(Excerpts from Original Internist, Dec.1 2008)
An enormous advantage that lipid antimicrobials have, as compared to drug antibiotics, is they do not readily form resistant organisms. For example, Bergsson demonstrated that S. aureus is killed by fatty acids, and especially by monocaprin,through disintegration of the cell membrane, leaving the cell wall intact.
Antibiotic Resistant Organisms
When first discovered, antibiotics like penicillin were hailed as medical miracles against infectious disease. The first bacterium to be successfully inactivated by penicillin was Staphylococcus aureus (SA). This bacterium, often a harmless passenger in the human body, can cause illness, such as pneumonia or toxic shock syndrome, when it overgrows or produces a toxin.
Shortly after the mass-producing of penicillin, microbes began appearing that could resist it. Alexander Fleming had commented that penicillin given in small doses could produce resistant organisms. This warning was not heeded since increasingly effective antibiotics were being discovered at a rapid pace. Overuse of antibiotics results in bacterial resistance not only to the antibiotic prescribed, but also often to other antibiotics.
Penicillin-resistant pneumonia was first detected in 1967, then penicillin-resistant gonorrhea. By 1993, Escherichia coli was resistant. Tuberculosis is now commonly resistant to many available common treatments. Other pathogens showing resistance to many different antibiotics include Pseudomonas Salmonella, Campylobacter, and Streptococci.
Methicillin was introduced in 1959 and was then the antibiotic of choice for penicillin-resistant organisms. Soon after its introduction however Methicillin-resistant Staphylococcus aureus (MRSA) were detected in 1961. Half of all Staphylococcus aureus infections in the US are resistant to penicillin, methicillin, tetracycline, and erythromycin. Today (MRSA) is a huge clinical problem.
Lipids Against Resistant Organisms
Obviously, a different approach to medical problems associated with infectious disease is desperately needed. The answer is to discover effective agents that create less resistant organisms, fewer complications and negative side effects than present conventional drug-based pharmaceuticals.
The disinfecting power of lipids has long been recognized. As part of a natural immune system, lipids would have advantages over artificial antibiotics. They arrive through the process of natural selection to provide protection against the most common potential pathogens. They do not readily give rise to resistant strains and do not become ineffective. (This has been supported by recent studies).
Since lipids are normal constituents of our body, it would also be expected that they would not be irritating, sensitizing, or toxic. The monoglyceride lipids have been shown to have antimicrobial affects against a wide spectrum of microorganisms.
Since these natural antimicrobials have been selected by evolutionary forces, it seems relatively unlikely that resistant bacterial strains would arise. This raises the possibility that these lipids could be used to treat skin infections – including those caused by antibiotic resistant organisms.
Staphylococcus, and Streptococcus did not exhibit any resistance to monolaurin. An ester of lauric acid, monolaurin (glycerol monolaurate) has been found to inhibit Staphylococcus aureus.
In vivo experiments with lauric acid esters indicate activity against nasal MRSA comparable to or greater than standard drug treatment with Mupirocin. The enormous advantage is that lipid antimicrobials, as compared to drug antibiotics, do not readily form resistant organisms.
S. aureus is killed by fatty acids, and especially by monocaprin, through disintegration of the cell membrane, leaving the cell wall intact. The ester form of monolaurin, inhibits synthesis of staphylococcal toxins by interfering with signal transduction.
The current way that antibiotics are used has limitations. A different approach to the problem includes natural non-toxic lipids. Of the lipids examined, pure monolaurin has properties that best fit a wide spectrum antimicrobial agent.
Monolaurin and Monocaprin are now known to affect microorganisms in several ways. Several mechanisms are involved may make it more difficult for the affected organisms to develop resistance. Biocides that have this mechanism for inactivation do not readily form resistant organisms.
A mechanism of antibacterial action of fatty acids and their derivatives while not clearly defined seems to involve disruption of the cell membrane permeability barrier and inhibition of amino acid uptake. It also involves a fatty acid interfering with viral assembly. In other words, viral constituents in the cell are made but these cannot form an ineffective particle.
The most active inhibitor was lauric acid (although acids with shorter or longer chain length also had effectiveness). Monolaurin is also effective in blocking or delaying the production of exotoxins by pathogenic gram-positive bacteria.
As a simple food supplement, (monolaurin) could be given before, or in conjunction with antibiotic therapy.
This would help reduce the number of bacteria becoming resistant to drugs as well as overcoming those bacteria like MRSA that are already resistant.
In view of all these positive effects, monolaurin should be more widely used for the prevention of health problems involving microorganisms either alone or in conjunction with classical antibiotic.