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The Most Important MEDICINE You'll Ever GROW.

COX-2 Inhibitors can ease pain and fight cancer--naturally.

We live in a painful world. An estimated 40 million people suffer from osteoarthritis (OA), and between 2 and 3 million more suffer from rheumatoid arthritis (RA). For decades the pain interventions of choice for these ailments--and a host of aches and pains--have been nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and Naproxen. Virtually every human being has taken one form or another of these medicines during in their lives. Moderate doses for short periods of time are effective and relatively benign, but long-term use of these medications can increase the risk of serious side effects, including kidney and liver damage and peptic ulcers. In fact, geriatrics on NSAIDs experience significantly more ulcers, gastrointestinal irritation (GI) and kidney failure than the overall population. Each year, as many as 9% of geriatric NSAID users require hospitalization due to serious GI toxicity, and RA patients who chronically use NSAIDs are believed to increase their risk of GI-related hospitalizations sixfold. An estimated 107,000 people every year are hospitalized due to problems resulting from the use of NSAIDs, and as many as 16,500 people died in 1999 from NSAID complications; approximately the same number of people died from AIDS-related complications last year.

In addition, more than 100,000 people die every year from unanticipated reactions to prescription pharmaceuticals. The General Accounting Office (GAO) reported in 1990 that more than half of the drugs newly approved by the FDA in one decade had "serious post-approval risks, including heart failure, birth defects, kidney failure, blindness and convulsions." That alone is reason enough think twice about the risks we may be taking when we introduce new medicines into our lives.

In 1971, Sir John Vane was the first to figure out exactly how aspirin relieves pain. Vane, who won the 1982 Nobel Prize in medicine for his ground-breaking work, discovered that aspirin decreases the production of the prostaglandins that are generated by the cyclooxygenase (COX) enzyme. Unfortunately, NSAIDs, some more than others, also inhibit the balance and protective features of the COX enzyme, which is essential for proper kidney function and for protecting the stomach. Scientists and pharmacists warn that if you were to inhibit all COX activity, which can happen with long-term use of NSAIDs, you may well run the risk of endangering some vital organs and systems.

The antidote to the serious side effect of long-term pain reliever use, however, may still be right under our noses. In their new book, Beyond Aspirin: Nature's Answer to Arthritis, Cancer & Alzheimer's Disease (Hohm Press, 2000), authors Thomas M. Newmark and Paul Schulick have become some of the first health experts to talk about the miracles of natural cyclooxygenase-2 inhibitors, better known as COX-2 inhibitors or COX-2-Is. Their book introduces readers to the concept that the COX-2-Is found in nature, in such medicinal herbs as ginger and turmeric, can spare a great deal of pain and many fatalities. They also found that the new pharmaceutical COX-2 Is--namely Celebrex and Vioxx--may work even more dramatically.


Consider arthritis, which is not necessarily an age-associated malady. (RA is frequent in youngsters, too.) As joints and their connective tissues degenerate, joints, cartilage and bone become tender and painful. The inflammation itself can stimulate bone deterioration, and impede bone and cartilage repair.

Joint tissues generally exist in a state of homeostatic (working) equilibrium, somewhere between tissue degradation and repair, until byproducts of an overstimulated COX-2 enzyme create a bigger inflammation that upsets the balance. Due to accumulated wear and tear, the body's ability to keep this inflammation in check diminishes with age, and we are less able to regenerate tissue and tame the fires of inflammation that "burn" the old tissue.

More than 70% of older adults suffer some osteoarthritis of the knee. In the osteoarthritic joint, inflammatory chemicals, which are byproducts of COX-2, are overproduced and overstimulate cartilage destruction. I personally take chondroitin and glucosamine to repair and replenish the cartilage, along with herbal COX-2-Is to contain the inflammation and pain.


Medical science was not even aware of COX-2 until the early 1990s, when scientists, led by Dr. Philip Needleman, discovered that more than one COX enzyme existed. They found that both enzymes could metabolize, or burn, a particular fat in the body. COX-1 maintains a housekeeping balance in the kidneys and stomach, while COX-2 creates pro-inflammatory chemicals from arachidonic acid.

Indeed, the right amount of COX-2 in the body may be critical to the homeostatic regulation of salt, water and body temperature, as well as in nerve transmission. This particular enzyme is induced in the ovaries and uterus during ovulation and implantation. One alarming study on mice showed that those subjects that had their COX-2 totally disabled experienced more stillbirths due to improper kidney function.

Science has also shown, however, that as COX-2 activity increases, the incidence of cancer increases as well. Inversely, as COX-2 is inhibited, colon and other cancers seem to diminish. Derivatives of arachidonic acid, which humans rely upon to synthesize prostaglandins, may be a major "high-octane fuel" for the growth of cancer cells. If prostate cancer cells are deprived of their fuel, they begin apoptosis within one to two hours--a mass-programmed suicide.

COX-2 is 60 times more prevalent in a cancerous pancreas than in a noncancerous one. Of 76 patients with colorectal cancer, all showed indications of the COX-2 enzyme, while tissue from noncancer patients reflected no presence of COX-2. There is a strong negative correlation between COX-2 expression and five-year survival rates from cancer. COX-2 may be present in as many as 90% of patients with primary rectal adenocarcinomas. Arthritis, too, is born of COX-2 inflammation, and inhibiting COX-2 seems to offer some arthritis relief. So, now that we've identified COX-2 as potentially harmful in a number of ways, how can we control it in the bloodstream?


With the discovery of the COX-2 enzyme in 1991, scientists scurried about seeking a "magic bullet" that would disrupt the inflammatory COX-2 pathway without overinhibiting the protective housekeeping features of COX-1. Researchers at the pharmaceutical firm Monsanto located the highly specific COX-2 inhibitor known as celecoxib, or Celebrex, which has 375 to 400 times more affinity for COX-2 than for COX-1. In theory, Celebrex blocks the creation of inflammatory hormones hundreds of times more powerfully than it disrupts processes in the kidney and stomach. Merck, another pharmaceutical company, synthesized Vioxx, which has a thousand-fold greater preference for inhibiting COX-2. In tests for postoperative pain, Celebrex was just as effective at relieving pain as conventional narcotics. It was also found to be as good as Naproxen, a popular NSAID, at relieving osteoarthritic hip pain. Vioxx was shown to relieve pain associated with menstrual cramps, and the FDA has now approved it for use against menstrual pain.

In December 1998, the FDA approved Celebrex, calling it the first so-called miracle or safe aspirin, for OA and RA. Tens of millions of people will soon have taken Celebrex, Vioxx or related compounds for pain relief instead of NSAIDs like Aleve and aspirin. Anyone who has ever taken an aspirin or other traditional NSAID is a prime candidate for the COX-2-Is pain relief revolution. But the cancer-fighting promise of these medicines may be more revolutionary still.

In August 1999, the FDA accelerated its "fast-track" review of Celebrex to prevent a rare type of colon cancer. My father and two of his brothers died of colon cancer, so my brothers and I get tested on a regular basis. I'm also watching this aspect of the COX-2 inhibitor story very closely. Monsanto recently announced its collaboration with the National Cancer Institute (NCI) to test Celebrex for effectiveness against colon cancer. In October 1999, researchers at M.D. Anderson reported that Celebrex reduced both the number and the size of colorectal polyps in patients with familial adenomatous polyposis (FAP), a precursor to colon cancer (I suspect that's what we Duke boys have, although my HMO has never called it that).

It's quite clear that the pharmaceutical companies are playing for much bigger stakes than "miracle" aspirin. The Wall Street Journal predicts that by 2003, COX-2-Is may prove successful in preventing colon cancer in high-risk patients. Science is also showing that COX-2-Is can prevent or even reverse several types of life-threatening cancers. So far, 50 studies show that COX-2-Is can prevent premalignant and malignant tumors in animals, and it's possible they can prevent bladder, esophageal and skin cancers as well. COX-2 inhibition could prove to be one of the most important preventive medical accomplishments of the new century.

Sound great? Not so fast. Since synthetic COX-2-Is are new, we do not yet understand all their properties. We don't have enough experience with pharmaceutical COX-2-Is to know if they will have unintended and undesirable side effects; the jury is still out on the side effects associated with their long-term use. Hence, I share Newmark and Schulick's tendency to respect the better, more balanced and more time-tested natural approach to COX-2 inhibition.


Cyclooxygenase, and its inhibitors, have probably been with us through the course of our evolution, but they were unknown, or at least unnamed, until fairly recently. Even so, humans have long recognized that certain natural compounds are effective in treating inflammation and pain. Over the course of time, we've gradually learned to use these herbs and spices to our advantage.

As MOTHER readers already know, the biochemistry of traditional herbs is more complex, better balanced, often more effective, and just plain safer than the synthesis of chemicals marketed by a pharmaceutical company. Therefore, I think it premature to call the pharmaceutical COX-2-Is the "safe aspirin"--it's simply too soon to tell. Admittedly, these drugs have the potential to powerfully and dramatically relieve pain and save lives, but it's not unlikely that they will also cause some pain and suffering. Synthetic COX-2-Is are a laser-like molecular weapon that must be handled with care.

So far, pharmaceutical rums seem to be thinking much more positively about their "safe aspirin" than do the herbalists. Predictably, they also seem to be ignoring the alternative, natural COX-2-Is. To determine some of the most effective herbal COX-2-Is researchers, including myself, have scoured hundreds of herbal treatises and multiple databases, including the University of Illinois Napralert Database (compiled by Norman Famsworth) and the United States Department of Agriculture (USDA) Phytochemical Database.

You can buy and try many of these herbs in newly prepared compound capsules or softgels. From your local natural pharmacy or health food store, the cost for these compounds will run around $30 a month (compared with $70 to $90 for comparable pharmaceuticals). On the other hand, you have to eat, so why not get your COX-2-Is from the spices, fruits and vegetables in your supermarket? I think it's safe to assume that the COX-2-Is you find in your food will be easier on your wallet while being much less likely to produce side effects. Zyflamend, Newmark and Schulick's new COX-2 blend, contains many of the more promising herbal COX-2-Is. I have all their ingredients (except holy basil and goldthread) thriving in my Green Farmacy Garden, but a prepared monthly supply of Zyflamend runs about $20.

Two softgels in a base of olive oil and beeswax contain: 100 mg holy basil 100 mg turmeric 100 mg ginger 100 mg green tea 100 mg rosemary 50 mg or 80 mg (if extract) Mexican bamboo (resveratrol) 40 mg Chinese goldthread 40 mg barberry root 40 mg oregano 20 mg baical skullcap

The RiverHill Wellness Center in Columbus, Maryland, has an effective combination product called Connective Tissue Repair (CTR), which is used for many chronic inflammatory conditions. CTR contains turmeric, ginger and bromelain (all excellent anti-inflammatory agents), plus turmeric (to detoxify the liver), quercetin (to reduce the histamine load that can aggravate nerve tissues), devil's claw and yucca (to cleanse joints of irritating waste). A daily dose of this product--two or three capsules--will cost you between 40 and 60 cents. CTR has resolved many chronic conditions, reduced pain without demineralizing the bone tissue (as do the NSAIDs) or weakening the immune system (as do steroids), and without causing stomach and/or GI ulceration. Many folks have regained their range of motion in affected joints, and their nerve pain has healed over time. Talk about effective, affordable and accessible!

If you're one of those nutritionally ambitious people who "strives for five," you'd be well-advised to "struggle for seven." It's easy to get your COX-2-Is by eating a a well-balanced diet loaded with fruits, veggies, nuts, beans and grains. And if the promoters of Celebrex are correct in believing that COX-2-Is can prevent colon cancers, there's no reason to hold back on upping your intake and possibly warding off that dreadful disease. (See "Easy Ways to Up Your Intake of COX-2-Is".)

Many of the foods we eat every day contain COX-2 inhibiting phytochemicals that our genes already know and recognize, so those of you who are polyp-prone might want to increase your dietary uptake of COX-2-Is in your herbs, fruits and veggies. There are plenty of natural COX-2 inhibitors out there, contained in any number of well-known anti-inflammatory food plants or GRAS (Generally Regarded As Safe) spices (for a list of herbs, see "Natural COX-2 Inhibitors").

Suffering from gardener's arthritis today, I'd certainly feel safer indulging in some of these natural COX-2-Is than in the expensive new pharmaceuticals that came out in 1999 and will continue to emerge in 2000.

A List of Herbs and Some of the Natural COX-2 Inhibitors They Contain

* chamomile

* celeryseed

* ginkgo (ginkgo

* leaves are not a food) for apigenin

* skullcap (not a food) for baicalein

* hops, barberry, goldenseal, goldthreed, Oregon grape, yellowroot (none of these are foods) for berberine

* boswellia (not a food) for boswellic acid

* rhubarb, currant and green tea for catechin

* green tea, cabbage, and chives for kaempferol

* clove, rosemary, thyme, sage, lavender, marjoram and ginseng

* cardamom, ginger and turmeric for curcumin

* feverfew (not a food)

* rosemary, sage, and thyme for ursolic acid

Go Natural

One bottle of 200mg-dose Celebrex (60 pills) costs between $150 and $200, A 60-pill bottle of 25mg-dose Vioxx will run you $100 to $125. Sales of both drugs are expected to reach $5 billion annually by 2003.

Easy Ways to Up Your Intake of COX-2-Is

1 Replace some or all of your coffee with green tea and/or chamomile infusion. Spice them up with clove, lavender, marjoram, rosemary, sage and thyme.

2 Eat more cabbage, celery, chives, currants and rhubarb.

3 Use more celeryseed, ginger, and turmeric in your teas and cooking.

4 Enjoy grape juice or red wine for their resveratrol--better yet, enjoy stuffed grape leaves.

Beyond Aspirin: Nature's Answer to Arthritis, Cancer & Alzheimer's Disease by Thomas M. Newmark and Paul Schulick. (Hohm Press, 2000). James A. Duke. "Paracelsus: Clippings from my COX Box." Journal of Medicinal Foods 1, no. 4 (1999): 293-98.

L.M. Posey. "Safety of COX-2 Inhibitors Explored at Digestive Disease Week." Pharmacy Today 6, no. 7 (2000): 13.
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Author:Duke, James
Publication:Mother Earth News
Geographic Code:1USA
Date:Jan 1, 2001
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