COX-2 is an enzyme that spreads inflammation throughout the body. It contributes to the production of inflammatory prostaglandins that are believed to be responsible for a myriad of aging diseases including arthritis, cardiovascular diseases, and neurodegenerative conditions such as dementia and Alzheimer’s Disease. It and other inflammatory compounds have also been implicated in the development and spread of many types of cancers.
In 1999, a supplement called Nexrutine was introduced that functions as a COX-2 inhibitor without many of the drawbacks of the various COX-2 inhibitor drugs that have been available for some time. Before further discussing Nexrutine, I’ll outline the problems with both traditional COX-2 inhibitors such as aspirin and also the widely prescribed selective COX-2 inhibitor medicines that have come to market in the last decade.
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Aspirin Fights Inflammation and Pain
One of the common recommendations for aging people is to take one 81mg “baby aspirin” tablet each day. That’s in part because aspirin is a COX-2 inhibitor that helps fight inflammation in the body. It is also reputed to help reduce the risk of heart attacks by reducing the potential for clots.
Aspirin, ibuprofen, and related NSAIDs (nonsteroidal anti-inflammatory drugs) also inhibit COX-1, an enzyme that helps protect the digestive system from damage and prevents out of control bleeding by producing thromboxane which can repair damage to leaky blood vessels by clotting action. This is part of the reason why these drugs are often implicated in gastrointestinal ulcers and stomach bleeding.
White willow bark extract contains salicin which is related to the salicylic acid that is the active ingredient in aspirin. However, many sources state that white willow bark inhibits COX-2 without inhibiting COX-1 as much as aspirin does.
If you want to use a supplement similar to aspirin for inflammation and pain relief with less risk of stomach ulcers and uncontrolled bleeding, look into using white willow bark as an alternative. But if you’re after the blood thinning effect, then aspirin may be superior to white willow bark.
Big Pharma Selective COX-2 Inhibitors Exposed As Dangerous
Pharmaceutical companies developed selective COX-2 inhibitors such as Celebrex and they have become some of the most widely prescribed drugs in the world. Some of these drugs also inhibited COX-1, but to a lesser degree than older NSAIDs. Therefore they should have a lower risk of producing stomach ulcers and uncontrolled bleeding.
Yet some of these drugs turned out to be dangerous and were withdrawn from the market. For example, in 2004 Merck’s Vioxx (generic rofecoxib) was found to increase the risk of heart attacks and strokes when used in large doses for long terms and was therefore removed from the market. Pfizer’s Celebrex (generic celecoxib), while it is still available, was revealed in 2009 to be backed by 21 fraudulent drug studies involving the discredited scientist Dr. Scott S. Reuben. Reuben was also involved in the drug approval process for Vioxx.
Nexrutine, a Natural Selective COX-2 Inhibitor
Researchers identified COX-2 inhibiting properties in a traditional Chinese herbal extract named huang bai from the Chinese phellodendron amurense tree. Unlike aspirin and most NSAIDs, it functions as a COX-2 inhibitor without blocking COX-1. In the US, this extract is sold as a brand name supplement called Nexrutine. Unlike COX-2 inhibitor drugs that target the COX-2 enzyme after it has been produced, Nexrutine suppresses the activity of the gene responsible for COX-2 production. The claims are that it does this without affecting protective COX-1 and acts more rapidly than other COX-2 inhibitors as they do not shut down much of the body’s COX-2 production as Nexrutine does.
Nexrutine® is a novel plant extract derived from the bark of the phellodendron tree of Asia. Nexrutine®’s action resembles that of the newest class of inflammation-fighting drugs, the COX-2 inhibitors, such as Celebrex®, Vioxx® and Bextra®. These blockbuster prescription drugs have been extensively researched in human trials and are proven effective at reducing inflammation by interfering with the activity of COX-2 (cyclooxygenase-2).
COX-2 is a villain. It is an intermediary enzyme: a link in a cascading chain of compounds which eventually trigger release of prostaglandins, resulting in inflammation. In Alzheimer’s disease this inflammatory damage spreads to neighboring cells in the brain. As they become inflamed they release stress chemicals in turn, which trigger more inflammation, setting into motion an accelerating spiral of decline.
Although scientists do not unanimously agree that halting inflammation may prevent the onset of Alzheimer’s and vascular dementia, many researchers continue to investigate the possibility. In one study on the effects of COX-2-inhibitor therapy, researchers concluded: “Our findings further support the importance of these disease-modifying drugs in the prevention and treatment of Alzheimer’s disease.”11 Other studies have also linked inflammatory processes with other neurodegenerative diseases, such as Lou Gehrig’s and Parkinson’s diseases.12,13
The COX-2 inhibitors are easier on the stomach than commonly available over-the-counter NSAID medications, such as aspirin and ibuprofen, which can cause gastric bleeding when taken in high doses. NSAIDs block both COX-2 and its more benevolent cousin, COX-1, which is necessary for stomach lining protection. Thus, compounds that block COX-2 selectively are at least as effective as NSAIDs at relieving inflammation, but are supposedly better tolerated by the body. While the makers of COX-2 inhibiting drugs claim they are safe for the stomach, reports published after the drugs were approved show that they can cause gastric side effects in certain individuals. One reason is that so-called COX-2 inhibitor drugs also suppress some COX-1.
Unlike expensive prescription COX-2 inhibitors, plant-derived Nexrutine® inhibits the gene expression of COX-2 rather than directly inhibiting the enzyme, in effect cutting the problem off at the source, rather than intervening once COX-2 is released. This difference in mechanism of action also explains the rapid onset of Nexrutine®’s anti-inflammatory action. Seventy-nine percent of subjects who used Nexrutine® for two weeks agreed that Nexrutine® helped relieve or avoid the general aches and pains associated with overexertion and physical activity, and there was no evidence of side effects at recommended dosages.14
Nexrutine and Cancer
Inflammation is one of the driving forces in many cancers. COX-2, TNF-a (Tumor Necrosis Factor alpha), and NF-kB (Nuclear Factor kappa B) are three of the inflammatory compounds found to enable the growth of certain types of cancers. Researchers have found that Nexrutine is able to suppress the effects of COX-2, TNF-a, and NF-kB on inflammation that drives the growth of prostate cancer tumors.
Epidemiological and laboratory studies support the hypothesis that several plant components influence prostate carcinogenesis and holds promise for disease prevention. Previously we reported that Nexrutine® (bark extract from Phellodendron amurense) inhibits proliferation of prostate cancer cells and prostate tumor development in the transgenic adenocarcinoma of mouse prostate (TRAMP) model through modulation of Akt signaling pathway. In the present investigation we conducted studies to further define the mechanism of action of Nexrutine® and to identify the active component associated with its biological activity.
Nexrutine for Muscle and Joint Pain and Arthritis
Next Pharmaceuticals funded a study of its ingredient Nexrutine for use in treating muscle and joint pain in 2004. The researchers found that 72% of the 53 study participants who used the supplement at three doses of 250mg per day for two weeks reported it was effective at reducing muscle and joint pain from physical activity. There were no significant reported side effects.
For arthritis sufferers, a Life Extension article from 2003 recommends the use of Nexrutine with nettle leaf extract. Note that nettle leaf extract is different from the nettle root extract usually used to suppress prostate inflammation. You can use a combination of both nettle leaf and nettle root extracts along with Nexrutine for even more inflammation protection.
Pharmaceutical companies proclaimed a new era in arthritis management with the advent of the COX-2 inhibitors such as Celebrex® and Vioxx®. Unfortunately, these drugs work against themselves by upsetting the system of checks and balances through which the body regulates inflammation. A brief review of arthritis and the biochemical pathways leading to inflammation will help us understand the fly in this ointment—and what we can do about it.
Several years ago, German researchers discovered that a traditional European herbal remedy for rheumatism, nettle leaf extract, inhibits TNF-alpha and IL-1 beta.
Nettle “may inhibit the inflammatory cascade in autoimmune diseases and rheumatoid arthritis,” concluded a team of researchers.
It is interesting to note that the prescription drug Enbrel®, approved for the treatment of rheumatoid arthritis, acts by suppressing TNF-alpha.
Nettle leaf extract thus makes the ideal complement to COX-2 inhibitors, by virtue of its ability to counteract their negative effects. The herbal COX-2 inhibitor Nexrutine® is derived from the bark of the phellodendron tree, which folk healers use to treat arthritis and other ailments. Prescription COX-2 inhibitors intervene in the inflammation cascade by blocking the action of the COX-2 enzyme. But Nexrutine® inhibits the gene expression of COX-2, preventing its manufacture in the first place. This difference in mechanism of action may account for the rapidity of Nexrutine®’s inflammation-quenching action. According to reports from subjects who used Nexrutine® for two weeks, 79% agreed that Nexrutine® helped relieve or avoid the general aches and pains associated with overexertion and physical activity. No side effects were reported at recommended dosages.
If you’re suffering from arthritis, you should click through to Natural Help for Arthritis Sufferers and read the full article. It explains why a mix of anti-inflammatory supplements that inhibit multiple types of inflammatory molecules is superior to just one supplement or drug and further covers another supplement called 5-LOXIN derived from the Indian Boswellia serrata plant that inhibits the 5-LOX inflammatory pathway.
Nexrutine for Anti-Aging Usage
Since inflammation is a major driving force behind so many of the diseases of aging, taking supplements or drugs that prevent inflammation from becoming a problem seems to be a good approach to preventing the development of age-related diseases. Nexrutine is relatively inexpensive and free from known significant side effects, unlike aspirin, ibuprofen, Celebrex, and other COX-2 inhibitors. If you are suffering from arthritis or simply want to take inexpensive measures to help lower your theoretical risk of inflammation-driven diseases, Nexrutine is worth a look.
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