Allicin Has Been Used for Opportunistic Infections of AIDS Patients

The Applications of Allicin in Preventing and Treating Opportunistic Infections of AIDS

                                           Qingcai Zhang,

                                            Sino-Med Research Institute

                                           20 East 46th Street, Suite 1402

                                                New York, NY 10017

I. Opportunistic Infections of AIDS

              Immune deficiency caused by HIV infection is not inherently life-threatening.  It creates a milieu for many pathogens to invade and infect the host as opportunistic infections (OIs). The invaders can be bacteria, mycobacteria, fungi, protozoa or viruses. The OIs can be a single or multiple organisms infection. Most AIDS related deaths are due to such opportunistic infections. Consequently, the successful treatment of opportunistic diseases is crucial to the aim of prolonging and improving the HIV-infected person’s life. In recent years, more treatments have become available for the treatment of life-threatening OIs, increasing the life span of AIDS patients. This, however, is a double edged sword: As patients live longer, they are vulnerable to OIs for a longer time span. This provides more opportunities for OIs to occur. That is to say that increased longevity has allowed for an increase in the incidence and prevalence of OIs. In caring for the HIV infected population, treating and preventing OIs assumes greater importance, especially when the CD4 count drops below 200.  Many Chinese herbal remedies have been found to be effective in treating OIs. Some of them can be used as replacement for conventional pharmaceuticals, which usually are more toxic and expensive and others fill gaps in conventional treatments. Allicin is one of the most effective Chinese herbal remedies for treating and preventing the OIs of AIDS.

              When I was searching Chinese herbal remedies for OIs, I speculated that the pathogens of OIs might be less virulent than non-opportunistic germs since they are pitted against a less capable adversary. The common germs can make common people sick, but the OI germs have a higher infection rate in the immune-compromised cohorts. Allicin has been successfully used to treat many kinds of common infectious diseases should be able to treat OIs.

              What would we require of drugs capable of treating OIs? They must have low toxicity. They should be tolerable on a long-term basis, especially after certain OIs have already occurred. The secondary treatment and prevention of relapse must be safe enough to be taken potentially for the duration of the patient’s life. The treatment must have both low acute and minimal cumulative toxicity. Allicin is virtually non-toxic and meets the above criteria.

              Due to the patient’s immune-compromised condition, the OIs are usually caused by multiple agents including combinations of bacteria, protozoa, fungi and viruses.  Therefore, the remedies must have a very broad anti-infection spectrum. Most pharmaceuticals are designed specifically for one kind of infectious agent. This requires the patient has to receive panoply of different drugs. Overlapping and potentially cumulative toxicities of these drugs can render such regimens unsafe, intolerable and, therefore, unacceptable. Sometimes conventional antibiotics which suppress bacterial infection are made from fungi, which then can facilitate the growth of a fungus. In the same way, Western anti-fungal drugs sometimes encourage bacterial infections. Instead of solving a problem, a new one is created. Pharmacological studies have found that Allicin has a very wide spectrum of anti-infectious ability that can cover bacteria, protozoa, fungi and viruses. It is an ideal candidate to use for the scenario of multi-agent co-infection.

              For OIs’ prevention, I like the concept– MOPPS — Multi Opportunistic Pathogen Prophylaxis. MOPPS is an active concept. It was designed as a treatment protocol to prevent multiple pathogens opportunistic co-infections. Any medicine can be used as a MOPPS must meet the above discussed conditions. Allicin is an ideal herbal candidate for MOPPS.

 II. Allicin Pharmacology

              Thanks to the integration of Traditional Chinese Medicine (TCM) and modern Western medicine in China, the pharmacology and pharmacokinetics of many commonly used Chinese herbs, such as garlic, are now known. Utilizing pharmacological data of herbal remedies, we can use herbs almost in the same way as we do with pharmaceutical drugs. For many key herbs, we know their physiological effects, the correct therapeutic dose, their metabolism and toxicity. We can also use an understanding of the therapeutic mechanism of an herbal remedy to broaden its application to diseases similar to the prototypic application.  This method was used to research the applications of allicin in AIDS.

              Allicin is a highly purified and concentrated garlic essence. Garlic bulb contains volatile oil, of which allitin is the major constituent. When the fresh bulb was smashed, allitin is decomposed into allicin by allinase. Allicin produces garlic’s characteristic odor. Many deodorized garlic products are promoted but are not useful for against infections. The odor of the garlic is the responsible part of anti-infection properties. Chinese scientists have purified this active ingredient of garlic and determined its molecular formula to be C6H10S3. Chemically, is called diallyl trisulfide and it is chemically stable.  

              Pharmacological studies found that Allicin has a very broad anti-infectious spectrum. It has anti-bacterial, anti-mycobacterial, anti-fungal, anti-protozoa, and anti-viral properties.  Its 0.5% aqueous solution is lethal to Salmonella typhi within five minutes after contact. It is significantly bacteriostatic or bactericidal against the following: Staphpyloccocci, Neisseria meningitides, Streptococcus pneumonia, Shigella dysentery, Corynebaccterium diphtheriae, Escherichia coli, Salmonella typhi and paratyphi, Mycobacterium tuberculosis, var. hominis, and Vibrio cholerae.  Bacteria resistant to penicillin, streptomycin, chloramphenicol, or chlortetracycline are sensitive to allicin. Antifungal action was observed in vitro, such as Schlemm’s Dermatomyces flavosa, Trichophyton vilaceum, and Candida albicansIn vitro bacterostatic tests proved that 1-125 mcg/ml of diallyl thiosulfonate was as inhibitory to Candida albicans as 0.05-1 mcg/ml was to Cryptococcus rubrae and 3.2-12.5 mcg/ml was to Cryptococcus.   The minimum inhibitory concentration of allicin on fungi was 1 mcg/ml. Its effects were about the same as that of amphotericin B, but was far less toxic. The mechanism of the antibacterial action of diallyl thiosulfonate involves the binding of the oxygen atom of its molecule with cystein to avert the formation of cysteine, thus interrupting oxidation and reduction in the bacteria.

              Allicin (diallyl thiosulfonate) also has antiprotozoal effects.  Ameba trophozoites soon lost their activity upon direct contact with the 5-15% aqueous suspension of the bulb. Experiments using direct contact and fumigation methods showed that garlic juice killed all Trichomonas organisms in 10-25 minutes, and the volatile components in 90-180 minutes, whereas 0.5% of the bulb filtrate acting for five minutes deactivated Trichmonas vaginalis. Besides anti-infectious effects, allicin has antineoplastic, immune enhancing and blood lipid reducing effects.

              Allicin’s pharmacokinetics has been well studied. After intake of 35S-labeled allicin orally, the total radioactivity in organs peaked in four hours, and in eight hours declined to half the peak value. Ten minutes after intravenous injection of allicin into mice, serum drug concentration was highest in the lungs, and, in descending order, in the heart, intestines, blood, fat, brain, muscles, spleen, and liver. The metabolism of allicin in the body was very rapid. Most of the intravenous dose was transformed into water-soluble metabolites within 10 minutes. The major route of excretion was via the urine and partly the feces.

              Allicin has almost no toxicity with an LD50 is 134.9 mg/kg in mice which is 134.9 times higher than its therapeutic dose (1 mg/kg). In animal studies, rabbits were fed a 0.15% solution of allicin at a dose of 3 ml/kg twice daily for 10 weeks. The animals were euthanized and post-mortem examination was performed. No pathological changes were observed in the liver, spleen, adrenal glands, and lungs. Allicin is a very safe substance with an extraordinary therapeutic index.

III. Clinical Applications in AIDS

              Garlic has a long history of medical applications.   In Chinese medicine, it is described as to have an acrid taste and a “warm” property. Traditionally, it is used as a Qi (vital energy) stimulant. It has stomach-warming, digestant, anti-inflammatory, detoxicant, and antihelminthic effects. It is used for indigestion, edema, diarrhea, dysentery, whooping cough, carbuncle, furuncle, tinea capitis, snake bites, and insect stings.

              For more than 20 years Chinese hospitals have produced a highly purified form of Allicin which has been administered as an intravenous infusion for bacillary dysentery, amebic dysentery, deep fungal infections, whooping cough, endobronchial tuberculosis, oxyuriasis and trichomonas vaginitis. For most conditions, the cure rate is 80 percent or better. I have used it extensively in my practice. It is potent enough to treat many common infections in non-immune-deficient patients and also for many different kinds of OIs in AIDS patients. The following is a brief summary of the clinical applications of allicin.

              1) Allicin as a MOPPS. For every patient whose CD4 count < 200, or whose CD4 percentage < 20% of lymph cells, I use allicin as the primary prophylaxis. I have designed two forms of aerosolized allicin treatments for the protection of the respiratory tract. With equipment similar to that employed for pentamidine inhalation, the patient inhales a nebulized allicin solution for 20 to 30 minutes to saturate the respiratory tract. As an alternative, an aerosol spray is carried by the patient and used as prescribed. Both forms use a concentration of 500 mcg allicin/ml. Most germs can be inhibited with a concentration of only 1 – 25 mcg/ml. This method can prevent and treat airborne infections.

              To prevent infections from food and other oral sources, an allicin vial containing 30 mg allicin/2ml solution is provided. This solution must be diluted to 8 to 10 oz with water. The diluted solution is used as a gargle and then swallowed or given as retention enema. For most patients, without acute infections, this treatment can be done twice a week. When there is an acute infection, this treatment can be done twice a day.  Recently, I helped a Chinese company developed a new, enterically coated, time release capsule of allicin. Each capsule contains 25mg of allicin. This form avoids the stimulation of gastric peristalsis and keeps the blood level of allicin more stable. Using this capsule, a patient can take much bigger dose and hence achieve better therapeutic and preventive effects.

              The majority of OIs are associated with two pathways. If we protect the respiratory and digestive tracts most infections can be prevented. From my personal observations, all patients who complied with these treatments, rarely complained of any dangerous new infections, such as Pneumocystis carinii pneumonia (PCP).    In a few patients whose CD4 cell count was less than 10, serious OIs were avoided for years as long as they adhered to these treatments on a regular basis.             

2) I have used allicin aerosol and nebulization inhalation to treat respiratory tract infections such as sinusitis, laryngitis, sore throat, bronchitis and residual symptoms of pneumonia. This inhalation treatment plus Chinese herbal formulas, such as Blue Dragon Combination, can very effectively treat most respiratory tract infections. One of QCZ’s HIV patients, who had suffered common bacterial pneumonia with high temperature, used high dose of allicin capsules (180 mg/day) plus three to four nebulized inhalations a day and thus was able to avoid hospitalization.

              3)  I have used allicin for treating cryptosporidiosis and microsporidiosis. They are very common in patients with CD4 cells count lower than 100. Five cases have been successfully treated with allicin. After these initial successes, a research proposal was submitted to the Office of Alternative Medicine of National Institute of Health (NIH). Although it received a very courteous evaluation, no funding was offered. Only after the AIDS Research Alliance of Los Angeles found this treatment has potential, this clinical trial was funded and conducted.   They published their phase I pilot trial in Searchlight of Spring issue of 1996. The primary result was very encouraging and found that allicin can clear cryptosporidium in patients with less than 50 CD4 cells.

              I have used allicin as a protozoa killer and adds some Chinese herbal formulas to stop the diarrhea and re-establish the digestive function and acupuncture on the acu-points: ST-36, ST-25, CV-12, SI-3, SP-6.  The combined treatment has proved more effective than use of allicin alone. A typical patient, Mr. B. with a CD4 count of zero for two years, and Kaposi’s Sarcoma, cryptosporidiosis and microsporidiosis had severe diarrhea. Using the combined treatment, his cryptosporidiosis and microsporidiosis cleared up within two weeks. Following clinical recovery, six stool tests and two colonoscopies found that these two protozoa had been cleared. Recently a larger dose oral of allicin, 180 mg per day was used for another case of cryptosporidiosis. Mr. G. has 30 CD4 cells, with cryptosporidiosis and severe diarrhea. He took 180mg allicin capsule per day and his protozoa were cleared within two weeks, diarrhea stopped and his CD4 count improved to 140.

              4) Allicin has been successfully used for treating an AIDS patient with crypotococcus neoformans meningitis. At the Berlin International AIDS Conference in 1993, Dr. Joan Presterley of Alaska reported one patient who failed to respond to all Western anti-fungal treatments. The patient had been comatose for four days. Following administration of allicin, the patient regained consciousness and recovered from the meningitis. Reported in China more than 10 years previously, this application has been successful in many cases. One of my patients, Mr. N., once had a serum titer of cryptococcus very high, with explosive vomiting and stiff neck. Taking allicin 120 mg per day for two weeks, his symptoms disappeared and the titer nomalized.

              5) Candida albicans infections respond to allicin. It is very effective for oral thrush and candidal esophagitis. For female patients who have frequent vaginal candida infection, using the same concentration of the aerosol solution to wet a tampon and insert into the vagina overnight for a few days will clear the candidiasis.

              6) Allicin can be used to treat mycobacterial infections. Tuberculosis and Mycobacterium avium-intracellulare (MAI) are common infections in advanced AIDS patients. Long-term use of conventional anti-TB and anti-MAI treatments is intolerable for these very weak patients. Allicin has been successfully used in China to treat bronchial TB. Allicin is a very good alternative, especially for drug-resistant TB and MAI.

              7) In my practice, I often see patients with long-term low-grade fever (around 100 degrees F). Many have no definite diagnosis, despite extensive laboratory tests. For these patients, I use an intensive regimen of allicin (nebulization inhalation and oral dose) and herbal formula, which usually normalizes their fever and prevents relapse.

              Allicin is really a wonderful herbal remedy. It is not only very effective in treating many OIs of AIDS, but it has no side effects apart from its somewhat unpleasant odor. Due to the purity of the allicin, however, the odor is short-lived. Moreover, allicin benefits the cardiovascular system and enhances immunity. A recently published study conducted by Chinese researchers concluded that allicin is a very strong anti-oxidant.

(This article was written before 1997. Recently it was edited by Dr. Max Haid, MD, Lic. Ac.

The Article showed that Allicin has wide spectrum of anti-infection effects.)

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