Worldwide, there has been a resurgence in the use of herbal medicines. In 2004, approximately 29 percent of Americans used some form of herbal medicine, following a steady increase in usage during the preceding 10 years. Part of this renewed interest is fueled by the general belief that herbal medicines are safer than the synthetic chemicals offered by conventional medicine. However, weren?t most of today?s chemical drugs originally derived from plants?
According to the World Health Organization, approximately 60 percent of modern drugs were derived from plants. In fact, prior to 1806, all drugs were either of vegetable or mineral origin. In 1806, a German apprentice pharmacist named Sert?rner, for the first time in history, succeeded in isolating a pure compound from a plant. The compound? Morphine, named after Morpheus, the Greek god of dreams or sleep. The plant? The opium poppy, the seed capsule of which was traditionally used to promote sleep (Booth, 1998).
Since then, medical researchers have been on the hunt for the proverbial magic bullet, that active constituent that is thought to give a plant its medicinal effect. The question facing all of us today is which is better, the original herbal medicine or the modern, synthetic version? While an exploration of a few treatments may not answer this question entirely, it may nevertheless give us food for thought within the context of the growing interest in natural medicines.
Sometime in the 1700s, a French medical researcher looking for a remedy to treat his father-in-law?s arthritic pain found a report of the historic use of willow bark for treating pain due to arthritis. While the remedy proved ineffective, it later stimulated interest among others who, in 1830, identified salicin as an active compound of willow. Many salicin-rich plants such as willow, meadowsweet and wintergreen had historically been used internally and externally to ease arthritic pain. However, the medicos of the time continually sought ways to further purify and isolate the plant?s pain-easing compound, which led to the development of salicylic acid, sodium salicylate and then acetyl-salicylic acid—today?s aspirin.
However, there was a significant drawback: These compounds were irritating to the stomach lining, often resulting in bleeding. In an attempt to create a less irritating medicine, a chemist at the Bayer company in Germany further refined the acetyl-salicylic acid into today?s buffered aspirin (Leake, 1975). Noting that salicin, the precursor of acetyl-salicylic acid, had previously been isolated from the plant Spiraea ulmoides, the German researchers named the new compound acetyl-spiric acid followed by aspiric acid, and finally, aSPIRin. While the name was originally a brand name, which was the property of Bayer of Germany, it became so widely used that it eventually became generically applied to all acetyl-salicylic acid compounds.
And, what of the herbal sources of aspirin?s precursor, salicin? Interestingly, stomach irritation was not a side effect of the botanical progenitors, some of which were specifically used to treat digestive upset. Several other problems with the use of aspirin, which were not historically evident with its herbal counterparts, have been found in modern times. These include the ability of aspirin to thin the blood, which can lead to bleeding problems beyond that secondary to stomach irritation; a propensity to cause allergic reactions in sensitive individuals; and a correlation, albeit a weak one, with the development of Reye?s syndrome in children.
Specifically, the herbal preparations that were the original sources of salicin—willow bark, wintergreen, birch bark and the leaves and barks of poplar trees—do not have the same blood thinning effect as aspirin, have rarely been associated with allergic reactions and were never correlated with Reye?s syndrome. Therefore, for many, the natural sources of salicin may be safer choices for the management of everyday minor aches and pains of arthritis and headaches, and to reduce fevers.
Willow bark: The barks of various species of willow (Salix) have been used since at least the first century, when it was reported by Dioscorides that a decoction and poultice of willow would treat inflammation associated with gout. After Dioscorides, many European medical authorities continued to use various willow preparations for the same purposes, as well as for its ability to reduce fevers, kill intestinal worms (Mayer and Mayer, 1949), and act as an astringent. Willow was also officially recognized in the United States Pharmacopoeia from the first edition in 1820 to the 10th edition in 1926. Beginning with the 11th edition, aspirin replaced the natural willow preparations (Upton, 1999).
Willow was used in the late 1800s by a group of physicians known as the Eclectics. Eclectic physicians predominantly used herbal medicines while conventional medical practitioners were still using leeches and mercury compounds. In contrast to the bleeding and stomach-irritating effects of aspirin, the Eclectics specifically used willow for its anti-inflammatory properties as well as to stop minor hemorrhages and for digestive discomfort (Jones and Scudder, 1858). Willow is still widely used in herbal compounds today, either as the crude herb itself or in preparations standardized to specific potencies of the naturally occurring salicin.
Meadowsweet: Currently known as Filipendula ulmoides, in former times meadowsweet was known by the name Spirea ulmoides, the plant that provided the original source of the aspirin precursor salicin. Though not widely used in American herbal medicine, meadowsweet has long been prominent among European herbalists, who employ it as a digestive aid, unlike aspirin, to specifically soothe an irritated stomach mucosa (Hoffmann, 2004). Like willow, it was also used as a mild astringent to stop bleeding.
Wintergreen: The leaves of this plant are naturally rich in salicylates. Most often, the distilled oil of wintergreen is diluted and used topically to help relieve arthritic pain, sciatica and, when a drop is massaged around the temples, headaches. It is also used diluted in other oils as a general liniment (Morton, 1977).
This neuropeptide (a compound that stimulates nerve cell receptors) derived from cayenne peppers was approved as a topical over-the-counter analgesic a number of years ago. Capsaicin blocks the transmission of pain by depleting a neurotransmitter called substance P, a substance correlated with pain. In clinical trials, topical creams of capsaicin (0.025 percent to 0.075 percent) have been used to treat painful skin disorders such as shingles, psoriasis, phantom pain syndrome and diabetic neuropathy, to name a few. One of its most common uses is for relieving pain caused by arthritis.
Cayenne pepper: Many spices such as cayenne were used historically as topical rubs and liniments. Traditionally, cayenne was used both internally and externally. Internally, it was used as a circulatory tonic, an antispasmodic, for digestive complaints and to promote sweating. Externally it was used to promote local circulation. Some of these traditional uses have been codified by the German health ministry (Commission E), which approves of its use for the treatment of pain caused by muscle spasm and arthritic conditions. Cayenne pepper naturally contains 0.02 percent capsaicin (Tyler, 1994), the same amount contained in many of the OTC products.
A traditional preparation recommended by Jethro Kloss in his classic text Back to Eden was made by gently boiling 1 tablespoon of cayenne pepper in 1 pint of apple cider vinegar for 10 minutes. This was bottled and was considered as a premier liniment that could be used externally for deep-seated congestions, when rubbed on the back or chest, and for arthritis.
In 1719, a researcher named Caspar Neumann discovered the compound thymol from the common household spice thyme (Thymus vulgaris). Much later, in 1953, Italian researchers found that compounds in thyme exhibited antibiotic activity against two families of bacteria (gram positive and gram negative). It has been official in various pharmacopoeias as an antimicrobial drug since the 16th century (Morton, 1977), and is a primary ingredient in the popular conventional mouthwash Listerine. Used in its isolated form, thymol carries with it a host of side effects including diarrhea, nausea, vomiting and a depressant effect on the heart (Morton, 1977). Such side effects are typical of pure essential oils, due to the high concentration of pure compounds.
Thyme: A common house spice, thyme has also been used since antiquity for its antimicrobial activity. In the late 1800s, it was widely used for upper respiratory infections and for whooping cough, especially in children. It was used in many different ways, but primarily as a tincture (alcohol extract), tea (especially for children) and even as an inhalant by boiling the herb in water and inhaling the steam. The side effects noted above with pure thymol have never been reported to be associated with the crude herb, likely because of the much lower concentration of oil that exists in the entire plant, as well as the poor solubility of oils in water.
Ephedrine and pseudo-ephedrine
Commonly used in over-the-counter antihistamines, allergy and cold medications, these two compounds were originally derived from the Chinese herb Ephedra sinica. Used in Chinese medicine since the first century, ephedra is a perfect example of a great herb gone bad through modern purification, isolation, concentration and inappropriate use. Despite its long history of use in China, Western medicine only learned of the bronchodilating and antihistamine effects of ephedra in the late 1800s. As with aspirin, modern researchers were not content with the natural form of the drug and so a similar course of purification and isolation was soon under way, leading to the development of pure ephedrine and pseudo-ephedrine products, such as Sudafed. While not inherently problematic, the availability of the pure, concentrated compounds leads to their use in botanical dietary supplements to cut the appetite and jack up metabolism in a rush of stress-like nervous energy. With it comes an increase in blood pressure, cardiac arrythmia, heart attacks, strokes and death, none of which were associated with the herb itself.
Ephedrine and pseudo-ephedrine alternative
Ephedra: In Chinese medicine, ephedra is used in a very specific way—usually very deliberately combined with other herbs—specifically to avoid such side effects as noted above. It is also used for specific upper respiratory system ailments and for certain types of colds and flu, rather than in fad weight-loss products or energy stimulants. When used in the traditional manner, side effects are seldom seen and rarely dangerous. Traditional preparations typically contain less or the same amount of total ephedrine alkaloids as are in approved OTC preparations, which are considered safe. Unfortunately, the popular misuse of ephedra led to its recent banning, though the U.S. Food and Drug Administration chose to ban only the herbal products, while the OTC counterparts remain on the market, as do Chinese medicines.
Try herbs first
Those of us who reach for the herbal product over the synthetic have a belief in the superiority of nature. This is partly based on the fact that botanicals that contain sometimes hundreds of different compounds, many with complementary actions, work via multiple pathways. These types of medicines tend to be broader acting and are more likely to affect some physiological mechanism that historical herbal experience has demonstrated results in a positive change. It is also partly based on the fact that relatively crude botanicals and their extracts are typically less potent than the pure concentrated compounds of Western medicine. While a modicum of activity is lost with decreasing potency, a greater margin of safety is awarded. In contrast, the pure, highly concentrated isolates elicit a very narrowly focused activity, which produce a marked, often imbalanced, pharmacological effect. While sometimes necessary, the potential for toxicity of these is much greater. We herbal advocates believe in first trying the natural, complete spectrum herbal versus its highly purified, often synthetic counterparts. If the natural remedy does not work, we can always reach for the more modernized drug versions with their increased risk of toxicity and increased price.
Roy Upton is trained in Western and traditional Chinese herbalism and has worked professionally as an herbalist for more than 22 years. He is vice president of the American Herbalists Guild, serves on the board of directors of the Botanical Medicine Academy, is the executive director and editor of the American Herbal Pharmacopoeia, and is general manager of the California-based herbal company Planetary Formulas.
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