Supplement Spotlight: Monolaurin, Allicin, Cascara, and LDN

I'd like to think I'm beyond my frantic ("natural") pill-popping days, birthed from fear of GI distress. As I recount in Breaking Free From SIBO: My IBS Story And “Cure”, an unpleasant bout of food poisoning coupled with 3 years living in a mold invested apartment catalyzed a transition from pride-worthy, resilient digestion, to unbearable bloating and bowel movements (or lack thereof), christened with a medical diagnosis of "SIBO": small intestinal bacterial overgrowth - a condition quite rampant in those struggling with IBS. Along the way, my thyroid took a hit as well, and addressing that aspect yielded a miraculous salvation in my digestive health (thank goodness!) While in the darkest moments of my SIBO days, I slammed my system with a seemingly unending slew of supplements, convinced each new supplement would be the one.

Much has changed since then.

I'm now comparatively hesitant of supplements, preferring to focus on a food-based approach to healing. I shudder looking at the hundreds, if not thousands, of dollars spent on false hopes encapsulated in gelatin or cellulose capsules. There are simply too many fluctuating lifestyle, diet, and environmental factors which can influence one's constitution at any given time, and ascertaining cause and effect with supplements yields muddy waters. I'm also increasingly wary of entering supplement attack mode, desiring instead to focus on restore mode. My goal these days is handle the bad guys (which I'm pretty sure are still hanging around to some extent), without encouraging the cascading inflammatory response often inevitable when you go to war, and which, quite frankly, I'm sick of.

So without further adieu, here are a few supplements I am currently using, in hopes of cultivating resilient health.

MONOLAURIN

Monolaurin from coconut oil

When I first supplemented with Monolaurin, its effects faded into the confusing supplement tapestry of the time. I recently decided to try it again now that I'm on the up and up, and I gotta say, I like this stuff. Like really.

Monoluarin (or Glycerol monolaurate) is a compound found in human breast milk and coconut oil, composed of lauric acid bound to glycerol. It harbors natural, antibacterial, anti-viral, and anti-Candida properties. These antimicrobial powers are the exact kind you want: very broad and powerful, while discouraging resistance, and also sparing "good" bacteria. Monolaurin basically targets all the bad things all the time, without losing steam, and without making your body freak out in the process.

Studies have validated monoluarin's effectiveness against an overwhelming span of microbes responsible for disease, including anaerobes, aerobes, gram-positive bacteria, gram-negative bacteria, non-gram-staining bacteria, particularly resilient mycobacteria (oh hey tuberculosis and leprosy!), viruses, and fungi. In fact, a 2016 study found monolaurin rivaled the primary heralded anti-fungal drug, fluconazole, in effectiveness for combating Candida. Pretty cool.

Monolaurin can target these nefarious organisms' biofilms: complex protective matrixes of sugars, proteins and acids, something conventional antibiotics typically don't touch. It may also target membranes and prevent viruses from attaching to the body's cells. Furthermore, these various microbes do not typically develop resistance to monolaurin, which is too often the problem with modern antibiotic therapy. And yet even given its awesome power, monolaurin does not affect the "good" bacteria we need, such as lactobacilli. This is possibly because these good bacteria produce their own tetramic acids which act similarly to monolaurin, familiarizing them to the compound.

But wait! Here comes one of my favorite things about monolaurin!

Normally, entering #attacktheinvaders mode results in a slew of inflammatory chemical messengers. Studies show, however, that monolaurin may actually down regulate some of the genes for the body's own pro-inflammatory cytokines (such as IL-1α and IL-1β.) This lack of inflammation also further hinders viruses and fungi. Basically, monolaurin lets you go to war with less worry of collateral damage. This makes monolaurin a total win in my book, since dealing with inflammation is one of my least favorite things about supplementation. 

As summarized in Glycerol Monolaurate Antibacterial Activity in Broth and Biofilm Cultures , "We refer to [Monolaurin] as a dual acting anti-infective because it kills bacteria, while at the same time stabilizing mucosal and skin surfaces to prevent inflammation that may be required for microbial infection to occur. [Monolaurin] has many advantages to other agents because of its safety record and because resistance is unlikely to develop." Check out the link below for more info on Monolaurin! 

Monolaurin: Quite the Superhero

ALLICIN (Garlic)

allicin in garlic

Like monolaurin, garlic's antibacterial powers are potent and broad, attacking a vast range of bacteria, and fungi (including Candida), while also potentially sparing the good bacteria in our bodies. One study even found garlic completely eradicate giardia infection in patients within 3 days. Garlic may wield its power by attacking invader membranes and reducing their oxygen, growth, and fat/protein/acid synthesis.

Garlic's key antibacterial weapon may be allicin, a compound which forms from alliin in freshly crushed garlic. It actually forms as a defense mechanism in "injured" garlic, and is highly antibacterial in nature, like a natural pesticide.  Even though garlic is listed as "high FODMAPs" on the low FODMAP diet prescribed to minimize bacterial fermentation in the gut, garlic (and particularly allicin) seems to be one of the main antibacterials for SIBO with which many people find success.

Aged garlic is also gaining popularity. While some studies have shown no anti-fungal activity, others reveal antimicrobial power. Though aged garlic contains less of the volatile allicin, it features higher amounts of other beneficial and antioxidant compounds, such as allicin, S-allylcysteine, sallylmercaptocysteine and selenium.

Garlic does have a sinister side of course: the dreaded garlic smell. The stench can linger in an individual for days, since compounds in garlic are difficult for the body to breakdown. The garlic smell is notorious for being undetectable by the offender, meaning you may wreak of garlic and not realize it. Alas! Although I love the taste and medicinal benefits of garlic, I don't love how it makes me smell. As such, I try to moderate my intake and, and also use the supplement form of allicin, my favorite being AllicinPlus-C.

CASCARA SAGRADA 

natural herbal laxative

I hesitate to ever seemingly encourage laxatives, as the goal here is to yield a self-sustaining, functioning digestive state not requiring external influences for proper peristalsis. That said, some herbal components can really help get things flowing, especially when you're in a bind (no pun intended). Perhaps more importantly, some may even boast additional health benefits. Ultimately, I believe it's better to tonify and support healthy elimination via natural means, rather than turning to chemical laxative concoctions, which I personally won't touch.

For starters, two vital compounds for health just so happen to promote bowel movements as well: namely, magnesium and vitamin C. I can  wholeheartedly recommend these, regardless of your digestive state.  But when you're looking for something a little more specific, you may consider Cascara Sagrada. 

Cascara comes from a type of buckthorn bark, and contains chemicals with natural laxative properties, such as hydroxyanthracene glycosides and the anthraquinone emodin. While overuse of cascara can lead to loose stools, finding the right amount may support healthy waste and toxin elimination, in a sort of adaptogen-esque nature. Proper fluid balance is also key, and cascara may support intestinal movement while maintaining the proper amount of fluid in the intestines.

Studies also suggest the emodin (found in cascara) may actually bear anti-viral, anti-cancer and anti-carcinogen properties. Emodin is also anti-inflammatory and protective against oxidative stress. So smart supplementation with cascara may not only address kinks in elimination, but provide other benefits as well. 

It is pertinent to only consume aged cascara, which breaks down potentially harmful compounds in the fresh plant. I personally like the Nature's Sunshine brand.

LOW DOSE NALTREXONE (LDN)

LDN

Many (if not most) pharmaceutical drugs mask symptoms while perpetuating the root problem, much to the joy of the financial industry creating the pills in the first place. After all, if NSAIDs (nonsteroidal anti-inflammatory drug like Advil, Aleve, Motrin, etc.) actually cured headaches, they'd render themselves obsolete, since you wouldn't need to buy them again. If statins actually cured the cholesterol problem, you wouldn't need more statins. Not to sound conspiratorial, but a perpetual cycle of sustained disease masquerading as health management is the ideal situation for pharmaceutical companies. The sicker you are, the richer they are!

That said, Low Dose Naltrexone (LDN) may be one of the few "drugs" which I can actually wholeheartedly stand behind.

Naltrexone is an opioid antagonist. It was initially developed for those struggling with substance abuse, since doses of 50.0–100.0 mg block opioid receptors in the hypothalamus and nullify the pleasurable effects of addictive substances. It was later discovered that low doses of around .5-4.5 mg (aka: "LDN") very temporarily blocked endorphin receptors. When the body then does its "endorphin" check following LDN administration, it senses a deficit in endorphins, and begins generating more endorphins in response.

Endorphins help relieve pain and fear in the body, and boost the immune system. Prescription pain medications often temporarily alleviate pain by interfering with or mimicking the body's own opiate signaling. This yields the lamentable effect of encouraging the body to build a tolerance, and stop producing its own pain relieving neurotransmitters (oh hey pain pill addiction!). LDN, however, does the opposite: it "convinces" the body to make more of its own natural painkillers.

With conventional pain pills, it's like always being given food, and finding yourself unable to eat if food isnt handed to you. With LDN, it's like being told there's no food in the first place, forcing you to go out and find it. The former makes you weak and helpless, the later makes your strong and resourceful. 

Studies have shown LDN benefits fibromyalgia (a chronic pain illness) better than placebo, and may help other inflammatory conditions such as arthritis or lupus. LDN even holds potential for cancer, since those afflicted  tend to feature extremely low endorphin levels. (In fact, studies suggest that people are most likely to develop cancer after the death of a spouse - which leads to period of low endorphin levels.) By supporting endorphin production, LDN has been shown to benefit AIDS patients, and dramatically reduce cancer or promotes remission in mice. Endorphins can even directly instigate apoptosis, or cell death, directly on cancer cells in a Petri dish, possibly by activating opiate receptors in the cancer cells themselves. And lastly (and most pertinent to this article), LDN may benefit chronic infections by supporting the immune system. I'm looking at you SIBO!

Beyond opioid receptors, LDN may exhibit pain-relieving, anti-inflammatory, and healing effects by other means. LDN may influence microglial cells, which are part of the central nervous system and immune system and instigate inflammatory things like cytokines, reactive oxygen species, nitric oxide, and excretory amino acids. Microglial cells can be triggered via a number of mechanisms, and can yield unpleasant conditions to the bearer, from pain to exhaustion to mood problems to even toxicity.

Unlike pharmaceuticals, LDN has extremely low side effects, the worst of which seem to be temporary insomnia and/or vivid dreams. LDN is also not euphoric within itself, nor addictive.

Returning to our current subject: LDN may be particularly healing for the digestive tract. In addition to improving inflammation by modulating opiate receptors, a 2016 study found LDN directly stimulated healing of intestinal cells in vitro (AKA: directly in the Petri dish, with no mediating body involved.) And Chron's disease, a condition of inflammation in the digestive tract, has been most scientifically studied and supported for LDN benefits. LDN also functions a prokinetic, stimulating motility of the small intestine, which is vital for proper digestion and clearance of bacterial buildup and toxins. Basically, when you're seeking healing mode, LDN has totally got your back. By the way, did you know the cells of the small intestine replace themselves every 2-4 days? (The cells of your skin's epidermis, by comparison, can take 10-30 days!) This means rapid healing of your GI tract is totally possible, and LDN may be just the catalysis you need really run with it!

As for the proper LDN dosage, that calls for trial and error and your own personal constitution. You're looking for the dose which creates minimal time blocked of endorphins, with maximum resulting endorphin generation by the body. Depending on how your body reacts, that could be anywhere from .5mg - 4.5 mg. I recommend starting low, and titrating up till you find your happy place. The common protocol calls for taking LDN in the evening, around 9pm or so. This is because the body naturally produces around 90% of its endorphins between 2 and 4 am. Taking LDN at night allows for endorphin blockage and clearance by this prime endorphin-producing time. In fact, studies show correct administration may increase endorphin production by an estimated 300% in the wee hours of the morning. And since the half-life of beta endorphin is around 20 hours, that means you still get the endorphin effects all throughout the next day! That said, some people struggle with adopting to a night dose due to sleep problems, and do better with a morning dose. In any case, most people ultimately report enhanced sleep on LDN, once the dosage kinks are worked out. I personally started with an evening dose, shifted to a morning dose, but now am back to an evening dose. 

I personally love my daily LDN, which helps me massively with inflammation and healing.​ I plan to continue taking it indefinitely. At present, LDN has not been grabbed up by any major pharmaceutical companies, which has positives and negatives. On the one hand, if a company began producing a mainstream version of LDN, it would make the wonder drug far more accessible (finding a doctor to prescribe LDN can be tricky), and also affordable to those with insurance plans covering it. That said, the mainstream version of LDN would potentially include unnecessary and possibly inflammatory fillers. It could also make LDN, if more regulated, not  as accessible, and actually more expensive for those without insurance plans covering it. For now,  you can get get LDN with a doctors prescription through compounding pharmacies, for around $30-90 a month. 

For more information on LDN, I recommend the GOT ENDORPHINS? LDN (Low Dose Naltrexone) Facebook group.

HONORABLE MENTIONS

In addition to Monolaurin, Allicin, Cascara, and LDN, I tend to tinker with a few other supplements, based on my current state. For starters, I usually take a soil based probiotic, such as Prescript Assist or Megaspore (available at https://rebelhealthtribe.com/), and eat small amounts of fermented food, like raw unpasteurized sauerkraut. (My all time favorite is Rejuvenate Foods, available at some Whole Foods if you're lucky!) I was actually going to include probiotics in this post, but realized the topic warranted a MUCH longer (forthcoming) discussion. (You can sign up for email updates if you want to know when I post about that!) With dinner, I take adequate HCL with Pepsin to promote stomach acid vital for digestion (something I've done consistently for years and haven't stopped). I've also started  using Ox Bile, to support fat digestion and discourage bacterial overgrowth.  I throw in the occasional Oil of Oregano.  More recent experimentation has featured L'Ornithine, a nonessential amino acid which may help reduce ammonia generated as byproducts of protein metabolism, or even from intestinal yeast or bacterial overgrowths. I'm still vastly familiarizing myself with amino acids concept, so I shall report back on that one. Proteolytic enzymes such as serrapeptase (made by the Japanese silkworm) as well as proteolytic enzyme blends have proven wondrous for inflammation, though I've laid off them as of late. On occasion I stick some reduced glutathione under my tongue, and I've recently brought back some Vitamin C  powder, which I honestly forgot about until I recently listened to a Bulletproof Podcast episode on the subject. One go-to supplement I used for years, but which is now completely absent, is caffeine, either in pure form or from green tea extract. Again, I think I'll save that discussion for a future post. 

THE TAKEAWAY

I realize listing all these supplements can make it seem like there's a lot going on, but in reality, I'm growing increasingly more aware of what supplementation helps my body, what supplementation potentially hurts it, and what supplementation equates to snake oil. On a long term basis, I truly only see myself taking LDN, as well as natural desiccated thyroid (for as long as I need it.) In any case, I encourage you to embrace supplementation with awareness, out of a desire to supercharge your being, rather than out of fear. Never, never out of fear. The placebo affect alone is worth its weight in gold, so when you do supplement, look for the best, and may you continue to grow in your wonderful journey!

How about you? What supplements have you found support health and restoration?​

REFERENCES

Inactivation of visna virus and other enveloped viruses by free fatty acids and monoglycerides: https://www.ncbi.nlm.nih.gov/pubmed/8030974
Glycerol monolaurate prevents mucosal SIV transmission: https://www.ncbi.nlm.nih.gov/pubmed/19262509
Glycerol Monolaurate Antibacterial Activity in Broth and Biofilm Cultures http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0040350
In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4924139/
http://www.gidoctor.net/client_files/file/Naltrexone-Side-Effects-and-Efficacy-in-GI-
Garlic: a review of potential therapeutic effects: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4103721/
Garlic Revisited: Antimicrobial Activity of Allicin-Containing Garlic Extracts against Burkholderia cepacia Complex: http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0112726
Cascara, energy, cancer and the FDA's laxative abuse: http://raypeat.com/articles/articles/cascara-energy-cancer-fda-laxative-abuse.shtml
Emodin induces apoptosis in human promyeloleukemic HL-60 cells accompanied by activation of caspase 3 cascade but independent of reactive oxygen species production https://www.ncbi.nlm.nih.gov/pubmed/12445860
Celecoxib acts in a cyclooxygenase-2-independent manner and in synergy with emodin to suppress rat cholangiocarcinoma growth in vitro through a mechanism involving enhanced Akt inactivation and increased activation of caspases-9 and -3 https://www.ncbi.nlm.nih.gov/pubmed/12657721
Apoptosis of human hepatoma HepG2 cells induced by emodin in vitro: https://www.ncbi.nlm.nih.gov/pubmed/14693052
Inactivation of enveloped viruses by anthraquinones extracted from plants: https://www.ncbi.nlm.nih.gov/pubmed/1810179
Cascara sagrada (Rhombus purshiana): http://www.sigmaaldrich.com/life-science/nutrition-research/learning-center/plant-profiler/rhamnus-purshiana.html
The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3962576/
Low-dose naltrexone therapy improves active Crohn's disease: https://www.ncbi.nlm.nih.gov/pubmed/17222320
Therapy with the Opioid Antagonist Naltrexone Promotes Mucosal Healing in Active Crohn’s Disease: A Randomized Placebo-Controlled Trial https://www.ncbi.nlm.nih.gov/pubmed/21380937
P096 Low-dose naltrexone reduces in-vitro endoplasmic reticulum stress and stimulates wound healing in intestinal epithelial cells https://www.ecco-ibd.eu/index.php/publications/congress-abstract-s/abstracts-2016/item/p096-low-dose-naltrexone-reduces-in-vitro-endoplasmic-reticulum-stress-and-stimulates-wound-healing-in-intestinal-epithelialx00a0cells.html
low-dose naltrexone for normalizing immune system function: http://todayspractitioner.com/wp-content/uploads/2013/10/Bernard-Bihari-MD-Low-dose-Naltrexone-for-Normalizing-Immune-System-Function-athm_19_2_bihari_56_65.pdf
Garlic Revisited: Antimicrobial Activity of Allicin-Containing Garlic Extracts against Burkholderia cepacia Complex http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0112726
http://book.bionumbers.org/how-quickly-do-different-cells-in-the-body-replace-themselves/​
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