the majority of energy drinks that are on the market often aim to achieve both goals. Red Bull formula: 80mg caffeine, undisclosed taurine quantity, plus Vitamin B3.Vitamin B5, Vitamin B6 and Vitamin B12.
Simple formula: modest caffeine dose balanced by taurine’s calming effects for a smooth experience. B-vitamins enhance Red Bull’s mild energizing effects. With low caffeine and taurine, it offers a smooth experience.
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