EPISODE THREE OF "THE CHELATION WARS." WHAT EXACTLY IS LIPOIC ACID?"
Updated: Apr 6
In past articles, I wrote about the YouTube interview of Chris Shade by Becky Davila. Number one is about the chronic illness epidemic in children and what might be causing it and the disagreement between Christopher Shade, PhD, owner of Quicksilver Scientific and my teacher, Andrew Hall Cutler, PhD about the cause and remedy for the situation. Number two is about some of the more inflammatory and irritating things Shade had to say about Andy… the fact that he called us a cult and said that the Cutler protocol is made up out of whole cloth….compared to his company, Quicksilver Scientific's products which are so marvelous, all natural and effective.
The most important difference in this controversy is whether alpha lipoic acid (ALA) is or is not a chelator. Is ALA just an agent that encourages the body to make glutathione, or is it (or its metabolites) an actual dithiol, fat and water-soluble chelator of mercury? A fat-soluble chelator can move metals in and out of body compartments. If ALA is just an agent that encourages the body to produce glutathione, you can take any form of it and as much of it as you want at any old time. If it is a chelator, it needs to be taken on a strict half-life schedule or else it will move mercury from some place harmless in the body to some place where great harm can occur….like the brain. This even more so if the person taking the ALA has amalgams in their mouth. In this case the ALA will allow the lipid barriers to “open” and the body’s natural tendency to seek equilibrium across the formerly impermeable membranes will force the metals INTO the cells rather than the way we want them to go, which is OUT.
The study Gregus Z, et al. 1992. Toxicology and Applied Pharmacology, 114,88-96 discusses how ALA works. Shade read this study and concluded that ALA is an NRF2 upregulator and any detoxing ability it has is because it makes the body produce more glutathione which leads the body to detox in a “natural” way.
Andy Cutler came to a very different conclusion from reading this study.
I spent a lot of time with it. It is really a good interesting paper. My reading of it was that it was conclusive proof of the chelating ability of ALA, and also was very useful in establishing the pharmacokinetics especially as excretion rates from the paper matched those in the Leskova study to the extent they can be compared by appropriate calculations.
So who is more qualified to evaluate this scientific study, Shade or Andy Cutler? This is what Andy said about his own qualifications as a chemist.
(There are) distinctions within the very general field of chemistry as to what specialized knowledge we have. Most people are aware that chemistry breaks down into organic chemistry, inorganic chemistry, etc. There are finer subdivisions and I happened to be the guy with exactly the right specialized knowledge who had to figure it out right for my own sake, and who could read (with great difficulty) Russian language papers, and who was very used to actually looking up and reading and interpreting journal papers for whether they were actually correct (which is almost never done in academic situations, I learned this as an industrial consultant).
Kinetics is not a common thing for chemists to know and the relevant part of kinetics here actually is considered chemical engineering - but a chemical engineer would never have known enough descriptive chemistry to figure the rest of the relevant material out.
Also, a lot of the biochemistry I know is, well, biochemistry, which is again a different field than chemistry and is not common for chemists to know even if they work in areas like Boyd Haley does. I knew it primarily out of personal interest from a fellow postdoc telling me about the Life Extension Foundation and its theories that taking vitamins properly can prolong lifespan.
My personal experience in universities was that people NEVER, EVER, EVER, EVER, EVER, EVER, UNDER ANY CIRCUMSTANCES, NO MATTER WHAT, learn material outside their field of specialization after they get their PhD. It is just not done. I was kind of a misfit for doing so. While there is a lot of babbling about interdisciplinary work it is almost never done because people won't even learn enough about other specialties to be able to talk to each other and define research projects. (I can vouch for that in chemistry). So, an academic chemist is not in a professional environment conducive to learning things like chemical engineering kinetics or inorganic descriptive chemistry (which includes how mercury binds to things and what kinds of complexes it forms).
So basically, a lot of luck winnowed all the people interested in mercury detox down to me. Hopefully some others with the relevant knowledge will show up. I think there are a lot of people in industry and a reasonable number in academia who also could figure it out pretty quickly or even already know it but they lack the personal experience of getting toxic to motivate them to ask the basic questions necessary to realize that the medical literature is, to put it politely, inaccurate on this issue.
Dr. Shade refers to himself as “the person who knows the most about mercury,” but he is an organic chemist with little to no background in chemical kinetics. He simply is not qualified to appraise the relevant papers to assess ALA as a chelator. Further, unlike Andy, he has a financial interest in promoting his products and keeping people buying them, so he has little motive to verify that Andy was right and a lot to discredit him.
Below is a discussion of Gregus Z, et al. 1992. Toxicology and Applied Pharmacology, 114,88-96. To understand this paper, it is important to know about the various forms of mercury and how they exert their harmful effects.
Vapor mercury (Hg0) is the form that can off-gas from amalgam fillings and evaporate in the oral cavity. The vapor can enter the lungs, get into the blood stream and also cross the cellular membranes (because it is fat soluble). Methylmercury (CH3Hg+ ( MM in the Gregus paper) is one form of organic mercury commonly found in fish. It is readily absorbed into the body from the intestines where it will go to the blood stream and circulation. Ethylmercury (C2H5 Hg) is the form of organic mercury that is found in the Thimerosal component of vaccines. When this is injected, it goes directly into blood circulation. Organic mercury is fat soluble and can cross cellular membrane so these forms all get into the brain readily.
All three of these forms will circulate in the blood and enter into cells, organs and the brain where the mercury will be attracted to sulfhydryl (SH) groups. Inside the cells the body slowly converts the vapor mercury and organic mercury to inorganic mercury (Hg++). Inorganic mercury is not fat soluble. Because of this, it will become stuck in the cells, organs and the brain and not be able to leave. While some natural processes may remove small quantities of inorganic mercury from organs over a very long time, whatever is in the brain basically remains there for life. That is why we need a fat-soluble chelator that is able to cross the blood/brain barrier to get into the brain to remove inorganic mercury. The Gregus study shows that alpha lipoic is such a fat-soluble chelator.
In the Gregus study, rats were injected with specific metals and alpha lipoic acid. Bile was collected for analysis every 30 min. At the end of the three hour experiments the rats were sacrificed and samples of blood and tissues were collected for analysis.
The experiments showed that alpha lipoic acid dramatically increased the excretion of Hg++ into bile. At the lowest lipoic acid dose there was a 12-fold increase of Hg++ excretion while at the largest dose, a 40-fold increase in Hg++ was found in bile. Shade theorizes that the observed increase of Hg++ in bile is the result of alpha lipoic acid activating Nrf2 (Nuclear factor erythroid-related factor 2) which would subsequently increase glutathione and it is the glutathione that is responsible for moving the mercury. But Gregus et al (1992), did a further series of experiments that treated rats with DEM (diethyl maleate). DEM depletes liver glutathione. The experiments showed that this pretreatment “did not influence significantly the biliary excretion of Hg++ during the first 2h after administration of mercuric chloride”. If Shade's theory was correct then we would expect the DEM treatment (depletion of glutathione) to decrease the biliary excretion of Hg++ BUT IT DOES NOT! This clearly shows that Shade’s theory is wrong.
Another important aspect of this study is illustrated in table 1. The control rats (mercury treated but not ALA treated) had 0.59 nmol Hg++ per gram in brain at the end of the experiment. The mercury/ALA treated rats had 1.72 nmol Hg++ per gram in the brain at the end of the experiment. As explained earlier Hg++ does not move across the BBB because it is not fat soluble. In that case, how could the ALA treatment increase Hg++ by almost three-fold in the brain? The only way that the Hg++ could move into the rats’ brains was if the ALA somehow “helped” or “chelated” the mercury and moved it in. Shade’s theory that glutathione is responsible for moving the mercury is contradicted by his own statement (at 54:48 in the interview) “There’s (sic) no transporters for glutathione to go into the system”.
In the body, substances tend to move from areas of higher concentration to areas of lower concentration. In the case of Gregus’ rats, when they were injected with mercury chloride (Hg++) the blood contained a higher concentration of mercury than the brain. The treatment with ALA allowed the inorganic mercury to cross the otherwise impermeable membrane of the blood/brain barrier and move into the brain. The direction (into the brain) followed a concentration gradient from higher to lower concentration. It is for this reason that Andy Cutler has always advised not to take ALA when there is ANY mercury amalgam in the mouth and also to avoid ALA in the first three months after the final removal of amalgam fillings. When the final amalgam is removed the daily off-gassing from the amalgams will stop trickling into the blood and with time the concentration of mercury in blood will drop. Once the concentration in blood is lower than that of the brain (3 months after final removal) then it is safe to take ALA on a proper chelation schedule to start the removal of mercury from the brain.
If patients take ALA when they still have amalgam fillings in their mouths the ALA will draw from the huge reservoir of mercury of the fillings and transport it INTO the brain and organs because the concentration gradient favors that direction. If they wait to take ALA until 3 months after final amalgam removal, the mercury concentration of blood will be lower than that in the brain and the concentration gradient will favor removal from the brain.
Chris Shade has misinterpreted the Gregus study. He has a financial incentive to control the narrative and promote the sales of Quicksilver’s expensive products. He also knows that most people (doctors and dentists included) won’t have time to review papers. If they do, without the appropriate background they might have difficulty understanding and interpreting the studies. Perhaps Shade doesn’t even understand these studies himself. But this underscores the importance of taking responsibility for your own health and not giving that responsibility away to someone who is more interested in financial gain than the well-being of mercury poisoned patients.
Another study that Andy Cutler used when he was developing his chelation protocol is Leskova GE. [Protective effect of lipoic acid amide in experimental mercurialism]. Gig Tr Prof Zabol 1979 Jun;(6):27-30. Most people are not aware of this paper because it is written in Russian. In the Leskova study rats were treated with mercury vapor. Half of these rats were treated with lipoic acid (technically they used lipoic acid amide). The experiments went on for 5 months. The lipoic acid treated rats excreted 59.6% more mercury in urine and feces as compared to the control rats with no treatment. The mercury concentration in the kidneys of the control rats was 1.5 X higher than the lipoic acid treated rats at the end of the experiment. The mercury concentration in the liver of the control rats was more than 2 X higher than the treated rats. The investigators concluded that: “The protective action of lipoic acid amide is based, on the one hand, on binding to mercury and excreting it from the organism and, on the other hand, on the protection of carbothiolic groups of some biologically active compounds.” (Emphasis added)
Shade makes an argument that ALA does not have the right shape to act as a mercury chelator. (At 45:10 in the interview Shade says “Now mercury has a geometry to its binding that is 180 degrees. It has to have a binder come in here and come in there. And to do that on a single molecule you need very long arms on that molecule to wrap around and get that 180 degree binding.” Let’s just ignore the fact that Shade is eliminating his own favorite molecule, glutathione, as a chelator in this argument. Bjørklund et al (G. Bjørklund, J. Aaseth, G. Crisponi, et al., Insights on alpha lipoic and dihydrolipoic acids as promising scavengers of oxidative stress and possible chelators in mercury toxicology, Journal of Inorganic Biochemistry, Volume 195, June 2019, Pages 111-119 ) proposed “a possible chemical structure of the complex between DHLA and Hg2+, based on the considerations in the International System”. It is not complicated and rebuts Shade’s “wrong shape” argument. (see below)
A a number of Quicksilver products contain R-LA. These products have no warning that they should not be taken with amalgam fillings in or with recent exposures to mercury. Taking R-LA with amalgam fillings will do the same thing as taking ALA, move mercury from the fillings and send it to the brain and organs. We feel obliged to explain this to people to keep them from harm.
Furthermore, Andy said to never use R-LA, even on a proper chelation schedule. All of the people who got better with ACC used ordinary RS lipoic acid and people who did attempt chelation with the R-LA reported worsening. Here is a quote from Andy Cutler:
Almost all studies are done with RS (regular, plain old) lipoic acid.Thus it is more proper to say that R-lipoic acid hasn't been proven to do any of the things that lipoic acid has been proven to do, than vice versa. All relevant literature and human experience with chelation has used regular RS-lipoic acid, not R-lipoic acid. Since they are in fact different, using R-lipoic acid is turning yourself into an original medical experiment, with the expected high probability of a negative outcome.
Approximately 3 months after all amalgam has been removed it is safe to take ALA (not R-LA). To be used safely, it must be taken at intervals of every 3h or less around the clock for several days on chelation cycles. This will get the net movement of mercury going OUT of the brain and body. If amalgam free patients take Quicksilver R-LA products in single doses (as prescribed on the labels) the LA metabolites will move some mercury INTO the brain and organs with every dose. In the long term this will concentrate mercury in these sensitive locations leading to regression. In our support groups we get hundreds of reports from people who took LA infrequently and regressed substantially over time. Some of these same people then used ALA on a proper schedule and were able to reverse their symptoms.
At this link you can read testimonials from people who injured themselves with improper chelation. Pay special attention to the stories about using lipoic acid on different schedules. For copyright reasons I can’t quote the stories directly so you will need to go to the webpage.
Here are two more examples of people's actual experience. We get this sort of report all the time in our support groups.
I accidentally took liposomal vitamin C without realizing it had R-ALA because it wasn’t listed in the ingredients, just part of a list on a flap of the box. It made me feel like garbage, horribly depressed, tired, yucky
I just finished round 73, am still in the dump phase. I chelated improperly (before finding this group, by taking R-ALA daily) for almost a year and saw my cognition decline. That damage is now reversed, plus there are other concrete gains.
We are constantly told that that it is not scientific to rely on anecdotal evidence. But observation is the first step in the scientific method. When you start seeing hundreds of people saying the same thing it becomes profound observation.
This is a long and technical article, but the subject of it is terribly important. Andy once mentioned to me that the misuse of lipoic acid was “the alternative medicine community’s contribution to the mercury holocaust.” Alpha lipoic acid is a powerful, fat soluble chelator for mercury, arsenic and cadmium should be taken on its half-life or not at all.
Everybody in humanity has some mercury in their body. Taking ALA improperly will move some of that mercury into the brain and other sensitive organs rather than out into the toilet. We can blame the medical establishment for filling us up with mercury, but we can blame the alternative medical community for compounding the situation by prescribing ALA improperly. It is sold everywhere, even in supermarkets, in huge doses per capsule. Doctors and naturopaths that I have talked to about this have never even heard of the concern and go on prescribing it in huge doses for diabetic neuropathy. I hope many people will read this article and take the warning about the misuse of alpha lipoic acid to heart.