Life Extension Magazine®
It may surprise you that of the ten leading causes of death in this country—including heart disease, cancer, and diabetes—seven are linked to a single enzyme in your body.1 It's called 5-lipoxygenase or 5-LOX and in excess can create a cascade of dangerous inflammatory conditions throughout your body. Ironically, the same systemic inflammation triggered by 5-LOX once defended early humans against exposure to infectious disease. With these diseases now largely eradicated, the pro-inflammatory action of 5-LOX is not only unnecessary, but lethal to aging humans.2-5 Long known to researchers for its role in arthritis, pharmaceutical companies are trying to develop safe drugs to defuse 5-LOX, but the few "5-LOX inhibitors" currently available are proving no safer than other anti-inflammatory drugs.6,7 The good news is that a superior form of a natural 5-LOX inhibitor has recently been developed. This highly purified extract of boswellia has been shown to effectively inhibit excess 5-LOX at the molecular level. This article describes recent data on the anti-inflammatory mechanisms of boswellia extract and its multimodal protective effects against age-related problems such as cancer, heart disease, and neurodegenerative disorders. Readers will be encouraged to discover a new extract that absorbs into the blood 52% better than previously available boswellia. Excess 5-LOX Cripples and Kills Millions of AmericansIn response to poor dietary choices, our bodies suffer an overload of arachidonic acid. To remove arachidonic acid, the body increases production of enzymes like 5-lipoxygenase (5-LOX). Elevated 5-LOX and end products formed from degradation of arachidonic acid result in a constellation of age-related disorders. The graphic below (Figure 1) is re-printed from the February 2007 issue of Life Extension Magazine®. It clearly shows common foods in the Western diet that cause excess arachidonic acid to accumulate and the deadly cascade caused by elevated 5-LOX. 5-LOX stimulates the manufacture in the body of pro-inflammatory molecules called leukotrienes.8 Hundreds of published studies connect leukotrienes to cardiovascular disease,9 cancer,10-16 arthritis,17-19 and breathing disorders such as asthma and chronic obstructive pulmonary disease (COPD).8 They have also been implicated in Alzheimer's,20-25 inflammatory bowel diseases,26-28 and osteoporosis.29,30 Following healthier dietary patterns reduces 5-LOX levels, yet typical foods consumed by Americans today make it challenging to optimally suppress 5-LOX and its deadly metabolites. Fortunately, an Indian plant extract has demonstrated profound inhibiting effects against the 5-lipoxygenase (5-LOX) enzyme. Clinical Validation for a Traditional TreatmentFor millennia, traditional cultures prized the fragrant leaves of the boswellia tree both as aromatics and medicinals capable of reducing fever, rheumatism, and gastrointestinal disorders.
Modern researchers first validated boswellia's medical relevance with the discovery of boswellic acids. One in particular, AKBA (3-acetyl-11-keto-betaboswellic acid), was shown to bind directly to the 5-LOX enzyme in our bodies, preventing it from facilitating production of pro-inflammatory leukotrienes.39,40 Subsequent animal experiments confirmed that boswellia extracts exert a powerful anti-inflammatory effect, particularly in alleviating joint swelling in arthritis.41 Early trials in humans yielded similarly compelling results that paralleled traditional uses. Boswellia extracts proved to be an effective treatment in patients suffering from rheumatoid arthritis, Crohn's disease, ulcerative colitis, and asthma.39,42 Detailed safety and toxicological testing of boswellia extracts demonstrated their broad safety spectrum with both internal and external use.43 A Superior Form of BoswelliaThe limitation in using boswellia extracts as 5-LOX inhibitors is that they are difficult to absorb into the bloodstream (scientists call this "bioavailability").44 Recently, a novel boswellia extract was developed in which the plant's bioactive components were suspended in non-volatile oil also derived from boswellia. Researchers found this extract to be 52% more bioavailable compared to standard boswellia extracts.44 It offered superior protection from damage to joint cartilage induced by pro-inflammatory molecules and provided 15% better inhibition of certain pro-inflammatory molecules, including TNF-alpha and MMP3, compared with standard boswellia extracts.44 Clinical studies of patients with osteoarthritis are already confirming the important improvements in effectiveness offered by the new formulation.45 This makes sense based on a wealth of data showing life-enhancing benefits that boswellia extracts can afford through their blockade of dangerous 5-LOX and other mediators of inflammation. Cardiovascular ProtectionFor more than 20 years, we have known of the major role played by inflammation in the development of atherosclerosis, which is the occlusion and hardening of the arteries. In 1991, it was discovered that end products of 5-LOX were involved in the formation of atherosclerosis.52,53
Within a decade, the hunt was on for 5-LOX inhibitors that could prevent or even reverse cardiovascular aging.54 Boswellia extracts emerged as the most prominent natural sources of 5-LOX-inhibiting, anti-atherosclerotic compounds.55 In vascular tissue, boswellia extracts exert multiple complementary effects. They possess powerful free radical–quenching effects.56 Boswellia extracts lower total cholesterol by up to 48% and boost artery-cleansing high-density lipoprotein (HDL) by as much as 30%.57 It is boswellia extracts' inhibition of 5-LOX and other inflammatory factors, however, which is generating intense interest among heart specialists. In human capillary lining (endothelial) cells, the extracts significantly prevented expression of specific molecules central to forming atherosclerotic lesions.43,58 Boswellia exerted this effect by favorably modulating 113 genes, all of which were involved in producing blood vessel inflammation.58,59 Extracts rich in AKBA, a key bioactive agent in boswellia, caused a 50% reduction in the size of atherosclerotic lesions.60 They also significantly reduced activity of several different coagulation (clotting) factors in the blood.56 Neuroprotection and Brain HealthConstituents of a resin from a boswellia species have been shown to be potent stimulators of a brain receptor system called TRPV3 that lowers anxiety and exerts antidepressant-like effects.61 A major component of Boswellia carterri (called Incensole acetate) inhibits inflammatory mediators in brain tissue, an effect that offers significant hope in treatment of brain injury.62 That's because a dangerous inflammatory response follows brain injury within hours, contributing to a substantial portion of the long-lasting neurological deficit. Incensole acetate specifically inhibits degeneration of brain cells in the hippocampus, the region responsible for memory processing.62 Animal models confirm this effect. Laboratory rats treated with a drug to impair memory, along with boswellia extract, performed significantly better on tests involving spatial orientation and learning than did animals treated with the drug alone.63 A similar result was shown in healthy animals not treated with a memory-destroying drug. Extracts of Boswellia papyrifera—one of five species of boswellia used in the making of frankincense—increase spatial memory retention, enabling the animals to quickly find their way out of a maze.64 |
ChemopreventionAKBA, a principal component of boswellia, acts by numerous mechanisms to prevent cancer cells from proliferating. It induces apoptosis, or programmed cell death, by switching on the aptly named "death receptor" on cancer cell surfaces, an effect accompanied by activation of so-called "suicide" pathways inside cancer cells.65 Boswellic acid also blocks important signaling molecules required for cancer cell replication.66 And AKBA further inhibits tumor growth by suppressing a growth factor, VEGF (vascular endothelial growth factor), required by cancers to grow necessary new blood vessels.67 Boswellia oil extracts can distinguish between healthy and cancerous tissue, suppressing tumor cell viability but sparing normal cells.68 Finally, AKBA has recently been shown to suppress activity of a cellular receptor, CXCR4, that cancer cells use to trigger the metastases that account for 90% of cancer deaths. To date, boswellia extracts have also shown promise in reducing malignant cell growth, replication, or metastases in cancers of the prostate, bladder, cervix, colon, as well as in multiple myeloma, a cancer of the bone marrow. 66-73
Boswellia Extracts Relieve Arthritis SufferingEarly studies involved combinations of boswellia extracts with other known natural anti-inflammatory agents such as Withania somnifera (ashwagandha), Curcuma longa (curcumin), and zinc. In one such study, 42 patients were randomly assigned to receive this combination of nutrients or a placebo for 3 months.85 The treated group, but not the placebo recipients, demonstrated a significant drop in pain severity and disability scores. A similar study included the widely used WOMAC score of physical function difficulty and demonstrated significant reductions in that parameter as well as in pain and disability.86 No significant side effects were noted in either study.
More recently, studies have been conducted using boswellia extracts alone in double-blind, placebo-controlled trials, with doses up to 3,600 mg per day. Again, significant reductions are routinely reported in all parameters, including joint pain and swelling, ability to flex the joint, and increased walking distances.87 A 2008 study using a purified extract containing 30% of the vital AKBA was conducted among 70 patients with osteoarthritis.88 Subjects received the extract at doses of either 100 or 250 mg per day, or a placebo, for 90 days. Both doses of the extract, but not the placebo, resulted in clinically and statistically significant improvements in pain scores and physical function.88 Several other features of this study are worthy of notice. First, samples of joint fluid revealed a significant reduction in MMP-3 (matrix metalloproteinase-3), the inflammatory enzyme responsible for much of the cartilage destruction seen in osteoarthritis. Secondly, improvements in pain and functional ability were evident as early as 7 days into the 90-day treatment program. A follow-up study was conducted in 2010 to evaluate the efficacy of both the standard 30% AKBA extract and the newer, more bioavailable extract.45 Patients received just 100 mg of either supplement, or placebo, again for 90 days. In this case, both supplements produced significant improvements in pain scores and function and a reduction in MMP-3 levels. In both groups, improvements were evident in only 7 days, although the highly bioavailable preparation was more effective in providing a meaningful level of joint protection.
SummaryThe enzyme 5-lipoxygenase or 5-LOX triggers seven of the top ten leading causes of death in the United States, including cancer and heart disease. Excess 5-LOX leads to deadly release of pro-inflammatory molecules, including leukotrienes. While few safe drugs exist to neutralize 5-LOX, an exciting natural 5-LOX inhibitor with greater absorbability was recently developed. An abundance of compelling data indicates that the bioactive compounds in boswellia block the inflammatory response induced by 5-LOX that accelerates the onset of multiple killer diseases of aging. This new form of boswellia has been shown to absorb 52% better into the bloodstream, thus providing more of this natural 5-lipoxygenase inhibitor to cells throughout the body. If you have any questions on the scientific content of this article, please call a Life Extension® Health Advisor at 1-866-864-3027.
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