Excerpted from: Health Store News, February 1996 / March 1996

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Wonderful Benefits of Lapacho
by Dan Mowrey

Dr. Daniel Mowery
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Lapacho is found in the rain forests and mountains of Paraguay, Argentina and Brazil. This plant holds great promise for the effective treatment of cancers such as leukemia, Candida and other troublesome infections, as well as debilitating diseases (including arthritis) and a host of other complaints.
The medicinal part of the tree is the bark, specifically the inner lining of the bark, called the phloem (pronounced floam). The use of whole bark, containing the dead wood, naturally dilutes the activity of the material. Lapacho is also known by the Portuguese name of Pau d'arco and by tribal names such as taheebo and ipe roxo. Some texts distinguish between lapacho colorado (red lapacho=ipe roxo) which grows in cooler climates such as high in the Andes and high places in Paraguay. Recent evidence suggests that these two varieties of lapacho possess superior medicinal properties with a slight bow going to the purple as the best of all.
Most of the chemical analyses of lapacho have been performed on the heartwood of the tree rather than on the phloem, or inner lining of the bark, which is used medicinally. It is unclear why this has occurred. One reason may be that the heartwood contains enough quantities of a couple of important constituents. Mainly lapachol and tabebuin, to satisfy current research interests. It is probably safe to assume that the living bark contains a similar set of active contstituents to the heartwood plus some others that make it more effective and would account for the living bark's greater popularity as a folk medicine. Traditionally, as anyone who chooses to examine the herbal literature of the world can verify, it is the living bark of a plant, especially a tree or shrub, that is used medicinally, not the heartwood. The reason is simple: the nutrients and representative families of chemical substances used to sustain the life of the tree are found in greatest concentration in the cambium layer and phloem of the living bark.
The life processes of a mature tree are carried out in the thin corridor lying between the outer bark and the inner heartwood. Pull the bark off of a tree and you will notice moist, very thin layers of tissue that seem to shred when picked at with the hands. This is the cambium layer. Its purpose is to create new tree tissues, such as phloem, through cell division. The newest, youngest phloem cells are just outside the cambium. As new phloem is added, older cells are crushed and pressed into the bark. Younger, newer cells added to the inside of the cambium layer are called xylem. New xylem is called sapwood; older xylem is crushed and pressed into the heart of the tree. It is therefore known as heartwood. The actively conducting tissues of a tree are the thin layers of fresh xylem and phloem on each side of the cambium. The outer bark and heartwood are, essentially, inactive materials that only serve to provide strength to the tree. Indiscriminate combing of older less active layers of bark and tree with the younger, living tissues results in a dramatic dilution of active principle and medicinal value. Yet it is a common practice of commercial lapacho suppliers.
Lapacho is just one of a number of plant substances known as napthaquinones (N-factors) that occur in lapacho. Anthraquinones, or A-factors, comprise another important class of compounds. The N-factors are not common except in herbal tonics. Seldom do both N- and A-factors occur in the same species. Several of the remarkable properties of lapacho may be due to a probable synergy between A- and N-factors.
Quercitin, xyloidone and other flavonoids are also present in lapacho; these undoubtedly contribute to the plant's effectiveness in the treatment of tumors and infections.
The native Indians of Brazil, northern Argentina, Paraguay, Bolivia and other south American countries have used lapacho for medicinal purposes for thousands of years; there are indications that its use may actually antedate the Incas. Before the advent of the Spanish, the Guarani and Tupi-Nambo tribes in particular used great quantities of lapacho tea. In the high Andes, the Calawaya, the Quechua, Aymara and other tribes used lapacho (taheebo to them) for many complaints.
Lapacho is applied externally and internally for the treatment of fevers, infections, colds, flu, syphilis, cancer, respiratory problems, skin ulcerations and boils, dysentery, gastrointestinal problems of all kinds, debilitating conditions such as arthritis and prostatitis, and circulation disturbances. Other conditions reportedly cured with lapacho include lupus, diabetes, Hodgkin's disease, osteomyelitis, Parkinson's disease and psoriasis.
Lapacho is used to relieve pain, kill germs, increase the flow of urine, and even as an antidote to poisons. Its use in many ways parallels that of echinacea on this continent and ginseng in Asia, except that its actions appear to exceed them both in terms of its potential as a cancer treatment. The Guarani, Tupi and other tribes called the lapacho tree tajy, meaning "to have strength and vigor," or simply "the divine tree." Modern Guarani Indians prefer the purple lapacho but also use the red lapacho. And they use only the inner linings of the bark.
Research on lapacho has been going on for a long time. E. Paterno isolated the active constituent, lapacho, in 1884. In 1896, S.C. Hooker established the chemical structure of lapachol, and L.F. Fieser synthesized the substance in 1927! So it would be a mistake to call lapacho a modern discovery.
As early as 1873 physicians were aware of the healing action of lapacho. Dr. Joaqin Almeida Pinto wrote during that year, "Pau D'Arco: Medicinal Properties: prescribed as a fever-reducer; the bark is used against ulcers; also used for venereal and rheumatic disorders and especially useful for skin disorders, especially eczema, herpes, and the mange." Another physician, Dr. Walter Accorsi, reported that lapacho "eliminated the pains caused by the disease [cancer] and multiplies the body's production of red corpuscles."
However, the science of lapacho began properly with the work of Theodoro Meyer in Argentina, who tried for decades with little success to convince the medical world of the value of lapacho for infections and cancer. Data from his laboratory are astounding in terms of the success rate observed when applying the herb to dozens of different kinds of cancer. Much of Meyer's work was primitive by modern research standards; most of it lacked adequate controls and statistical evaluation. But the sheer bulk of it is good evidence for the efficacy of lapacho. The Meyer era ended at his death in 1972, with the scientific world left still largely unconvinced of the usefulness of lapacho as a modern medicinal agent. Perhaps the most important thing Meyer accomplished, from a scientific point of view, was to bring lapacho to the attention of the rest of the world, to extract the plant from the jungles of the Amazon and announce, "here is a folk remedy with great promise for all mankind."
Independent of meyer, a physician in Brazil, about 1960, after hearing a tale of its miraculous curative powers, used lapacho to treat his brother who was lying in a Santa Andre, Brazil hospital dying of cancer. His brother recovered, and the physician, Dr. Orlando de Santi, began to use the herb to treat other cancer patients at the hospital. Other physicians joined the team, and after a few months, several cures were recorded. In the typical case, pain disappeared rapidly and sometimes complete remission was achieved in as little as four weeks.
Because of the work at the Municipal Hospital of Santo Andre, lapacho has become a standard of treatment for some kinds of cancer and for all kinds of infections in medical establishments throughout Brazil.

It should be noted that after the first reports of "miraculous" herbal cures appeared in Brazil, the national government ordered a blackout of any more public statements by doctors involved in the research. The silence was finally broken by Alec De Montmorency, who in 1981 published a lengthy review of the ongoing clinical work in Brazil. This report succeeded in stimulating worldwide interest in the plant. (emphasis mine - kr)

In 1968, Dr. Prats Ruiz of Concepcion, Paraguay, successfully treated three cases of leukemia in his private clinic. Some of these results were widely published and also helped to establish the popularity of lapacho among the "civilized" inhabitants of South American countries.
American physicians, of course, tend to look disparagingly upon clinical evidence from backward areas of South America, preferring instead sanitized evidence from their own brightly lit laboratories. The weight of the South American clinical evidence has not been sufficient to cause widespread acceptance of the treatment outside South America, but it has stimulated research interest abroad. Pharmaceutical companies regularly screen lapacho for the presence of substances that could be the basis for new drug applications. As we shall see, however, no isolated component of lapacho comes anywhere close to being equal to the combined activity of all constituents or, in other words, to the whole herb.
A common thread that runs throughout early and current empirical and clinical reports of lapacho treatment is the consistent observation that the herb eliminates many of the orthodox medications. There is no explanation of this action, but it is so often seen that one cannot easily doubt its validity. Pain, hair loss and immune dysfunction are among the symptoms most commonly eliminated.
While scientific research on lapacho has been going on for decades, most of it is worthless from a medicinal point of view. Some of it, however, is very good and has resulted in the isolation of several individual medicinally active constituents and in the analysis of their properties. The current interest in AIDS has stimulated renewed interest in lapacho since the herb is such an effective antiviral substance.

Effects of Lapacho

The following is a summary of some of the effects of lapacho and/or any of its constituents that have been validated by modern research:

  • Laxative effect
    Regular use of lapacho will maintain regularity of bowel movements. This property is undoubtedly due to the presence of the naphthaquinones and anthraquinones. Users of lapacho universally report a pleasant and moderate loosening of the bowels that leads to greater regularity without any unpleasant side effects such as diarrhea.

  • Anticancer effect
    The greater part of the research on lapacho, both in the United States and in other countries, has dealt directly with the cancer question. Obviously this issue is of great importance. Any tendency of lapacho to ameliorate the course of cancer should be made known to all persons likely to benefit from it. The absence of side effects makes lapacho a treatment of choice, even in conjunction with standard forms of therapy. The user has nothing to lose and much to gain from the judicious use of lapacho. Naturally, any and all treatment of a cancerous condition should be done under the supervision of a qualified physician.
    Some constituents or groups of constituents of lapacho have indeed been found to suppress tumor formation and reduce tumor viability, both in experimental animal trials and in clinical settings involving human patients. In addition, anecdotal data abounds to such an extent that to overlook its importance is to turn one's back on a potentially invaluable source of aid and health. Leukemia has proven particularly susceptible to the application of lapacho and several of its constituents. Some researchers feel that lapacho is one of the most important anti-tumor agents in the entire world.
    Part of the effectiveness of lapacho may stem from its observed ability to stimulate the production of red blood cells in bone marrow. Increased red blood cell production would improve the oxygen-carrying capacity of the blood. This, in turn, could have important implications for the health of tissues throughout the body. Also needed for oxygen transport by red cells is iron. This might explain the augmentation in lapacho's therapeutic properties when it is combined with iron-rich yerba maté, another South American plant; in fact, it is native practice to almost always combine these two plant species.
    National Cancer Institute research on the anti-cancer action of lapacho has been disappointing. Unfortunately, the NCI restricted its investigations to lapachol, and once it found that this substance had side effects that offset its potential therapeutic benefits, it abandoned the project. From the perspective of a tonic, one can readily perceive the fallacy of that approach and would suspect that the problems in the research stemmed directly from employing isolated herbal constituents. As one might also suspect, research that utilized whole lapacho has produced clinical anticancer effects without side effects.
    Animal research in the United States made a gigantic stride forward when it was discovered that lapachol inhibited solid tumors (Walker carcinosarcoma 256 and Ehrlich solid carcinoma) and Ehrlich ascites cell tumors. Such research then took a gigantic stride backwards when clinical toxicity of lapachol prematurely ended those investigations.
    One interesting line of research has shown that lapachol is more effective when ingested orally than when injected into the gut or into the muscles. These results contradict a substantial amount of research on orthodox drugs that indicates the superiority of injectable routes. What is the meaing of this anomaly? Could it be a sign that naturally routes of administration (i.e., oral) are better suited for natural substances? The further removed from the natural state the more active substances become when injected directly into the blood stream and the less able the natural processes of the body are in dealing with them.
    Using the wood of the plant, several researchers have studied the effects of lapachol, alpha- and beta-lapachone and xyloidone on experimental cancer (Yoshida's sarcoma and Walker 256 carcinosarcoma). As high as 84 percent inhibition was observed on Yoshida's sarcoma, and no toxicity was found.
    In one clinical study, South American researchers administered lapachol to patients with various forms of cancer, including adeno-carcinoma of the liver, breast and prostate and squamous-cell carcinoma of the palate and uterine cervix. Taken orally, the substance resulted in temporary reduction of all conditions and in significant reduction in pain. Duration of treatment was anywhere from 30 to 720 days, with an average of about two months. For example, one patient with liver cancer experienced a significant reduction in jaundices accompanied by other signs of improvement after eight days of therapy. These results were in close accord with results obtained by the same researchers in animal studies. One wonders what the administration of whole purple lapacho phloem might have accomplished in this setting; other lines of evidence suggest that even better results might have been obtained.
    A note on nausea: In the human study reported above, some patients dropped out of the experiment due to nausea. This is a common observation in some, but certainly not all, people who begin to expericence the cleansing action of lapacho (and other healthful herbs). As toxins (and toxic medicines) and wastes are drawn out of the cells, or flushed out, or are physiologically drawn out of the cells through the action of the herb, they tend at times to accumulate in the blood, lymph, lymph nodes, skin, liver and kidneys awaiting the opportunity to be expelled from the body. Backing up, they can on occasion produce sensations such as nausea; the body may even try to rid itself of some toxic substances by vomiting. Not to worry. These transient signs dissipate once the toxins are moving freely from the body. They are a positive sign that the herb is working. Remember the body only has three basic processes for getting rid of wastes: lower bowel movement, sweating and urinating. The use of lapacho can so overload these processes in the early stages that discomfort may be produced.

  • Antioxidant effect
    In vitro trials show definite inhibition of free radicals and inflammatory leukotrienes by lapapcho constituents. This property might underlie the effectivenesss of lapacho against skin cancer and definitely helps to explain observed antiaging effects. Modern science has recently uncovered the importance of free radicals in the generation of many debilitating diseases from cancer to arthritis. These molecules are even heavily implicated in the normal aging process. Reversing their action has become big business in world health circles. Antioxidants, or free-radical scavengers, have emerged as premier candidates for the role of healers and disease preventers. Among the antioxidants few have greater potency than lapachol.

  • Analgesic effect
    The administration of lapacho is consistently credited in reports issuing from South American clinics as a primary modality for lessening the pain associated with several kinds of cancer, especially cancer of the prostate, liver or breast. Arthritic pain has also been relieved with lapacho ingestion.

  • Antimicrobial / antiparasitic effects
    Includes inhibition and destruction of gram positive and acid-fast bacteria (B. subtilis M. pyogenes aureus, etc.), yeasts, fungi, viruses and several kinds of parasites. Two troublesome families of viruses inhibited by lapachol are noteworthy, herpes viruses and HIV's. Together these viruses account for much of the misery of mankind. The antimalarial activity of lapacho spawned a great deal of research interest in the early decades of this century. A 1948 article reviewed the progress and indicated that the N-factors, especially lapachol, were among the most promising antimalarial substances known at that time. Lapacho's immuno-stimulating action is due in part to its potent antimicrobial effects.
    One of the strongest actions of lapacho is against viruses. The range of viruses inactivated by lapacho extends from those that cause the common cold to those that are responsible for AIDS. It has been shown to actively inhibit, kill or stunt the growth of several dangerous viruses including herpes virus hominis types I and II, polio virus, vesicular stomatitis virus, avian myeloblastosis virus, murine leukemia virus, Friend virus and Rous sarcoma virus. Several other viruses are also inhibited by lapacho's N- and A-factors.
    One N-factor, beta-lapachone, inhibits enzymes in virus cells that directly affect the synthesis of DNA and RNA. It is also a potent inhibitor of the enzyme reverse transcriptase, involved in RNA/DNA relationships. Once these processes are inhibited, the virus is unable to take over the reproductive processes of the cell and cannot, therefore, replicate itself and infect other cells. Such inhibition is a characteristic of most substances that are being tested for activity against AIDS and Epstein-Barr. The enzyme in question is a key to the action of retroviruses. These viruses, also known as ribodeoxyviruses or oncornaviruses, have been implicated in the development of several kinds of experimental cancers. Beta-lapachone is obtained simply by treating lapachol with sulfuric acid, and tests show that it has a unique method of action vis-a-vis the reverse transcriptase inhibition.
    Note: Sulfurous compounds in some plants, especially yerba mate, when combined with lapacho, might provide a catalytic base for the transformation of lapachol to beta-lapachone and hence increase the effectiveness of lapacho. In this light, it is interesting to note that native folklore teaches that yerba mate is a catalyst for lapacho; yerba mate becomes the foundation for lapacho therapy.
    Lapacho components have been intensively studied in terms of their action against two rather nasty parasites, Schistosoma mansoni and Trypanosoma cruzi, both responisble for considerable disease and misery in tropical countries. Lapacho was effective against both. Taken by mouth, lapachol is eventually secreted onto the skin via the sebaceous glands where it acts as a topical barrier, inactivating micro-organisms soon after they contact the skin. Meanwhile, throughout the GI tract, it is performing the identical function on the mucous membranes, preventing the penetration of parasites. The mechanism of action is not well understood but is felt to involve the uncoupling of cellular respiration (see the following section on mechanisms of action), the stimulation of lipid peroxidation and superoxide production and the inhibition of DNA/RNA biosynthesis.

  • Antifungal effect
    Lapacho is often singled out as the premier treatment of Candida or yeast infections. Lapachol, N-factors and xyloidone appear to be the primary active principles. By the mid-70s the list of N-factors that inhibited Candida albicans and other fungi had grown to several dozen.
    It would be misleading to categorically state that the N-factors in lapacho have proven antimicrobial and antifungal activity in and of themselves. Studies have shown that the manner in which they occur in the plant must be taken into consideration. We know, for example, that antifungal activity is lost when the N-factors are tightly bound to highly water-soluble or highly fat-soluble groups. It has not been clearly determined how the N-factors occur in lapacho.
    N-factors, obtainable from various chemical supply companies, have become favorite testing agents in government and university labs due to the rise in yeast infections resulting from increased use of cyto-toxic drugs, corticosteroids, antibiotics and immunosuppressants.
    An interesting application has been reported in which toe and fingernail fungal infections are relieved by soaking these appendages in lapacho tea off and on for a couple of weeks.

  • Anti-inflammatory
    The anti-inflammatory and healing action of lapacho extracts was demonstrated in a study in which purple lapacho extract was administered to patients with cervicitis and cervicovaginitis, conditions resulting variously from infections (Candida albicans, Trichomonas vaginalis, chemical irritations and mechanical irritiation. The lapacho extract was applied intravaginally via gauze tampons soaked in the extract and renewed every 24 hours. The treatment proved to be highly effective. One wonders what might happen were the tampon method combined with the ingestion of strong teas.

  • Other beneficial effects
    Routine screenings have revealed several minor properties of lapacho that might occur if needed in certain individuals: diuretic, sedative, decongestant and hypotensive, to name a few. Unfortunately, space limitations preclude a lengthy discussion of all the benefits of lapacho, but some of the major actions listed above require further elaboration, which will be given in the next section.

    Mechanisms of Action

    Every cell of the body requires oxygen and glucose to obtain energy for life-sustaining functions. The oxygen and glucose are subjected to a fairly complex metabolic process in the tiny energy-producing structures in the cell called mitochondria. This process requires numerous enzymes and coenzymes. The oxygen and glucose are converted to carbon dioxide and water which are then returned to the blood. The CO2 is exhaled by the lungs (hence this metabolic process is often called respiration); excess water is eventually drawn off through perspiration or through the kidneys. During this conversion, several electrons are freed, which are immediately utilized by another pathway to produce ATP (adenosine triphosphate), the energy currency of the cell. ATP is the molecule every cell is required to utilize, or spend, to obtain energy. The two paths, one for breakdown of glucose and one for synthesis of ATP, are tightly coupled together. Should they become uncoupled, the cell can no longer obtain energy and it dies, a process referred to as uncoupling of oxidative phosphorylation; many of them resemble the N-factors in lapacho. In fact, it has been found that lapacho works like other benzoquionones; i.e., it uncouples the mitochondrial oxidative phosphorylation occurring in cancerous cells but not in healthy ones. This selective killing (cytotoxicity) of tumor cells is what makes lapacho such a potentially valuable agent for the treatment of cancer.
    One of the games science plays is attempting to discover at what point cellular respiration is broken up by chemical agents. The components of lapacho seem to interrupt the process at several points, usually by inhibiting an enzyme or coenzyme that is required for the next step in the chain to occur properly. For instance, lapacho inhibits the proper functioning of AT-Pase, the enzyme that catalyzes the final step in the formation of ATP.
    Lapachol has also been shown to inhibit the amount of another substance required for cellular reproduction: uridine triphosphate. This molecule is the main source of substances (called pyrimidine nucleotides) that are required by cells in order to build DNA, RNA and most other important proteins of the body. Lapacho may actually block the synthesis of pyrimidines in cancer cells (by inhibiting the enzyme dihydroorotate dehydrogenase). The result would be certain cellular death.
    There is also evidence that lapacho interacts directly with the nucleic acids of the DNA helix in cancerous cells. If such interaction, or bonding, takes place, DNA replication would be impossible. The result is also eventual death of the cell.
    Finally, the lapacho constituent beta-lapachone has been shown to weaken malignant cells, even to the point of cellular death by stimulating a process known as lipid peroxidation, which produces toxic molecules.

    Safety Data

    While there can be no doubt that lapacho is highly toxic to many kinds of cancer cells, viruses, bacteria, fungi, parasites and other kinds of microorganisms, the substance appears to be without any kind of significant toxicity to healthy human cells. The side effects mainly encountered (and usually with isolated lapacho constituents) are limited to nausea and anticoagulant effects in very high doses, a tendency to loosen the bowels and diarrhea in very high doses. As indicated earlier, some nausea should be expected as a natural consequence of the detoxification process. The FDA gave lapacho a clean bill of health in 1981.
    Some trials have indicated that lapachol has antivitamin K action. Other constituents have a provitamin K action; it is likely, therefore, that the two actions cancel each other out (except possibly when one or the other is necessary, as one would expect from an herbal tonic).
    Perhaps the most significant study on toxicity was published in 1970 by researchers from Charles Pfizer & Co., Inc. Looking specifically at lapachol, these investigators found that all signs of lapachol toxicity in animals were completely reversible and even self-limiting; i.e., over time the signs of toxicity decreased and even disappeared within the time constraints of the study.

    Yerba Maté