Understanding Sulforaphane

Sulforaphane and the G.E.M.M Protocol

Sulforaphane plays a key role in restoring the normal balance of the gut and its microbiota. Its many functions are the key to correcting many intestinal issues as well as food intolerances. As part of the G.E.M.M. Protocol, sulforaphane helps to correct a range of conditions in more distant organs of the body. Visit the Learning Centre to learn more about Gut Ecology and Metabolic Modulation (the G.E.M.M. Protocol.)

As the demand for this ingredient has grown, so too has the number of broccoli sprout products in the market. So unregulated is the entry of such products into the market that it is difficult if not impossible for a consumer, or even a clinician, to determine the worth of such products. The science which underpins sulforaphane’s benefits in humans is generally more complex than for many of the nutraceutical ingredients which have gone before it.

Consequently, unwary consumers can be buying products which have little if any beneficial effect on health because the manufacturer does not understand the chemistry and is not skilled in manufacturing a finished product which retains the sulforaphane activity needed for enhancing the function in human cells.

The Science of Sulforaphane

For decades, the superior benefits of broccoli and other cruciferous vegetables have been acknowledged for their ability to prevent chronic disease – but until the early 1990s, no-one really knew why. The story began to unfold when researchers at Johns Hopkins University discovered that broccoli sprouts were a highly-concentrated source of sulforaphane, the molecule that potently activates the enzymes found to be integral to cancer prevention. In particular, they found that the cancer-preventive effects were due to the increase in Phase 2 detoxification enzymes in liver cells.

The Glutathione-S-transferase family and Quinone reductase enzymes among others increased very significantly in the presence of sulforaphane. Since then, more than 2000 peer-reviewed studies on sulforaphane have been published, a significant number of these being clinical trials with positive outcomes.

Unravelling the Sulforaphane Mechanisms

Cell and tissue damage accelerate rapidly in an oxidative environment but the opposite is the case when an antioxidative redox status predominates. This fact has contributed to the common practice of prescribing high doses of antioxidant supplements, even though cells make their own antioxidant enzymes when required.
Cell-Logic, Understanding sulforaphane

For sulforaphane to have disease-preventive effects, one might assume that it would be classified as an ‘antioxidant’. Perhaps counter-intuitively, sulforaphane was shown to be a weak pro-oxidant. What has emerged in recent decades is that prevention of any disease is best achieved when weak pro-oxidant signals act as stressors to ‘tell’ the cell when it needs to activate its endogenous defences.

Food molecules like sulforaphane are exactly that – weak pro-oxidant stressors that send nutrigenomic signals to activate the cell’s own defences. By contrast, direct-acting antioxidants can mask those essential pro-oxidant signals, countering Nature’s key inbuilt defensive mechanisms. For this reason, prescribing higher than dietary levels of antioxidant vitamins, A, C, E, beta-carotene and NAC should be avoided when prescribing sulforaphane and/or GliSODin®.

Instead of supplying direct-acting supplemental antioxidants at regular intervals, Nature’s mechanisms exert a modulating effect on redox status, increasing or decreasing the synthesis of antioxidant enzymes as the cell requires.

Sulforaphane is the most potent activator of Nrf2, the Master Transcription Factor which governs the core cellular defence processes by enhancing the expression of over 200 cytoprotective genes.

The cellular defences are largely governed by the cellular ‘switch’ Nrf2. When activated by weak pro-oxidant signals, Nrf2 simultaneously upregulates the several hundred cytoprotective genes. These genes include those coding for the antioxidant and Phase 2 detoxification enzymes, glutathione synthesis, the Vitamin D receptors, metallothionein (Nature’s heavy metal chelator) and many more.

Sulforaphane is acknowledged as the most potent of the naturally-occurring Nrf2 activators. With high bioavailability of around 80%, it allows the clinician to provide a concentrated and efficacious dose by prescribing just a few capsules daily. These doses readily match the doses used in the sulforaphane clinical trials.

Modulated activity of Nrf2 is essential for human cells to function at their peak. Another transcription factor, NF-kB plays key roles in maintaining cellular homeostasis. Whilst NF-kB is essential in destroying infectious organisms, it must be carefully modulated by healthy cells to prevent uncontrolled inflammation.

Nrf2 and NF-kB operate together to modulate normal cell function, ‘switching on’ and ‘switching off’ inflammatory processes as required. This is an important principle encompassed by the G.E.M.M. Protocol. This approach utilises Nrf2 and NF-kB and also targets other mechanisms that simultaneously influence the control of infection, allergy, unnecessary inflammation and autoimmunity.

When EnduraCell® as either powder or capsules is ingested, moisture initiates the action of the myrosinase enzyme on the glucoraphanin precursor; sulforaphane is then rapidly produced in situ.

The very first cells with which sulforaphane comes in contact are the epithelial cells lining the gut. Rapid sulforaphane absorption into these cells activates Nrf2, thereby upregulating a host of cell-protective genes in the epithelia. It is this process which explains why sulforaphane is the foundation therapy for the G.E.M.M. Protocol and why it has such profound effects on gut function.

Sulforaphane is a key intervention for addressing a dysfunctional gut barrier, gut dysbiosis, H. pylori infection, IBS, food intolerances and related issues. Its actions are supported by Gemmune I.B. and other G.E.M.M formulations necessary to restore the ecology of the gut environment.

Selected Mechanisms by which Sulforaphane impacts the Gut-Immune Interface.

The G.E.M.M. course describes other cell-defensive mechanisms associated with sulforaphane. Several of these applicable to gut health are:

  1. Sulforaphane inhibits the binding of pro-inflammatory endotoxin (LPS) to TLR4 on epithelial membranes, especially the gut epithelium.
  2. Sulforaphane upregulates beta-defensins and other selective anti-microbial molecules which destroy pathogens without harming the commensal microbiota.
  3. Sulforaphane inhibits the enzyme, urease which Helicobacter pylori utilises to create the alkaline gastric environment it prefers.

The Power of Nutrigenomics

The most important documented attribute of sulforaphane is its ‘Nutrigenomic’ effect. This is the property whereby sulforaphane activates around 200 genes related to the way human cells defend themselves against the many daily assaults on their normal function. This is why sulforaphane can exhibit beneficial effects on so many seemingly – unrelated conditions. What’s more, unlike the polyphenolics such as those from green tea, grapes (including resveratrol), berries, turmeric (curcumin) and others, sulforaphane is highly – bioavailable, enabling it to readily enter the cells in significant amounts.

Cell-Logic, Power of nutrigenomics

What’s on the Labels?

A glance at the labels and Product Specification sheets which accompany many of these products reveals that the manufacturers and marketers have little knowledge of the subtleties of sulforaphane. Some products naively claim to contain sulforaphane; this is not possible as sulforaphane itself is unstable. The product should instead contain the two precursors, glucoraphanin and myrosinase which react when the product is consumed. Be very suspicious of any product claiming to contain sulforaphane.

Be wary of Broccoli ‘Extracts’

Be equally wary of products described as ‘extracts’ of either broccoli seed or sprouts. ‘Extracts’ must be produced in a way that completely destroys the activity of the myrosinase enzyme. As such, they are incapable of producing sulforaphane when consumed in a supplement or food. Many are labelled with a term contrived for marketing purposes, ‘sulforaphane glucosinolate’, presumably to imply that the product releases or contains sulforaphane. This is a misleading name for the correct chemical name ‘glucoraphanin’. Most importantly, ‘sulforaphane glucosinolate’ is not a scientific term and there is no need to create an ambiguous term to describe ‘glucoraphanin’. The majority of the available products (including those for clinicians) are of this type.

What to look for

For a product to be capable of producing sulforaphane when consumed, it must contain both glucoraphanin and the myrosinase enzyme. Because an extract has no myrosinase activity, the inert glucoraphanin it contains is unable to produce sulforaphane. However, when a consumer reads a label which states, for example, “30mg sulforaphane glucosinolate”, he or she is likely to assume that the product contains 30mg of sulforaphane. Two well – designed recent studies1, 2highlight the fact that such products have no inherent sulforaphane – releasing capacity and that consumers can be misled into believing that such products are delivering benefits that are not possible with such products. Most consumers of course, have no way of determining the accuracy or reliability of such information and so, not surprisingly the products with the clever marketing campaigns sell well, in spite of the quality (or otherwise) of the ingredient. In addition, these same clinical trials highlight the benefits of using a whole broccoli sprout powder in order to take advantage of its other bioactives compounds.

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