Demystifying the Benefits of Food-Based Alkaloids

Alkaloid-rich foods have gained tremendous popularity over the last few decades because of the purported various wellness benefits. One of their most prominent representatives on the market in North America is the Southeast Asian Kratom leaf, which is traditionally chewed by the local farmers to ease a hard day of backbreaking labor, or powdered, and mixed into a matcha-like concoction to be enjoyed by Westerners. More notorious examples are tobacco plants, and coffee beans, among others. Nevertheless, despite limited scientific evidence supporting some daring claims about the beneficial properties of these natural gifts from gardens, farms, forests, and even jungles, people still have their reservations about utilizing many of them. 

The reason for this adaptation hesitancy might lie in cultural ignorance. After all, humans instinctively fear what they don’t understand, and for a good reason. Uncharted territories can be quite dangerous. However, just like with these bioactive consumables, their seemingly frightening character owes more to the lack of knowledge on their proper “path of exploration”, rather than them, per se. Each and every person can get the most out of these products if only they were aware of what they are, and how to use them. 

Let’s dive in!

What Are Alkaloids?

Alkaloids are nitrogen-containing physiologically active organic compounds produced by most organisms, spanning all biological kingdoms and domains of life. In their pristine state i.e. as free-bases, they are relatively alkaline; hence, the name and almost universally bitter taste. Plants make them from amino acids and related substances for a variety of reasons. Because some are synthesized for passive protection against predators, and some are responsible for growth regulation and nutrient storage, such substances can be poisonous, or may even possess therapeutic properties. Oftentimes, since the organisms themselves need to survive while maintaining a certain level of these chemicals to fend off attackers, the difference between a beneficial alkaloid, and a harmful one is its amount or concentration. While the latter may be tolerable, or even good for any given plant, the same dose could be lethal for some unfortunate hungry mammal. Reduce the exposure, and that poor animal might actually gain something good from seemingly the same compound. The reason for this disparity in reaction is that the metabolic processes may differ widely between varying species, or even individuals, let alone between members of different biological kingdoms; hence, at the first glance, dangerous alkaloids can be employed for good, and even benefit our health if applied correctly. Limited scientific inquiry helps us figure out how, and overwhelmingly supports this notion. 

Generally, people in positions of authority have trouble recognizing complexities involved in biopharmacology and supposedly “scientific” journalists made the matters worse, dabbling in damaging sensationalism. It is no wonder. The reductionist Western medicine attempts to simplify healthcare to the point that severely restricts any ground-breaking innovations nature has already provided for us and the public is more attracted to negative news stories. Whether the malfaisance on their part is intentional is utterly irrelevant. Lack of understanding, or care has led them to smear the reputation of alkaloids-boasting foods over the years; however, the alarmists seem to forget the old adage: “Sola dosis facit venenum” (The dose makes the poison), and it couldn’t be more true in this regard.

Bottom line: if you are tempted to indulge in some alkaloid-rich products, by themselves, or as an ingredient in an exotic recipe, you’ll be fine as long as you do not stray too far from the recommended amounts and handling instructions. Hell, you just might even benefit from it.

What Are the Most Prominent Alkaloids Found in Consumable Plants?

Here is a list of the good alkaloids most often found in plant-based foods:

Atropine

Atropine occurs in many plants belonging to the nightshade family. While the most famous member of the family, Belladonna, is highly poisonous even in small amounts, its close relatives are healthy and delicious. They include the tomato, potato, eggplant, bell pepper, chili pepper, some berries and many other species.

At low doses, atropine relaxes the smooth muscles of the digestive system, bladder, skin and various parts of the body. It also increases the heart rate. Doctors use it to treat some heart problems and the symptoms of insecticide poisoning. On the other hand, at high doses, atropine can cause confusion, hallucinations and exaggeration of its other effects. The poisonous nightshade contains both high doses of atropine, and other alkaloids like scopolamine and hyoscyamine intolerable for humans even at low doses; hence it cannot directly be utilized for our benefit. Nevertheless, knowing the muscle relaxant properties of atropine, industrious women of the Middle Ages found a cosmetic use for its oil, dropped into eyes: pupil dilation, which signals sexual arousement to the opposite gender, similarly to red blush and lipstick. Unfortunately, they were not aware of the systemic damage this produced as the poison made its way into the general bloodstream. If it’s any consolation, at least the poor gals were able to reproduce before it became apparent… and oculists nowadays have a handy tool for eye exams.

Capsaicin

Capsaicin is the alkaloid responsible for the spicy taste of chile peppers like cayenne, tabasco, jalapeno etc. It produces a burning sensation when it comes into contact with various body tissues. This makes it the active ingredient for pepper spray. In medicine, capsaicin cream is used for treating backaches and joint pains because it works similarly to heat therapy. 

The alkaloid’s mechanism of action is mediated through the TRPV1 nociceptive receptors, which are partially responsible for the burning sensation. Because of capsaicin’s agonistic reaction with the system, scientists are currently exploring its potential role in combating obesity, as it mimics the metabolic “exercise mode”, and it was also recently found to be a symptomatic reliever of Cannabinoid Hyperemesis Syndrome (CHS), previously remedied with steamy bath soaks. Hot stuff, eh? *touch* Pshh.

Catecholamines

Catecholamines are a subtype of monoamines which include adrenaline, noradrenaline and dopamine. Human body produces these natural stimulants in the adrenal gland from each other, starting from tyrosine amino acid, or its precursor phenylalanine. At normal blood serum concentrations, they sharpen your mind, wake up the rest of your body and reward you with a sense of accomplishment from gratifying behavior. At higher quantities, released in stressful situations, or through consumption of psychostimulants, these hormones/neurotransmitters get you ready for the so-called “fight-or-flight response.” However, chronically high catecholamine levels can lead to sleep problems, palpitations, hallucinations and other issues.

While there aren’t any plant-based foods rich in fully formed catecholamines, there are a few that temporarily increase their blood concentrations: coffee, tea, bananas, citrus fruits, vanilla and cocoa. Usually the other phyto-stimulants like caffeine and theobromine in these products are responsible for the feedback release of the natural ones; however, consuming their precursor amino acids, which are ubiquitous in modern food supply, can also build your stock piles, and may be more beneficial in the long-term. While forcing an increase of active concentrations in the blood serum with releasing agents sounds appealing, it actually results in lower baseline amounts down the line. On the other hand, once the human body accumulates enough catecholamine supply, it releases them more readily without this downside.

Unfortunately, there are rate-limiting steps in the conversion of one amino acid to another, before they get to the gland and turn into dopamine, so going for the most direct precursor, L-Dopa, might be your best bet. Please be mindful that L-Dopa is actually a part of the prescription regimen for Parkinson’s disease, characterized by catecholamine deficiency. Without another prescribed medicine preserving the amino acid in its pristine state in the gut, it may convert into the cardio-vascularly damaging dopamine before it passes the blood-brain barrier, which is no bueno. It remains in the periphery, wrecking havoc because none of it can get to the brain once synthesized. Nevertheless, the consumption of the Velvet Bean (Mucuna Pruriens) extracts, which are 15% L-Dopa, seems to not present such issues for a reason that is so far poorly understood, but most probably have something to do with the remaining components of the bean. In fact, limited research, as well as traditional use by the locals, promises a world of benefits for motivation and male fertility with few side effects. Guys, take note.

Methylxanthines

Methylxanthines are an alkaloid group that boasts celebrities like caffeine; however, the lesser known theophylline and theobromine belong to this class as well. Their natural plant sources include coffee, cola, guarana, cocoa and tea among others. They are so ubiquitous because xanthine, the precursor compound, is present in surprisingly vast numbers of living organisms.

Methylxanthines are stimulants with antioxidant and anti-inflammatory properties. Both may help lower risk of cancer and tolerate chronic pain associated with various health conditions. They can also loosen up the lungs’ smooth muscles, which control oxygen entry and carbon dioxide removal.

Because of their bronchodilating and vasoconstricting effects, caffeine is given to newborns with breathing problems and some patients with chronic headaches. Meanwhile, theophylline and theobromine are used on people with asthma and COPD.

In contrast to other more dangerous stimulants like amphetamines, methylxanthines work backwards, and indirectly. Instead of indiscriminately releasing dopamine followed by a cascading reaction where it converts uncontrollably into the rest of catecholamines, caffeine-type “uppers” target the adenosine receptor system, responsible for preparing your body to sleep on the cellular level. By binding the receptors without activating them, methylxanthines compete with adenosine, thereby blocking its function. In a natural feedback response, as the body receives the message that sleep is off the table, the adrenal gland releases adrenaline to boost wakefulness and awareness, which has a relatively minor ripple effect on its related neurotransmitters. Higher doses produce more adrenaline, which has a greater impact on the other catecholamines and results in a higher risk of adverse reactions. As more ATP (adenosine triphosphate) molecules are broken down by cells for energy, the concentration of the sleep-inducing compound increases and reaches a point where it outcompetes these natural stimulants, rendering them ineffective. Hence, tolerance to this excitatory effect rises rapidly and is largely dependent on individual baseline sensitivity to adenosine. So don’t go crazy, kids. Perhaps, that 8th cup of coffee is not doing you any good today, or… ever. 

Nicotine

Nicotine is an alkaloid related to the vitamin B3, niacin (nicotinic acid). It is most abundant in tobacco leaf, with trace amounts present in nightshade vegetables and tea. At low doses, it can stimulate the brain, nerves, heart and blood vessels, which sharpens mental focus and wards off anxiety. 

Nevertheless, chronic nicotine intake is extremely addictive, and acute toxicity from an overdose is not pleasant, at all. As much as 33% of once-a-month smokers go on to develop an addiction, and more than 70% of those who begin smoking daily suffer the same fate. Meanwhile, consuming it on an empty stomach may also cause the smoker to become sick. Still, it is important to the field of medicine because it helps people quit smoking tobacco, which is by far the greatest threat associated with this alkaloid. Trouble is that due to its chemical similarity to the Vitamin B3, edible concoctions may outcompete the latter for absorption in the gut, and result in a dangerous deficiency in the process. For that reason, replacement therapies are focused on different routes of administration like vaporizers, transdermal patches, and gums.

Opium Alkaloids (Opiates)

The poppy seed is one of the favorite food garnishes in many European and Asian cultures. After all, it is a staple in a wide variety of dessert options worldwide. While the vast majority of people are familiar with the black pinhead balls, few are aware that they contain trace amounts of opium alkaloids, opiates, a chemical class that includes morphine and codeine. It is not that surprising, however, considering they come from opium poppy plants (Papaver somniferum L.), which is the most abundant source for these compounds. Remember “The Wizard of Oz”? Yeah, those poppies. The vast majority of alkaloids are derived from poppy milk, opium, contained in the budding flowers; however, non-processed seeds also get a little bit of the action by association. At strictly controlled doses, opiates can relatively safely alleviate pain, coughing diarrhea, and supply a euphoric experience that will be hard to forget. That being said, overdoses are extremely dangerous and may cause nausea, projectile vomiting, unconsciousness, seizures, and respiratory depression, which may end fatally. Chronic opiate, and related synthetic/semi-synthetic opioid intake is likely to lead to addiction, as well as liver damage. This is facilitated by progressive tolerance increases that may also lead to people taking more than they need, or can handle.

While generally all natural opiates, as well as semi-synthetic opioids, have a very similar target of action, the slight differences in their chemical structure contribute greatly to their ability to cross the blood-brain barrier and cause different side effects. This means that their potency disparity roughly hinges on the onset speed, which also varies with the concentrations consumed of any given one. The higher the amount in a single dose, the faster it gets to your brain, the more pronounced is the subjective experience. Hence, a couple of poppy seed dainishes won’t do much for you, but a tea made with a sizable amount very well might. Unfortunately, most of them on the market today are pretreated with heat and water to minimize the chance of that happening. The real chefs go for the raw thing, though, because that impacts the flavor these little balls of joy can contribute and a little side of euphoric alkaloids has never hurt anyone.

Piperine

Piperine is the main alkaloid found in long and black peppers and is responsible for their biting, spicy taste. It is quite similar to capsaicin in that regard, although the burning sensation is distinctly different. Not only is the former much less potent per pure weight, but also it appears tasteless the moment it makes contact with your tongue, after which the burning sensation follows. 

Aside from combating inflammation, piperine can boost your metabolism. In fact, the bioavailability of many nutrients and supplements, like turmeric, benefits greatly from its presence in the gut. The perks don’t end there. Limited research has suggested that it may even offset detrimental effects of a junk food diet. Regular intake of the alkaloid can help improve blood sugar control and prevent obesity, as well as fatty liver disease. Well, if one can handle it, that is. The aromatic properties of the source is another reason to add it to your recipe if that wasn’t enough to convince you.

Quinine

Quinine is a bitter substance most abundantly found in the cinchona plant. It is mixed in small quantities with seltzer and a dash of some sweeter flavoring to create tonic water. Strangely: some people love it while others just can’t stand it. Fun fact: the subjective perception of its taste is genetically determined. So if you can drink it and even enjoy it like any other soda, thank your ancestors. They did you a solid. 

This alkaloid is a potent anti-proliferation agent that only semi-selectively targets parasitic cells in the body; hence, it’s diluted in water for safe concentration to minimize the damage inflicted on healthy human cells. Quinine overdose produces irregular pulses, blood abnormalities, hypersensitivity and many other side effects. Historically, equatorial sailors mixed the alkaloid-based drink into cocktails with alcoholic beverages like gin for prophylaxis against malaria. Who said you can’t mix work with pleasure? They certainly did! Sadly, the fun did not last for long because the malarial parasite quickly mutated and developed tolerance to the substance. This started off a race to find a quinine derivative that would safely provide the now lost protection, which culminated with the discovery of the now infamous hydroxychloroquine.

Serotonin

Serotonin is a monoamine neurotransmitter/hormone of indoleamine subtype synthesized by the body from the essential amino acid tryptophan. The rich sources of the latter include leafy greens, pineapples, papayas, walnuts, bananas, coffee, turkey, along with nightshade berries and vegetables. While not an alkaloid, per se, it is structurally similar and its precursor is food-based. Just like every other neurotransmitter involved in CNS (central nervous system i.e. the brain and its direct nerves), this molecule by design cannot cross the blood-brain barrier, so even if there were rich food sources of serotonin, it would be utterly counter-productive to consume them. The indoleamine would remain in the periphery (i.e. the body), and potentially wreak havoc on its normal functions. In contrast, the precursor amino acids get uptaken up by transporting enzymes into the brain, after which the conversion takes place, and serotonin is stored in the neurons (brain cells), ready to be released when needed.

While it used to be considered a “happiness hormone”, there is a raging debate amongst psychopharmacologists, neurochemists, and neurologists whether the serotonergic signaling system is that simple. The initial thinking was born out by the extreme jubilating effect potent releasing agents like MDMA (“molly”/”ecstasy”) have on people. A competing theory suggests that it is actually a “hormone of misery”, and receptor downregulation (shut off) caused by overstimulation is what’s responsible for the feeling of content one experiences upon a massive serotonin dump. The piece of evidence that lends credence to the latter explanation is that serotonin reuptake inhibitors, SSRIs, which are widely used as a long-term treatment for depression, have little to none therapeutic value when initially administered. If the former theory was correct, they should cause an instant increase in activity of receptors by potentiating the already released serotonin and one would expect the benefits to not take long to follow. Unfortunately, that is not the case and most people need to take them for prolonged periods of time to notice any improvement; therefore, it is reasonable to assume that the delay is caused by a more gradual receptor down-regulation, which is the culprit of the general mood change. 

Healthy stores of serotonin also promote good sleep, and low levels are associated with insomnia. How so? Well, once the lights go out, the familiar rest-inducing hormone, melatonin, is derived by the body from it. If you’re tossing and tossing and turning, consider supplementing a bit higher up the stream.

The problem with ingesting tryptophan to boost serotonin stockpiles in the brain is similar to that of consuming tyrosine to do the same for catecholamines. The rate-limiting step of converting it into 5-HTP, which is then converted into 5-HT (the chemical name for the compound in question), presents a sizable barrier to any readily appreciable effects, unless a person is already extremely deficient. On the other hand, just like with its monoamine relatives, consuming the most direct precursor, 5-HTP, may theoretically prove dangerous for the heart valve because the conversion can also take place in the gut and the blood-brain barrier will not let the desired molecule reach the cognitive organ where it is safe to circulate. So far there are no solid studies on humans showing one way or another whether this possible side effect actually inflicts the damage serious enough to cause any issues; nevertheless, the effectiveness of the supplement would also go down, as peripheral serotonin is not in any way beneficial either. 

Kratom Alkaloids

Hailing from Southeast Asia, Mitragyna Speciosa tree is an extremely gifted plant in this regard. Its dried leaf, Kratom, boasts so many alkaloids that it would take a book to describe them all, especially considering their effect and mechanism of action are so elusive. Mitragynine is the most abundant and well studied of them all, comprising roughly 60% of the total alkaloid content. Its primary metabolite, 7-hydroxymitragynine, makes up roughly 2% of it while speciogynine and paynantheine are second and third most concentrated alkaloids, respectively, having barely distinguishable structural deviation from the primary one. The rest are present at concentrations below 1%, so the lion’s share of the perceptual effects people expect from Kratom most likely does not come from them. Despite that, their isolated bioactivity appears to be widely divergent, ranging from immuno-stimulating to muscle relaxing, so it is possible that the more exotic alkaloids have their role to play in the overall reaction, as well.

The most intriguing part about these phytochemicals is that most of them are indole-based. The word may be familiar to you from earlier in the article, or if you’ve heard anything about psychedelics. Chemicals like serotonin, psilocybin, and LSD all share a basic chemical skeleton with Kratom alkaloids. Don’t worry, though. You won’t see anything unusual upon ingesting them. The mysterious part is that they can be both stimulating and relaxing. What you can experience only depends on the serving size.  

Even with all of the research taking place, somebody is yet to come up with a definitive answer as to how exactly these compounds work, what precisely they do, and what is the recommended serving size for any given individual. The fact that alkaloid profile tends to vary throughout batches, let alone locations, only complicates the matter. The drying process, soil composition, genetics and maturity level all contribute to the end product pros and cons. That being said, the most recent studies suggest that 7-hydroxymitragynine is the most potent molecule in the plant, despite not comprising an overwhelmingly significant portion of the whole. It is theorized that the conversion rate at which mitragynine turns into it in the body is what determines the nature of the psychoactive impact; therefore, the most pronounced difference in effect results from varying drying processes and maturity levels, which facilitate the same oxidative reaction before any of it is ingested. On the other hand, the general potency i.e. overall alkaloid content has less to do with the harvest/post-harvest processing and more with the growing conditions.

 

Sadly and unfortunately, FDA prohibits us from expounding any further on what consumers might expect from ingesting it. Best we can do is just forewarn you that there’s an addiction risk, and possibility of liver damage with an excessive intake combined with natural potentiators that block liver enzymes responsible for alkaloid breakdown. The examples of these include white grapefruit and dandelions among other botanicals, fruits and vegetables. Please, proceed with caution, and try to familiarize yourself with other, less restricted sources. Happy hunting! 

How Can You Maximize the Benefits of Foods Containing Alkaloids?

As one can see from the descriptions of select alkaloids, dose doesn’t always make the medicine. Some of them contaminate harvested crops, while others form due to poor storage conditions and none of them are good for you. Others, like the steroid alkaloid solanine, are present in trace amounts and can accumulate in the body when taken for prolonged time periods.

How can you avoid toxins when consuming alkaloid-rich foods? Here are some tips:

  • Wash fresh fruits, grains and vegetables thoroughly before consumption to eliminate harmful contaminants like pesticides.
  • Store food under the best conditions. For example, kratom and nightshade are especially sensitive to sunlight, so it is best to keep them in a dark storage space. In General, low temperatures and humidity prevent bad alkaloid or microbial formation and vitamin losses.
  • Cook your food well to reduce plant toxins that denature with heat and may accompany all the goodies you are looking to get. Be careful to not degrade them as well, though.
  • Keep a well-balanced diet. Remember that anything taken in excess can hurt you. Balancing your intake limits your exposure to any alkaloid group.

Following these suggestions will help ensure that your alkaloid infused gastronomic experiences are nothing but pleasant and healthy.

The Bottomline: Alkaloids and Health Maintenance Go Together

Just like with everything in life, proper consideration and moderation are crucial. Choosing a product that is right for you, and using it sparingly while following all recommended procedures will most likely turn out great despite all the dangers ascribed to them. However, these housewife tales are not completely without merit. The impact the alkaloid-rich foods have is profound and can go both ways. As long as you are fully cognizant of this, your experience with them will be the one for which your brain, mind and body will thank you.

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