Recently, Trevor Steyn, having another unprovoked and unnecessary cheap commercial dig at parabens and mineral oil, announced that he utilises silver chloride and grapefruit seed extract to preserve his aqueous cream and abovementioned product ranges (Pharmaceutical & Cosmetic Review, March 2006). Sounds good? But is it? I have in my research and development work at Gaia Research personally pioneered internationally the use of colloidal and ionic silver as personal care preservatives. It is a fact that silver chloride is insoluble and therefore almost entirely inactive as a microbicide, so application in such ‘crude’ ‘organic’ ‘natural’ products could not possibly be effective. Interestingly, the only means by which silver chloride can be rendered soluble and hence effective is by the introduction of potentially toxic ammonia. I know this better than anyone else, having put forward the “Ammonia Hypothesis” to explain how silver chloride might be microbicidal inside the chloride-rich human gut and body (Click Here for my undisputed thesis on the subject).

This would require the addition of ammonia to the product, or alternatively the decomposition of the product itself to produce ammonia, since ammonia is the only effective solvent for otherwise insoluble silver chloride. Ammonia can be a perfectly ‘natural’, but potentially toxic product arising from the decomposition of nitrogen-rich organic compounds in vegetable matter (Seekins B, Biocycle, 40(11), 1999) or a product of ‘industrial synthesis’. The former is what I have predicted occurs in products bulked predominantly with superfluous plant material of inevitable decomposition potential coupled with inadequate preservation to safely handle challenges that even parabens might fail to meet. See my ‘Mineral vs. Plant Oil’ report for an exposé of this breakdown process.

Grapefruit seed extract (GSE) The only means by which the GSE could be even weakly effective long term over the life of a natural product, would be for it to be preserved with parabens or some other preservative to prevent any ‘natural?’ preservative itself from decomposing and becoming ineffective. Clearly this would be a telling double-standard sham, making a total mockery of claimed ‘organic’ and ‘natural’ standards for such product ranges, but without my exposé, how would any one know this, let alone be appraised of the risks? The name implies that GSE is produced by a simple extraction of grapefruit seeds, but it is actually a multi-step synthesised product merely using waste grapefruit seed and pulp as main raw material. Claims for the efficacy of GSE as an alternative to conventional preservatives are legion via books, magazines and the Internet, so much so that questions arose in the scientific community about its composition and whether commercial GSE might be adulterated with synthetic preservatives. So how does GSE stand up to scrutiny?

Using sophisticated analytical methods to compare commercial grapefruit seed extracts (GSE) from different manufacturers with laboratory grapefruit seed extract, one research group identified the synthetic preservative agents methyl paraben and triclosan (Sakamoto S et al, Bull Natl Inst Health Sci, 114, 38-42, 1996). Another group, using newer analytical methods, also with commercial GSE, additionally identified another synthetic preservative benzethonium chloride. Levels of cheat ingredients were significant, as high as 10% (22% by weight) of benzethonium chloride. Only one sample had no adulteration, but this and the laboratory extracts also had no significant antimicrobial activity. (von Woedtke T et al, Pharmazie, 54, 452-456, 1999) Using even more modern sophisticated analytical methods, yet another group, setting out to determine whether perhaps benzethonium chloride or a similar molecular weight quaternary ammonium compound was formed during the extraction of active components of grapefruit seeds, demonstrated conclusively that synthetic benzethonium chloride, an antimicrobial agent used in disinfection products, was being either added to or deliberately artificially synthesised from Grapefruit Seed Extract (Takeoka G et al, J Agric Food Chem, 49(7), 2001). These practices are ongoing despite exposé, troubling given the widespread use and belief in GSE as natural and safe, when there are in fact toxicity and allergenicity concerns (Takeoka G et al, J Agric Food Chem, 53(19), 2005); (Takeoka G et al, Meeting Abstr, Afgd Paper No. 50, ACS Nat'l Meeting, Mar 2005, San Diego, CA.).

All peer reviewed scientific studies apparently showing efficacy for GSE have likely been as a result of tests using adulterated material, these proprietary products having been accepted at face value, so all tests prior to and several post exposé are scientifically invalid and worthless, irrespective of their number (Reagor L et al, J Altern Compl Med, 8(3), 2002); (Heggers J et al, J Altern Compl Med, 8(4), 2002); (Edwards-Jones V, Burns, 30(8), 2004); (Zayachkivska O, J Physiol Pharmacol, 56(Suppl 1), 2005). Some researchers have found non-proprietary extracts to be ineffective (Calori-Domingues M, Foseca H, Food Addit Contam, 12, 347-350, 1995) and the few reporting positive results, were feeble activity (Cvetnic Z, Vladimir-Knezevic S, Acta Pharm, 54(3), 2004) or poorly controlled equivalency studies (Oyelami O, J Altern Compl Med, 11(2), 2005)

The majority, if not all the activity is attributable to the preservatives with which GSE is adulterated, including, but not limited to the abovementioned. To the degree to which adulterants (Parabens, Triclosan and/or Benzethonium chloride) are absent, so are higher concentrations of GSE needed to elicit effects due to feeble action and this too is not without some increased risk due to toxic natural constituents of the seed (and possibly other ingredients) itself. Where the benzethonium chloride has not been deliberately added, it is deliberately artificially synthesised from several natural phenolics present in the seed into synthetic quaternary ammonium compounds during ‘manufacture’ of the GSE to afford it more significant activity or retain any feeble activity that it, like most fruit seeds/skins barely sufficiently posses for self-preservation. Chemical manufacturers, typically in this type of synthesis, use chemical catalysts. Synthetic ammonium chloride is the catalyst used to synthesise what in the final analysis is the synthetic chemical, benzethonium chloride. GSE is a synthetic chemical compound, is not ‘organic’ or ‘natural’ and should not be permitted in such products.

There is another issue with grapefruit seed extract (GSE); its high endocrine disrupting potential, since several of the compounds that manufacturers point out are in GSE, in particular the flavones, are known to have estrogenic activity (Barrett J. Phytoestrogens, friends or foes? - Environmental Health Perspectives 104(5), 1996). GSE has never been evaluated for its estrogenic activity. This topic has been dealt with extensively in the previous data on the high relative safety of parabens, which risk again pales into insignificance against this barrage of endocrine disruptors of uncalculated risk, revealing all GSE preserved products as possible tragic excuses for what are held to be exceptionally safe and efficacious ‘organic natural personal care products’.

Benzethonium chloride, as detected in so-called Grapefruit seed extract (GSE), is a quaternary ammonium cationic disinfectant, a Class 2 poison because of its teratogenicity (induction of congenital defects). Cationic detergents are more toxic than other detergents due to their caustic and systemic toxic effects. Contamination of the eye may lead to corneal lesions. Oral solutions can lead to depression of the central nervous system, seizures, coma and death. (Budavari S (Ed), The Merck Index, Merck & Co, NJ, 1989); (Swiss Toxicological Information Centre, News, STIC, Univ Zurich, 7-11-2005) Topical contact can cause irritation and injury to the eyes and skin and long-term - dermatitis (Grant W, Toxicology of the Eye, Charles C. Thomas Publisher, 1986); (International Chemical Safety Cards, Benzethonium chloride, ICSC: 0387, NIOSH, March 27, 1996), and also vaginal irritation (Goodman L & A Gilman (Eds), Pharmacological Basis of Therapeutics, Macmillan, NY, 1975).

Dermal exposure to short and long-term, low to high levels of benzethonium chloride in several rodent studies caused epithelial and sebaceous gland hyperplasia at the site of application (National Toxicology Program, Abstract for TR-438 - Benzethonium Chloride, July 1995). Benzethonium chloride is an endocrine disruptor (Endocrine Toxicants, Scorecard, Registry of Toxic Effects of Chemical Substances, August, 1997). Health concerns include toxicity, safety limits on use, purity and manufacturing, and also estrogenic / endocrine disruptor effects, raising concern for impaired fertility or development and increased risks for certain cancers (Ingredient Report: Benzethonium Chloride, Environmental Working Group, 2006).

Triclosan (as detected in a considerable variety and proportion of adulterated GSE) has been reported recently to be photochemically converted to toxic dichlorodibenzo-p-dioxin (DCDD) within mere minutes in the environment (Lores M et al, Anal Bioanal Chem, 381(6), 2005); (Latch D et al, Environ Toxicol Chem, 24(3), 2005); (Sanchez-Prado L et al, Anal Bioanal Chem, 384(7-8), 2006); (Yu J et al, Chemosphere, Mar 27, 2006 – E-pub ahead of print), so it may not be detectable until applied to the skin, where the hidden damage proceeds unseen, though contact dermatitis and photoallergies may present when the skin is exposed to sunlight (Durbize E et al Contact Dermatitis 48(3), 2003); (Hazmap, Triclosan, Natl Inst Health, USA, 20 July, 2004) Triclosan is genotoxic and may irreversibly alter DNA strands (Ciniglia C et al, J Hazard Mater, 122(3), 2005). Triclosan also reacts with free chlorine in tap water to produce intermediate compounds that convert into dioxins upon exposure to UV-radiation (from the sun or other sources). Dioxins are extremely toxic and are very potent endocrine disruptors. They are chemically very stable, are eliminated very slowly and can bioaccumulate to dangerous levels and persist for a very long time. (Wikipedia, Triclosan, 30 April 2006)