On Willow Bark, Aspirin, Papain and Papayas

 

On Willow Bark, Aspirin, Papain and Papayas

 

by:  ju-boo lim

 

Yesterday evening I received a small information through our WhatsApp Chat from Professor Andrew Charles Gomez, a very famous Senior Consultant Otolaryngologist (ENT Surgeon), and a friend of mine about willow bark below in purple-pink (with minor editing to remove unnecessary icons)   

“Have you ever wondered where aspirin came from? Well, let me take you on a journey back in time, to the banks of rivers where graceful white willow trees have been growing for centuries. These trees hold a secret that our ancestors knew very well - a natural pain reliever that's been used for millennia.  In fact, willow bark, also known as Salix alba, was used all around the world. From the banks of the Nile to the riversides of China, from ancient Greece to South America, willow bark was the go-to remedy for pain and fever. Even Hippocrates, the father of medicine, sang its praises.

 Fast forward to the 19th century, and science starts to unravel the willow's secrets.

In 1827, scientists isolated salicylic acid from the bark. Then, in a stroke of genius (or perhaps a headache), chemists synthesized acetylsalicylic acid in 1897, giving birth to what we know today as aspirin. Now, in the modern world, white willow bark is making a comeback.

People are beginning to rediscover this natural remedy which offers relief from pain and inflammation without the harsh side effects often associated with synthetic drugs. When you consume white willow bark, your body converts salicin into salicylic acid - the same active ingredient found in aspirin. But because your body processes it more slowly, you get longer-lasting relief with potentially fewer side effects.

It's like nature designed its own time-release pain reliever.  Plus, it’s packed with flavonoids and polyphenols that fight inflammation and act as antioxidants.

Willow bark extract works in several ways.  It fights inflammation by blocking substances in the body that cause swelling and pain.  It acts as an antioxidant, protecting cells from damage caused by harmful molecules. It may even help fight certain types of cancer by encouraging the death of cancer cells, particularly in colon and lung cancers. So, whether you're battling arthritis, nursing a headache, dealing with period cramps, or just feeling achy, white willow might be your new best friend. Sounds all too good to be true right. Well, science has also put willow bark back in the spotlight.

A recent meta-analysis of five clinical trials involving 329 arthritis sufferers showed that willow bark significantly outperformed placebo in pain relief and improved physical function, without increasing side effects.

While more research is needed (isn't it always). One thing is clear: willow bark isn’t just a relic of the past. It's nature's time-tested pain reliever, making a grand re-entrance into the world of natural health.

So, the next time you reach for pain relief, why not consider this ancient remedy. After all, sometimes the best solutions are the ones that have been right under our noses - or should we say, growing along our riverbanks - all along. Ready to give it a try.

 Here are some ways to incorporate this natural remedy into your life:

Steep the bark in hot water for a soothing, pain-relieving tea. Take a few drops of white willow tincture under your tongue for quick absorption. Pop a capsule or tablet for those who prefer a no-fuss option. Look for creams or ointments for localised pain relief.

Please note that while white willow bark is natural, it's not for everyone. If you're allergic to aspirin, pregnant, breastfeeding, or taking blood thinners, it's best to steer clear.

As always, chat with your healthcare provider before adding any new supplement to your routine”

(End of Quote) 

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In response to Professor Charles Andrew Gomez letter, here’s my professional view comparing natural salicin in willow bark with synthetic aspirin which is a chemical called acetylsalicylic acid.

Willow bark, the bark of several varieties of willow tree, has been used for centuries as a pain reliever. The active ingredient in the medicine made from willow bark is called salicin, but the accompanying flavonoids and other phytochemicals might be part of what make willow bark effective. For this reason, some people prefer to chew on the unprocessed bark of the willow tree. Aspirin is acetylsalicylic acid, and salicin is the precursor of salicylic acid, comprising about 1% of the white willow bark extract, whereas other glycosides comprise about 12%.

Some people use willow bark as an alternative to aspirin, particularly those that experience chronic headaches or back pain.

The question some of my very well-informed and university educated patients of mine, including some of my former clinician (medical doctor) colleagues they often ask me is, which would be better, safer, more long lasting, salicin from willow bark or synthetic aspirin in terms of clinical efficacy and side effects since aspirin being a NSAID (non-steroidal anti-inflammatory drugs) can cause gastric bleeding or other gastrointestinal irritation.

Some also ask me, does salicin or willow bark cause the same side effects as aspirin?

Let me try to explain using what I know in pharmacology and pharmacognosy integrated for comparison

Willow bark and its active ingredient, salicin, have indeed been used for centuries as natural pain relievers. The question about the comparison between willow bark (salicin) and synthetic aspirin (acetylsalicylic acid) in terms of clinical efficacy, safety, and side effects is quite pertinent.

The clinical efficacy of aspirin is widely known for its efficacy in relieving pain, reducing inflammation, and lowering fever. It is also used as an antiplatelet agent to prevent blood clots, making it beneficial for patients at risk of heart attack or stroke.

Because aspirin has been extensively studied, its dosage and effects are well understood and predictable. But if we compare willow bark (salicin), this is a natural medicine from the plants which also contain not just salicin, but many other supporting phytochemicals and flavonoids than pure synthetic aspirin. Their combined synergistic action with other natural compounds is considered safer, more effective and more advisable for long-use for mild to moderate pain relief together with its anti-inflammatory properties. See also details of this explanation here:

https://scientificlogic.blogspot.com/2024/07/growing-acceptance-of-traditional.html

A passage taken from the above link is explained here in chocolate colour:

“In TCM its medical principle is on balancing Yin and Yang, Qi (vital energy) flows through meridians. TCM is not just about acupuncture, moxibustion, cupping and massages. It is much more than these. They too use medicinal herbs and other natural botanical medicines running into hundreds of different kinds. They are used in combination with each other in low dosage to avoid toxicities and for sustained therapeutic effects.  Their combination in low dosage, unlike synthetic drugs that is given in isolation at higher dosages, is aimed at a holistic approach so that these combination herbal medicines are working in different directions to provide a synergistic effect that will provide a much better and sustained therapeutic outcome than using a single drug working alone in isolation. The synergy of a combination of several natural medicines from different plants and herbs working together holistically naturally would produce a therapeutic effect greater than the sum of their separate effects. This is so unlike a pure isolated drug working alone as practised in conventional allopathic medicine. 

Another way of putting this is, it is like forcing a table to stand on one or two legs no matter how strong instead using four legs. How could we expect the body to establish homeostasis or yin and yang using a single pure and isolated chemical drug instead of a combination of several low dose medicines from plants and Nature. But the health of the body depends almost entirely on its ability to establish biochemical and physiological homeostasis or yin and yang. Think this over logically with a scientific brain  

This is one of the setbacks in conventional medicine where a single, pure, and isolated drug is given for life just to control the disease such as diabetes, hypertension or other cardiovascular diseases, etc with no hope of any permanent cure. A combination of natural plant-based medicine prescribed at low dosages is just like a charcoal or coal fire that produces heat and warmth for a very, very long time, unlike a petrol fire that is similar to pharmaceutical drugs that suddenly burst into a huge flame and soon dies away unless more petrol is added to keep the fire burning. That is why some drugs need to be taken for life. Which would you prefer? But pharmaceutical companies want it this way for their continuous business.”

(End of Quote)  

However, high doses or long-term use of salicin can still cause gastrointestinal issues similar to aspirin, such as stomach cramps, nausea, and ulcers.

To explain slightly further, the presence of other compounds like flavonoids and polyphenols may enhance its therapeutic effects, although the exact contribution of these compounds is not fully understood. However, there is less clinical data on willow bark compared to aspirin, making it harder to precisely predict its exact clinical efficacy and optimal dosage.

On the safety and side effects aspect, aspirin common side effects include gastrointestinal irritation, ulcers, and bleeding. These occur because aspirin inhibits cyclooxygenase-1 (COX-1), an enzyme that protects the stomach lining. It can also cause allergic reactions in some individuals and should be used cautiously in those with certain medical conditions, such as asthma.

Whereas for salicin in willow bark this is generally considered gentler on the stomach compared to aspirin because salicin is converted to salicylic acid after it is absorbed in the intestines, which may reduce direct gastric irritation. Since willow bark contains other active compounds, there is a potential for interactions and side effects do not present in aspirin.

In terms of dosage control aspirin provides a standardized dose, ensuring consistent therapeutic effects. Willow bark, being a natural product, may have variability in the concentration of active compounds, leading to inconsistent efficacy.

Willow bark's additional compounds may offer complementary health benefits but also introduce variability and potential for side effects. These additional natural compounds provide phytochemical benefits over synthetic aspirin.  For chronic conditions, long-term safety is a key consideration. Aspirin's side effects are well-documented, while the long-term safety profile of willow bark is less clear due to fewer studies.

But for acute use, aspirin may be more effective and predictable due to its well-researched pharmacological profile. However, it comes with a higher risk of gastrointestinal side effects.

But for chronic use, I would strongly recommend and prescribe willow bark as this might be preferred by those looking for a natural remedy with potentially fewer immediate gastrointestinal side effects. Nevertheless, users should be cautious about long-term use and potential variability in effectiveness and safety.

Ultimately, the choice between willow bark and aspirin should be guided by individual health conditions, the severity of symptoms, and in consultation with a well-versed and qualified clinician who is trained in both, conventional drug-based medicine as well as in botanical medicine. Unfortunately, it is very hard to find such a doctor with a double university degree in integrative medicine.  Only such as medical doctor trained in both areas of medicine can consider personal medical history and potential in conventional allopathic drug-based medicine and in natural medicine

Let me give you another example in both these two areas of medicine I am familiar with.

Papain is a proteolytic enzyme derived from the latex of papaya. For this reason, the crushed leaves of papaya containing the milk of papaya is used as a meat tenderizer. If someone were to take papain tablets, he may get nausea and gastric discomfort. Would he experience the same if he eats papaya, even raw papaya or its leaves?

 If he eats raw papaya together with its latex, then why is it he does not suffer from gastric discomfort, since papaya latex too has papain?  Is it because papain from papaya is in the natural form, whereas pharmaceutical papain is synthetic which has a slightly different molecular configuration? Let’s try to answer this very challenging question that is beyond the expertise of medical doctors. Perhaps nutritionists are more qualified to explain and able to answer this question.  

Eating natural papaya, including raw papaya and its leaves, generally results in fewer side effects compared to taking papain tablets. Here's why.

Consuming papaya in its whole form, we are not just ingesting papain. Papaya contains various other components like fibres, vitamins, and minerals that may help buffer and moderate the action of papain, reducing its direct impact on the stomach lining. There are other enzymes and compounds in papaya too.  The presence of other enzymes and compounds in natural papaya can have a synergistic effect, possibly reducing irritation and aiding in digestion. The amount of papain ingested from eating papaya is much lower and more gradual, leading to a milder effect. Consider also their natural vs. synthetic effects on the body.  

Even though the papain in papaya is natural, it’s unlikely to be significantly different in molecular structure compared to pharmaceutical papain, as both are derived from the same enzyme. However, the natural form in the context of the whole fruit or leaves includes additional bioactive compounds that can affect how our body responds.

Consider the digestive process of the whole papaya too.  The natural fibres and water content in papaya can help to slow down the digestion and absorption process, reducing the likelihood of gastrointestinal discomfort.

This is different with concentration and dosage for papain tablets. The tablet typically contains a concentrated form of the enzyme. This high concentration can be more likely to cause irritation and discomfort in the gastrointestinal tract, especially if taken on an empty stomach or in high doses.

Even though pharmaceutical papain is usually derived from natural sources, its purified and concentrated form can lead to a different interaction with the digestive system. Furthermore, papain tablets can rapidly release a high concentration of the enzyme, which can irritate the stomach lining and lead to symptoms like nausea and discomfort.

To make this easier to understand for everybody, for medical doctors and for non-clinicians, natural form of papain in papaya, consumed as part of the whole fruit or leaves, is less likely to cause gastrointestinal discomfort compared to the concentrated form in papain tablets is due to the lower concentration, the presence of other moderating compounds, and the slower, more buffered digestion process.

Do you think my explanation is correct?  If not, you should then challenge me to explain why it is if a patient were to take pharmaceutical papain together with food or after food, some would still get slight nausea since the food would have acted as a buffering agent and have diluted the direct action of the papain? Readers who are intelligent enough should challenge me to explain this.

Here’s what I would tell all of them. Even when taken with or after food, pharmaceutical papain can still cause slight nausea due to several factors.

First, the high concentration and potency of pharmaceutical papain, meaning, even when diluted by food, the enzyme remains highly concentrated compared to the natural amount found in papaya. This high potency can still lead to irritation in sensitive individuals.

Second, the proteolytic activity of papain (ability to break down proteins) is strong, and even in the presence of food, it can irritate the stomach lining or affect the digestive process in a way that leads to discomfort.

Third, there is also individual sensitivity, meaning variability in response.  People's tolerance to digestive enzymes varies. Some individuals may have a more sensitive stomach lining or a different gastrointestinal response to concentrated enzymes, leading to nausea despite the presence of food.

Fourth, consider their formulation differences for tablet composition. The other components in the pharmaceutical formulation, such as binders, fillers, or coatings, might also contribute to gastrointestinal discomfort. These additives can sometimes cause reactions or alter the release and absorption of the enzyme.

Fifth, there is delayed release, extended exposure, and absorption. In some cases, the papain might not mix evenly with the food, leading to localized high concentrations that can irritate the stomach lining over time, even if the overall dosage is diluted.

Sixth, there is gastric emptying and timing and interaction with food.  The timing of taking the papain tablet relative to meal can also affect how it interacts with the stomach contents. If the tablet is taken too soon before or after a meal, it might still come into contact with the stomach lining in a concentrated form.

To make my explanation simpler to understand for everyone without needing to undergo a formal technical course in both pharmacology and pharmacognosy like I did years ago, despite the buffering effect of food, the high concentration and potent proteolytic activity of pharmaceutical papain, individual sensitivity, formulation differences, and timing of ingestion can still lead to slight nausea or gastric discomfort.

This is the huge difference between the choice of conventional drug-based medicine and natural botanical medicine.

Which one would you prefer? WHO estimates nearly 90 % (80 – 88 %) of the world population, including those from well-educated advanced countries like China, United States, Europe as well as the UK uses traditional medicine due to their clinical efficacies and long-term positive outcome.

Take care with the medicine you chose and take!