Truth About Grapefruit Seed Extract

Since my original post on Grapefruit Seed Extract, I've stumbled upon some new eye-opening information, so I thought I'd expand the subject here.

The big controversy that's been going on for years with Grapefruit Seed Extract lies in its potential to be contaminated with benzalkonium chloride, parabens, and triclosan.  Numerous studies have tested samples of commercially produced GSE and found these contaminants to be present.  (See here, here, here and here.)  The biggest contaminant found is benzalkonium chloride, a chemical that rates a 7 in the cosmetics database that's a known immune system toxin, skin toxin, and possible cancer risk.

Some studies have shown that without these contaminants, a truly natural extract of grapefruit seed and pulp in ethanol or glycerin, had no antibacterial properties.  However, GSE apologists claim that GSE can be effective without these contaminants.  So, what is the truth? Is there such thing as a "pure" GSE, and if so, is it effective?

Grapefruit Seed Extract was first developed in 1972 by a man by the name of Dr. Jacob Harich.  Today, there is one main manufacturer of GSE that defenders claim is pure.  It is sold under the name Citricidal. This website describes how it is made:

   1. Grapefruit pulp and seed is dried and ground into a fine powder.
   2. The powder is dissolved in purified water and distilled to remove the fiber and pectin.
   3. The distilled slurry is spray dried at low temperatures forming a concentrated flavonoid powder.
   4. This concentrated powder is dissolved in vegetable glycerine and heated.
   5. Food grade ammonium chloride and ascorbic acid are added, and this mixture is heated under pressure. The amount of ammonium chloride remaining in finished Citricidal is 15-19%; the amount of ascorbic acid remaining is 2.5-3.0%.
   6. The ammoniated mixture undergoes catalytic conversion using natural catalysts, including hydrochloric acid and natural enzymes. There is no residue of hydrochloric acid after the reaction.
   7. The slurry is cooled, filtered, and treated with ultraviolet light.

As you can see, this isn't a truly natural process, it being treated with hydrochloric acid and ammonium chloride.  After all the chemical reactions occur, the final composition of the extract is made up of about 60% diphenol hydroxybenzene, a chemical classified as a quaternary ammonium chloride--the same as benzethonium chloride.  In fact, it is nearly chemically identical to benzethonium chloride. This is one possible reason that lab tests have shown GSE to be "contaminated" with benzethonium chloride--the equipment possibly misread the diphenol hydroxybenzene.

Typically, when a truly natural extract is made, plant matter is let to steep in a solvent such as water (as in making tea), in alcohol (like the vanilla extract you'd use in baking), or in glycerin (like with many herbal supplements you'd find at the health food stores) to extract the plant's beneficial or desirable compounds, whether it be a flavor, smell, or antioxidant.  It's a one or two step process that doesn't involve other chemical processing.  GSE is clearly not a natural extract, but a synthetic ingredient, considering it goes through 7 steps of processing and the extract doesn't retain the original compounds present in grapefruit.

Mountain Rose Herbs, one of the most respected and trusted suppliers of organic herbs, extracts, and essential oils lists the composition of the pure GSE they sell (which is most likely Citricidal brand):

Ascorbic Acid- 3%

Glycerol- 36%

Diphenol Hydroxybenzene (Quaternary compound from Grapefruit Bioflavinoid)- 58.5%

Heavy Metals- None detected

Benzethonium Chloride- None Detected

Methyl Hydroxybenzoate - None Detected

Propyl Hydroxybenzoate - None Detected

Triclosan- None Detected

So, while it is pure from other contaminants, it is primarily diphenol hydroxybenzene.  One fallacy I've found on discussion boards online have been that since it comes from Mountain Rose Herbs, it must be safe and organic.  You'll notice that this ingredient is not classified as certified organic on their website.

When I first posted my Chemical of the Day on GSE, there were some comments written on the post.  I have to now revise my original replies with this new information in mind.

Sally Leachko founder Meaodwlake Farm wrote:

I applaud your efforts Stepahnie. However, you are only exposing your readers to a fraction of the information available about GSE and controversy that surrounds this ingredient. Is some GSE contaminated? It appears so. Is all? Absolutely not. Meadowlake Farm Honeybee Products uses organic GSE from one source and we've had it tested by an independent lab multiple times. Contrary to what you indicate it has some anti-microbial properties, that is why we use it as a part of our proprietary 100% natural preservation system.

I originally commended her efforts to make sure that her extract was pure.  However, even though her extract isn't contaminated with other chemicals, knowing that "pure" GSE is composed of mainly diphenyl hydroxybenzene, I am forced to rescind my comments.  And while I'm sure that her motives are good (their company seems to work a lot towards sustainability and organic causes), I think that the industry is rife with misinformation, even from suppliers of chemicals to companies.

Another reader of my original post wrote:

If the ingredient is listed as Extracts of Organic Grapefruit Seed (certified organic by Soil Association Certification Limited) in a product would it be okay?

I originally thought, sure, it's certified organic, it's fine.  However, now I have more information and have to change my reply.

Right now, Citricidal is actually made from organic grapefruit.  But, whether it's organic grapefruit or not, the extract is still going to contain diphenol hydroxybenzene.  But how did this company get a GSE that was certified organic, it being a synthetic chemical?  Well, notice that the certifying body isn't the USDA, by the Soil Association.  The Soil Association is the European organic standard, and the requirements are much less strict than that of the USDA.  They will allow and certify a synthetic chemical like GSE if it meets certain criteria for biodegradability, aquatic toxicity and bioaccumulation.  So, since the grapefruits were organically grown, and it meets the requirements, they approve the extract as organic, even though it's a synthetic chemical.  The Soil Association also approves phenoxyethanol as a preservative ingredient.  The USDA will not certify GSE, or allow it in a certified organic product.  If you see a USDA certified organic product with GSE, it is illegally labelled.  GSE is not on the USDA's list of approved non-organic substances (they allow a few non-organic ingredients like vitamin E in to their products).   

So, let's take a look at diphenol hydroxybenzone.  Why exactly do we want to avoid it?

The makers of GSE states that it's been extensively tested for toxicity and health effects and claim that it is safe.  However, all of these studies only tested the effects when it was taken internally.  When taken internally, chemicals have a chance to be metabolized and broken down by the body.  However, when applied topically, they can be absorbed in the skin and enter the bloodstream in their whole form.

The problem that I see with diphenol hydroxybenzene is the fact that on a molecular level, it's full of benzene rings.  The name "diphenol" means that there are two phenol groups.  Phenol is a benzene ring with one hydrogen and one oxygen molecule.  Chemicals with benzene rings are particularly worrisome in personal care products because once they enter the bloodstream they can mimic the hormone estrogen.  [For a detailed explanation of this, check out my article on Japanese Honeysuckle Extract.]  Estrogen is primarily made up of benzene rings, and our estrogen receptors are made to "fit" benzene rings.  So, when a chemical with a benzene ring enters the body, it has the potential to lock up in the estrogen receptor and can stimulate it. Estrogen mimickers also have the potential to raise levels of estrogen by inhibiting the function of an enzyme called SULT1E1, that helps to remove estrogen from the body. [For more on this, read my article here, scrolling down to "where my discussion begins."]

The strange thing with diphenol hydroxybenzene is that there are no chemical diagrams provided by the manufacturer (or anywhere, even in organic chemistry guides), and the name of the chemical doesn't help (as it should) in finding its chemical structure.  Hydroxybenzene is just another name for phenol, so the name means "2 phenol phenol," which is weird.  My guess is that it's a simplified name for the chemical.

The two hexagonal rings you see in the structure are the problematic benzene rings that I was talking about.  And indeed, this chemical has been shown to be an endocrine/reproductive disruptor by a 1995 RTEC study.  It also carries the risk of being a strong skin irritant, and it showed tumor formation at moderate doses.  (see the Cosmetics Database report) However, in its defense, according to National Toxicology Program studies, it exhibited no evidence of carcinogenity or endocrine disruption in a two-year rat and mouse study.  This study did, however, show that the animals treated with benzethonium chloride did have increased inflammation in the body and a slightly lower survival rate than the control group.

The bottom line is that while there is conflicting evidence of the other negative health effects of benzethonium chloride (and the diphenol hydroxybenzene present in GSE), at the very least it's a skin irritant that increases inflammation in the body.  My personal opinion on it is that it is safer than other preservatives. However, if you prescribe to an organic mindset and lifestyle, you will want to avoid Grapefruit Seed Extract, for it is nothing other than a synthetic chemical.

Note: Grapefruit essential oil is natural, and not the same thing as Grapefruit Seed Extract.

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