The Forgotten Flavonoid
A British friend of mine, trained in homeopathy, suggested to me many years ago that the best treatment for varicose veins (and hemorrhoids) was the flavonoid rutin. This inexpensive supplement was at the time commonly available, though now it is seemingly forgotten, and seldom found.
Having been dealing with varicose veins for a good portion of my adult life, it was only recently I remembered his advice and started taking rutin regularly. In years past I have used many herbal treatments, including pycnogenol (which worked very well when I was a couple of decades younger), horse chestnut, diosin, and a general mix of citrus bioflavonoids.
Now, focusing on rutin to treat this condition, I must say that I have been impressed by the relatively rapid response I have seen. Rutin in no time at all has visibly reduced the expression of these damaged blood vessels, such that I will most likely stay on it for years to come. (Flavonoids such as rutin should be taken with vitamin C as they work together synergistically.)
Once deciding that rutin was my new best friend, I visited PubMed to see what other benefits it might provide. I was surprised to find that rutin has a lot of research done on it, and is well worth being part of any nutritional supplement regimen. Now, let’s have a look at some of those benefits. (Check out this older blog of mine for more on the subject of Varicose Veins.)
Flavonoids are a class of pigments, found in most plant-based foods, which have powerful antioxidant properties. The flavonoid rutin is found in high amounts in apricots, buckwheat, cherries, grapes, grapefruit, onions, oranges, plums, tea, and wine.
Rutin “consists of the flavonol quercetin and the disaccharide rutinose. Rutin has been reported to exert diverse biological effects such as antitumor and antimicrobial mainly associated with its antioxidant and anti-inflammatory activities”. (Source)
It is interesting that the flavonoid quercetin is a major component of rutin, and to discover that “the complexity of natural rutin has impeded the development of rutin derived drugs”. (Source)
Let’s begin by looking at the antioxidant, and anti-inflammatory, properties of rutin, as many of the ensuing benefits to health that it provides, can be traced to these basic biological functions.
One study examined the “protective efficacy of rutin over liver, kidney, and brain dysfunctions”. In their opening statement, the researchers stated that “rutin is better than well-known antithrombotic agents (drugs that reduce the formation of blood clots) Juniferdin, or Bacitracin”. Now, that alone is reason for anyone middle aged or older to be taking rutin, since blood clots can lead to heart attacks, stroke, and other medical conditions.
In this study, “rutin showed protective effects against...multi-organ dysfunctions due to its anti-inflammatory and antioxidant properties. Therefore, rutin may be developed and practiced as a food supplement to cope with acute organ dysfunctions caused by inflammatory and oxidative damage”. (Source)
Rutin has been established to have antihyperglycemic properties (lowers blood glucose levels), so it was examined for “its protective effects against the development of diabetic complications”.
“Mechanisms for the antihyperglycemic effect of rutin include a decrease of carbohydrates absorption from the small intestine, inhibition of tissue gluconeogenesis, an increase of tissue glucose uptake, stimulation of insulin secretion from beta cells, and protecting Langerhans islet against degeneration. Rutin also decreases the formation of sorbitol, reactive oxygen species, advanced glycation end-product precursors, and inflammatory cytokines.”
These effects are considered to be responsible for the protective effect of rutin against diabetes-induced kidney disease, nerve damage, liver damage, and cardiovascular disorders. “Taken together, the results of current experimental studies support the potential of rutin to prevent or treat pathologies associated with diabetes.” (Source)
From one scourge of modern living, diabetes, to another, namely cancer. This study opens with the matter-of-fact statement that “rutin is a safe anticancer agent with minor side effects'' compared to chemotherapy. Therefore, these researchers set out to discover the mechanisms of its anticancer effect. Unfortunately, those mechanisms will be inexplicable to many of us, as they are highly technical in nature, nonetheless I will reproduce them below for those readers with a greater understanding of biochemistry.
“Both in-vivo and in-vitro examinations on anticancer mechanisms of this natural agent have been widely carried out. Regulation of different cellular signaling pathways such as Wnt/β-catenin, p53-independent pathway, PI3K/Akt, JAK/STAT, MAPK, p53, apoptosis as well as NF-ĸB signaling pathways helps to mediate the anticancer impacts of this agent.” (Source)
Inflammatory Bowel Disease
Inflammatory bowel disease (IBD) is a form of chronic inflammatory disorders of the gastrointestinal system, most commonly represented by Crohn’s disease and ulcerative colitis. Some scientists, finding that quercetin, though a proven anti-inflammatory, failed to show benefit against IBD, decided to examine rutin. (As we saw at the beginning, quercetin is a component of rutin.)
They found that rutin was “proven to possess a significant IBD therapeutic potential in experimental animals”, possibly because the rutin had an “ability to serve as a prodrug that delivers the bioactive quercetin close to the IBD site”.
The researchers also discovered “potential mechanisms of action far beyond antioxidant effects such as suppression of proinflammatory mediators' release and expression of inflammatory proteins (e.g. adhesion molecules, cyclooxygenase, nitric oxide synthase, etc.)”. (Source)
Another study confirmed the idea that rutin worked by effectively getting quercetin to the site of inflammation.
“Our data suggest that rutin acted as a quercetin deliverer to the large intestine and its anti-inflammatory action in TNBS-induced colitis rats may be through quercetin-mediated inhibition of TNF-alpha-induced NFkappaB activation.” (Source)
Many neurodegenerative diseases (NDs) (including Alzheimer's disease, Parkinson's disease, and Huntington's disease), “share common mechanisms such as neuronal loss, apoptosis, mitochondrial dysfunction, oxidative stress, and inflammation”.
The therapeutic potential of rutin for treating NDs has been examined in many studies, and has been found to be helpful because it addresses many of those mechanisms shared by these diseases.
An overview of such studies determined that rutin had the following mechanisms of action: “reduction of proinflammatory cytokines, improved antioxidant enzyme activities, activation of the mitogen-activated protein kinase cascade, downregulation of mRNA expression of PD-linked and proapoptotic genes, upregulation of the ion transport and antiapoptotic genes, and restoration of the activities of mitochondrial complex enzymes. Taken together, these findings suggest that rutin may be a promising neuroprotective compound for the treatment of NDs”. (Source)
But wait, there’s more. “Due to the ability of rutin and/or its metabolites to cross the blood brain barrier, it has also been shown to modify the cognitive and various behavioral symptoms of neurodegenerative diseases.” (Source)
Crossing the blood brain barrier is no small deal, as very few substances are capable of it, and those that can, do much to prevent and reverse neurological disorders. (For more on the subject of the blood brain barrier, have a read of this blog of mine, as well as this one.)
Studies have shown that high exposure to fluoride (NaF) induces neurotoxicity, and calcification of the pineal gland. One study I discovered demonstrated that rutin reduces the effect of fluoride induced toxicity in the cerebrum and striatum of rats. (Source)
A study was “conducted to evaluate the potential ameliorative effects of rutin on mercury chloride (HgCl2)-induced hepatotoxicity (liver damage) in adult male rats. The data of the present study suggest that rutin effectively suppresses HgCl2-induced hepatotoxicity by ameliorating oxidative stress, inflammation and apoptosis (cell death)”.(Source)
As I discussed in more detail in Health Secrets for the 21st Century Volume Two, rutin has a proven benefit for protecting the body from radiation damage. It does this by scavenging free radicals, and both preventing and reversing DNA damage. (Source)
I opened with how rutin is traditionally used to treat vein issues, so I will put a couple of links in here, just to confirm the scientific validity of that premise.
“Rutin supplement is recommended for the treatment of various diseases such as varicose veins, internal bleeding, or hemorrhoids.” (Source)
“There is moderate quality evidence to suggest that rutosides appear to help relieve the symptoms of varicose veins in late pregnancy.” (Source)
These days, no overview of any nutritional substance would be complete without seeing if it had any potential benefit for treating COVID-19. And, wouldn’t you know, rutin does have some potential for that. No real surprise when we remember part of its make up include quercetin, which has already been determined to be of value in this fight. (More info on quercetin and COVID is covered in the second part of this newsletter.)
Also, remember how under antidiabetic effect, and neuroprotective agent, rutin “decreased inflammatory cytokines”? The “cytokine storm” is one of the symptoms of COVID-19 that leads to severe symptoms, and even death, so clearly rutin is of advantage here.
Furthermore, “to fight COVID-19, various traditional antiviral medicines have been prescribed in China to infected patients with mild to moderate symptoms and received unexpected success in controlling the disease”.
“Exploring the molecular mechanisms of how these herbal medicines interact with the SARS-CoV-2 virus that causes COVID-19” is very technical in nature, nonetheless I will include some of that clinical material here.
“It is well known that the main protease (Mpro) of SARS-CoV-2 plays an important role in maturation of many viral proteins such as the RNA-dependent RNA polymerase. Here, we explore the underlying molecular mechanisms of the computationally determined top candidate, namely, rutin which is a key component in many traditional antiviral medicines such as Lianhuaqinwen and Shuanghuanlian, for inhibiting the viral target-Mpro.”
“Using in silico methods (docking and molecular dynamics simulations), we revealed the dynamics and energetics of rutin when interacting with the Mpro of SARS-CoV-2, suggesting that the highly hydrophilic rutin molecule can be bound inside the Mpro's pocket (active site) and possibly inhibit its biological functions.”
So much benefit from such a simple, inexpensive supplement, and I only stopped here because I had no more time to devote to this newsletter. I could have found even more material had I continued winding my way through the links in Pubmed.
We do use some rutin in our vitamin C complex in the NutriPods products, though this amount would not be considered a therapeutic dose.
Those seeking a therapeutic dose of rutin should ingest from 500 to 1000 mg daily (in divided doses), along with some vitamin C. (I suggest a gram of vitamin C, three times daily as a minimum dose for health benefits.)